{"title":"ENHANCEMENT OF DISSOLUTION AND BIOAVAILABILITY OF SIMVASTATIN BY SOLID DISPERSION TECHNIQUE USING SUGAR-BASED CARRIERS","authors":"Venkata Naga JYOTHI NAKKA, Kumar Shiva Gubbiyappa, Nagesh Nagaraju","doi":"10.22159/ijap.2024v16i1.49442","DOIUrl":null,"url":null,"abstract":"Objective: The research aims to enhance poorly water-soluble drug Simvastatin (SMV) solubility and bioavailability by solid dispersion (SD) using various sugar carriers like lactulose, xylitol, Sorbitol, and soluplus.\nMethods: First, the drug was subjected to determine bulk density, carr’s index, Hausner’s ratio, angle of repose, solubility analysis in various solvents like 0.1 N HCl, 6.8pH, 7.2pH phosphate buffers, methanol, and ethanol and preformulation studies. via various carrier concentrations (1:0.5, 1:1, 1:1.5, 1:2, and 1:3), SMV solid dispersions (SD s) were made by solvent evaporation and fusion. The various physiochemical parameters of each formulation were tested.\nResults: For various physicochemical criteria, all of the formulations were found to be within the allowed pharmacopoeial limits. Preformulation studies such as FT-IR demonstrated the lack of interactions between drugs and excipients. In comparison to the other solvents, 0.1N HCl showed SMV to be more soluble. The SDs underwent yield, entrapment, and in vitro drug release study evaluations. 88 to 100.68% recovery rates and 92 to 101% capture efficiency were observed. While SDs containing Sorbitol released 74-98% of the medicine, formulations utilizing Sorbitol demonstrated 80-99% drug release, and formulations using xylitol as a carrier released 83-99% of the drug. For more than 60 min, the formulation, including lactulose, delivered 91-100% of the Simvastatin dose.\nConclusion: Lactulose-containing SMV SDs demonstrated superior release characteristics, and an optimized formulation with a 1:1.5 drug-to-carrier ratio has been chosen.","PeriodicalId":13737,"journal":{"name":"International Journal of Applied Pharmaceutics","volume":"24 8","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-01-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Applied Pharmaceutics","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.22159/ijap.2024v16i1.49442","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 0
Abstract
Objective: The research aims to enhance poorly water-soluble drug Simvastatin (SMV) solubility and bioavailability by solid dispersion (SD) using various sugar carriers like lactulose, xylitol, Sorbitol, and soluplus.
Methods: First, the drug was subjected to determine bulk density, carr’s index, Hausner’s ratio, angle of repose, solubility analysis in various solvents like 0.1 N HCl, 6.8pH, 7.2pH phosphate buffers, methanol, and ethanol and preformulation studies. via various carrier concentrations (1:0.5, 1:1, 1:1.5, 1:2, and 1:3), SMV solid dispersions (SD s) were made by solvent evaporation and fusion. The various physiochemical parameters of each formulation were tested.
Results: For various physicochemical criteria, all of the formulations were found to be within the allowed pharmacopoeial limits. Preformulation studies such as FT-IR demonstrated the lack of interactions between drugs and excipients. In comparison to the other solvents, 0.1N HCl showed SMV to be more soluble. The SDs underwent yield, entrapment, and in vitro drug release study evaluations. 88 to 100.68% recovery rates and 92 to 101% capture efficiency were observed. While SDs containing Sorbitol released 74-98% of the medicine, formulations utilizing Sorbitol demonstrated 80-99% drug release, and formulations using xylitol as a carrier released 83-99% of the drug. For more than 60 min, the formulation, including lactulose, delivered 91-100% of the Simvastatin dose.
Conclusion: Lactulose-containing SMV SDs demonstrated superior release characteristics, and an optimized formulation with a 1:1.5 drug-to-carrier ratio has been chosen.
期刊介绍:
International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.