Ambrisentan oral tablets and preparation method thereof

Abstract

The invention provides ambrisentan oral tablets and a preparation method thereof. The ambrisentan tablets contain the following ingredients in parts by weight of 1 part of ambrisentan, 8-25 parts of lactose, 3-10 parts of microcrystalline cellulose, 0.3-1.0 part of croscarmellose sodium and 0.05-0.5 part of magnesium stearate. The prepared ambrisentan tablets are smooth in surface, good in contentuniformity, high in dissolution rate, small in dissolution differences between batches, high in in vivo biological availability, simple in preparation technology, easy to operate, low in cost and good in repeatability, and preparation quality and medication safety can be notably elevated.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an ambrisentan tablet and a production method thereof. Background technique [0002] Pulmonary arterial hypertension (PAH) is a specific type of PH and is a severe, progressive and life-threatening disease of the pulmonary vasculature characterized by extreme vasoconstriction and abnormal proliferation of smooth muscle cells in the walls of the pulmonary arteries. Severe constriction of blood vessels in the lungs results in very high pressure in the pulmonary arteries. These high pressures make it difficult for the heart to pump blood through the lungs for oxidation. Patients with PAH suffer from extreme shortness of breath as the heart works hard to pump against these high pressures. Patients with PAH typically develop a marked increase in pulmonary vascular resistance (PVR) and a sustained increase in pulmonary arterial pressure (PAP), which eventually l...

AI Technical Summary

Problems solved by technology

[0006] Ambrisentan is a poorly soluble drug, in water and 0.1mol L -1 It is almost insoluble in hydrochloric acid solution, and often encounters the problem of low dissolution rate or even unqualified in the actual production of tablets

And because the content of ambrisentan in the preparation is low, it is difficult to fully mix it during preparation, so there is often a problem of large dissolution differences between tablets when performing dissolution testing, especially when expanding production, the dissolution differences of each batch greater sex, directly affecting the safety and effectiveness of the drug

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