In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers | ||
| Journal of Advanced Pharmacy Research | ||
| Article 3, Volume 3, Issue 2, April 2019, Pages 62-67 PDF (338.19 K) | ||
| Document Type: Research Article | ||
| DOI: 10.21608/aprh.2019.7629.1075 | ||
| Authors | ||
| Kholoud Ali* 1; Khaled AboZeid1; Mohamed Nasr2 | ||
| 1Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ahram Canadian University, Egypt. | ||
| 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Egypt. | ||
| Abstract | ||
| Objectives: Solid dispersion is a unique and promising approach for improving the oral absorption and oral bioavailability of the poorly water soluble drugs. Atorvastatin Calcium (ATV) is an anti-hyper lipidemic agent, It belongs to class II drugs according to the biopharmaceutical classification system (BCS), and undergoes extensive first-pass metabolism after oral absorption exhibiting 12% bioavailability. The Objective of the present study is to investigate the effect of formulating the hydrophobic drug (ATV) in a solid dispersion form on its bioavailability. Methods: ATV solid dispersion (ATV-SD) was prepared by microwave induced fusion method, containing poloxamer188 as a hydrophillic carrier. The resultant ATV-SD was compressed into tablets with other ingredients and was evaluated against pure ATV tablets, in vitro dissolution study was carried out to compare the dissolution profiles of the prepared ATV-SD against the pure form of ATV. In vivo study was conducted using healthy male volunteers (n = 6). A high performance liquid chromatography method was employed to determine the level of drug in human plasma. Results: In vitro dissolution study revealed an enhancement in the dissolution profile of ATV-SD. The study of pharmacokinetics parameters also showed an enhancement after oral administration of ATV-SD tablet when compared with pure ATV tablets, where , the AUC0–60h and Cmax were increased after intake of ATV-SD tablets orally compared with that of pure ATV tablets. Conclusion: All these could be demonstrated that ATV-SD would be prospective means for enhancing higher oral bioavailability of ATV. | ||
| Keywords | ||
| Atorvastatin; bioavailability; hyperlipidemia; microwave; Poloxamer; Solid dispersion | ||
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