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Original Article

Inclusion complexes of atorvastatin calcium–sulfobutyl ether β cyclodextrin with enhanced hypolipidemic activity

Anureet Arora, Geeta Aggarwal, Thakur Gurjeet Singh, Manjinder Singh, Gitika Arora, Manju Nagpal.

Cited by 3 Articles

The aim of present study was to explore the impact of Atorvastatin (ATR) Sulfobutylether beta-cyclodextrin complex (ATR-SBE-β-CD) on ATR dissolution behavior. Various batches of inclusion complexes were formulated using various drug: polymer ratios (1:1, 1:3 and 1:5); using β-CD and SBE-β-CD and using two methods (freeze drying and kneading method). Phase solubility studies were carried out of all the complexes and ratio 1:5 (ATR- SBE-β-CD) prepared by freeze drying yield maximum solubility enhancement (30-fold in comparison to pure drug). Fourier transformation infrared spectroscopy (FT-IR), Powder X-ray diffraction (X-RD), Scanning electron microscopy (SEM), Differential scanning calorimetry (DSC) studies was also carried out. FTIR studies showed no drug polymer interaction. DSC and SEM studies suggested incorporation of drug into inclusion complexes of cyclodextrin. Solid dispersion via Freeze drying technique using SBE-β-CD (1:3 ratio of drug to polymer) produces better dissolution characteristics in comparison to kneading method. The results revealed superiority of SBE-β-CD over β-CD for solubility enhancement of poorly soluble drugs (owing to amorphous nature and more stable form of SBE β-CD). No significant drug loss was observed in solid dispersion batch (as per results of drug content analysis) during storage for 3 months under accelerated conditions. Further In vivo Pharmacodynamics Studies of selected batch were carried out by inducing obesity in rats by feeding them with a high-fat diet. Group I (normal control group) received normal chow diet and group II, group III, group IV (High fat diet group, optimized formulation group and disease control group) received HFD for 1 month and were further evaluated for BMI, Blood glucose, lipid profile, liver profile and Histopathological examination. The results so obtained depicted that optimized formulation of Atorvastatin (10 mg/kg, p.o.) showed better results in comparison to pure Atorvastatin Calcium (10 mg/kg, p.o.).

Key words: Cyclodextrins, Solubility, Dissolution, Histopathology, Stability, Obesity

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