Desloratadine external preparation and preparation method thereof

Abstract

The invention relates to a desloratadine external preparation and a preparation method thereof. The external preparation takes desloratadine as a main drug and is used for treating allergic skin inflammation. The desloratadine external preparation can increase the concentration of free drug in skin local tissues of the part with the allergic skin inflammation of a body through percutaneous absorption, have an effective histamine sensitization antagonism role, better play local antianaphylaxis and anti-inflammation efficacies and reduce adverse reactions. The external formulation does not pass through the gastrointestinal tract, thereby avoiding the first pass effect and reduce the probability of occurrence of adverse reactions. The external preparation can be directly applied at the affected side, and the onset of action is rapid. Furthermore, the dose and the coverage area of the external preparation can be selected according to the area and the severity of the affected site, and the external preparation is convenient to use and convenient to carry.

Description

Technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a desloratadine external preparation and a preparation method thereof. Background technique [0002] Desloratadine is a non-sedative long-acting tricyclic antihistamine and the active metabolite of loratadine. It can selectively block peripheral H1 receptors and inhibit various allergic inflammations. The release of chemical mediators, such as inhibiting the release of histamine, prostaglandins, and leukocyte mediators from mast cells and basophils, to relieve symptoms related to allergic rhinitis or chronic idiopathic urticaria. [0003] At present, the dosage forms of desloratadine on the market are mainly oral dosage forms such as tablets, dispersible tablets, and syrups. When these oral dosage forms are taken orally, the gastrointestinal tract will have a first-pass effect on the drug, and the metabolic effects of food and gastric emptying on the drug. Moreover, the oral...

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