[Comparison study of lipo PGE1 preparations].
The comparison study was performed with 3 kinds of Lipo PGE(1) (5 microg/ml) preparations (Formulation A, B, and C), which are now used in clinical. Under alkali condition, Lipo PGE(1) (5 microg/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 microm, 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.
Institute of Medical Science, St. Marianna University School of Medicine, Kawasaki, Japan. m2take@marianna-u.ac.jp
Mitsuko
M
Takenaga
Yuki
Y
Ohta
Yukie
Y
Tokura
Akemi
A
Hamaguchi
Rie
R
Igarashi
D000527:Alprostadil / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology; D000818:Animals; D001783:Blood Flow Velocity / Q000187:drug effects; D004339:Drug Compounding; D016503:Drug Delivery Systems; D007509:Irritants; D008297:Male; D008863:Microspheres; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000187:drug effects
D007509:Irritants; D000527:Alprostadil