2-methoxyestradiol transdermal liniment and 2-methoxyestradiol transdermal patch

Abstract

The invention relates to a 2-methoxyestradiol transdermal liniment and a 2-methoxyestradiol transdermal patch, effectively solving the problems of poor water-solubility, poor curative effect, the existence of liver first-pass effect, wide distribution in vivo of a 2-methoxyestradiol oral agent. The invention comprises two agent types of the 2-methoxyestradiol transdermal liniment and the 2-methoxyestradiol transdermal patch, wherein the 2-methoxyestradiol transdermal liniment comprises the following components in percentage by weight relative to total does of 100 percent: 74-98 percent of basic carrier, 0.5-2 percent of 2-methoxyestradiol and 1-25 percent of accelerant; and the 2-methoxyestradiol transdermal patch comprises the following components in percentage by weight relative to the total dose of 100 percent: 74-98 percent of basic carrier, 0.5-2 percent of 2-methoxyestradiol, 1-25 percent of accelerant, and 0.5-2 percent of hydroxypropylmethyl cellulose. The invention is convenient to use, enables the medicines to reach nidus directly through local transdermal permeation and enable the nidus to maintain higher curative concentration for a long time, thereby enhancing curative effect and avoiding liver first-pass effect and whole body distribution. The invention is an innovation in medicine.

Description

1. Technical field [0001] The invention relates to the field of medicine, in particular to a 2-methoxyestradiol transdermal liniment and a patch. 2. Background technology [0002] 2-Methoxyestradiol is an anticancer drug, mainly used in the treatment of breast cancer, prostate cancer and other diseases, and it is also an anti-inflammatory drug, used in the treatment of arthritis, etc., and its dosage form is oral tablet dose, taken 1 or 2 times a day. But the water solubility of this drug is poor, there is a certain liver first-pass effect, and the body is widely distributed. The curative effect of oral administration is not ideal, and it is difficult to maintain the effective therapeutic concentration of the target site. What about the liver's first-pass effect and liniments and patches that prevent systemic distribution? 3. Contents of the invention [0003] For the above situation, in order to overcome the defects of the prior art, the purpose of the present invention...

AI Technical Summary

Problems solved by technology

[0003] In view of the above situation, in order to overcome the defects of the prior art, the purpose of the present invention is to provide a kind of 2-methoxyestradiol transdermal liniment and patch, which can effectively solve the water-soluble problem of 2-methoxyestradiol oral preparations. Poor property, poor curative effect, hepatic first-pass effect is arranged, and the problem of wide distribution in the body, the technical scheme of its solution is, the present invention is made of 2-methoxyestradiol transdermal liniment and 2-methoxyestradiol transdermal There are two dosage forms of patch, wherein, 2-methoxyestradiol transdermal liniment is calculated by mass percentage: basic carrier 74%-98%, 2-methoxyestradiol 0.5%-2% and Accelerator 1-25%, the total amount is 100%, and 2-methoxyestradiol and accelerator are added to the basic carrier, and the liniment of the present invention is mixed uniformly or in mass percentage: basic carrier 74%- 98%, 2-methoxyestradiol 0.5%-2%, accelerator 1-25% and hydroxypropyl methylcellulose (HPMC) 0.5%-2%, the total amount is 100% to make 2-methoxy estradiol transdermal patch, add 2-methoxyestradiol and accelerator in the basic carrier, mix evenly, add hypromellose while stirring, stir evenly, place for 12-14 hours, get 2 - a viscous solution of methoxyestradiol, a release gasket coated with a polyester film (3M, USA) encapsulated in a rate-controlling membrane ethylene vinyl acetate (3M, USA) and a basement membrane polyester membrane (3M, USA ), heat seal, cut into a blank patch, respectively inject the viscous solution of 2-methoxyestradiol into the release ring from the unheated side of the blank patch with a syringe, heat seal, that is, the patch of the present invention agent; said basic carrier is a mixture made by mixing isopropyl myristate (IPM) and ethanol in a mass ratio of 7-9: 1-3; said accelerator is di-octyl succinate sulfonic acid Any one of sodium AOT, menthol, oil-soluble azone, N-methylpyrrolidone NMP, eucalyptus oil or a mixture of any two

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