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Composite medicinal preparation containing conjugated estrogens

A technology combining estrogen and pharmaceutical preparations, applied in creams or ointments, can solve the problems of reducing bleeding risk, endometrial shedding, prolonged bleeding, etc. Effect

Inactive Publication Date: 2012-02-01
NANJING TEFENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Women supplement estrogen according to hormone replacement therapy, but due to individual differences and different specifications of estrogen products, estrogen in the body is often too high with estrogen supplementation, which stimulates endometrial shedding, causes uterine bleeding, and long-term time bleeding tendency
So far, in the published patents at home and abroad, there is no pharmaceutical preparation composed of conjugated estrogen and misoprostol, and there is no related application of the combination pharmaceutical preparation containing conjugated estrogen to reduce the risk of bleeding in hormone replacement therapy. patent

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: Combined estrogen misoprostol suppository

[0031] Raw Material No. 1 2 3 conjugated estrogen 0.01% 0.08% 3.2% Misoprostol 0.01% 0.03% 0.08% matrix 93% 96.64% 91.12% stabilizer Mannitol 4.8% Lactose 2.2% Glucose 2.2% buffer Citrate 2.18% Phosphate 1.05% Citric acid 3.4% β-cyclodextrin 0.8% 2.4% 0.2%

[0032] The preparation steps are:

[0033] ①Matrix preparation: mix a certain amount of gelatin with an equal amount of water, soak for 1 hour, heat to 80°C in a water bath to dissolve, then add a certain amount of glycerin, stir, and steam to remove excess water;

[0034] ②Add stabilizers, buffers, and β-cyclodextrin to the matrix, stir well, control the temperature at 37~40°C, add conjugated estrogen and misoprostol, stir well, and then pour in sterilized at 37~40°C Bacteria and coated with lubricant in the duckbill or bullet-shaped plug mold;

[0035] ③ Cool to normal room temperatur...

Embodiment 2

[0037] Example 2: Conjugated estrogen misoprostol cream

[0038] Raw Material No. 1 2 3 conjugated estrogen 0.01% 0.08% 3.2% Misoprostol 0.005% 0.03% 0.08% Sodium dodecyl sulfate 2.6% 4.8% 1.1% glycerin 20% 8% 16% Propylene Glycol Stearate 0.4% 1.6% 0.9% Ethylparaben 0.02% 0.5% 0.92% water 45.8% 68.93% 43.21% stearic acid 6.7% 5.2% 8.9% liquid paraffin 9.515% 2.36% 7.47% white beeswax 1.05% 2.75% 3.89% Glyceryl monostearate 2.4% 1.3% 4.83% cetyl alcohol 2.8% 1.85% 3.8% mineral oil 8.7% 2.6% 5.7%

[0039] The preparation steps are:

[0040] ① Preparation of oil phase: Take liquid paraffin, white peak wax, stearic acid, mineral oil, glyceryl monostearate, propylene glycol stearate, ethylparaben, and cetyl alcohol, mix them in a container, and heat on a water bath Melt to 50~100℃ to make oil phase;

[0041] ②Preparation of the water phase: Take sodium lauryl s...

Embodiment 3

[0045] Embodiment 3: Combined estrogen misoprostol ointment

[0046] Raw Material No. 1 2 3 conjugated estrogen 0.01% 0.08% 3.2% Misoprostol 0.005% 0.03% 0.08% Sodium dodecyl sulfate 2.6% 4.8% 1.1% glycerin 20% 8% 16.5% Propylene Glycol Stearate 0.4% 1.6% 0.9% Ethylparaben 0.02% 0.5% 0.92% water 45.8% 71.7 3% 43.71% Methyl stearate 6.9% 2.4% 10% liquid paraffin 9.315% 2.36% 5.37% white beeswax 1.05% 2.75% 3.89% Glyceryl monostearate 2.4% 1.3% 4.83% cetyl alcohol 2.8% 1.85% 3.8% mineral oil 8.7% 2.6% 5.7%

[0047] The preparation steps are:

[0048]① Preparation of the oil phase: Take liquid paraffin, white peak wax, methyl stearate, mineral oil, glyceryl monostearate, propylene glycol stearate, ethylparaben, and cetyl alcohol, mix them in a container, and put them in a water bath Heat and melt to 50~100℃ to make oil phase;

[0049] ②Preparation of water pha...

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PUM

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Abstract

The invention discloses a composite medicinal preparation containing conjugated estrogens, and the composite medicinal preparation is a suppository, cream or ointment. The preparation comprises the following components in percentage by weight: 0.01 to 4 percent of conjugated estrogens, 0.01 to 0.1 percent of misoprostol, 0.01 to 5 percent of stabilizing agent or bacteriostat, 0.8 to 4 percent of buffering agent or emulsifier, and 84.9 to 99.17 percent of human acceptable matrix. The medicinal preparation consisting of the oncjugated estrogens and misoprostol can be used for reducing uterus bleeding tendency caused by endometrium shedding due to estrogen supplement while preventing and treating climacteric syndrome appearing during physiological or induced menopause of females, as well as preventing and treating osteoporosis and coronary heart disease.

Description

Technical field [0001] The present invention involves a drug preparation composed of estrogen and meol, and the human body acceptable substrate, including suppository, milk paste or ointment, and also involves its preparation methods.The drug preparations composed of estrogen and macolycol alcohol can prevent and treat menopausal syndrome, prevention and treatment of osteoporosis and coronary heart disease that prevents and treat women's physiological or artificial menopause.The tendency of uterine bleeding caused by endometrial endometrium. Background technique [0002] In 1932, Geict and Sielmen proposed for the first time using estrogen for symptomatic treatment. In 1939, humans extracted estrogen from the pregnancy mother urine, and estrogen alternatives really started.Commodized production of hormone replacement products.There are two types of natural and synthetic types of estrogen. Its main components are more than ten sodium sodium sodium sodium sodium sodium sodium sodiu...

Claims

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Application Information

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IPC IPC(8): A61K31/566A61K31/565A61K31/5575A61P15/12A61P19/10A61P15/00A61P9/10
Inventor 陶亮何秀丽温天文李述彬朱怀柏夏秋月孙柏旺
Owner NANJING TEFENG PHARMA
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