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Oxybutynine ethosomal composition and preparation method thereof

A technology for oxybutynin alcohol and composition, which is applied in the field of oxybutynin-containing alcohol body composition and preparation thereof, and can solve the problems of low oxybutynin permeability and the like

Inactive Publication Date: 2014-07-02
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The above prior art does not solve the problem of low penetration rate of oxybutynin. The inventor unexpectedly found that the transdermal preparation of oxybutynin into ethosomes can significantly improve the transdermal rate of oxybutynin. The oxybutynin ethosome gel can not only significantly reduce the side effects of oxybutynin, but also improve the curative effect, which brings good news to patients, and has simple composition and preparation process, and is suitable for industrial production

Method used

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  • Oxybutynine ethosomal composition and preparation method thereof
  • Oxybutynine ethosomal composition and preparation method thereof
  • Oxybutynine ethosomal composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0108] This embodiment is the preparation of oxybutynin hydrochloride ethosome:

[0109]

[0110] The preparation process of the above prescription is as follows: Weigh the prescription amount of phospholipids and oxybutynin hydrochloride, dissolve them in absolute ethanol, stir at a mechanical speed of 700rpm in a water bath at 30°C, and slowly add the above alcohol solution dropwise into the water , and continue to stir for 30min, take it out, cool to room temperature, homogenize at a speed of 10000rpm for 1min, filter with a 0.22um filter membrane respectively, add an antioxidant, and stir evenly to obtain oxybutynin hydrochloride ethotoplast, its appearance It is a light yellow transparent liquid, and the particle size of the prepared ethosome is D 90 The values ​​are: Prescription 1: 485nm; Prescription 2: 285nm; Prescription 3: 106nm; Prescription 4: 55nm.

Embodiment 2

[0112] This embodiment is the preparation of oxybutynin hydrochloride ethosome:

[0113]

[0114] The preparation process of above-mentioned prescription is with embodiment 1. The particle size D of the prepared ethosomes 90 The values ​​are: Prescription 5: 326nm; Prescription 6: 164nm; Prescription 7: 48nm; Prescription 8: 30nm.

Embodiment 3

[0116] This embodiment is the preparation of oxybutynin hydrochloride ethosome:

[0117]

[0118] The preparation process of above-mentioned prescription is with embodiment 1. The particle size D of the prepared ethosomes 90 The values ​​are: Prescription 9: 650nm; Prescription 10: 360nm; Prescription 11: 92nm; Prescription 12: 210nm; Prescription 13: 293nm.

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Abstract

The invention relates to an oxybutynine ethosomal composition and a preparation method thereof. The oxybutynine ethosomal composition mainly comprises oxybutynine or a pharmaceutically acceptable salt, phospholipid, short-chain alcohol and water. The composition is prepared into a proper preparation form, such as gel and the like. The oxybutynine ethosomal composition is used for transdermal drug delivery and has higher permeation rate and bioavailability than those of an oxybutynine transdermal drug delivery preparation, such as gel and the like.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to an ethosome composition containing oxybutynin and a preparation method thereof. The ethosome composition of oxybutynin is mainly composed of oxybutynin or its pharmaceutically acceptable It consists of salts or solvates, phospholipids, short-chain alcohols and water. Background technique [0002] Oxybutynin is both an M3 receptor blocker and a calcium ion channel blocker. It has dual pharmacological effects of inhibiting bladder detrusor contraction, and is an effective clinical drug commonly used in the treatment of overactive bladder (OAB). [0003] The molecular formula of oxybutynin is shown in the figure below: [0004] [0005] Oxybutynin preparations currently on the market at home and abroad include oral solid preparations, oral solutions, transdermal patches, and gels. [0006] Oxybutynin is metabolized by the liver after oral administration, an...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/216A61K9/00A61K9/107A61K9/06A61K9/70A61K9/12A61P13/10
Inventor 张涛刘芬邓杰
Owner CHONGQING PHARMA RES INST
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