RAMU SAMINENI - Academia.edu (original) (raw)

Papers by RAMU SAMINENI

Research journal of pharmacy and technology, Jul 29, 2022

The bronopol and kathon are chemical preservative which prevent degradation of milk samples and m... more The bronopol and kathon are chemical preservative which prevent degradation of milk samples and maintain authenticity in analysis. The detection is based on HPLC-UV-Vis spectroscopy, in which C 18 column (250 mm 9 4.6 mm, 5 lm) was used for chromatographic separations, with a mobile phase comprising 0.1% phosphoric acid in water: Methanol: 0.1% phosphoric acid in acetonitrile (80:10:10) at a flow rate 0.8 ml/min at ambient temperature and with the UV detection at 250 nm for bronopol and 274 nm for kathon. The retention time of bronopol, kathon (MI 2-methyl-4-isothiazolin-3-one) and kathon (CMI 5-chloro-2-methyl-4-isothiazolin-3-one) was 4.52 min, 3.98 min and 6.68 min respectively with a total run time of 10 min. The linearity of the method was satisfactory with regression coefficient (R 2) = 0.99. The limit of quantification was 72, 240, 390 mg L-1 for bronopol, kathon (MI) and kathon (CMI) respectively. Five spiked levels (62.5, 125, 250, 500 and 1000 mg L-1) were used to determine the recovery of bronopol, kathon (MI) and kathon (CMI) which was found to be 95.41 ± 11.84, 95.75 ± 8.21 and 92.22 ± 14.64% respectively, with relative standard deviations in the range 5.9-14.6%. The standardized analytical method was successfully used to rapidly detect bronopol and kathon in milk samples.

Research Journal of Pharmaceutical Dosage Forms and Technology, 2019

INDIAN DRUGS

5-Chloro-N-((2-oxo-3-(4-(3-oxomorpholino) phenyl) oxazolidin-5-yl) methyl) thiophene-2-carboxamid... more 5-Chloro-N-((2-oxo-3-(4-(3-oxomorpholino) phenyl) oxazolidin-5-yl) methyl) thiophene-2-carboxamide derivatives were synthesized in a simple and efficient approach using 2-(oxiran-2-ylmethyl) isoindoline-1, 3-dione, 4-(4-aminophenyl) morpholin-3-one, and 5-chlorothiophene-2-carbonyl chloride by stepwise synthesis. Three compounds 3, 4 and 7 were designed, prepared, and screened for anticancer activity against HeLa, MCF- 7, A-549 and K-562 and antibacterial activities against Gram +ve and Gram -ve strains. The carboxamide moieties proved to be capable for the development of new anticancer and anti-bacterial agents. Docking studies carried out on target receptors caspase-3 HeLa cell line and Staphylococcus aureus DNA-Gyrase also supported the anticancer and antimicrobial activity of compounds 3, 4 and 7

A gene (<i>PSTG2</i>) coding for a novel β-glucosidase belonging to glycoside hydrola... more A gene (<i>PSTG2</i>) coding for a novel β-glucosidase belonging to glycoside hydrolase family 3 was identified in the vicinity of the previously identified β-glucosidase gene [sesaminol triglucoside (STG)-hydrolyzing β-glucosidase, PSTG1] in the genome of <i>Paenibacillus</i> sp. strain KB0549. Compared with PSTG1, recombinant PSTG2 more specifically acted on the β-1,2-glucosidic linkage of the STG molecule to transiently accumulate a larger amount of 6-<i>O</i>-(β-D-glucopyranosyl)-β-D-glucopyranosylsesaminol.

EUROPEAN CHEMICAL BULLETIN, 2023

Nanosponges are small sponges where they reach the target site and stick to that surface and init... more Nanosponges are small sponges where they reach the target site and stick to that surface and initiate to release in a controlled manner they canalso be loaded with the various types ofmedications.Drugs loaded with Nanosponges improves their dissolution rate, solubility, rate of release, stability, reduces the frequency of dosing and improves bioavailability.
Nanosponges are mostly used in targeted drug delivery system. Drug delivery is the major problem faced in the pharmaceutical field from a long time by the invention ofNanosponge technology has become important step so that we can minimize some problems like poor solubility, poor stability and dosing frequency. The main advantage of this Nanosponge is it can be loaded by both hydrophilic and lipophilic drugs.The present review article is to discuss about the general introduction, composition of Nanosponges, drugs loaded with Nanosponges, different preparation techniques and evaluations methods for the Nanosponge tablets. Zeta potential, Fourier transform-infrared spectroscopy, determination of percentage yield, particle size analysis, porosity, invitro dissolution studies and entrapment efficiency by these characterizations we can know the inclusion complexes formed in between drug and Nanosponges, mainly lansoprazole loaded Nanosponges characterization parameters and evaluations are presented in this article.Nanosponges can deliver the drug through various routes like oral, topical, aerosol and parenteral administration.

