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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
Anhydrous forms often dissolve faster but sometimes are less soluble. 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.
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 ...
It has the most rapid onset and offset of the volatile anesthetic drugs used for general anesthesia due to its low solubility in blood. Some drawbacks of desflurane are its low potency, its pungency and its high cost (though at low flow fresh gas rates, the cost difference between desflurane and isoflurane appears to be insignificant [2]).
It is hydrophobic with very low solubility in water, but good solubility in many organic solvents. [8] As a phytochemical , THC is assumed to be involved in the plant's evolutionary adaptation against insect predation , ultraviolet light , and environmental stress .
Elimination half-life: Dose-dependent; 2–3 h for low doses ... Solubility in water: 3 ... Aspirin is known to interact with other drugs. For example, ...
Lipinski's rule of five, also known as Pfizer's rule of five or simply the rule of five (RO5), is a rule of thumb to evaluate druglikeness or determine if a chemical compound with a certain pharmacological or biological activity has chemical properties and physical properties that would likely make it an orally active drug in humans.