FORMULATION AND IN VITRO EVALUATION OF EZETIMIBE RAPIDMELTS

T NEELIMA RANI; Y INDIRA MUZIB

doi:10.22159/ajpcr.2020.v13i5.36620

T NEELIMA RANI Department of Pharmaceutics, Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Visvavidyalayam (Women’s University), Tirupati, Andhra Pradesh, India.
Y INDIRA MUZIB Department of Pharmaceutics, Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Visvavidyalayam (Women’s University), Tirupati, Andhra Pradesh, India.

DOI https://doi.org/10.22159/ajpcr.2020.v13i5.36620

Abstract

Objective: The main objective of the present research was formulation and evaluation of ezetimibe rapidmelts.

Methods: As ezetimibe comes under Class II drug, solubility of the drug should be increased before formulation. For that solid dispersions were prepared with β-CD and PVP K-30 using coevaporation and kneading method. Among those solid dispersions prepared with β-CD (1:1.5) using coevaporation method has given better drug entrapment values compared to other solid dispersions. Those solid dispersions were formulated as rapidmelts using direct compression. In direct compression method, rapidmelts were prepared using superdisintegrants such as crospovidone, croscarmellose sodium, and starch 1500. Those are evaluated for both pre-compression and post-compression parameters. Rapidmelts of ezetimibe were prepared using sublimation method with subliming agents camphor, urea, and ammonium bicarbonate. The concentrations of subliming agents were found to be 2.5, 5.0, and 7.5%.

Results: Rapidmelts prepared using direct compression and sublimation methods were evaluated for weight variation, hardness, friability, % drug content, and disintegration time. The best formulation was subjected to stability testing for 6 months at 25°C/60% RH and 40°C/75% RH. All the prepared formulations compiled with the pharmacopeial limits. In all the formulations, results suggest that E12 formulation has given the best results.

Conclusion: From the result, it was concluded that rapidmelts prepared using sublimation method which has given better result than direct compression method. That final formulation was further evaluated for in vivo studies using rabbits.

Keywords: Ezetimibe, Nil, PEG 6000, PEG 4000, Coevaporation, Kneading, Direct compression, Sublimation, Superdisintegrants, Subliming agents

References

1. Rani TN, Muzib YI. Rapid melts: A review. Int J Pharm Chem Sci 2014;3:118-30.
2. Velmurugan S, Vinushitha S. Oral disintegrating tablets: An overview. Int J Chem Pharm Sci 2010;1:1-12.
3. Patidar K, kshirsagar MD, Saini V, Joshi PB, Soni M. Solid dispersion technology: A boon for poorly soluble drugs. Indian J Drug Deliv 2011;3:83-90.
4. Elbary AA, Ali AA, Aboud H. Enhanced dissolution of meloxicam from orodispersible tablets prepared by different methods. Bull Fac Pharm 2012;50:89-97.
5. Mahesh A, Shastri N, Sadanandam M. Development of taste masked fast disintegrating films of levocetirizine dihydrochloride for oral use. Curr Drug Deliv 2010;7:21-7.
6. Guptaa S, Hasnainb MS, Agarwala SS. Formulation and evaluation of oral disintegrating tablets of itopride hydrochloride using ion exchange resins as drug carrier. Asian J Pharm Sci 2012;7:207-18.
7. Raheem A, Singh R, Hiremath A, Nayak NS, Kamath KS. Formulation and comparative evaluation of ondansetron hydrochloride mouth dissolving tablets in India. Int J Pharm Pharm Sci 2019;11:57-64.
8. Agiba AM, Eldin AB. Insights into formulation technologies and novel strategies for the design of orally disintegrating dosage forms: A comprehensive industrial review. Int J Pharm Pharm Sci 2019;11:8-20.