600:
25:
529:, comprising two layers of phospholipids in which the charged hydrophilic heads face outwards and the uncharged hydrophobic fatty acid chains are in the middle of the layer. The fatty acid chains repel ionized, charged molecules. This means that the ionized molecules cannot pass through the intestinal membrane and be absorbed.
221:
The rate of dissolution is a key target for controlling the duration of a drug's effect, and as such, several dosage forms that contain the same active ingredient may be available, differing only in the rate of dissolution. If a drug is supplied in a form that is not readily dissolved, it may be
433:
of a compound. Different polymorphs have different solubility and dissolution rate characteristics. Specifically, crystalline forms dissolve slower than amorphous forms since they require more energy to leave the lattice during dissolution. The stablest crystalline polymorph has the lowest
578:
of a compound—these chemical variants may be more readily absorbed and then metabolized by the body into the active compound. However, changing the structure of a molecule is less predictable than altering dissolution properties, since changes in chemical structure may affect the
226:
since the medication will not have to be taken as often. Additionally, slow-release dosage forms may maintain concentrations within an acceptable therapeutic range over a longer period, whereas quick-release dosage forms may have sharper peaks and troughs in serum concentration.
521:
will affect its absorption, since ionic molecules are charged. Solubility favors charged species, and permeability favors neutral species. Some molecules have special exchange proteins and channels to facilitate movement from the lumen into the circulation.
190:, since a drug must be absorbed before any medicinal effects can take place. Moreover, the drug's pharmacokinetic profile can be easily and significantly changed by adjusting factors that affect absorption.
312:
893:"Bioavailability of triple-bead mixed amphetamine salts compared with a dose-augmentation strategy of mixed amphetamine salts extended release plus mixed amphetamine salts immediate release"
418:
As can be inferred from the Noyes–Whitney equation, the rate of dissolution may be modified primarily by altering the surface area of the solid by altering the particle size (e.g., with
355:
467:
Coatings on a tablet or pellet may act as barriers to reducing the dissolution rate. Coatings may also be used to control where dissolution takes place. For example,
394:
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dissolution rate. Dissolution also differs between anhydrous and hydrous forms of a drug. Anhydrous forms often dissolve faster but sometimes are less soluble.
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First-order absorption: rate of absorption is proportional to the amount of drug remaining to be absorbed. Representative examples include typical cases of
422:). For many drugs, reducing the particle size reduces the dose needed to achieve the same therapeutic effect. The particle size reduction increases the
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Absorption also varies depending on bioactivity, resonance, the inductive effect, isosterism, bio-isosterism, and consideration, amongst others.
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The solubility and permeability of a drug candidate are important physicochemical properties the scientist wants to know as early as possible.
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offers a way to determine the proportion of a substance that is ionized at a given pH. In the stomach, drugs that are
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Ions cannot passively diffuse through the gastrointestinal tract because the epithelial cell membrane is made up of a
517:. Pure lipid bilayers are generally permeable only to small, uncharged solutes. Hence, whether or not a molecule is
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Alsanosi, Safaa
Mohammed M.; Skiffington, Craig; Padmanabhan, Sandosh (2014). "Pharmacokinetic Pharmacogenomics".
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administration does not involve absorption, and there is no loss of drug. The fastest route of absorption is
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This aspect of absorption has been targeted by medicinal chemists. For example, they may choose an
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Oral ingestion is the most common route of administration of pharmaceuticals. Passing through the
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is the journey of a drug travelling from the site of administration to the site of action.
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Zero-order absorption: rate of absorption is constant. A common example is continuous
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released gradually and act for longer. Having a longer duration of action may improve
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Instantaneous absorption: absorption is nearly immediate. A common example is bolus
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that is more likely to be in a non-ionic form. Also, the chemists may develop
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Yang, Y.; Zhao, Y.; Yu, A.; Sun, D.; Yu, L.X. (2017). "Oral Drug
Absorption".
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Drugs held in solution do not need to be dissolved before being absorbed.
