Desloratadine patch and preparation method thereof

A technology of desloratadine and patch, which is applied in the field of desloratadine patch and its preparation, can solve the problems such as the severity of symptoms and the difficulty in grasping the dosage, slow onset of effect, and increased harm to human body, so as to avoid First-pass effect, avoiding slow onset, improving solubility

Inactive Publication Date: 2011-01-05
HANGZHOU SHARPLY PHARM R&D INSTIT +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Problems existing in common dosage forms at present: (1) Existing dichloride dosage forms are all taken orally, and the general problems existing in oral preparations are that the onset of action is slow, and the first-pass effect of the gastrointestinal tract is obvious, and the bioavailability of drugs is not high
[0006] (2) Both oral tablets and capsules need to be taken with water, which is inconvenient to take and tastes bitter
However, the syrup is generally bulky, heavy, and inconvenient to carry
[0007] (3) The specifications and doses of tablets and capsules are fixed, and it is difficult to grasp the severity of symptoms and dosage, especially for skin allergy symptoms, taking too much will increase the harm to human body
However, it is difficult for desloratadine to pass through the stratum corneum of the skin and can only stay on the skin surface. According to the prior art, it is difficult for desloratadine to penetrate the stratum corneum of the skin for external use and cannot reach an effective tissue concentration in the skin tissue. Therefore, its anti-allergic and anti-inflammatory effects cannot be exerted

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Prescription: desloratadine 5mg beta-cyclodextrin 5mg

[0036] Acrylic resin 2mg Aluminum hydroxide 0.05mg

[0037] Crospovidone 0.05mg PVPK90 1mg

[0038] EDTA 0.01mg Tartaric acid 0.02mg

[0039] N-methyl-pyrrolidone 2mg Glycerin 0.5mg

[0040] Distilled water 20ml

[0041] The preparation process is as follows:

[0042] (1) The raw material of desloratadine is pulverized with an ultrafine pulverizer until the particle size is less than 10 microns, dissolved in 3 times the amount of β-cyclodextrin and heated to 60°C in purified water, and the pulverized desloratadine Slowly add the raw materials into the β-cyclodextrin aqueous solution, stir and grind while adding, keep grinding for 4 hours until it becomes a paste, refrigerate, filter, wash with tartaric acid, and dry to obtain the inclusion complex of desloratadine β-cyclodextrin thing;

[0043] (2) Add aluminum hydroxide and EDTA to an appropriate amount of glycerin, and after fully mixing, add an appropriate...

Embodiment 2

[0049] Prescription: desloratadine 3mg β-cyclodextrin 4mg

[0050] Sodium Carboxymethyl Cellulose 3mg Aluminum Glycol 0.05mg

[0051] Crospovidone 0.05mg PVPK90 1mg

[0052] Azone 3mg Distilled water 20ml

[0053] The preparation process is as follows:

[0054](1) The raw material of desloratadine is pulverized with an ultrafine pulverizer until the particle size is less than 10 microns, dissolved in 3 times the amount of β-cyclodextrin and heated to 60°C in purified water, and the pulverized desloratadine Slowly add the raw materials into the β-cyclodextrin aqueous solution, stir and grind while adding, keep grinding for 3 hours until it becomes a paste, refrigerate, filter, and dry to obtain the inclusion complex of desloratadine β-cyclodextrin;

[0055] (2) Aluminum glyoxate and sodium carboxymethylcellulose are added to fully mix to obtain a matrix;

[0056] (3) dissolving desloratadine β-cyclodextrin inclusion compound in an appropriate amount of water, dissolving cro...

Embodiment 3

[0060] Prescription: desloratadine 7mg β-cyclodextrin 6mg

[0061] NP700 4mg Aluminum Glycinate 0.05mg

[0062] Crospovidone 0.05mg PVPK90 1mg

[0063] EDTA 0.01mg Tartaric acid 0.02mg

[0064] Laurocaprazine 3mg Distilled water 20ml

[0065] Preparation method: (1) The desloratadine raw material is pulverized to a particle size of less than 10 microns with an ultrafine pulverizer, dissolved in 3 times the amount of β-cyclodextrin and heated to 60°C in purified water, and the pulverized desloratadine Ratadine raw materials are slowly added to the β-cyclopaste viscous aqueous solution, stirred and ground while adding, and kept grinding for 4 hours until it becomes a paste, refrigerated, filtered, washed with tartaric acid, and dried to obtain desloratadine β-cyclopaste clathrate;

[0066] (2) Add aluminum glycinate and EDTA to an appropriate amount of glycerin, mix thoroughly, add to NP700, and continue to mix thoroughly to obtain a matrix;

[0067] (3) dissolving deslorat...

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Abstract

The invention relates to a desloratadine patch and a preparation method thereof. The desloratadine patch comprises a patch film and medicament components on the patch film, wherein the medicament components comprise main component desloratadine and auxiliary materials; and the auxiliary materials comprise a solubilizing agent, a substrate, a cross-linking agent, an excipient and an osmosis reinforcing agent. The invention overcomes the bias that in the prior art, the desloratadine is considered to be difficult to externally penetrate through the skin cuticle and not to reach effective tissue concentration in the skin tissue so as not to exert the curative effects of allergic resistance and inflammation resistance, solves the problem of poor solubility of the desloratadine, improves the permeability of the desloratadine on the skin cuticle, ensures that the desloratadine rapidly arrives at the affected part and takes the effect rapidly and solves the problems of inconspicuous effect-taking and obvious first pass effect on gastrointestinal tract of the traditional patch. The desloratadine patch has the advantages of good curative effect, rapid action, less toxic or side effect and convenient use.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a desloratadine patch and a preparation method thereof. Background technique [0002] Desloratadine is a non-sedating long-acting tricyclic antihistamine, which is an active metabolite of loratadine, and can inhibit various allergic inflammatory processes by selectively blocking peripheral H1 receptors. Release of chemical mediators, such as: inhibit mast cells and basophils from releasing histamine, prostaglandins, leukocyte mediators, etc., relieve symptoms related to allergic rhinitis or chronic idiopathic urticaria. [0003] Currently, the dosage forms of desloratadine on the market are mainly oral dosage forms such as tablets, dispersible tablets, and syrups. These oral dosage forms experience first-pass drug effects in the gastrointestinal tract during oral administration, as well as metabolic effects of food and gastric emptying on the drug. And oral dosage for...

Claims

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Application Information

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IPC IPC(8): A61K9/70A61K31/4545A61K47/40A61P37/08
Inventor 范敏华刘华周学来
Owner HANGZHOU SHARPLY PHARM R&D INSTIT
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