NEWS

When the solubility of drugs in water is less than x%, the development and bioavailability of drug preparations will be limited and affected. In the Pharmacopoeia and the list of essential drugs, more than one third of them are insoluble or insoluble in water. It is of great significance to increase the solubility in water to improve the efficacy. It has been widely studied for many years to increase the water solubility of betacyclodextrin (β - CD) or its derivatives with drugs. However, the low solubility of β - CD limits its application. In particular, intravenous injection of β - CD can cause the increase of blood urea nitrogen. When absorbed through renal tubules, it will crystallize due to its low water solubility, resulting in tissue necrosis. Therefore, the derivatives of β - CD represented by hydroxypropyl betacyclodextrin (HP - β - CD) can be used to prepare various dosage forms such as intravenous injection, oral administration and so on, because of their high safety dose, good blood solubility, unchanged efficacy, increased water solubility and stability.

The method for preparing the complexes of organic drugs and betacyclodextrin derivatives is as follows: the derivatives of betacyclodextrin (β - CD) represented by hydroxypropyl betacyclodextrin (HP - β - CD) are as follows The main body takes organic drug molecules or other organic molecules as the guest, takes the presence of water as the necessary condition, through recognition and assembly, to generate stable weak bond (non bond) binding water-soluble coordination compounds (or complexes, supramolecular compounds).

In a clean environment:

a. Adding solvent into organic medicine or other organic matter to dissolve it;

b. A solution of β - CD derivative with critical value (molecular ratio or mass ratio of forming stable coordination compound) is added to the solution obtained in step a to convert the solvent into aqueous solution. According to the principle of supramolecular chemical intermolecular interaction, stable water-soluble coordination compound is generated through recognition and assembly.