Quality Enhancement by Inclusion Complex Formation of Simvastatin Tablets

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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

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  • 1. Stancu C Sima A. Statins: mechanism of action and effects. J Cell Mol Med. 2001;5:378-387.

  • 2. Jun SW. Inclusion complex of simvastatin with hydroxypropyl-betacyclodextrin using supercritical antisolvent (SAS) process MS thesis Chungnam National University Daejeon Korea 2006

  • 3. Rédai E Sipos E Kiss A Tőkés B. Szimvasztatin zárványkomplex képzése random metil-β-ciclodextrinnel. Orvostudományi Értesítő. 2011;84(2): 101-103.

  • 4. *** Primellose - product sheet information DFE Pharma

  • 5. Pani NR Nath LK Bhunia B. Formulation development and optimization of immediate release nateglinide tablets by factorial design. Drug discoveries & Therapeutics. 2010;4(6):453-458.

  • 6. http://www.specialtyminerals.com/specialty-applications/specialtymarkets-for-minerals/nutritional-supplements/talc-as-a-glidant-lubricant

  • 7. *** European Pharmacopoeia 7.0. vol.2 Council of Europe Strasbourg 2010

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