Chromatographia

Since the stability of the pharmaceuticals plays a crucial role in efficacy and safety while usin... more Since the stability of the pharmaceuticals plays a crucial role in efficacy and safety while using them in the treatment of disorders, the evaluation of purity and impurity profiling of pharmaceuticals is of utmost importance using efficient analytical techniques. The present study explains the identification, isolation, and characterization of stress degradation products of the anti-human immunovirus drug Darunavir. The degradation study was performed to evaluate the stability profile of Darunavir in different stress conditions like hydrolytic, oxidative, thermal, and photolytic conditions as per the ICH guidelines. Degradation products were identified using ultra-performance liquid chromatography coupled with mass spectrometry, isolated using semi-preparative high-performance liquid chromatography, and structural characterization by HRMS and 1 H, 13 C NMR (1D, 2D). Darunavir is relatively stable in oxidative, thermal, and photolytic conditions; however, considerable degradation was observed in acid and base hydrolysis. A total of five degradation products were identified and isolated in acid and base degradation. DP-1, DP-2, & DP-3 were observed in acid conditions, whereas in base conditions, along with DP-2, two more DPs, i.e., DP-4 & DP-5, were identified. Among the five DPs, two degradation products, namely DP-1: N-(4-(N-(3-amino-2-hydroxy-4-phenylbutyl)-N-isobutylsulfamoyl) phenyl) acetimidamide. & DP-3: hexahydrofuro[2,3-b] furan-3-yl(4-((4-acetimidamido-N-isobutylphenyl)sulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate, are novel, remaining degradation products DP-2: 4-amino-N-(3-amino-2-hydroxy-4-phenylbutyl)-N-isobutylbenzenesulfonamide, DP-4: 4-amino-N-(((5S)-4-benzyl-2-oxooxazolidin-5-yl) methyl)-N-isobutyl benzenesulfonamide and DP-5: methyl ((3S)-4-((4amino-N-isobutylphenyl) sulfonamido)-3-hydroxy-1-phenylbutan-2-yl) carbamate are already reported tentatively using a single analytical technique coupled with mass analysis without any evidence from NMR and IR data. Hence, the present study focused on using High-Resolution Mass, 1D, and 2D 1 H, 13 C NMR data for concrete confirmation of structures for degradation products.

Journal of Pharmaceutical Negative Results, Oct 22, 2022

Background: Cocrystals are defined as multiple component structures whose components interact thr... more Background: Cocrystals are defined as multiple component structures whose components interact through non-covalent interactions. Cocrystals can enhance other essential properties of the APIs. Aim: The current research work focuses on formulating and evaluating novel co-crystals of Lamotrigine anti-epileptic drug (BCS-II) Methods: The Cocrystals of Lamotrigine drug with different cocrystals formers like Saccharin sodium, 4-Hydroxy benzoic acid, and Methyl paraben used with molar ratios (1:1) were prepared by solvent drop method, co-grinding method, and solvent evaporation method. Results: The results signify the establishment of intermolecular interaction within the cocrystals. In the novel cocrystals, Lamotrigine was determined to be engaged in the hydrogen bond interaction with the complementary functional groups of Saccharin sodium, 4-Hydroxy benzoic acid, and methyl paraben. Compared with the pure Lamotrigine flow properties for prepared co-crystal by using solvent evaporation method crystals are showing excellent flow properties. LTG-SAC CF I, LTG-HBA I, and LTG-MP III showed 49.6 folds, 7.4 folds, and 3.36 folds improved solubility respectively. The dissolution test showed that the LTG-SAC CF I, LTG-HBA I, and LTG-MP III cocrystals exhibited a 1.09-fold, 1.08-fold, and 1.07-fold higher dissolution rate than the pure Lamotrigine. Conclusions: LTG-SAC CF I, LTG-HBA I, and LTG-MP III cocrystals showed modification in the chemical environment, intermolecular interactions were established, improved flow properties with enhanced intrinsic solubility and in-vitro dissolution rate than pure drug.

Research Journal of Pharmacy and Technology

Objective: The objective of this work is to develop a precise, accurate and validated reverse pha... more Objective: The objective of this work is to develop a precise, accurate and validated reverse phase ultra-performance liquid chromatographic technique for effective simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation. Method: Separation of the selected drugs was optimized after several trials including changing mobile phase and its composition, stationary phase, flow rate, column temperature, etc. Finally the separation of drugs was achieved on BEH C18 column using a mixture of methanol and phosphate buffer having pH 3.5 in the ratio of 65:35 v/v as mobile phase with flow rate of 0.3 ml/min and the analytes were detected at a wavelength of 260 nm. Results: The developed method was validated by determining the parameters like linearity, system suitability, recovery, precision, specificity, robustness, ruggedness, LOD, and LOQ as per the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (...

