CN1194679C - External Tranilast lipid gel prepn and its prepn process - Google Patents
External Tranilast lipid gel prepn and its prepn process Download PDFInfo
- Publication number
- CN1194679C CN1194679C CNB011139080A CN01113908A CN1194679C CN 1194679 C CN1194679 C CN 1194679C CN B011139080 A CNB011139080 A CN B011139080A CN 01113908 A CN01113908 A CN 01113908A CN 1194679 C CN1194679 C CN 1194679C
- Authority
- CN
- China
- Prior art keywords
- tranilast
- phospholipid
- lipid gel
- concentration
- external
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
Abstract
The present invention relates to an external Tranilast lipid gel preparation, which can cause water-insoluble Tranilast to be prepared into an external preparation. The external Tranilast lipid gel preparation comprises macromolecules of Tranilast, phosphatide, etanol, cellulose derivatives, carbopol classes, polyvinylpyrrolidone, chitin, etc., wherein the concentration of the Tranilast is from 0.05% to 10%, the concentration of the phosphatide is from 5% to 90%, and the concentration of macromolecules of the carbopol class or the polyvinylpyrrolidone or the chitin, etc. is from 0.1% to 4%. According to the proportion, the Tranilast and the phosphatide are mixed, and the etanol and the cellulose derivatives are added; the mixture is dissolved by heating, stirred and homogenized.
Description
Technical field
The present invention relates to medical technical field, exactly it is a kind of tranilast external lipid gel and method for making thereof.
Background technology
Tranilast (tranilast) is an allergy preparations, can suppress mast cell degranulation, and the retardance histamine waited the release of sensitive media.This product still can suppress partial anaphylaxis.The clinical bronchial asthma that is used for also can be used for preventing and treating allergic dermatitis and other anaphylactic diseases.Insoluble in the tranilast water, difficulty is made external preparation, has document to make 10% ointment abroad, be used for the treatment of diseases such as keloid, and liposome has following advantage as transdermal drug delivery system: the Intradermal concentration that 1, can greatly improve medicine; 2, the long period is kept the Intradermal drug level; 3, reduce the blood volume of going into of medicine, thereby reduce systemic side effects.The phospholipid concentration of conventional preparation liposome liquid is 2%, is higher than this concentration, and then some character of system are unfavorable for administration.And for hydrophobic drug, often need to reduce the crystallize of medicine by improving phospholipid concentration.
Summary of the invention
The purpose of this invention is to provide a kind of tranilast external lipid gel, it can be made under the higher phosphorous lipid concentration, and technology is fairly simple, makes external preparation for tranilast an approach is provided.
The objective of the invention is to be achieved by the following scheme, it comprises tranilast, phospholipid, ethanol, cellulose derivative, Carbopol (carbopol) class, macromolecule such as polyvinylpyrrolidone and chitin, it is characterized in that: the concentration of tranilast is 0.05%～10%, and the concentration of phospholipid is 5%～90%, and the concentration of cellulose derivative or Carbopol (carbopol) class or macromolecules such as polyvinylpyrrolidone or chitin is 0.1%～4%.Phospholipid is natural phospholipid or synthetic phospholipid.Natural phospholipid is soybean phospholipid and egg yolk lecithin, and synthetic phospholipid is semisynthetic hydrogenated soy phosphatidyl choline and complete synthesis phospholipid distearyl phosphatidyl choline.Cellulose derivative is hydroxypropyl cellulose or sodium carboxymethyl cellulose or hydroxypropyl cellulose.Choose tranilast and phospholipid mixing by said ratio, add ethanol, heating for dissolving by above-mentioned adding cellulose derivative or Carbopol (carbopol) class or macromolecules such as polyvinylpyrrolidone or chitin, stirs homogenize.Advantage of the present invention is: can make the tranilast lipid gel under the higher phosphorous lipid concentration, technology is fairly simple, is fit to industrial application, and awkward water-soluble tranilast is made the approach that external preparation has been opened up an application.
The specific embodiment
The present invention is described in further detail below in conjunction with embodiment.
Following embodiment just for setting forth the present invention, does not limit application of the present invention.
Embodiment 1:0.1% tranilast lipid gel
0.1% tranilast and the oral soybean lecithin of 10g are mixed, add an amount of ethanol, heating for dissolving in the gained solution, adds 1% Gonak 90g, stirs, and homogenize promptly gets the lipid gel.The gel that takes a morsel, behind the dilute with water, the visible a large amount of liposomees of microscopically.
Embodiment 2:1% tranilast and 20g Ovum Gallus domesticus Flavus lecithin, the 1g cholesterol adds an amount of ethanol, and heating for dissolving in the gained solution, adds 1.5% carboxymethylcellulose sodium solution 78g, stirs, homogenize, promptly.
Embodiment 3:0.5% tranilast lipid gel
0.5g tranilast and 15g hydrogenated soy phosphatidyl choline are mixed, add an amount of ethanol, heating for dissolving in the gained solution, adds 1.2% polyvinylpyrrolidonesolution solution 84.5g, stir, and homogenize, promptly.The gel that takes a morsel, behind the dilute with water, the visible a large amount of liposomees of microscopically.
Embodiment 4: the crystallize velocity ratio
0.1 tranilast and 5g phospholipid are mixed, add an amount of dissolve with ethanol, add 95ml water, stir, become emulsus liposome liquid, this liquid was placed 7 days, promptly had more medicine crystal to separate out.And the product of " embodiment 1 " was placed after 9 months, and medicine crystal is not arranged yet.
