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Slow-release mifepristone vaginal ring preparation and application thereof

A vaginal ring and sustained-release technology, applied in the directions of non-active ingredients medical preparations, female contraceptives, medical preparations containing active ingredients, etc. Effects of dissolution, improved bioavailability, improved bioavailability and drug compliance

Inactive Publication Date: 2012-07-25
NAT RES INST FOR FAMILY PLANNING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

02136837.6 disclosed the patent on the preparation of mifepristone semi-solid matrix preparations, 200610042252.6 reported the preparation of gels and films in vaginal formulations of mifepristone, and 200510027902.5, 03116893.0, 02111977.5, 01112712.0, etc. mentioned that mifepristone Pristone is prepared into a vaginal ring, but there is no detailed description of mifepristone vaginal ring preparations. 01268469.4 discloses a vaginal ring for slow-release mifepristone. The content of the invention does not describe the specific process, and there are no examples

Method used

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  • Slow-release mifepristone vaginal ring preparation and application thereof
  • Slow-release mifepristone vaginal ring preparation and application thereof
  • Slow-release mifepristone vaginal ring preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Drug: 30mg

[0037] PVP: 60mg

[0038] Silicone rubber: 2.91g

[0039] Using PVP as the dispersion medium, prepare mifepristone solid dispersion by solvent method, mix it with silicone rubber evenly to obtain drug-containing silicone rubber, cut it into a straight silicone rubber tube, put it into a mold, and vulcanize it on a flat plate Hot press vulcanization on the machine to obtain the mifepristone type A vaginal ring; press the silicone rubber into a thin skin with a thickness of 0.05 mm, wrap the silicone rubber ring prepared above, and hot press vulcanize to obtain the mifepristone type B vaginal ring ring.

Embodiment 2

[0041] Drug: 30mg

[0042] PEG6000: 60mg

[0043] Sodium dodecyl sulfate: 4mg

[0044] Silicone rubber: 2.906g

[0045] Weigh an appropriate amount of mifepristone, use PEG 6000 as a dispersion medium, prepare a solid dispersion by solvent method, add an appropriate amount of sodium dodecylsulfonate, mix it with a certain amount of silicone rubber, and obtain a drug-containing silicone rubber , cut into a straight silicone rubber tube, put it into a mould, and vulcanize it by hot pressing on a flat vulcanizer to obtain a mifepristone A-type vaginal ring; press the silicone rubber into a thin skin with a thickness of 0.05mm, and wrap it on the above-mentioned prepared The silicone rubber ring is molded by hot pressing and vulcanization, which is the mifepristone B-type vaginal ring.

Embodiment 3

[0047] Drug: 50mg

[0048] PVP: 100mg

[0049] Sodium dodecyl sulfate: 4mg

[0050] Silicone rubber: 4.846g

[0051] Using PVP as the dispersion medium, the mifepristone solid dispersion was prepared by the solvent method, adding an appropriate amount of sodium dodecyl sulfate, and mixing it with a certain amount of silicone rubber to obtain a drug-containing silicone rubber, which was cut into a straight The silicone rubber tube is put into the mold, and is hot-pressed and vulcanized on a flat vulcanizing machine to obtain a mifepristone A-type vaginal ring with a large cross-sectional area; the silicone rubber is pressed into a thin skin with a thickness of 0.05mm, and the silicon rubber tube prepared above is coated. The rubber ring is hot-pressed and vulcanized to obtain the mifepristone B-type vaginal ring.

[0052] Compared with the products of comparative examples, the products of Examples 1-3 of the present invention, the mifepristone A-type vaginal ring starts to rel...

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Abstract

The invention relates to a preparation method for two types of slow-release mifepristone vaginal ring preparations. The first type of slow-release mifepristone vaginal ring preparation includes from 1.0 to 4.5 wt% of mifepristone, from 1.5 to 13.5 wt% of drug scattered carrier, from 0.05 to 20 wt% of surfactant and from 62 to 97.45wt% of medical high polymer release control materials. The second type of slow-release mifepristone vaginal ring preparation includes from 1.0 to 4.5 wt% of mifepristone, from 1.5 to 13.5 wt% of drug scattered carrier, from 0.05 to 20 wt% of surfactant, from 62 to 97.45wt% of medical high polymer release control materials, and a thin release control membrane covered on the outside of each slow-release mifepristone vaginal ring preparation. Due to the preparation method, a slow-release mifepristone vaginal ring can slowly release the mifepristone within seven days, a first pass effect and gastrointestinal reaction of mifepristone orally taken drug are avoided, bioavailability of the drug and pharmacy compliance of a patient are improved.

Description

technical field [0001] The invention relates to the field of novel contraceptives, in particular to a slow-release vaginal ring preparation loaded with mifepristone and its application. Background technique [0002] With the rapid development of society and the continuous expansion of the world's population, it is imminent to actively adopt safe and effective contraceptive measures to control the population, improve the quality of the population and the health of the whole people. Moreover, the accelerated pace of life and increasingly fierce competition have increased the pressure on people, especially professional women, and gynecological diseases, such as uterine fibroids, are coming one after another. It can be seen that caring for women's health cannot be ignored. [0003] Mifepristone (Mifepristone) was originally developed and produced by the French company Roussel-Uclaf in the 1980s. It has strong anti-progestin and anti-glucocorticoid effects, but almost no progest...

Claims

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Application Information

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IPC IPC(8): A61F6/06A61K31/567A61K47/34A61P15/00A61P15/18
Inventor 付伟宁美英段雪艳张莹陈凯刘颖王佳庆
Owner NAT RES INST FOR FAMILY PLANNING
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