Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Microemulsion transdermal gel agent of butylphthalide or derivative thereof, and preparation method thereof

A derivative, butylphthalide technology, applied in the field of medicine, can solve the problems of difficult industrialized production, improved water solubility, and many key control points, so as to improve the safety and comfort of medication, reduce irritation, and reduce oiliness. effect of feeling

Active Publication Date: 2011-09-14
SHIJIAZHUANG PHARMA GRP NBP PHARMA CO LTD
View PDF14 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Because butylphthalide is an oily liquid that is insoluble in water, it is difficult to make suitable preparations. Chinese patent CN200310119336.1, titled "Butylphthalide Soft Capsules and Its Preparation Process", discloses that butylphthalide is dispersed in vegetable oil as a The soft capsules were prepared from the contents, but because there was no link to improve its water solubility in the process of preparing soft capsules, this had a certain impact on the absorption of its products after disintegration in the body
Chinese patent CN200510102355.2, titled "Butylphthalide Intravenous Emulsion and Its Application", discloses that butylphthalide is made into intravenous emulsion. Although the water solubility of butylphthalide is improved, the preparation process requires high-speed shearing and homogenization. , industrialized production is difficult and costly
At present, the dosage forms of butylphthalide on the market include soft capsules and injections. Although the injections that have been marketed overcome the first-pass effect of oral dosage forms and improve the speed of onset of action, the preparation process of injections is complicated and there are many key control points. Moreover, the patient compliance of the injection dosage form is poor

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Microemulsion transdermal gel agent of butylphthalide or derivative thereof, and preparation method thereof
  • Microemulsion transdermal gel agent of butylphthalide or derivative thereof, and preparation method thereof
  • Microemulsion transdermal gel agent of butylphthalide or derivative thereof, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Butylphthalide 0.2g;

[0046] Medium-chain triglycerides 1.6g;

[0047] Polyoxyethylene hydrogenated castor oil 2g;

[0048] Glycerin 1g;

[0049] Azone 0.1g;

[0050] Purified water 5g;

[0051] Weigh butylphthalide, add it to medium-carbon chain triglyceride, stir evenly, then add polyoxyethylene hydrogenated castor oil and glycerin, mix evenly, add azone, then add purified water, stir to make it a microemulsion gel, Its particle size was measured to be about 68nm.

Embodiment 2

[0053] Butylphthalide 0.4g;

[0054] Medium-chain triglycerides 2g;

[0055] Polyoxyethylene hydrogenated castor oil 2g;

[0056] Glycerin 1g;

[0057] Azone 0.1g;

[0058] Purified water 4.6g;

[0059] Weigh butylphthalide, add it to medium-carbon chain triglyceride, stir evenly, then add polyoxyethylene hydrogenated castor oil and glycerin, mix evenly, add azone, then add purified water, stir to make it a microemulsion gel, Its particle size was measured to be about 41 nm.

Embodiment 3

[0061] Butylphthalide 0.6g;

[0062] Medium-chain triglycerides 2g;

[0063] Polyoxyethylene hydrogenated castor oil 2g;

[0064] Propylene glycol 1g;

[0065] Azone 0.1g;

[0066] Purified water 4.3g;

[0067] Weigh butylphthalide, add it to medium-carbon chain triglyceride, mix evenly, then add polyoxyethylene hydrogenated castor oil, propylene glycol, mix evenly, add azone, then add purified water, stir to make it a microemulsion gel, Its particle size was measured to be about 41 nm.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention relates to a microemulsion transdermal gel agent of butylphthalide or a derivative thereof, and a preparation method thereof, and belongs to the technical field of medicaments. The technical scheme is that: the microemulsion transdermal gel agent is prepared mainly from the following ingredients in part by weight: 1 to 5 parts of oil phase, 1 to 5 parts of emulsifying agent, 0.1 to 1 part of auxiliary emulsifying agent, 1.5 to 15 parts of purified water and 0.003 to 0.5 part of transdermal accelerator. Compared with a comparison example, the microemulsion transdermal gel agent of the butylphthalide or the derivative thereof almost does not influence the microemulsion appearance and granular size under the conditions of centrifugation and high temperature, and is a dynamic and thermodynamic stable system. An in vitro transdermal performance test proves that the microemulsion transdermal gel agent of the butylphthalide or the derivative thereof has good transdermal absorbability. In conclusion, the microemulsion transdermal gel agent of the butylphthalide or the derivative thereof has the simple preparation method, does not need the procedures of high-speed cutting or homogenizing and the like, has small product granular size, and contributes to industrialization.

Description

technical field [0001] The present invention relates to a new drug dosage form with butylphthalide or its derivatives as the active ingredient and its preparation method, in particular to a microemulsion transdermal gel of butylphthalide or its derivatives and its preparation method. field of medical technology. Background technique [0002] Butylphthalide, full name 3-butyl-1(H)-isobenzofuranone, also known as apigenin A, is a racemate extracted from celery seed, and can also be synthesized artificially for the treatment of mild Moderate ischemic stroke. Chinese patent CN98125618.X, titled "Apigenin A in the preparation of medicines for preventing and treating diseases caused by cerebral ischemia in mammals or humans", Chinese patent CN03137457.3, titled "Prevention of L-n-butylphthalide and the use of treating dementia” and Chinese patent CN200410001748.X, titled “Application of L-butylphthalide in the Preparation of Drugs for the Prevention and Treatment of Cerebral Isc...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/22A61K31/365A61K31/44A61K31/5375A61P9/10
Inventor 牛锋李品颖郭海波刘福利焦魁良梁振江贾美娜
Owner SHIJIAZHUANG PHARMA GRP NBP PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com