黎洪珊, 魏树礼, 卢炜. 平阳霉素油包明胶微球乳剂(S/O)的研究J. 药学学报, 1995, 30(5): 390-394.
引用本文: 黎洪珊, 魏树礼, 卢炜. 平阳霉素油包明胶微球乳剂(S/O)的研究J. 药学学报, 1995, 30(5): 390-394.
HS Li, SL Wei , W Lu, . STUDIES ON GELATIN MICROSPHERES-IN-OIL EMULSION OF PINGYANGMYCINJ. Acta Pharmaceutica Sinica, 1995, 30(5): 390-394.
Citation: HS Li, SL Wei , W Lu, . STUDIES ON GELATIN MICROSPHERES-IN-OIL EMULSION OF PINGYANGMYCINJ. Acta Pharmaceutica Sinica, 1995, 30(5): 390-394.

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

  • 摘要: 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。

     

    Abstract: 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.

     

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