Methimazole microemulsion, methimazole microemulsion gel and preparation method and application thereof

A technology of methimazole and microemulsion gel, which is applied in the field of microemulsion gel transdermal preparation and its preparation, and the field of methimazole microemulsion for the treatment of hyperthyroidism, which can solve the problem of limited transdermal application and difficult penetration of hydrophilic drugs Skin and other problems, to achieve the effect of reducing the number of administration, improving drug loading capacity, and increasing penetration

Active Publication Date: 2019-01-11
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Methimazole (MML) has a molecular weight of 114.16 and a melting point of 143-146°C. It is suitable for transdermal administration, but its structure contains sulfhydryl groups. It is a hydrophilic drug and its solubility in water can be as high as 200mg / mL , and hydrophilic drugs are difficult to penetrate the skin, thus limiting its transdermal application

Method used

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  • Methimazole microemulsion, methimazole microemulsion gel and preparation method and application thereof
  • Methimazole microemulsion, methimazole microemulsion gel and preparation method and application thereof
  • Methimazole microemulsion, methimazole microemulsion gel and preparation method and application thereof

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Embodiment 1

[0039]

[0040] Preparation Process:

[0041] 1) Weigh the oil phase, surfactant, and co-surfactant of the prescription amount, and mix evenly under magnetic stirring;

[0042] 2) Weigh the prescribed amount of water and add it dropwise to the above-mentioned mixed solution, and after mixing evenly under magnetic stirring, a blank microemulsion solution is obtained;

[0043] 3) Add the prescribed amount of transdermal accelerator into the microemulsion solution, and mix evenly under magnetic stirring;

[0044] 4) Add the prescribed amount of methimazole raw material drug into the blank microemulsion, the ultrasonic temperature is 25°C, and after 5 minutes of complete dissolution, a transparent drug-containing microemulsion solution is obtained;

[0045] 5) Add the prescribed amount of gel matrix into the above microemulsion, and stir evenly after it is fully swollen to obtain a uniform microemulsion gel.

Embodiment 2

[0047]

[0048] Preparation method: with embodiment 1

Embodiment 3

[0050]

[0051] Preparation method: with embodiment 1

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Abstract

The invention relates to methimazole microemulsion, methimazole microemulsion-based gel and a preparation method and application of the methimazole microemulsion. The methimazole microemulsion comprises methimazole, oil, surfactant, cosurfactant, water and transdermal Enhancer according to a weight ratio of 1:(1.40-4.25):(5.13-15.45):(5.13-15.45):(1.40-8.32):(0.26:1.26). The methimazole microemulsion-based gel is prepared by adding gel matrix into the methimazole microemulsion, allowing swelling and performing uniform mixing. The methimazole microemulsion and the methimazole microemulsion-based gel are directly applicable to affected parts, are also applicable to the preparation of hyperthyroidism pharmaceuticals such as patches or plasters, and have the advantages such as good solubility, high penetration capacity, long acting time, evident improvement in therapeutic effect, fewer times of administration, and convenience of administration.

Description

technical field [0001] The invention relates to a new dosage form of methimazole, in particular to a methimazole microemulsion and microemulsion gel transdermal preparation for treating hyperthyroidism, a preparation method and application thereof. Background technique [0002] Hyperthyroidism (hyperthyroidism, referred to as hyperthyroidism) is the thyrotoxicosis caused by the excessive production of thyroid hormone by the thyroid gland itself. Goiter, memory loss, emotional instability, depression, lethargy, fatigue, weakness of limbs, muscle atrophy, loss of appetite, indigestion, constipation, nausea, vomiting, polyuria, nocturia, thirst, tachycardia, Symptoms such as nervousness and weight loss. The incidence of hyperthyroidism is increasing year by year, and it has become the second most serious endocrinology disease after diabetes. According to data from the 2013 International Thyroid Knowledge Awareness Week press conference, there are currently more than 15 million...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/70A61K9/06A61K31/4164A61K47/22A61P5/16
Inventor 纪宏宇吴琳华庄宇婷毛雨婷
Owner HARBIN MEDICAL UNIVERSITY
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