Buccal absorption of ergotamine tartrate using the bioadhesive tablet system in guinea-pigs.
The buccal administration of ergotamine tartrate (ET) combined with polyvinyl alcohol (PVA) gel brought about higher plasma concentration of ET compared with that of oral administration of capsules in guinea-pigs. T(max) of ET in plasma of buccal administration was significantly smaller than that of oral administration. For the buccal dosage form of ET, the bioadhesive tablet system (BTS) was newly developed. It consisted of a reservoir of drug and an adhesive region. BTS showed better absorption of ET compared with PVA gel in guinea pigs. Among several pharmaceutical bases in the reservoir of BTS, Witepsol W-35 was most effective. It is likely that the high lipophilic property of Witepsol W-35 in which ET was dissolved facilitated the drug release by its relatively low melting point (around 35 degrees C), consequently a rapid absorption. In addition, the enhancing activity of the cod-liver oil extract (CLOE) in hydrophilic ointment on the in vivo buccal ET absorption was clarified to be comparable to that in the in vitro study utilizing the keratinized epithelial-free membrane (KEF-membrane) of the hamster cheek pouch.
Tsutsumi
Keiko
K
Department of Pharmaceutics, Hoshi University, Ebara 2-4-41, Shinagawa, Tokyo 142-8501, Japan.
Obata
Yasuko
Y
Nagai
Tsuneji
T
Loftsson
Thorsteinn
T
Takayama
Kozo
K
D000042:Absorption; D000269:Adhesives; D000316:Adrenergic alpha-Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D000465:Algorithms; D000818:Animals; D019540:Area Under Curve; D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D004878:Ergotamine / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D005079:Excipients; D005782:Gels; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009061:Mouth Mucosa / Q000378:metabolism*; D009824:Ointments; D011142:Polyvinyl Alcohol; D013607:Tablets
D000269:Adhesives; D000316:Adrenergic alpha-Agonists; D002214:Capsules; D005079:Excipients; D005782:Gels; D009824:Ointments; D013607:Tablets; D011142:Polyvinyl Alcohol; D004878:Ergotamine