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Granisetron cataplasm and a preparation method thereof

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, and difficulty in taking medicines, so as to avoid gastrointestinal irritation, reduce the number of administrations, and reduce blood medicines. effect of concentration

Inactive Publication Date: 2009-03-04
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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  • Granisetron cataplasm and a preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1 Preparation - granisetron cataplasm

[0012] Components and ratio:

[0013] Gelatin 2g NP-700 2g

[0014] Sodium Carboxymethyl Cellulose 4g Ca(OH) 2 0.3g

[0015] Polyvinylpyrrolidone 6g Propylene glycol 20g

[0016] D-Sorbitol 38g Kaolin 2g

[0017] Distilled water 60g Azone 8g

[0018] Glycerin 8g Granisetron Hydrochloride 0.6g

[0019] Polyethylene glycol—200 1g

[0020] The preparation method is:

[0021] 1. Prepare (I) phase solution: add water to fully swell the gelatin 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.

[0022] 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) solution.

[0023] 3. Mix (I) and (II) phase solutions, a...

Embodiment 2

[0024] Example 2 Preparation of granisetron cataplasm

[0025] Components and ratio:

[0026] Gelatin 2g NP-700 0.2g

[0027] Sodium carboxymethylcellulose 4g Al(OH) 3 0.18g

[0028] Polyvinylpyrrolidone 4g Propylene glycol 20g

[0029] D-Sorbitol 32g Zinc Oxide 4g

[0030] Distilled water 60g Camphor 6g

[0031] Glycerin 10g Citric acid (20%) 0.4ml

[0032] Isopropanol 1g Granisetron Hydrochloride 0.6g

[0033] The preparation method is:

[0034] 1, prepare (I) phase solution (same as embodiment 1).

[0035] 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.

[0036] 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, covered with anti-adhesive film, cut into 4×5cm 2...

Embodiment 3

[0037] Example 3 Preparation of granisetron cataplasm

[0038] Formula and ratio:

[0039] Gelatin 2g NP-700 0.6g

[0040] Sodium carboxymethylcellulose 3g AlCl 3 0.2g

[0041] Polyvinylpyrrolidone 6g Propylene glycol 20g

[0042] D-Sorbitol 36g Kaolin 6g

[0043] Distilled water 60g Azone 8g

[0044] Glycerin 10g Citric acid (20%) 0.4ml

[0045] Oleic acid 0.5g Granisetron free base 0.6g

[0046] The preparation method is:

[0047]1, preparation (I) phase solution: (same as embodiment 1).

[0048] 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.

[0049] 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 cataplasm of the obtained cataplasm is the finished c...

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