Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150301
Twinkle Tarole, P. Daroi, V. Munipalli, Sayali Warde, Raman S Singh, Anindita Nandi, Vaidun Bhaskar
In recent years much more attention has gained by antiviral drugs because of severe acute respiratory syndrome coronavirus-2 (SARS-CoV) infection. Molnupiravir is one of the favorable drugs for SARS-CoV-2 treatment. The present study aimed to develop and validate a simple, rapid, stable, selective, sensitive, accurate, robust, and economical RP-HPLC method for determining molnupiravir in its capsule dosage form. The chromatographic separation was achieved on inert sustain C18 column (250 mm x 4.6 mm x 5 μ) at 40°. Isocratic elution was performed with 25 mM KH2PO4 buffer (pH 3.0) and methanol (60:40 v/v) as mobile phase at flow rate of 1.0 mL/min with 50 μL injection volume. The detection was conceded out at 242 nm. The developed RP-HPLC method yielded a suitable retention time of 4.2 minutes for molnupiravir. The developed method was validated according to the International Council on Harmonization (ICH) guidelines and established to be linear in the range of 10 to 70 μg/mL with a linear regression coefficient of 0.9993. The %RSD for the method precision and system precision was found to be less than 2.0%. The %assay of the formulation is 101.52%. The LoD and LoQ were found to be 0.25 and 0.75 μg/mL, respectively. The specificity of the method established using forced degradation studies in which the drug is subjected to the stressed conditions such as thermal, acidic, basic oxidative and photolytic degradation. The developed and validated RP-HPLC method for molnupiravir takes short time and can be used for routine quality analysis of marketed Molnupiravir in capsule dosage form.
近年来，由于严重急性呼吸系统综合征冠状病毒-2（SARS-CoV）感染，抗病毒药物受到越来越多的关注。莫仑匹韦是治疗 SARS-CoV-2 的首选药物之一。本研究旨在开发并验证一种简单、快速、稳定、选择性强、灵敏、准确、稳健且经济的 RP-HPLC 方法，用于测定胶囊剂中的莫仑吡韦。色谱分离采用惰性C18色谱柱（250 mm x 4.6 mm x 5 μ），柱温40°。以 25 mM KH2PO4 缓冲溶液（pH 3.0）和甲醇（60:40 v/v）为流动相进行等度洗脱，流速为 1.0 mL/min，进样量为 50 μL。检测波长为 242 nm。所建立的RP-HPLC方法的molnupiravir保留时间为4.2分钟。根据国际协调理事会（ICH）指南对所开发的方法进行了验证，结果表明该方法在 10 至 70 μg/mL 范围内线性关系良好，线性回归系数为 0.9993。方法精密度和系统精密度的 %RSD 均小于 2.0%。制剂的检测率为 101.52%。LoD 和 LoQ 分别为 0.25 和 0.75 μg/mL。该方法的特异性是通过强制降解研究确定的，在强制降解研究中，药物会受到热降解、酸性降解、碱性氧化降解和光解降解等压力条件的影响。所开发和验证的 RP-HPLC 法测定莫仑匹拉韦所需时间短，可用于市场上胶囊剂型莫仑匹拉韦的常规质量分析。
{"title":"Stability Indicating RP-HPLC Method Development for the Estimation of Molnupiravir in Capsule Dosage Form","authors":"Twinkle Tarole, P. Daroi, V. Munipalli, Sayali Warde, Raman S Singh, Anindita Nandi, Vaidun Bhaskar","doi":"10.25004/ijpsdr.2023.150301","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150301","url":null,"abstract":"In recent years much more attention has gained by antiviral drugs because of severe acute respiratory syndrome coronavirus-2 (SARS-CoV) infection. Molnupiravir is one of the favorable drugs for SARS-CoV-2 treatment. The present study aimed to develop and validate a simple, rapid, stable, selective, sensitive, accurate, robust, and economical RP-HPLC method for determining molnupiravir in its capsule dosage form. The chromatographic separation was achieved on inert sustain C18 column (250 mm x 4.6 mm x 5 μ) at 40°. Isocratic elution was performed with 25 mM KH2PO4 buffer (pH 3.0) and methanol (60:40 v/v) as mobile phase at flow rate of 1.0 mL/min with 50 μL injection volume. The detection was conceded out at 242 nm. The developed RP-HPLC method yielded