延胡索酸泰妙菌素口服固体制剂体外溶出度的探究

Dissolution Rate of Tiamulin Fumarate Solid Oral Preparation Using in Vitro Method

本试验旨在评价延胡索酸泰妙菌素口服固体受试制剂和参比制剂的体外溶出度。试验采用桨法测定溶出度,50rpm/min,溶出介质分别为pH1.2盐酸溶液、pH3.8醋酸盐缓冲液、pH4.8磷酸盐缓冲液、pH6.8磷酸盐缓冲液和水,温度37±0.5℃,参比制剂和受试制剂0.34g/杯,取样时间为第1、2、5、10、15、30、45和60min,高效液相色谱法检测药物成分含量。结果表明延胡索酸泰妙菌素在溶出介质中比较稳定,受试制剂和参比制剂在15min内的溶出率大于85%,在五个溶出介质中的差异因子(f1)小于15%。因此,受试制剂和参比制剂的溶出行为相似,生物利用度不受溶出行为的限制。

This experiment was conducted to evaluate the dissolution rate of tiamulin fumarate solid oral preparation in vitro. The paddle method at 50 rpm and 37±0.5 ℃ was used. The dissolution medium were pH 1.2 hydrochloric acid solution, pH 3.8 acetic acid salt buffer, pH 4.8 and pH 6.8 phosphate buffer and water,respectively. The reference and the test preparation were 0.34 g per cup. Sampling at 1, 2, 5, 10, 15, 30, 45 and 60 min was collected for the rapid dissolving characteristics. The tiamulin fumarate in the dissolution mediums was detected by the high performance liquid chromatography. T h e tiamulin fumarate was stable in the dissolution mediums. T h e dissolution rates of the reference and the test preparations were more than 85 percent. The difference factor(f1) between the reference and the test preparations in the dissolution mediums was less than 15 percent. In conclusion, dissolution profiles of the reference and the test preparation are similar. The dissolution behaves like a solution and have no bioavailabilityproblems.