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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.
Absorption is the journey of a drug travelling from the site of administration to the site of action. [ 1 ] [ 2 ] The drug travels by some route of administration ( oral , topical-dermal , etc.) in a chosen dosage form (e.g., tablets , capsules , or in solution ). [ 3 ]
Drug administration via the nasal cavity yields rapid drug absorption and therapeutic effects. [33] This is because drug absorption through the nasal passages does not go through the gut before entering capillaries situated at tissue cells and then systemic circulation and such absorption route allows transport of drugs into the central nervous ...
Multiphasic absorption: Drugs injected intravenously are removed from the plasma through two primary mechanisms: (1) Distribution to body tissues and (2) metabolism + excretion of the drugs. The resulting decrease of the drug's plasma concentration follows a biphasic pattern (see figure). Plasma drug concentration vs time after an IV dose
Drug metabolism is the metabolic breakdown of drugs by living organisms, usually through specialized enzymatic systems. More generally, xenobiotic metabolism (from the Greek xenos "stranger" and biotic "related to living beings") is the set of metabolic pathways that modify the chemical structure of xenobiotics, which are compounds foreign to an organism's normal biochemistry, such as any drug ...
Time course of drug plasma concentrations over 96 hours following oral administrations every 24 hours (τ). Absorption half-life 1 h, elimination half-life 12 h. Biological half-life ( elimination half-life , pharmacological half-life ) is the time taken for concentration of a biological substance (such as a medication ) to decrease from its ...
A V D greater than the total volume of body water (approximately 42 liters in humans [5]) is possible, and would indicate that the drug is highly distributed into tissue. In other words, the volume of distribution is smaller in the drug staying in the plasma than that of a drug that is widely distributed in tissues. [6]
Penetration enhancers have been applied to improve the absorption of poorly permeable, hydrophilic drugs or macromolecules. [10] Permeation enhancers that have been used successfully for oral drug development include medium-chain fatty acids like caprylic acid [11] or caprate, or its amino acid ester like Salcaprozate sodium (SNAC). [12]