a suitable retention time of 4.2 minutes for molnupiravir. The developed method was validated according to the International Council on Harmonization (ICH) guidelines and established to be linear in the range of 10 to 70 μg/mL with a linear regression coefficient of 0.9993. The %RSD for the method precision and system precision was found to be less than 2.0%. The %assay of the formulation is 101.52%. The LoD and LoQ were found to be 0.25 and 0.75 μg/mL, respectively. The specificity of the method established using forced degradation studies in which the drug is subjected to the stressed conditions such as thermal, acidic, basic oxidative and photolytic degradation. The developed and validated RP-HPLC method for molnupiravir takes short time and can be used for routine quality analysis of marketed Molnupiravir in capsule dosage form.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139367462","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150304
Parul A. Ittadwar, P. Puranik
Famotidine is an H2 receptor antagonist belonging to the BCS Class II, characterized by low solubility and limited oral bioavailability. The current study encompasses the formulation of novel famotidine phospholipid complex (FHC) with the aid of design of experiments (Central Composite Design) using solvent evaporation technique to overcome the disadvantages of Famotidine. To further enhance the physicochemical properties of FHC, it was incorporated into gastro-retentive floating tablets (GRDDS) using direct compression technique with sodium bicarbonate as a gas generating agent and its properties were compared to famotidine floating tablets. The pre-compression parameters, namely bulk density, tapped density, Hausner’s ratio, Carr’s compressibility index and angle of repose were evaluated. The flow properties of FHC granules were found to be better than the plain famotidine granules. The postcompression parameters, namely thickness, hardness, friability, weight variation, drug content and swelling index showed better results for FHC as compared to famotidine floating tablets. In-vitro buoyancy study indicated that the floating lag time for FHC tablets (110 ± 0.021 seconds) was higher than famotidine tablets (36 ± 0.033 seconds) owing to the higher molecular weight of phosphatidylcholine. But the total floating time for FHC tablets was found to be more than 18 hours and for famotidine tablets it was ~12 hours, indicating the improved residence time and buoyancy. The in-vitro dissolution study depicted that the cumulative release for FHC tablets (99.84 ± 0.058%) was enhanced 1.07 fold than Famotidine tablets (92.73 ± 0.028%) and 1.6 fold than marketed tablet, Famocid (62.24 ± 0.023%). When kinetic modeling was performed, famotidine tablet followed zero order kinetics, whereas FHC tablet followed Higuchi model indicating a modified and sustained release pattern. The statistical analysis for %cumulative release performed using ANOVA and Dunnett’s test showed the p-value to be below 0.05 (0.0043) indicating that the analysis model was significant. An accelerated stability study was performed for a period of 6 months at 25 ± 2°C; 60 ± 5% RH. FHC tablets showed a better stability profile than famotidine tablets. In conclusion, FHC gastro-retentive floating tablets showed improved flow properties, post compression properties, better drug content, improved in-vitro buoyancy and enhanced cumulative release and stability profile.
