Desloratadine patch and preparation method thereof

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...

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