Pharmaceutical Chemistry Research Papers - Academia.edu (original) (raw)

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- Engineering, Microfluidics, Fluorescence Microscopy, Lab On A Chip
- by Tom van Den Kerkhof
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- Rheology, Pharmaceutical Technology, Pharmaceutical Chemistry, Lasers
- by Mark Walland
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- Immunology, Pharmaceutical Chemistry, Medicine, Prospective studies
- by Shahiq uz Zaman
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- Pharmaceutical Chemistry, Antioxidants, Humans, Color
- by Aura Rusu
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- Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Analysis, Quinolones
- by Michael Cima and +1
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- Fluorescence, Pharmaceutical Technology, Pharmaceutical Chemistry, Light
- by Craig Bunt
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- Engineering, Chemical Engineering, Analytical Chemistry, Biomedical Engineering

Widespread use of generic drugs is considered to be indispensable if reductions in total health care costs are to be achieved, but the market share of such drugs remains low. In general, generic drugs have the same active ingredients as brand-name drugs, but this is not always the case. Thus, toxicity profiles may vary when brand-name and generic drugs are compared. We retrospectively investigated the incidence of hyponatremia in patients receiving brand-name cisplatin (CDDP) and a generic counterpart thereof. We reviewed the medical records of patients treated with brand-name CDDP (n=53) and a generic formulation (n=26), and compared the incidences of hyponatremia and renal toxicity. Toxicities were graded using the Common Terminology Criteria for Adverse Events, version 4.0. Differences between groups were evaluated using the Student's t-test, and the odds ratio for hyponatremia was estimated via logistic regression analysis. Serum creatinine levels after chemotherapy increase...

- by Katsuyuki Kiura
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- Pharmaceutical Chemistry, Humans, Female, Male

Classically, the end point detection during fluid bed drying has been performed using indirect parameters, such as the product temperature or the humidity of the outlet drying air. This paper aims at comparing those classic methods to both in-line moisture and solid-state determination by means of Process Analytical Technology (PAT) tools (Raman and NIR spectroscopy) and a mass balance approach. The six-segmented fluid bed drying system being part of a fully continuous from-powder-to-tablet production line (ConsiGma™-25) was used for this study. A theophylline:lactose:PVP (30:67.5:2.5) blend was chosen as model formulation. For the development of the NIR-based moisture determination model, 15 calibration experiments in the fluid bed dryer were performed. Six test experiments were conducted afterwards, and the product was monitored in-line with NIR and Raman spectroscopy during drying. The results (drying endpoint and residual moisture) obtained via the NIR-based moisture determinati...

- by Chris Vervaet and +1
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- Pharmaceutical Technology, Raman Spectroscopy, Pharmaceutical Chemistry, Near Infrared Spectroscopy
- by Suresh Venkataram
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- Pharmacokinetics, Pharmaceutical Chemistry, Dosage Form, Lipids

Identification of the constituents of Amaranthus spinosus was carried out using ethanol extract of the dried leaf of the plant. Microbial detection of zone of inhibition was also carried out. The extract yield from the leaves was 17.40 g while phytochemical screening indicated the presence of saponins, alkaloids, flavonoids, terpenoids and glycosides in the leaf extract. The antimicrobial assay indicated that methanolic extract of the plant were slightly active against the test isolates with the extract being more active against Staphylococcus aureus (15mm), Aspergillus flavus (15mm), E. coli. (13mm) and Mucor spp (10mm). Hence methanol extract of this plant has potent medical values.

The effect of six different preservatives on the production process and stability of resveratrol nanosuspensions was investigated. Nanosuspensions of the anti-oxidant resveratrol were prepared by high pressure homogenization (1,500 bar, 20 homogenization cycles). The preservatives used were: caprylyl glycol (0.75%), Euxyl PE 9010 (1.0%), Hydrolite-5 (2.0), Phenonip (0.75%), Rokonsal PB-5 (0.5%) and MultiEx Naturotics (2.0%). Preservation is essential for oral and dermal nanosuspensions, but can impair the stability. The effect of the preservatives on stability as a function of cycle numbers was determined by size measurements (photon correlation spectroscopy (PCS), laser diffraction (LD) and light microscopy). Zeta potential measurements were performed for determination of the Stern potential (measurements in water) and as stability criterion (measurements in original dispersion medium), to elucidate the mechanism of destabilization. The preservatives could be placed into three grou...