{"title":"Formulation and Evaluation of Gastro-retentive Drug Delivery System of Novel Famotidine Phospholipid Complex","authors":"Parul A. Ittadwar, P. Puranik","doi":"10.25004/ijpsdr.2023.150304","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150304","url":null,"abstract":"Famotidine is an H2 receptor antagonist belonging to the BCS Class II, characterized by low solubility and limited oral bioavailability. The current study encompasses the formulation of novel famotidine phospholipid complex (FHC) with the aid of design of experiments (Central Composite Design) using solvent evaporation technique to overcome the disadvantages of Famotidine. To further enhance the physicochemical properties of FHC, it was incorporated into gastro-retentive floating tablets (GRDDS) using direct compression technique with sodium bicarbonate as a gas generating agent and its properties were compared to famotidine floating tablets. The pre-compression parameters, namely bulk density, tapped density, Hausner’s ratio, Carr’s compressibility index and angle of repose were evaluated. The flow properties of FHC granules were found to be better than the plain famotidine granules. The postcompression parameters, namely thickness, hardness, friability, weight variation, drug content and swelling index showed better results for FHC as compared to famotidine floating tablets. In-vitro buoyancy study indicated that the floating lag time for FHC tablets (110 ± 0.021 seconds) was higher than famotidine tablets (36 ± 0.033 seconds) owing to the higher molecular weight of phosphatidylcholine. But the total floating time for FHC tablets was found to be more than 18 hours and for famotidine tablets it was ~12 hours, indicating the improved residence time and buoyancy. The in-vitro dissolution study depicted that the cumulative release for FHC tablets (99.84 ± 0.058%) was enhanced 1.07 fold than Famotidine tablets (92.73 ± 0.028%) and 1.6 fold than marketed tablet, Famocid (62.24 ± 0.023%). When kinetic modeling was performed, famotidine tablet followed zero order kinetics, whereas FHC tablet followed Higuchi model indicating a modified and sustained release pattern. The statistical analysis for %cumulative release performed using ANOVA and Dunnett’s test showed the p-value to be below 0.05 (0.0043) indicating that the analysis model was significant. An accelerated stability study was performed for a period of 6 months at 25 ± 2°C; 60 ± 5% RH. FHC tablets showed a better stability profile than famotidine tablets. In conclusion, FHC gastro-retentive floating tablets showed improved flow properties, post compression properties, better drug content, improved in-vitro buoyancy and enhanced cumulative release and stability profile.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139366396","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150320
Sushma Pallekona, A.K Pawar, Divya Molleti
This research describes a novel technique for the selective separation of degradants from API employing HPLC and online coupling of a triple quadrupole mass analyzer and PDA detector with a SCIEX QTRAP 5500 mass spectrometer. Chromatography was used to separate all degradants on the column Agilent eclipse XDB (150 mm x 4.6 mm, 3.5 μ) with mobile phase ACN: 0.1% TEA (40:60) %v/v. The highest absorption was found to occur at 220 nm, which allows for simultaneous detection without being impacted by the placebo matrix. According to the general ICH recommendations, the suggested RP-HPLC method was accepted. All of the metrics- specificity, linearity, LoD, LoQ, accuracy, precision and robustness of validation were deemed sufficient. The proposed method exhibits strong correlation and great linearity over the range of (12.5–75 μg/mL). The accuracy trials produced consistent recoveries (95–105%), while the precision experiments' percent RSD was less than 2%. The intrinsic stability of the drug molecules in the current formulation could be ascertained by conducting forced degradation studies to assess the degradation products produced under various stress settings. The degradants produced were well separated and further characterized by MS/MS studies. The newly devised approach was demonstrated to be stable and sensitive to all degradants during validation tests. Validation trials demonstrate that the newly developed method was also accurate, precise, resilient, selective, and linear within the necessary operating range.
