Carvedilol-asccharin amorphous compound

Abstract

The invention relates to a carvedilol-asccharin amorphous compound. The carvedilol-asccharin amorphous compound is obtained by combination of carvedilol and asccharin. Based on Cu-K alpha radiation, an X-ray powder diffraction spectrum represented by a degree of 2 theta does not comprise a sharp diffraction peak. The powder X-ray diffraction spectrum of the carvedilol-asccharin amorphous compound is different from those of carvedilol crystals and a physical mixture of carvedilol crystals and asccharin crystals and thus the carvedilol-asccharin amorphous compound is a novel amorphous compound completely different from carvedilol crystals and the physical mixture of carvedilol crystals and asccharin crystals. The carvedilol-asccharin amorphous compound can obviously improve solubility of carvedilol in various mediums.

Description

Technical field The invention belongs to the technical field of medicine, and specifically relates to a carvedilol saccharin co-amorphous substance formed by combining carvedilol and saccharin at a molar ratio of 1:1 and a preparation method thereof. Background technique Carvedilol, whose chemical name is 1-carbazole-4-oxy-3-[2-(2-methoxyphenoxy)ethylamino]-2-propanol, is a new type of vasodilator . Clinically, it can be used to treat essential hypertension and cardiac insufficiency. Carvedilol has both α1 and non-selective β-receptor blocking effects within the therapeutic dose range, and has no intrinsic sympathomimetic activity. This product blocks post-synaptic membrane α receptors, thereby dilating blood vessels and reducing peripheral vascular resistance; blocking β receptors, inhibits kidney secretion of renin, blocks the renin-angiotensin-aldosterone system, and reduces blood pressure effect. Carvedilol lowers blood pressure quickly and can maintain the lowering ef...

AI Technical Summary

Problems solved by technology

Carvedilol is a class II drug in the biopharmaceutical classification system, which is insoluble in water and has a significant first-pass effect, making its absolute bioavailability only 25%-35%

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