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Solubilizing effect of 2- Hydroxypropyl-beta-cyclodextrin on loratadine

Loratadine, a second-g-eneration H2 receptor antagonist, is a potent and long-acting tricyclic antihistamine, which is mainly used in the treatment of allergic rhinitis, seasonal rhinitis, skin allergy, urticaria and allergic asthma. Loratadine preparations listed in China are slow in absorption and low in bioavailability because loratadine is fat-soluble and insoluble in water.

In recent years, cyclodextrins have become the most widely used insoluble drug inclusion materials, especially when hydrophilic 2-hydroxypropyl- beta-cyclodextrin form inclusion compounds with insoluble drugs, it can improve the solubility, dissolution rate and bioavailability of drugs. The results show that the solubility of loratadine is the highest when the PH of 2-hydroxypropyl- beta-cyclodextrin is 3.5.  However, when the PH is 5.5 and 6.5, the drug is mainly incorporated into 2-hydroxypropyl- beta-cyclodextrin in molecular form, and the drug is relatively stable at this time. Therefore, although the oil-water distribution coefficient of the drug is greater than that of the PH 4.5, the concentration of the drug is still greater than that of the PH 4.5.

Shandong Binzhou Zhiyuan Biological Technology Co., Ltd is a professional production of cyclodextrin enterprises, if you have any questions, want to solve some problems related to cyclodextrin, welcome to call for details.

Leading Manufacture And Solution Provider Of Cyclodextrin Derivatives