平阳霉素油包明胶微球乳剂（S／O）的研究

STUDIES ON GELATIN MICROSPHERES-IN-OIL EMULSION OF PINGYANGMYCIN

用超声分散法制得内相为平阳霉素明胶微球，外相为注射用油的乳剂Ｓ／Ｏ。其内相独立圆整，在外相中分散均匀，粒径为１．６７±０．６９μｍ。乳剂于０℃下贮存稳定，含药量为１４．０３±０．１５ｍｇ·ｍｌ－１；体外释药速率符合零级方程，累积释药５０％的时间为１２．０ｈ。动物实验表明其血药浓度平稳持久，具有极好的淋巴亲和性，并有可能降低肺毒性。

As a drug for lymphosarcoma,pingyangmycin(A5)is not widely used because of its toxicities ,short half-life and low affinity to lymph.For the purpose of delivering A5 to the lymph system to strengthen and sustain its effects and to lower its toxicities ,its gelatin microspheres-in-oil emulsion(S/O)was studied in vitro and in vivo.By ultrasonication ,gelatin microspheres with diameters of 1.67±0.69 μm were homogeneously dispersed in oil to form the S/O,which was a pseudoplastic flow and stable under 0℃ for at least 1 month.With the content of 14.03±0.15 mg· ml-1, A5released from the emulsion in a zero order rate with t0.5 of 12.0h.In vivo experiments showed that the S/O emulsion exhibited potent lymphotropicity ,prolonged plasma concentration and a probably lower pulmonary toxicity.