International Journal of Pharmaceutical Sciences and Drug Research最新文献

{"title":"HYPOLIPIDEMIC ACTIVITY OF HIPTAGE BENGHLENSIS LEAF EXTRACTS ON HIGH FAT DIET INDUCED HYPERLIPIDAEMIC RATS","authors":"P. Samal, K. P. Meena, Jaya Shree, Rajesh Choudhary","doi":"10.25004/ijpsdr.2023.150316","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150316","url":null,"abstract":"The present study was designed to evaluate the hypolipidemic effects of aqueous extract (HBAE) and ethanolic extract (HBEE) of Hiptage benghalensis leaves using a high-fat-diet induced hyperlipidemic animal model. Albino male wistar rats (120–150 g) were split into various groups, each of which had six individuals. Normal rats (group I) were received 0.3% carboxy methyl cellulose (CMC) with a standard laboratory diet, while hyperlipidemic rats (group II, III, IV, V, VI and VII) were fed high-fat diet for induction of hyperlipidemia. Hyperlipidaemic control group (group II) received 0.3% CMC (10 mL/kg/day), standard group (group III) received gemfibrozil (50 mg/kg/day, p.o.), HBAE groups (group IV and V) received aqueous extract of H. benghalensis (100 and 200 mg/kg/day, p.o.), and HBEE groups (group VI and VII) received an ethanolic extract of H. benghalensis (100 and 200 mg/kg/day, p.o.), concurrent with high fat diet for consecutive four weeks. The HBAE and HBEE treatments led to a significant (p < 0.05) reduction in serum lipids (TC, TG, LDL and VLDL) and elevation in cardioprotective HDL, when compared to hyperlipidaemic rats (group II). Phytochemical screening revealed the presence of phytoconstituents such as alkaloids, flavonoids, saponins, tannins, phenolic compounds and steroids, which may be attributed to observed hypolipidemic effects. The present study’s findings concluded that HBEE (200 mg/kg, p.o.) had potent hypolipidemic effects.","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":"139366470","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}

{"title":"GC-MS Analysis and Molecular Docking of Plant-based Compounds from Medicinal Plant Sida acuta Burm F. for Antibacterial Potential","authors":"Adline Anita, D. Selvaraj","doi":"10.25004/ijpsdr.2023.150309","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150309","url":null,"abstract":"Antimicrobial-resistant bacteria cause severe public health issues and mortalities. The evolution of multi-drug resistant bacteria shifted the focus of researchers towards traditional medicine involving bioactive compounds. Plants with bioactive compounds play a pivotal role in treating human diseases. Many of the plant-based bioactive compounds were proven to have the ability to inhibit bacterial growth through different modes of action. Thus, plant-based compounds have been focused on finding potential molecules with antibacterial efficiency to overcome bacterial infection problems. So, in the present study, phytocompounds of Sida acuta Burm F. leaf extract were identified using GC-MS technique and phytocompounds with antibacterial potential were identified through a molecular docking study. The qualitative test carried out indicated the presence of carbohydrates, alkaloids, phenols, terpenoids, flavonoids, amino acids, steroids, glycosides, saponins, quinones and coumarins in the extract. The GC-MS analysis showed the presence of 30 phytocompounds and molecular docking studies revealed the best binding affinity of the phytocompounds Pyrido[1,2-a]pyrimidine, Acetonitrile,2-(6-phenantridinyl), 5H-Imidazo(2,1-a)isoindole,2-phenyl and Pyrido[1,2-a]pyrimidine towards E. coli biomolecules- 1PHO, 5I5H, 5UW2 and 6NTW respectively. The present study concludes that the phytocompounds of S. acuta have appreciable antibacterial efficiency","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":"139366868","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}

