Bikhazi A B, Baasiri G M, Boulos N Z, Khuri R N
J Pharm Sci. 1983 Mar;72(3):296-9. doi: 10.1002/jps.2600720322.
Transport of alprostadil (prostaglandin E1) and dinoprost (prostaglandin F2 alpha) was studied in enzymatically dispersed normal and streptozocin-treated rat hepatocytes prepared by collagenase perfusion. Cell suspensions incubated at 37 degrees were sampled at time intervals for a period of 5 min and the supernatant analyzed for prostaglandins after centrifugation. The data analysis employed a theory and a model for solute transfer at the cell membrane-water interphase. Biophysical parameters such as the effective partition and the apparent permeability constants were used to define the transport mechanism. The apparent permeability coefficient of alprostadil and dinoprost transfer through normal hepatocytes was calculated to be 5 X 10(-3) and 3 X 10(-3) cm/sec with a mean partition coefficient of 1345 and 764 for both solutes, respectively. The permeability coefficient of alprostadil and dinoprost transfer through diabetic hepatocytes were 3 X 10(-3) and 2 X 10(-3) cm/sec with partition coefficient of 572 and 206, respectively. The results showed differences in prostaglandin transport between normal and diabetic hepatocytes, resulting from morphological and lipid alteration in the cytoplasmic membrane.
通过胶原酶灌注制备的正常大鼠和链脲佐菌素处理的大鼠肝细胞，对前列地尔（前列腺素E1）和地诺前列素（前列腺素F2α）的转运进行了研究。在37℃孵育的细胞悬液每隔一定时间取样5分钟，离心后分析上清液中的前列腺素。数据分析采用细胞膜 - 水界面溶质转运的理论和模型。有效分配系数和表观渗透常数等生物物理参数用于确定转运机制。计算得出前列地尔和地诺前列素通过正常肝细胞的表观渗透系数分别为5×10⁻³和3×10⁻³厘米/秒，两种溶质的平均分配系数分别为1345和764。前列地尔和地诺前列素通过糖尿病肝细胞的渗透系数分别为3×10⁻³和2×10⁻³厘米/秒，分配系数分别为572和206。结果表明，正常和糖尿病肝细胞之间前列腺素转运存在差异，这是由细胞质膜的形态和脂质改变引起的。
