平阳霉素明胶微球复乳S／o／w的研究

Gelatin microspheres-in-oil-in-water(s/o/w)multiple emulsion ofpingyangmycin

将超声分散法制得的油包平阳霉素明胶微球乳剂ｓ／ｏ分散于３％豆磷脂水溶液中，形成复合乳剂ｓ／ｏ／ｗ。复乳中ｓ／ｏ微珠的粒径为１７．０７±８．６８μｍ。其含药量为１４．８６～１５．００ｍｇ／ｍｌ，体外释药符合Ｈｉｇｕｃｈｉ方程。动物实验表明：其血药浓度平稳持久，具有良好的淋巴亲和性，并可能降低肺毒性。且流动性和通针性均较好。

As a drug for lymphosarcoma,pingyangmycin(A_5) is not widely used because of itstoxicities,small T_(1/2),and low affinity to lymph.To deliver A_5 to lymph system to strenghen andsustain its effects,and to lower its toxicities,we studied in vitro and in vivo its gelatin micro-spheres-in-oil-in-water multiple emulsion(s/o/w).A_5 gelatin microspheres-in-oil(s/o) emulsion,prepared by ultrasonication,was dispersed in 3%lecithin(from soybean)solution to form the s/o/w.The multiple emulsion was a Newton flow and stable under 23℃ for 24 h.With the contentof 14.86～15.00 mg/ml,A_5 released from the emulsion in a Higuchi Equation with t_(0.5) of 5.0 h invitro.In vivo experiments in rabbits showed that the drug in the multiple emulsion,by subcuta-neous injection,had a potent lymphotropicity,a valuable prolonged plasma C-T curve and aprobably lower toxicity to lung.