Open access jounrals, Dec 14, 2020

Effect of sodium alginate in combination with natural and synthetic polymers on the release of ve... more Effect of sodium alginate in combination with natural and synthetic polymers on the release of verapamil hcl from its floating

International Journal of Research in Pharmaceutical Sciences, 2021

The goal of the research is to design and optimize Nebivolol Hydrochloride immediate-release tabl... more The goal of the research is to design and optimize Nebivolol Hydrochloride immediate-release tablet using response surface methodology. Nebivolol Hydrochloride immediate-release tablets used in the treatment of heart attacks, myocardial infarction. Response surface methodology calculations for this optimization study were performed utilizing Minitab 17. Different formulations of immediate-release were prepared by applying 2 factors 3 levels full factorial design using Minitab 17, which gave 9 formulations by using the wet granulation method. Independent variables like the amount of hydroxypropyl methylcellulose (X1), and microcrystalline cellulose (X2) and dependent variables like the per cent drug release at 45 minutes (Y1), disintegration (Y2) were selected for optimization. The prepared batches of Nebivolol Hydrochloride immediate-release tablets were evaluated for the pre-compression and post-compression parameters like weight variation, thickness, hardness, and friability, disi...

Effect of coformers on novel co-crystals of gabapentin: an in vivo approach - Drug readily crosse... more Effect of coformers on novel co-crystals of gabapentin: an in vivo approach - Drug readily crosses the blood-brain barrier

American Journal of Advanced Drug Delivery, 2013

Formulation research is oriented towards safety, efficacy and quick onset of action of existing d... more Formulation research is oriented towards safety, efficacy and quick onset of action of existing drug molecule through novel concepts of drug delivery. Orally disintegrating tablets of sumatriptan succinate were prepared by direct compression method to provide faster relief from pain to migraine sufferers. About twelve formulations for the present study were carried out based on 2 level 2 factor full factorial design for each set of superdisintegrants. Croscarmellose sodium, Crospovidone and Sodium starch glycolate (SSG) were used as superdisintegrants, while microcrystalline cellulose was used as diluent. The prepared batches of tablets were evaluated for weight variation, hardness, friability, wetting time, invitro dispersion time, drug content and invitro dissolution studies. The formulation containing combination of Croscarmellose sodium and Sodium starch glycolate showed rapid invitro dispersion time as compared to other formulations . The optimized formulation dispersed in 8 se...

Turkish Journal of Pharmaceutical Sciences, 2021

Biopharmaceutical Classification System (BCS) is an advanced tool utilised for classifying medici... more Biopharmaceutical Classification System (BCS) is an advanced tool utilised for classifying medicines based on dissolution, water solubility, and intestinal permeability, which affect the absorption of active pharmaceutical ingredients from immediate release solid oral forms. It is useful to the formulation researcher to develop novel dosage forms based on modernistic rather than experimental approaches. The current review focuses on the fundamentals, objectives, guidance of BCS, characteristics of BCS drugs, their importance and applications of BCS. This review explains the challenges in drug development in terms of solubility and in vivo disposition. In the current review, new strategies for improving BCS II drug solubility as well as biopharmaceutical drug disposition properties which are utilised throughout the early stages of drug development and commercialisation are mainly discussed.

Research Journal of Pharmaceutical Dosage Forms and Technology, 2019

Objective: The main objective of the study was to formulate the oral disintegrating films loaded ... more Objective: The main objective of the study was to formulate the oral disintegrating films loaded with atenolol by solvent-casting method and to carry out its evaluation studies. Methods: The films were prepared using the film-forming hydrophilic polymer like hydroxypropyl methylcellulose (E-5) and super disintegrant like pectin in various proportions.The formulated oral films were characterized for Fourier transform infrared (FTIR) and morphological evaluations. Various physicochemical parameters such as weight variation, folding endurance, surface pH, in vitro disintegration, and in vitro dissolution studies were carried out. Results: FTIR studies revealed that there was no drug-polymer interaction. The morphological evaluation of films showed that all the films were homogenous and transparent. The folding endurance test ensured that the films had sufficient brittleness and by weight variation test, it was inferred that all the films were within the deviation. The surface pH study showed the pH of the films was around neutral pH. The drug was well distributed in all the films. The films disintegrated within 120 s and the fastest being disintegrated in 30 s. Based on all the evaluation parameters, F6 had shown optimal performance and remarkable increase in drug release of 94.38% in 2 min. Conclusion: Thus, formulated oral disintegrating films can be termed as an alternative approach to deliver atenolol.

