Microemulsion and mixed micelle for oral administration as new drug formulations for highly hydrophilic drugs.
Microemulsions (MEs) and mixed micelles (MMs) have been used as new drug formulations for high hydrophilic drugs such as cefpirom and cefodizim for oral administration. Cefpirom and cefodizim are neither actively nor passively transported across cell membranes. Up to date, they can be only administrated intravenously (i.v.) or intramuscularly (i.m.). The rabbit (Chinchilla) in vivo model was used in the present work to investigate ways of overcoming the poor oral absorption of these cephalosporins. The cephalosporins at 100mg/kg were formulated in MEs and MMs and administered intraduodenally (i.d.). Very low bioavailability (2.5-3.0%) was observed, if cefpirom or cefodizim i.d. were applied without colloidal vehicle. However, the addition of the cephalosporins to ME or MM is shown to be highly effective in increasing the bioavailability values (up to 64% absolute bioavailability) of the model drugs. In conclusion, MEs and MMs improve essentially the oral bioavailability of the high hydrophilic drugs.
Mrestani
Yahya
Y
Institute of Applied Dermatopharmacy, Martin-Luther-University Halle-Wittenberg, Halle, Germany. yahya.mrestanit@pharmazie.uni-halle.de
Behbood
Laila
L
Härtl
Albert
A
Neubert
Reinhard H H
RH
D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D002439:Cefotaxime / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D002511:Cephalosporins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D004339:Drug Compounding / Q000379:methods; D004655:Emulsions / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D005260:Female; D007408:Intestinal Absorption; D008823:Micelles; D011817:Rabbits; D000097572:Cefpirome
D002439:Cefotaxime; D002511:Cephalosporins; D004337:Drug Carriers; D004655:Emulsions; D008823:Micelles; D000097572:Cefpirome; C033356:cefodizime