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Absorption drugs

The intestinal tract consists of duodenum, jejunum, ileum, colon, and rectum. The total length of the small intestinal tract comprises 3-4 m in humans with duodenum having 12-15 cm, 150 cm jejunum and 70 cm ileum. Its apparent inner surface of approximately 3000 cm is extended by microvilli to approximately 200 m.  [Pg.239]

The small intestinal tract is the major place of digestion and absorption. Protein digestion reaches approximately 15% in the stomach, and in the lower intestine, the hydrolyzed fraction amounts to about 60%. Seventy percent of fats, 60% of carbohydrates, and about 30% of protein and peptide are absorbed within the duodenum. Within enterocytes, triglycerides are resynthesized from long-chain fatty acids and transformed into chylomicrons, which are transported via the lymphatic system, whereas short- and medium-chain fatty acids are directly transported into mesenteric and portal vein system. [Pg.239]

For the absorption of carbohydrates, amino acids, and peptides, a variety of transport systems following facilitated diffusion and active mechanisms have been identified on a molecular and functional level. D-Glucose is mainly absorbed via the Na -dependent transporter SGLTl in the brush-border membrane of enterocytes [18-20]. It is transported across the basolateral membrane by facilitated diffusion via the hexose transporter GLUT-2. Besides SGLTl, the Na +-independent transport protein GLUT-5 is localized in the apical enterocyte membrane, recognizing fructose as a substrate [21]. [Pg.239]

The ileal bile acid transporter (IBAT) transports conjugated bile acids in a Na + -dependent manner. Like the peptide transporter, it serves as a target for prodrugs, which consist of drugs being coupled to the hydroxyl group at position 3 of the steroid ring system of a bile acid [25, 26]. [Pg.240]

Several studies highlight the use of mdrl-knockout mice to investigate P-glyco-protein function in vivo [45, 46]. In bile duct-ligated mice, 16% of digoxin administered i.v. was secreted into the gut lumen of control animals, whereas only 2% was secreted in mdrl-knockout mice [47], This finding supports the earlier observations [Pg.241]


Historically, drug absorption, distribution, metabolism, excretion, and toxicity ADMET) studies in animal models were performed after the identification of a lead compound. In order to avoid costs, nowadays pharmaceutical companies evaluate the ADMET profiles of potential leads at an earlier stage of the development... [Pg.607]

This generally describes the process of drug absorption into the body, distribution throughout the body, metabolism by degrad a tive and metabolizing enzymes in the body, and finally elimination from the body. It is useful to consider each of these steps because together they summarize pharmacokinetics. [Pg.163]

Chan LM, Lowes S, Hirst BH (2004) The ABCs of drug transport in intestine and liver efflux proteins limiting drug absorption and bioavailability. Eur J Pharm Sci 21 25—51... [Pg.8]

A special case for reduced bioavailabilty results from first-pass extraction that sometimes might be subjected to saturable Michaelis-Menten absorption kinetics. The lower the hepatic drug clearance is (Clhep) in relation to liver blood flow (Ql), or the faster the drug absorption rate constant (Ka), and the higher the dose (D) are, the more bioavailable is the drug (F). [Pg.956]

Dopa — see Phenylalanine, dihydroxy-Dopplerite structure, 6, 849 Douglasite structure, 6, 846 Down s syndrome Alzheimer s disease, 6,770 DPP A process, 6,911 Drugs absorption metals, 6, 774... [Pg.124]