Research Journal of Pharmacy and Technology, 2019

Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are t... more Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are the major constraints during the development of new product. Various approaches have been used for enhancement of solubility of poorly aqueous soluble drugs, but success of these approaches depends on physical and chemical nature of molecules being developed. Co-crystallization of drug substances offers a great opportunity for the development of new drug products with superior physicochemical properties such as melting point, flow ability, solubility, stability, bioavailability and permeability, while preserving the pharmacological properties of the active pharmaceutical ingredient. Co-crystals are multi-component systems in which two components, an active pharmaceutical ingredient and a co-former were present in different stichiomentric ratios and bonded together with non-covalent interactions in the crystal lattice. This review article presents a systematic overview of pharmaceutical co-crystals. Differences between co-crystals with salts, solvates and hydrates are summarized along with the advantages of co-crystals with examples. The theoretical parameters underlying the selection of co-formers and screening of co-crystals have been summarized and different methods of co-crystal formation and evaluation have been explained.

Introduction: To synthesize silver nitrate nanoparticles (AgNPs) using aqueous leaf extracts of L... more Introduction: To synthesize silver nitrate nanoparticles (AgNPs) using aqueous leaf extracts of Lantana camara as a reducing agent and evaluates its antimicrobial activity. Materials and Methods: L. camara extract acts both reducing agents as well as capping agent. Fourier-transform infrared (FT-IR) study was used for identifying the compounds responsible for the reduction of silver ions, the functional groups present in the plant extract. Various techniques used to characterize synthesized nanoparticles are dynamic light scattering, transmission electron microscopy (TEM), energy diffraction X-ray, and ultraviolet-visible (UV Vis) spectrophotometer were performed to characterize synthesized AgNPs. Results and Discussion: From the FTIR study, it was confirmed the presence of some functional groups capping the AgNPs. UV-Vis spectrophotometer showed an absorbance peak in the range of 436-446 nm. The average particle size of the prepared AgNPs was found to be 86 nm. In addition, the antimicrobial activity of prepared AgNPs was found to be higher than plain extract using various Grampositive and Gram-negative bacteria. Conclusions: From the results, it can be concluded that green synthesis of AgNPs from L. camera extract is easy, fast, one step, eco-friendly, and alternative conventional methods. The synthesized AgNP preparations from L. camara leaf extract show potential for application as broad-spectrum antimicrobial agents.

Objective: The objective of this work is to develop a precise, accurate and validated reverse pha... more Objective: The objective of this work is to develop a precise, accurate and validated reverse phase ultraperformance liquid chromatographic technique for effective simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation. Method: Separation of the selected drugs was optimized after several trials including changing mobile phase and its composition, stationary phase, flow rate, column temperature, etc. Finally the separation of drugs was achieved on BEH C18 column using a mixture of methanol and phosphate buffer having pH 3.5 in the ratio of 65:35 v/v as mobile phase with flow rate of 0.3 ml/min and the analytes were detected at a wavelength of 260 nm. Results: The developed method was validated by determining the parameters like linearity, system suitability, recovery, precision, specificity, robustness, ruggedness, LOD, and LOQ as per the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) guidelines. The system suitability parameters were within the limits, retention times (Rt) for Emtricitabine, Tenofovir and Efavirenz were found to be 0.432, 0.671, and 2.772 min respectively. The method showed linearity between the concentration range of 10-50 μg/ml for Emtricitabine (r 2 = 0.9987), 15-75 μg/ml for Tenofovir (r 2 = 0.9983) and 30-150 μg/ml for Efavirenz (r 2 = 0.9982). The percentage recovery results at 50%, 100% and 150% of Emtricitabine, Tenofovir and Efavirenz were found to be in the range of 99.45 %-100.15 %. Since there was no interference due to excipients and mobile phase, the method was found to be specific. The assay results of the combined tablet dosage form by the developed method were identified as in good agreement with the acceptance limit. Conclusions: The current method was proved to be effective for routine simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation.

Background: Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingr... more Background: Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are the major constraints during the development of new product Aim: The aim of the current work is to formulate and evaluate the Gabapentin co-crystals with various co formers like benzoic acid, salicylic acid and Tartaric acid. Method: Novel co-crystals in current study was prepared by using solvent drop method, co-grinding method and solvent evaporation method in stichiomentric ratio of 1:1. Co-crystals were characterized by standard calibration curve, FTIR, PXRD, flow properties, intrinsic solubility, dissolution rate and in vivo study. Results: The prepared multicomponent co-crystal formulations evaluated for saturation solubility analysis in case of pure Gabapentin showed 5.99 (mg/ml), GBP-TA CF showed high solubility values 13.52 folds solubility increases. The new crystalline forms are characterized by PXRD and NMR. Conclusion: The drug release profile high in GBP-BA CF (98.3%) at the end of 360 th minute while compared to other formulations. GBP-TA CF showed high regression value (0.998) and diffusion release exponent showed 0.792 so this formulation was selected as optimized formulation following non Fickian release mechanism, and selected for in vivo study. The percentage protection high in GBP-TA co crystal formulation dose of 10 mg/kg compared to other doses. The dose size decreases and percentage protection increasing showing greater control of toxicity.

