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Tanshinone IIA lipid complexes and micelle composition thereof for injection

A lipoplex and tanshinone technology, applied in the direction of drug combination, drug delivery, medical preparations of non-active ingredients, etc., can solve the problem of adding steps

Inactive Publication Date: 2009-05-27
SHENYANG WOSEN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Simultaneously because need carry out sulfonation reaction to tanshinone IIA, increase unnecessary step

Method used

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  • Tanshinone IIA lipid complexes and micelle composition thereof for injection
  • Tanshinone IIA lipid complexes and micelle composition thereof for injection
  • Tanshinone IIA lipid complexes and micelle composition thereof for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032]Take 500mg of Tanshinone IIA, 2.0g of egg yolk lecithin, 400mg of sodium cholesterol sulfate, and 10mg of vitamin E, and dissolve them in methanol at 30°C as the organic phase; dissolve 0.5g of PEG400 in 90ml of water for injection, heat to 30°C as the water phase, The organic phase was injected into the water phase under stirring at 30°C, and the stirring was continued for 5 minutes, and then the methanol was evaporated under reduced pressure to obtain the tanshinone IIA lipid complex with blue opalescence, and its average particle size was measured to be 82±17nm. Add water for injection to make up to a total volume of 100ml, filter and sterilize with a 0.22μm microporous membrane, dispense 2ml / tube, and sterilize at 121°C for 30min to obtain an injection.

[0033] Add trehalose 5g to the prepared lipoplex, water for injection to 100ml, filter and sterilize with a 0.22μm microporous membrane, pack 2ml / branch, and freeze-dry under aseptic operation to obtain final product...

Embodiment 2

[0035] Take 1.0g of tanshinone IIA, 3.0g of soybean lecithin, and 500mg of sodium cholesterol sulfate, and dissolve them in absolute ethanol at 35°C as the organic phase; dissolve 1.0g of PEG200 in 90ml of water for injection, heat to 35°C as the water phase, and The organic phase was injected into the water phase under stirring at 35°C, and the stirring was continued for 10 minutes, and then the ethanol was evaporated under reduced pressure to obtain the tanshinone IIA lipid complex with blue opalescence, and its average particle size was measured to be 72±12nm. Add water for injection to make up to a total volume of 100ml, filter and sterilize with a 0.22μm microporous membrane, dispense 2ml / tube, and sterilize at 121°C for 30min to obtain an injection.

[0036] Add trehalose 5g to the prepared lipoplex, water for injection to 100ml, filter and sterilize with a 0.22μm microporous membrane, pack 4ml / branch, and freeze-dry under aseptic operation to obtain final product. The f...

Embodiment 3

[0038] Take 2.0 mg of tanshinone IIA, 10 g of soybean lecithin, and 5 g of sodium cholesterol sulfonate, and dissolve it in tetrahydrofuran at 35 °C as the organic phase; dissolve 1885 g of poloxamer in 950 ml of water for injection, heat it to 35 °C as the water phase, and stir at 35 °C Inject the organic phase into the water phase, continue to stir for 10 minutes, and then evaporate the tetrahydrofuran under reduced pressure to obtain the tanshinone IIA lipid complex with blue opalescence. For 100ml, use a 0.22μm microporous membrane to filter and sterilize, aliquot 2ml / tube, and sterilize at 121°C for 30min to obtain the injection.

[0039] Add trehalose 5g to the prepared lipoplex, water for injection to 100ml, filter and sterilize with a 0.22μm microporous membrane, pack 4ml / branch, and freeze-dry under aseptic operation to obtain final product. The freeze-dried preparation was diluted with physiological saline, and the average particle size was measured to be 70±18nm.

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Abstract

The invention provides a tanshinone IIA lipid compound and a micellar compound used in the injection of the tanshinone IIA lipid compound. The tanshinone IIA lipid compound is composed of tanshinone IIA with a therapeutic dose, phospholipid, cholesterol sulfate or / and similar cholesterol derivative, additive and injection water. By means of the lipidization of the docetaxel, the problem that the tanshinone IIA does not dissolve is water and then cannot be directly prepared into an injection. The tanshinone IIA lipid compound injection provided by the invention has the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to the preparation of a tanshinone IIA lipid complex and a micelle composition for injection thereof. Background technique [0002] Tanshinone IIA (Tanshinone IIA), CAS NO.: 568-72-9, molecular formula: C 19 h 18 o 3 Molecular weight: 294.33, the structural formula is: [0003] [0004] The Structure of Tanshinon IIA The Structure of Sodium Tanshinon IIA It is the dry root and rhizome extract of Salvia miltiorrhiza Bge. The crystalline powder is red and has a melting point of 209°C to 210°C. It is easily soluble in organic solvents such as ethanol, acetone, and ether, and slightly soluble in water. This product can increase the coronary flow, improve the collateral circulation and local blood supply of the ischemic myocardium, improve the metabolic disorder of the hypoxic myocardium, improve the ability of the myocardium to withstand hypoxia, inhibit platelet aggreg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61K9/00A61K9/12A61K47/24A61P9/10
Inventor 德瑞克·王张晓君徐飒
Owner SHENYANG WOSEN PHARMA INST
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