Fast dissolving Tablet Formulation and Evaluation: Effort to Enhance Solubility of Angiotensin II Receptor Antagonist (ARB) Telmisartan Antihypertensive Drug

Author: Jadhav A.B., Nawale R.B. and Khan M.A.

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Abstract

An Angiotensin II receptor antagonist (ARB) Telmisartan is the Antihypertensive category drug used in the management of hypertension (HTN); it is a BCS class II medication. The low solubility of drugs place restrictions on formulation development and drug delivery. The present research work was aimed to improve the solubility of Telmisartan by solid dispersion technique, which will enhance the oral bioavailability of the drug. Solid dispersion of Telmisartan was prepared using Poloxamer 407 and Poloxamer 188 as a carrier and subsequently fast dissolving tablets using croscarmellose sodium and crospovidone as super disintegrants while mannitol as taste enhancer. During the preliminary formulation studies, it was found that the effect of croscarmellose sodium and crospovidone showed positive response on the % drug release and disintegration time of the tablet. Formulation M9 having 5% of croscarmellose sodium and 6% of crospovidone produces best effect and has 97.49 % release. This formulation had disintegration time of 31 sec. and shown better mechanical strength. Formulation M9 was compared with marketed product of Telmisartan tablets which shown 92.46 % drug release in 1 hr. From this observation it was predict that the formulated tablets of Telmisartan (M9) were improved and effective and hence can conclude that the solubility of Telmisartan increased

Keywords

Telmisartan, solubility enhancement, solid dispersion

Conclusion

The study was aimed to improve the solubility of poorly soluble antihypertensive drugs using Solid dispersion technique. It was observed that for preparation of solid dispersion, fusion method was selected with drug: Poloxamer 188 in 1:1 proportion and using this solid dispersion fast dissolving tablet with superdisintegrants croscarmellose sodium and crospovidone were formulated. Design expert software, version 11.1.2.0 was used to generate statistical model. It was found that the tablet showed minimum disintegration time (31 sec) and maximum (97.49 %) drug release at 5% of croscarmellose sodium and 6% of crospovidone viz., batch M9. The final optimized formulation (M9) was compared with marketed product of Telmisartan tablets which shows 92.46 % drug release in 1 hr. From this observation it was concluded that the formulated tablets of Telmisartan (M9) were better as shown better dissolution

References

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How to cite this article

Jadhav A.B., Nawale R.B. and Khan M.A. (2023). Fast dissolving Tablet Formulation and evaluation: Effort to enhance solubility of Angiotensin II receptor antagonist (ARB) Telmisartan Antihypertensive drug. Biological Forum – An International Journal, 15(1): 780-789