Pharmaceutical Formulation Technology Research Papers (original) (raw)

2025, Current Opinion in Pharmacology

Recent advances in HIV vaccine development include initiation of the first efficacy trials and substantial expansion of the preclinical pipeline. Several preclinical candidate vaccines have induced strong cellular immune responses and provided impressive protection against AIDS in non-human primate models; however, candidates that induce broadly neutralizing antibodies remain elusive.

2025, Drug Development and Industrial Pharmacy

The waste of inedible parts of pineapple, particularly in tropical countries, contributes to environmental burden. This study aimed to utilize pineapple stem waste as a source of starch-based pharmaceutical excipient. The starch was isolated from pineapple stem waste using a simple process without applying harsh chemicals. The isolated starch (PSS) was then physically modified through gelatinization and spray drying to improve its physical properties. Starch characteristics were identified by FTIR, TGA, and XRD analysis. The SEM imaging showed morphological change with reduced surface roughness due to physical modification of the starch. Decreased crystallinity of modified starch (MPS) was confirmed by our XRD results: the peaks of A-type crystalline at 2h of 13 , 15 , 18 , and 23 were present in PSS, yet mostly absent in MPS. Thermogravimetric analysis showed that MPS behaved differently from PSS and the degradation events occurred at lower temperature. When the starch was spray-dried without prior gelatinization process, the physicochemical characteristics of spray-dried starch resembled untreated starch. Moisture content in PSS (10.66%) decreased after gelatinization to 7.3%. Potential use of MPS was demonstrated by its powder flowability (Student's t test, p < 0.05), swelling capacity (Student's t test, p < 0.05), and compaction profile. In summary, our findings demonstrated that modified pineapple starch showed better physical characteristics and quite promising as a tablet binder and disintegrant.

2025, Advanced Pharmaceutical Bulletin

Purpose: This study was aimed to evaluate the site-specific drug delivery of 5-FU with chitosan (CS) as a carrier and quercetin (Qu) against induced colon cancer in Wistar rats. Methods: Cross-linked CS-Qu nanoparticles (NPs) were prepared by ionotropic gelation method. Physicochemical characterization of NPs was performed by Fourier-transform infrared (FTIR) spectroscopy, dynamic light scattering (DLS), in vitro drug release, and drug loading efficiency (LE). 1, 2-Dimethylhydrazine (DMH) and dextran sulfate sodium (DSS) were applied to induce adenocarcinoma tumors on inbred male Wistar rats’ colon. The treatment group of rats was administered through enema with NPs dispersion. Hematoxylin and eosin staining were performed to the histopathological examination of tumors. Results: Zeta potential and particle size for NPs were +53.5 ± 5 mV and 179 ± 28 nm, respectively. About 96% Qu LE was obtained with a maximum release of 5.63 ±1.59% and 4.62 ± 1.33% after 24 hours in PB solution wit...

2025

In spite of advances in diagnostic modalities, diagnosis of acute myocardial infarction is challenging. During the last decade B-type natriuretic peptide (BNP) has been recognized as a useful marker for the detection of acute and chronic left ventricular dysfunction. BNP is released by the ventricles as a hormonal response to increased wall stress, pressure and volume overload. It correlates very closely with heart failure, as well as clinical response to treatment and prognosis. This study was designed to examine the plasma levels of brain natriuretic peptide as well as CK-MB & troponin I as a diagnostic marker in acute myocardial infarction patients. This study was conducted on 90 consecutive patients who presented in the emergency department within 6 hrs of having acute chest pain and on 90 healthy age and sex matched volunteers who formed the control group. The plasma levels of brain natriuretic peptide using the quantitative immunofluorescence assay and CK-MB was estimated by I...

2025, Indonesian Journal of Pharmaceutical Education

SNEDDS are isotropic mixtures of oil, surfactant, and cosurfactant that produce spontaneous nanoemulsions once they make contact with gastric juices in order to increase the solubility of active pharmaceutical ingredients. One of the active pharmaceutical ingredients with low solubility is Astaxanthin. This research aims at formulating, characterizing, and evaluating SNEDDS containing Astaxanthin in the form of droplets. This research is a laboratory experiment. SNEDDS containing Astaxanthin droplets are made in 3 formulas using the ratio of surfactants and cosurfactants which are characterized to produce F1, F2, and F3 transmittance values of 91%, 90%, and 95%, respectively. Furthermore, the F1 particle size value of 183.75 nm obtains a PDI value of 0.272, the F2 particle sizevalue of 195.25 nm obtains a PDI value of 0.341, and the F3 particle size value of 105.75 nm obtains a PDI value of 0.392. This signifies that the absorption efficiency of F1, F2, and F3 are 94.62%, 94.35%, and 95.57%, respectively. The evaluation reveals the insignificant changes in the emulsion viscosities of SNEDDS containing Astaxanthin liquid drop after having received a stability test for 28 days using Paired T. Test data analysis (p<0.05). The research findings show that the F3 of 72% surfactant and 18% co-surfactant concentrations are the best formula in producing SNEDDS. It concludes thar the higher the surfactant concentration produced, the greater the ability to, oil droplets resulting in obtaining small partidles and high absorption efficiency.

2025, International Journal of Pharmaceutical Sciences and Medicine

Bilosomes are bilayer vesicles that transport lipids incorporating non-ionic surfactants and bile salts. The current review was based on the properties, materials used in the preparation, various methods of formulation, characterization parameters and various pharmaceutical and clinical applications. They are spherical, uni-lamellar, and 5-200 nm-sized and vesicles with many membranes. Under normal conditions, bile acids exist as ionised bile salts after being synthesised in the liver and stored in the gall bladder. They have a steroid nucleus that is both hydrophilic. Materials used in bilosomes comprise of lipids, non-ionic surfactants and bile salts. Bilosomes are prepared by various methods including Reverse phase evaporation, Thin Film Hydration and Hot Homogenization. Bilosomes are characterized in terms of particle size, polydispersity index (PDI), zeta potential, ultracentrifugation, entrapment efficiency, in-vitro drug release and stability. Bilosomes have wide range of app...

