Tanshinone IIA microemulsions and preparing method thereof

Abstract

The invention discloses a tanshinone II A microemulsion preparation which has targeting and comparatively high entrapment efficiency and drug-loading rate, is not haemolytic and mainly applied to the treatment of tumor and a preparation method thereof. The invention comprises the following raw materials by weight percentage: 0.6-0.8 percent of tanshinone II A, 0.6-1.8 percent of phosphotide for injection, 2.5-3 percent of glycerin for injection, 1.5-3 percent of F68 for injection, 11-15 percent of ethyl oleate and water for injection. The preparation method of the invention is that first the tanshinone II A is dissolved in the ethyl oleate to prepare the oil phase mixture solution; next the phosphotide for injection, the glycerin for injection and the F68 for injection are dissolved in the water for injection which accounts for 60-70percent of the total water for injection to prepare the water phase solution; then the oil phase solution and the water phase solution are respectively preheated to 60-70DEG C and the oil phase solution is slowly dropped to the water phase solution when the water phase solution is blended; the mixed solution is then sheared for 1-2minutes in a high shearing dispersing emulsification machine and filtrated with a 0.8Mum filtration membrane when the solution is still hot and the rest water for injection is added to the filtrate; the liquid obtained from step d is homogenized by a high pressure emulsification machine and next filtrated with the 0.8 Mum filtration membrane; finally the filtrate obtained from step e is packaged, filled with nitrogen, sealed and disinfected.

Description

Technical field: [0001] The invention relates to a tanshinone IIA pharmaceutical dosage form and a preparation method, in particular to a tanshinone IIA microemulsion preparation and its preparation which are targeted, are mainly used for anti-tumor, have high encapsulation efficiency, drug loading, and do not produce hemolysis method. Background technique: [0002] Tanshinone is a fat-soluble active ingredient extracted from the root of Salvia miltiorrhiza, a traditional Chinese medicine for promoting blood circulation and removing blood stasis. It has a variety of biological activities. [0003] Tanshinone IIA (Tanshinone IIA, Tan-IIA) is a monomer component in tanshinone. It has been reported in the literature that the antitumor activity of tanshinone is mainly realized by tanshinone IIA. Therefore, tanshinone IIA is more effective than tanshinone in antitumor performance. superior. However, because tanshinone IIA solid preparations are difficult to absorb, and tanshino...

AI Technical Summary

Problems solved by technology

However, because tanshinone IIA solid preparations are difficult to absorb, and tanshinone IIA is a fat-soluble drug that is insoluble in water, only tanshinone IIA sulfonate sodium salt injection has been clinically used so far.

Tanshinone IIA sulfonate sodium salt injection can increase coronary flow, improve myocardial hypoxia resistance, inhibit platelet aggregation and antithrombotic formation, and can also increase myocardial contractility under a certain dose, but some patients feel pain after intramuscular injection , Individual patients have skin rashes, and do not have sustained release and targeting

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