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Pessulum containing hydrophilic lipophilic carrier

A vaginal ring, solid dispersion technology, applied in the direction of drug devices, other medical devices, etc.

Inactive Publication Date: 2014-02-19
SHANGHAI INST OF PLANNED PARENTHOOD RES +6
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is not mentioned in the prior art that it can be used as a special drug carrier, so that it can work together with the silicone rubber as the matrix of the vaginal ring to achieve double precise controlled release.

Method used

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  • Pessulum containing hydrophilic lipophilic carrier
  • Pessulum containing hydrophilic lipophilic carrier
  • Pessulum containing hydrophilic lipophilic carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Vaginal rings containing oxybutynin hydrochloride:

[0021] (1) 50 mg of oxybutynin hydrochloride and 150 mg of glyceryl monostearate were mixed, heated to 60° C., and cooled to obtain a solid dispersion.

[0022] (2) Preparation of emulsion: add 0.3g of diethanolamine to 10g of water, heat to 100°C, then slowly add 3g of preheated glyceryl monostearate, stir evenly and cool to obtain a drug-free emulsion. Mix 50 mg of oxybutynin hydrochloride and 150 mg of the emulsion evenly to obtain the drug-containing emulsion.

[0023] (3) Preparation of cream: add 0.2 g of poloxamer to 6 g of water, heat to 100°C, then slowly add 3 g of preheated glyceryl monostearate, stir evenly and cool to obtain a drug-free cream. 50 mg of oxybutynin hydrochloride and 150 mg of cream are uniformly mixed to obtain a drug-containing cream.

[0024] Preparation of Silicone Rubber Controlled Release Tube: The silicone rubber compound was mixed 5 times until soft, placed in a silicone rubber ext...

Embodiment 2

[0038] Vaginal ring containing oxybutynin hydrochloride

[0039] (1) 50 mg of oxybutynin hydrochloride and 200 mg of glyceryl monostearate were mixed, heated to 60° C., and cooled to obtain a solid dispersion.

[0040] (2) Preparation of emulsion: add 0.3g of diethanolamine to 10g of water, heat to 100°C, then slowly add 3g of preheated glyceryl monostearate, stir evenly and cool to obtain a drug-free emulsion. Mix 50 mg of oxybutynin hydrochloride and 200 mg of the emulsion evenly to obtain the drug-containing emulsion.

[0041] (3) Preparation of cream: add 0.2 g of poloxamer to 6 g of water, heat to 100°C, then slowly add 3 g of preheated glyceryl monostearate, stir evenly and cool to obtain a drug-free cream. Mix 50 mg of oxybutynin hydrochloride and 200 mg of cream evenly to obtain the medicated cream.

[0042] Preparation of Silicone Rubber Controlled Release Tube: The silicone rubber compound was mixed 5 times until soft, placed in a silicone rubber extruder, and extr...

Embodiment 3

[0046] Vaginal ring containing letrozole

[0047] (1) Mix 400 mg of letrozole and 150 mg of glyceryl monostearate, heat to 60°C and cool to obtain a solid dispersion.

[0048] (2) Preparation of emulsion: add 0.3g of diethanolamine to 10g of water, heat to 100°C, then slowly add 3g of preheated glyceryl monostearate, stir evenly and cool to obtain a drug-free emulsion. Letrozole 400mg and 150mg emulsion are uniformly mixed to obtain a drug-containing emulsion.

[0049] (3) Preparation of cream: add 0.2 g of poloxamer to 6 g of water, heat to 100°C, then slowly add 3 g of preheated glyceryl monostearate, stir evenly and cool to obtain a drug-free cream. Letrozole 400mg and 150mg cream are evenly mixed to obtain a medicated cream.

[0050] Preparation of Silicone Rubber Controlled Release Tube: The silicone rubber compound was kneaded 5 times until soft, placed in a silicone rubber extruder, and extruded according to the size of a silicone rubber tube with a length of 13 cm an...

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Abstract

The invention relates to a pessulum containing a hydrophilic lipophilic carrier. Particularly, the pessulum containing the hydrophilic lipophilic carrier comprises a silicone rubber tube and a mixture, wherein the silicone rubber tube is filled with the mixture containing medicine and glycerin monostearate. The weight ratio of the medicine to the glycerin monostearate is 1:50 to 50:1 and the mixture accounts for 5% to 30% of the weight of the silicone rubber tube. The invention further provides a preparation method of the pessulum. According to the pessulum containing the hydrophilic lipophilic carrier, the special carrier capable of accurately controlling medicine release is provided and is the glycerin monostearate. The hydrophilic lipophilic carrier promotes penetration of the medicine through the silicone rubber tube, silicone rubber has the release control characteristic, and therefore the purpose of double accurate release control is achieved.

Description

technical field [0001] The invention relates to a controlled-release vaginal ring containing a hydrophilic and lipophilic carrier. Background technique [0002] Some water-soluble or fat-soluble drugs or drugs with certain structural properties are simply put into the silicone rubber tube, and it is difficult to directly penetrate the tube wall of the silicone rubber tube, which may be caused by the basic properties of silicone rubber. Therefore, it is necessary to add a hydrophilic and lipophilic carrier to promote drug penetration through the silicone rubber, which has special properties of the controlled release tube wall. [0003] Glyceryl monostearate is an emulsifier and additive for food; it is used as an emulsifier in cosmetics and pharmaceutical ointments to make the paste delicate and smooth; it is used as an emulsifier for industrial silk oils and a lubricant for textiles; it is used in plastic films It can be used as dripping agent and anti-fogging agent; it can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61M31/00
Inventor 邵海浩李元春沈慈丹陈建兴陈旭峰袁维姝
Owner SHANGHAI INST OF PLANNED PARENTHOOD RES