Study Set Content:
Lach and associates used cyclodextrins to trap, stabilize, and solubilize
sulfonamides, tetracyclines, morphine, aspirin, benzocaine, ephedrine, reserpine, and testosterone.
The aqueous solubility of (blank) (0.5 mg/liter) -a drug used topically in the treatment of acne
retinoic acid
The aqueous solubility of retinoic acid (0.5 mg/liter) -a drug used topically in the treatment of acne is increased to 160 mg/liter by complexation with
𝞫-CD.
The dissolution rates of famotidine, a potent drug in the treatment of gastric and duodenal ulcers, and that of tolbutamide, an oral antidiabetic drug, are both increased by complexation with
𝞫-CD.
ends to favor pH-dependent hydrolysis of indomethacin in aqueous solution,
𝝰-CD
𝝰-CD tends to favor pH-dependent hydrolysis of indomethacin in aqueous solution, whereas (blank) Inhibits it
CD
𝞫-CD (1.8 g/100 ml at 25 C) is often insufficient to stabilize drugs at therapeutic doses and is also associated with (blank) when CD is administered by parenteral routes.
nephrotoxicity
The relatively low aqueous solubility of the cyclodextrins may be due to the formation of (blank) between the OH groups, which prevents their interaction with water molecules.
intramolecular hydrogen bonds
of some of the OH groups In CD reduces the intermolecular hydrogen bonding, leaving some OH groups free to Interact with water, thus increasing the aqueous solubility of CD.
Partial methylation (alkylation)
Amorphous derivatives of 𝞫-CD and y-CD are more effective as solubilizing agents for
sex hormones
Complexes of testosterone with (blank) allow an efficient transport of hormone into the circulation when given sublingually
amorphous hydroxypropyl 𝞫-CD
Hydrophobic forms of 𝞫-CD have been useful as
sustained-release drug carriers.
Release rate of the water-soluble calcium antagonist diltiazem was significantly decreased by complexation with
ethylated B-CD
ethylated B-CD used to retard the delivery of
isosorbide dinitrate
ethylated B-CD used to retard the delivery of isosorbide dinitrate, a
vasodilator
may improve the organoleptic characteristics of oral liquid formulations:
CD
Bitter taste of suspensions of (blank), is greatly suppressed by complexation of the drug with 𝞫-CD.
femoxetine, an antidepressant
MA CROMOLECULAR INCLUSION COMPOUNDS OR MOLECULAR SIEVES examples
Zeolites, dextrins, silica gels, and related substances
The atoms are arranged in three dimensions to produce
cages and channels
may be made to a definite pore size so as to separate molecules of different dimensions, and they are also capable of ion exchange.
Synthetic zeolites