Research journal of pharmacy and technology, Jul 29, 2022

The bronopol and kathon are chemical preservative which prevent degradation of milk samples and m... more The bronopol and kathon are chemical preservative which prevent degradation of milk samples and maintain authenticity in analysis. The detection is based on HPLC-UV-Vis spectroscopy, in which C 18 column (250 mm 9 4.6 mm, 5 lm) was used for chromatographic separations, with a mobile phase comprising 0.1% phosphoric acid in water: Methanol: 0.1% phosphoric acid in acetonitrile (80:10:10) at a flow rate 0.8 ml/min at ambient temperature and with the UV detection at 250 nm for bronopol and 274 nm for kathon. The retention time of bronopol, kathon (MI 2-methyl-4-isothiazolin-3-one) and kathon (CMI 5-chloro-2-methyl-4-isothiazolin-3-one) was 4.52 min, 3.98 min and 6.68 min respectively with a total run time of 10 min. The linearity of the method was satisfactory with regression coefficient (R 2) = 0.99. The limit of quantification was 72, 240, 390 mg L-1 for bronopol, kathon (MI) and kathon (CMI) respectively. Five spiked levels (62.5, 125, 250, 500 and 1000 mg L-1) were used to determine the recovery of bronopol, kathon (MI) and kathon (CMI) which was found to be 95.41 ± 11.84, 95.75 ± 8.21 and 92.22 ± 14.64% respectively, with relative standard deviations in the range 5.9-14.6%. The standardized analytical method was successfully used to rapidly detect bronopol and kathon in milk samples.

Research Journal of Pharmaceutical Dosage Forms and Technology, 2019

INDIAN DRUGS

5-Chloro-N-((2-oxo-3-(4-(3-oxomorpholino) phenyl) oxazolidin-5-yl) methyl) thiophene-2-carboxamid... more 5-Chloro-N-((2-oxo-3-(4-(3-oxomorpholino) phenyl) oxazolidin-5-yl) methyl) thiophene-2-carboxamide derivatives were synthesized in a simple and efficient approach using 2-(oxiran-2-ylmethyl) isoindoline-1, 3-dione, 4-(4-aminophenyl) morpholin-3-one, and 5-chlorothiophene-2-carbonyl chloride by stepwise synthesis. Three compounds 3, 4 and 7 were designed, prepared, and screened for anticancer activity against HeLa, MCF- 7, A-549 and K-562 and antibacterial activities against Gram +ve and Gram -ve strains. The carboxamide moieties proved to be capable for the development of new anticancer and anti-bacterial agents. Docking studies carried out on target receptors caspase-3 HeLa cell line and Staphylococcus aureus DNA-Gyrase also supported the anticancer and antimicrobial activity of compounds 3, 4 and 7

A gene (<i>PSTG2</i>) coding for a novel β-glucosidase belonging to glycoside hydrola... more A gene (<i>PSTG2</i>) coding for a novel β-glucosidase belonging to glycoside hydrolase family 3 was identified in the vicinity of the previously identified β-glucosidase gene [sesaminol triglucoside (STG)-hydrolyzing β-glucosidase, PSTG1] in the genome of <i>Paenibacillus</i> sp. strain KB0549. Compared with PSTG1, recombinant PSTG2 more specifically acted on the β-1,2-glucosidic linkage of the STG molecule to transiently accumulate a larger amount of 6-<i>O</i>-(β-D-glucopyranosyl)-β-D-glucopyranosylsesaminol.

EUROPEAN CHEMICAL BULLETIN, 2023

Nanosponges are small sponges where they reach the target site and stick to that surface and init... more Nanosponges are small sponges where they reach the target site and stick to that surface and initiate to release in a controlled manner they canalso be loaded with the various types ofmedications.Drugs loaded with Nanosponges improves their dissolution rate, solubility, rate of release, stability, reduces the frequency of dosing and improves bioavailability.
Nanosponges are mostly used in targeted drug delivery system. Drug delivery is the major problem faced in the pharmaceutical field from a long time by the invention ofNanosponge technology has become important step so that we can minimize some problems like poor solubility, poor stability and dosing frequency. The main advantage of this Nanosponge is it can be loaded by both hydrophilic and lipophilic drugs.The present review article is to discuss about the general introduction, composition of Nanosponges, drugs loaded with Nanosponges, different preparation techniques and evaluations methods for the Nanosponge tablets. Zeta potential, Fourier transform-infrared spectroscopy, determination of percentage yield, particle size analysis, porosity, invitro dissolution studies and entrapment efficiency by these characterizations we can know the inclusion complexes formed in between drug and Nanosponges, mainly lansoprazole loaded Nanosponges characterization parameters and evaluations are presented in this article.Nanosponges can deliver the drug through various routes like oral, topical, aerosol and parenteral administration.

