Formulation and Evaluation of Ezetimibe Lyophilized Dry Emulsion Tablets
This article presents the development of lyophilized dry emulsion tablets prepared with the dry emulsion technique to enhance the in-vitro dissolution and in-vivo performance of the poorly bioavailable drug Ezetimibe. Ezetimibe (EZT) is a lipid-lowering drug that inhibits intestinal uptake of dietary and biliary cholesterol without affecting the absorption of fat-soluble nutrients. Ezetimibe has a very low solubility and dissolution rate resulting in highly variable bioavailability, which is also in part due to extensive efflux by p-glycoprotein (P-Gp). Tablets were fabricated by freezedrying o/w emulsions of Ezetimibe. The Emulsions were prepared using a matrix former solution (alginate or gelatin, 2 or 4%) containing a sugar alcohol (mannitol), as the water phase and Labrafac® as the oil phase under proper homogenization. In the present study friability, disintegration time, and in-vitro dissolutionof lyophilized dry emulsion tablets were done. Results showed the significant influence of the matrix former and emulsifier type on the disintegration time. In-vitro dissolution studies revealed the enhanced dissolution rate of Ezetimibe from the lyophilized tablets compared to the plain drug. DSC studies proved presence of the drug in the amorphous form in the fabricated tablets. The obtained results suggest a promising, easy-to-manufacture and effective dosage form for the treatment of hyperlipidemia.
Keywords: Ezetimibe, lyophilized dry emulsion tablet, and hyperlipidemia, freeze drying, Labrafac.
2. Patil PP, Kate V, Payghan S, Potential Investigation of Peceol for formulation of Ezetimibe self nano emulsifying Drug Delivery Systems Asian Journal of Biomedical and Pharmaceutical Sciences, 2016, 21-32.
3. Patil PP, Kate V, Payghan S, Development and Stability Assessment of Solid Self-micro Emulsifying System for Oral Bioavailability of Ezetimibe using Spray-drying Technique, Inventi Rapid: Pharmaceutical Process Development, 2016, 1-8.
5. Niczinger NA, Barnab´as K´allai S, Lengyel P, Antal K, Physicochemical analysis in the evaluation of reconstituted dry emulsion tablets, Journal of Pharmaceutical and Biomedical Analysis, 2016, 1-16.
6. Aulton, M.E, Pharmaceutics: The Science of Dosage Form Design. 2nd ed. Churchill Livingstone, Edinburgh, Scotland, 2002, 390-393.
7. Vora, N., Rana, V, Preparation and optimization of mouth/orally dissolving tablets using a combination of glycine, carboxymethyl cellulose and sodium alginate: a comparison with superdisintegrants, Pharmaceutical development and technology 2013, 233-243.
8. Stange U, Fuhrling C, Gieseler H, Formulation, preparation, and evaluation of novel orally disintegrating tablets containing taste-masked naproxen sodium granules and naratriptan hydrochloride, Journal of pharmaceutical sciences 103, 2014 1233-1245.
9. Liling G, Jiachao X, Xin G, Xiaoting F, Qing, Z, Effects of ionic crosslinking on physical and mechanical properties of alginate mulching films. Carbohydrate polymers 136, 2016, 259-265.
10. Sastry, SV, Nyshadham, JR, Fix, JA, Recent technological advances in oral drug delivery - a review. Pharmaceutical science & technology today 3, 2000, 138-145.
11. Xing, Q, Yates, K, Vogt, C, Qian, Z, Frost, MC, Zhao, F, Increasing mechanical strength of gelatin hydrogels by divalent metal ion removal. Scientific reports 4, 2014, 4706.
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