6 results about "Desloratadine" patented technology

The present application relates to a kind of HPLC-MS / MS detection method of detecting in human plasma, desloratadine and 3-hydroxydesloratadine in human plasma, it includes the following steps: (1) human plasma sample pretreatment;(2) liquid chromatography-mass spectrometry detection, using mobile phase A and mobile phase B as mixed mobile phase is carried out gradient elution, wherein: mobile phase A is methanol-acetonitrile mixed solution, in mixed solution methanol and acetonitrile volume ratio is 4-6:6-4;Mobile phase B is 2-20mM ammonium formate aqueous solution;(3) the determination of the concentration of human plasma in lopatadine, desloratadine and 3-hydroxydesloratadine.The present application uses lopatadine-d4, desloratadine-d5, 3-hydroxydesloratadine-d4 as deuterium internal standard, using Agilent, ZORBAX Eclipse XDB-Phenyl is carried out gradient elution, deuterium internal standard and the measured substance has the same retention time, chemical property and matrix effect, the reproducibility, accuracy of determining the concentration of lopatadine, desloratadine and 3-hydroxydesloratadine in plasma are good.The method of the present application can be used to evaluate the bioequivalence of lopatadine.

The invention discloses an application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide in preparation of drugs for treating allergic diseases, and belongs to the technical field of biological medicines. The invention discloses a new pharmaceutical application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide for the first time, and the N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide serving as an anti-allergic antagonist can effectively inhibit phospholipase C activity of stimulated cells and mediated calcium mobilization thereof in vitro. And the effective dose of the desloratadine, which is a positive drug, is lower in vivo to generate a comparable anti-allergic effect with the desloratadine. Meanwhile, in animal models of allergic rhinitis and atopic dermatitis, compared with a positive drug desloratadine, the compound can effectively inhibit the pathological progress of diseases at a lower dosage. Therefore, the compound has a definite effect of inhibiting in-vitro and in-vivo anaphylaxis, and can be effectively applied to the development of drugs for treating allergic diseases.

This invention relates to the field of pharmaceutical technology for myocardial fibrosis. Specifically, it provides the application of histamine H1 receptor antagonists in the preparation of drugs for treating myocardial fibrosis. This invention utilizes a stress overload mouse model constructed via TAC surgery to simulate the in vivo process of myocardial fibrosis, and a TGF-β1-induced fibrotic cell model. Combined with network pharmacology analysis and histamine H1 receptor gene knockout mice, the anti-myocardial fibrosis effects and mechanisms of action of the histamine H1 receptor antagonists brompheniramine maleate (BHM) and desloratadine (DLT) were investigated at both the systemic and cellular levels, providing a theoretical and experimental basis for the development of new anti-myocardial fibrosis drugs.

The present invention relates to a renal disease treatment effect obtained by the co-administration of desloratadine, which is an antihistamine, and duloxetine, which is a serotonin reuptake inhibitor. It has been identified that, when desloratadine and duloxetine are co-administered, the formation and growth of cysts were inhibited in an ADPKD animal model, the renal function was also maintained at a normal value, liver cysts and liver fibrosis caused by ADPKD were treated, renal fibrosis was significantly treated in in vitro and animal renal fibrosis models, and, in particular, the effects were synergistically increased.

The present application relates to a kind of preparation methods of desloratadine tablets, which includes pre-gelatinized starch slurry and desloratadine mixing, fluidized bed granulation, whole grain, total mixing, tabletting, coating and the like steps.The present application precisely controls the key process parameters in preparation process, so that the impurity content of product is less, and the product quality is improved.The preparation process of the method of the present application is relatively simple, easy to operate, easy to popularize and apply, and the formula of the method is relatively simple, and the cost is controllable.