{"title":"Selective Separation and Mass Spectral Characterization of Degradants in Viloxazine by LC-MS/MS","authors":"Sushma Pallekona, A.K Pawar, Divya Molleti","doi":"10.25004/ijpsdr.2023.150320","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150320","url":null,"abstract":"This research describes a novel technique for the selective separation of degradants from API employing HPLC and online coupling of a triple quadrupole mass analyzer and PDA detector with a SCIEX QTRAP 5500 mass spectrometer. Chromatography was used to separate all degradants on the column Agilent eclipse XDB (150 mm x 4.6 mm, 3.5 μ) with mobile phase ACN: 0.1% TEA (40:60) %v/v. The highest absorption was found to occur at 220 nm, which allows for simultaneous detection without being impacted by the placebo matrix. According to the general ICH recommendations, the suggested RP-HPLC method was accepted. All of the metrics- specificity, linearity, LoD, LoQ, accuracy, precision and robustness of validation were deemed sufficient. The proposed method exhibits strong correlation and great linearity over the range of (12.5–75 μg/mL). The accuracy trials produced consistent recoveries (95–105%), while the precision experiments' percent RSD was less than 2%. The intrinsic stability of the drug molecules in the current formulation could be ascertained by conducting forced degradation studies to assess the degradation products produced under various stress settings. The degradants produced were well separated and further characterized by MS/MS studies. The newly devised approach was demonstrated to be stable and sensitive to all degradants during validation tests. Validation trials demonstrate that the newly developed method was also accurate, precise, resilient, selective, and linear within the necessary operating range.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139367497","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150318
Rajendra R Khade, S. Butle
Lumefantrine low/variable bioavailability with low aqueous solubility is associated with their crystallinity and P-glycoprotein (P-gp) mediated efflux. Herein, to improve the dissolution and hence the oral bioavailability, amorphous solid dispersions (SD) of lumefantrine (LUMF) containing piperine (PIP), a P-gp and CYP3A4 inhibitor, were prepared with Copovidone/Kollidon® VA 64 (KOL) at three different ratios with increasing content of the polymer. The PIP-LUMF-KOL SD at ratio of 1:6:18 demonstrated higher aqueous solubility of LUMF and hence were characterized by DSC, FTIR and XRD. The improved dissolution resulting due to loss of crystallinity of LUMF was confirmed by DSC thermogram and XRD diffractogram of LUMF-PIP-SD while FTIR studies investigated the possible intermolecular interactions between LUMF and PIP and /or KOL. DSC and dissolution experiments validated the stability of LUMFPIP- Sol SD for 90 days under stressed humidity and temperature conditions. Overall, the data suggest that the SD of LUMF incorporated with P-gp inhibitor PIP, enhances dissolution and hence could improve the bioavailability of LUMF.
{"title":"Formulation Development and Characterization of Lumefantrine Solid Dispersion with Piperine for Solubility Enhancement","authors":"Rajendra R Khade, S. Butle","doi":"10.25004/ijpsdr.2023.150318","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150318","url":null,"abstract":"Lumefantrine low/variable bioavailability with low aqueous solubility is associated with their crystallinity and P-glycoprotein (P-gp) mediated efflux. Herein, to improve the dissolution and hence the oral bioavailability, amorphous solid dispersions (SD) of lumefantrine (LUMF) containing piperine (PIP), a P-gp and CYP3A4 inhibitor, were prepared with Copovidone/Kollidon® VA 64 (KOL) at three different ratios with increasing content of the polymer. The PIP-LUMF-KOL SD at ratio of 1:6:18 demonstrated higher aqueous solubility of LUMF and hence were characterized by DSC, FTIR and XRD. The improved dissolution resulting due to loss of crystallinity of LUMF was confirmed by DSC thermogram and XRD diffractogram of LUMF-PIP-SD while FTIR studies investigated the possible intermolecular interactions between LUMF and PIP and /or KOL. DSC and dissolution experiments validated the stability of LUMFPIP- Sol SD for 90 days under stressed humidity and temperature conditions. Overall, the data suggest that the SD of LUMF incorporated with P-gp inhibitor PIP, enhances dissolution and hence could improve the bioavailability of LUMF.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139367627","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
According to earlier research, using niosomes as drug carriers, particularly for antifungal drugs, produces greater results than using alternative carriers. Niosomes has the capacity to encapsulate both hydrophilic and hydrophobic pharmaceuticals, as well as their prolonged stability in circulation. This work aimed to prepare and evaluate luliconazole niosomal gel for antifungal activity. In this study, niosomes containing luliconazole were prepared by thin film hydration technique using non-ionic surfactant (Span 60 and Tween 80) and cholesterol at different concentrations. The prepared formulations were evaluated for optical microscopy, drug entrapment efficiency, drug content, in-vitro drug release study, and stability studies. The ratio 2:1 of span 60 and cholesterol showed better results. Hence it was optimized as the final vesicle formulation. The FTIR study concluded there was no interaction between Luliconazole and any of the excipients. The niosomes gel was evaluated for various parameters of all the formulations. The 1% Carbopol 934 gel shows the best and most promising results. The niosomal gel formulation could be a useful dosage form to increase efficacy by the transdermal route. The potential of a secure and efficient therapy for difficult clinical applications is made possible by the development of niosomes with target specificity. Therefore, niosomes gel may be considered the best vesicular carrier for the effective delivery of luliconazole through the skin.