Chromatographia

Since the stability of the pharmaceuticals plays a crucial role in efficacy and safety while usin... more Since the stability of the pharmaceuticals plays a crucial role in efficacy and safety while using them in the treatment of disorders, the evaluation of purity and impurity profiling of pharmaceuticals is of utmost importance using efficient analytical techniques. The present study explains the identification, isolation, and characterization of stress degradation products of the anti-human immunovirus drug Darunavir. The degradation study was performed to evaluate the stability profile of Darunavir in different stress conditions like hydrolytic, oxidative, thermal, and photolytic conditions as per the ICH guidelines. Degradation products were identified using ultra-performance liquid chromatography coupled with mass spectrometry, isolated using semi-preparative high-performance liquid chromatography, and structural characterization by HRMS and 1 H, 13 C NMR (1D, 2D). Darunavir is relatively stable in oxidative, thermal, and photolytic conditions; however, considerable degradation was observed in acid and base hydrolysis. A total of five degradation products were identified and isolated in acid and base degradation. DP-1, DP-2, & DP-3 were observed in acid conditions, whereas in base conditions, along with DP-2, two more DPs, i.e., DP-4 & DP-5, were identified. Among the five DPs, two degradation products, namely DP-1: N-(4-(N-(3-amino-2-hydroxy-4-phenylbutyl)-N-isobutylsulfamoyl) phenyl) acetimidamide. & DP-3: hexahydrofuro[2,3-b] furan-3-yl(4-((4-acetimidamido-N-isobutylphenyl)sulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate, are novel, remaining degradation products DP-2: 4-amino-N-(3-amino-2-hydroxy-4-phenylbutyl)-N-isobutylbenzenesulfonamide, DP-4: 4-amino-N-(((5S)-4-benzyl-2-oxooxazolidin-5-yl) methyl)-N-isobutyl benzenesulfonamide and DP-5: methyl ((3S)-4-((4amino-N-isobutylphenyl) sulfonamido)-3-hydroxy-1-phenylbutan-2-yl) carbamate are already reported tentatively using a single analytical technique coupled with mass analysis without any evidence from NMR and IR data. Hence, the present study focused on using High-Resolution Mass, 1D, and 2D 1 H, 13 C NMR data for concrete confirmation of structures for degradation products.

Journal of Pharmaceutical Negative Results, Oct 22, 2022

Background: Cocrystals are defined as multiple component structures whose components interact thr... more Background: Cocrystals are defined as multiple component structures whose components interact through non-covalent interactions. Cocrystals can enhance other essential properties of the APIs. Aim: The current research work focuses on formulating and evaluating novel co-crystals of Lamotrigine anti-epileptic drug (BCS-II) Methods: The Cocrystals of Lamotrigine drug with different cocrystals formers like Saccharin sodium, 4-Hydroxy benzoic acid, and Methyl paraben used with molar ratios (1:1) were prepared by solvent drop method, co-grinding method, and solvent evaporation method. Results: The results signify the establishment of intermolecular interaction within the cocrystals. In the novel cocrystals, Lamotrigine was determined to be engaged in the hydrogen bond interaction with the complementary functional groups of Saccharin sodium, 4-Hydroxy benzoic acid, and methyl paraben. Compared with the pure Lamotrigine flow properties for prepared co-crystal by using solvent evaporation method crystals are showing excellent flow properties. LTG-SAC CF I, LTG-HBA I, and LTG-MP III showed 49.6 folds, 7.4 folds, and 3.36 folds improved solubility respectively. The dissolution test showed that the LTG-SAC CF I, LTG-HBA I, and LTG-MP III cocrystals exhibited a 1.09-fold, 1.08-fold, and 1.07-fold higher dissolution rate than the pure Lamotrigine. Conclusions: LTG-SAC CF I, LTG-HBA I, and LTG-MP III cocrystals showed modification in the chemical environment, intermolecular interactions were established, improved flow properties with enhanced intrinsic solubility and in-vitro dissolution rate than pure drug.

Research Journal of Pharmacy and Technology

Objective: The objective of this work is to develop a precise, accurate and validated reverse pha... more Objective: The objective of this work is to develop a precise, accurate and validated reverse phase ultra-performance liquid chromatographic technique for effective simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation. Method: Separation of the selected drugs was optimized after several trials including changing mobile phase and its composition, stationary phase, flow rate, column temperature, etc. Finally the separation of drugs was achieved on BEH C18 column using a mixture of methanol and phosphate buffer having pH 3.5 in the ratio of 65:35 v/v as mobile phase with flow rate of 0.3 ml/min and the analytes were detected at a wavelength of 260 nm. Results: The developed method was validated by determining the parameters like linearity, system suitability, recovery, precision, specificity, robustness, ruggedness, LOD, and LOQ as per the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (...