2025, Food Science and Applied Biotechnology

In the context of growing interest for functional foods and cosmetic products, emulsified products such as dressings or lotions have been proposed to deliver probiotics and plant extracts with interesting biological (e. g. anti-inflammatory) properties due to their daily consumption or application on skin, respectively. Besides these positive effects, emulsified products containing water are often prone to microbial growth justifying thus the addition of preservatives such as parabens in their formulation. Safety concerns regarding some synthetic preservatives have stimulated the development of natural antimicrobial ingredients (namely from plant or microbial origin) for the preservation of food or cosmetic products. Besides direct addition of antimicrobial biomolecules, the addition of living bioprotective bacteria such as probiotic lactic acid bacteria (LAB) is a promising approach. Franco-Bulgarian ESCAPE project ambition is to identify synergistic combinations of such probiotic ...

2025, Revista médica del Instituto Mexicano del Seguro Social

Introducción: la sepsis neonatal nosocomial es la principal causa de mortalidad y morbilidad en unidades de cuidados intensivos neonatales. El objetivo de esta investigación fue determinar factores de riesgo neonatales y ambientales... more

2025, International journal of pharmaceutics

A new shadowgraphic imaging method and an associated instrument for analyzing the physical stability of pharmaceutical suspensions are introduced in this paper. The new suspension tester consists mainly of a high-resolution camera that takes sequential shadowgraphic images of emulsions or suspensions and a 2D collimated LED for simultaneous whole-sample illumination in bright field. A built-in ultrasonic bath provides controlled initial agitation to the samples of interest. Sequential images acquired by the experimental setup were used to derive normalized transmission profiles from which an instability index was developed for quantitative stability comparison between samples. Instrument performance was verified by measuring the stability of a series of oil-in-water emulsions prepared with surfactant mixtures of different ratios. The new instrument correctly determined the required hydrophilic-lipophilic balance for sunflower oil to be 7.0. The stability of a pressurized suspension ...

2025, Vaccine

Regulatory potency test for rabies vaccines requires mice vaccination followed by challenge with a live virus via intracerebral route. An alternative in vitro test, consistent with the "3R's" (Reduce, Replace, Refine) was designed to quantify active glycoprotein G using seroneutralizing monoclonal antibodies. This versatile ELISA targets well conformed neutralizing epitopes. Therefore, it quantifies only the trimeric prefusion form of glycoprotein G known to elicits the production of viral neutralizing antibodies. The ELISA makes it possible to quantify the rabies antigen during all steps of the product cycle (i.e. viral cultivation, downstream process, formulation and product stability in the presence of aluminum gel or other vaccine valence). Moreover, the batch-to-batch consistency of our active ingredients and formulated products could be demonstrated.

2025, Phytotherapy Research

Natural products historically have been a rich source of lead molecules in drug discovery, based on their capability to create unique and diverse chemical structures. However, it is also true that the vast number of metabolites typically present in natural products and their huge dynamic range results in the loss of many possibly bioactive natural compounds, becoming an inextricable obstacle for drug development. Recently, new strategies which favour a holistic approach as opposed to the traditional reductionist methods used previously, have been introduced with the purpose of overcoming the bottlenecks in natural product research. This approach is based on the application of new technologies, including metabolomics, for example. Metabolomics allows a systematic study of a complex mixture such as a phytochemical preparation, which can be linked to observations obtained through biological testing systems without the need for isolating active principles. This may put drug discovery fr...

2025, Vaccine

Efficient antigen extraction from vaccines formulated on aluminum hydroxide gels is a critical step for the evaluation of the quality of vaccines following formulation. It has been shown in our laboratory that the efficiency of antigen extraction from vaccines formulated on Alhydrogel decreased significantly with increased storage time. To increase antigen extraction efficiency, the present study determined the effect of surfactants on antigen recovery from vaccine formulations. The Plasmodium falciparum apical membrane antigen 1 (AMA1) formulated on Alhydrogel and stored at 2-8°C for 3 years was used as a model in this study. The AMA1 on Alhydrogel was extracted in the presence or absence of 30 mM sodium dodecyl sulfate (SDS) or 20mM cetylpyridinium chloride in the extraction buffer (0.60 M citrate, 0.55 M phosphate, pH 8.5) using our standard antigen extraction protocols. Extracted AMA1 antigen was analyzed by 4-20% Tris-glycine SDS-PAGE followed by silver staining or western blot...

2025, Journal of Pharmaceutical and Biomedical Analysis

Water contents of superdisintegrant pharmaceutical excipients were determined by attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy using simple linear regression. Water contents of the investigated three common superdisintegrants (crospovidone, croscarmellose sodium, sodium starch glycolate) varied over a wide range (0-24%, w/w). In the case of crospovidone three different samples from two manufacturers were examined in order to study the effects of different grades on the calibration curves. Water content determinations were based on strong absorption of water between 3700 and 2800 cm -1 , other spectral changes associated with the different compaction of samples on the ATR crystal using the same pressure were followed by the infrared region between 1510 and 1050 cm -1 . The calibration curves were constructed using the ratio of absorbance intensities in the two investigated regions. Using appropriate baseline correction the linearity of the calibration curves was maintained over the entire investigated water content regions and the effect of particle size on the calibration was not significant in the case of crospovidones from the same manufacturer. The described method enables the water content determination of powdered hygroscopic materials containing homogeneously distributed water.

2025

No cenario atual, as bacterias resistentes sao uma preocupacao crescente para a Organizacao Mundial da Saude (OMS), devido a resistencia adquirida pelo uso indiscriminado de antibioticos. Novas alternativas farmacologicas como, por exemplo, as plantas medicinais, sao de grande interesse para a industria farmaceutica. O objetivo deste trabalho foi realizar um levantamento dos metodos de avaliacao da atividade antimicrobiana utilizados em bioextratos de aroeira e da propolis em publicacoes de revistas e jornais com fator de impacto no intervalo 1,295 a 4 e por consequencia classificacao no Qualis CAPES de B1 a A1 na area de avaliacao Medicina II (abrange a area de infectologia), Farmacia ou Ciencias Biologicas III (abrange a area de microbiologia) no periodo entre o ano 2000 a 2017. Como metodologia foi adotada um pesquisa de natureza qualitativa, com uma abordagem exploratoria atraves de uma revisao de literatura de metodos de extracao da Aroeira e do Propolis. Dos metodos utilizados...

