Novel formulation of piperazine ferulate and preparation method thereof

A technology of piperazine ferulate and injection, applied in the field of injection of piperazine ferulate and its preparation

Inactive Publication Date: 2012-01-25
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 method that can overcome the poor dissolution rate, low bioavailability, and The new preparation of piperazine ferulate and the preparation method thereof, namely piperazine ferulate, which have disadvantages such as slow action, can significantly improve the bioavailability of piperazine ferulate, and the onset of effect is more rapid. Provide a more ideal treatment drug for patients with infarction, kidney disease, diabetic vascular complications and other diseases
[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

[0026] Preparation of Piperazine Ferulic Acid Small Volume Injection

[0027] A. take by weighing 80 piperazine ferulic acid;

[0028] B. piperazine ferulic acid was added to 1800ml of water for injection, stirred, and 20% sodium carbonate solution was slowly added to adjust the pH value, so that the pH value of the solution reached 6.2, and piperazine ferulic acid was completely dissolved at this moment;

[0029] C. in the above-mentioned piperazine ferulic acid solution, add an appropriate amount of activated carbon, stir at room temperature for 30 minutes, decarbonize and filter;

[0030] 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 autoclaved to obtain piperazine ferulic acid small-volume injection.

Embodiment 2

[0032] Preparation of Piperazine Ferulic Acid Injection Powder

[0033] A. Weigh 300g piperazine ferulate;

[0034] B. Add piperazine ferulic acid to 3000ml of water for injection, stir, slowly add 2mol / L sodium hydroxide solution to adjust the pH value, make the pH value 7.5, and dissolve piperazine ferulic acid completely; then add 200 g of mannitol, stir , to dissolve completely;

[0035] C. in the above-mentioned piperazine ferulic acid solution, add activated carbon, decarbonize and filter after stirring at room temperature for 60 minutes;

[0036] 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 vials and freeze-dried to obtain piperazine ferulic acid powder for injection.

Embodiment 3

[0038] Preparation of Piperazine Ferulic Acid Large Volume Injection

[0039] A. Weigh 100g piperazine ferulic acid;

[0040] B. Add piperazine ferulate to 2000ml of water for injection, stir, slowly add sodium lactate solution to adjust pH value, make pH reach 5.8, stir, piperazine ferulate is completely dissolved.

[0041] C. in the above-mentioned piperazine ferulic acid solution, add activated carbon, decarbonize and filter after stirring at room temperature for 30 minutes;

[0042] D. The above-mentioned filtrate was filtered with a microporous membrane, and water for injection was added to the full amount; it was divided into 100ml glass bottles, stoppered, capped, and sterilized by autoclaving to obtain piperazine ferulic acid large-capacity injection.

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Abstract

The invention discloses a injection 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, and the agent is the water of injection. 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 10mlof 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 an injection 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 in-dep...

Claims

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Application Information

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