Embodiment 5: the Intradermal distribution test
The rat hair is removed, be coated with down the product and tranilast 10% ointment of " embodiment 1 " respectively, once a day, shared medicine three days was wiped left drug on the skin surface with normal saline on the 4th day, put to death rat, take medicine position skin, extract, measure drug level in the skin with organic solvent, lipid gel group can reach 10 μ g/g, and the ointment group only has 1 μ g/g.
Claims (5)
1, tranilast external lipid gel, it comprises tranilast, phospholipid, ethanol, cellulose derivative, carbopol class, polyvinylpyrrolidone and chitin macromolecule, it is characterized in that: the concentration of tranilast is 0.05%～10%, the concentration of phospholipid is 5%～90%, cellulose derivative or carbopol class or polyvinylpyrrolidone or the high molecular concentration of chitin are 0.1%～4%, and surplus is an ethanol.
2, tranilast external lipid gel according to claim 1 is characterized in that: phospholipid is natural phospholipid or synthetic phospholipid.
3, tranilast external lipid gel according to claim 2, it is characterized in that: natural phospholipid is soybean phospholipid and egg yolk lecithin, synthetic phospholipid is semisynthetic hydrogenated soy phosphatidyl choline and complete synthesis phospholipid distearoyl phosphatidylcholine.
4, tranilast external lipid gel according to claim 1 is characterized in that: cellulose derivative is hydroxypropyl cellulose or sodium carboxymethyl cellulose or hydroxypropyl cellulose.
5, a kind of method for making as right 1 described tranilast external lipid gel is characterized in that: choose tranilast and phospholipid and mix, add ethanol, heating for dissolving, add cellulose derivative or carbopol class or polyvinylpyrrolidone or chitin macromolecule again, stir homogenize.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB011139080A CN1194679C (en) | 2001-04-28 | 2001-04-28 | External Tranilast lipid gel prepn and its prepn process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB011139080A CN1194679C (en) | 2001-04-28 | 2001-04-28 | External Tranilast lipid gel prepn and its prepn process |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1383816A CN1383816A (en) | 2002-12-11 |
| CN1194679C true CN1194679C (en) | 2005-03-30 |
Family
ID=4660605
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB011139080A Expired - Fee Related CN1194679C (en) | 2001-04-28 | 2001-04-28 | External Tranilast lipid gel prepn and its prepn process |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1194679C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101152164B (en) * | 2007-09-14 | 2011-04-06 | 李世荣 | Anti-cicatrix externally used pad pasting containing anti-hypertrophy cell medicament and method for preparing the same |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7618651B2 (en) | 2004-06-24 | 2009-11-17 | Idexx Laboratories | Pharmaceutical compositions for drug delivery and methods of treating or preventing conditions using same |
| US7858115B2 (en) | 2004-06-24 | 2010-12-28 | Idexx Laboratories | Phospholipid gel compositions for drug delivery and methods of treating conditions using same |
-
2001
- 2001-04-28 CN CNB011139080A patent/CN1194679C/en not_active Expired - Fee Related
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101152164B (en) * | 2007-09-14 | 2011-04-06 | 李世荣 | Anti-cicatrix externally used pad pasting containing anti-hypertrophy cell medicament and method for preparing the same |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1383816A (en) | 2002-12-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Kamel et al. | Development of a novel vesicular system using a binary mixture of sorbitan monostearate and polyethylene glycol fatty acid esters for rectal delivery of rutin | |
| DE69922243T2 (en) | SOLID LIPID NANOSPHERES SUITABLE FOR A FAST INTRODUCTION IN CELLS | |
| US4897308A (en) | Compositions comprising aqueous dispersions of lipid spheres | |
| KR100949848B1 (en) | Nanoemulsion composition comprising Vitamin-C derivative and method for preparing thereof | |
| US20080292688A1 (en) | Liposome and preparation method of the same | |
| CN102429913A (en) | Compound clobetasol propionate liposome and preparation thereof | |
| CH702736B1 (en) | Phospholipid emulsion which includes Dihydroquerzetin. | |
| CN101773553B (en) | Semiaquilegia root extract, preparation method and application thereof | |
| CN113041210B (en) | Colchicine external composition | |
| CN1194679C (en) | External Tranilast lipid gel prepn and its prepn process | |
| CN102397255B (en) | Progesterone ethosome, and preparation method and application thereof | |
| CN102526032B (en) | Formula of liposome preparation containing compound amino acid and preparation method thereof | |
| WO1997021428A1 (en) | Cortisone spray for topical administration | |
| CN100502850C (en) | Medicinal composition of total capsicine compounds and beta-cyclodextrin or derivative of beta-cyclodextrin | |
| CN108743534A (en) | A kind of Celastrol or tripterine derivate vesica and preparation method thereof | |
| CN110448525A (en) | A kind of external application Finasteride lipid nanometer preparation and preparation method thereof prevented hair loss with growth-promoting hair | |
| CN111265482B (en) | Glycyrrhetinic acid and/or folic acid ligand modified cantharidin solid lipid nanoparticle and preparation method thereof | |
| CN114177278A (en) | Liposome preparation | |
| CN104288110B (en) | 5alpha-androstane-3beta,5,6beta-triol injection and preparing method thereof | |
| EP2255790B1 (en) | Liposome composition comprising naproxen, and a method of obtaining same | |
| CN113456592A (en) | Antiseptic and anti-inflammatory liposome and preparation method thereof | |
| CN1686156A (en) | Clamycin structurization emulsion composition | |
| CN101548946B (en) | Curcumin nano-lipid injection liquid, preparation method and application thereof | |
| CN102641276B (en) | Compound clobetasol propionate mixed micellar solution and preparation method thereof | |
| CN103040723B (en) | Xiyanping lipidosome injection |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20050330 Termination date: 20100428 |