The comparison study was performed with 3 kinds of Lipo PGE
1 (5 μg/ml) preparations (Formulation A, B, and C), which are now used in clinical. Under alkali condition, Lipo PGE
1 (5 μg/ml) preparations in combination with physiological solution containing calcium ion were susceptible to stop dropping because of the formation of aggregates. There was a difference of feasibility to form aggregates among these preparations. The percentage of PGE
1 in the LM (lipid microspheres) was 68.8% (Formulation A) when determined by filtration with the pore size of 0.1 μm, and the respective value (%) of Formulation B and Formulation C was 43.0% and 13.9%. This indicates that the latter formulations were significantly susceptible to leak from the LM. PGE
1 can induce an extensive irritation. The potency of irritation was the most in Formulation C. This seems similar with the result of LM retention of PGE
1. PGE
1 increased the blood flow. Formulation A reached the peak by 2.27 fold, which was significantly higher than Formulation C and PGE
1 alone (PGE
1-cyclodextrin, PGE
1-CD). The peak was also significantly higher in Formulation B than that of PGE
1-CD. The AUC value of blood flow rate showed a significant increase in Formulation A and Formulation B as compared to that of PGE
1-CD. Drug retention in the LM can be a determinant factor for drug distribution and pharmacological effect. This study indicates that there can be some differences among Lipo PGE
1 preparations, which have the same drug dose.
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