Kaewnopparat N, Kaewnopparat S, Rojanarat W, Ingkatawornwong S
Prince of Songkla University, Hat-Yai, Songkla Thailand.
Int J Pharm Compd. 2004 Jul-Aug;8(4):310-2.
The objective of this study was to develop a rapid-release diazepam suppository. Four kinds of diazepam suppositories were formulated: (1) a conventional suppository with Witepsol H-15 as a base, (2) a conventional suppository with mixed polyethylene glycols as a base, (3) a hollow-type suppository with Witepsol H-15 as a base that contained diazepam solution in its cavity and (4) a hollow-type suppository with Witepsol H-15 as a base that contained diazepam powder in its cavity. The result of the differential scanning calorimetry thermograms indicated that diazepam dissolved in Witepsol base had a strong affinity to the lipophiic base while diazepam dispersed in polyethylene glycol base was still in the crystalline form. The release study of prepared suppositories showed that the release of diazepam from suppository 1 and suppository 4 was very slow. The diazepam released from suppository 2 after 5 minutes was about 30%. The diazepam released from suppository 3 after 5 minutes was about 85%, which was significantly faster than that of the other three formulations (1, 2, and 4). The hollow-type suppository that contained diazepam solution was found to be the most effective rapid-release formulation.
本研究的目的是研制一种速释地西泮栓剂。制备了四种地西泮栓剂：（1）以Witepsol H - 15为基质的常规栓剂；（2）以混合聚乙二醇为基质的常规栓剂；（3）以Witepsol H - 15为基质的中空型栓剂，其腔内含地西泮溶液；（4）以Witepsol H - 15为基质的中空型栓剂，其腔内含地西泮粉末。差示扫描量热法热谱图结果表明，溶解在Witepsol基质中的地西泮与亲脂性基质有很强的亲和力，而分散在聚乙二醇基质中的地西泮仍为结晶形式。对所制备栓剂的释放研究表明，栓剂1和栓剂4中地西泮的释放非常缓慢。栓剂2在5分钟后释放的地西泮约为30%。栓剂3在5分钟后释放的地西泮约为85%，明显快于其他三种制剂（1、2和4）。发现含有地西泮溶液的中空型栓剂是最有效的速释制剂。
