CN1383816A - External Tranilast lipid gel prepn and its prepn process - Google Patents
External Tranilast lipid gel prepn and its prepn process Download PDFInfo
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- CN1383816A CN1383816A CN 01113908 CN01113908A CN1383816A CN 1383816 A CN1383816 A CN 1383816A CN 01113908 CN01113908 CN 01113908 CN 01113908 A CN01113908 A CN 01113908A CN 1383816 A CN1383816 A CN 1383816A
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- tranilast
- phospholipid
- carbopol
- lipid gel
- prepn
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Abstract
The present invention prepares externally applied preparation of water insoluble Trainlast. The lipid gel includes Tranilast in 0.05-10 wt%; phospholipid in 5-90 wt%; alcohol; and cellulose derivative, Carbopol, polyvinylpyrrolidone or chitosan in 0.1-4 w. It is prepared through mixing, heating to dissolve, stirring and homogenizing.
Description
The present invention relates to medical technical field, exactly it is that a kind of tranilast is made external lipid gel and method for making thereof.
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, is 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.
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 macromolecules such as tranilast, phospholipid, ethanol, cellulose derivative, Carbopol (carbopol) class, polyvinylpyrrolidone and chitin, it is characterized in that: the concentration of tranilast is 0.05%～10%, 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 distearoyl phosphatidylcholine.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 is adding cellulose derivative or Carbopol (carbopol) class or macromolecules such as polyvinylpyrrolidone or chitin by said ratio, 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 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
0.1g 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 lipid gel
With 1g 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, stir, and 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
0.1g 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, coat 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 macromolecules such as tranilast, phospholipid, ethanol, cellulose derivative, Carbopol (carbopol) class, polyvinylpyrrolidone and chitin, it is characterized in that: the concentration of tranilast is 0.05%～10%, 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%.
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, it is characterized in that: choose tranilast and phospholipid mixing by said ratio, add ethanol, heating for dissolving, adding cellulose derivative or Carbopol (carbopol) class or macromolecules such as polyvinylpyrrolidone or chitin by said ratio, 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 true CN1383816A (en) | 2002-12-11 |
| CN1194679C CN1194679C (en) | 2005-03-30 |
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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 |
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| CN (1) | CN1194679C (en) |
Cited By (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 |
| US7846472B2 (en) | 2004-06-24 | 2010-12-07 | Idexx Laboratories | Phospholipid gel compositions for drug delivery and methods of treating conditions using same |
Families Citing this family (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 |
-
2001
- 2001-04-28 CN CNB011139080A patent/CN1194679C/en not_active Expired - Fee Related
Cited By (5)
| 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 |
| US7622138B2 (en) | 2004-06-24 | 2009-11-24 | TDEXX Laboratories | Pharmaceutical compositions for drug delivery and methods of treating or preventing conditions using same |
| US7846472B2 (en) | 2004-06-24 | 2010-12-07 | Idexx Laboratories | Phospholipid gel compositions for drug delivery and methods of treating 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 |
| US8361496B2 (en) | 2004-06-24 | 2013-01-29 | Idexx Laboratories Inc. | Phospholipid gel compositions for drug delivery and methods of treating conditions using same |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1194679C (en) | 2005-03-30 |
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Granted publication date: 20050330 Termination date: 20100428 |