CN1470239A

CN1470239A - Testosterone intradermic sustained preparation

Info

Publication number: CN1470239A
Application number: CNA021266832A
Authority: CN
Inventors: 王怀秀
Original assignee: Individual
Current assignee: Individual
Priority date: 2002-07-28
Filing date: 2002-07-28
Publication date: 2004-01-28

Abstract

The invention is a percutaneous absorptive preparation of teststerone. Spread teststerone percutaneous absorption preparation on the skin of scrotum or other parts, the teststerone can permeate the skin to slowly and continuously enter blood circulation, which not only effectively increases teststerone blood concentration, but also keeps teststerone blood concentration stable, so as to achieve the androgen substitution cure for the male sufferer whose gonad function is low.

Description

Testosterone intradermic sustained preparation

The present invention is the percutaneous delayed testosterone-releasing preparation that is used for male gonad hypofunction patient.

Male gonad hypofunction patient PA level is low, shows as the manlike obstacle of sexual dysfunction and secondary sex characteristics.Its Therapeutic Method is an androgen replacement.Treated with oral testosterone, but medicine after being absorbed, digestive tract is at first gone into liver through portal vein wherein most of i.e. inefficacy before the performance drug effect because first pass effect is decomposed in the past.17 α-alkanisation androgen such as methyl testosterone can delay catabolism, but prolonged application can cause cholestasis hepatitis even hepatocarcinoma, so should not be used for the long-term replacement therapy of male gonad hypofunction patient.Though the injection testosterone can be avoided first pass effect, the medicine blood concentration raises immediately significantly after injection, descends rapidly again thereafter, does not meet physiological requirement.It is relatively stable that testosterone subdermal implantation method can be kept the plasma testosterone level, and a heeling-in can be kept 4-6 month, performs the operation but cost an arm and a leg and need, and is difficult for being accepted by the patient.

The transdermal formulation that the objective of the invention is to contain testosterone be coated in scrotum or the skin at other position of being easy to absorb on, the testosterone intradermic skin is slowly absorbed constantly, keep more stable PA concentration, reach hormone replacement therapy effect male gonad hypofunction patient.

Above-mentioned purpose realizes by following measure.The method of preparation testosterone intradermic absorbable preparation is exemplified below:

Prescription: stearic acid 110g, propylene glycol 100g, 10% ammonia solution 30ml, 10% hibitane alcohol liquid 5ml, ethanol 30ml, testosterone 10g, adding distil water make total amount become 1000g.

Compound method: (1) is dissolved in the 10g testosterone in 30ml ethanol and the 70g propylene glycol; (2) the 700ml distilled water is heated to 85-90 ℃, adds stearic acid 110g, constantly be stirred to molten entirely; (3) keep 85 ℃ of temperature, stir adding 10% ammonia solution down, stirred 2-3 minute; (4) add testosterone solution and 5ml10% hibitane alcohol liquid, stirred 15 minutes; (5) with above-mentioned product chilling, room temperature was placed 10-12 hour then, will remain 30g propylene glycol and distilled water mixed liquor again and add, and made total amount become 1000g, stirred evenly.

After preparation finishes, the testosterone intradermic absorbable preparation is packed.During use, regularly evenly be coated on a certain amount of transdermal formulation on the skin at patient's scrotum or other position every day, massages, and disappears until transdermal formulation.

Theoretical basis and advantage that testosterone intradermic absorbs are as follows: the molecular weight of (1) testosterone is less than 300, and is fat-soluble, is easy to enter blood circulation by skin, can effectively improve the haemoconcentration of testosterone, the first pass effect when having avoided oral testosterone simultaneously.(2) slow releasing function had been played in the slowly release of the blood capillary in dermal tissue after the epidermis of skin absorbed the drug, and can make the haemoconcentration of testosterone keep stable.(3) because applied testosterone is a normal hormone in the body, so human body is had no side effect.

At human body, the efficient difference of the skin absorbs medicine of different parts.Through scrotum applications of testosterone transdermal formulation following advantage is arranged: the principal element that (1) influences drug absorption is the cuticle thickness and the shallow degree of blood capillary distribution table of epidermis.The skin of scrotum horny layer as thin as a wafer, blood capillary distributes and almost to reach epidermal area and abundanter.According to surveying and determination, to some drugs, the infiltration rate of scrotum is 10 times of skin of abdomen, is 100 times of vola skin; (2) androgenic physiological action mainly is to realize by the dihydrotestosterone that testosterone generates after 5 α-reduction.Because of containing abundant 5 in the skin of scrotum, a part of testosterone promptly is converted into dihydrotestosterone in absorption process, and blood plasma dihydrotestosterone concentration is obviously improved, the performance higher physiological activities; (3) when scrotum absorbs testosterone, the therapeutic dose testosterone is no more than normal range through the estrogen that aromatization produces.

Claims

A kind of transdermal formulation that is used for male gonad hypofunction patient is carried out the testosterone replacement therapy is characterized in that said preparation is made up of testosterone, transdermal formulation substrate.