{"title":"Design and In-vivo Evaluation of Quercetin Nanosponges-based Buccal Tablets of Quercetin","authors":"P. Gujjula, A. Parameswari","doi":"10.25004/ijpsdr.2023.150310","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150310","url":null,"abstract":"The objective was to increase the bioavailability of quercetin by creating a controlled release formulation using nanosponges based on cyclodextrin. Based on the early testing, a 3-factor, 3-level Box-Behnken design with quercetin was loaded into nanosponges using the freeze-drying process. The prepared nanosponges were examined after being described and made into tablets. The quercetin-loaded nanosponges have particle sizes ranging from 36.45 to 135.27 nm, encapsulation efficiencies ranging from 42.37 to 88.44%, and drug release percentages at 6 hours ranging from 53.04 to 82.64%. The FTIR, DSC, and XRD investigations validated the Quercetin interaction with nanosponges. The medicine released from the nanosponges buccal tablets in-vitro at a rate of 99.75%, and stability testing showed no significant changes within six months after the nanosponges were transformed into tablets. In-vivo studies in rats showed that quercetin optimised nanosponges tablets Cmax of 6.27 ± 0.06 ng/mL was significantly higher (p","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":"139366865","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}

{"title":"Comparative Cardioprotective Effect of Herbs of Hridya dashemani (Karamarda- Carissa carandas L., Badara- Ziziphus jujuba Lam.) versus Arjuna-Terminalia arjuna (Roxb.ex.DC.) Wight&Arn. against Isoprenaline induced Myocardial Infarction in Rats","authors":"Harini A Rao, Veena M S, Lalitha B R, Sudhakara Bhat","doi":"10.25004/ijpsdr.2023.150313","DOIUrl":"https://doi.org/10.25004/ijpsdr.2023.150313","url":null,"abstract":"Hridya dashemani (ten cardioprotective herbs) includes fruits of Amra, Amrataka, Lakucha, Karamarda, Vrukshamla, Amlavetasa, Kuvala, Badara, Dadima and Matulunga. In Ayurveda, these herbs have been known to be conducive to heart. The present study was designed to evaluate the cardioprotective action of two herbs of Hridya dashemani fruits of Karamarda (Carissa carandas L.) and fruits of Badara (Ziziphus jujuba Lam.)] on the basis of biochemical&histopathological parameters in isoprenaline (ISO) induced myocardial infarction (MI) in experimental rats and to compare with stem bark of Arjuna (Terminalia arjuna (Roxb.ex.DC.) Wight&Arn.), a well-known cardioprotective herb. Total 36 male wistar albino rats were randomly divided into six groups. Group I- normal control (NC), group II- ISO induced MI, group IIIpositive control with hesperidin (100 mg/kg b.w), group IV- Badara (Z. jujuba – 450 mg/kg b.w), group V- Karamarda (C. carandus – 450 mg/kg b.w), group VI- Arjuna (T. arjuna – 450 mg/kg b.w). After 21 days of pre-treatment, experimental MI was induced in all groups except NC by injecting ISO subcutaneously (85 mg/kg) on 19th&20th day at an interval of 24 hours. Serum biochemical parameters, including cardiac biomarkers and histopathological examination of heart tissues were evaluated. ISO treated rats had a significant (p < 0.05) elevation in serum levels of diagnostic marker enzymes (AST, ALT, CK-MB, LDH, ALP) when compared to NC. All the pre-treated groups had significantly (p < 0.05) reduced marker enzyme serum levels compared to the ISO treated control. The protective role of these herbs was further confirmed by histopathological examination. The comparison revealed that Karamarda (C. carandus) pre-treated had similar protective effect as Arjuna (T. arjuna) in various biochemical parameters (AST, ALT, ALP, LDH, CK-MB, HDL, cholesterol, creatinine). It may be concluded from the present study that 450 mg/kg b.w of water extract of the above herbs have cardioprotective action against isoprenaline induced MI, with Karamarda (C. carandus), Arjuna (T. arjuna) having almost similar effects. The study paves way to further evaluate these herbs as preventive and curative in cardiovascular disease (CVD) clinical management.","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":"139367090","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}

