Progesterone sustained-release composition and application thereof

A slow-release composition and a technology for progesterone, which are applied in the field of biomedicine, can solve the problems of affecting the stability of drug release of long-acting preparations, unable to adapt to clinical needs of progesterone, unfavorable product quality control, etc. The gel structure is dense and the effect of promoting drug absorption

Active Publication Date: 2021-12-03
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Second, the degradation time is long: the degradation time of different types of PLGA is 1 to 6 months, and it is very limited to adjust the degradation rate only by the molecular weight and molecular weight distribution of PLGA homopolymer, and the homopolymer in situ gel alone cannot The release of drugs that meet the release cycle of less than one month
Third, the drug loading limit: due to high safety and high water compatibility, the solvents of the PLGA system currently on the market are all N-methyl-2-pyrrolidone (NMP), but the solubility of the drug in the solvent and the in-situ Due to the limitation of gel injection volume (generally less than 2mL), the PLGA system is mainly used for small doses of drugs or drugs with high solubility in NMP, such as (monthly administration of 7.5mg), (monthly administration of 90mg or 120mg), (The solubility of buprenorphine in NMP is greater than 300mg / mL)
And for progesterone this dose is big (administration 300mg~600mg every month), the drug of low solubility in amphipathic solvent, existing PLGA system can't adapt to the clinical demand of progesterone because of the long drug release cycle; , the preparation system also has the disadvantage of serious burst release phenomenon, which seriously affects the release stability of its long-acting preparations and is not conducive to product quality control

Method used

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  • Progesterone sustained-release composition and application thereof
  • Progesterone sustained-release composition and application thereof
  • Progesterone sustained-release composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Gel Phase Transition Process of Fatty Acid Sustained Release Composition

[0031] According to the prescription in Table 1, 200 mg of different types of fatty acids, 100 mg of progesterone, 700 mg of NMP, and 50 mg of biodegradable polymer were weighed respectively, and heated and stirred for 2 hours to obtain a clear and transparent solution.

[0032] The resulting solution was poured into 5 mL of PBS (pH=7.4), and the formability of the gel in vitro was examined. The results are shown in Table 1.

[0033] Table 1 Preparation and Formability of Different Matrix Fats

[0034] prescription Types of fatty acids mixed matrix gel time Prescription 1 stearic acid none 20s Prescription 2 Arachidic acid none 22s Prescription 3 palmitic acid none 23s Prescription 4 Lauric acid none 21s Prescription 5 myristic acid none 22s Prescription 6 behenic acid none 25s Prescription 7 palmitoleic acid no...

Embodiment 2

[0037] Prescription Screening of Different Kinds of Solvents

[0038] Weigh 20% (w / w) of fatty acid and 10% (w / w) of progesterone respectively, weigh different kinds of solvents according to Table 2, heat and stir for 3 hours, and obtain a clear and transparent solution.

[0039] The obtained solution was poured into 5 mL of PBS (pH=7.4), and the formability of the gel in vitro was examined. The results are shown in Table 2.

[0040] Table 2 Prescription screening and formability investigation of different solvents

[0041] prescription solvent Solution Appearance Formability Prescription 1 70%NMP Clarity and transparency Completely formed Prescription 2 70% PEG-400 Clarity and transparency Completely formed Prescription 3 70%PEG-600 Clarity and transparency Completely formed Prescription 4 70% ethyl lactate Clarity and transparency Completely formed Prescription 5 70% Glyceryl Triacetate Clarity and transpare...

Embodiment 3

[0044] Study on the Inhibitory Burst Release Characteristics of Fatty Acids with Different Concentrations

[0045] The sustained-release composition containing 10% (w / w) of progesterone and different concentrations of fatty acids and PLGA mixed matrix injections containing 0.5% SDS-10mL PBS buffer solution (pH=7.4), in a constant temperature shaker (37 ° C, 100rmp) in vitro release test. Take out 10 mL of buffer solution at the set time point, and add an equal volume of fresh PBS buffer solution, and calculate the cumulative release rate of progesterone. The results are shown in Table 3.

[0046] Table 3 Sustained-release characteristics of different concentrations of fatty acids

[0047] prescription Fatty acid concentration (w / w) PLGA concentration (w / w) 1 hour burst Comparative example 1 0％ 20％ 7.79％ Prescription 1 1％ 19％ 5.01％ Prescription 2 2％ 18％ 3.55％ Prescription 3 5％ 15％ 2.74％ Prescription 4 8％ 12％ 1.95％ P...

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Abstract

The invention discloses a progesterone sustained-release composition and application thereof, and belongs to the technical field of biological medicine. The progesterone sustained-release composition comprises the following raw materials of, in percentage by mass, 1%-30% of progesterone, 1%-40% of fatty acid and 40%-80% of a solvent, wherein the sum of the mass fractions of the components is 100%. According to the progesterone sustained-release composition and the application thereof, the drug release speed can be flexibly adjusted by adjusting the variety and proportion of fatty acid, and the drug release period of 3 days-15 days is realized; and drug absorption is promoted through fatty acid, and drug release is more complete, so that clinical drug delivery requirements of drugs with the drug release period of 3 days-15 days and large daily dose are met.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a slow-release progesterone composition and its application. Background technique [0002] Progesterone is a natural progesterone secreted by the ovary. It is the drug of choice for clinical luteal phase support and has a significant protective effect on the endometrium of women. Clinically marketed dosage forms mainly include oral capsules, gel suppositories, intramuscular oil-soluble preparations, etc. Among them, oral progesterone preparations have a serious first-pass effect, and the oral bioavailability is only 10%, resulting in poor curative effect and relatively large side effects. Therefore, intramuscular injection of oil solution is commonly used clinically. The existing progesterone injection requires daily injection, and it is a long-term injection. It is extremely inconvenient to inject progesterone every day. At the same time, oil solution injection ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K31/57A61K47/12A61P15/00
CPCA61K31/57A61K9/06A61K47/12A61K9/0024A61P15/00
Inventor 姚静王宸
Owner CHINA PHARM UNIV
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