降压药替米沙坦漂浮微球的研制及评价

Shikha Baghel Chauhan, Sakshi Nainwani
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引用次数: 0

摘要

替米沙坦是治疗高血压的最佳选择之一,无论是联合用药还是单独用药。替米沙坦属于II类拮抗剂血管紧张素转换酶抑制剂。高血压的主要原因之一是血管收缩,因此血压升高可以通过具有血管收缩特性的药物来控制替米沙坦就是其中之一,它还可以放松血管。这里选择的剂型是漂浮微球,因为它可以在很长一段时间内持续释放药物。漂浮微球有漂浮在胃液上的倾向,因此增加了胃潴留时间。这些是优于传统形式,因为它们提供减少胃刺激的优势,较少的给药频率将需要,因为它提供缓慢的持续释放延长的时间。本研究旨在制备替米沙坦漂浮微球并对其进行评价。所采用的工艺是磁力搅拌器溶剂蒸发法。已经配制的替米沙坦微球具有较低的生物利用度、药物夹带和较低的释放动力学,因此我们的主要目标是配制这样一种具有更高生物利用度、药物夹带和更大动力学释放的制剂,为了配制这样的制剂,我们选择使用不同比例的聚合物Eudragit RS 100、乙基纤维素和恒定剂量的药物。配制后,进行各种表征,包括微量物学性质、漂浮效率、溶解度、药物包封效率以及产率和释放动力学。研究表明,以不同比例使用一种以上的聚合物对微球的各个参数都有影响。
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Formulation and Evaluation of Floating Microspheres for an Antihypertensive drug Telmisartan
Telmisartan is one of the best options either in combination or alone, to treat hypertension. telmisartan belongs to class II antagonist angiotensin converting enzyme inhibitor. One of the main causes of hypertension is vasoconstriction of blood vessels hence increasing blood pressure which can be controlled by drugs that have vasoconstriction property and telmisartan is one of them, and it also relaxes the blood vessels. The dosage form opted here is floating microspheres as it can provide sustain release of drug over long period of time. Floating microspheres have a tendency to float over gastric fluid hence increasing gastric retention time. These are preferred over conventional form as they provide advantage of reducing gastric irritation, lesser dosing frequency will be required as it provide slow continuous release for prolong period of time. The present research aims to formulate telmisartan floating microspheres and its evaluation. The technique used is solvent evaporation method by using magnetic stirrer. Already formulated telmisartan microspheres have lower bioavailability, drug entrapment and lower release kinetics so our main aim is to formulate such a preparation which have greater bioavailability, drug entrapment and greater kinetic release, and to formulate such a formulation we have opted using variant ratios of polymer Eudragit RS 100, Ethyl Cellulose with constant dose of drug. After formulation, various characterization is done that include micromeritics properties, floating efficiency, solubility, drug entrapment efficiency along with yield and release kinetics. The study revealed that, using a more than one polymer in a different ratio have an impact on every parameter of microspheres.
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