2025

Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Mouth dissolving tablets constitute an innovative dosage forms that overcome the problems of swallowing and provides a quick onset of action. The purpose of this study was to formulate and evaluate mouth dissolving tablet of loratadine using a special preparation technology (pharmaburst Technology) with a super disintegrating agent (Croscarmellose sodium). Tablets were prepared by direct compression technique. The granules were evaluated for angle of repose, bulk density, tapped density, bulkiness, compressibility index and hausners ratio. The tablets were evaluated for hardness, thickness, uniformity of weight, friability, wetting time, water absorption ratio, disintegration time and drug content. In vitro release studies were performed using USP-II (paddle method) in 900ml of pH 1.2 at 50rpm. The physical properties of the prepared tablets did not show any significant variati...

2025, Applied Microbiology and Biotechnology

Forced by major drawbacks of egg-based influenza virus production, several studies focused on the establishment and optimization of cell-based production systems. Among numerous possible host cell lines from duck, monkey, canine, chicken, mouse, and human origin, only a few will meet regulatory requirements, accomplish industrial standards, and result in high virus titers. From primary virus isolation up to large-scale manufacturing of human vaccines, however, the most logical choice seems to be the use of human cell lines. For this reason, we evaluated the recently established CAP cell line derived from human amniocytes for its potential in influenza virus production in suspension culture in small scale shaker flask and stirred tank bioreactor experiments. Different human and animal influenza viruses could be adapted to produce hemagglutination (HA) titers of at least 2.0 log 10 HA units/100 μL without further process optimization. Adjusting trypsin activity as well as infection conditions (multiplicity of infection, infection medium) resulted in HA titers of up to 3.2 log 10 HA units/100 μL and maximum cell-specific virus productivities of 6,400 virions/cell (for human influenza A/PR/8/34 as a reference). Surface membrane expression of sialyloligosaccharides as well as HA N-glycosylation patterns were characterized. Overall, experimental results clearly demonstrate the potential of CAP cells for achieving high virus yields for different influenza strains and the option to introduce a highly attractive fully characterized human cell line compliant with regulatory and industrial requirements as an alternative for influenza virus vaccine production.

2025, Special publication

Knowledge of the three-dimensional structures of protein targets has the potential to greatly accelerate drug discovery, but technical challenges and time constraints have traditionally limited its use to lead optimization. Its application is now being extended beyond structure determination into new approaches for lead discovery. Structure-activity relationships by nuclear magnetic resonance have been widely used to detect ligand binding and to give some indication of the location of the binding site. X-ray crystallography has the advantage of defining ligand-binding sites with greater certainty. High-throughput approaches make this method applicable to screening to identify molecular fragments that bind protein targets, and to defining precisely their binding sites. X-ray crystallography can then be used as a rapid technique to guide the elaboration of the fragments into larger molecular weight compounds that might be useful leads for drug discovery.

2025, AAPS PharmSciTech

The aim of the study was to understand the impact of different concentrations of the additive material, magnesium stearate (MGST), and the active pharmaceutical ingredient (API), respectively, on the physicochemical properties and aerosol performance of comilled formulations for high-dose delivery. Initially, blends of API/lactose with different concentrations of MGST (1-7.5% w/w) were prepared and comilled by the jet-mill apparatus. The optimal concentration of MGST in comilled formulations was investigated, specifically for agglomerate structure and strength, particle size, uniformity of content, surface coverage, and aerosol performance. Secondly, comilled formulations with different API (1-40% w/w) concentrations were prepared and similarly analyzed. Comilled 5% MGST (w/w) formulation resulted in a significant improvement in in vitro aerosol performance due to the reduction in agglomerate size and strength compared to the formulation comilled without MGST. Higher concentrations ...

2025, World Journal of Microbiology and Biotechnology

Microalgae have been used in food, cosmetic, and biofuel industries as a natural source of lipids, vitamins, pigments and antioxidants for a long time. Green microalgae, as potent photobioreactors, can be considered as an economical expression system to produce recombinant therapeutical proteins at large-scale due to low cost of production and scaling-up capitalization owning to the inexpensive medium requirement, fast growth rate, and the ease of manipulation. These microalgae possess all benefit eukaryotic expression systems including the ability of posttranslational modifications required for proper folding and stability of active proteins. Among the many items regarded as recombinant protein production, this review compares the different expression systems with green microalgae like Dunaliella by viewing the nuclear/chloroplast transformation challenges/benefits, related selection markers/reporter genes, and crucial factors/strategies affecting the increase of foreign protein expression in microalgae transformants. Some important factors were discussed regarding the increase of protein yielding in microalgae transformants including: transformation-associated genotypic modifications, endogenous regulatory factors, promoters, codon optimization, enhancer elements, and milking of recombinant protein.

2025, International Journal of Pharmaceutics

Therapeutic strategies based on oral delivery of bilayer (and multilayer) tablets are gaining more acceptance among brand and generic products due to a confluence of factors including advanced delivery strategies, patient compliance and combination therapy. Successful manufacturing of these ever more complex systems needs to overcome a series of challenges from formulation design to tablet press monitoring and control. This article provides an overview of the state-of-the-art of bilayer tablet technology, highlighting the main benefits of this type of oral dosage forms while providing a description of current challenges and advances toward improving manufacturing practices and product quality. Several aspects relevant to bilayer tablet manufacturing are addressed including material properties, lubrication, layer ordering, layer thickness, layer weight control, as well as first and final compression forces. A section is also devoted to bilayer tablet characterization that present additional complexities associated with interfaces between layers. The available features of the manufacturing equipment for bilayer tablet production are also described indicating the different strategies for sensing and controls offered by bilayer tablet press manufacturers. Finally, a roadmap for bilayer tablet manufacturing is advanced as a guideline to formulation design and selection of process parameters and equipment.

