A kind of sorafenib organogel and preparation method thereof

Abstract

The invention provides a sorafenib organogel and preparation method thereof. The sorafenib organogel is composed of an organic gelatinizing agent, an organic solvent, a dispersion stabilizer and an active medicine, wherein the organogel is a thermosensitive organogel with the gelatinizing temperature of 40-50 DEG C, the organogel is in a solution state at a high temperature and in a gel state after being cooled, and can be fast dispersed into a nanometer solution in the presence of water. The organogel disclosed by the invention is capable of obviously improving the in vitro dissolution rate of the sorafenib and the bioavailability of rat oral administration; the gel disclosed by the invention has the characteristics of being less in dosage of the gelatinizing agent, good in security, simple in preparation method and wide in use, and can be processed into preparations in various administration routes so that the application prospect is good.

Description

technical field [0001] The invention relates to a new drug dosage form and new technology of sorafenib, in particular to an organogel and a preparation method thereof. Background technique [0002] Sorafenib (sorafenib) chemical name 4-{4-[3-(4-chloro-3-trifluoromethyl-phenyl-ureide]-phenoxy}-pyridine-2-carboxylic acid methylamine, Molecular formula: C 21 h 16 CIF 3 N 4 o 3 , Molecular weight 464.8g / mol. The tosylate salt form of sorafenib is used clinically, and its molecular structure is as follows: [0003] [0004] Sorafenib is a new type of multi-target drug, which exerts anticancer activity mainly through two ways. ① Inhibit the activity of Raf-1 and B-Raf serine and threonine kinases, thereby inhibiting the RAS / RAF / MEK / ERK signaling pathway and inhibiting the proliferation of tumor cells. ②Inhibit tumor angiogenesis. Tumor growth depends on the formation of new blood vessels. Sorafenib blocks the formation of tumor new blood vessels and cuts off the nutrie...

AI Technical Summary

Problems solved by technology

There are some reports of oral organogel recently, for example ibuprofen organogel (IwanagaK.etal., IntJPharm, 388:123-128, 2010) is to use 12-hydroxystearic acid as organogel, soybean oil as Organic solvent is made, and this organogel formulation ibuprofen oral absolute bioavailability reaches 98%, and the area under the plasma concentration curve (AUC) is 1.3 times of ibuprofen soybean oil solution, and ibuprofen aqueous suspension 1.5 times that of formulation, but the absorption rate is slow, organogel peak concentration (Cmax)<soybean oil solution<aqueous suspension, showing sustained release effect

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