ENHANCEMENT OF DISSOLUTION AND BIOAVAILABILITY OF SIMVASTATIN BY SOLID DISPERSION TECHNIQUE USING SUGAR-BASED CARRIERS

VENKATA NAGA JYOTHI NAKKA; KUMAR SHIVA GUBBIYAPPA; NAGESH NAGARAJU

doi:10.22159/ijap.2024v16i1.49442

Authors

VENKATA NAGA JYOTHI NAKKA Research Scholar Gitam School of Pharmacy, Gitam Deemed to be University, Rudraram, Hyderabad, India. Department of Pharmaceutics, KL College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Guntur-522302, Andhra Pradesh, India https://orcid.org/0000-0001-7405-435X
KUMAR SHIVA GUBBIYAPPA Principal, GITAM School of Pharmacy, GITAM Deemed to be University, Rudraram, Patencheru, Sanga Reddy-502329, Telangana, India https://orcid.org/0000-0002-9075-6535
NAGESH NAGARAJU Senior Vice President, F R and D, APL Research Centre, Aurobindo Pharma Ltd, Sy. No. 313, Bachupally, Medchal, Malkajgiri-500090, Hyderabad, Telangana, India https://orcid.org/0009-0009-4793-623X

DOI:

https://doi.org/10.22159/ijap.2024v16i1.49442

Keywords:

Simvastatin, Xylitol, Soluplus, Lactulose, Sorbitol, Solvent evaporation

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.

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