Li H S, Wei S L, Lu W
School of Pharmacy, Beijing Medical University.
Yao Xue Xue Bao. 1995;30(5):390-4.
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 microns were homogeneously dispersed in oil to form the S/O, which was a pseudoplastic flow and stable under 0 degrees C for at least 1 month. With the content of 14.03 +/- 0.15 mg.ml-1, A5 released from the emulsion in a zero order rate with t0.5 of 12.0 h. In vivo experiments showed that the S/O emulsion exhibited potent lymphotropicity, prolonged plasma concentration and a probably lower pulmonary toxicity.
作为一种治疗淋巴肉瘤的药物，平阳霉素（A5）由于其毒性、半衰期短以及对淋巴的亲和力低而未被广泛使用。为了将A5输送到淋巴系统以增强和维持其疗效并降低其毒性，对其油包明胶微球乳剂（S/O）进行了体内外研究。通过超声处理，直径为1.67±0.69微米的明胶微球均匀分散在油中形成S/O，其为假塑性流体，在0℃下至少稳定1个月。A5从乳剂中以零级速率释放，含量为14.03±0.15mg·ml-1，t0.5为12.0小时。体内实验表明，S/O乳剂具有很强的亲淋巴性，可延长血浆浓度，且肺部毒性可能较低。