{"title":"DEVELOPMENT AND EVALUATION OF LULICNAZOLE NIOSOMAL TRANSDERMAL DRUG DELIVERY SYSTEM","authors":"Manasi Patharwat, Rani Ghosalkar, Kedar Bavaskar, Ashish Jain","doi":"10.25004/ijpsdr.2023.150312","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150312","url":null,"abstract":"According to earlier research, using niosomes as drug carriers, particularly for antifungal drugs, produces greater results than using alternative carriers. Niosomes has the capacity to encapsulate both hydrophilic and hydrophobic pharmaceuticals, as well as their prolonged stability in circulation. This work aimed to prepare and evaluate luliconazole niosomal gel for antifungal activity. In this study, niosomes containing luliconazole were prepared by thin film hydration technique using non-ionic surfactant (Span 60 and Tween 80) and cholesterol at different concentrations. The prepared formulations were evaluated for optical microscopy, drug entrapment efficiency, drug content, in-vitro drug release study, and stability studies. The ratio 2:1 of span 60 and cholesterol showed better results. Hence it was optimized as the final vesicle formulation. The FTIR study concluded there was no interaction between Luliconazole and any of the excipients. The niosomes gel was evaluated for various parameters of all the formulations. The 1% Carbopol 934 gel shows the best and most promising results. The niosomal gel formulation could be a useful dosage form to increase efficacy by the transdermal route. The potential of a secure and efficient therapy for difficult clinical applications is made possible by the development of niosomes with target specificity. Therefore, niosomes gel may be considered the best vesicular carrier for the effective delivery of luliconazole through the skin.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139367781","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150311
M. Gambhire, V. Gambhire, Abhijit Kulkarni, R. Dolas, Anuja Mulay, Manali Bhide
In the present study, metformin hydrochloride-loaded microspheres were prepared for filling into the periodontal pockets with or without grafts for the treatment of periodontitis. For this purpose, chitosan was chosen as a polymer and used at different drug/polymer ratios in the preparation of microspheres by emulsion cross-linking method. Optimization was carried out by implementing a three-factor, three-level Box–Behnken design. Mathematical models were generated by regression analysis for responses of particle size (PS) and entrapment efficiency (EE). The experimental design took into account the preparation of optimized formulation with maximum %EE and minimum PS at optimum process conditions for the microsphere formulation by reducing chemical use and formulation time, in an economical way. The optimized formulation was selected on the basis of the desirability function and was further evaluated with respect to the particle size, entrapment efficiency, in-vitro drug release, differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectroscopy and surface morphology studies. The results of release studies were evaluated kinetically and statistically. Particle size and entrapment efficiency of the selected batch were found to be in the range of 40.2 to 59.6 μm and 85 to 95%, respectively. The DSC studies revealed molecular dispersion and conversion of the drug into an amorphous form. Surface morphology of microspheres was analyzed by scanning electron microscopy (SEM) and found to be spherical in shape with a smooth surface. The mean particle size, EE, and in-vitro drug release of the optimized batch were found to be 51.4 ± 4.8 μm, 96.5 ± 1.42%, and 79.8 ± 3.1%, respectively. The release kinetics showed that the release followed the Peppas model, and the main mechanism of drug release was diffusion. These sustained-release chitosan microspheres could be a promising drug delivery system for local delivery of metformin hydrochloride in the treatment of periodontitis.
