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Preparation method of gossypol acetate calcium alginate gel microspheres

A technology of gossypol acetate and calcium alginate, which is applied to medical preparations with no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve the toxic and side effects of hypokalemia, hinder the promotion and use of drugs, Concentration instability and other problems, to achieve the effect of inhibiting toxic and side effects, stable and effective drug concentration, and good drug release

Active Publication Date: 2020-10-16
山东海诺知识产权运营管理有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But gossypol acetate has toxic and side effects of hypokalemia, and its metabolism in the body is slow, and the drug concentration in the body is extremely unstable after oral administration, thus hindering its clinical promotion and use.

Method used

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  • Preparation method of gossypol acetate calcium alginate gel microspheres
  • Preparation method of gossypol acetate calcium alginate gel microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] The method for preparing gossypol acetate calcium alginate gel microspheres in this embodiment,

[0025] It includes the following steps:

[0026] (1) Dissolve gossypol acetate in N,N-dimethylacetamide to obtain solution A, the concentration of gossypol acetate in solution A is 1mg / ml;

[0027] (2) Dissolve ε-polylysine, diclofenac potassium, and potassium chloride in water to obtain solution B. In solution B, the concentration of ε-polylysine is 1 mg / ml, and the concentration of diclofenac potassium is 0.5 mg / ml. The potassium concentration is 3mg / ml;

[0028] (3) The stock solution is obtained after mixing solution A and solution B evenly;

[0029] (4) Dissolve calcium chloride in water to prepare a solution with a mass concentration of 0.5%. The calcium ion concentration affects the release rate of the drug in the microspheres. As the calcium ion concentration increases, the release rate of the drug in the microspheres slows down. When the calcium ion concentration is too lo...

Embodiment 2

[0034] The method for preparing gossypol acetate calcium alginate gel microspheres in this embodiment,

[0035] It includes the following steps:

[0036] (1) Dissolve gossypol acetate in N,N-dimethylacetamide to obtain solution A, the concentration of gossypol acetate in solution A is 2mg / ml;

[0037] (2) Dissolve ε-polylysine, diclofenac potassium, and potassium chloride in water to obtain solution B. In solution B, the concentration of ε-polylysine is 3 mg / ml, and the concentration of diclofenac potassium is 2 mg / ml. The potassium concentration is 5mg / ml;

[0038] (3) The stock solution is obtained after mixing solution A and solution B evenly;

[0039] (4) Dissolve calcium chloride in water to prepare a solution with a mass concentration of 2%. The calcium ion concentration affects the release rate of the drug in the microspheres. As the calcium ion concentration increases, the release rate of the drug in the microspheres slows down. When the calcium ion concentration is too low, t...

Embodiment 3

[0044] The method for preparing gossypol acetate calcium alginate gel microspheres in this embodiment,

[0045] It includes the following steps:

[0046] (1) Dissolve gossypol acetate in N,N-dimethylacetamide to obtain solution A, the concentration of gossypol acetate in solution A is 1mg / ml;

[0047] (2) Dissolve ε-polylysine, diclofenac potassium, and potassium chloride in water to obtain solution B. In solution B, the concentration of ε-polylysine is 2 mg / ml, and the concentration of diclofenac potassium is 1 mg / ml. The potassium concentration is 4mg / ml;

[0048] (3) The stock solution is obtained after mixing solution A and solution B evenly;

[0049] (4) Dissolve calcium chloride in water to prepare a solution with a mass concentration of 1%. The calcium ion concentration affects the release rate of the drug in the microspheres. As the calcium ion concentration increases, the release rate of the drug in the microspheres slows down. When the calcium ion concentration is too low, t...

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Abstract

The invention discloses a preparation method of gossypol acetate calcium alginate gel microspheres. Gossypol acetate is dissolved into N,N-dimethyl acetamide; epsilon-polylysine, diclofenac potassiumand potassium chloride are dissolved into water; the solution is uniformly mixed to obtain a stock solution; calcium chloride is dissolved into water; sodium alginate is dissolved into water to be prepared into a solution with the mass concentration being 1 to 2 percent; the stock solution is added into the sodium alginate solution; stirring is performed till the uniform mixing; a micro quantity injection pump is used for dripping the solution into the calcium chloride solution; gelatinization is performed for 20 to 40min to obtain microspheres. A buffer solution is used for flushing the microspheres to obtain the gossypol acetate calcium alginate gel microspheres. The gossypol acetate calcium alginate gel microspheres have the advantages of high embedding rate, good swelling property andgood medicine release property.

Description

Technical field [0001] The invention relates to a medicine containing gossypol acetate, in particular to a method for preparing gossypol acetate calcium alginate gel microspheres. Background technique [0002] Gossypol acetate is a male contraceptive and is also used to treat gynecological diseases, including menorrhagia or disorder, uterine fibroids, endometriosis, etc. Gossypol acetate has been widely used as a drug in developed countries such as the United States. On the one hand, its application is anti-tumor; on the other hand, it is used in gynecological diseases such as endometriosis. The American Chemical Abstracts reported at the same time that the compound formed by the condensation of gossypol and β-sulfamate has a strong immunosuppressive effect, and its anti-tumor effect is worthy of promotion. However, gossypol acetate has the toxic side effects of hypokalemia, and its metabolism in the body is slow, and the oral drug concentration in the body is extremely unstable...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/11A61K9/16A61K31/19A61K33/14A61K31/196A61K33/00A61K31/785A61K47/36A61P15/16
CPCA61K9/1652A61K31/11A61K31/19A61K31/196A61K31/785A61K33/00A61K33/14A61K2300/00
Inventor 任冉
Owner 山东海诺知识产权运营管理有限公司
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