Characteristics and application of CHO-HP cholesterol

CHO-HP is a high purity injectable pharmaceutical excipient produced under cGMP conditions, with DMF number 024780 and pharmaceutical excipient registration number F20170000106. As the only cholesterol injection grade excipients in China, it has a wide range of applications. Compared with the usual animal tissue extraction method to produce cholesterol in China, CHO-HP adopts semi-synthetic method to produce wool oil as raw material, with a purity of more than 99%, and there is no virus contamination of animal tissue. Therefore, in the international market, CHO-HP is widely used in a variety of liposome products.

CHO-HP is a white powdered solid with good stability at room temperature, but it is sensitive to light, so it needs to be kept away from light and properly sealed. If stored correctly, it is valid for up to 5 years. The substance is readily soluble in triLV methane (1g/4.5ml), dissolved in Et₂O (1g/2.8ml), slightly dissolved in AC, ethyl acetate, or ether, but only weakly dissolved in ethanol, and almost insoluble in water (0.2mg/100ml).

CHO HP is a special purpose excipient for injection liposomes, which can enhance the stability of liposome membrane, reduce drug leakage and enhance the ability of liposome vesicles to resist changes in external conditions.

Preparation of AmBisome in amphotericin B liposomes

(1) Dissolve amphotericin B, HSPC, CHO HP, DSPG and tocopherol with appropriate solvents, remove the organic solvent by reducing pressure, and put it aside.

(2) Dissolve sucrose and C4H4Na2O4·6H2O with water for injection, and adjust the pH of the solution to 5~6, and then set aside.

(3) The solution obtained in the second step is added to the solution in the first step for hydration and dispersion. The liposomes are prepared by means of homogenizers, microfluidizers or extruders with a controlled particle size of less than 100nm.

(4) The prepared liposomes were aseptically filtered, packaged, and freeze-dried to obtain AmBisome.

Preparation of daunorubicin liposome Daunoxome

(1) Dissolve DSPC and CHO HP in appropriate solvent, and remove the organic solvent by reducing pressure, and set it aside.

(2) Dissolve glycerin, sucrose and citric acid in water for injection, and set the solution aside.

(3) The solution obtained in the second step is added to the dissolved solution in the first step for hydration and dispersion. Liposomes are prepared by homogenizer, microfluidizer or extruder and the particle size is controlled.

(4) The PH gradient method was used to load daunorubicin into the liposomes, while regulating the pH of the external phase to 4.9~6.

(5) Daunorubicin liposomes can be obtained by adding calcium chloride solution. The particle size is 45nm and the encapsulation rate is greater than 90%.