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Preparation and evaluation of self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin.
J Pharm Pharmacol. 2006 Sep; 58(9):1183-91.JP

Abstract

Atorvastatin is insoluble in aqueous solution and the bioavailability after oral administration is low. Self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin have been successfully prepared to improve its bioavailability. SMEDDS is a mixture of lipid, surfactant, and cosurfactant, which are emulsified in aqueous medium under gentle digestive motility in the gastrointestinal tract. Pseudo-ternary phase diagrams composed of various excipients were plotted. Droplet size, zeta-potential and long-term physical stability of the formulations were investigated. The release of atorvastatin from SMEDDS capsules was studied using the dialysis bag method in 0.1 M HCl and phosphate buffer (pH 7.4), compared with the release of atorvastatin from a conventional tablet. A pharmacokinetic study was performed in 6 beagle dogs after oral administration of 6 mg kg-1 atorvastatin. The bioavailability of atorvastatin SMEDDS capsules was significantly increased compared with that of the conventional tablet. SMEDDS capsules consisting of Labrafil, propylene glycol and Cremophor RH40 provided the greatest bioavailability. Our studies indicate that the use of SMEDDS for the delivery of atorvastatin can improve its bioavailability.

Authors+Show Affiliations

Department of Pharmacy, Huashan Hospital, Fudan University, 12 Wulumuqi M. Road, Shanghai, 200040, China. hairong_shen@163.comNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

16945176

Citation

Shen, HaiRong, and MingKang Zhong. "Preparation and Evaluation of Self-microemulsifying Drug Delivery Systems (SMEDDS) Containing Atorvastatin." The Journal of Pharmacy and Pharmacology, vol. 58, no. 9, 2006, pp. 1183-91.
Shen H, Zhong M. Preparation and evaluation of self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin. J Pharm Pharmacol. 2006;58(9):1183-91.
Shen, H., & Zhong, M. (2006). Preparation and evaluation of self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin. The Journal of Pharmacy and Pharmacology, 58(9), 1183-91.
Shen H, Zhong M. Preparation and Evaluation of Self-microemulsifying Drug Delivery Systems (SMEDDS) Containing Atorvastatin. J Pharm Pharmacol. 2006;58(9):1183-91. PubMed PMID: 16945176.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and evaluation of self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin. AU - Shen,HaiRong, AU - Zhong,MingKang, PY - 2006/9/2/pubmed PY - 2006/12/27/medline PY - 2006/9/2/entrez SP - 1183 EP - 91 JF - The Journal of pharmacy and pharmacology JO - J Pharm Pharmacol VL - 58 IS - 9 N2 - Atorvastatin is insoluble in aqueous solution and the bioavailability after oral administration is low. Self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin have been successfully prepared to improve its bioavailability. SMEDDS is a mixture of lipid, surfactant, and cosurfactant, which are emulsified in aqueous medium under gentle digestive motility in the gastrointestinal tract. Pseudo-ternary phase diagrams composed of various excipients were plotted. Droplet size, zeta-potential and long-term physical stability of the formulations were investigated. The release of atorvastatin from SMEDDS capsules was studied using the dialysis bag method in 0.1 M HCl and phosphate buffer (pH 7.4), compared with the release of atorvastatin from a conventional tablet. A pharmacokinetic study was performed in 6 beagle dogs after oral administration of 6 mg kg-1 atorvastatin. The bioavailability of atorvastatin SMEDDS capsules was significantly increased compared with that of the conventional tablet. SMEDDS capsules consisting of Labrafil, propylene glycol and Cremophor RH40 provided the greatest bioavailability. Our studies indicate that the use of SMEDDS for the delivery of atorvastatin can improve its bioavailability. SN - 0022-3573 UR - https://www.unboundmedicine.com/medline/citation/16945176/Preparation_and_evaluation_of_self_microemulsifying_drug_delivery_systems__SMEDDS__containing_atorvastatin_ L2 - https://doi.org/10.1211/jpp.58.9.0004 DB - PRIME DP - Unbound Medicine ER -