Open access jounrals, Dec 14, 2020

Effect of sodium alginate in combination with natural and synthetic polymers on the release of ve... more Effect of sodium alginate in combination with natural and synthetic polymers on the release of verapamil hcl from its floating

International Journal of Research in Pharmaceutical Sciences, 2021

The goal of the research is to design and optimize Nebivolol Hydrochloride immediate-release tabl... more The goal of the research is to design and optimize Nebivolol Hydrochloride immediate-release tablet using response surface methodology. Nebivolol Hydrochloride immediate-release tablets used in the treatment of heart attacks, myocardial infarction. Response surface methodology calculations for this optimization study were performed utilizing Minitab 17. Different formulations of immediate-release were prepared by applying 2 factors 3 levels full factorial design using Minitab 17, which gave 9 formulations by using the wet granulation method. Independent variables like the amount of hydroxypropyl methylcellulose (X1), and microcrystalline cellulose (X2) and dependent variables like the per cent drug release at 45 minutes (Y1), disintegration (Y2) were selected for optimization. The prepared batches of Nebivolol Hydrochloride immediate-release tablets were evaluated for the pre-compression and post-compression parameters like weight variation, thickness, hardness, and friability, disi...

Effect of coformers on novel co-crystals of gabapentin: an in vivo approach - Drug readily crosse... more Effect of coformers on novel co-crystals of gabapentin: an in vivo approach - Drug readily crosses the blood-brain barrier

American Journal of Advanced Drug Delivery, 2013

Formulation research is oriented towards safety, efficacy and quick onset of action of existing d... more Formulation research is oriented towards safety, efficacy and quick onset of action of existing drug molecule through novel concepts of drug delivery. Orally disintegrating tablets of sumatriptan succinate were prepared by direct compression method to provide faster relief from pain to migraine sufferers. About twelve formulations for the present study were carried out based on 2 level 2 factor full factorial design for each set of superdisintegrants. Croscarmellose sodium, Crospovidone and Sodium starch glycolate (SSG) were used as superdisintegrants, while microcrystalline cellulose was used as diluent. The prepared batches of tablets were evaluated for weight variation, hardness, friability, wetting time, invitro dispersion time, drug content and invitro dissolution studies. The formulation containing combination of Croscarmellose sodium and Sodium starch glycolate showed rapid invitro dispersion time as compared to other formulations . The optimized formulation dispersed in 8 se...

Turkish Journal of Pharmaceutical Sciences, 2021

Biopharmaceutical Classification System (BCS) is an advanced tool utilised for classifying medici... more Biopharmaceutical Classification System (BCS) is an advanced tool utilised for classifying medicines based on dissolution, water solubility, and intestinal permeability, which affect the absorption of active pharmaceutical ingredients from immediate release solid oral forms. It is useful to the formulation researcher to develop novel dosage forms based on modernistic rather than experimental approaches. The current review focuses on the fundamentals, objectives, guidance of BCS, characteristics of BCS drugs, their importance and applications of BCS. This review explains the challenges in drug development in terms of solubility and in vivo disposition. In the current review, new strategies for improving BCS II drug solubility as well as biopharmaceutical drug disposition properties which are utilised throughout the early stages of drug development and commercialisation are mainly discussed.

Research Journal of Pharmaceutical Dosage Forms and Technology, 2019

Objective: The main objective of the study was to formulate the oral disintegrating films loaded ... more Objective: The main objective of the study was to formulate the oral disintegrating films loaded with atenolol by solvent-casting method and to carry out its evaluation studies. Methods: The films were prepared using the film-forming hydrophilic polymer like hydroxypropyl methylcellulose (E-5) and super disintegrant like pectin in various proportions.The formulated oral films were characterized for Fourier transform infrared (FTIR) and morphological evaluations. Various physicochemical parameters such as weight variation, folding endurance, surface pH, in vitro disintegration, and in vitro dissolution studies were carried out. Results: FTIR studies revealed that there was no drug-polymer interaction. The morphological evaluation of films showed that all the films were homogenous and transparent. The folding endurance test ensured that the films had sufficient brittleness and by weight variation test, it was inferred that all the films were within the deviation. The surface pH study showed the pH of the films was around neutral pH. The drug was well distributed in all the films. The films disintegrated within 120 s and the fastest being disintegrated in 30 s. Based on all the evaluation parameters, F6 had shown optimal performance and remarkable increase in drug release of 94.38% in 2 min. Conclusion: Thus, formulated oral disintegrating films can be termed as an alternative approach to deliver atenolol.

Research Journal of Pharmacy and Technology, 2019

Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are t... more Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are the major constraints during the development of new product. Various approaches have been used for enhancement of solubility of poorly aqueous soluble drugs, but success of these approaches depends on physical and chemical nature of molecules being developed. Co-crystallization of drug substances offers a great opportunity for the development of new drug products with superior physicochemical properties such as melting point, flow ability, solubility, stability, bioavailability and permeability, while preserving the pharmacological properties of the active pharmaceutical ingredient. Co-crystals are multi-component systems in which two components, an active pharmaceutical ingredient and a co-former were present in different stichiomentric ratios and bonded together with non-covalent interactions in the crystal lattice. This review article presents a systematic overview of pharmaceutical co-crystals. Differences between co-crystals with salts, solvates and hydrates are summarized along with the advantages of co-crystals with examples. The theoretical parameters underlying the selection of co-formers and screening of co-crystals have been summarized and different methods of co-crystal formation and evaluation have been explained.

