Lipid microballoon injection solution for progestational hormone drug and preparation method thereof

A technology of injection and microspheres, applied in pharmaceutical formulations, drug combinations, drug delivery, etc., can solve the problems of obvious pain, inaccurate dosage, redness and swelling, and achieve the effect of enriching choices and avoiding liver first-pass effect.

Active Publication Date: 2016-11-09
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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  • Lipid microballoon injection solution for progestational hormone drug and preparation method thereof
  • Lipid microballoon injection solution for progestational hormone drug and preparation method thereof
  • Lipid microballoon injection solution for progestational hormone drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Example 1 Prescription screening of progesterone lipid microsphere injection

[0084] 1. Screening of stabilizers

[0085] The stabilizer used in the lipid microsphere injection can increase the intermolecular force and the surface charge of the emulsion droplets, improve the physical stability of the emulsion through electrostatic repulsion, increase the strength of the lipid microsphere interface film, 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 formulation. The average particle size, Di90, and PDI are closely related to the safety and stability of injectable 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 inspection indexes, and the prescriptions containing different stabilizers are compared, and t...

Embodiment 2

[0103] Example 2 Preparation of Progesterone Lipid Microsphere Injection

[0104] prescription:

[0105]

[0106] Method:

[0107] (1) The mixture of soybean oil for injection and medium-chain triglyceride is heated to 70°C to 75°C, egg yolk lecithin PC-98T, egg yolk lecithin PL-100M, phosphatidyl glycerol, and progesterone are added, and the obtained The mixture is subjected to shearing treatment until the whole is dissolved and dispersed uniformly, so as to obtain the first mixture containing the oil phase of progesterone.

[0108] (2) The water for injection is heated to 70° C., glycerol for injection is added, and the resulting mixture is stirred well, so as to obtain a second mixture that forms an aqueous phase.

[0109] (3) Mixing the first mixture and the second mixture, shearing while mixing, rotating at 15000 rpm for 15 minutes, so as to obtain a third mixture for forming colostrum.

[0110] (4) The pH value of the third mixture is adjusted to 7.0 with sodium hy...

Embodiment 3

[0124] Example 3 Preparation of Progesterone Lipid Microsphere Injection

[0125] prescription:

[0126]

[0127]

[0128] Method:

[0129] (1) The mixture of soybean oil for injection and medium-chain triglyceride is heated to 70°C to 75°C, egg yolk lecithin PC-98T, egg yolk lecithin PL-100M, phosphatidyl glycerol, and progesterone are added, and the obtained The mixture is subjected to shearing treatment until the whole is dissolved and dispersed uniformly, so as to obtain the first mixture containing the oil phase of progesterone.

[0130] (2) The water for injection is heated to 70° C., glycerol for injection is added, and the resulting mixture is stirred well, so as to obtain a second mixture that forms an aqueous phase.

[0131] (3) Mixing the first mixture and the second mixture, shearing while mixing, and rotating at 10,000 rpm for 30 minutes, so as to obtain a third mixture for forming colostrum.

[0132] (4) The pH value of the third mixture is adjusted to 8...

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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, in particular, the invention relates to a progesterone drug progesterone lipid microsphere injection and a preparation method thereof. Background technique [0002] As a progestin, progesterone is mainly used for injection (intramuscular injection) during artificial insemination, but the current injection uses benzyl alcohol and soybean oil as solvents, and this dosage form has the following disadvantages: (1) When injecting oil, local It is highly irritating and has obvious pain, which is easy to cause tension and anxiety in patients; (2) The oil spreads slowly, and the injected liquid is easy to re-infiltrate, resulting in inaccurate doses, and at the same time it is easy to cause pain at the injection point and infection; (3) because the drug has a long medication cycle (progesterone injection is often required for 10 to 12 weeks after in vitro fertilization-embryo transfer...

Claims

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Application Information

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Patent Type & Authority Applications(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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