血压昼夜节律脉动片的处方与优化

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引用次数: 0

摘要

昼夜节律是人体的一个24小时周期,人体在上午相对于下午或晚上有不同的方面。血压在一天中有两个时间升高,一个在清晨,另一个在傍晚。本课题工作的目的是设计用于联合用药治疗血压的脉动片。在大多数情况下,血浆去甲肾上腺素水平和血浆肾上腺素活性在早晨增加;这两种激素都有可能引起冠状动脉血管收缩,因此,需要一种能在早晨达到药物血药浓度峰值并能控制早晨血压升高的制剂。在滞后期奈比洛尔的脉动释放与姜黄素的持续释放保持血压的严重度。采用稀释剂直接压缩超崩解法制备奈比洛尔芯片。F10批在短时间内释药效果良好,为最佳处方。奈比洛尔的缓释时间随包衣水平的增加而延长,而药物释放速度基本不变,无论包衣水平如何,奈比洛尔的缓释时间为8 ~ 8.5h, 9h后药物释放。药物缓释95%以上,姜黄素释放稳定。因此,这种方法可以提供一种有用的手段,可能有助于晨间BP患者,开发联合药物治疗的PDDS是克服单药(即奈比洛尔药物治疗)和口服给药副作用的一种有希望的方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation and Optimization of Pulsatile Tablet for Circadian Rhythm of Blood Pressure
Circadian rhythm is a 24-hour cycle of human body, the body different aspect in the morning as compare to afternoon or night. The blood pressure rises in two time in a day, one is at early morning and second one is at evening.The aim of present project work was to design the pulsatile tablet for treatment of blood pressure with combination drug therapy. in most cases it is seen that the increasing in Plasma norepinephrine level and plasma renin activity in the morning; both hormones are potential to induce coronary vasoconstriction, therefore, there is a need to a such formulation who achieve peak plasma concentration of drug at morning and can control morning spate of B.P. The pulsatile release of nebivolol after the lag time with sustain release of curcumin which maintain the severity of blood Pressure. The Formulation of Core tablet of nebivolol was prepared by using superdisintegrate by direct compression with diluent. F10 batch was found to be optimized formulation as it shown potent drug release within short time. The lag time was prolonged with an increase of the coating level, whereas the drug release rate was almost constant, irrespective of the coating level the lag time of nebivolol was found to be 8 to 8.5hrsand drug release after 9hrs. drug release was above 95% after lag time with constant release of curcumin. Hence, this approach can provide a useful means and may be helpful for patients with morning spate of BP and development of PDDS of combination drug therapy is a promising approach to overcome the side effect of single drug i.e. nebivolol drug therapy and also oral drug delivery.
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