2025, International journal of pharmaceutics

Bilayer tablets are generating great interest recently as they can achieve controlled delivery of different drugs with pre-defined release profiles. However, the production of such tablets has been facing great challenges as the layered tablets are prone to delaminate or fracture in the individual layers due to insufficient bonding strength of layers and adhesion at the interfaces. This paper will provide an insight into the role of interfacial topography on the performance of the bilayer tablets. In this study, two widely used pharmaceutical excipients: microcrystalline cellulose and lactose were investigated. Bilayer tablets were manufactured with a range of first and second layer compression forces. A crack of known dimensions was introduced at the interface to investigate the crack propagation mechanisms upon axially loading the bilayer tablet, and to determine the stress intensity factor (K(I)) of the interface (will be discussed in a separate paper). The results indicated that...

2025, International Journal of Pharmaceutics

2025, Acta poloniae pharmaceutica

The objective of this study was to formulate stable and controlled release microparticles for simultaneous delivery and UV spectrophotometric detection in combined dosage of an non-steroidal anti-inflammatory drug (NSAID) (nimesulide, NMS) and a spasmolytic agent (tizanidine, TZN) to maintain plasma concentration that may increase patients compliance, improved therapeutic efficacy, The aim was also to reduce severity of upper GI side effects of NMS because of alteration in delivery pattern via slow release of drug from microparticles and to increase the benefits of spasticity and disability for spastic patients by administering TZN in a modified release formulation as these two drugs are often prescribed in combination for the management of pain associated with muscles spasm. Ethyl cellulose was used as a retardant polymer. Drug-polymer and drug-drug compatibility study were conducted by different analytical tests. Microparticles were prepared by coacervation thermal change method. ...

2025, SLAS Discovery

High-throughput screening (HTS) is widely used in the pharmaceutical industry to identify novel chemical starting points for drug discovery projects. The current study focuses on the relationship between molecular hit rate in recent in-house HTS and four common molecular descriptors: lipophilicity (ClogP), size (heavy atom count, HEV), fraction of sp3-hybridized carbons (Fsp3), and fraction of molecular framework ( fMF). The molecular hit rate is defined as the fraction of times the molecule has been assigned as active in the HTS campaigns where it has been screened. Beta-binomial statistical models were built to model the molecular hit rate as a function of these descriptors. The advantage of the beta-binomial statistical models is that the correlation between the descriptors is taken into account. Higher degree polynomial terms of the descriptors were also added into the beta-binomial statistic model to improve the model quality. The relative influence of different molecular descr...

2025

Many kinds of technology have already been used to develop kunyit asam preparation, one of the development is to make kunyit asam preparation in a form of granul effervescent. The aim of this research is to know how the physical characteristic of granul effervescent from kunyit asam with different fillers such as dekstrosa, sukrosa and dekstrosa-sukrosa (50 : 50). Clinical tests of physical characteristic of granul effervescent from kunyit asam include moisture content, flow time, angle of repose, solubility time, bulk volume, tapping and it was added by additional clinical tested that is ALT and the sensitivity of flavour. Based on this research, the result of formula I (dekstrosa) had moisture content 2.84 %, flow time 8.25 seconds, angle of repose 32.61°, solubility time 1.45 minutes,bulk volume 42.165 g/100 ml, tapping 9,50%, the ALT bacterian was 1.7x10 1 CFU/ml, kapang 3.3x10 1 Propagul/ml and have not too sweet, quite salty, quite acid, not bitter taste. Formula II (sukrosa) ...

2025, University of Bath

In recent years there has been growing interest in the self-emulsified lipid technology as an approach for the oral delivery of hydrophobic compounds. The use of combinatorial chemistry in synthesizing active molecules has produced wide range of drugs with high molecular weight and poor water solubility. The rout for tablet formulation restricts the bioavailability of these compounds due to their low intrinsic water solubility and hence slow dissolution rate which' is a key step in the absorption of these compounds. Therefore, if a rapid onset action is required the choice for tablet formulation is not an efficient approach. Various formulation methods have been attempted to improve the bioavailability of lipophilic compounds of which, selfemulsifying drug delivery systems (SEDDS) exhibit the most successful approach. Dissolution and disintegration steps are not necessary for drugs formulated in SEDDS as they are presented to the GIT in a soluble form dissolved within the lipid matrix, and. ready for absorption after the emulsification process takes place. In order to facilitate dealing with these lipid systems, they were classified into type I, n, IIIA and EUB based on various physicochemical factors. In the design for a successful lipid formulation, various key elements in the composition have to be optimized to obtain dispersions with minimum emulsion droplet size, less sensitive to the presence of electrolytes in the emulsification media and are able to maintain the drug in solution after the dispersion of the formulation. These elements include; type of oil, the use of cosurfactant (mixed mono/di-glycerides), oil-cosurfactant ratio, type of surfactant and the inclusion of cosolvents. In this study a self-emulsifying type II formulation was developed composed of Miglyol 812 (medium chain triglycerides), Imwitor 988 (medium chain mono/di-glycerides) and the non-ionic surfactant Tagat TO. The constituents of this system are considered to be water insoluble materials which make the formulation highly unlikely to loose its solvent capacity after dispersion. Very fine dispersions of droplet size between 50 and 60nm which are arbitrary called o/w microemulsions were obtained at Miglyol 812/Imwitor ratios of 70/30 or 60/40 and at Tagat TO concentration of 30% w/w. Phase behaviour studies of these systems have shown regions of no liquid crystalline material (LC) yet, extended areas of water solubilization (L2) was observed. This indicates that 'Diffusion and Stranding' theory is the putative mechanism for the emulsification process in these systems. These systems appear to be prone to the effect of electrolytes present in the emulsification media. Furthermore, Physical characterization of resultant dispersions of type IE selfmicro-emulsified lipid system composed of Miglyol 812/Imwitor 988-Cremophor RH40 was carried out. Optimum dispersions of ~30nm were obtained using oil blends o f Miglyol 812/Imwitor 988 at ratios of 1:1 and Cremophor RH40 at concentration of 30% w/w. In order to find alternatives to Cremophor RH40 because of its waxy nature at ambient temperature, various hydrophilic surfactants were screened for microemulsion systems. Self-micro-emulsifying systems were obtained using blends o f Miglyol 812/Imwitor 988 at ratios of 1:1 in the case Cremophor EL, and at ratio of 2:3 in the case of Crillet 4 or Tagat 02. The inclusion of water-soluble cosolvents in SEDDS formulations was found to accelerate precipitation of drug after dispersion depending on the emulsification media. Oil-cosurfactant ratio, type of surfactant and the amount of included water-miscible cosolvents can influence the solubilization behaviour of the drug after dispersion. Finally, Solid self-micro-emulsified lipid systems (SMELS) were developed from eutectic mixtures of various solid carrier systems and oil mixtures. These new vehicles have the potential of presenting the dmg to the GIT in the amorphous state with no susceptibility to the aging processes. iv Contents Origin and Scope of this Study X CHAPTER 1 1 composed of oil blends of Miglyol 812/Imwotor 988 and various surfactant systems, investigating mechanistic processes involved in emulsification and exploring the fate x of dissolved drug after the dispersion of the formulation, and secondly; preparing self micro-emulsified lipid systems as a solid dosage form in order to replace costly and inconvenient soft gelatin capsule forms. * Sodium bis(2-ethylhexyl)-sulfocucinate (AOT) • Zwitterionic surfactants A particular important class of this type is the naturally occurring Phosphoglycerides, which include Phosphatidylethanolamine (PE) and Phosphatidylcholine (PC). • Nonionic surfactants Examples of nonionic surfactants include * Polyoxyethylenated fatty alcohol (Brij sereies) * Sorbitan esters (Span series) * Polyoxyethylene glycerol fatty acid esters (Tagat series) * Hydrogenated caster oil ethoxylates (Cremophor series) * Polyoxyethelene sorbitan esters (Tween series) The safest surfactants to be used orally are the nonionic types and the most widely used are probably the ethoxylated esters of fatty acids such as Tweens and Spans. Nonionic surfactant molecules contain a polar hydrophilic group (polyoxyethylene chain) and a non-polar (lipophilic) chain. This amphilicity results in a double affinity which can only be satisfied at a polar-non-polar interface. Nonionic surfactant-oilwater systems (nSOW) are usually 'pseudo ternary' i.e. the surfactant may be a mixture of surfactants, the aqueous phase may be a salt solution and the oil phase may be a mixture of oils or contain dissolved polymers.

