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Testosterone undecanoate slow-release medicine composition, preparation method thereof and application

A technology of testosterone undecanoate and mixture, which is applied in the field of medicine and can solve problems such as injection pain, poor compliance, and short half-life

Active Publication Date: 2019-03-05
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, due to the short half-life of the drug (testosterone undecanoate is rapidly hydrolyzed by serum esterase after being absorbed into the blood), the patient takes soft capsules (3-4 capsules in total) multiple times a day, and the compliance is poor
[0006] The clinically used long-acting preparation testosterone undecanoate oil injection, its prescription consists of benzyl benzoate and injection oil, in which benzyl benzoate may cause allergic reactions, and oil may cause pulmonary oil embolism and injection pain and other adverse reactions

Method used

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  • Testosterone undecanoate slow-release medicine composition, preparation method thereof and application
  • Testosterone undecanoate slow-release medicine composition, preparation method thereof and application
  • Testosterone undecanoate slow-release medicine composition, preparation method thereof and application

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1－3

[0090] Preparation Example 1-3: Preparation of Testosterone Undecanoate Suspension (Sample 1-3)

[0091]

[0092] Preparation:

[0093] According to the above proportioning, at room temperature, soybean lecithin and docusate sodium were added into water and stirred, after the dispersion was uniform, the sieved testosterone undecanoate raw material was added, and mixed in a dispersing emulsifying homogenizer (Shanghai Hengchuan Machinery Co., Ltd. Company, C25) and fully disperse evenly again (Gear A, 2min), then pour it into the sample cup of a high-pressure homogenizer with a condensing device, and cycle several times under a low pressure of 200bar-300bar, until the ceramic beads and the valve seat are no obvious After the impact sound, pressurize to 500bar*10 to get 4.8μm crystal suspension (corresponding to sample 1), continue to 800bar*10, 1100bar*10 to get 1.2μm crystal suspension (corresponding to sample 2), Continue to 1300bar*10, and then 800bar*10 to obtain a 30...

preparation example 4－8

[0097] Preparation Example 4-8: Preparation of Testosterone Undecanoate Suspension (Sample 4-8)

[0098]Sample 4 prescription composition: 12.5 g of testosterone undecanoate, 1 g of Tween 20, and 0.5 g of docusate sodium.

[0099] Sample 5 prescription composition: 12.5 g of testosterone undecanoate, 2 g of polyethylene glycol 4000, and 1 g of docusate sodium.

[0100] Sample 6 prescription composition: 12.5 g of testosterone undecanoate, 1 g of hydroxypropyl cellulose, and 1 g of docusate sodium.

[0101] Sample 7 prescription composition: 12.5 g of testosterone undecanoate, 1 g of hypromellose, and 0.5 g of TPGS.

[0102] Sample 8 prescription composition: 12.5 g of testosterone undecanoate, 1 g of polysorbate 80, and 1 g of TPGS.

[0103] The preparation method is as follows:

[0104] According to the above proportioning, at room temperature, the two kinds of stabilizers of the prescribed amount are successively added into water and stirred, and after the dispersion is...

preparation example 9－11

[0107] Preparation example 9-11: Preparation of testosterone undecanoate freeze-dried powder (lyophilized samples 1-3)

[0108] Take 2ml each of samples 1-3 prepared in preparation examples 1-3 and place them in a vial, add mannitol with a solid content of 20%, mix well, pre-freeze at -60°C, and slowly heat at -40°C Sublimation under vacuum conditions, and finally heating and sublimation under vacuum at +25°C to obtain testosterone undecanoate freeze-dried powder, that is, freeze-dried samples 1-3. The specification is 0.25g / bottle.

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Abstract

The invention belongs to the technical field of medicines, and relates to testosterone undecanoate suspension, a preparation method thereof and an application, in particular to testosterone undecanoate suspension which comprises testosterone undecanoate, stabilizers and water. The content of the testosterone undecanoate is 10%-50%, the particle diameter D10 of the testosterone undecanoate is 0.2-0.5 micrometer, the particle diameter D50 of the testosterone undecanoate is 0.5-1.5 micrometers, the particle diameter D90 of the testosterone undecanoate is 2.2-6.0 micrometers, the stabilizers include first stabilizers and second stabilizers, the weight ratio of the first stabilizers to the second stabilizers is (1-10):(1-20), and the weight ratio of the testosterone undecanoate to the stabilizers is (1-20):(1-20). The testosterone undecanoate suspension is good in stability and high bioavailability and low in irritation, redissolved conditions after sedimentation are good, and in-vivo hormone level can be stably maintained for a long time.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a suspension of testosterone undecanoate, its freeze-dried preparation, its preparation method and application. Background technique [0002] Male hypogonadism is characterized by insufficient production of endogenous testosterone, resulting in abnormally low levels of circulating testosterone, ie, serum testosterone levels below 10 nmol / l. The clinical manifestations of male hypogonadism are varied. Testosterone deficiency is associated with symptoms of varying severity such as sexual dysfunction, loss of muscle mass and strength, depressed mood, and osteoporosis. Some men will experience male climacteric syndrome during the specific period from middle age to old age, which is due to the decline of androgen levels and abnormal androgen receptors caused by various factors. Nowadays, with the increase of social pressure, some young people will also have symptoms of hypogonadism. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/19A61K31/568A61K47/24A61K47/20A61P5/26A61P15/00A61P21/00A61P25/24A61P19/10
CPCA61K47/20A61K47/24A61K9/0019A61K9/10A61K9/19A61K31/568
Inventor 郑爱萍肖家超张慧李迎高静孙建绪
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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