Introduction to biopharmaceutics (part:03)
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This document introduces concepts related to biopharmaceutics including Fick's first law of diffusion, gastrointestinal physiology, and the relationship between drug products and their pharmacological action. It defines key terms such as absorption, distribution, metabolism, and excretion. Fick's first law states that the rate of diffusion across a membrane is proportional to the difference in drug concentration on each side. The document also describes the anatomy and protective mucous layer of the gastrointestinal tract, and explains that orally administered drugs must dissolve before being absorbed and distributed throughout the body, where they may act, be stored, metabolized, or excreted.
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Here is an outline of the advantages and disadvantages of the specified routes of drug administration:
Oral route:
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Sublingual route:
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Drug absorption from git , Drug absorption from git , DIGESTION AND ABSORPTION , Transcellular / intracellular , transport , .Passive Transport Processes , Passive diffusion , Pore transport , Ion- pair transport , Facilitated or mediated diffusion
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Here is an outline of the advantages and disadvantages of the specified routes of drug administration:
Oral route:
- Advantages: Ease of administration, patient acceptance
- Disadvantages: Extensive first-pass metabolism in liver, variable absorption, gastrointestinal irritation
Sublingual route:
- Advantages: Rapid onset, avoids first-pass metabolism
- Disadvantages: Small surface area, drug must be soluble and pass buccal mucosa
Rectal route:
- Advantages: Avoidance of first-pass metabolism, noninvasive
- Disadvantages: Variable and slow absorption, not suitable for all drugs, socially unacceptable
Inhalational route:
- Advantages
Drug distribution
Drug distribution involves the reversible transfer of drugs between compartments like blood and tissues. Several factors affect how drugs are distributed, including tissue permeability, organ size and blood flow, and binding to tissue components. Drugs with certain physicochemical properties like small molecular size and appropriate lipophilicity more easily pass through barriers and cell membranes into tissues. Additionally, tissues with greater blood flow and perfusion rates allow for faster drug distribution. Finally, the extent to which drugs bind to proteins and other components in blood and tissues impacts their distribution.
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This document discusses factors that influence drug absorption in the gastrointestinal tract (GIT). It covers membrane physiology, GIT motility, the effect of age, clinical factors like diseases, and how food and drugs can impact drug absorption in the GIT. Key factors mentioned are gastric emptying rate, intestinal pH, surface area, transit time, blood flow, and how these can be altered by disease states or drugs, influencing a drug's absorption and bioavailability.
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When a drug is administered orally, it is absorbed through the gastrointestinal tract and enters the portal circulation, which carries blood directly from the intestines to the liver. This exposes the drug to high concentrations of hepatic drug metabolizing enzymes before it reaches systemic circulation. Many drugs, including propranolol, are extensively metabolized in the liver during first pass. This reduces the amount of unchanged/active drug that reaches the systemic circulation compared to intravenous administration, which bypasses first pass metabolism. Therefore, a higher oral dose is needed to achieve the same systemic drug concentration as a lower intravenous dose.
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This document discusses principles of drug action and distribution in the body. It begins by explaining that drugs modify existing functions and have multiple actions determined by their interaction with the body. It then defines pharmaceutical equivalents as drugs with the same active ingredients and administration route. Bioequivalence and therapeutic equivalents are also defined. The document goes on to discuss factors that influence drug absorption like ionization, solubility, and metabolism. It also covers transport mechanisms and how drug distribution is affected by factors like blood flow, protein binding, and volume of distribution.
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The document discusses gastrointestinal absorption of drugs. It describes the major absorption sites in the gastrointestinal tract including the stomach, small intestine and large intestine. It then discusses the various mechanisms of drug absorption including passive diffusion, carrier-mediated transport such as facilitated diffusion and active transport, ionic diffusion, ion pair transport, and endocytosis. Carrier-mediated transport uses carriers or enzymes to transport drugs against or along a concentration gradient, while passive diffusion occurs down a concentration gradient without carriers.
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Pharmacokinetics is the quantitative study of how drugs move through the body via absorption, distribution, metabolism, and excretion. Drugs are absorbed via processes like passive diffusion, active transport, or endocytosis and enter systemic circulation. However, first-pass metabolism in the liver and gut can reduce oral bioavailability by metabolizing drugs before they reach systemic circulation. Factors like dosage form properties, physiological conditions, and disease states can impact drug absorption and bioavailability.