2025

Quality by Design (QbD) refers to a holistic approach towards drug development. The purpose of research was to implement quality by design to study prospective process validation of 4 mg Salbutamol Sulphate Tablets with risk-based approach. Validation is one of the important steps in achieving and maintaining the quality of the final product. Quality Target Product Profile, Critical Quality Attributes, Critical Process Parameters, Design Space and control strategy are identified with the help of Quality Risk Management. Three initial batches of same size, method, equipment was taken for process validation. The critical parameters involved in sifting, dry mixing, preparation of granulating solution, wet mixing, drying, sizing, lubrication, compression were identified and evaluated. The formulation properties of three initial batches of process validated tablets are compared with the marketed products of Salbutamol Sulphate Tablets (Astahlin tab and Salbetol tab). Results obtained wit...

2025

Pendahuluan:Candida adalah jamur yang hidup pada manusia khususnya pada daerah rongga mulut, saluran cerna dan vagina. Candida merupakan mikroflora normal dalam rongga mulut. Candidasp.dilaporkan mengalami perubahan dari jamur oportunis yang jarang menyebabkan infeksi opotunistik. Prevalensi Candidiasis oral di Indonesia mencapai 84% sampai tahun 2009. Flukonazol sistemik efektif untuk Candida albicans97,9%. Terapi topikal miconazol memberi hasil 92,8% efektif dengan mikonazol. Tujuan: Penelitian ini bermaksud membandingkan daya hambat fluokonazol dengan mikonazol terhadap jamur Candida albicans. Metode:Penelitian ini merupakan penelitian eksperimental laboratorik dengan sampelsebanyak 32 biakan Candida albicans dibagi dalam 2 kelompok perlakuan yaitu dengan antijamur flukonazol dan mikonazol kemudian diukur diameter zona hambatnya. Uji statistik yang digunakan adalah uji Man-Whitney. Hasil: Penelitian ini menunjukkan dari kedua kelompok perlakuan tersebut kelompok flukonazol lebih ...

2025, Research in Pharmaceutical Sciences

Background and Aims: Children are particularly vulnerable to iron deficiency which is associated with a high risk of long-term impairment in mental and motor development. Liquid preparations may cause teeth staining and metallic taste of iron that reduce its compliance. One of the methods to control drug release from liquid dosage forms is the use of ion exchange resins. Methods: Amberlite IPR64 (a Weak acidic resin) was contacted with a Fe2+ solution to be loaded. The amount of drug loaded was determined by atomic absorption spectrometry. To prepare a drug -resin suspension, xantan gum, sorbitol and sucrose were utilized as suspending agents and flavorant respectively. Drug release in NaCl 0.7% solution as a simulated natural saliva and in SGF (simulated Gastric fluid) without enzyme as an acidic medium was determined. The taste of suspensions was evaluated with compare a marketed ferrous sulfate syrup using volunteer taste panels. The formulation was successful in taste masking. Drug release in NaCl 0.7% solution was much slower than it in SGF. Kinetics of release from iron -resin suspension in SGF without enzyme and NaCl 0.7% media followed particle diffusion and zero order kinetics, respectively. Conclusions: Ion exchange by weak acidic resins is a pH-dependent process. So they are suitable drug delivery systems for iron because they don't exchange their ions rapidly in neutral pH of saliva and are able to protect Fe2+ ions from contacting with tongue. In contrast it can immediately release them in acidic gastric fluid before passing out narrow absorption region of Fe2+.

