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Soluble micro-needle containing slightly-soluble contraceptives and preparation method of soluble micro-needle

A contraceptive drug and insoluble technology, which is applied in the direction of medical preparations containing active ingredients, medical preparations with non-active ingredients, microneedles, etc., can solve the problems of slow drug transdermal rate and achieve improved transdermal penetration efficiency, Avoid stimulant effects

Inactive Publication Date: 2017-10-10
广州新济薇娜生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the currently marketed transdermal preparations are mainly patches. Due to the slow drug transdermal rate of patches, it is difficult to deliver a large amount of drugs in a short time. Therefore, the penetration of drugs can only be increased by prolonging the use time of patches. This is somewhat inconvenient

Method used

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  • Soluble micro-needle containing slightly-soluble contraceptives and preparation method of soluble micro-needle
  • Soluble micro-needle containing slightly-soluble contraceptives and preparation method of soluble micro-needle
  • Soluble micro-needle containing slightly-soluble contraceptives and preparation method of soluble micro-needle

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Embodiment 1

[0044] This embodiment provides a soluble microneedle containing a poorly soluble contraceptive drug and a preparation method thereof, the preparation method comprising the following steps:

[0045] 1) Preparation of base solution

[0046] Weigh 1 g of dextran 40 and dissolve it in 2 mL of deionized water, and swell overnight to obtain a base solution.

[0047] 2) Preparation of levonorgestrel cyclodextrin inclusion compound

[0048] Weigh 2g hydroxypropyl-β-cyclodextrin (1.3×10^ -3 mol) was dissolved in 2mL deionized water, and after stirring until completely dissolved, 0.03g levonorgestrel (9.6×10^ -5 mol), the mol ratio of levonorgestrel to hydroxypropyl-β-cyclodextrin is 1:13, and the magnetic stirring reaction is 2h, and then the solution is freeze-dried for 48h to obtain the levonorgestrel-cyclodextrin package compound.

[0049] 3) Preparation of needle tip solution

[0050] Weigh 1 g of dextran 40, dissolve it in 2 mL of deionized water, and swell overnight to obta...

Embodiment 2

[0054] This embodiment provides a soluble microneedle containing a poorly soluble contraceptive drug and a preparation method thereof, the preparation method comprising the following steps:

[0055] 1) Preparation of base solution

[0056] With embodiment 1.

[0057] 2) Preparation of levonorgestrel cyclodextrin inclusion compound

[0058] Weigh 6g hydroxypropyl-β-cyclodextrin (3.9×10^ -3 mol) was dissolved in 6mL deionized water, and after stirring until completely dissolved, 0.03g levonorgestrel (9.6×10^ -5 mol), the mol ratio of levonorgestrel to hydroxypropyl-β-cyclodextrin is 1:40, magnetic stirring reaction 2h, then this solution is freeze-dried 48h, obtains levonorgestrel cyclodextrin package compound.

[0059] 3) Preparation of needle tip solution

[0060] With embodiment 1.

[0061] 4) Preparation of soluble microneedles loaded with levonorgestrel

[0062] With embodiment 1.

Embodiment 3

[0064] This embodiment provides a soluble microneedle containing a poorly soluble contraceptive drug and a preparation method thereof, the preparation method comprising the following steps:

[0065] 1) Preparation of base solution

[0066] With embodiment 1.

[0067] 2) Preparation of levonorgestrel cyclodextrin inclusion compound

[0068] With embodiment 1.

[0069] 3) Preparation of needle tip solution

[0070] Weigh 1 g of dextran 40, dissolve it in 2 mL of deionized water, and swell overnight to obtain a dextran solution; weigh 1 g of levonorgestrel cyclodextrin inclusion compound and dissolve it in 1 mL of deionized water to obtain a drug-containing solution. Mix the dextran solution and the drug-containing solution at a ratio of 1:2 (v / v) to obtain the needle tip solution.

[0071] 4) Preparation of soluble microneedles loaded with levonorgestrel

[0072] With embodiment 1.

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Abstract

The invention relates to a soluble micro-needle containing slightly-soluble contraceptives and a preparation method of the soluble micro-needle. The soluble micro-needle comprises a base and a needle tip, wherein the needle tip is prepared by a cyclodextrin inclusion compound, a micro-needle framework material and a solvent, the cyclodextrin inclusion compound is prepared by the slightly-soluble contraceptives, beta-cyclodextrin and a solvent, and the mole ratio of the slightly-soluble contraceptives to the beta-cyclodextrin is 1:(1-40); the micro-needle framework material is selected from at least one of dextran, hyaluronic acid and chitosan; the mass ratio of the micro-needle framework material to the cyclodextrin inclusion compound is 1:(0.2-5). The soluble micro-needle has the advantages that the soluble micro-needle is good in mechanical performance and good in percutaneous absorption effect; compared with a traditional transdermal patch, the soluble micro-needle greatly increases the percutaneous penetration efficiency of drugs, has similar effects as oral-taking preparations and avoids drug irritation to gastrointestinal tracts.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a soluble microneedle containing a poorly soluble contraceptive drug and a preparation method thereof. Background technique [0002] Contraceptives, especially emergency contraceptives, are one of the commonly used contraceptive methods at present. The dosage forms of this type of drugs are mainly single drugs or compound preparations. Common dosage forms include tablets, drop pills and implants. Among them, the application of tablets most. However, during the use of the tablet, the gastrointestinal tract will be irritated and cause vomiting, which requires repeated administration, resulting in low compliance. Researchers at home and abroad have been committed to improving the shortcomings of traditional dosage forms to meet the contraceptive needs of different groups of people. [0003] Among many dosage forms, transdermal drug delivery has broad applicatio...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K47/69A61K45/00A61K47/26A61K47/36A61P15/18A61K31/567
CPCA61K45/00A61K47/26A61K47/36A61K9/0021A61K31/567A61M2037/0046A61M2037/0053
Inventor 陈航平李革姚港涛任春艳
Owner 广州新济薇娜生物科技有限公司
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