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The document discusses drug absorption and factors affecting it. It defines absorption as the movement of an unchanged drug from the site of administration to systemic circulation by crossing biological membranes. The main mechanisms of drug absorption discussed are passive diffusion, carrier-mediated transport, and endocytosis. Pharmaceutical factors that can affect the rate of drug absorption include disintegration time, dissolution time, manufacturing variables like granulation method and compression force, and the type of excipients used in the formulation.
FACTORS AFFECTING DRUG ABSORPTION
This presentation is uploaded by Suraj Mandal. In which description about Factors affecting drug absorption
Drug absorption from GIT
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Drug distributionvpp
1. False
2. False
3. False, distribution is a passive process
4. False, it allows only small, non ionized and lipophilic drugs to diffuse passively
5. False, placental barrier is more permeable than BBB
6. Basic drugs will bound to the glycoproteins.
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This document discusses pharmacokinetics, specifically absorption, distribution, metabolism, and excretion of drugs. It covers the following key points:
- Drug absorption occurs through various routes like the gastrointestinal tract, lungs, skin and is influenced by factors like pH, blood flow and lipid solubility.
- Distribution of drugs depends on capillary permeability, blood flow, protein binding and is described using the volume of distribution.
- Metabolism occurs mainly in the liver through cytochrome P450 enzymes and conjugation reactions, and can inactivate drugs, produce active metabolites, or activate prodrugs.
- Absorption, distribution and metabolism determine the bioavailability of drugs and their delivery to sites of action.
Mechanism of drug absorption in git
1. Drug absorption involves the movement of unchanged drug molecules from the site of administration into systemic circulation. It occurs primarily through the gastrointestinal (GI) tract and is influenced by factors like solubility, permeability, and transport mechanisms.
2. There are three main mechanisms of drug transport across the GI tract - transcellular, paracellular, and vesicular. Transcellular transport occurs across cells and includes passive diffusion, active transport, and carrier-mediated transport. Paracellular transport is between cell junctions. Vesicular transport involves endocytosis within cells.
3. The most common mechanism is passive diffusion, which does not require energy. Other mechanisms like active transport and carrier-mediated transport use
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- 1. I N T R O D U C T I O N TO B I O P H A R M A C E U T I C S PA RT: 3
- 2. CONTENTS • Fick's first law • Gastrointestinal (GI) Physiology • Relationship between drug product and pharmacological action • Definitions of Drugs: Absorption Distribution Metabolism Excretion
- 3. FICK'S FIRST LAW • Passive transport is described by Fick's first law which state that the rate of diffusion across a membrane is proportional to the difference in drug concentration on each side of the membrane. • Therefore, the rate of drug differs from the membrane, • 𝐝𝐜 𝐝𝐭 = 𝐤𝐦 𝐟 ADh (CGIT - CB) Where, dc dt = rate of diffusion K = specific permeability of the drug 𝒎 𝒇 = partition coefficient of the drug between the biology membrane and gastrointestinal fluid A = surface area of biological membrane h = thickness of the biologic membrane D = partition or diffusion coefficient CGIT = concentration of drug in GI fluid CB = concentration of drug in blood
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- 5. 3)GASTROINTESTINAL (GI) PHYSIOLOGY: - The gastrointestinal tract is a muscular tube approximately 6 m in length with varying diameters. - It stretches from the mouth to the anus and consists of four main anatomical areas: the oesophagus, the stomach, the small intestine and the large intestine or colon. - The majority of the gastrointestinal epithelium is covered by a layer of mucous. This is a viscoelastic translucent aqueous gel that is secreted throughout the GIT, acting as a protective layer and a mechanical barrier.
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- 9. Absorption: The transfer of drug from the site of administration to the blood stream is called absorption. Distribution: Drug distribution refers to the reversible transfer of drug between the blood and the extravascular fluid and tissue of the body (for example fat, muscle and brain tissue). Metabolism: It is chemical alteration of drug in the body where in non-polar lipids soluble compound are made more polar lipids insoluble, so that they are easily excreted. - Primary site of drug metabolism: liver Other: kidney, intestine, lungs, plasma. Excretion: excretion is the process whereby drug or metabolites are irreversibly transfer from the internal to the external environment. Excretion is the passage out of systematically absorbed drug. - Principal organ involved: • Kidney, lungs, biliary system, intestine, saliva milk.
- 10. …….T0 BE CONTINUED….. .....Part 4 will be published on 15/04/2021…..