In vitro and in vivo percutaneous absorption of topical dosage forms: case studies.
This article evaluated the influence of vehicle compositions on topical drug availability. In vitro drug release and in vivo experiments were performed in case of the hydrophilic ketamine hydrochloride and the lipophilic piroxicam. Ketamine hydrochloride is a NMDA receptor antagonist that has been useful for anesthesia and analgesia. The study of transdermal ketamine delivery is a novelty, because nobody has investigated the hypnotic effects of ketamine after this administration route. In vitro measurements gave a good basis for screening among the developed products. The physiological changes after ketamine administration showed, that there were significant differences among the parameters tested (breathing rate, duration of sleep) from the developed products (hydrogel, lyotropic liquid crystal and o/w cream) compared to the reference product (Carbopol gel). The in vivo feedback for piroxicam was the measurement of the anti-inflammatory activity by edema inhibition percentage. Significant differences were measured in case of the developed systems compared to the reference.
Csóka
I
I
Department of Pharmaceutical Technology, University of Szeged, Szeged, Hungary.
Csányi
E
E
Zapantis
G
G
Nagy
E
E
Fehér-Kiss
A
A
Horváth
G
G
Blazsó
G
G
Eros
I
I
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004355:Drug Stability; D018691:Excitatory Amino Acid Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D005612:Freeze Drying; D006863:Hydrogen-Ion Concentration; D007649:Ketamine / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D009824:Ointments / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D010894:Piroxicam / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D012995:Solubility; D013997:Time Factors; D014961:X-Ray Diffraction
D000894:Anti-Inflammatory Agents, Non-Steroidal; D018691:Excitatory Amino Acid Antagonists; D009824:Ointments; D010894:Piroxicam; D007649:Ketamine