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Progesterone ethosome, and preparation method and application thereof

A progesterone and ethosome technology, which is applied in liposome delivery, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the limitations of the wide application of progesterone transdermal drug delivery system, cumulative penetration and penetration rate Low, no progesterone ethosomes reported, to achieve the effect of improving bioavailability and therapeutic index, reducing drug dosage and side effects, and simple method

Active Publication Date: 2012-04-04
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, the colostrum is often subjected to probe ultrasound under ice-water bath conditions to obtain ethosomes, but the probe will generate metal ions during the ultrasound process, which is easy to contaminate the sample. At the same time, the amount of sample prepared by this method is small, and it is difficult to realize industrialization. mass production
In addition, when the progesterone solution is directly used for transdermal research, its cumulative penetration and penetration rate are low, which limits the wide application of progesterone as a transdermal drug delivery system
And there is no report of progesterone ethosome in the prior art

Method used

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  • Progesterone ethosome, and preparation method and application thereof
  • Progesterone ethosome, and preparation method and application thereof
  • Progesterone ethosome, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049]The percentage in the prescription is the weight share ratio of this component in the whole prescription, and the following examples are the same.

[0050] Progesterone 0.125%

[0051] Yolk Lecithin 2.5%

[0052] Cholesterol 0.4%

[0053] Tween-80 1%

[0054] Ethanol 30%

[0055] The balance is deionized water

[0056] The preparation method step of progesterone ethosome is as follows:

[0057] Step 1: Fully mix and dissolve progesterone, egg yolk lecithin, cholesterol and absolute ethanol to form an alcohol phase; fully mix Tween-80 and deionized water to form a water phase;

[0058] Step 2: Heat the water phase and the oil phase to 40°C respectively, keep the temperature constant, add the alcohol phase to the water phase under stirring conditions, and make colostrum;

[0059] Step 3: Homogenize colostrum high-pressure milk to obtain a suspension;

[0060] Step 4: Stir the ethosome suspension for 30 minutes and perform secondary emulsification;

[0061] Step 5: ...

Embodiment 2

[0068] The percentage in the prescription is the weight share ratio of this component in the whole prescription, and the following examples are the same.

[0069] Progesterone 0.6%

[0070] Yolk Lecithin 2.5%

[0071] Cholesterol 0.4%

[0072] Tween-80 1%

[0073] Ethanol 30%

[0074] The balance is deionized water

[0075] The preparation method step of progesterone ethosome is as follows:

[0076] Step 1: Fully mix and dissolve progesterone, egg yolk lecithin, cholesterol and absolute ethanol to form an alcohol phase; fully mix Tween-80 and deionized water to form a water phase;

[0077] Step 2: Heat the water phase and the oil phase to 40°C respectively, keep the temperature constant, add the alcohol phase to the water phase under stirring conditions, and make colostrum;

[0078] Step 3: Homogenize colostrum high-pressure milk to obtain a suspension;

[0079] Step 4: Stir the ethosome suspension for 15 minutes for secondary emulsification;

[0080] Step 5: The suspe...

Embodiment 3

[0083] The percentage in the prescription is the weight share ratio of this component in the whole prescription, and the following examples are the same.

[0084] Progesterone 0.2%

[0085] Yolk Lecithin 3%

[0086] Tween-80 0.5%

[0087] Propylene Glycol 30%

[0088] The balance is deionized water

[0089] The preparation method step of progesterone ethosome is as follows:

[0090] Step 1: Fully mix and dissolve progesterone, egg yolk lecithin, and propylene glycol to form an alcohol phase; fully mix Tween-80 and deionized water to form a water phase;

[0091] Step 2: Heat the water phase and the oil phase to 30°C respectively, keep the temperature constant, add the alcohol phase to the water phase under stirring conditions, and make colostrum;

[0092] Step 3: Homogenize colostrum high-pressure milk to obtain a suspension;

[0093] Step 4: Stir the ethosome suspension for 20 minutes for secondary emulsification;

[0094] Step 5: The suspension is placed at 0-4°C, cool...

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Abstract

The invention provides a progesterone ethosome. Progesterone is encapsulated in an ethosome. The progesterone ethosome comprises the following components in percentage by weight: 0.1 to 1 percent of progesterone, 1 to 8 percent of lipid materials, 0 to 0.6 percent of cholesterol, 20 to 50 percent of short-chain alcohols, 0 to 3 percent of nonionic surfactant and the balance of water. The preparation method comprises the following steps of: mixing and dissolving the progesterone, the lipid materials, the cholesterol and the short-chain alcohols to prepare an alcohol phase; with stirring, adding the alcohol phase into a nonionic surfactant-containing aqueous phase to prepare primary emulsion under the condition of stirring; homogenizing the primary emulsion under a high pressure to obtain asuspension; stirring the ethosome suspension for 15 to 30 minutes to perform emulsification for the second time; and curing the suspension by cooling the suspension at 0 to 4 DEG C to obtain the progesterone ethosome. Because the high-pressure homogenization method is adopted to prepare the progesterone ethosome, the progesterone ethosome is low in stimulation to skin and high in transdermal delivery ability, and metal ion pollution which is easy to cause by the probe ultrasound method of the traditional homogenization method is avoided. Therefore, the progesterone ethosome is suitable for industrial production. The progesterone ethosome can be prepared into a transdermal drug delivery system, a mucosal drug delivery system, and topical dosage forms, such as a paster, a gel and the like. The progesterone ethosome is mainly applied to hormone replacement therapy, secondary amenorrhea, functional aplastic bleeding, premenstrual syndrome and the like clinically.

Description

technical field [0001] The invention relates to a progesterone ethosome and a preparation method and application thereof, belonging to the technical field of pharmacy. technical background [0002] Progesterone was synthesized and sold for the first time in 1934, which is exactly the same in structure and composition as endogenous progesterone. It often produces effects on the basis of estrogen, which can transform the endometrium from the proliferative phase to the secretory phase, thereby promoting the endometrial maturation, exfoliation and maintenance of the menstrual cycle; it can also prepare 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. [0003] Progesterone is a physiological hormone, which has the advantages of not counteracting the increase of high-density lipoprotein (HDL) and the reduction of cardiovascular disease (CVD). Clinically, it ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/57A61P5/34A61P15/00
Inventor 张蜀邓红林华庆张肖玲
Owner GUANGDONG PHARMA UNIV
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