2025, Journal of Virological Methods

To formulate inactivated influenza vaccines, the concentration of hemagglutinin (HA) must be accurately determined. The standard test currently used to measure HA in influenza vaccines is the Single Radial Immunodiffusion (SRID) assay. We developed a very rapid, simple and sensitive alternative quantitative HA assay, namely the Latex Agglutination Assay (LAA). The LAA uses the Spherotest ® technology, which is based on the agglutination of HAspecific immunoglobulin-coated latex beads. The amount of HA in a sample is calculated from the level of bead agglutination by a simple absorbance measurement at 405 nm against a standard curve generated using a monovalent vaccine standard. In less than 2 hours, tens of samples could be quantified using the LAA as opposed to 2 days for the SRID assay. Ten steps are required to complete an SRID assay as compared to 6 steps for the LAA, from sample preparation through spectrophotometric analysis. Furthermore, the limit of detection of the LAA was found to be approximately 15 ng HA/mL, similar to an ELISA, with the quantification of less than 1.8 μg HA/mL. The quantification limit of the SRID is usually considered to be approximately 5 μg HA/mL. The development of the assay and a comparison of the titers obtained by SRID and LAA for several monovalent vaccines corresponding to various strains were performed. For A/H5N1 and A/H1N1 monovalent vaccines, the LAA was found to be linear and accurate as compared to the SRID. The precision of the LAA was close to that of the standard test, and good reproducibility from one laboratory to another was observed. Moreover, the LAA enabled HA quantification in AlOOH-adjuvanted and in emulsion-adjuvanted low-dose vaccines as well as unadjuvanted vaccines. In conclusion, LAA may be useful to rapidly and accurately measure influenza HA protein in monovalent vaccines, especially in those containing less than 5 μg/mL of HA in the presence of an adjuvant.

2025, Journal of Virological Methods

2025, AAPS PharmSciTech

A transdermal formulation of indomethacin (IMC) was developed by incorporation into cholesteryl cetyl carbonate (CCC). The liquid crystalline phase properties of the IMC-CCC mixture were detected by polarized light microscopy and differential scanning calorimetry. A low drug loading was obtained (1-5 %) similar to that used in conventional topical IMC in a clinical setting. A controlled release of IMC was found over 12 h. A low amount of IMC in 1 % IMC-CCC permeated the stratum corneum. Further formulation development has been carried out by the addition of lauryl alcohol into 5 % IMC-CCC mixture it was found that the permeation of IMC was significantly improved to 45 % within 24 h.

2025

Pulsatile Drug Delivery systems (PDDS) are basically time-controlled drug delivery systems in which the system controls the lag time and drug is released in an immediate or extended fashion. The present study was conducted to develop and evaluate pulsatile release tablets of Rabeprazole sodium for the treatment of peptic ulcers. The compression coated tablets consisted of a core tablet containing drug with superdisintegrant, which was further coated by erodible outer layer consisted of HPMC K4M, ethyl cellulose and xanthan gum. After carrying out preformulation studies, the developed tablets were evaluated for post-compression parameters like weight variation, thickness, hardness, friability, drug content and in-vitro drug release study. The best formulation was selected on the basis of post-compression parameters and was subjected to accelerated stability studies for 1 month. Amongst 6 formulations prepared, C5 produced convincing results with a maximum cumulative drug release of 99.97% in 195 minutes. Also the formulation didn't show any significant changes during 1 month period of stress testing. By virtue of its release pattern and delivering the drug at the right time, right place and in right amounts, the developed delivery system holds good promises of benefiting the patients suffering from peptic ulcers.

2025, Ni Luh Putu Shintya Riani

ABSTRAK Negara Indonesia pada umumnya banyak menggunakan obat golongan analgetik dan antipiretik disamping jenis obat lainnya. Jenis obat tersebut banyak ragam dan bentuknya sesuai merk dagangnya dan beredar luas di pasar bebas, took obat, apotek, rumah sakit dan pusat pelayanan kesehatan masyarakat.Salah satu obat yang termasuk kedalam obat analgetik dan atipiretik adalah parasetamol. Tujuan dari penelitian ini adalah untuk menetapkan kadar parasetamol dalam sediaan tablet dan persen recovery parasetamol pada sediaan tablet dengan menggunakan metode analisis spektrofotometri ultraviolet-visible. Penelitian ini menggunakan metode true-eksperimen (eksperimen murni) yang dilakukan di laboratorium Kimia UNAR. Sampel yang digunakan adalah tablet parasetamol yang dijual di Kota padangsidimpuan yang di ambil secara acak. Hasil yang diperoleh adalah kadar parasetamol pada sediaan tablet parasetamol dengan 6 merek dagang yang berbeda berturut turut adalah merek A adalah 511 mg, merek B adalah 538 mg, merek C adalah 220 mg, merek D adalah 448 mg, merek E adalah 527 mg dan merek F adalah 448 mg. Data persentase recovery parasetamol dalam tablet parasetamol adalah telah sesuai Farmakope Indonesia edisi VI tahun 2020 yaitu tidak kurang dari 90% dan tidak lebih dari 110%.

2025, Asian Journal of Pharmaceutics

The main objective of present research work is to formulate the floating tablets of atenolol using 32 factorial design. Atenolol, β-blocker belongs to Biopharmaceutical Classification System Class-III. The floating tablets of atenolol were prepared employing different concentrations of hydroxypropyl methylcellulose (HPMC) K15M and sodium bicarbonate in different combinations by direct compression technique using 32 factorial design. The concentration of HPMC K15M and sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2, respectively, whereas time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%), and 90% (t90%) were selected as dependent variables. Totally, nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, floating lag time, in vitro drug release. From the results, concluded that all the formulation were found to be within the pharmacopoeial limits and the i...

2025

This narrative review aims to synthesize existing research on the formulation and evaluation of various cosmetic products, focusing on herbal lipsticks, salicylic acid face serum, and other dermatological formulations. The studies analyzed highlight the importance of natural ingredients, formulation stability, and efficacy in skincare and cosmetic products. By comparing multiple studies, this review provides insights into the advantages, challenges, and future directions of cosmetic formulation.

2025, Critical Reviews in Therapeutic Drug Carrier Systems

Poor aqueous solubility impedes a drug's bioavailability and challenges its pharmaceutical development. Pharmaceutical development of drugs with poor water solubility requires the establishment of a suitable formulation layout among various techniques. Various approaches have been investigated extensively to improve the aqueous solubility and poor dissolution rate of BCS class II and IV drugs. In this literature review, novel formulation options, particularly for class II drugs designed for applications such as micronization, selfemulsification, cyclodextrin complexation, co-crystallisation, super critical fluid technology, solubilisation by change in pH, salt formation, co-solvents, melt granulation, and solid dispersion, liposomal/niosomal formulations, are discussed in detail to introduce biopharmaceutical challenges and recent approaches to facilitate more efficient drug formulation and development.