- by Kwabena Ofori-kwakye
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- Water, Electrochemistry, Nanoparticles, Pharmaceutical Chemistry
- by Daryl Drummond
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- Biomedical Engineering, Breast Cancer, Nanoparticle, Nanoparticles

Dry powder formulations are often composed of fine drug particles and coarser carrier particles, typically alpha-lactose monohydrate. However, the performance of a powder formulation may be highly dependent on the lactose quality and source. This study investigated the characteristics of lactose that influence the drug-to-carrier interaction and the performance of lactose-based dry powder inhaler formulations. The selected lactoses differed in the preparation processes and the content of fine lactose particles. Efficiency testing was done using fluticasone propionate and terbutaline sulphate as model drugs. Inverse gas chromatography was used to determine the surface heterogeneity distribution of different energy sites of the lactose and to understand the mechanism by which the fine carrier particles can improve the performance of dry powder inhalers. To assess the adhesion of respirable-sized drug to carrier particles, a simple method was developed based on aspiration and consideri...

- by Marie-Pierre Flament
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- Pharmaceutical Technology, Pharmaceutical Chemistry, Aerosols, Adsorption
- by Mari lia
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- Pharmaceutical Chemistry, Aerosols, Lung Cancer, Humans

Autophagy is an intracellular bulk degradation process for elimination of damaged macromolecules and organelles. In the past decades, the scientific community has gained increasingly detailed understanding of the role of autophagy in myocardial homeostasis, although still many controversies remain. In the ischemic myocardium, autophagy appears to be beneficial for survival, whereas upon reperfusion the process may induce cell death. However, the overall effect of autophagy seems to depend on the duration and intensity of stress, as along with the extent of autophagy within myocardial tissue. Reperfusion of an ischemic heart maybe harmful, but it is an essential process for myocardial survival. One of the major adverse consequences of reperfusion is the occurrence of ventricular fibrillation (VF). In the present study, we investigated the possible connection between autophagy and VF. Isolated mouse hearts were subjected to ischemia/reperfusion (I/R) and divided into two groups based on the development of VF at the beginning of reperfusion. Western blot analysis was conducted for autophagy-associated proteins LC3B, ATG-5, ATG-7, ATG-12, Bcl-2 and Beclin-1 proteins. Significantly higher level of Beclin-1 and LC3B-II/LC3B-I ratio (both definitive autophagy biomarkers) was observed in the fibrillated myocardium, versus tissue from the nonfibrillated hearts. Interestingly, although Bcl-2 is a major regulator of Beclin-1, level of this protein was not significantly altered in tissue from fibrillated, versus non-fibrillated hearts. Moreover, Atg7 expression showed a trend, albeit nonsignificant, towards elevation in fibrillated versus non-fibrillated hearts. Results of the present investigation demonstrate a possible link between VF and autophagy. Studies by authors of this report to evaluate potential etiologic relationships between the two processes are ongoing.

- by Cyril Reboul and +2
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- Pharmaceutical Technology, Autophagy, Pharmaceutical Chemistry, Ischemia Reperfusion Injury
- by Bill Doub
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- Drug delivery, Pharmaceutical Chemistry, Adhesion, Quality Control

Recent studies have implicated the orexin system as a critical regulator of sleep/wake states, feeding behavior, and reward processes. Orexin deficiency results in narcolepsy-cataplexy in humans, dogs, and rodents, suggesting that the orexin system is particularly important for maintenance of wakefulness. Orexin agonists and antagonists are thought to be promising avenues toward the treatment of sleep disorders, eating disorders, and drug addiction. In this chapter, we discuss the current understanding of the physiological roles of orexins in regulation of arousal, sleep/wake states, energy homeostasis, and reward systems.

