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Alltrenogest sustained-release injection and preparation method and application thereof

A technology for allyrogestin and injection, which is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and medical preparations without active ingredients, etc. Sexual issues, etc.

Active Publication Date: 2021-09-07
JIANGXI AGRICULTURAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the case of a large number of gilts, it takes a lot of manpower and time to spray and squeeze oral administration one by one, and the cooperation of the pigs is required.
The clinical experience of some pig farms shows that this method of use is not convenient, the compliance of pigs to drug administration is not good, and it is easy to cause over-dosing, under-dosing, and repeated dosing.

Method used

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  • Alltrenogest sustained-release injection and preparation method and application thereof
  • Alltrenogest sustained-release injection and preparation method and application thereof
  • Alltrenogest sustained-release injection and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1: the preparation of allyl progesterone injection

[0022] An allylgestrine injection, the preparation method of which comprises: weighing dimethyl sulfoxide and sucrose acetate isobutyrate, and mixing them at a mass ratio of 4:1 at 27°C to obtain a clear, precipitate-free, transparent solvents such as figure 1 As shown, then add allylgestrine, the preparation obtains the allylgestrine content that is 160mg / mL clarification does not have the allylgestrine injection of precipitation, as figure 2 shown.

Embodiment 2

[0023] Embodiment 2: the mensuration of release degree in vitro

[0024] (1) First prepare 0.01mol / L PBS buffer solution of pH7.4, mix 1.6gNaCl, 0.04g KH 2 PO 4 , 0.58gNa 2 HPO 4 , 0.04g KCl was added to the beaker, dissolved with a certain amount of distilled water, then transferred to a 200mL volumetric flask for constant volume, and finally the pH of the solution was adjusted to 7.4 with HCl.

[0025] Take 5mL of absolute ethanol into a 10mL volumetric flask, and then dilute with PBS buffer to prepare 50% ethanol PBS buffer.

[0026] (2) Three parts (injections 1, 2, 3) of the allylgestrine injection in Example 1 (the content of allylgestrine is 160 mg / mL), one part without allylgestrine and only dimethyl The blank injection of sulfoxide and sucrose acetate isobutyrate (dimethyl sulfoxide and sucrose acetate isobutyrate were mixed at a mass ratio of 4:1 at 27°C to obtain a clear solution without precipitation, transparent solvent), a part of dimethyl sulfoxide solution...

Embodiment 3

[0035] Embodiment 3: the mensuration of recovery rate and stability

[0036] (1) Preparation of standard curve

[0037] Prepare a solution of allylregestin absolute ethanol with a concentration of 1 mg / mL as the mother liquor, and dilute the mother liquor into 100 μg / mL, 80 μg / mL, 60 μg / mL, 40 μg / mL and 20 μg / mL of allylregestin absolute ethanol standard solution. Using absolute ethanol as a blank, measure the absorbance of the standard solution of each concentration respectively, and record it well, and make a standard curve. The results are as follows: Figure 4 As shown, the correlation coefficient r 2 >0.99, good linear performance.

[0038] (2) determination of content, recovery and stability

[0039] Get 4 samples of allylgestrine sustained-release injection in Example 1 (corresponding to 0-3), be mixed with dehydrated alcohol into 20, 40, 80 μ g / mL allylgestrine solution, measured content, recovery The rates and coefficients of variation are shown in Table 2. It can...

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Abstract

The invention discloses an altrenogest injection and a preparation method and application thereof. The altrenogest injection is obtained by mixing altrenogest and a solvent, and the solvent is obtained by mixing dimethyl sulfoxide and sucrose acetate isobutyrate according to the mass ratio of 4 to 1. The prepared altrenogest sustained-release injection can realize in-vitro slow release, is good in stability, can reduce the administration frequency of pigs, reduces the labor intensity of administration work, and can effectively popularize a sow estrus synchronization technology.

Description

technical field [0001] The invention belongs to the field of preparations for suppressing estrus in sows, and in particular relates to an allylgestrine sustained-release injection and a preparation method and application thereof. Background technique [0002] Altrenogest is a synthetic animal progestogen, which is a progesterone-mimetic drug, and is mostly used clinically to promote regular estrus in female animals. Its appearance is white crystalline powder, which is fat-soluble and easily penetrates into target cells, and then binds to specific receptors. Allylprogesterone was originally developed by Intervet / Schering-Plough Animal Health Products Company as an oil-based spray-squeeze oral agent, administered continuously for 18 days at a dose of 20mg / d per sow, which can inhibit estrus and achieve synchronous estrus, thereby effectively regulating The production rhythm of sows is adjusted from scattered breeding to batch breeding to realize cycle production. In terms of...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K31/567A61K47/20A61K47/26A61P15/08
CPCA61K31/567A61K9/0019A61K47/20A61K47/26A61K9/08A61P15/08
Inventor 王忠王立琦刘宝生王小莺鲍光明彭剑玲黄小晴
Owner JIANGXI AGRICULTURAL UNIVERSITY
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