Solid oral preparation containing telmisartan and preparation method thereof

Abstract

The invention provides a solid oral preparation without a surfactant. The solid oral preparation comprises the following components in percentage by weight: 5-25% of telmisartan, an alkaline reagent and the balance of pharmaceutically acceptable vectors, wherein the weight of the alkaline reagent is equal to 7-20% of that of telmisartan. The invention also provides a method for preparing the solid oral preparation. The preparation prepared by the method can be quickly and sufficiently released in the psychophysical pH range of gastrointestinal tracts; and compared with the prior art, the preparation method has the advantages that the process is simpler, the quality of the soli oral preparation is more stable, the cost is greatly saved, and the efficiency is improved.

Description

technical field [0001] The present invention relates to a solid oral preparation containing telmisartan, more specifically to a tablet containing telmisartan. The invention also provides a tablet preparation method suitable for industrial production. Background technique [0002] Telmisartan is an angiotensin II receptor antagonist developed for the treatment of hypertension and other medical conditions. Its chemical name is 4'-[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)benzimidazol-1-ylmethyl]biphenyl-2-carboxylic acid common chemical name. The CAS registry number is 144701-48-4. Molecular formula is C 33 h 30 N 4 o 2 , and its molecular weight is 514.63. has the following structure. [0003] [0004] Telmisartan tablets are products developed by Boehringer Ingelheim, Germany, and the trade name is Mecasu The preparation specification is 20mg / 40mg / 80mg tablet. Mecaso It was first listed in the United States in 1999, listed in the UK in 2000, and li...

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Problems solved by technology

Patent CN200710041363.X can indeed improve the dissolution of telmisartan by dissolving telmisartan, alkaline reagent and povidone together in aqueous solution or alcohol aqueous solution as a binder granulation method, but this method also has two problems. Insufficiency: at first more alkaline reagents are used in this method, and the phenomenon that gastric juice partial alkali causes indigestion unavoidably can take place after patient takes; Secondly inventor finds in practice that the aqueous solution of telmisartan and alkaline reagent is relatively Viscous, adding povidone will increase the viscosity of the solution, and it is very difficult to use this viscous solution for fluidized bed granulation, and a little carelessness in the process will cause the bed to collapse and cause granulation failure , there are only two ways to solve this problem, one is to dilute the aqueous solution to reduce the viscosity of the aqueous solution, but this will cause the fluidized bed granulation time to be prolonged, and lose the time-saving and labor-saving advantages of fluidized bed granulation; the other is For example, the preferred method in the patent is to dissolve telmisartan, alkaline reagents and povidone in a high-alcohol aqueous solution. This method can greatly reduce the viscosity of the solution, but due to the use of high-dose ethanol granulation, the production capacity is increased. The risk of explosion in the environment puts forward higher requirements for equipment and production workshops

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