Ezetimibe orally disintegrating tablet and preparation method thereof

Abstract

The invention discloses an orally disintegrating tablet which takes ezetimibe as an effective ingredient and has an effect of treating hypercholesteremia and a preparation method thereof. Regarding the problem of poor water solubility of ezetimibe, under the condition that a surfactant is not used, on the one hand, the grain diameter is reduced by adopting a micronization technology or the disintegrating tablet is prepared into a solid dispersion so as to improve the solubility, and on the other hand, the tablet can be quickly disintegrated in the oral cavity by means of the formula, so that the disintegrating tablet can be dissolved quickly. Furthermore, the invention aims to provide the ezetimibe orally disintegrating tablet which is simple in preparation process, convenient to take, quick in response and remarkable in curative effect; the orally disintegrating tablet can be taken without drinking water, can be quickly disintegrated in tens of seconds in the oral cavity, and is especially suitable for old people, children and patients with swallowing difficulty.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an ezetimibe orally disintegrating tablet and a preparation method thereof. Background technique [0002] Ezetimibe is an oral, potent lipid-lowering drug. It is the first selective cholesterol absorption inhibitor jointly developed by Schering-Plough and Merck. This product is the first cholesterol absorption drug approved by the US FDA. Selective inhibitor drugs, trade name Zetia. The product was approved by the FDA on October 25, 2002 and launched in the United States on November 30, 2002. Currently, ezetimibe is mainly used for the treatment of primary hypercholesterolemia, homozygous familial hypercholesterolemia, homozygous familial sitosterolemia and mixed hyperlipidemia. [0003] Its mechanism of action is to attach to the brush border of small intestinal villi, inhibit the absorption of cholesterol, thereby reducing the transfer of cholesterol fro...

AI Technical Summary

Problems solved by technology

[0005] Ezetimibe is insoluble in water, and when its solid dosage form is used orally, common formulations such as tablets often limit its bioavailability due to its dissolution rate, thereby affecting the efficacy of the drug

[0006] At present, there is no public information about ezetimibe orally disintegrating tablets, and its oral solid preparations on the market are ordinary tablets. Therefore, a kind of ezetimibe orally disintegrating tablets was invented. It can disintegrate quickly within seconds, and is suitable for the elderly, children and patients with dysphagia. It is a topic worthy of research

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