ENHANCEMENT OF TRANSDERMAL DELIVERY BY SUPERFLUOUS THERMODYNAMIC POTENTIAL. III. PERCUTANEOUS ABSORPTION OF NIFEDIPINE IN RATS

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概要

• 論文の詳細を見る

• The bioavailability of percutaneous nifedipine was studied in rats. To improve the transdermal delivery of nifedipine, concentration changes due to loss of a volatile component in the vehicle were utilized. The percutaneous absorption of nifedipine was enhanced from binary solvent systems of acetone and propylene glycol (PG) or isopropyl myristate (IPM), compared with the results from simple PG or IPM saturated with the drug. In contrast, no appreciable increases in the percutaneous absorption of nifedipine from PG or IPM above controls were observed for pretreatment of the dosing site with acetone. From a ternary vehicle of volatile/nonvolatile-hydrophile/nonvolatile-lipophile solvent system, i.e., acetone-PG-IPM, a very dramatic enhancement in the bioavailability of nifedipine was noted. In addition, a marked increase in the penetration of PG from the ternary solvent system was found, compared with the result from the binary solvent system of acetone and PG. Nifedipine solutions with the volatile component eventually caused precipitaion at the dosing site and so reduced the plasma nifedipine concentration. The precipitation was inhibited or retarded when polymer additives were incorporated in the ternary solvent system, and the high plasma nifedipine concentrations were maintained. This effect was not diminished when the formulation was administered immediately after the evaporation of acetone. The area under the plasma nifedipine concentration-time curve from the ternary solvent system with a polymer additive was higher by about 75 times than that from PG saturated with the drug. From these observations, we conclude that the increase in the transdermal delivery of nifedipine was caused by the increase in the thermodynamic activity of the drug in the nonvolatile vehicle following the evaporation of the volatile component.

• 公益社団法人日本薬学会の論文

著者

• Sugimoto Isao

  Pharmaceutical Research Center Kanebo Ltd.

• Kondo Shuji

  Pharmaceuticals Research Center Kanebo Ltd.

• YAMANAKA CHIAKI

  Pharmaceuticals Research Center, Kanebo, Ltd.

• Yamanaka Chiaki

  Pharmaceuticals Research Center Kanebo Ltd.

関連論文

• SOLID DISPERSIONS OF POORLY WATER-SOLUBLE DRUGS WITH ENTERIC COATING AGENTS
• ENHANCEMENT OF TRANSDERMAL DELIVERY BY SUPERFLUOUS THERMODYNAMIC POTENTIAL. ii. IN VITRO-IN VIVO CORRELATION OF PERCUTANEOUS NIFEDIPINE TRANSPORT
• Effects of Penetration Enhancers on Percutaneous Absorption of Nifedipine. Comparison between Deet and Azone
• MOMENT ANALYSIS OF INTRAVENOUS, INTRADUODENAL, BUCCAL, RECTAL AND PERCUTANEOUS NIFEDIPINE IN RATS
• ENHANCEMENT OF TRANSDERMAL DELIVERY BY SUPERFLUOUS THERMODYNAMIC POTENTIAL. III. PERCUTANEOUS ABSORPTION OF NIFEDIPINE IN RATS
• STABILITY OF CIANIDANOL IN AQUEOUS SOLUTION AND IN SOLID STATE
• The Effect of Additives on the Oral Mucosal Absorption of Human Calcitonin in Rats
• ENHANCEMENT OF TRANSDERMAL DELIVERY BY SUPERFLUOUS THERMODYNAMIC POTENTIAL. I. THERMODYNAMIC ANALYSIS OF NIFEDIPINE TRANSPORT ACROSS THE LIPOIDAL BARRIER

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