Estradiol transdermal spray and its preparation method

Abstract

The invention discloses an estradiol transdermal spray and its preparation method. Each 8.1mL of the spray is composed of 130-145mg of estradiol, 650-750mg of 2-ethylhexyl salicylate, and the balance 95% ethanol. The estradiol transdermal spray avoids an unstable storage problem of a spray, improves the uniformity of the estradiol, improves the absorptivity and also enhances the drug effect. The estradiol transdermal spray has the advantages of realization of the entrance of the drug to the body in a continuous constant absorption rate for a long time after one-time administration, administration frequency reduction, lasting maintenance, stable and controllable plasma concentration or pharmacological effect, and enhancement of the treatment effect of the drug. A soup formed after the spray is sprayed on a skin surface can be rapidly dried, and forms a protection film on the administrated skin surface, so the transfer of the drug to clothes and other people through contact is difficult, and the average blood concentration of the drug in the body within 24h is not influenced by the cleaning of the administrated position 1h after the administration, thereby the drug compliance of a patient is enhanced.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an estradiol transdermal spray and a preparation method thereof. Background technique [0002] Estrogen is used in postmenopausal women with a uterus, and progesterone is used to reduce the risk of endometrial cancer. When using estrogen alone or in combination with a progestin, the lowest effective dose and the shortest duration of treatment should be prescribed to ensure consistency of treatment goals and risks for the individual woman. Treatment of postmenopausal women should be reassessed periodically at clinically appropriate intervals (eg, 3- to 6-month intervals) to determine whether continued treatment is warranted. [0003] Endogenous estrogens are primarily responsible for the formation and maintenance of the female reproductive system and secondary sex characteristics. Although there is a dynamic balance between metabolic transformations of estrogen in the ...

AI Technical Summary

Problems solved by technology

According to the prescription composition of a kind of estradiol spray disclosed in U.S. Patent No. 6,923,983, ethanol is used as the solvent, but the stability of the spray prepared according to the disclosed content of the patent is relatively poor, and the ethanol has serious damage during 6 months. The volatilization of the solution significantly reduces the homogeneity of the solution, resulting in a decrease in the absorption effect

[0013] Chinese patent CN102018672A discloses a kind of estradiol transdermal spray and its preparation method. In order to achieve the purpose of continuous and stable administration of estradiol transdermal spray, a polymer capable of forming a film is added to make estradiol Glycol transdermal sprays have good film-forming speed and film-forming properties when used. Although this film-forming spray solves the problem of drug effect persistence, it leads to poor skin air permeability when patients use it, which affects drug absorption. , there is a sense of stickiness, and it is uncomfortable and poorly compliant

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