{"title":"Quality by Design Enabled Development and Optimization of the Nanoparticulate System of Cabazitaxel","authors":"M. Paithankar, M. Bhalekar","doi":"10.25004/ijpsdr.2022.140115","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140115","url":null,"abstract":"Cabazitaxel (CTX), a novel taxane derivative, has proven effective in many solid tumors. It is also approved in many countries for multiple uses in solid tumors. The current marketed formulation lacks the tumortargeting ability, and its uneven distribution in the body causes toxicity to normal tissues. Further, it is a surfactant (polysorbate 80) based micellar formulation composed of ethanol as a co-solvent to improve the solubility of CTX, which causes severe and life-threatening side effects. Hence, to avoid the problem\u0000associated with this conventional CTX formulation, the nanoparticulate drug delivery system of CTX was\u0000developed by employing the Quality by Design (QbD) approach. The CTX nanoparticulate system was\u0000developed by employing a bottom-up followed by a top-down approach. The size reduction was obtained\u0000by High-Pressure Homogenizer (HPH). The formulation optimization was done using QbD approach. Design\u0000of experiments (DoE) was used to understand the effect of various formulation and process variables on\u0000a dependent variable like particle size distribution.\u0000The stabilizer concentration, concentration of solubilizer, HPH pressure, and passes were selected as\u0000independent factors while particle size distribution was selected as a dependent factor for evaluation.\u0000The nanoparticulate system was developed using PEG-400 as solubilizing agents, while Soya\u0000Phosphatidylcholine (SPC) was used as a surface stabilizer. Response surface plots revealed a decrease in\u0000particle size with increasing concentration of SPC and PEG 400. Similarly, a decrease in particle size with increased HPH passes and pressure was found. The optimum concentrations of SPC and PEG 400 were\u0000found to be 20% and 2.5%, respectively. 20 KPSI pressure and 5 HPH passes were derived as optimized\u0000processing parameters from DoE. The optimized formulation had a size of 43.5 nm, with PDI is less than 0.4. Due to its narrow particle size distribution, the formulation did not show any increase in particle size or aggregation up to 24 hours. The present research confirms the feasibility of developing the nanoparticulate system of CTX using the bottom-up followed by the top-down technique. The formulation was systematically optimized using QbD approach. The optimum concentration of PEG 400 as solubilizer and concentration of SPC as stabilizer was obtained from DoE, yielding optimum particle size and stability","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74760968","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}

{"title":"Quantitative and Qualitative Assessment of Marketed Nutraceuticals for Active Ingredients and Heavy Metals for Safety and Efficacy","authors":"A. Dhiman, Rohit Bansal","doi":"10.25004/ijpsdr.2022.140109","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140109","url":null,"abstract":"The global nutraceutical market is expanding fast, and people nowadays are inclined towards nutraceutical supplements for daily micronutrient needs and health benefits in some disease conditions. Hence, ensuring the safe and effective use of these supplements is the need of the hour. The current study is aimed at determining the accuracy and regulatory compliance of marketed nutraceutical formulations by quantifying the active nutraceutical ingredients and heavy metal content in these formulations using advanced analytical techniques. Total 12 marketed formulations were selected and analyzed in NABL (National Accreditation Board for Testing and Calibration Laboratories) accredited laboratory using High-performance liquid chromatography (HPLC) and inductively coupled plasma-mass-spectrometry (ICP-MS). The quantified values were compared with label-stated values and recommended values as per FSSAI. The quantified values in two lycopene samples varied significantly (-16 and +16%) from the label stated content and were found non-compliant with the regulatory recommendations. The measured intake values of calcium and vitamin D varied from 24 to 204% from the recommended daily allowances established by FSSAI. The quantified daily intake values varied from 4.2 to 58 mg and from 4 to 21.5 mg for lycopene and lutein, respectively. Heavy metal content determination resulted in two samples deviating from the tolerance limits of heavy metals for lead and arsenic. The mean values for lead and arsenic were found to be 2.482 ± 6.921 and 0.311 ± 0.655 ppm, respectively. The present study results provided vital information on the composition of marketed nutraceutical formulations. The regulatory agencies require stringent monitoring practices to ensure compliance with the existing regulatory guidelines to provide the consumer safe and effective nutraceutical products.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76427552","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}

