CN1161119C - Lefunomide plaster and its prepn - Google Patents

Lefunomide plaster and its prepn Download PDF

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Publication number
CN1161119C
CN1161119C CNB021124760A CN02112476A CN1161119C CN 1161119 C CN1161119 C CN 1161119C CN B021124760 A CNB021124760 A CN B021124760A CN 02112476 A CN02112476 A CN 02112476A CN 1161119 C CN1161119 C CN 1161119C
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phase solution
leflunomide
solution
preparation
lefunomide
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CN1387847A (en
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胡晋红
刘成
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Second Military Medical University SMMU
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Second Military Medical University SMMU
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Abstract

The present invention relates to the technical field of medicine, particularly to a novel dosage type of an immunosuppressant (leflunomide), namely a cataplasm and a preparation method thereof. The cataplasm is made from the substrate components which are water soluble macromolecular compounds: gelatin, sodium carboxymethyl cellulose, polyvinylpyrrolidone, sorbitol, sodium polyacrylate, kaolin, methyl glycol and a crosslinking agent, namely a glutaraldehyde solution. The preparation method comprises: water soluble macromolecular compounds are divided into two groups and respectively made into a first phase solution and a second phase solution; the leflunomide (medicine) is added, and meanwhile, the second phase solution is prepared; the glutaraldehyde solution (crosslinking agent) is added after the first phase solution and the second phase solution are evenly mixed so that the macromolecular compounds are crosslinked to form a gel skeleton type substrate; the gel skeleton type substrate is laid on nonwoven fabrics; and an antisticking film is attached to the nonwoven fabrics and then dried to obtain the leflunomide cataplasm. The cataplasm has the advantages of large loaded dosage, good ventilation property and proper skin adhesiveness, prevents various adverse reactions on gastrointestinal tracts from oral administration leflunomide tablets and enhances curative effect since the drug concentration in the inflammation position is enhanced.

Description

Lefunomide plaster and preparation method thereof
Technical field: the present invention relates to medical technical field, is a kind of novel form--cataplasma and preparation method thereof of immunosuppressant leflunomide.
Background technology: leflunomide (Leflunomide) is a kind of have antiinflammatory and immunosuppressive action De isoxazole derivant, to the treatment rheumatoid arthritis with remarkable effect, tablet is only arranged at present, untoward reaction with anorexia, stomachache, diarrhoea, feel sick, gastrointestinal symptom such as vomiting, gastritis and gastroenteritis and liver function injury be for the most common, for improve leflunomide at the drug level of inflammatory local joint, strengthen antiinflammatory action, reduce the untoward reaction that the whole body administration causes, the local leflunomide percutaneous drug administration preparation that uses of research is highly significant.
Summary of the invention: the present invention is the special one-tenth cataplasma of fluorine rice in the future, and the cataplasma drug loading is big, and good permeability is good to skin adherence.Usually the leflunomide therapeutic dose is bigger, the preparation Lefunomide plaster has not only improved drug level, the enhancing antiinflammatory action of leflunomide at the inflammatory local joint, and reduced the fluctuation of leflunomide blood drug level, thereby reduced drug-induced untoward reaction.The prescription of cataplasma of the present invention and proportioning are: water-soluble high-molecular compound gelatin 0.5g, sodium carboxymethyl cellulose 1g, polyvinylpyrrolidone 1.75g, sorbitol 10g, sodium polyacrylate 0.125-0.5g, Kaolin 1-2g, propylene glycol 5-10ml and cross-linking agent 25% glutaraldehyde solution 3.5ml.Earlier water-soluble high-molecular compound is divided two groups to make I phase solution and II solution mutually respectively, the adding of medicine leflunomide with the preparation II mutually solution carry out simultaneously, to add the cross-linking agent glutaraldehyde solution behind I, the II phase solution mix homogeneously again, macromolecular compound is cross-linked with each other forms gel skeleton type substrate.Concrete preparation method is:
1. prepare I phase solution: under 50 ℃ of water-baths, gelatin fully is dissolved in the water, with adding in the gelatin solution behind sodium carboxymethyl cellulose, polyvinylpyrrolidone, the sorbitol mix homogeneously, adds the abundant swelling of water and promptly get I phase solution again.
2. prepare II phase solution: leflunomide is scattered in the propylene glycol with sodium polyacrylate, Kaolin, stirs and promptly get II phase solution.
3. preparation Lefunomide plaster: II phase solution is added in the I phase solution, obtain even thickness mastic behind the stirring and evenly mixing; Glutaraldehyde solution is added in this mastic, stir, be laid on the non-woven fabrics after full cross-linked, cover antiadhesion barrier, promptly get Lefunomide plaster after the oven dry.
The specific embodiment:
Embodiment 1: the preparation Lefunomide plaster
Prescription and proportioning thereof:
Figure C0211247600042
25% glutaraldehyde 3.5ml
Preparation method:
1. prepare I phase solution: under 50 ℃ of water-baths, gelatin fully is dissolved in the water, with adding in the gelatin solution behind sodium carboxymethyl cellulose, polyvinylpyrrolidone, the sorbitol mix homogeneously, adds the abundant swelling of water and promptly get I phase solution again;
2. prepare H phase solution: leflunomide and sodium polyacrylate, Kaolin are scattered in the propylene glycol together, stir and promptly get II phase solution;
3. preparation Lefunomide plaster: II phase solution is added in the I phase solution, obtain even thickness mastic behind the stirring and evenly mixing; Glutaraldehyde solution is added in this mastic, stir, be laid on about 400cm2 on the non-woven fabrics after full cross-linked, cover antiadhesion barrier.Put in the baking oven 60 ℃ of dryings 12 hours, and promptly got Lefunomide plaster.Be cut into 5, every contains leflunomide 100mg.

