Novel formulation of piperazine ferulate and preparation method thereof

A technology of piperazine ferulic acid and new dosage forms, which is applied in the field of new dosage forms of piperazine ferulic acid and its preparation, can solve the problems of low solubility, low bioavailability and poor dissolution rate of piperazine ferulic acid, etc. Achieve rapid drug administration, high bioavailability, and rapid onset of effect

Inactive Publication Date: 2010-12-22
SICHUAN BAOSHENGKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is to provide a new preparation of piperazine ferulate which can overcome the shortcomings of poor drug dissolution, low bioavailability and slow onset of action in the prior art piperazine ferulate oral preparations and its preparation The method, that is, piperazine ferulate injection, can significantly improve the bioavailability of piperazine ferulate, and the onset of effect is more rapid, providing a more effective treatment for patients with severe coronary heart disease, cerebral infarction, kidney disease, diabetic vascular complications and other diseases. ideal therapeutic drug
[0007] Another object of the present invention is to overcome the problem of low solubility of piperazine ferulate in the prior art

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation of small volume injection of piperazine ferulate

[0026] A. take by weighing 80 piperazine ferulate;

[0027] B. Add piperazine ferulate to 1800ml water for injection, stir, slowly add 20% sodium carbonate solution to adjust the pH value, make the pH value of the solution reach 6.2, and now the piperazine ferulate dissolves completely;

[0028] C. Add an appropriate amount of activated carbon in the above-mentioned piperazine ferulic acid solution, decarbonize and filter after stirring at room temperature for 30 minutes;

[0029] D. The above-mentioned filtrate is filtered with a microporous membrane, and water for injection is added to the full amount; it is divided into 10ml brown ampoules, melted and sealed, and sterilized by autoclaving to obtain piperazine ferulic acid small-volume injection.

Embodiment 2

[0031] Preparation of piperazine ferulate injection powder

[0032] A. take by weighing 300g piperazine ferulate;

[0033] B. Add piperazine ferulate to 3000ml water for injection, stir, slowly add 2mol / L sodium hydroxide solution to adjust the pH value, make the pH value 7.5, and completely dissolve piperazine ferulate; add 200g mannitol, stir , to completely dissolve;

[0034] C. add gac to above-mentioned piperazine ferulic acid solution, decarbonize and filter after stirring at room temperature for 60 minutes;

[0035] D. The above-mentioned filtrate is filtered with a microporous membrane again, and water for injection is added to the full amount; it is divided into 10ml vials and freeze-dried to obtain piperazine ferulic acid powder for injection.

Embodiment 3

[0037] Preparation of large volume injection of piperazine ferulate

[0038] A. take by weighing 100g piperazine ferulate;

[0039] B. Add piperazine ferulate to 2000ml water for injection, stir, slowly add sodium lactate solution to adjust the pH value, make the pH reach 5.8, stir, piperazine ferulate dissolves completely.

[0040] C. Add activated carbon in the above-mentioned piperazine ferulic acid solution, decarbonize and filter after stirring at room temperature for 30 minutes;

[0041] D. The above-mentioned filtrate is filtered with a microporous membrane again, and water for injection is added to the full amount; it is divided into 100ml glass bottles, stoppered, capped, and sterilized by autoclaving to obtain a large-capacity piperazine ferulic acid injection.

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Abstract

The invention discloses a novel formulation of piperazine ferulate and a preparation method thereof. The novel formulation of the piperazine ferulate is prepared by the steps of dissolving piperazine ferulate as a medicine component into a solvent and regulating the pH value to be 5.0-8.0 with a pH regulating agent so that the piperazine ferulate is fully dissolved to prepare an injection. The content of the piperazine ferulate in the novel formulation is 27-200mg/ml. The invention broadens the clinical application range of the piperazine ferulate, has the characteristics of high medicine dissolubility, high bioavailability, rapid medicine administration, more quick effect-taking, stronger treatment effect, and the like, is especially suitable for preventing and treating patients suffering from heavy cerebral infarction, nephroma, coronary heart disease, vascular complication in diabetes mellitus and dysphagia, overcomes the problem of low dissolubility of the piperazine ferulate in the prior art, and realizes the solubilization of the piperazine ferulate by regulating the pH value with the pH regulating agent, wherein at least 500mg of piperazine ferulate can be dissolved in 10ml of water solution with pH value of 5.5.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to an endothelin receptor antagonist injection and a preparation method thereof, which are used for the prevention and treatment of endothelin-induced coronary heart disease, cerebral infarction, kidney disease, diabetic vascular complications and other diseases, specifically, The invention relates to a new dosage form of piperazine ferulate and a preparation method thereof. Background technique [0002] Piperazine ferulate, whose chemical name is 3-methoxy-4-hydroxypiperazine cinnamate, is chemically synthesized from ferulic acid and piperazine. Ferulic acid is a ubiquitous phenolic acid. In the plant cell wall, it is cross-linked with polysaccharides and lignin to form a part of the cell wall. Strong antioxidant activity and antiseptic effect are widely used in medicine, pesticides, health care products, cosmetic raw materials and food additives. In recent years, extensive and i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/19A61K31/495A61K47/02A61K47/12A61P9/10A61P13/12A61P9/14
Inventor 唐楷
Owner SICHUAN BAOSHENGKANG PHARMA
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