Li Haiyan, Tan Yonggang, Yang Lixia, Gao Lijun, Wang Tao, Yang Xi, Quan Dongqin
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences , Beijing , China.
J Microencapsul. 2015;32(2):175-80. doi: 10.3109/02652048.2014.985340. Epub 2014 Nov 21.
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 in vitro 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 in vivo were studied after a single dose of 1 mg/kg loratadine in beagle dogs. The SMEDDS formulations displayed higher Cmax and AUC, approximately 9 and 5 times increase than those of market tablets (p < 0.01) respectively. These results demonstrated that SMEDDS formulations had significantly increased the oral absorption of loratadine in beagle dogs.
本研究的目的是通过自微乳化药物递送系统（SMEDDS）来提高对pH敏感的药物氯雷他定的口服吸收。在蒸馏水中乳化后对最佳SMEDDS进行分析和评估，其直径为26.57±0.71nm，ζ电位为-30.5±4.5mV。在不同pH值的释放介质中进行体外溶出实验，SMEDDS制剂能够在不同介质中完全释放氯雷他定，而市售片剂仅在pH 1.2的介质中表现相似。此外，在比格犬单次给予1mg/kg氯雷他定后，研究了氯雷他定制剂在体内的口服生物利用度和药代动力学行为。SMEDDS制剂显示出更高的Cmax和AUC，分别比市售片剂增加了约9倍和5倍（p<0.01）。这些结果表明，SMEDDS制剂显著提高了氯雷他定在比格犬中的口服吸收。