- by Taizo Matsuki
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- Pharmaceutical Chemistry, Medicine, Dogs, Narcolepsy

Drugs contamination to wastewater from health care facilities and the pharma industry is a growing problem attracting scientific solution and engineering treatments. This study was performed for the adsorptive removal of paracetamol from water employing activated carbon (AC) prepared from Cannabis Sativum Hemp (CSH). The used CSH is spontaneously available lignocellulosic biomass that nurtures on the roadside and in uncultivated lands naturally. Process performance was optimized by studying the consequences of experimental features, such as pH, particle size, temperature, retention time, stirring speed, and adsorbent dose. Adsorption dynamics were studied employing Langmuir isotherms and Freundlich isotherms. Isothermal dynamics showed that the adsorption of paracetamol on the developed adsorbent was favorable. The kinetics analysis elucidated that the adsorption follows the pseudo second-order model preferably as the value of R 2 = 0.9893. The maximum adsorption capacity of developed activated carbon was found to be 16.18 mg/g. The study results proved that the CSH is an efficient, cheap, and sustainable feedstock for the manufacturing of AC to be used for the efficient removal of paracetamol from an aqueous system.

- by Giorgio Gasparini
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- Pharmaceutical Chemistry, Humans, Bacteria, Orthopedics
- by Mohammad Nutan
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- Pharmaceutical Technology, Pharmaceutical Chemistry, Animals, Male
- by K. Seifert
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- Microbiology, Medical Microbiology, Pharmaceutical Chemistry, Intestinal Parasites
- by Duke Fitch
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- Organic Chemistry, Pharmaceutical Chemistry, Humans, Animals
- by Rosa Cusidó and +1
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- Pharmaceutical Chemistry, Plants, Paclitaxel, Structure activity Relationship
- by Elisabeth Peeters and +1
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- Pharmaceutical Technology, Raman Spectroscopy, Pharmaceutical Chemistry, Near Infrared Spectroscopy
- by Fabrice Krier and +3
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- Analytical Chemistry, NIRS, Pharmaceutical Chemistry, HPLC

The present study aimed to produce verapamil hydrochloride-loaded solid lipid microparticles (SLM) by the w/o/w emulsion solvent evaporation technique, using diethyl ether as solvent phase, glyceryl monostearate as biodegradable polymer and Span 60 as surfactant. SLM of spherical shape were prepared by simple dilution of the emulsion with water. To increase the lipid load the process was conducted at 50 degrees C, and in order to reach sub-micron size, a high-shear homogenizer was used. The encapsulation efficiency of prepared SLM reached 74.29 +/- 0.76%. Particle size (98.55 +/- 1.42 microm), surface morphology (spherical) and drug loading efficiency (18.57 +/- 1.25% w/w) were investigated. And optimization of drug polymer ratio (3:1), nature and concentration of emulsion stabilizer in the external aqueous (0.1%), phase viscosity of external aqueous phase (0.5%), volume of external aqueous phase and stirring rate (1000 rpm) were detected. Analysis of microsphere content after proce...

Oral dosage forms are the most popular way of taking medication, despite having some disadvantages compared with other methods like risk of slow absorption of the medicament, which can be overcome by administering the drug in liquid form, therefore, possibly allowing the use of a lower dosage. However, instability of many drugs in liquid dosage form limits its use. Effervescent technique can be used as alternate to develop a dosage form which can accelerate drug disintegration and dissolution, is usually applied in quick release preparations. Along with the development of new pharmaceutical technique, effervescent tablet are more and more extensively to adjust the behaviour of drug release, such as in sustained and controlled release preparations, pulsatile drug delivery systems, and so on. This review demonstrated the new applying of effervescent technique in effervescent tablets. Keywords: Effervescent Tablet, Sustained release, Floating Delivery System

- by HIren patel
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- Materials Science, Chemistry, Pharmacogenomics, Pharmaceutical Technology
- by Shilpa Shrotriya
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- Pharmacology, Pharmacy, Pharmacy Practice, Pharmaceutical Chemistry

