Riociguat oral application preparation and preparation method therefor

Abstract

The invention provides a Riociguat oral application preparation and a preparation method therefor and relates to the technical field of pharmaceutical preparations. The invention aims at developing the Riociguat oral application preparation with good absorption, high bioavailability and higher medication compliance. The oral application preparation comprises the ingredients in percentage by weight: 10%-20% of Riociguat, 20%-35% of oil phase, 2%-18% of emulsifier and 30%-65% of co-emulsifier. Simultaneously, the invention further provides the preparation method for the oral application preparation. The preparation method comprises the steps of uniformly mixing the oil phase, the emulsifier and the co-emulsifier, then, adding the Riociguat, carrying out treatment with a high-pressure homogenizer so as to obtain an emulsion, then, adsorbing the emulsion to an adsorbent firstly by fluidized-bed spray drying equipment, then, carrying out coating, and finally, preparing capsules or tablets.The Riociguat oral application preparation can serve as a long-acting sustained-release efficient drug for treating pulmonary artery hypertension.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a riociguat oral preparation with good absorption, high bioavailability and higher drug compliance and a preparation method thereof. Background technique [0002] Riociguat (riociguat), chemical name N-[4,6-diamino-2-[1-[(2-fluorophenyl)methyl]-1H-pyrazolo[3,4-b]pyridine -3-yl]-5-pyrimidinyl]-N-methylcarbamate methyl ester, the molecular weight is 422.4157. It is a soluble guanylate cyclase activator developed by Bayer AG of Germany. It is an important signaling enzyme that can be activated by nitric oxide (NO) to catalyze the conversion of guanosine triphosphate (GTP) into the first The two-messenger cyclic guanosine monophosphate (cGMP), was the first drug of any class to be approved by the FDA as a drug for the treatment of pulmonary arterial hypertension and the first drug of any class to be shown to be effective in patients with chronic thromboembolic pu...

AI Technical Summary

Problems solved by technology

[0005] In view of the deficiencies in the prior art mentioned in the above-mentioned background technology, the object of the present invention is to develop a new oral preparation of riociguat, which greatly improves the in vitro dissolution rate of riociguat on the one hand, promotes absorption, and solves the problem of The problem of its poor solubility, on the other hand, makes it have the function of long-acting sustained release, so as to reduce the frequency of its administration and improve the safety of its administration at the same time

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