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Lipid-soluble drugs are absorbed more rapidly than water-soluble drugs.
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Miles Hacker; William S. Messer; Kenneth A. Bachmann (19 June 2009).
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The rate of dissolution may also be altered by choosing a suitable
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C is the concentration of the solid in the bulk dissolution medium.
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552:, weak acids will have a higher absorption in the highly acidic
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Types of absorption in pharmacokinetics include the following:
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940:"Pharmacokinetics: Optimising safe and effective prescribing"
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Kaplan
Pharmacology 2010, Video Lectures, Absorption chapter
206:, the contents of the capsule or tablet are absorbed by the
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567:) will diffuse more readily since they will be non-ionic.
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may act as barriers to some drugs. They are essentially
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and the dissolution rate and does not affect solubility.
307:{\displaystyle {\frac {dW}{dt}}={\frac {DA(C_{s}-C)}{L}}}
210:. The absorbed pharmaceutical is then passed through the
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544:) will be present mainly in their non-ionic form, and
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563:environment of the intestines—weak bases (such as
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440:is also used to control solubility. For example,
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16:Movement of a drug into the bloodstream or lymph
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1057:. Hoboken, N.J: Wiley-Interscience/J. Wiley.
985:Pharmaceutical Science & Technology Today
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823:Kaplan Pharmacology 2010, page 6, Absorption
230:The rate of dissolution is described by the
155:). Absorption by some other routes, such as
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628:. Unsourced material may be challenged and
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801:"Drug Absorption - Clinical Pharmacology"
648:Learn how and when to remove this message
464:these esters to release the parent drug.
396:is the concentration of the solid in the
109:Learn how and when to remove this message
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448:of drugs have decreased solubility in
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1020:Pharmacology: Principles and Practice
979:Curatolo, William (1 December 1998).
937:
890:
870:"Medication Routes of Administration"
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897:Current Medical Research and Opinion
626:adding citations to reliable sources
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559:However, the reverse is true in the
47:adding citations to reliable sources
18:
841:
13:
1893:Minimum bactericidal concentration
1041:
776:10.1016/b978-0-12-802447-8.00012-1
768:Developing Solid Oral Dosage Forms
743:10.1016/b978-0-12-386882-4.00017-7
14:
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1023:. Academic Press. pp. 212–.
182:Absorption is a primary focus in
1883:Minimum inhibitory concentration
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350:{\displaystyle {\frac {dW}{dt}}}
23:
1823:WHO list of essential medicines
1316:Non-specific effect of vaccines
1053:Absorption and Drug Development
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805:MSD Manual Professional Edition
34:needs additional citations for
1878:Antimicrobial pharmacodynamics
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861:
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770:. Elsevier. pp. 331–354.
737:. Elsevier. pp. 341–364.
534:Henderson-Hasselbalch equation
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58:"Absorption" pharmacology
1:
1803:Functional analog (chemistry)
997:10.1016/S1461-5347(98)00097-2
719:
709:Gastrointestinal transit time
488:
1356:Hill equation (biochemistry)
400:layer surrounding the solid.
7:
868:Jean, Kim; Orlando, Jesus.
702:
357:is the rate of dissolution.
10:
1944:
1871:Antimicrobial pharmacology
1351:Dose–response relationship
1281:Desensitization (medicine)
844:"Routes of administration"
799:LE.JENNIFER (2020-03-27).
1793:Coinduction (anesthetics)
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127:The drug travels by some
1858:Multiple drug resistance
1831:Tolerance and resistance
1199:Physiological antagonist
991:(9). Elsevier: 387–393.
909:10.1185/030079907x182095
663:
1609:Neuropsychopharmacology
1371:Cheng-Prussoff Equation
1366:Del Castillo Katz model
1293:Other effects of ligand
1276:Receptor (biochemistry)
1194:Irreversible antagonist
696:intramuscular injection
515:semipermeable membranes
161:intramuscular injection
129:route of administration
1745:Classical pharmacology
1506:Plasma protein binding
1481:Volume of distribution
1189:Competitive antagonist
692:subcutaneous injection
583:properties of a drug.
