Dissolution evaluation in vitro and bioavailability in vivo of self-microemulsifying drug delivery systems for pH-sensitive drug loratadine. (March 2015)

• Record Type: Journal Article
• Authors: Li, Haiyan; Tan, Yonggang; Yang, Lixia; Gao, Lijun; Wang, Tao; Yang, Xi; Quan, Dongqin
• Is Part Of: Journal of microencapsulation. Volume 32:Number 2(2015:Mar.)
• Page Start: 175
• Page End: 180
• Publication Date: 2015-03
• Subjects: Microencapsulation -- Periodicals; Controlled release technology -- Periodicals; 615.19
• DOI: 10.3109/02652048.2014.985340
• Languages: English
• ISSNs: 0265-2048

Abstract

<abstract> <title>Abstract</title> <p>The aim of this study was to improve the oral absorption of loratadine, a pH-sensitive drug, by self-microemulsifying drug delivery systems (SMEDDSs). The optimal SMEDDS was analysed and evaluated after emulsification in distilled water with diameter of 26.57 ± 0.71 nm and zeta potential of −30.5 ± 4.5 mV. Dissolution experiments <italic>in vitro</italic> were carried out in different released media of pH values and the SMEDDS formulations were able to release loratadine completely in different media while market tablets just performed similarly in the media of pH 1.2. Furthermore, the oral bioavailability and the pharmacokinetic behaviour of loratadine formulations <italic>in vivo</italic> were studied after a single dose of 1 mg/kg loratadine in beagle dogs. The SMEDDS formulations displayed higher <italic>C</italic>_max and AUC, approximately 9 and 5 times increase than those of market tablets (<italic>p</italic> &lt; 0.01) respectively. These results demonstrated that SMEDDS formulations had significantly increased the oral absorption of loratadine in beagle dogs.</p> </abstract>