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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.
According to the Biopharmaceutics Classification System (BCS) drug substances are classified to four classes upon their solubility and permeability: [1] Class I – high permeability, high solubility. Example: metoprolol, paracetamol [2] Those compounds are well absorbed and their absorption rate is usually higher than excretion.
The drug apparent permeability (P app) is calculated by normalizing the drug flux (j) over the initial concentration of the API in the donor compartment (c 0) as: Equation 2: = / Dimensionally, the P app represents a velocity, and it is normally expressed in cm/sec. The highest is the permeability, the highest is expected to be the ...
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
The model equations follow the principles of mass transport, fluid dynamics, and biochemistry in order to simulate the fate of a substance in the body. [9] Compartments are usually defined by grouping organs or tissues with similar blood perfusion rate and lipid content (i.e. organs for which chemicals' concentration vs. time profiles will be similar).
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 ...
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 ]
Enterohepatic circulation of drugs. Enterohepatic circulation is the circulation of biliary acids, bilirubin, drugs or other substances from the liver to the bile, followed by entry into the small intestine, absorption by the enterocyte and transport back to the liver.