{"title":"Design, Optimization and Characterization of Metformin Hydrochloride Loaded Biodegradable Microspheres using Box Behnken design for Local Delivery in Periodontitis","authors":"M. Gambhire, V. Gambhire, Abhijit Kulkarni, R. Dolas, Anuja Mulay, Manali Bhide","doi":"10.25004/ijpsdr.2023.150311","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150311","url":null,"abstract":"In the present study, metformin hydrochloride-loaded microspheres were prepared for filling into the periodontal pockets with or without grafts for the treatment of periodontitis. For this purpose, chitosan was chosen as a polymer and used at different drug/polymer ratios in the preparation of microspheres by emulsion cross-linking method. Optimization was carried out by implementing a three-factor, three-level Box–Behnken design. Mathematical models were generated by regression analysis for responses of particle size (PS) and entrapment efficiency (EE). The experimental design took into account the preparation of optimized formulation with maximum %EE and minimum PS at optimum process conditions for the microsphere formulation by reducing chemical use and formulation time, in an economical way. The optimized formulation was selected on the basis of the desirability function and was further evaluated with respect to the particle size, entrapment efficiency, in-vitro drug release, differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectroscopy and surface morphology studies. The results of release studies were evaluated kinetically and statistically. Particle size and entrapment efficiency of the selected batch were found to be in the range of 40.2 to 59.6 μm and 85 to 95%, respectively. The DSC studies revealed molecular dispersion and conversion of the drug into an amorphous form. Surface morphology of microspheres was analyzed by scanning electron microscopy (SEM) and found to be spherical in shape with a smooth surface. The mean particle size, EE, and in-vitro drug release of the optimized batch were found to be 51.4 ± 4.8 μm, 96.5 ± 1.42%, and 79.8 ± 3.1%, respectively. The release kinetics showed that the release followed the Peppas model, and the main mechanism of drug release was diffusion. These sustained-release chitosan microspheres could be a promising drug delivery system for local delivery of metformin hydrochloride in the treatment of periodontitis.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139366349","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150315
D. Ashokan, K. Rajathi
Members of the quinoline family include several alkaloids. Alkaloids are found in foods and beverages that humans consume daily and in various stimulants. Among many other activities, they act against inflammation, cancer, bacteria, fungi and pain. Modifications of the alkyl chain after N-alkylation can alter the physicochemical properties and affect its multifunctional properties. This article describes the preparation and structural identification of five quinolinium sulfonamide ionic liquids that differ in N-alkylation functional group and chain length. Functional group and alkyl chain length in the N-alkylation of ionic liquids of quinolinium sulfonamide ionic liquids significantly affected the antioxidant activity and C-1 showed the highest antioxidant activity with the lowest IC50 of 20.56. Variation of substituents in the N-alkylation of ionic liquids of quinolinium sulfonamide also significantly affected its antibacterial and antifungus activity, with C-1 exhibiting the greatest activity. In addition, experimental results indicate that quinolinium sulfonamide ionic liquids significantly prolong normal human plasma’s prothrombin time (PT).
{"title":"Synthesis, Structural Identification and Biological Potencies of Quinolinium Sulfonamide Ionic Liquids","authors":"D. Ashokan, K. Rajathi","doi":"10.25004/ijpsdr.2023.150315","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150315","url":null,"abstract":"Members of the quinoline family include several alkaloids. Alkaloids are found in foods and beverages that humans consume daily and in various stimulants. Among many other activities, they act against inflammation, cancer, bacteria, fungi and pain. Modifications of the alkyl chain after N-alkylation can alter the physicochemical properties and affect its multifunctional properties. This article describes the preparation and structural identification of five quinolinium sulfonamide ionic liquids that differ in N-alkylation functional group and chain length. Functional group and alkyl chain length in the N-alkylation of ionic liquids of quinolinium sulfonamide ionic liquids significantly affected the antioxidant activity and C-1 showed the highest antioxidant activity with the lowest IC50 of 20.56. Variation of substituents in the N-alkylation of ionic liquids of quinolinium sulfonamide also significantly affected its antibacterial and antifungus activity, with C-1 exhibiting the greatest activity. In addition, experimental results indicate that quinolinium sulfonamide ionic liquids significantly prolong normal human plasma’s prothrombin time (PT).","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139367116","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150314