2025, International Journal of Pharmaceutical Sciences and Medicine

Dithiocarbamate complex compounds can be used as an antibacterial and antifungal. Zinc compounds function as antioxidants, antibacterials, and zinc can stop the proliferation of cancer cells. Based on some of the activities of these groups, it is expected that the Zinc (II) N-Benzylmethyl Dithiocarbamate complex compound has the potential to be developed as a new drug candidate. A toxicity test must be carried out to determine the level of safety of the compound. The objective of this study was to determine the LD50 value and determine the category of toxicity of the Zinc (II) N-Benzyl methyl Dithiocarbamate compound in white mice (Mus muscles). Methods This research is a laboratory experimental study using 40 white mice, consisting of 20 male mice and 20 female mice. As for the treatment, namely the Na CMC group as a negative control, the dose of the test substance was 240, 480, 960mg/Kg BW. Observations of mice were carried out for 24 hours by observing the number of dead animals ...

2025, Clinical and Vaccine Immunology

Quantification of hepatitis B surface antigen (HBsAg) or relative in vitro potency in the final vaccines is a prerequisite for hepatitis B vaccine batch release. The commercial kit for automated analysis (AxSYM) is expensive, and an alternative is required for the estimation of HBsAg in hepatitis B vaccines. Mouse monoclonal antibodies (MAbs) specific for HBsAg were developed and characterized. One of the monoclonal antibodies (HBs06) was used in development of an immunocapture ELISA (IC-ELISA) as an unlabeled capture antibody and biotin-labeled detection antibody. The IC-ELISA was standardized and validated using experimental hepatitis B vaccine batches with various HBsAg concentrations per dose and commercial vaccines. The vaccine was treated with an alkaline solubilizer to desorb the HBsAg from Algel-adjuvanted vaccines before testing, and the sensitivity of the test was 5 ng/ml. A good correlation could be observed between the HBsAg estimates derived by both formats, except for ...

2025, Clinical and Vaccine Immunology

The potency of rabies vaccines, determined using the NIH mouse protection test, can be directly correlated to the amount of rabies virus glycoprotein (RV GP) present in the vaccine. In an effort to develop a simple and sensitive enzyme-linked immunosorbent assay (ELISA) using recombinant diabody for quantification of RV GP, the variable heavy (VH) and light chain (VL) domains of an RV GP-specific human monoclonal antibody (MAb) secreted by a human × mouse heterohybridoma (human MAb R16E5) was amplified, linked using splicing by overlap extension PCR (SOE PCR), and expressed as a recombinant diabody (D06) in the pET28a bacterial expression system. The diabody D06 was purified by immobilized metal affinity chromatography on a nickel-nitrilotriacetic acid (NTA) agarose column and characterized. The purified diabody was used in combination with a well-characterized RV GP-specific mouse MAb, M5B4, to develop an immunocapture ELISA (IC-ELISA) for the quantification of RV GP in human rabie...

2025

Herbal shampoo is a cosmetic preparation formulated using natural plant-based ingredients to cleanse,
nourish, and protect the scalp and hair. Unlike commercial shampoos that contain synthetic surfactants, herbal
shampoos utilize natural saponins and bioactive compounds from herbs
Herbal shampoos are mild formulations that cleanse the hair and scalp while maintaining moisture balance
and hair health. Unlike conventional shampoos, Aloe vera and essential oils provide nourishment and
hydration, while SLS acts as a foaming and cleansing agent. Sorbitol enhances conditioning, and parabens
ensure product stability by preventing microbial contamination. The formulation is standardized by evaluating
organoleptic properties, physicochemical parameters, and cleansing efficiency.

2025, International Journal of Applied Pharmaceutics

Objective: Terconazole is a potent antifungal agent characterized by insufficient aqueous solubility; which is a significant challenge for formulation development and therapeutic efficacy. The current research aimed to develop and optimize an innovative carrier system using micro-sponges to improve the solubility and dissolution rate of Terconazole. Methods: Fifteen formulations of Terconazole-loaded micro-sponges were prepared by quasi-emulsion solvent diffusion technique, with various parameters such as polymer type and concentration, emulsifying agent concentration, plasticizer percentage, and pore inducer amount being systematically investigated. The impact of these parameters on particle size, production yield, loading efficiency, saturation solubility, and In vitro dissolution profiles was thoroughly assessed. Results: The results indicated that formula F15, comprising 0.1g Eudragit L100, 25 mg Poly Vinyl Alcohol (PVA), 0.1 ml glycerol, and 1.5g Pre-Gelatinized Starch (PGS), exhibited the smallest particle size, higher production yield and loading efficiency, achieving a remarkable nine-fold enhancement in saturation solubility (752.26±19.84µg/ml) compared to pure Terconazole of 83.42±3.39µg/ml. furthermore, the percentage of Terconazole released after one hour from F15 was 92.85%, significantly higher than the 33.54% from its pure powder. Scanning Electron Microscope (SEM) analysis revealed highly porous structures of the micro-sponges, while Fourier Transform Infra-Red (FTIR) studies showed no evidence of chemical interaction, and Differential Scanning Calorimetry (DSC) indicated no change in Terconazole's nature during micro-sponges production. Conclusion: Overall, the findings suggest that micro-sponges represent a promising system for enhancing the saturation solubility and dissolution rate of poorly water-soluble Terconazole, potentially improving its bioavailability and therapeutic outcomes in clinical settings, especially ocular medications. The implications of this study extend beyond Terconazole, offering valuable insights and methodologies that can be applied to improve the solubility and bioavailability of a wide range of pharmaceutical compounds.

