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Preparation method and application of progesterone eutectic

A technology of progesterone and co-crystal, which is applied in the field of preparation of progesterone co-crystal, can solve the problems of aseptic abscess absorption and recovery taking a long time, easy to form local induration, and no treatment method, so as to reduce dosage and related side effects, Good stability and improved solubility

Pending Publication Date: 2022-06-21
CHINA RESOURCES ZIZHU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its main advantages are definite curative effect and low price. The main disadvantages are: pain and irritation at the injection site, easy formation of local induration, local induration, absorption and recovery of sterile abscess takes a long time, these are normal phenomena of intramuscular injection of progesterone, no specific effective treatment

Method used

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  • Preparation method and application of progesterone eutectic
  • Preparation method and application of progesterone eutectic
  • Preparation method and application of progesterone eutectic

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Weigh 943.4 mg (3.0 mmol) of progesterone and 501.4 mg (3.0 mmol) of o-nitrobenzoic acid into a ball mill (planetary ball mill, Nanjing Chishun Technology Development Co., Ltd.), add 0.2 mL of ethyl acetate as a co-solvent, and mill at 28 Hz. 40min, the obtained white powder is progesterone-o-nitrobenzoic acid co-crystal.

[0046] Single crystal culture method: Take 100 mg of the above-mentioned progesterone-o-nitrobenzoic acid co-crystal powder, add 15 ml of methanol to dissolve, slowly evaporate the solvent, and obtain colorless bulk crystals in about 1 week.

Embodiment 2

[0048] Weigh 943.4 mg (3.0 mmol) of progesterone and 501.4 mg (3.0 mmol) of m-nitrobenzoic acid into a ball mill (planetary ball mill, Nanjing Chishun Technology Development Co., Ltd.), add 0.2 mL of ethyl acetate as a co-solvent, and mill at 28 Hz. 40min, the obtained white powder is progesterone-m-nitrobenzene co-crystal.

[0049] Single crystal cultivation method: Take 100 mg of the above progesterone-m-nitrobenzoic acid co-crystal powder, add 15 ml of methanol to dissolve, and slowly evaporate the solvent, and colorless bulk crystals are obtained in about 1 week.

Embodiment 3

[0051] Weigh 943.4 mg (3.0 mmol) of progesterone and 501.4 mg (3.0 mmol) of p-nitrobenzoic acid into a ball mill (planetary ball mill, Nanjing Chishun Technology Development Co., Ltd.), add 0.2 mL of ethyl acetate as a co-solvent, and mill at 28 Hz. After 40 min, the obtained white powder was progesterone-p-nitrobenzene co-crystal.

[0052] Single crystal cultivation method: Take 100 mg of the above-mentioned progesterone-p-nitrobenzoic acid co-crystal powder, add 15 ml of methanol to dissolve, and slowly evaporate the solvent to obtain colorless bulk crystals in about 1 week.

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Abstract

The invention discloses a preparation method and application of progesterone eutecticum. The progesterone eutectic is formed by an active component progesterone and a eutectic former nitrobenzoic acid, and the progesterone and the nitrobenzoic acid are connected through a hydrogen bond; wherein the molar ratio of progesterone to nitrobenzoic acid is 1: 1. The progesterone-nitrobenzoic acid eutectic (o-nitrobenzoic acid, m-nitrobenzoic acid and p-nitrobenzoic acid) prepared by the invention is good in stability, the solubility is remarkably improved, and the irritation and adverse reaction of progesterone can be reduced by increasing the solubility of progesterone. And the eutectic technology can control the release of progesterone and prolong the delivery of progesterone, and has the application value of reducing dosage and related side effects. The eutectic reagent used in the preparation method is low in price, ball milling and other low-production-cost methods are adopted in preparation, the drug production cost is not remarkably increased when the drug water solubility is improved, and it can be guaranteed that the price of the eutectic drug is basically stable.

Description

technical field [0001] The invention belongs to the technical field of drug co-crystal preparation, in particular to a preparation method and application of a progesterone co-crystal. Background technique [0002] Drug co-crystal is the formation of a "supramolecular" with a fixed composition and a single melting point between drug molecules and co-crystal reagents through intermolecular forces such as hydrogen bonds. Existing research results show that the use of co-crystal reagents with better water solubility and insoluble drugs to form drug co-crystals can significantly improve the water solubility and bioavailability of insoluble drugs without changing the molecular structure of the drug. The latest key technologies for the physicochemical properties of drugs such as water solubility, permeability and stability. In 2013, the US FDA issued guidelines for the drug co-crystal industry, listing drug co-crystals as drug excipients; in 2016, the principle was revised to furt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J7/00C07C205/57C07C201/12A61K31/57A61P5/34
CPCC07J7/002C07C205/57A61P5/34C07B2200/13
Inventor 贺颖王延松杨振华万雨薇李佳阳
Owner CHINA RESOURCES ZIZHU PHARMA