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目的研制在唾液中迅速崩解,含高剂量活性成分37.5%(W/W)的片剂。方法分别通过直接压片、湿法制粒和模制法制备含罗通定、崩解剂和其它赋形剂的口腔崩解片。应用单因素实验选择使用不同的崩解剂和赋形剂以确保最佳崩解。同时按照常规药典方法和润湿时间测定方法测定崩解时间。结果通过直接压片得到的硬度40kg·mm-2的片剂(80mg)在健康志愿者口腔中于15秒内快速崩解;湿法制粒所得片剂也具足够硬度,崩解时间稍长但可接受(口腔中25秒内);模制法所得片剂在口腔中40秒内崩解,但硬度低(2kg·mm-2)。三种不同制备方法所得片剂的崩解时间与各自的润湿时间相似。体外崩解时间和润湿时间均和体内崩解时间相似,后者和口腔内崩解时间显示更好的相关性。结论可以通过上述三种方法和片剂制备中的常用赋形剂制备口腔崩解片。体外崩解时间和润湿时间是评价口腔崩解片体外崩解时间的必要指标。
Objective To develop a tablet that rapidly disintegrates in saliva and contains a high dose of 37.5% (W / W) of the active ingredient. Methods Orally disintegrating tablets containing lootidine, disintegrant and other excipients were prepared by direct compression, wet granulation and molding respectively. The use of single factor experiments chose to use different disintegrants and excipients to ensure optimal disintegration. The disintegration time was determined according to the routine Pharmacopoeia method and the wetting time determination method. Results Tablets (80 mg) with a hardness of 40 kg · mm-2 obtained by direct compression quickly disintegrated in the oral cavity of healthy volunteers in 15 seconds; tablets obtained by wet granulation also had sufficient hardness and slightly longer disintegration time Acceptable (within 25 seconds in oral cavity); tablets obtained by molding disintegrate within 40 seconds in the oral cavity, but with low hardness (2 kg · mm-2). The disintegration time of the tablets obtained by the three different preparation methods is similar to the respective wetting time. Both the in vitro disintegration time and the wetting time are similar to the in vivo disintegration time, which shows a better correlation with the oral disintegration time. Conclusion Orally disintegrating tablets can be prepared by the above-mentioned three methods and the usual excipients used in tablet preparation. The in vitro disintegration time and the wetting time are necessary indicators for evaluating the in vitro disintegration time of orally disintegrating tablets.