Drug delivery function of DDSs in clinical use: Changes in phase-distribution of PGE1 in lipid emulsions after dilution with aqueous infusions

Yuji Kurosaki, Bibari Hino, Keita Yamauchi, Kayo Kamiya, Hiromu Kawasaki

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

To guarantee the drug delivery function of the DDS drugs in clinical use, supplementary information closely related to the diverse clinical usage is required in addition to information listed on the Products Information. Changes in the phase-distribution of PGE1 in lipo-PGE1(Palux inj. and Liple ®), a targeting-type DDS, after 10-times dilution with 6 aqueous infusions frequently prescribed for clinical treatment, i. e., 5% Otsuka Toueki (Glucose Injection JP), Otsuka Seisholcuchu (Isotonic Sodium Chioride Solution JP), Klinit ® (Xylitol Injection JP), Physiosol ®·3, Hartmann's Solution pH : 8 and Intralipos ® 10%, were examined in vitro. Total amounts of PGE1 and the amounts of PGE1 in the aqueous phase were determined by the ultrafiltration method to estimate phase-distribution ratios of PGE1 after 10-times dilution. Total amounts of PGE1 did not decrease after the dilution with each aqueous infusion. The amount of PGE1 in the lipid emulsion phase decreased from 87% to 75, 72, 61, 47 and 20% after the dilution with Physiosol ®·3, 5% Otsuka Toueki, Klinit ®, Otsuka Seishokuchu and Hartmann's Solution pH : 8, respectively, but not with Intralipos ® 10%. The release of PGE1 from the lipid emulsions occurred in relatively short period of time after the dilution and the phase-distribution ratios of PGE1 were unchanged throughout the experiment for 6 h. These findings strongly suggest that the dilution with Hartmann's Solution pH : 8 and Isotonic Sodium Chloride Solution is not necessarily the recommended prescriptions for combination with lipo-PGE1in maintaining its drug delivery function by the pharmaceutical view points. High pH of aqueous infusion combined with lipo-PGE1 for dilution tends to increase the release.

Original languageEnglish
Pages (from-to)441-447
Number of pages7
JournalDrug Delivery System
Volume13
Issue number6
DOIs
Publication statusPublished - 1998

Fingerprint

Alprostadil
Emulsions
Lipids
Pharmaceutical Preparations
Xylitol
Injections
Ultrafiltration
Sodium Chloride
Prescriptions
Sodium
Glucose

Keywords

  • aqueous infusion
  • DDS
  • drug information
  • lipid emulsion
  • lipo-PGE

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Drug delivery function of DDSs in clinical use : Changes in phase-distribution of PGE1 in lipid emulsions after dilution with aqueous infusions. / Kurosaki, Yuji; Hino, Bibari; Yamauchi, Keita; Kamiya, Kayo; Kawasaki, Hiromu.

In: Drug Delivery System, Vol. 13, No. 6, 1998, p. 441-447.

Research output: Contribution to journalArticle

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abstract = "To guarantee the drug delivery function of the DDS drugs in clinical use, supplementary information closely related to the diverse clinical usage is required in addition to information listed on the Products Information. Changes in the phase-distribution of PGE1 in lipo-PGE1(Palux inj. and Liple {\circledR}), a targeting-type DDS, after 10-times dilution with 6 aqueous infusions frequently prescribed for clinical treatment, i. e., 5{\%} Otsuka Toueki (Glucose Injection JP), Otsuka Seisholcuchu (Isotonic Sodium Chioride Solution JP), Klinit {\circledR} (Xylitol Injection JP), Physiosol {\circledR}·3, Hartmann's Solution pH : 8 and Intralipos {\circledR} 10{\%}, were examined in vitro. Total amounts of PGE1 and the amounts of PGE1 in the aqueous phase were determined by the ultrafiltration method to estimate phase-distribution ratios of PGE1 after 10-times dilution. Total amounts of PGE1 did not decrease after the dilution with each aqueous infusion. The amount of PGE1 in the lipid emulsion phase decreased from 87{\%} to 75, 72, 61, 47 and 20{\%} after the dilution with Physiosol {\circledR}·3, 5{\%} Otsuka Toueki, Klinit {\circledR}, Otsuka Seishokuchu and Hartmann's Solution pH : 8, respectively, but not with Intralipos {\circledR} 10{\%}. The release of PGE1 from the lipid emulsions occurred in relatively short period of time after the dilution and the phase-distribution ratios of PGE1 were unchanged throughout the experiment for 6 h. These findings strongly suggest that the dilution with Hartmann's Solution pH : 8 and Isotonic Sodium Chloride Solution is not necessarily the recommended prescriptions for combination with lipo-PGE1in maintaining its drug delivery function by the pharmaceutical view points. High pH of aqueous infusion combined with lipo-PGE1 for dilution tends to increase the release.",
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