Enteric solid dispersion of cyclosporin A (CyA) having potential to improve availability of CyA in rabbit.
The availability of cyclosporin A (CyA) administered as an enteric solid dispersion preparation of which the composition is CyA:HCO-60:HP-55 = 1:2:8 was evaluated in rabbits. The additives are surfactant (polyoxyethylated, 60 mumol, castor oil derivative, HCO-60) and enteric coating material (hydroxypropylmethyl cellulose phthalate, HP-55), which are generally used as pharmaceutical additives. Both the systemic and lymphatic availabilities of CyA from this solid preparation were measured in rabbits after intrastomach administration, 7 mg CyA/kg, and were compared with those from conventional oily solution, Sandimmun. The mean systemic availability of CyA from the solid preparation was 57% which is about 1.5 times greater than that obtained from Sandimmun. The amounts of CyA transferred into the thoracic lymphatics within 12 h from solid dosage form and Sandimmun are 0.62 +/- 0.16(S.D.)% and 0.13 +/- 0.05% of the administered CyA dose. These results support the usefulness of the new solid dosage form of CyA.
Takada
K
K
Oh-hashi
M
M
Furuya
Y
Y
Yoshikawa
H
H
Muranishi
S
S
D000818:Animals; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D003524:Cyclosporins / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011817:Rabbits
D003524:Cyclosporins