Figure 13 presents a schematic diagram for drug absorption from the peritoneal cavity. As mentioned above, particles (e.g., erythrocytes, bacteria, colloidal gold, and liposomes) which are not able to pass capillary membranes are removed from the peritoneal cavity via the lymphatic system (Fig. 13, I and II). Relatively low molecular weight compounds (e.g., drugs) are exclusively absorbed via splenic blood capillaries into the portal vein (Fig. 13, III). Figure 13 presents a schematic diagram for drug absorption from the peritoneal cavity. As mentioned above, particles (e.g., erythrocytes, bacteria, colloidal gold, and liposomes) which are not able to pass capillary membranes are removed from the peritoneal cavity via the lymphatic system (Fig. 13, I and II). Relatively low molecular weight compounds (e.g., drugs) are exclusively absorbed via splenic blood capillaries into the portal vein (Fig. 13, III).
FIGURE 13 Schematic diagram for drug absorption fi om the peritoneal cavity. I and II represent the lymphatic system and III represents splenic blood capillaries. (Adapted from Hirano and Hunt, 1985.)... [Pg.302]

Artursson P and Karlsson J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Commun 1991 175 880-5. [Pg.509]

The concept of maximum absorbable dose (MAD) relates drug absorption to solubility via [27, 28] ... [Pg.31]

Van de Waterbeemd, H., Smith, D. A., Beaumont, K., Walker, D. K. Property-based design optimization of drug absorption and pharmacokinetics. [Pg.43]

Kerns, E. H., Di, L. Physicochemical profiling overview of the screens. Drug Discov. Today Technol. 2004, 1, 343-348. Van de Waterbeemd, H. Physicochemical approaches to drug absorption. In Drug Eioavailability (Methods and Principles in Medicinal Chemistry), Van de Waterbeemd, H., Lennernas, H., Artursson, P. (eds.), Wiley-VGH, Weinheim, 2003, pp. 3-20. [Pg.43]

Avdeef, A., Tsinman, O. PAM PA -a drug absorption in vitro model 13. Chemical selectivity due to membrane hydrogen bonding in comho comparisons of HDM-, DOPC-, and DS-PAMPA models. Eur. J. Pharm. Set. 2006, 28, 43-50. [Pg.44]

Reppas, C., Shah, V. P. Dissolution testing as a prognostic tool for oral drug absorption immediate release dosage forms. Pharm. Res. 1998, 15, 11-22. [Pg.45]

Camenisch, G., Van de Waterbeemd, H Folkers, G. Review of theoretical passive drug absorption models historical background, recent development and limitations. Pharm. Acta. Helv. 1996, 73, 309-327. [Pg.45]

E. P., McEarland,. W., Schaper, K.-J. Quantitative estimation of drug absorption in humans for passively transported compounds on the basis of their physico-chemical parameters. [Pg.46]

Van de Waterbeemd, H. Intestinal permeability prediction from theory. In Oral Drug Absorption, Dressman, J. B., Lennemas, H. (eds.), Dekker, New York, 2000, pp. 31-49. [Pg.47]

Palm, K., Luthman, K., Ungell, A.-L., Strandlund, G., Beigi, F., Lundahl, P., Artursson, P. Evaluation of dynamic polar molecular surface area as predictor of drug absorption comparison with other computational and experimental predictors. J. Med. Chem. 1998, 41, 5382-5392. [Pg.47]

Stenberg, P., Norinder, U., Luthman, K., Artursson, P. Experimental and computational screening models for the prediction of intestinal drug absorption. [Pg.47]

Avdeef, A., Strafford, M., Block, E., Balogh, M. P., Chambliss, W., Khan, I. Drug absorption in vitro model filter-immobilized artifidal membranes 2. Studies of the permeability properties of lactones in Piper methysticum Forst. Eur.J. Pharm. Sci. 2001, 14, 271-280. [Pg.50]

PSA was also shown to play an important role in explaining human in vivo jejunum permeability [18]. A model based on PSA and calculated log P for the prediction of drug absorption [19] was developed for 199 well-absorbed and 35... [Pg.114]

Since experimental determination of intestinal absorption is quite demanding, Caco-2 cell monolayers have been successfully used to model passive drug absorption. Several models for the prediction of Caco-2 permeability using PSA were developed, including those of van de Waterbeemd et al. [5] and Palm et al. [22] who found that relationships between Caco-2 permeability and PSA is stronger than with Clog D, Krarup et al. [23] who used dynamic PSA calculated for water accessible molecular surface and Bergstrom et al. [24]. [Pg.115]

