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Class III – low permeability, high solubility . Example: cimetidine; The absorption is limited by the permeation rate but the drug is solvated very fast. If the formulation does not change the permeability or gastro-intestinal duration time, then class I criteria can be applied. Class IV – low permeability, low solubility . Example: bifonazole
The overall incidence of adverse drug reactions to sulfa antibiotics is approximately 3%, close to penicillin; [3] hence medications containing sulfonamides are prescribed carefully. Sulfonamide drugs were the first broadly effective antibacterials to be used systemically, and paved the way for the antibiotic revolution in medicine.
Esterification is also used to control solubility. For example, stearate and estolate esters of drugs have decreased solubility in gastric fluid. Later, esterases in the gastrointestinal tract (GIT) wall and blood hydrolyze these esters to release the parent drug. Coatings on a tablet or pellet may act as barriers to reducing the dissolution rate.
Solubility in water can be estimated from the number of hydrogen bond donors vs. alkyl sidechains in the molecule. Low water solubility translates to slow absorption and action. Too many hydrogen bond donors, on the other hand, lead to low fat solubility, so that the drug cannot penetrate the cell membrane to reach the inside of the cell.
An example for a simple case (mono-compartmental) would be to administer D=8 mg/kg to a human. A human has a blood volume of around V b l o o d = {\displaystyle V_{blood}=} 0.08 L/kg . [ 7 ] This gives a C 0 = {\displaystyle C_{0}=} 100 μg/mL if the drug stays in the blood stream only, and thus its volume of distribution is the same as V b l o ...
For example, it is a building block in the preparation of the antibiotic linezolid, the anticancer agent gefitinib (brand name Iressa) and the analgesic dextromoramide. In research and in industry, the low cost and polarity of morpholine lead to its common use as a solvent for chemical reactions.
Ruthenium anti-cancer drugs are coordination complexes of ruthenium complexes that have anticancer properties. They promise to provide alternatives to platinum -based drugs for anticancer therapy. [ 1 ] [ 2 ] Triruthenium carbonyl complexes containing maltol, ethylmaltol, N-phenyl and N-benzyl 4-pyridones show excellent anticancer activity.
For example, is a derivate called CKD-602, which is a potent topoisomerase I inhibitor and successfully overcomes the poor water solubility and toxicity seen with CPT. [ 19 ] [ 20 ] Considerably greater activity can be achieved by putting electron-withdrawing groups like amino, nitro , bromo or chloro at position 9 and 10 and hydroxyl group at ...