Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN, 46285, USA,
Drugs R D. 2013 Dec;13(4):281-8. doi: 10.1007/s40268-013-0030-8.
Orodispersible tablets (ODTs) are tablet or wafer forms of medication that disintegrate in the mouth, aided only by saliva. ODTs rely on different fast dissolve/disintegration manufacturing technologies.
Disintegration time differences for several olanzapine ODT forms were investigated. Risperdal M-Tab(®) was included as a non-olanzapine ODT comparator.
Eleven olanzapine ODT examples and orodispersible risperidone strengths were evaluated in vitro for formulation composition, manufacturing method, disintegration and dissolution characteristics, and formulation differences in comparison with freeze dried Zydis(®) ODT. Automated dissolution test equipment captured ODT dissolution rates by measuring real-time release of active ingredient. A high-speed video camera was used to capture tablet disintegration times in warm simulated saliva.
The main outcome measure was the disintegration and dissolution characteristics of the ODT formulations.
The ODT manufacturing method was associated with time to disintegrate; the fastest were freeze dried tablets, followed by soft compressed tablets and then hard/dense tablets. Olanzapine Zydis(®) was the only ODT that completely disintegrated in less than 4 s for all strengths (5, 10, 15, and 20 mg), followed by 5-mg Prolanz FAST(®) (12 s) and then risperidone ODT 4 mg (40 s). Reasons for slow dissolution of the olanzapine generics may include low product potency, excipient binding, excipient solubility, active ingredient particle size and incomplete disintegration.
Differences in the formulation and manufacturing process of olanzapine ODTs appear to have a strong influence on the disintegration time of the active compound; differences that may potentially impact their use in clinical practice.
口崩片（ODTs）是指在口腔中崩解的片剂或薄片面剂，仅靠唾液就能帮助崩解。ODTs 依赖于不同的快速溶解/崩解制造技术。
研究了几种奥氮平 ODT 形式的崩解时间差异。利培酮 M-Tab（®）作为非奥氮平 ODT 对照物被纳入研究。
对 11 种奥氮平 ODT 样本和速溶利培酮制剂进行了体外评估，评估内容包括配方组成、制造方法、崩解和溶解特性，以及与冻干 Zydis（®）ODT 的配方差异。自动溶解测试设备通过实时测量活性成分的释放来捕捉 ODT 溶解速率。高速摄像机用于在温暖的模拟唾液中捕捉片剂崩解时间。
主要观察指标是 ODT 配方的崩解和溶解特性。
ODT 的制造方法与崩解时间有关；崩解最快的是冻干片剂，其次是软压片剂，然后是硬片剂。奥氮平 Zydis（®）是唯一一种所有规格（5、10、15 和 20mg）在 4 秒内完全崩解的 ODT，其次是 5mg Prolanz FAST（®）（12 秒），然后是利培酮 ODT 4mg（40 秒）。奥氮平仿制药溶解缓慢的原因可能包括产品效力低、赋形剂结合、赋形剂溶解度、活性成分粒径和不完全崩解。
奥氮平 ODT 的配方和制造工艺差异似乎对活性化合物的崩解时间有很强的影响；这些差异可能会对它们在临床实践中的应用产生影响。