Pooja A Kansagara, D.J. Pandya
Each year, tons of weeds are burned or allowed to dry throughout the world. Despite folklore claims that Commelina benghalensis can treat leprosy, fever, snake bites, jaundice, sore throats, headaches, and constipation in both humans and animals, the ubiquitous Indian plant always dies the same way every year. By creating a formulation based on the evaluation of its potential ethnomedicinal properties, the current work attempts to utilize this weed. The complete plant was extracted once at a time using solvents with increasing polarity. Each extract’s anti-ulcer and laxative efficacy was investigated using appropriate animal models. The ethnomedicinal claims of the plant were supported by the discovery that the methanolic extract was the most bioactive, followed by the aqueous extract. Important classes of phytoconstituents such as phenolics, alkaloids, saponins, steroids&triterpenoids, flavonoids, and carbohydrates were found by phytochemical screening. From the purified fraction of the most bioactive extract, many chemicals, including stigmasterol and β-sitosterol, were discovered using GC-MS. Using TLC experiments and HPTLC, a chromatographic fingerprint was created. Effervescent granules of the methanolic extract were created and tested on animal models in order to bring the research to the public for their benefit. They were found to be effective as an anti-ulcer and laxative, which was compatible with our goal to create a “Best from Waste” product.
{"title":"Best from Waste: Bioactivity-guided Formulation Development from a Common Weed - Commelina benghalensis","authors":"Pooja A Kansagara, D.J. Pandya","doi":"10.25004/ijpsdr.2023.150314","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150314","url":null,"abstract":"Each year, tons of weeds are burned or allowed to dry throughout the world. Despite folklore claims that Commelina benghalensis can treat leprosy, fever, snake bites, jaundice, sore throats, headaches, and constipation in both humans and animals, the ubiquitous Indian plant always dies the same way every year. By creating a formulation based on the evaluation of its potential ethnomedicinal properties, the current work attempts to utilize this weed. The complete plant was extracted once at a time using solvents with increasing polarity. Each extract’s anti-ulcer and laxative efficacy was investigated using appropriate animal models. The ethnomedicinal claims of the plant were supported by the discovery that the methanolic extract was the most bioactive, followed by the aqueous extract. Important classes of phytoconstituents such as phenolics, alkaloids, saponins, steroids&triterpenoids, flavonoids, and carbohydrates were found by phytochemical screening. From the purified fraction of the most bioactive extract, many chemicals, including stigmasterol and β-sitosterol, were discovered using GC-MS. Using TLC experiments and HPTLC, a chromatographic fingerprint was created. Effervescent granules of the methanolic extract were created and tested on animal models in order to bring the research to the public for their benefit. They were found to be effective as an anti-ulcer and laxative, which was compatible with our goal to create a “Best from Waste” product.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139366486","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150317
Moussa Koné, Hermann N Guessan, A. J. N’gouan, Frederica M-Koblavi, E. Megnassan
Through structure-based molecular design, we virtually design new subnanomolar range antimalarial, inhibitors of Plasmodium falciparum M17 aminopeptidase (PfA-M17). We developed the complexation QSAR models from hydroxamic acid derivatives (HDA). A linear correlation was established between the computed Gibbs free energies of binding (GFE: ΔΔGcom) and observed enzyme inhibition constants (Ki exp) for each training set pKi exp = , R2 = 0.97. The predictive power of the QSAR model was validated with 3D-QSAR pharmacophore generation (PH4): pKi exp = 0.707×pKi pred − 2.5182, R2 = 0.89. We then conducted a study on catalytic residues to exploit the different interactions (enzyme: inhibitor). Structural information from the models guided us in designing a virtual combinatorial library (VCL) of more than 56 thousand HDAs. The PH4 screening retained 48 new and potent HDAs with predicted inhibitory potencies pKi pre up to 73 times lower than that of HDA1 (pKi exp = 2.5 nM). Combining molecular modeling and PH4 in-silico screening of the VCL resulted in the proposed novel potent antimalarial agent candidates with favorable pharmacokinetic profiles.