2025, International Journal of Applied Pharmaceutics

Objective: The study aims to investigate the effects of combining Ethyl Cellulose (EC) and Xanthan Gum (XG) matrix on the physical properties dissolution profiles and determine the optimal formula for sustained-release theophylline tablets. Methods: We used the Design Expert 13 software with the Simplex Lattice Design (SLD) models EC (A) and XG (B) to obtain the sustained release tablet formula of theophylline, which yielded seven formulas: F1 (80:120), F2 (110:90), F3 (120:80), F4 (90:110), F5 (100:100), F6 (120:180), and F7 (80:120). Granule evaluation included flowability rate, angle of repose, and compressibility index. Tablet evaluation included weight uniformity, hardness, friability, uniformity of content, and dissolution rate. Results: The physical properties of granules and tablets from the optimal formula showed that all test parameters met the standards. The granule flow rate was 11.98 g/sec, angle of repose 33.65, compressibility index 13.36%, tablet weight uniformity (%CV) 0.40%, tablet hardness 15.18, tablet friability 0.36%, content uniformity 98.03%, dissolution rate 11.30 mg/h. The effect of XG was more dominant in improving flow properties, angle of repose, compressibility index, weight uniformity, hardness, content uniformity, and dissolution rate. On the contrary, the more dominant EC could increase tablet friability and sustained drug release from the matrix. Conclusion: The optimal formula for theophylline sustained-release tablets contains a combination of EC: XG ingredients with a concentration of 107.03:92.97 mg, respectively, with a desirability value of 0.507.

2025, Journal of Pharmaceutical and Biomedical Analysis

The purpose of the present study was to investigate the possibility of improving the dissolution properties of glisentide, a poorly water-soluble antidiabetic drug, by grinding in a high energy micromill, alone or in mixture with polyvinylpyrrolidone (PVP). Conventional and modulated differential scanning calorimetry (DSC, MDSC), thermogravimetry (TGA), X-ray powder diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), hot-stage FT-IR thermomicroscopy and scanning electron microscopy (SEM) were used to characterize the drug solid state, whereas its dissolution rates were determined according to the dispersed amount method. The techniques utilized enabled exclusion of polymorphism phenomena as a consequence of mechanical treatment, and revealed a progressive drug amorphization during grinding. In particular, MDSC allowed a clear determination of the glass transition temperature of the amorphous drug, enabling separation of glass transition from enthalpic relaxation. The amorphous state of the ground drug was the main responsible factor for the obtained 100% dissolution efficiency increase in comparison with the untreated drug. Further significant increases in dissolution properties, directly related to the polymer content in the mixture, were obtained by co-grinding with PVP, whose presence clearly favored drug amorphization, allowing a strong reduction of time and frequency of grinding necessary for obtaining complete drug amorphization.

2025, ijabpt.com

Solid dosage forms are coated for a number of reasons, the most important of which is controlling the release profiles and bioavailability of the active ingredient. The amount of coating on the surface of a tablet is critical to the effectiveness of the oral dosage form. Tablets are usually coated in horizontal rotating pans with the coating sprayed onto the free surface of the tablet bed. Tablets must have a coating mass that lies within a prescribed range with very little inter-and intra-tablet coating variability. Using the Discrete Element Method (DEM), tablet coating can be simulated on the computer. Simulation data provide the position, velocity, and orientation of each tablet within the coater, allowing accurate measurements of the time and orientation that each tablet spends exposed to the coating spray.

2025

Fast dissolving tablets (FDT’s) are becoming more trendy in geriatric patients as it provides better patient-compilance, fast-action, and moreover; easy to administer even without water. Even they have played an emerging role in pediatrics patients because of incomplete development of muscular and nervous system. FDT’s are disintegrating or dissolve quickly in the saliva providing rapid onset of action. With the aid of superdisintegrants (excipients), the normal tablets/ capsules pharmacological-action has been enhanced; leading to what we say fast dissolving tablets. FDTs have advantages such as easy portability and manufacturing, accurate dosing, good chemical and physical stability nd an ideal alternative for geriatric and pediatric patients. FDTs have disintegrated quickly, absorb faster so, in vitro drug release time improve and this property of drugs (dosage form) enhanced bioavailability. FDT formulations have the advantage of both conventional tablet formulation and liquid d...

2025, Journal of Dentistry & Public Health

O termo fitoterapia vem do latim, “phyton” que significa planta, e “terapia” relacionado ao tratamento, cujo primeiro relato manuscrito em 1500 a.C. titulado “Papiro de Ebers”. A fitoterapia é a ciência que utiliza plantas para o tratamento de diversas enfermidades humanas. No Brasil, estudos demonstram um interesse do Sistema Único de Saúde (SUS) a respeito dos medicamentos fitoterápicos entre as décadas de 70 e 80, principalmente na atenção primária à saúde devido a diminuição do custo, porém poucos estudos observacionais são encontrados na literatura a respeito da utilização dos mesmos no sistema. O presente estudo trata-se de uma revisão de literatura com o objetivo de relatar os principais medicamentos fitoterápicos com ação antiinflamatória, como uma opção terapêutica para pacientes que não podem ou não desejam fazer uso dos antiinflamatórios não-esteroides (AINES). Para a sua construção realizou-se uma busca por artigos nas bases de dados PubMed, Scielo e na plataforma BVSalu...

2025

Dentin hipersensitif merupakan masalah utama dalam bidang kedokteran gigi. Pada umumnya lebih dari 90% area hipersensitif adalah terbukanya dentin di daerah akar gigi, biasanya di permukaan bukal gigi. Tujuan penelitian adalah untuk memperoleh efektivitas iontoforesis NaF 2% dan KCl terhadap nilai ambang nyeri dan kadar matrix metalloproteinase (MMP-8). Penelitian eksperimental dilakukan dengan cara mengukur nilai ambang nyeri gigi menggunakan vitalytester dan mengambil cairan gusi (GCF) menggunakan paper point sebelum dan sesudah iontoforesis pada gigi yang mengalami resesi gusi yang diamati selama 2 minggu dengan indikator kadar MMP-8 menggunakan metode ELISA. Sampel penelitian dibagi dalam beberapa kelompok perlakuan yaitu dilakukan iontoforesis dengan NaF 2%, KCl 2%, KCl 3%, KCl 3,5%, KCl 4%. Rancangan analisis untuk ambang nyeri dan kadar MMP-8 sebelum dan sesudah iontoforesis dengan paired T-test dan analysis of varians.Untuk mengetahui pengaruh berbagai konsentrasi bahan terh...