A novel stability-indicating reverse phase high performance liquid chromatography method was developed and validated for the simultaneous determination of Celecoxib (CEL) and Diacerein (DIN) and its impurities in capsule dosage form. The method was developed using L1 column with gradient using the mobile phase consist of Solution A (pH = 2.3 buffer) and Solution B (methanol and acetonitrile; 50 : 50, v/v). The eluted compounds were monitored at 255 nm. CEL and DIN were subjected to oxidative, acid, base, hydrolytic, thermal and photolytic stress conditions. The developed method was validated as per International Conference on Harmonisation guidelines with respect to specificity, linearity, limit of detection, limit of quantitation, accuracy, precision and robustness. The limit of quantitation results were ranged from 0.07 to 0.09 µg/mL for CEL impurities and 0.052 to 0.065 µg/mL for DIN impurities. This method is suitable for the estimation of impurities and assay of CEL and DIN in ...

- by Christian Silva
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- Chemistry, Pharmaceutical Technology, Pharmaceutical Chemistry, Medicine
- by Melis Cagdas
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- Pharmaceutical Chemistry, Ultrafiltration, Cholesterol, Pharmaceutical

The aim of this work was the evaluation of conductivity assessments for the monitoring and controlling the release study process of chlorhexidine and lidocaine hydrochloride from the ionic polyacrylic gel, applying different temperatures. According to performed measurements of release, the chlorhexidine, characterized by very low water solubility, is observed in the acceptor compartment in the amount of 2.0-3.0% and its level depends of the temperature. The amount of well soluble lidocaine hydrochloride released in parallel conditions was between 60 and 70%. Beyond, the assessments confirm the presence of a specific bond between the chlorhexidine imine groups and polyacrylic acid carboxylic groups. Presented method may be applied in the prediction of release rates, before actual release analysis, and may assure better evaluation of the systems.

- by Vanja Kokol
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- Polymers, Pharmaceutical Chemistry, Temperature, Solubility

Objective: In this study, the antioxidant activities of methanolic extract of marketed tobacco products were evaluated by different in vitro antioxidant methods. Materials and methods: The different marketed tobacco products were extracted with methanol by means of maceration process. These extracts were screened for antioxidant activity by different in vitro assay methods including Reducing power assay, Phosphomolybdenum assay, Iron chelating assay and Nitric oxide scavenging activity. The screening was carried out at different concentration including 100, 200, and 300µg/ml in reducing power assay, phosphomolybdate assay and Nitric oxide scavenging activity while in chelating assay the extract was used in concentration of 50, 100, 150 and 200µg/ml. Results: All Tobacco products exhibit the antioxidant potential with increasing concentration. The anti-oxidant activity of the marketed tobacco product might be attributed to its polyphenolic content and other phytochemical constituents. Hence, further investigation need to be carried out to isolate and identify the anti-oxidant compounds present in the Tobacco extract. Conclusion: Our study concluded that, the Tobacco causes addiction and dependence but till it has many folklore traditional medicinal uses. If it is used in positive way then it has power to treat and protect but if misused then it have power to harm the body.

- by Prachi Barsagade
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- Pharmaceutical Chemistry

Animals are used as experimental models to reproduce human diseases. To date, various animal models have been successfully
developed by numerous methods to simulate human diseases including chronic kidney disease (CKD). Such models have played a
central role in developing dialysis, transplantation experiments and more importantly in the discovery of new therapeutic agents
from natural product for the care of patients with kidney disease. This review focuses on key information on in vivo models of
CKD that have been developed through spontaneous, acquired and genetic approaches. Most of the experiments related to CKD
have been carried out on rodent models such as mice and rats. Spontaneous disease models of CKD are generated by various
metabolic and immunological methods. Nephrotoxic agents including adenine, adriamycin, cisplatin, folic acid, aristolochic acid
and oxalate are used to induce CKD in addition to nephrectomy and unilateral ureteral obstruction models. Further, animal models
developed through forward and reverse genetic approaches provide artificial models of CKD. Developing animal models to
approximate human CKD is a challenging task since it requires reflecting the effect of age, sex, and comorbidities in addition to
the disease condition. But, their usage to tease out the processes which can cause pathologic changes in a biological system is still
important for the health care improvements related to CKD. However, no animal model can exactly simulate response in human
CKD.
Keywords: Acquired methods, Animal models, Chronic kidney disease, Genetic approaches, Nephrotoxic agents, Spontaneous
models.

