A kind of riociguat oral preparation and preparation method thereof

Abstract

A riociguat oral preparation and a preparation method thereof, relating to the technical field of pharmaceutical preparations, aiming to develop a riociguat oral preparation with good absorption, high bioavailability and higher drug compliance, the oral preparation contains parts by weight Riociguat 10-20%, oil phase 20-35%, emulsifier 2-18%, co-emulsifier 30-65%, also provides the preparation method of the oral preparation, comprising: oil phase, emulsifier Mix evenly with co-emulsifier, add riociguat, process the emulsion with a high-pressure homogenizer, and then use the fluidized bed spray drying equipment to first absorb the emulsion on the adsorbent, then coat it, and finally prepare it into capsules or tablets . The riociguat oral preparation can be used as a long-acting, sustained-release and high-efficiency drug for treating pulmonary 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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