Ali, K., AboZeid, K., Nasr, M. (2019). In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers. Journal of Advanced Pharmacy Research, 3(2), 62-67. doi: 10.21608/aprh.2019.7629.1075
Kholoud Ali; Khaled AboZeid; Mohamed Nasr. "In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers". Journal of Advanced Pharmacy Research, 3, 2, 2019, 62-67. doi: 10.21608/aprh.2019.7629.1075
Ali, K., AboZeid, K., Nasr, M. (2019). 'In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers', Journal of Advanced Pharmacy Research, 3(2), pp. 62-67. doi: 10.21608/aprh.2019.7629.1075
Ali, K., AboZeid, K., Nasr, M. In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers. Journal of Advanced Pharmacy Research, 2019; 3(2): 62-67. doi: 10.21608/aprh.2019.7629.1075
In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers
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.