{"title":"Ameliorative Role of Mixed Hydro-methanolic (60:40) Extract of Andrographis paniculata on Chromium (VI)-induced Immunomodulation in Male Albino Rats","authors":"S. Dey, Durgapada Dolai","doi":"10.25004/ijpsdr.2022.140117","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140117","url":null,"abstract":"The immune system controls the body’s homeostatic state and helps to defend against infections. Activation and expansion of many biomolecules are crucial for the homeostatic state. Chromium, a common heavy metal found in nature, is an active in its hexavalent state. The abundant use of chromium in paints, steel plants, intoxicated the workers and modulates their body homeostasis. In this article, we were intended to evaluate the role of Andrographis paniculata Nees extract on restoration of the body homeostatic state in terms of immune system. For the present investigation, a group of male albino rats (80–100 g) were\u0000induced by intraperitonial injection of vehicle (0.9% NaCl), Potassium dichromate (K2Cr2O7) (0.8 mg /\u0000100 g body weight / day), K2Cr2O7 plus mixed hydro-methanol solvent extract in the ratio of 60:40 at a\u0000dose of 500 mg/kg body weight daily at an interval of six hours after injection of K2Cr2O7 for a period\u0000of 28 days. We found that Cr (VI) induces a hyper response of pro-inflammatory cytokines followed by\u0000apoptosis in liver and lung tissue. Excess production of reactive oxygen species (ROS) is controlling the\u0000whole phenomena. The A. paniculata Nees extract successively inhibit the ROS generation, as a result a\u0000significant quenching of pro-inflammatory cytokine production was noted. A. paniculata Nees extract\u0000prompted decrease amount of ROS and its associated inflammation provoke the cell survival and helps\u0000to maintain a homeostatic state of the body","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79407018","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}

{"title":"Enantioselective RP-UFLC Method for the Simultaneous Estimation of Sitagliptin (STG) Enantiomers (R and S) in the Racemic Mixture and their Pharmacokinetic Assessment in Male Wistar Rats","authors":"C. Veeresham, C. Srinivas, Husna Kanwal Qureshi, P. Shyam","doi":"10.25004/ijpsdr.2022.140108","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140108","url":null,"abstract":"The present work aims to develop and validate a simple, rapid, and reproducible reverse phase ultra-fast liquid chromatography method with a UV detector (RP-UFLC-UV) was developed for the separation and determination of sitagliptin (STG) enantiomers (S-(STG) and R-(STG)) simultaneously. Baseline separation was achieved on Lux cellulose-1 column, (cellulose tri-(3,5-dimethyl phenyl carbamate (Chiralcel OD-RH, 250 mm × 4.6 mm, 5 µm) column and mobile phase consisted of 20mM borate buffer solution (pH = 9±0.05) and ACN in the ratio of (60:40, v/v) at a flow rate of 0.8 mL/min was used. Detection of peaks was monitored at 262 nm. For analyzing the STG enantiomers in the rat serum and pure API, a method was developed using the chiral RP-UFLC-UV method was validated. The single oral dose of 2.5 mg/kg of STG racemate was administered to a group of 6 healthy rats for a comparative pharmacokinetic study of both the enantiomers. The linear range of the calibration curve for each enantiomer was 0.5–64 µg/mL. The\u0000precision of this method at concentrations between 0.5–48 µg/mL was within 8.65% and the % recovery\u0000(accuracy) of both sitagliptin (STG) enantiomers (S-(STG) and R-(STG) were 98.47–101.02% and 98.93-\u0000100.52%. The precision at LLOQ (0.5 µg/mL) was between 8.65%-7.09%, which was poor than that at QC\u0000levels, and the average extraction recovery was higher than 85% for both sitagliptin (SGT) enantiomers\u0000at QC levels, and its pharmacokinetics of enantiomers was found to be stereoselective.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83701102","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}

