Telmisartan enteric-coated tablets and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to telmisartan enteric-coated tablets and a preparation method thereof. The telmisartan enteric-coated tablets are each composed of a tablet core, an isolating layer and an enteric coating. The table cores are composed of, by weight, 20-40 parts of telmisartan, 8-20 parts of poly-L-arginine, 10-60 parts ofmannitol, 60-160 parts of microcrystalline celluloses, 3-9 parts of povidone and 0.5-3 parts of magnesium stearate. Poly-L-arginine is adopted for alkalizing telmisartan, in this way, the solublenessof telmisartan can be improved remarkably, and moisture absorption is reduced; meanwhile, mannitol is added, in this way, powder with good fluidity can be obtained, and the prepared tablets are high in dissolution rate and good in stability; common rapid-disintegration oral administration preparations are prepared into the enteric-coated tables, in this way, it can be avoided that the preparationsdisintegrate in gastric acid, and telmisartan is separated out, the bioavailability of telmisartan is improved remarkably, and application prospects are good.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a telmisartan enteric-coated tablet and a preparation method thereof. Background technique [0002] Telmisartan is a specific non-peptide angiotensin II receptor (AT1 type) antagonist developed by Karl Thomae GmbH (Karl Thomae) and approved to be marketed in the United States and the European Union in 1998 under the trade name Micardis (Mecasuol). Telmisartan can selectively and irreversibly block the binding of angiotensin II to AT1 receptors in many tissues (such as vascular smooth muscle and adrenal gland), thereby blocking the vasoconstriction and aldosterone secretion of angiotensin II, so that Blood pressure is lowered, but it does not affect other receptor systems in cardiovascular regulation, and has a good application prospect. [0003] However, telmisartan belongs to Class II in the BCS classification, and has low solubility, low dissolution rate...

AI Technical Summary

Problems solved by technology

However, it has been found in practice that when telmisartan is alkalized to make enteric-coated tablets, its contents are likely to interact with the enteric coating, which may easily cause cracks in the coating layer, moisture absorption, and poor stability.

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