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29070

In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers

Article

Last updated: 03 Jan 2025

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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.

DOI

10.21608/aprh.2019.7629.1075

Keywords

Atorvastatin, bioavailability, hyperlipidemia, microwave, Poloxamer, Solid dispersion

Authors

First Name

Kholoud

Last Name

Ali

MiddleName

-

Affiliation

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ahram Canadian University, Egypt.

Email

kholoud.mohy@hotmail.com

City

cairo

Orcid

-

First Name

Khaled

Last Name

AboZeid

MiddleName

-

Affiliation

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ahram Canadian University, Egypt.

Email

khaledazeid@yahoo.com

City

cairo

Orcid

-

First Name

Mohamed

Last Name

Nasr

MiddleName

-

Affiliation

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Egypt.

Email

m2nasr@yahoo.com

City

Cairo

Orcid

-

Volume

3

Article Issue

2

Related Issue

5196

Issue Date

2019-04-01

Receive Date

2019-01-26

Publish Date

2019-04-01

Page Start

62

Page End

67

Print ISSN

2357-0547

Online ISSN

2357-0539

Link

https://aprh.journals.ekb.eg/article_29070.html

Detail API

https://aprh.journals.ekb.eg/service?article_code=29070

Order

3

Type

Research Article

Type Code

318

Publication Type

Journal

Publication Title

Journal of Advanced Pharmacy Research

Publication Link

https://aprh.journals.ekb.eg/

MainTitle

In vivo Absorption Study of Solid Dispersion Containing Atorvastatin Calcium in Human Volunteers

Details

Type

Article

Created At

22 Jan 2023