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Formulation development and rheological studies of palatable cefetamet pivoxil hydrochloride dry powder suspension

机译:可口的头孢他美盐必治西盐酸盐干粉悬浮液的配方开发和流变学研究

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Background and the purpose of the studyBecause of its intense bitter taste and susceptibility to moisture Cefetamet Pivoxil (CPH) is presently available only in the form of tablet. The aim of this study was to develop taste masked CPH dry powder suspension.MethodsMethods employed for formulations were: a) Film coating of CPH using Eudragit E100 and subsequent adsorption on different carriers such as spray-dried lactose, sodium starch glycolate and spray-dried mannitol and b) Complexation of CPH with three different ion exchange resins indion 234 amberlite IRP64 and amberlite IRP69.ResultsTaste viz evaluation as recognized by volunteers revealed that coating with Eudragit E100 and subsequent adsorption on different carriers do not mask the bitter taste of the drug. Suspensions prepared using amberlite IRP64 and amberlite IRP69 were extremely palatable with no bitter after taste. They showed pseudoplastic flow behavior and were too viscous even after shearing for sufficient duration of time and exhibited poor pourability. The suspension made with indion 234 was palatable with slight or no bitter after taste. It demonstrated plastic flow with negligible thixotropy. It had moderate viscosity at rest and could be poured after a reasonable amount of shaking. CPH dry powder suspensions were very unstable under different conditions except under refrigeration. A 5% degradation of drug was occurred in reconstituted suspension in 4 days period when stored at room temperature.ConclusionDry powder suspension prepared with indion 234 having 5% overages was stable even after 4th day of reconstitution and palatable with slight or no bitter after taste.
机译:研究的背景和目的由于其强烈的苦味和对水分的敏感性,目前仅以片剂形式提供头孢他美酯(CPH)。这项研究的目的是开发掩味的CPH干粉悬浮液。方法制剂所采用的方法是:a)用Eudragit E100对CPH进行膜包衣,然后吸附在不同的载体上,如喷雾干燥的乳糖,淀粉羟乙酸钠和喷雾干燥甘露醇和b)CPH与三种不同的离子交换树脂Indion 234 Amberlite IRP64和Amberlite IRP69的络合。结果自愿者对口味的评估发现,Eudragit E100的包衣和随后在不同载体上的吸附不会掩盖药物的苦味。使用Amberlite IRP64和Amberlite IRP69制备的悬浮液非常可口,且没有苦味。它们表现出假塑性流动行为,即使在剪切足够长的时间后仍太粘,并且显示出较差的可倾倒性。用靛蓝234制成的悬浮液是可口的,味淡或无苦味。它表现出塑性流动,触变性可忽略不计。它在静止时具有适度的粘度,可以在合理的摇动量后倒出。 CPH干粉悬浮液在不同条件下(冷藏除外)非常不稳定。在室温下放置4天后,重构的悬浮液中药物的降解率为5%。结论用重度为5%的indion 234制备的干粉悬浮液即使在重构的第4天仍是稳定的,并且可口,味淡或无苦味。

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