Preparation and Evaluation of Telmisartan Solid Dispersion as Sublingual Tablets

Journal of the Faculty of Medicine Baghdad Pub Date : 2024-01-01 DOI:10.32007/jfacmedbagdad.2145

Hiba Ayad Aziz, Entidhar J. Al-Akkam

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Abstract

Background: Telmisartan is an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension and renal disease. Based on the Biopharmaceutical Classification System. It’s a Class II poorly soluble drug. Objective: To prepare a sublingual tablet by increasing the dissolution and solubility of Telmisartan utilizing the solid dispersion method. Methods: Three methods were obtained to prepare the solid dispersion of telmisartan: solvent evaporation, Kneading, and microwave method. Each method uses surplus as a hydrophilic carrier in different ratios of 1%, 2%, and 3%. Preparation of ternary solid dispersion by adding potassium carbonate salt to the binary solid dispersion. After that preparing the sublingual tablets by applying a direct compression method, using different types and ratios of superdisintegrants such as crospovidone, croscarmellose and sodium starch glycolate in 5% and 10%. Study the evaluation tests of sublingual tablets, such as friability, hardness, disintegration time and dissolution time. Results: The solid dispersion showed an improvement in solubility over the pure medication. The best result was obtained with the formula (Telmisartan, soluplus and k2co3 salt at 1:1:0.3 ratio) prepared by microwave method, in this method and the high ratio of soluplus, the solubility increased more than the solvent evaporation and kneading method. The selected tablet is prepared using crospovidone 10% as a superdisintegrant that appears disintegration time in 5 seconds and releases in 1 min in dissolution media. Conclusion: The solubility and dissolution of Telmisartan were improved by microwave-based ternary solid dispersion using hydrophilic carriers and salt in a ratio of 1:1:0.3 (drug: carrier: salt). The analysis exerts the increases in wettability, enhanced solubility, and dissolution due to conversion from crystal to amorphous state. Received May. 2023 Accepted Aug. 2023 Published Jan. 2024

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制备和评估作为舌下片剂的替米沙坦固体分散体

背景：替米沙坦是一种抗高血压血管紧张素 II 受体拮抗剂，常用于治疗高血压和肾病。根据生物制药分类系统，它属于第二类难溶性药物。目标：制备舌下含片：利用固体分散法提高替米沙坦的溶解度和可溶性，制备舌下片剂：方法：用三种方法制备替米沙坦的固体分散体：溶剂蒸发法、捏和法和微波法。每种方法都使用剩余物作为亲水性载体，比例分别为 1%、2% 和 3%。在二元固体分散体中加入碳酸钾盐，制备三元固体分散体。研究舌下片剂的评估测试，如易碎性、硬度、崩解时间和溶解时间：结果：与纯药物相比，固体分散体的溶解度有所提高。用微波法制备的配方（替米沙坦、苏合香和 k2co3 盐的比例为 1:1:0.3）效果最好，该方法和高比例的苏合香比溶剂蒸发法和捏合法的溶解度提高得更多。所选片剂使用 10%的氯磺丙酮作为超崩解剂，在溶解介质中的崩解时间为 5 秒，释放时间为 1 分钟：使用亲水性载体和盐以 1:1:0.3 的比例（药物：载体：盐）进行微波三元固体分散，可提高替米沙坦的溶解度和溶出度。分析结果表明，由于从晶体状态转化为无定形状态，该药物的润湿性、溶解性和溶解度均有所提高。2023 年 8 月接受 2024 年 1 月发表

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Journal of the Faculty of Medicine Baghdad

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