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Progesterone sustained-release microcapsule preparation and preparation method thereof

A progesterone, sustained-release technology, applied in the field of medicine, can solve the problems of high bioavailability, low bioavailability, small dosage, etc., and achieve the effects of large distribution area, good reproducibility, and reduction of toxic and side effects

Active Publication Date: 2016-11-02
ZHEJIANG ASEN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] One of the objectives of the present invention is to propose a progesterone microcapsule with high dissolution rate and long action time in view of the defects of large dosage, low dissolution rate, short action time, low bioavailability and serious adverse reactions in the prior art Sustained-release preparation and preparation method thereof, so as to realize small dosage, less frequency of taking, high dissolution rate, high bioavailability and few adverse reactions

Method used

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  • Progesterone sustained-release microcapsule preparation and preparation method thereof
  • Progesterone sustained-release microcapsule preparation and preparation method thereof
  • Progesterone sustained-release microcapsule preparation and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0043]

[0044] Dissolve progesterone powder and soybean lecithin in soybean oil to obtain progesterone oil solution for later use; dissolve ethyl cellulose in acetone to obtain suspension a; under stirring state, add progesterone oil solution to Suspension a, to obtain suspension b. Tween-80 was dissolved in liquid paraffin to obtain solution c. Slowly add suspension b to solution c and stir for 30 minutes to make an emulsion. The emulsion is slowly added to a certain amount of distilled water, continuously stirred for 1-2 hours, then suction filtered, the solid is washed with water, dried, and packed into a capsule shell. For the preparation process, see figure 1 .

[0045] The particle size of the progesterone-ethylcellulose slow-release microcapsule is less than 150 μm, the progesterone content in the microcapsule is 2.0% (percentage by weight), and the cumulative dissolution rate of the progesterone in water for 24 hours is 92%. Figure 4 .

Embodiment 2

[0047]

[0048] Dissolve progesterone powder and egg yolk lecithin in peanut oil to obtain progesterone oil solution for later use; dissolve ethyl cellulose in ethyl acetate to obtain suspension a; under stirring state, mix progesterone oil solution, Added to suspension a to obtain suspension b. Dissolve SDS in liquid paraffin to obtain solution c. Slowly add suspension b to solution c and stir for 30 minutes to make an emulsion. The emulsion is slowly added to a certain amount of distilled water, continuously stirred for 1-2 hours, then suction filtered, the solid is washed with water, dried, and packed into a capsule shell.

[0049] The particle size of the progesterone-ethylcellulose sustained-release microcapsule is less than 100 μm, the progesterone content in the microcapsule is 5.0% (percentage by weight), and the cumulative dissolution rate of the progesterone in water for 24 hours is 97%.

Embodiment 3

[0051]

[0052] Dissolve progesterone powder and egg yolk lecithin in coconut oil to obtain progesterone oil solution for later use; dissolve ethyl cellulose in acetone to obtain suspension a; under stirring state, add progesterone oil solution to to suspension a to obtain suspension b. Polyethylene glycol laurate was dissolved in water to obtain solution c. Slowly add suspension b to solution c and stir for 30 minutes to make an emulsion. The emulsion is slowly added to a certain amount of distilled water, continuously stirred for 1-2 hours, then suction filtered, the solid is washed with water, dried, and packed into a capsule shell.

[0053] The particle size of the progesterone-ethylcellulose slow-release microcapsule is less than 150 μm, the progesterone content in the microcapsule is 4.0% (percentage by weight), and the cumulative dissolution rate of the progesterone in water for 24 hours is 82%.

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Abstract

The invention relates to a progesterone sustained-release microcapsule preparation and a preparation method thereof and belongs to the technical field of drugs. An oil solution is prepared from oil-soluble progesterone powder and the progesterone sustained-release microcapsule is prepared through an emulsification-solvent diffusing method. The progesterone powder is processed to form the oil solution so that solubility is improved. Through selection of a wall material, release in vitro and in vivo is improved. The prepared progesterone-ethyl cellulose sustained-release microcapsule has a drug loading ratio of 10%, particle sizes less than 150 microns and a large gastrointestinal tract distribution area, improves progesterone dissolvability, improves bioavailability, reduces gastrointestinal tract irritation and reduces drug toxic or side effects.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a progesterone microcapsule sustained-release preparation and a preparation method thereof. Background technique [0002] Progesterone is a human natural progesterone secreted by the corpus luteum of the ovary. It is necessary to maintain pregnancy and has the general effect of progesterone. It tends to act on the basis of the action of estrogen, enabling the endometrium to transition from the proliferative phase to the secretory phase, thereby promoting endometrial maturation, exfoliation, and maintenance of the menstrual cycle; it also prepares the uterus for embryo implantation , It can stabilize the endometrium and protect the fetus in the first trimester, which is a necessary condition for successful pregnancy. It is mainly used clinically for menstrual disorders, amenorrhea, dysfunctional uterine bleeding, corpus luteum insufficiency, threatened abortion and habitual abortion, prem...

Claims

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Application Information

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IPC IPC(8): A61K9/66A61K31/57A61K47/38A61P15/00A61P7/04A61P15/06
CPCA61K9/0002A61K9/5042A61K31/57
Inventor 邓金明
Owner ZHEJIANG ASEN PHARMA
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