Utilization of diethyl-beta-cyclodextrin as a sustained-release carrier for isosorbide dinitrate.
Heptakis(2,6-di-O-ethyl)-beta-cyclodextrin (2) was prepared and its physicochemical properties, such as aqueous solubility and surface activity, were compared with those of beta-cyclodextrin (1) and heptakis(2,6-di-O-methyl)-beta-cyclodextrin (3). A possible utility of 2 as a sustained-release drug carrier was examined using a water-soluble drug, isosorbide dinitrate. The dissolution and release rates of isosorbide dinitrate from capsule and tablet forms were significantly retarded by the complexation with 2. The sustained-release pattern of isosorbide dinitrate was produced for a long period after the oral administration of a single dose of capsule or tablet containing the 2 complex to rats. The results indicated that 2 may serve as a hydrophobic drug carrier for sustained-release of isosorbide dinitrate.
Hirayama
F
F
Faculty of Pharmaceutical Sciences, Kumamoto University, Japan.
Hirashima
N
N
Abe
K
K
Uekama
K
K
Ijitsu
T
T
Ueno
M
M
D000818:Animals; D002214:Capsules; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003505:Cyclodextrins; D003692:Delayed-Action Preparations; D003912:Dextrins; D004337:Drug Carriers; D007548:Isosorbide Dinitrate / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D012995:Solubility; D013213:Starch; D013607:Tablets; D047392:beta-Cyclodextrins
D002214:Capsules; D003505:Cyclodextrins; D003692:Delayed-Action Preparations; D003912:Dextrins; D004337:Drug Carriers; D013607:Tablets; D047392:beta-Cyclodextrins; C055959:heptakis(2,6-diethyl)beta-cyclodextrin; D013213:Starch; D007548:Isosorbide Dinitrate