The Faculty of Pharmacy discussed the master’s degree thesis, tagged “Preparation and Characterization of Telmisartan Solid Dispersion Systems for Administration as Sublingual Tablets,” by Hiba Ayad Aziz and her supervisor, Assist. Prof. Dr. Entidhar J. Al-Akkam, of the Department of Pharmaceutics, on August 9, 2023. The aim of this study was to prepare sublingual tablets of TEL by improving the solubility and dissolution rate of TEL through its incorporation into solid dispersion. Telmisartan (TEL) is an antihypertensive angiotensin II receptor antagonist drug commonly used to treat hypertension and renal disease. It belongs to class II (poorly soluble drug) according to the Biopharmaceutical Classification System (BCS). Forty-nine formulas of binary solid dispersion of TEL (20 mg) were prepared by using different types of hydrophilic carriers (PEG4000, PEG6000, poloxamer 407, poloxamer 188, and Soluplus), different drug carrier ratios (1:1, 1:2, and 1:3), and different methods of preparation (solvent evaporation, kneading, and microwave method). Results showed that Soluplus® gave the highest improvement in solubility of TEL and was considered the most effective carrier at a ratio of drug: carrier 1:3, as represented by F49 of binary SD, which was prepared by microwave method. Then, to get more effective results, a carrier that produced the highest improvement in solubility and dissolution of TEL was applied for the preparation of 14 formulas of ternary solid dispersion by adding potassium carbonate salt at different ratios. The best result of ternary solid dispersion was represented by F61, composed of TEL, Soluplus, and K2CO3 salt at a ratio of 1:1:0.3 and prepared by the microwave method. Formula F61 exhibited the best results of improvement in solubility and dissolution of TEL. It was processed to the analysis technique (differential scan calorimeter, Fourier transformation infrared, and X-ray diffraction), then applied for the preparation of sublingual tablets (T1-T6) by direct compression using different types and ratios of superdisintegrants (crospovidone, croscarmellose, and sodium starch glycolate at 5% and 10%). After the evaluation tests, the best formula was selected. In addition, the best formula of TEL sublingual tablets was represented by T6, which was composed of TEL, Soluplus, K2CO3 salt at a ratio of 1:1:0.3, and crospovidone at 10%. It exhibited the most acceptable evaluation parameters: hardness of 2.4 kg, friability of 0.08, disintegration time of 10 sec, drug content of 100%, and 100% release in 40 sec. The stability study indicated the stability of the selected formula after 4 months and was not affected by different temperatures. In conclusion, the solubility and dissolution of TEL were successfully improved by a solid dispersion approach and administered as sublingual tablets for increasing patient compliance with renal failure.
