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Dihydrotestosterone in-situ gel spray and preparation method thereof

A dihydrotestosterone and in-situ gel technology, which is applied in aerosol delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problem of full absorption of unfavorable drugs and speed of onset of effects, affecting drug absorption, and high therapeutic effect. Cost and other issues, to achieve good bioavailability and bioequivalence, improve transdermal penetration, and improve the effect of use compliance

Active Publication Date: 2019-05-03
GUANGDONG FOOD & DRUG VOCATIONAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are also some deficiencies: ①The method of use is unhygienic and inconvenient
When using Andractim gel, squeeze the gel on the genitals, and use tools or fingers to apply it on the root of the penis and the surface of the scrotum. When using tools or fingers, the gel drug may be contaminated and the operation is inconvenient; ②Andractim gel is not evenly applied , not conducive to the full absorption of the drug
Andractim gel coating is based on personal habits and experience. It is difficult to ensure uniform coating, and there are many folds in the scrotum. The gel is semi-solid and difficult to apply on the surface of the folds. In fact, the folds of the scrotum have a large surface area, which is a double Hydrotestosterone absorbs the main part through the genitals, which will greatly affect the absorption of drugs through the skin of the genitals, and will limit the drug content and speed of drug percutaneous penetration, which is not conducive to the full absorption of drugs and the speed of onset of action; ③The dosage of Andractim gel is arbitrary, which is not conducive to Play the best effect
The dosage of Andractim gel, according to personal habits and experience, the amount of extruded gel is more random, there is no clear dosage definition, and it is impossible to accurately control the dosage, which is not only detrimental to the efficacy of the drug, but also may lead to drug waste; ④ Andractim gel price Higher, increasing the economic burden of patients, it is not easy for most patients to take long-term medication
Andractim gel is not approved for import in my country, and can only be obtained through overseas purchases or purchasing agents. The overseas price is equivalent to more than RMB 1,500 per piece. The price is high, and long-term medication is required. The families of ordinary patients cannot afford such high treatment costs.

Method used

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  • Dihydrotestosterone in-situ gel spray and preparation method thereof
  • Dihydrotestosterone in-situ gel spray and preparation method thereof
  • Dihydrotestosterone in-situ gel spray and preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0036] A kind of preparation method of above-mentioned dihydrotestosterone in situ gel spray of the present invention, comprises the following steps:

[0037] (1) Preparation of dihydrotestosterone ethosomes: mix dihydrotestosterone, phospholipids, cholesterol and absolute ethanol, dissolve; add to the water phase under stirring conditions, homogenize, filter, and obtain dihydrotestosterone ethosomes ;

[0038] (2) Preparation of dihydrotestosterone in-situ gel spray: add temperature-sensitive gel excipients and viscosity modifiers into water to fully swell; refrigerate at 0-7°C; The body is mixed evenly, and the transdermal accelerator, antiseptic and moisturizing agent are added to mix evenly, the pH regulator is added, and water is added to obtain the dihydrotestosterone in-situ gel spray.

[0039] Specifically, in step (1), the stirring speed is 800r·min -1 ~1000min -1 . The method of homogenization is 8000~12 000r·min at 22-25°C -1 Stir at a constant speed for 4 to 6...

Embodiment 1

[0045] The preparation of embodiment 1 dihydrotestosterone oligosome

[0046] Precisely weigh 2.50 g of dihydrotestosterone, 15.00 g of soybean lecithin, and 1.00 g of cholesterol in 35 mL of absolute ethanol (density: 0.789 g ml -1 ), set a magnetic stirrer to stir 500r·min -1 To dissolve completely, and transfer to the syringe barrel. Take another 53.885g of distilled water in the Erlenmeyer flask, water bath 30°C, magnetic stirring 900r·min -1 , under sealed conditions, slowly drop the liquid in the syringe into the Erlenmeyer flask, continue to stir for 10 minutes after the dropwise addition, cool to room temperature, homogenize (magnetic stirring 10 000r min -1 ) for 5 minutes, filtered through a 0.22 μm microporous membrane, sealed and stored at 4°C.

Embodiment 2

[0047] The preparation of embodiment 2 dihydrotestosterone ethosomes

[0048] Precisely weigh 5.00 g of dihydrotestosterone, 20.00 g of soybean lecithin, and 0.50 g of cholesterol according to the prescription amount of 100 g of ethanol, and dissolve them in 40 mL of absolute ethanol (density: 0.789 g ml -1 ), set a magnetic stirrer to stir 500r·min -1 To dissolve completely, and transfer to the syringe barrel. Take another 42.94g of water for injection in the Erlenmeyer flask, water bath at 30°C, and magnetically stir at 900r min -1 , under sealed conditions, slowly drop the liquid in the syringe into the Erlenmeyer flask, continue to stir for 10 minutes after the dropwise addition, cool to room temperature, and ultrasonically (200W, ultrasonic 2s, stop 1s) in the ice bath for 1min, use Filter through a 0.22 μm microporous membrane, seal and store at 4°C.

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Abstract

The invention relates to a dihydrotestosterone in-situ gel spray and a preparation method thereof. The dihydrotestosterone in-situ gel spray is prepared from the following raw materials in percentageby mass of 25.00-75.00% of a dihydrotestosterone ethosome, 10.00-40.00% of a temperature-sensitive gel material, 0.50-10.00% of a transdermal enhancer, 0.50-10.00% of a humectant, 0-5.00% of a viscosity regulating agent, 0-5.00% of a pH regulator, 0-5.00% of a corrosion remover and 5.00-40.00% of water. The dihydrotestosterone ethosome is prepared from the following raw materials in percentage bymass of 0.10-20.00% of dihydrotestosterone, 5.00-30.00% of phospholipid, 0-5.00% of cholesterol, 20.00-50.00% of absolute ethyl alcohol, and 30.00-60.00% of water. The dihydrotestosterone in-situ gelspray has favorable pharmacokinetics and pharmacokinetic characteristics, is convenient to use, uniform to apply and controllable in administration dosage.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a dihydrotestosterone in-situ gel spray and a preparation method thereof. Background technique [0002] Micropenis is not uncommon in pediatric clinical practice. It is the most common sign of virilization and is caused by insufficient androgen production. It is often accompanied by other external genital dysplasia such as small testes, cryptorchidism, and small scrotum. According to epidemiological surveys, between 1985 and 2006, the incidence of micropenis in American children was about 2.6%. In recent years, with people's emphasis on children's reproductive development and the application of early diagnosis technology using small puberty hormone level changes, the demand for children's micropenis treatment drugs is becoming increasingly urgent. [0003] The development of the penis mainly depends on the androgen-testosterone secreted by the Leydig cells of the testi...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K9/06A61K9/127A61K47/24A61K47/28A61K47/10A61K31/568A61P15/00
Inventor 聂阳丁立黄海潮陈维佳郑海肖春芬郭珅珅
Owner GUANGDONG FOOD & DRUG VOCATIONAL COLLEGE
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