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Altrenogest nanometer emulsion and method for preparing same

A technology of tetraenylestrone and nanoemulsion, which is applied in the direction of emulsion delivery, pharmaceutical formula, medical preparations of non-active ingredients, etc., can solve the problem of not improving the reproductive rate of early weaned sows, increasing the birth weight of piglets, the number of piglets, Damage, poor stability and other problems, to achieve the effect of reducing labor and management costs, good thermodynamic stability, and good anti-corrosion performance

Inactive Publication Date: 2016-08-24
TIANJIN ZHONGSHENG TIAOZHAN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tetraenylestrone can cause sows to be in estrus at the same time, and can also increase the birth weight and number of piglets of piglets, reduce the generation of mummies, improve the delivery rate of sows, and prevent sows from premature birth and excessive backfat after weaning, but it cannot Improving the reproductive rate of early weaned sows
However, traditional oil solution preparations cannot improve the defects such as the steroid drug tetraenestrone being destroyed under acidic (gastric acid) conditions and poor stability after oral administration, resulting in low bioavailability, increased dosage, and increased Medication costs, etc., greatly limit its clinical application in veterinary medicine

Method used

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  • Altrenogest nanometer emulsion and method for preparing same
  • Altrenogest nanometer emulsion and method for preparing same
  • Altrenogest nanometer emulsion and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A tetraenylestrone nanoemulsion prepared from the following raw materials:

[0038]

[0039] The preparation method of above-mentioned tetraenylestrone nanoemulsion, comprises the steps:

[0040] (1) Under room temperature conditions, weigh the tetraenylestrone raw material according to the formula ratio and dissolve it in ethylene glycol first, and add the poloxamer and peanut oil in the formula amount, mix well and set aside;

[0041] (2) Use the water for injection of the formula amount as the water phase, and slowly add water for injection into the system at room temperature while stirring continuously until a clear and transparent liquid is formed, that is, the particle size is 10-100 nanometers, and the appearance is clear and uniform. tetraenestrone nanoemulsion.

Embodiment 2

[0043] A tetraenylestrone nanoemulsion is composed of the following raw materials:

[0044]

[0045] The preparation method of above-mentioned tetraenylestrone nanoemulsion, comprises the steps:

[0046] (1) At room temperature, weigh the tetraenestrone raw material according to the formula ratio and dissolve it in PEG-600 first, then add glyceryl monostearate and ethyl oleate in the formula amount, mix well and set aside;

[0047] (2) Use the water for injection of the formula amount as the water phase, slowly add the above water for injection into the system at room temperature, and keep stirring until a clear and transparent liquid is formed, that is, the particle size is 10-100 nanometers, and the appearance is clear. Uniform tetraenestrone nanoemulsion.

Embodiment 3

[0049] A tetraenylestrone nanoemulsion is composed of the following raw materials:

[0050]

[0051] The preparation method of above-mentioned tetraenylestrone nanoemulsion, comprises the steps:

[0052] (1) Under room temperature conditions, weigh the tetraenylestradione raw material according to the formula ratio and dissolve it in 1,2 propylene glycol, and add the polyoxyethylene ether hydrogenated castor oil (RH-50) and cottonseed oil of the formula amount, mix uniform spare;

[0053] (2) Use the water for injection of the formula amount as the water phase, slowly add the above water for injection into the system at room temperature, and keep stirring until a clear and transparent liquid is formed, that is, the particle size is 10-100 nanometers, and the appearance is clear. Uniform tetraenestrone nanoemulsion.

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Abstract

The invention provides altrenogest nanometer emulsion and a method for preparing the same. The altrenogest nanometer emulsion comprises, by weight, 0.1-1 part of altrenogest, 15-35 parts of surfactants, 1.5-20 parts of auxiliary surfactants, 2-30 parts of oil and 26-45 parts of water for injection. The altrenogest nanometer emulsion and the method have the advantages that the altrenogest nanometer emulsion is good in thermodynamic stability, stable emulsion states can be completely recovered after the altrenogest nanometer emulsion is heated until the temperature of the altrenogest nanometer emulsion reaches 80 DEG C, then the altrenogest nanometer emulsion is allowed to stand still and then is sufficiently vibrated, the altrenogest nanometer emulsion is good in storage stability, layering can be prevented after the altrenogest nanometer emulsion is allowed to stand for a long time, the altrenogest nanometer emulsion not only can be orally administered by the aid of drinking water, but also can be administered after being mixed with materials, oral administration nano-emulsion substrates can effectively protect the altrenogest from being damaged by gastric acid, and the shortcoming of first-pass effects of livers can be overcome; the method for preparing the altrenogest nanometer emulsion is simple, and accordingly requirements of large-scale industrial production can be met.

Description

technical field [0001] The invention relates to a tetraenylestrone pharmaceutical preparation and a preparation method thereof, in particular to a tetraenylestrone nanoemulsion and a preparation method thereof. Background technique [0002] Tetraenestrone (also known as allylgestrol) is a progestogen structurally related to the veterinary steroid trenbolone, a synthetic trienic C21 steroidal progestogen belonging to the 19-nortestosterone class. It is an orally active progestin. Like all steroids, tetratenestrone can penetrate into target cells through its own fat solubility and then bind to specific receptors to play a role. Its mode of action is similar to that of natural progesterone to inhibit the release of gonadotropins. Estrus drugs. [0003] In the veterinary field, tetraenylestrone is used to synchronize estrus in mare and sow. Tetraenylestrone can cause sows to be in estrus at the same time, and can also increase the birth weight and number of piglets of piglets...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K9/08A61K31/567A61P15/08
CPCA61K9/08A61K9/1075A61K31/567A61K47/44A61K47/10
Inventor 焦晓军龚伟勤韩贞珍程雪娇王建朱士江季昆王勇王猛余贵菊甄盼盼杨雪崔志刚张立会姜淋洁于小婷李丽琴王宇鹏李玲范庆增
Owner TIANJIN ZHONGSHENG TIAOZHAN BIOTECH
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