The two-part article aimed to investigate poloxamer 407-based microspheres as a novel platform for enhancing and controlling the delivery of atenolol across the oromucosal tissue. In the Part I of the work, atenolol-loaded poloxamers 407 microparticles were prepared by the solvent free spray congealing technology. This approach was feasible upon the high viscosity of the systems allowing for high loaded (20% w/w) non-aggregated microspheres. Several formulations were studied and the results demonstrated that the drug release patterns, solubility data, mucoadhesion to buccal tissue and gelling properties in saliva could be modified by adding different amount of an amphiphilic polymer-lipid excipient (Gelucire(®) 50/13) to poloxamer 407. Particularly, microspheres based only on poloxamer 407 exhibited very high solubility, mucoadhesive strength and gelling behaviour. To assess their potential as matrix for buccal application, the gelling property and the drug release from tablets obta...

- by Suchita Srivastava
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- Organic Chemistry, Cytotoxicity, Pharmaceutical Chemistry, Antioxidants
- by Daniel Canafax
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- Pharmaceutical Chemistry, Humans, Female, Male
- by Lumir Hanus
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- Pharmaceutical Chemistry

. An isocratic high-performance liquid chromatography (HPLC) procedure was developed for the dissolution rate studies and quantitative determination of valdecoxib in solid dosage forms and in active pharmaceutical ingredient. HPLC separation was carried out by reversed phase chromatography on a Syn-ergi ® fusion C 18 column (150 mm x 4.6 mm i.d.; 4 µm particle size), held at 30 ºC. The mobile phase con-sisted of water, pH 7.0/acetonitrile (52:48, v/v), run at a flow rate of 1.0 mL/min and with UV detection at 210 nm. Method validation investigated parameters such as the linearity (r 2 =0.9999), range, precision, ac-curacy, robustness and specificity. The method yielded good results with a quantitation limit of 50 ng/mL and a detection limit of 10 ng/mL. The dissolution test conditions and the dissolution medium was chosen as 0.5% of sodium lauryl sulfate in water at a stirring rate of 75 rpm. The described method can be successful-ly applied for the analysis of tablets, active pharm...

- by Marcio Fronza
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- Pharmacology, Analytical Chemistry, Pharmacy, Pharmaceutical Technology
- by Ted Whittem
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- Pharmaceutical Chemistry, Dogs, Prospective studies, Female
- by Andrew Lamb
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- Microbiology, Medical Microbiology, Pharmaceutical Chemistry, Escherichia coli
- by H. Elmoazzen
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- Engineering, Algorithms, Water, Biology
- by Christian Surber
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- Ophthalmology, Filtration, Pharmaceutical Chemistry, Sterilization

Microbubbles system is a newly invented non-invasive technique in which, in the presence of ultrasound waves or harmonic sounds
micropores shrinks and agitated to produce micro bubbles within the applied area. These bubbles have the capability to target any perfused
tissues within our body. Recently it was postulated that due to its narrow size range (1 to 10μm vesicular diameter) it can get easily engulf
by phagocytic blood cells which can be very effective on lymphocytic cancer. Micro bubbles are prepared by using mechanical agitation,
ultrasonication, pressurized gas-liquid mixing system etc. Micro bubbles are made up of a monolayer of protein shells, lipid shells, surfactant
shells, polymer shells, Polyelectrolyte multilayer shells. Initially, microbubbles are used as diagnostic tools but due to its versatility of uses and properties of surface conjugation of proteins, genes, micro molecular nutrients, drugs slowly it’s becoming a therapeutic delivery tool. ALBUNEX® (GE Healthcare) was the first albumin conjugated micro bubble which was been approved by US-FDA. Recently importance is been given for brain targeting using Micro bubble carrier system. It was observed that using passive and active transport micro streamed bubbles can able to transport through Blood Brain Barrier (BBB). It is very important to give more importance to its stability and canonization of globules for more industrial acceptability.