Krarup, L. H., Christensen, 1. T., Hovgaard, L., Frokjaer, S. Predicting drug absorption from molecular surface properties based on molecular dynamics simulations. Pharm. Res. 1998, 15, 972-978. [Pg.125]


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Absorption Drug Entry into the Bloodstream

Absorption analysis specific drug

Absorption drug design

Absorption drug development considerations

Absorption drugs, intestinal tract

Absorption enhancers enteral drug delivery

Absorption enhancers nasal drug delivery

Absorption enhancers oral drug delivery

Absorption enhancing systems, rectal drug

Absorption high extraction ratio drugs

Absorption nasal drug delivery

Absorption of drugs

Absorption of drugs applied to the eye

Absorption of macromolecular drugs

Absorption poorly absorbed drug moieties

Absorption protein drugs

Absorption variability with oral drug delivery

Absorption, 6-8 drug classification

Absorption, antimicrobial drugs

Absorption, distribution, and excretion of drugs

Absorption, distribution, metabolism drug delivery systems

Absorption, distribution, metabolism drug discovery studies

Absorption, distribution, metabolism drug solubility

Absorption, distribution, metabolism small-molecule drugs

Absorption, distribution, metabolism, and excretion of drugs

Absorption, drug across intestinal epithelium

Absorption, drug across nasal epithelium

Absorption, drug ester prodrugs

Absorption, drug food effects

Absorption, drug from rectal cavity

Absorption, drug gastrointestinal processes affecting

Absorption, drug improving poor oral

Absorption, drugs cell membrane role

Absorption, drugs definition

Acidic drugs absorption

Acidic drugs, oral absorption

Affecting Drug Absorption

Area under plasma concentration time curve drug absorption

Basic drugs absorption

Basic drugs, oral absorption

Bioavailability drug absorption

Bioequivalence drug absorption

Biopharmaceuticals oral drug absorption

Buccal absorption drug transport mechanism

Buccal cavity, absorption drugs

Caco drug absorption experiments

Carrier-Mediated Approaches to Drug Absorption

Cell permeation enhancers drug absorption

Chemical transdermal enhancers drug absorption

Children drug absorption

Chronic disease, oral drug absorption

Colon drug absorption

Colonic drug absorption

Colonic drug absorption enhancers

Colonic epithelium drug absorption barrier

Computational Approaches to Drug Absorption and Bioavailability

Computational drug absorption

Controlled release, drug absorption

Correlation Between Nasal Drug Absorption Models

Culture Models of the Corneal Epithelium and Reconstructed Cornea Equivalents for In Vitro Drug Absorption Studies

