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马来酸依那普利口崩片:在高血压大鼠中的压片和体内评价。

Enalapril maleate orally disintegrating tablets: tableting and in vivo evaluation in hypertensive rats.

机构信息

a Department of Industrial Pharmacy, Faculty of Pharmacy , Assiut University , Assiut , Egypt.

b Department of Pharmaceutics, Faculty of Pharmacy , El-Minia University , El-Minia , Egypt.

出版信息

Pharm Dev Technol. 2018 Jun;23(5):496-503. doi: 10.1080/10837450.2017.1329318. Epub 2017 May 29.

Abstract

The aim of this study was to develop orally disintegrating tablets (ODTs) for enalapril maleate (EnM) to facilitate its administration to the elderly or other patients having dysphagia. Compatibility between EnM and various excipients was studied using differential scanning calorimetry. ODTs of EnM were prepared by direct compression of EnM mixtures with various superdisintegrants. The tablets were evaluated for physical properties including drug content, hardness, friability, disintegration time, wetting time, and drug release. The antihypertensive effect of the optimum EnM ODTs was evaluated in vivo in hypertensive rats and compared with commercial EnM formulation. EnM ODTs had satisfactory results in terms of drug content and friability. Tablet wetting and disintegration were fast and dependent on the used superdisintegrant where croscarmellose showed the fastest wetting and disintegration time of ∼7 s. EnM release from the tablets was rapid where complete release was obtained in 10-15 min. Selected EnM ODTs rapidly and efficiently reduced the rat's blood pressure to its normal value within 1 h, compared with 4 h for EnM commercial formulation. These results confirm that EnM ODTs could find application in the management of hypertension in the elderly or other patients having dysphagia.

摘要

本研究旨在开发马来酸依那普利(EnM)口腔崩解片(ODTs),以方便将其施用于老年人或其他有吞咽困难的患者。使用差示扫描量热法研究了 EnM 与各种赋形剂之间的相容性。通过将 EnM 混合物与各种超崩解剂直接压缩制备 EnM ODTs。对片剂的物理性质进行了评估,包括药物含量、硬度、脆碎度、崩解时间、润湿时间和药物释放。在高血压大鼠体内评估了最佳 EnM ODTs 的降压效果,并与市售 EnM 制剂进行了比较。EnM ODTs 在药物含量和脆碎度方面具有令人满意的结果。片剂的润湿和崩解速度很快,取决于所用的超崩解剂,其中交联羧甲纤维素的润湿和崩解时间最快,约为 7s。EnM 从片剂中的释放很快,在 10-15min 内即可完全释放。与 EnM 市售制剂需要 4 小时相比,所选 EnM ODTs 可在 1 小时内迅速有效地将大鼠的血压降低到正常水平。这些结果证实,EnM ODTs 可在治疗老年人或其他有吞咽困难的患者的高血压方面得到应用。

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