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Altrenogest slow-release microsphere and preparation method thereof

A technology of allylorgestrel and slow-release microspheres, which is applied in the directions of pharmaceutical formulations, microcapsules, medical preparations of inactive ingredients, etc. The first-pass effect of drug effect time and other problems can reduce adverse reactions, reduce the number of administrations, and reduce toxic and side effects.

Active Publication Date: 2018-08-17
QILU ANIMAL HEALTH PROD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the dosage form of allylrenogest in the market is an oral solution, because the drug effect time is short, it is easy to produce the first-pass effect after oral administration, and frequent administration is required to maintain the effective concentration. 18 days, resulting in a long administration cycle, many times of use, extremely inconvenient use, and poor mouthfeel and taste palatability of the oral administration solution, and oral administration to animals is not easy to accept

Method used

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  • Altrenogest slow-release microsphere and preparation method thereof
  • Altrenogest slow-release microsphere and preparation method thereof
  • Altrenogest slow-release microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] A preparation method for allylgestrol sustained-release microspheres, the steps are as follows:

[0035] Weigh 0.12g of allylprogesterone, 0.96g of polymer material, add 8ml of dichloromethane, and ultrasonically dissolve it as the oil phase; take 0.25g of stevioside, 1.0g of gelatin, add 50ml of 0.2% Tween 80 solution, and ultrasonically dissolve, As the water phase; slowly add the oil phase to a certain proportion of the water phase under stirring conditions to form an O / W emulsion; add the O / W emulsion to the remaining water phase under stirring conditions, and stir at room temperature until organic The solvent was completely evaporated, extracted and filtered, washed with purified water for 3 times, and freeze-dried to obtain allylgestrin microspheres.

experiment example 1

[0037] Change different polymer materials, and conduct quality research and evaluation of allylgestrol microspheres prepared by different polymer materials

[0038] Table 1 Effect of different polymer materials on allylgestrol microspheres

[0039]

[0040]

[0041] It can be seen from the data in Table 1 that polycarbonate, polyamino acid, polylactic acid, polylactic acid-glycolic acid copolymer (PLGA) or polylactic acid-polyethylene glycol copolymer (PLA-PEG) are polymer materials, and The encapsulation rate of allylgestrin microspheres is more than 75%, the appearance is round, the particle size is large, and the dispersion is good; while other materials: polyacrylic resin, polyanhydride, polyhydroxybutyrate encapsulation rate are far less than the present invention , the particles are broken, the particle size is not uniform, and the dispersion is poor.

Embodiment 2

[0043] Dissolve allylprogesterone and PLA-PEG in 8ml of dichloromethane according to the prescription in Table 2, as the oil phase; take 0.25g of stevioside, 1.0g of gelatin, add 50ml of 0.2% different surfactant solutions, ultrasonically dissolve, and use as water phase; slowly add the oil phase to a certain proportion of the water phase under stirring conditions to form an O / W emulsion; add the O / W emulsion to the remaining water phase under stirring conditions, and stir at room temperature until the organic solvent volatilizes Completely, extract and filter, wash with purified water three times, freeze-dry to prepare allylgestrin microspheres.

[0044] Table 2 Composition of different surfactant formulations of allylgestrin microcapsules

[0045]

[0046]

[0047] The allylgestrin microsphere prepared by embodiment 2 is carried out quality research evaluation

[0048] The influence of table 3 different surfactants on allylgestrol microspheres

[0049] Surfa...

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Abstract

The invention relates to an altrenogest slow-release microsphere and a preparation method thereof. The preparation method comprises the following steps of dissolving altrenogest and a macromolecular material into an organic solvent, so as to form an oil phase; dissolving a releasing regulator and a flavor masking agent into a surfactant solution to form a water phase, and slowly adding the oil phase into a certain ratio of water phase, so as to form an O / W emulsion; adding the formed O / W emulsion into the residual water phase, and enabling the organic solvent to completely volatize; centrifuging, washing, and drying, so as to obtain the medicine microsphere. The altrenogest slow-release microsphere has the advantages that the slow-release effect is realized; after one-time administration,the altrenogest can be continuously and stably released for six days, so as to realize good slow release effect, and reduce the administration times of clinical medicine use; the occurrence of toxic or side effect and poor reaction is reduced, the palatability of the medicine is improved, the packaging rate is high and reaches 75% or above, the appearance is round, the granularity is large, and the dispersivity is good.

Description

Technical field: [0001] The invention relates to an allylgestin slow-release microsphere and a preparation method thereof, belonging to the technical field of veterinary medicines. Background technique [0002] my country is the world's largest pork producer and consumer, ranking first in the world in recent years. Pig raising is a traditional industry in my country. Recently, my country's pig raising is facing an era of structural adjustment, that is, it is gradually changing from free-range farming in the past to modern intensive farming. Modern intensive pig production requires that the breeding process of pigs can be more artificially controlled in order to realize batch management, so that the whole batch of sows can estrus, ovulate, breed and give birth at the same time. [0003] Sow estrus synchronization is a relatively new reproductive technology developed in recent years, that is, the use of hormones or other substances to artificially control and adjust the estru...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K9/50A61K47/34A61K31/567A61P15/08
CPCA61K9/5031A61K9/5089A61K31/567A61P15/08
Inventor 张智德魏秀丽黄娟王金美马庆祝王海挺
Owner QILU ANIMAL HEALTH PROD
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