Cyclodextrins drug absorption, enhancement

Delivery, drug design absorption

Digestion drug absorption factors

Drug Absorption Studies Using the Isolated Perfused Lung

Drug Absorption in the Lung

Drug absorption and permeability

Drug absorption aspirin

Drug absorption boundary layers

Drug absorption buccal mucosa

Drug absorption carrier-mediated approaches

Drug absorption carrier-mediated systems

Drug absorption colon role

Drug absorption convective

Drug absorption dosage form

Drug absorption enhancement

Drug absorption estimation

Drug absorption factors affecting

Drug absorption from the gastrointestinal tract

Drug absorption gastric emptying

Drug absorption gastric mucosa

Drug absorption genetic polymorphisms

Drug absorption grapefruit juice effect

Drug absorption in vivo

Drug absorption interactions

Drug absorption interactions affecting

Drug absorption intestinal mucosa

Drug absorption intestine

Drug absorption living tissues

Drug absorption macromolecules

Drug absorption mechanisms

Drug absorption membrane factors

Drug absorption metabolism studies

Drug absorption models

Drug absorption models limitations

Drug absorption oral cavity

Drug absorption oral cavity mucosa

Drug absorption orally delivered drugs

Drug absorption passive diffusion

Drug absorption perfusion cells

Drug absorption physiological factors

Drug absorption physiological factors affecting

Drug absorption process

Drug absorption receptor-mediated endocytosis

Drug absorption rectal suppositories

Drug absorption slow gastric emptying

Drug absorption small intestine secretions

Drug absorption splanchnic blood flow

Drug absorption stomach secretions

Drug absorption studies

Drug absorption sublingual drugs

Drug absorption surfactant effects

Drug absorption techniques

Drug absorption through skin

Drug absorption topical drugs

Drug absorption transcellular

Drug absorption transcomeal

Drug absorption transdermal drugs

Drug absorption unstirred layer

Drug absorption, and

Drug absorption, distribution

Drug absorption, distribution and excretion

Drug absorption, distribution metabolism, and excretion

Drug absorption, distribution studies

Drug absorption, distribution, metabolism, and

Drug absorption, pharmacokinetic

Drug absorption, pharmacokinetic administration routes

Drug absorption, pharmacokinetic renal disease

Drug action absorption

Drug candidates oral absorption potential

Drug development absorption

Drug disposition absorption

Drug disposition percutaneous absorption

Drug effects absorption

Drug properties absorption

Drug property improvement absorption enhancement

Drugs buccal absorption

Drugs measuring absorption

Duodenum, drug absorption

Effect of surfactants on drug absorption

Effects of Renal Disease on Drug Absorption

Emulsion drug absorption

Estimating Drug Absorption Trends from Physiochemical Characteristics

Extravascular administration drug absorption

Factors affecting passive drug absorption

Gastrointestinal Dissolution and Absorption of Class II Drugs

Gastrointestinal Dissolution and Absorption of Drugs

Gastrointestinal Transit and Drug Absorption

Gastrointestinal absorption, of drugs

Gastrointestinal drug absorption

Gastrointestinal drug absorption membrane factors

Gastrointestinal lipophilic drug absorption

Gastrointestinal lipophilic drug absorption barriers

Gastrointestinal lipophilic drug absorption enhancement

Gastrointestinal lipophilic drug absorption mechanisms

Gastrointestinal lipophilic drug absorption solubility

Gastrointestinal lipophilic drug absorption solutions

Gastrointestinal lipophilic drug absorption systems

Gastrointestinal system drug absorption

Gastrointestinal tract drug delivery absorption

Gastrointestinal tract processes affecting drug absorption

Gastrointestinal tract, drug absorption

Geriatric patient drug absorption

Hepatic portal system, drug absorption

Hydrophilic drugs absorption

Hydrophobic interactions drug absorption

Ileum, drug absorption

Infants oral drug absorption

Infants percutaneous drug absorption

Interstitial drug absorption

Intestinal drug absorption

Intestinal drug absorption fraction absorbed

Intestinal drug absorption in silico models

Intestinal drug absorption influencing factors

Intestinal drug absorption parameters influencing

Intestinal drug absorption permeability

Intestinal drug absorption prediction

Intestinal drug absorption solubility

Intestinal drug transport and absorption

Intestinal wall metabolism, during drug absorption

Intramuscular injection drug absorption from

