Development and in vivo assessment of a transdermal system for physostigmine
| Autor: | F. Fouchart, M. Vincenti, R. Vienet, Alain Pruvost, M. Istin, Jean-Marc Grognet, Henri Benech |
|---|---|
| Rok vydání: | 1998 |
| Předmět: |
Male
Physostigmine Chromatography biology Stereochemistry Chemistry Administration Topical Absorption (skin) Dosage form Drug Delivery Systems Pharmacokinetics PHY In vivo Area Under Curve medicine biology.protein Animals Cholinesterase Inhibitors Rabbits Half-Life Skin Transdermal medicine.drug Cholinesterase |
| Zdroj: | Methods and Findings in Experimental and Clinical Pharmacology. 20:489 |
| ISSN: | 2013-0155 |
| DOI: | 10.1358/mf.1998.20.6.485712 |
| Popis: | A copolymer was developed as a transdermal (TD) system for physostigmine. The loading was carried out with a solution of physostigmine (PHY) base (20 mg/ml) in water/ethanol: 80/20 (v/v) at 40 degrees C for 3 h. The PHY load was 5.3 mg/cm2 (n = 3). Desorption carried out in vitro showed that 70% was desorbed during the first 6 h. More than 50% of the PHY was degraded within 45 min in skin homogenate. The TD was tested in vivo in rabbits during a 24 h experiment. PHY was quantified using a validated HPLC method. AUC0-24 h was 245.2 +/- 337.2 h.ng/ml. The mean pad flux reached 4.6 +/- 6.3 micrograms/cm2 from 0 to 24 h and, 24 h after the application of the pad, 110 micrograms/cm2 of PHY had been passed through the skin. After removed of the patch, plasma concentrations first increased from 15.8 +/- 28.6 ng/ml (at 24 h) to 21.4 +/- 36.7 ng/ml, then decreased with an elimination half-life of 0.7 +/- 0.2 h. AChE inhibition percentages increased from 6.5 +/- 2.3% to 16.0 +/- 27.7%. In vitro and in vivo studies in rabbit have shown that this system is suitable for further investigations in order to obtain a possible carrier for PHY therapy. |
| Databáze: | OpenAIRE |
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