Claims (2)

1, a kind of Lefunomide plaster, comprise medicine, substrate, non-woven fabrics and antiadhesion barrier, it is characterized in that medicine is a leflunomide, substrate is by the water-soluble high-molecular compound gelatin, sodium carboxymethyl cellulose, polyvinylpyrrolidone, sorbitol, sodium polyacrylate, Kaolin, propylene glycol and cross-linking agent glutaraldehyde solution are formed, the ratio of each component is: gelatin 0.5g, sodium carboxymethyl cellulose 1g, polyvinylpyrrolidone 1.75g, sorbitol 10g, sodium polyacrylate 0.125-0.5g, Kaolin 1-2g, propylene glycol 5-10ml, 25% glutaraldehyde solution 3.5ml, leflunomide 0.4g.
2, the preparation method of the described Lefunomide plaster of claim 1, operating procedure is as follows:
(1) preparation I phase solution: gelatin fully is dissolved in the water, with adding in the gelatin solution behind sodium carboxymethyl cellulose, polyvinylpyrrolidone, the sorbitol mix homogeneously, adds the abundant swelling of water and promptly get I phase solution again;
(2) preparation II phase solution: leflunomide and sodium polyacrylate, Kaolin are scattered in the propylene glycol together, stir and promptly get II phase solution;
(3) preparation Lefunomide plaster: II phase solution is added in the I phase solution, obtain even thickness mastic behind the stirring and evenly mixing; Glutaraldehyde solution is added in this mastic, stir, be laid on the non-woven fabrics after full cross-linked, cover antiadhesion barrier, promptly get Lefunomide plaster after the oven dry.
CNB021124760A 2002-07-11 2002-07-11 Lefunomide plaster and its prepn Expired - Fee Related CN1161119C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CNB021124760A CN1161119C (en) 2002-07-11 2002-07-11 Lefunomide plaster and its prepn

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CNB021124760A CN1161119C (en) 2002-07-11 2002-07-11 Lefunomide plaster and its prepn

Publications (2)

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CN1387847A CN1387847A (en) 2003-01-01
CN1161119C true CN1161119C (en) 2004-08-11

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Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100502852C (en) * 2003-04-17 2009-06-24 中国人民解放军第二军医大学 Flurbiprofenbab preparation and its preparation method
US9278155B2 (en) 2003-06-05 2016-03-08 3M Innovative Properties Company Adhesive compositions, articles incorporating same and methods of manufacture
CN101563082A (en) * 2006-09-05 2009-10-21 窦德献 Composition and method for treating immune-mediated skin disorders

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