Progesterone drug lipid microsphere injection and preparation method thereof

A technology of injection and microspheres, which is applied in the fields of drug combination, drug delivery, and pharmaceutical formulation, can solve the problems of inaccurate dosage, obvious pain, and local irritation, and achieves rich clinical drug selection and preparation technology. Simple and stable formulation quality

Active Publication Date: 2019-03-08
WUHAN CONFORM PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Progesterone is as a kind of progestin, and during artificial insemination operation, mainly use its injection (intramuscular injection), but present injection adopts benzyl alcohol and soybean oil as solvent, and this dosage form has following shortcoming: (1) during oily injection, local Strong irritation, obvious pain, easy to cause tension and anxiety in patients; (2) The oil agent diffuses slowly, and the injected medicinal solution is easy to seep back, causing inaccurate dosage, and at the same time easily causing pain at the injection point and infection; (3) Because the drug has a long medication cycle (progesterone injections are often required for 10 to 12 weeks after in vitro fertilization-embryo transfer), long-term local injection of oil will cause local muscle tissue induration, etc.; (4) often Allergic reactions such as local redness and swelling; (5) When injecting, the injection resistance is high, and it is inconvenient for doctors to use
[0003] Therefore, research on progesterone-related preparations still needs to be strengthened

Method used

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  • Progesterone drug lipid microsphere injection and preparation method thereof
  • Progesterone drug lipid microsphere injection and preparation method thereof
  • Progesterone drug lipid microsphere injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Example 1 Progesterone Lipid Microsphere Injection Prescription Screening

[0084] 1. Screening of stabilizers

[0085] The stabilizer used in the liposphere injection can increase the intermolecular force and the surface charge of the emulsion droplet, improve the physical stability of the emulsion through electrostatic repulsion, increase the strength of the interface film of the liposphere, and increase the solubility of the drug. Therefore, it is necessary to investigate different stabilizers (phosphatidylglycerol, sodium oleate, oleic acid) and the dosage of stabilizers in the prescription. The average particle size, Di90, and PDI are closely related to the safety and stability of injection emulsions. Under the same process conditions, formulations with smaller average particle size, Di90, and PDI usually have better physical stability. , Di90, and PDI are the investigation indexes, and the prescriptions containing different stabilizers are compared, and the relev...

Embodiment 2

[0103] The preparation of embodiment 2 progesterone lipid microsphere injection

[0104] prescription:

[0105]

[0106] Preparation method:

[0107] (1) Heat the mixture of soybean oil and medium-chain triglycerides for injection to 70°C to 75°C, add egg yolk lecithin PC-98T, egg yolk lecithin PL-100M, phosphatidylglycerol, and progesterone. The mixture is subjected to shearing treatment until it is completely dissolved and dispersed evenly, so as to obtain the first mixture containing the progesterone oil phase.

[0108] (2) Heat the water for injection to 70° C., add glycerin for injection, and stir the obtained mixture evenly, so as to obtain a second mixture forming an aqueous phase.

[0109] (3) Mix the first mixture and the second mixture, and shear while mixing, at a rotation speed of 15,000 rpm, for 15 minutes, so as to obtain a third mixture that forms colostrum.

[0110] (4) Adjust the pH value of the third mixture to 7.0 with sodium hydroxide, and make up eno...

Embodiment 3

[0124] The preparation of embodiment 3 progesterone lipid microsphere injection

[0125] prescription:

[0126]

[0127]

[0128] Preparation method:

[0129] (1) Heat the mixture of soybean oil and medium-chain triglycerides for injection to 70°C-75°C, add egg yolk lecithin PC-98T, egg yolk lecithin PL-100M, phosphatidylglycerol, and progesterone, and the obtained The mixture is subjected to shearing treatment until it is completely dissolved and dispersed evenly, so as to obtain the first mixture containing the progesterone oil phase.

[0130] (2) Heat the water for injection to 70° C., add glycerin for injection, and stir the obtained mixture evenly, so as to obtain a second mixture forming an aqueous phase.

[0131] (3) Mix the first mixture and the second mixture, and shear while mixing, at a rotation speed of 10,000 rpm, for 30 minutes, so as to obtain a third mixture that forms colostrum.

[0132] (4) Use sodium hydroxide to adjust the pH value of the third mix...

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Abstract

The invention discloses a lipid microballoon injection solution for a progestational hormone drug and a preparation method thereof. The lipid microballoon injection solution for the progestational hormone drug comprises progestational hormone drug progesterone as a primary drug and pharmaceutically acceptable drug excipient, wherein the drug excipient comprises oil phase, emulsifier, osmotic pressure adjusting agent, stabilizer, pH value modifier and injection water. The lipid microballoon injection solution for the progestational hormone drug is stable in quality, free from injection irritation, high in safety, applicable to local intramuscular injection and intravenous injection, and beneficial to promotion of compliance of clinical medication of patient and enriches clinical medication selection.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations. Specifically, the invention relates to a progesterone drug progesterone lipid microsphere injection and a preparation method thereof. Background technique [0002] Progesterone is as a kind of progestin, and during artificial insemination operation, mainly use its injection (intramuscular injection), but present injection adopts benzyl alcohol and soybean oil as solvent, and this dosage form has following shortcoming: (1) during oily injection, local Strong irritation, obvious pain, easy to cause tension and anxiety in patients; (2) The oil agent diffuses slowly, and the injected medicinal solution is easy to seep back, causing inaccurate dosage, and at the same time easily causing pain at the injection point and infection; (3) Because the drug has a long medication cycle (progesterone injections are often required for 10 to 12 weeks after in vitro fertilization-embryo transfe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/57A61K47/24A61K47/44A61K47/14A61P15/00
CPCA61K9/0019A61K9/1075A61K31/57A61K47/14A61K47/24A61K47/44
Inventor 周小顺牟东升贺容丽李进
Owner WUHAN CONFORM PHARMA CO LTD
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