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SOLID DISPERSIONS, INCLUSION COMPLEXES, AND FAST-RELEASE TABLETS OF ATORVASTATIN: SOLID STATE CHARACTERIZATION, DISSOLUTION BEHAVIOR, AND IN VIVO PHARMACOKINETIC EVALUATION

Author Names : Dr. S. Dey
Page No. : 44-55
Read Hit : 928
Pdf Downloads Hit : 10  volume 1 issue 1
Article Overview

ARTICLE DESCRIPTION: 

Sanjay Dey, Bhaskar Mazumder. Solid Dispersions, Inclusion Complexes, And Fast-Release Tablets Of Atorvastatin: Solid State Characterization, Dissolution Behavior, And In Vivo Pharmacokinetic Evaluation , ASIO Journal of Drug Delivery, 2015, 1(1): 44-55.

ARTICLE TYPE: RESEARCH

dids/doi No.: 12.2015-38368922

Dids Link : http://dids.info/didslink/12.2015-21336482/

 

ABSTRACT:

The objective of the present study was to prepare solid dispersion (SD) and inclusion complexes of atorvastatin (ATV) using different hydrophilic carriers (polyethylene glycol (PEG 4000 and PEG 6000), polyvinyl pyrrolidone (PVP K30), and D-mannitol) and β-cyclodextrin (β-CD), respectively to improve the aqueous solubility and dissolution rate. Different drug: carrier ratios (1:1, 1:2, and 1:3) were used and their effects on the dissolution performance were studied. The physical state and drug-carrier interaction in solid state were analyzed by infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The dissolution rate of ATV from tablets containing β-CD inclusion complex was compared with conventional tablets without β-CD.  In vivo pharmacokinetic studies were performed on rabbits to compare the in vivo performance between tablets with or without inclusion complex. Improvement in the drug dissolution rate was observed in SDs and inclusion complexes as compared to the physical mixtures. Inclusion complexes of ATV with β-CD gave a better drug release profile as compared to among other formulations. Β-CD–based tablets exhibited a significant higher ATV dissolution than did conventional tablets prepared without β-CD. A shorter tmax and greater Cmax and AUC were obtained by using tablets prepared from inclusion complex as compared to conventional tablets. It can be concluded that the oral bioavailability of ATV could be improved by administration of tablets containing β-CD inclusion complex as compared to conventional tablets prepared without β-CD.

Keywords: Atorvastatin; solid dispersion; inclusion complex; phase solubility study, phase solubility study

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