Effect of Solid Dispersions, HP-β & γ- Cyclodextrin Inclusion Complexes on the Dissolution Rate of Simvastatin and Formulation Development & Evaluation of Simvastatin ODTs

Abstract

The objective of this study is to examine the effect of solid dispersions prepared with Hydroxy Propyl-β (HP-β) and γ-cyclodextrin (CD) inclusion complexes and polyethylene glycols (PEG) 3550 and 6000 on the dissolution rate of simvastatin and the formulation and evaluation of simvastatin orally disintegrating tablets (ODTs). Simvastatin is a hypolipidemic drug with low solubility and low oral bioavailability.

Methods:

• Solid dispersions were prepared with drug and PEG 3350 & 6000 in a 1:2 ratio (drug: polymer) and in combinations (Drug: PEG 3350: PEG 6000) in the ratio 1:2:1 & 1:1:2.

• Solid dispersions of simvastatin with HP-β (1:1,1:2,1:3) and γ-cyclodextrins (1:1,1:2) with different drug: carrier ratios were prepared by kneading technique.

• ODTs were prepared with drug: γ-CD solid dispersion in the ratio 1:2 along with super disintegrating agents such as crospovidone, sodium starch glycolate, and croscarmellose sodium in different amounts for different formulations F1-F9.

Results:

• Formulations were evaluated for physical appearance, weight variation, thickness, hardness, friability, content uniformity test, disintegration test, and in vitro release studies.

• Formulation F3 showed a disintegration rate of 48.16 sec ± 0.75 and a dissolution rate of 99.89 ± 0.31 for 20 minutes.

• Formulation F3 was found to be quicker in disintegration and faster in drug releasing, optimized for enhanced dissolution profile and bioavailability.