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Preparation method of ligustrazine phosphate powder injection

A technology of ligustrazine phosphate and ligustrazine powder, which is applied to medical preparations containing active ingredients, powder delivery, pharmaceutical formulations, etc., can solve the problems of low bioavailability, long production cycle, and many degradation products, and achieve the preparation method Simple, short production cycle, less degradation products

Active Publication Date: 2011-06-29
HAINAN HULUWA PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Compared with injections, oral solid preparations have the following disadvantages: (1) The bioavailability is low. All oral drugs must be absorbed through the gastrointestinal wall and then enter the portal vein. It is extensively metabolized and eliminated in the wall or liver, and the first-pass effect occurs
After freeze-drying, the product is porous and loose, and there are many degradation products. It is an amorphous crystal and has poor stability.
Using the freeze-drying method to prepare ligustrazine phosphate powder for injection requires the addition of molding agents, such as mannitol, which increases the impurities of the drug, and has a long production cycle, waste of energy, high cost, and low yield. Therefore, it needs to be developed Preparation method of ligustrazine phosphate powder for injection with industrialization prospect

Method used

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  • Preparation method of ligustrazine phosphate powder injection

Examples

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Comparison scheme
Effect test

Embodiment 1

[0030] Dissolve 100g of ligustrazine phosphate in ethanol, heat in a water bath at 60°C to aid dissolution, and prepare 1000mL of ligustrazine phosphate ethanol solution, add 1g of medicinal charcoal to absorb for 20 minutes, filter and decarbonize to obtain the filtrate, and filter the filtrate with a pore size of φ0. 22μm microporous filter membrane, after sterilizing and filtering, crystallize at 0°C for 5 hours, crystallize while stirring at a stirring rate of 1200 rpm, and dry the precipitated crystals at 50°C for 4 hours after filtration to obtain 98 grams of injection Ligustrazine phosphate was used to subpackage, stopper, and cap according to the marked amount of 0.1 g / bottle to prepare 980 ligustrazine phosphate powder injections for injection.

Embodiment 2

[0032] Dissolve 100g of ligustrazine phosphate in ethanol, heat it in a water bath at 60°C to help dissolve it, and prepare 1000mL of ligustrazine phosphate ethanol solution, add 5g of medicinal charcoal to absorb for 50 minutes, filter and decarbonize to obtain the filtrate, and filter the filtrate with a pore size of φ0. After sterilizing and filtering with a microporous membrane of 8 μm, crystallize at 35°C for 12 hours, crystallize while stirring at a stirring rate of 60 rpm, and dry the precipitated crystals at 0°C for 12 hours after filtration to obtain 96.2 grams of injection Ligustrazine phosphate was used to subpackage, stopper, and cap according to the marked amount of 0.1 g / bottle to prepare 962 ligustrazine phosphate powder injections for injection.

Embodiment 3

[0034] Dissolve 100g of ligustrazine phosphate in ethanol, heat it in a water bath at 60°C to help dissolve, and prepare 1000mL of ligustrazine phosphate ethanol solution, add 30g of medical charcoal to absorb for 120 minutes, filter and decarbonize to obtain the filtrate, and filter the filtrate with a pore size of φ0. 45 μm microporous filter membrane, after sterilizing and filtering, crystallize at 20°C for 48 hours, crystallize while stirring at a stirring rate of 2000 rpm, and dry the precipitated crystals at 80°C for 8 hours after filtration to obtain 95.2 g injection Ligustrazine phosphate was used to subpackage, stopper, and cap according to the marked amount of 0.1 g / bottle to prepare 952 ligustrazine phosphate powder injections for injection.

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Abstract

The invention discloses a preparation method of ligustrazine phosphate powder injection, comprising the following steps: dissolving ligustrazine phosphate into ethanol; adding medicinal carbon for adsorption; obtaining filter liquor through filtration and decarburization; degerming and filtering the filter liquor by a millipore filter membrane, and then crystallizing under the temperature of 0-35DEG C while stirring at the same time; drying crystallized crystals under the temperature of 0-80 DEG C, and then preparing the ligustrazine phosphate for the injection through subpackage, stopper addition and capping. The preparation method has the advantages of easy operation, short production period without special equipment, low cost and high yield coefficient and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of preparation of powder injection for injection, in particular to a preparation method of ligustrazine phosphate powder for injection. technical background [0002] Ligustrazine is the active ingredient of Ligusticum chuanxiong, and it is a cardiovascular and cerebrovascular drug developed in my country. Tetramethylpyrazine phosphate, English name: tetrarnethylpyrazine phosphate, chemical name: 2,3,5,6-tetramethylpyrazine phosphate monohydrate, molecular formula: C 18 h 12 N 3 h 3 PO 4 h 2 O, white or off-white crystalline powder, slightly smelly, bitter taste, is a calcium antagonist, has the effect of anti-platelet aggregation, depolymerizes the aggregated platelets, and can still expand small arteries and improve microcirculation And increase cerebral blood flow, has the effect of promoting blood circulation and removing blood stasis of antithrombosis and thrombolysis. [0003] At present, ligustrazine phos...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61P9/10A61P7/02A61K31/4965A61K9/14
Inventor 刘全国吴文安
Owner HAINAN HULUWA PHARMA GRP CO LTD
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