495:gastrointestinal tract
458:gastrointestinal tract
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232:Noyes–Whitney equation
1853:Antibiotic resistance
1645:Clinical pharmacology
1164:Physiological agonist
1124:Ligand (biochemistry)
1049:Avdeef, Alex (2003).
938:Mayor, Susan (2017).
891:Ermer, James (2007).
874:StatPearls Publishing
674:intravenous injection
471:only dissolve in the
460:(GIT) wall and blood
424:specific surface area
391:
389:{\displaystyle C_{s}}
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1750:Reverse pharmacology
1660:Pharmacoepidemiology
1501:Biological half-life
1381:Ligand binding assay
1255:Activity at receptor
1149:Irreversible agonist
851:The Laboratory Mouse
681:intravenous infusion
622:improve this section
527:phospholipid bilayer
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171:is often near 100%.
139:, etc.) in a chosen
43:improve this article
1798:Combination therapy
1686:Pharmacoinformatics
1655:Medicinal chemistry
1261:Mechanism of action
1080:Absorption of Drugs
688:oral administration
475:environment of the
403:D is the diffusion
188:medicinal chemistry
157:intravenous therapy
1768:Immunopharmacology
1718:Pharmacotoxicology
1619:Psychopharmacology
1411:Intrinsic activity
1311:Pleiotropy (drugs)
1232:Agonist-antagonist
1144:Endogenous agonist
714:Flip–flop kinetics
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842:Shimizu, Shinya.
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32:This article
30:
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1923:Pharmacology
1813:Chemotherapy
1773:Cell biology
1674:Biochemistry
1598:Neuroscience
1546:Distribution
1540:
1476:Loading dose
1159:Superagonist
1116:Pharmacology
1052:
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41:Please help
36:verification
33:
1898:Bactericide
1574:Compartment
1385:Patch clamp
1361:Schild plot
513:which form
503:bloodstream
405:coefficient
194:Dissolution
141:dosage form
1917:Categories
1778:Physiology
1710:Toxicology
1602:psychology
1551:Metabolism
1541:Absorption
1535:Liberation
1377:Organ bath
1305:Functional
1184:Antagonist
1177:Inhibitory
1132:Excitatory
944:Prescriber
880:: 121–141.
857:: 527–543.
810:2020-03-28
720:References
546:weak bases
538:weak acids
489:Ionization
477:intestines
414:thickness.
224:compliance
177:inhalation
122:Absorption
69:newspapers
1560:Clearance
1556:Excretion
1375:Methods (
638:July 2021
609:does not
540:(such as
462:hydrolyze
454:esterases
452:. Later,
431:polymorph
410:L is the
398:diffusion
360:A is the
290:−
200:esophagus
99:June 2018
1678:genetics
1650:Pharmacy
1637:Medicine
1447:Affinity
1406:Efficacy
1344:Analysis
1326:Toxicity
966:79073985
925:22893348
917:17519073
703:See also
576:prodrugs
565:caffeine
442:stearate
208:GI tract
153:solution
151:, or in
149:capsules
1588:Related
1531:(L)ADME
1485:Initial
1469:Metrics
1416:Potency
1399:Metrics
1301:Binding
1271:Binding
1139:Agonist
1002:21 July
630:removed
615:sources
554:stomach
542:aspirin
519:ionized
456:in the
317:Where:
216:kidneys
204:stomach
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145:tablets
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1787:Other
1524:LADME
962:S2CID
921:S2CID
847:(PDF)
664:Types
561:basic
473:basic
212:liver
90:JSTOR
76:books
1676:and
1600:and
1436:TD50
1432:LD50
1428:ED50
1424:IC50
1420:EC50
1222:Drug
1059:ISBN
1025:ISBN
1004:2021
913:PMID
780:ISBN
747:ISBN
613:any
611:cite
532:The
493:The
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186:and
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