PREPARATION AND EVALUATION OF RAPIDLY DISSOLVING ‎TABLET OF TELMISARTAN

Ali Shatla,Mohamed Osman

doi:10.21608/aprh.2018.2848.1050

Ali Shatla, Mohamed Osman

Open Access

https://doi.org/10.21608/aprh.2018.2848.1050

Copy DOI

Abstract

Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate. Conclusion: sodium bicarbonate can be utilized in the preparation of telmisartan FDT ‎with fast dissolution rate.‎

Highlights

Telmisartan is 2-(4-{[4-methyl-6-(1-methyl1H-1, 3 benzodiazol-2-yl) -2-propyl-1H-1, 3benzodiazol-1-yl methyl} phenyl) benzoic acid (Figure 1), approved as antihypertensive agent[1]
The recorded endothermic peak correlates with the specifications of the supplier which indicated that the melting point of the drug is in the range of 266.37273.37 °C
The pure hydroxypropyl methylcellulose E5 (HPMC E5) thermogram showed the melting point in the range of 313.71-373.93 °C (Figure 3A). This is similar to that recorded by other investigators[6,13] but it is important to note that the recorded thermograms of HPMC did not show the endothermic peak of the bound moisture indicating the dryness of the polymer

Summary

Introduction

Telmisartan is 2-(4-{[4-methyl-6-(1-methyl1H-1, 3 benzodiazol-2-yl) -2-propyl-1H-1, 3benzodiazol-1-yl methyl} phenyl) benzoic acid (Figure 1), approved as antihypertensive agent[1]. It exerts its action via competitive inhibition of the angiotensinconverting enzyme (ACE) with higher selectivity for (AT1) than (AT2) receptor. The poor solubility of telmisartan in biological fluids is one of its major problems which accounts for low bioavailability that reaches 42 % after oral administration. It shows high first-pass metabolism, which further reduces the oral bioavailability 5. The Optimizing drug dissolution rate is the main http://aprh.journals.ekb.eg/ 191

Methods

Results

Conclusion