Ion Pair Absorption of Ionized Drugs—Fact or Fiction

Ionizable drugs, enhanced absorption from

Jejunum, drug absorption

Kinetics drug absorption

Kinetics of Drug Absorption after Oral Administration

Lipophilic drug absorption

Lipophilic drug absorption activity

Lipophilic drug absorption approach

Lipophilic drug absorption barriers

Lipophilic drug absorption emulsions

Lipophilic drug absorption enhanced gastrointestinal

Lipophilic drug absorption enhancing

Lipophilic drug absorption enterocyte barriers

Lipophilic drug absorption lipid-based formulations

Lipophilic drug absorption lymphatic transport

Lipophilic drug absorption mechanisms

Lipophilic drug absorption prodrug approach

Lipophilic drug absorption self-emulsifying systems

Lipophilic drug absorption solubility

Lipophilic drug absorption systems

Lipophilic drug absorption water-soluble prodrug

Liver drug absorption

Lung Model Selection for Drug Absorption Studies

Lung airways drug absorption

Manufacturing processes, drug absorption

Metals drug absorption

Mixed micelles drug absorption

Molar absorptivity acidic drugs

Nasal absorption drug delivery systems

Nasal drug absorption

Nasal drug absorption advantage

Nasal drug absorption application

Nasal drug absorption factors influencing

Nasal drug absorption metabolism studies

Nasal drug absorption optimization

Nasal drug absorption permeability studies

Nasal drug absorption specific applications

Nasal drug delivery absorption enhancement

Nasal drug delivery absorption mechanisms

Nasal drug delivery systemic absorption

Neonates drug absorption

Neonates intramuscular drug absorption

Neonates oral drug absorption

Optimal drug absorption

Optimization of Drug Absorption Enhancement Strategies

Oral administration drug absorption after

Oral drug absorption

Oral drug absorption bioavailability

Oral drug absorption food, effect

Oral drug absorption gastric emptying time

Oral drug absorption gastrointestinal motility

Oral drug absorption general considerations

Oral drug absorption intestinal motility

Oral drug absorption kinetics

Oral drug absorption mass balance

Oral drug absorption physiologically-based models

Oral drug absorption prediction

Oral drug absorption process

Oral drug absorption rate-limiting

Oral drug absorption rate-limiting processes

Oral drug absorption, by chitosan

Oral drug delivery absorption variability

Orally delivered drugs absorption

PH, and drug absorption

Parenteral delivery routes drug absorption

Passive transport drug absorption

Percutaneous drug absorption

Permeability Studies and Characterization of Drug Absorption Pathways

Permeable drugs, absorption

Pharmacokinetics drug absorption

Pharmacokinetics, physiological aspects drug absorption

Pharmacology drug absorption

Physico-chemical Approaches to Drug Absorption

Physicochemical Approaches to Drug Absorption

Probabilistic Model for Drug Absorption

Profiling of Drug Absorption, Distribution, Metabolism and Elimination in Man the hADME Study

Pulmonary drug delivery absorption

Receptor-Mediated Endocytosis and Drug Absorption

Rectal absorption of drugs

Rectal drug absorption

Rectal drug absorption bile acids

Rectal drug absorption control

Rectal drug absorption difficulties

Rectal drug absorption enhancement

Rectal drug absorption enhancers

Rectal drug absorption enhancing mechanism

Rectal drug absorption modification

Rectal drug absorption surfactants

Rectum, drug absorption

Renal insufficiency drug absorption

Role of Transporters in Drug Absorption

Secretions from small intestine drug absorption

Secretions from stomach drug absorption

Small intestine drug absorption

Solubility drug absorption

Stomach, drug absorption

Strategies for Increasing Drug Absorption Targeting Transporters

Systemic drug absorption

Tetracycline drugs absorption

The Intestinal Mucosa as a Physical and Biochemical Barrier to Drug Absorption

The Isolated Perfused Lung for Drug Absorption Studies

The Small Intestine and Secretions Relevant to Drug Absorption

The process of drug absorption

Therapeutics, pharmacokinetic basis drug absorption

Transcellular Drug Absorption—Simple and Facilitated Diffusion

Transcorneal Drug Absorption into the Eye

Transdermal drug delivery absorption

Transport mechanisms drug absorption

Transporters drug absorption targeting

Uterine drug absorption

Vaginal drug absorption

Vitro Cellular Models for Nasal Drug Absorption Studies

Vitro Screening Models to Assess Intestinal Drug Absorption and Metabolism

Water-soluble drugs oral absorption

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