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Granisetron cataplasm and its prepn

A technology of granisetron hydrochloride and granise, which is applied in the field of medicine, can solve the problems of inability to effectively maintain blood drug levels, inconvenient use of injections, difficulty in taking medicine, etc., so as to avoid gastrointestinal irritation, reduce the number of drug administrations, and reduce blood drug levels. effect of concentration

Inactive Publication Date: 2006-05-17
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the dosage forms of the drug include tablets, capsules, and injections, but the existing dosage forms are insufficient, and the injections are inconvenient to use, and professional help is required; oral administration has strong first-pass metabolism, and patients often suffer from gastric Difficulty taking medication due to intestinal reactions; inability to effectively maintain stable blood drug levels

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Embodiment 1 preparation-granisetron cataplasm

[0012] gelatin

Sodium carboxymethyl cellulose

Polyvinylpyrrolidone

D-sorbitol

2g

4g

6g

38g

NP-700

Ca(OH) 2

Propylene Glycol

Kaolin

2g

0.3g

20g

2g

distilled water

Glycerin

polyethylene glycol-200

60g

8g

1g

Azone

Granisetron Hydrochloride

8g

0.6g

[0013] The preparation method is:

[0014] 1. Preparation of phase (I) solution: fully swell the gelatin with water according to the above ratio, dissolve it in a water bath at 60°C, mix D-sorbitol and granisetron hydrochloride evenly, add it to the gelatin, and stir thoroughly to obtain phase (I) solution.

[0015] 2. Prepare (II) phase solution: Dissolve azone in propylene glycol, mix well with sodium carboxymethylcellulose, polyvinylpyrrolidone, partially neutralized polyacrylic acid (NP-700), and kaolin to obtain phase (II...

Embodiment 2

[0017] Embodiment 2 prepares granisetron cataplasm

[0018] gelatin

Sodium carboxymethyl cellulose

Polyvinylpyrrolidone

D-sorbitol

distilled water

Glycerin

Isopropanol

2g

4g

4g

32g

60g

10g

1g

NP-700

Al(OH) 3

Propylene Glycol

Zinc oxide

Camphor

Citric acid (20%)

Granisetron Hydrochloride

0.2g

0.18g

20g

4g

6g

0.4ml

0.6g

[0019] The preparation method is:

[0020] 1, prepare (I) phase solution (same as embodiment 1).

[0021] 2. Prepare (II) phase solution: dissolve camphor in propylene glycol, mix well with sodium carboxymethylcellulose, polyvinylpyrrolidone, partially neutralized polyacrylic acid (NP-700), zinc oxide, and citric acid to obtain (II) ) phase solution.

[0022] 3. Mix (I) and (II) phase solutions, add glycerin, isopropanol, Al(OH) 3 , fully stirred, spread on non-woven fabric, baked at 50°C for 60 minutes, cov...

Embodiment 3

[0023] Embodiment 3 prepares granisetron cataplasm

[0024] gelatin

Sodium carboxymethyl cellulose

Polyvinylpyrrolidone

D-sorbitol

distilled water

Glycerin

Oleic acid

2g

3g

6g

36g

60g

10g

0.5g

NP-700

AlCl 3

Propylene Glycol

Kaolin

Azone

Citric acid (20%)

Granisetron free base

0.6g

0.2g

20g

6g

8g

0.4ml

0.6g

[0025] The preparation method is:

[0026] 1, preparation (I) phase solution: (same as embodiment 1).

[0027] 2. Preparation of the (II) phase solution: uniformly mix azone, propylene glycol, sodium carboxymethylcellulose, polyvinylpyrrolidone, NP-700, kaolin, and citric acid to obtain the (II) phase solution.

[0028] 3. Mix (I) and (II) phase solutions, add glycerin, oleic acid, AlCl 3 , fully stirred, spread on non-woven fabric, baked at 50°C for 30 minutes, covered with anti-adhesive film, cut into 4×5cm 2 The catap...

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PUM

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Abstract

The present invention relates to medicine technology, and is Granisetron cataplasm as 5-HT3 receptor agonist in new form. Granisetron is applied clinically in preventing and treating nausea, vomiting, etc caused by cytotoxicity treatment, and available Granisetron preparation forms have some demerits. The present invention prepares Granisetron into cataplasm with the hydrochloride or free alkali of Granisetron as main medicine component and some supplementary materials. The Granisetron cataplasm with transdermal administration has no first pass effect, reduced and constant systemic blood medicine concentration, less side effect, raised compliance and other advantages.

Description

Technical field: [0001] The present invention relates to the technical field of medicine, is 5-HT 3 A new dosage form of the receptor antagonist Granisetron (Granisetron) - cataplasm. Background technique: [0002] Granisetron is a potent, highly selective peripheral and central nervous system 5-HT 3 Receptor antagonists are used to prevent and treat symptoms such as nausea and vomiting caused by cytotoxic therapy (anti-tumor chemotherapy and radiotherapy). Compared with other traditional antiemetic drugs, they have the advantages of high efficiency, low toxicity, safety and reliability, etc. It has been widely used clinically. At present, the dosage forms of the drug include tablets, capsules, and injections, but the existing dosage forms are insufficient, and the injections are inconvenient to use, and professional help is required; oral administration has strong first-pass metabolism, and patients often suffer from gastric Intestinal reactions make it difficult to take...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/439A61P1/08
Inventor 胡晋红柳正青朱全刚
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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