<abstract xmlns="http://www.w3.org/1999/xhtml"><p> Introduction: Simvastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia. To enhance its bioavailability by inclusion complexation, as host molecule randommethyl-β-cyclodextrin had been used. After evaluating the complexes we chose the kneading product in 1:2 molar ratio for incorporation of 10 mg simvastatin tablets. Materials and methods: We prepared homogenous mixtures of the inclusion complex and some excipients. The tablets were prepared by direct compression. The tablets were evaluated in regard to: weight uniformity, thickness, diameter, hardness, friability, disintegration and dissolution profile. Results: Weights are in the range of 196-208 mg, diameter 6.83-6.86 mm, height 3.86-4.01 mm, hardness 78.3-113.1 N, friability 0.75- 1.19 %, disintegration above 15 minutes. The dissolved amounts of simvastatin from the tablets are higher compared to the dissolution of pure simvastatin, but lower than the dissolution of the complex itself. Excipients, like disintegrants and lubricants greatly influence the dissolution properties of the tablets. Conclusions: According to our results, tablets containing inclusion complex of simvastatin exhibit better solubility, according to the dissolved amount of simvastatin, than pure drug alone. Proper physical parameters of the tablets are obtained by application of 5 % Primellose</p></abstract>

Introduction: Simvastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia. To enhance its bioavailability by inclusion complexation, as host molecule randommethyl-β-cyclodextrin had been used. After evaluating the complexes we chose the kneading product in 1:2 molar ratio for incorporation of 10 mg simvastatin tablets. Materials and methods: We prepared homogenous mixtures of the inclusion complex and some excipients. The tablets were prepared by direct compression. The tablets were evaluated in regard to: weight uniformity, thickness, diameter, hardness, friability, disintegration and dissolution profile. Results: Weights are in the range of 196-208 mg, diameter 6.83-6.86 mm, height 3.86-4.01 mm, hardness 78.3-113.1 N, friability 0.75- 1.19 %, disintegration above 15 minutes. The dissolved amounts of simvastatin from the tablets are higher compared to the dissolution of pure simvastatin, but lower than the dissolution of the complex itself. Excipients, like disintegrants and lubricants greatly influence the dissolution properties of the tablets. Conclusions: According to our results, tablets containing inclusion complex of simvastatin exhibit better solubility, according to the dissolved amount of simvastatin, than pure drug alone. Proper physical parameters of the tablets are obtained by application of 5 % Primellose

Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets

Pharmaceutical Technology Department, Faculty of Pharmacy, University of Medicine and Pharmacy, Tîrgu Mureș, Romania

Physical Chemistry Department, Faculty of Pharmacy, University of Medicine and Pharmacy, Tîrgu Mureș, Romania

Pharmaceutical industry and management Department, Faculty of Pharmacy, University of Medicine and Pharmacy, Tîrgu Mureș, Romania

Acta Marisiensis - Seria Medica

{"article-title":"Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets"}

Introduction: Simvastatin is an inhibitor of hydroxy-methyl-glutaryl-coenzyme A reductase, used in the treatment of hypercholesterolemia. To enhance its...

Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets

Published Online: Mar 07, 2014

Page range: 223 - 225

DOI: https://doi.org/10.2478/amma-2013-0052

Keywords
simvastatin, randommethyl-β-cyclodextrin, dissolution, tablet

This content is open access.

Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets

Published Online: Mar 07, 2014

Page range: 223 - 225

DOI: https://doi.org/10.2478/amma-2013-0052

Keywordssimvastatin, randommethyl-β-cyclodextrin, dissolution, tablet

This content is open access.

Keywords
simvastatin, randommethyl-β-cyclodextrin, dissolution, tablet