IngentaConnect Effect of instillation method on the absorption of phenolsulphonp...

Authors: Nishida K.¹; Yoshida Y.¹; Mukai T.¹; Kawakami S.¹; Sakaeda T.²; Nakashima M.³; Sasaki H.³; Nakamura J.¹

Source: Journal of Pharmacy and Pharmacology, Volume 53, Number 10, 1 October 2001 , pp. 1341-1346(6)

Abstract:

We have examined the effect of the instillation method on the absorption of a drug from the liver and the small intestinal serosal surface in rats. We performed continuous microinstillation via an infusion pump and bolus instillation via a syringe, using phenolsulphonphthalein (phenol red) as the model drug. After continuous microinstillation of phenolsulphonphthalein 2.35mg in 235

L for 5min on the liver and small intestinal serosal surface in rats, the AUC (area under the curve) of the plasma concentration profile up to 60min was significantly higher compared with bolus instillation. A similar trend was observed after continuous microinstillation of phenolsulphonphthalein 2.35mg in 117.5

L for 2.5min. The calculated absorption rate constants (K_a) after continuous microinstillation of phenolsulphonphthalein based on a two-compartment model with first-order absorption were higher than those after bolus instillation on the liver and small intestinal serosal surface at either instillation concentration. Moreover, K_a was increased after continuous microinstillation of 2.35mg in 117.5

L at either instillation site. Instillation of phenolsulphonphthalein on the liver surface resulted in a 1.2- to 2.3-fold higher K_a compared with the small intestinal serosal surface. This tendency was marked after continuous microinstillation of 2.35mg in 117.5

L. In conclusion, absorption could be enhanced by instilling a small amount of drug solution on the liver surface gradually and continuously, suggesting a promising approach for instillation site-selective drug delivery in the peritoneal cavity.

Document Type: Research article

DOI: 10.1211/0022357011777837

Affiliations: 1: School of Pharmaceutical Sciences, Nagasaki University, 1-14 Bunkyo-machi, Nagasaki, Japan, 852-8521 2: Department of Hospital Pharmacy, School of Medicine, Kobe University, 7-5-2 Kusunoki-cho, Chuo-ku, Kobe, Japan, 650-0017 3: Department of Hospital Pharmacy, Nagasaki University School of Medicine, 1-7-1 Sakamoto, Nagasaki, Japan, 852-8501

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Effect of instillation method on the absorption of phenolsulphonphthalein as a model drug from the liver and small intestinal serosal surface in rats