{"title":"A Validated LC-MS/MS Method for Pharmacokinetic Study of Edoxaban in Healthy Rabbits","authors":"D. Vasanth, B. Rajkamal","doi":"10.25004/ijpsdr.2022.140112","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140112","url":null,"abstract":"A liquid chromatography-tandem mass spectrophotometric (LC–MS/MS) method was developed to quantify Edoxaban in rabbit plasma employing liquid liquid extraction with ethyl acetate. Developed method was validated for specificity, precision, accuracy, recovery, and stability characteristics. Chromatographic separation was achieved on Chromolith C18column (100 mm x 4.6 mm x 5 µm) with 70:30 ratio of methanol and 0.1% formic acid as an isocratic mobile phase with a flow rate of 0.80 mL/min. The developed LC-MS method was applied to assess pharmacokinetics parameters of edoxaban in healthy rabbits. Six Male albino rabbits weighing 2.0-2.5 Kg were randomly selected for the pharmacokinetic study. Blood samples (1-mL) were withdrawn from the marginal ear vein from 0 to 24 hours after administration (1.2 mg/kg). Plasma was separated by centrifugation and the plasma concentrations of edoxaban at various times were determined by LC-MS/MS. Pharmacokinetic parameters was calculated. Edoxaban showed Tmax of 2.0 and mean Cmax, AUC0®t andAUC0®a for Test formulation is 213.83 ± 10.46, 945.13 ± 24.32 and\u0000986.135 ± 19.31, respectively. A highly specific, rugged, and rapid method with sufficiently low LLOQ\u0000was developed to analyze routine samples of single dose or multiple-dose pharmacokinetics with any\u0000marketing formulation of edoxaban.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86675546","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}

{"title":"Design and Evaluation of Gastro-retentive Drug Delivery System for Glimepiride using Design of Experiment","authors":"Anil K. Sharma, Aseem Kumar, R. Dutt","doi":"10.25004/ijpsdr.2022.140114","DOIUrl":"https://doi.org/10.25004/ijpsdr.2022.140114","url":null,"abstract":"Glimepiride, oral sulfonyl urea, BCS class-II drug is used to treat diabetes (type-II). Due to its low solubility,\u0000it is an ideal candidate for solubility enhancement, leading to better bioavailability and subsequent dose. In the present study, the solid dispersion technique was used to improve the solubility using solvent evaporation method. The solid dispersions were prepared using affnisol 912 as a solubility enhancer. The prepared solid dispersions were evaluated for solubility in 0.1N HCl pH 1.2 and phosphate buffer pH 7.8 medium. The solubility of glimepiride in optimized solid dispersion (SD1) formulation was 682.44 µg/mL compared to 6.88 µg/mL for pure drug in pH 7.8 medium. The solid dispersion (SD1) was further formulated into the tablets. The gastro-retentive and mucoadhesive properties were contributed to the tablets by HPMC K4M and Carbopol 940, respectively. Factorial design (Central composite design) was used to optimize the gastro-retentive tablets. The tablet formulations showed good mucoadhesive properties and drug release up to 12 hours in pH 1.2 with 0.5% SLS medium. The optimized formulation (F2) showed cumulative drug release up to 97.20 ± 0.99% in 12 hours. The drug release kinetics also showed that the drug is release by dissolution and diffusion from the drug matrix. The gastro-retention studies in rabbits also showed the tablets remain within the GIT up to 12 hours as confirmed by x-ray images.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88528974","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}