Introduction: To synthesize silver nitrate nanoparticles (AgNPs) using aqueous leaf extracts of L... more Introduction: To synthesize silver nitrate nanoparticles (AgNPs) using aqueous leaf extracts of Lantana camara as a reducing agent and evaluates its antimicrobial activity. Materials and Methods: L. camara extract acts both reducing agents as well as capping agent. Fourier-transform infrared (FT-IR) study was used for identifying the compounds responsible for the reduction of silver ions, the functional groups present in the plant extract. Various techniques used to characterize synthesized nanoparticles are dynamic light scattering, transmission electron microscopy (TEM), energy diffraction X-ray, and ultraviolet-visible (UV Vis) spectrophotometer were performed to characterize synthesized AgNPs. Results and Discussion: From the FTIR study, it was confirmed the presence of some functional groups capping the AgNPs. UV-Vis spectrophotometer showed an absorbance peak in the range of 436-446 nm. The average particle size of the prepared AgNPs was found to be 86 nm. In addition, the antimicrobial activity of prepared AgNPs was found to be higher than plain extract using various Grampositive and Gram-negative bacteria. Conclusions: From the results, it can be concluded that green synthesis of AgNPs from L. camera extract is easy, fast, one step, eco-friendly, and alternative conventional methods. The synthesized AgNP preparations from L. camara leaf extract show potential for application as broad-spectrum antimicrobial agents.

Objective: The objective of this work is to develop a precise, accurate and validated reverse pha... more Objective: The objective of this work is to develop a precise, accurate and validated reverse phase ultraperformance liquid chromatographic technique for effective simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation. Method: Separation of the selected drugs was optimized after several trials including changing mobile phase and its composition, stationary phase, flow rate, column temperature, etc. Finally the separation of drugs was achieved on BEH C18 column using a mixture of methanol and phosphate buffer having pH 3.5 in the ratio of 65:35 v/v as mobile phase with flow rate of 0.3 ml/min and the analytes were detected at a wavelength of 260 nm. Results: The developed method was validated by determining the parameters like linearity, system suitability, recovery, precision, specificity, robustness, ruggedness, LOD, and LOQ as per the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use (ICH) guidelines. The system suitability parameters were within the limits, retention times (Rt) for Emtricitabine, Tenofovir and Efavirenz were found to be 0.432, 0.671, and 2.772 min respectively. The method showed linearity between the concentration range of 10-50 μg/ml for Emtricitabine (r 2 = 0.9987), 15-75 μg/ml for Tenofovir (r 2 = 0.9983) and 30-150 μg/ml for Efavirenz (r 2 = 0.9982). The percentage recovery results at 50%, 100% and 150% of Emtricitabine, Tenofovir and Efavirenz were found to be in the range of 99.45 %-100.15 %. Since there was no interference due to excipients and mobile phase, the method was found to be specific. The assay results of the combined tablet dosage form by the developed method were identified as in good agreement with the acceptance limit. Conclusions: The current method was proved to be effective for routine simultaneous determination of Emtricitabine, Tenofovir and Efavirenz in bulk and tablet formulation.

Background: Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingr... more Background: Poor aqueous solubility and low oral bioavailability of an active pharmaceutical ingredient are the major constraints during the development of new product Aim: The aim of the current work is to formulate and evaluate the Gabapentin co-crystals with various co formers like benzoic acid, salicylic acid and Tartaric acid. Method: Novel co-crystals in current study was prepared by using solvent drop method, co-grinding method and solvent evaporation method in stichiomentric ratio of 1:1. Co-crystals were characterized by standard calibration curve, FTIR, PXRD, flow properties, intrinsic solubility, dissolution rate and in vivo study. Results: The prepared multicomponent co-crystal formulations evaluated for saturation solubility analysis in case of pure Gabapentin showed 5.99 (mg/ml), GBP-TA CF showed high solubility values 13.52 folds solubility increases. The new crystalline forms are characterized by PXRD and NMR. Conclusion: The drug release profile high in GBP-BA CF (98.3%) at the end of 360 th minute while compared to other formulations. GBP-TA CF showed high regression value (0.998) and diffusion release exponent showed 0.792 so this formulation was selected as optimized formulation following non Fickian release mechanism, and selected for in vivo study. The percentage protection high in GBP-TA co crystal formulation dose of 10 mg/kg compared to other doses. The dose size decreases and percentage protection increasing showing greater control of toxicity.