{"title":"Computer-aided Design of New Hydroxamic Acid Derivatives Targeting the Plasmodium falciparum M17 Metallo-aminopeptidase with Favorable Pharmacokinetic Profile","authors":"Moussa Koné, Hermann N Guessan, A. J. N’gouan, Frederica M-Koblavi, E. Megnassan","doi":"10.25004/ijpsdr.2023.150317","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150317","url":null,"abstract":"Through structure-based molecular design, we virtually design new subnanomolar range antimalarial, inhibitors of Plasmodium falciparum M17 aminopeptidase (PfA-M17). We developed the complexation QSAR models from hydroxamic acid derivatives (HDA). A linear correlation was established between the computed Gibbs free energies of binding (GFE: ΔΔGcom) and observed enzyme inhibition constants (Ki exp) for each training set pKi exp = , R2 = 0.97. The predictive power of the QSAR model was validated with 3D-QSAR pharmacophore generation (PH4): pKi exp = 0.707×pKi pred − 2.5182, R2 = 0.89. We then conducted a study on catalytic residues to exploit the different interactions (enzyme: inhibitor). Structural information from the models guided us in designing a virtual combinatorial library (VCL) of more than 56 thousand HDAs. The PH4 screening retained 48 new and potent HDAs with predicted inhibitory potencies pKi pre up to 73 times lower than that of HDA1 (pKi exp = 2.5 nM). Combining molecular modeling and PH4 in-silico screening of the VCL resulted in the proposed novel potent antimalarial agent candidates with favorable pharmacokinetic profiles.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139366737","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2023-06-30DOI: 10.25004/ijpsdr.2023.150305
Ashwini Pharne, S. Gabhe, S. Gabhe
A present study was undertaken to understand the impact of piperine and some of its derivatives on the bioavailability of verapamil used in the treatment of cardiac disorders. On oral administration, it undergoes fast biotransformation resulting in its low bioavailability. Its bioavailability varies between 20 and 35%. Piperine (a well-known bioenhancer) has been reported to improve the bioavailability of a wide range of structurally and therapeutically varied medicines. Hence some derivatives of piperine were synthesized and evaluated for their bioenhancing effect on verapamil. The bioenhancing effect of piperine and synthesized derivatives was investigated and compared using a validated HPLC method per USFDA guidelines. The pharmacokinetic characteristics of verapamil alone and when combined with piperine and its synthetic analogs were also investigated. When administered to wistar rats, it was discovered that verapamil bioavailability was 1.54 times higher when given with piperine and 2.42 times higher when given with morpholine derivative. The study undertaken indicates that some synthetic derivatives of piperine can be successfully used to enhance the bioavailability of verapamil to a considerable extent
{"title":"Evaluation of Bioenhancing Effect of Piperine and its Analogs on the Pharmacokinetics of Verapamil","authors":"Ashwini Pharne, S. Gabhe, S. Gabhe","doi":"10.25004/ijpsdr.2023.150305","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150305","url":null,"abstract":"A present study was undertaken to understand the impact of piperine and some of its derivatives on the bioavailability of verapamil used in the treatment of cardiac disorders. On oral administration, it undergoes fast biotransformation resulting in its low bioavailability. Its bioavailability varies between 20 and 35%. Piperine (a well-known bioenhancer) has been reported to improve the bioavailability of a wide range of structurally and therapeutically varied medicines. Hence some derivatives of piperine were synthesized and evaluated for their bioenhancing effect on verapamil. The bioenhancing effect of piperine and synthesized derivatives was investigated and compared using a validated HPLC method per USFDA guidelines. The pharmacokinetic characteristics of verapamil alone and when combined with piperine and its synthetic analogs were also investigated. When administered to wistar rats, it was discovered that verapamil bioavailability was 1.54 times higher when given with piperine and 2.42 times higher when given with morpholine derivative. The study undertaken indicates that some synthetic derivatives of piperine can be successfully used to enhance the bioavailability of verapamil to a considerable extent","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139366770","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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