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Absorption (pharmacology)

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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
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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
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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
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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.
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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.
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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
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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,
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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
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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
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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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will be in their ionic form. Since non-ionic species diffuse more readily through
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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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Types of absorption in pharmacokinetics include the following:
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Kaplan Pharmacology 2010, Video Lectures, Absorption chapter
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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 1672: 1830: 1292: 544:) will be present mainly in their non-ionic form, and 375: 326: 243: 735:
Handbook of Pharmacogenomics and Stratified Medicine
1254: 49:. Unsourced material may be challenged and removed. 1050: 563:environment of the intestines—weak bases (such as 388: 349: 306: 440:is also used to control solubility. For example, 1914: 1010: 16:Movement of a drug into the bloodstream or lymph 792: 1735: 1100: 1057:. Hoboken, N.J: Wiley-Interscience/J. Wiley. 985:Pharmaceutical Science & Technology Today 765: 1048: 823:Kaplan Pharmacology 2010, page 6, Absorption 230:The rate of dissolution is described by the 155:). Absorption by some other routes, such as 798: 628:. Unsourced material may be challenged and 1107: 1093: 1708: 1176: 1131: 955: 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 978: 1635: 1343: 867: 1915: 1468: 1398: 448:of drugs have decreased solubility in 1088: 1020:Pharmacology: Principles and Practice 979:Curatolo, William (1 December 1998). 937: 890: 870:"Medication Routes of Administration" 1523: 897:Current Medical Research and Opinion 626:adding citations to reliable sources 593: 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: 1939: 1073: 1023:. Academic Press. pp. 212–. 182:Absorption is a primary focus in 1883:Minimum inhibitory concentration 1114: 598: 589: 350:{\displaystyle {\frac {dW}{dt}}} 23: 1823:WHO list of essential medicines 1316:Non-specific effect of vaccines 1053:Absorption and Drug Development 972: 805:MSD Manual Professional Edition 34:needs additional citations for 1878:Antimicrobial pharmacodynamics 931: 884: 861: 835: 826: 817: 770:. Elsevier. pp. 331–354. 737:. Elsevier. pp. 341–364. 534:Henderson-Hasselbalch equation 295: 276: 193: 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) 1786: 1587: 1459: 1245: 1122: 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 390: 351: 308: 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}} 352: 309: 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 373: 324: 241: 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 386: 347: 304: 1910: 1909: 1906: 1905: 1866: 1865: 1763:Photopharmacology 1758: 1757: 1731: 1730: 1704: 1703: 1668: 1667: 1631: 1630: 1624:Electrophysiology 1614:Neuropharmacology 1569: 1568: 1519: 1518: 1455: 1454: 1442:Therapeutic index 1394: 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1346: 1342: 1331: 1330:Neurotoxicity 1327: 1324: 1322: 1319: 1317: 1314: 1312: 1309: 1306: 1302: 1299:Selectivity ( 1298: 1297: 1295: 1291: 1282: 1279: 1277: 1274: 1272: 1269: 1267: 1264: 1262: 1259: 1257: 1253: 1250: 1248: 1244: 1238: 1237:Pharmacophore 1235: 1233: 1230: 1228: 1225: 1223: 1220: 1219: 1210: 1207: 1205: 1202: 1200: 1197: 1195: 1192: 1190: 1187: 1185: 1182: 1181: 1179: 1175: 1165: 1162: 1160: 1157: 1155: 1152: 1150: 1147: 1145: 1142: 1140: 1137: 1136: 1134: 1130: 1127: 1125: 1121: 1117: 1110: 1105: 1103: 1098: 1096: 1091: 1090: 1087: 1081: 1078: 1077: 1066: 1064:0-471-42365-3 1060: 1055: 1054: 1047: 1046: 1032: 1026: 1022: 1021: 1013: 998: 994: 990: 986: 982: 975: 967: 963: 958: 953: 949: 945: 941: 934: 926: 922: 918: 914: 910: 906: 902: 898: 894: 887: 879: 875: 871: 864: 856: 852: 845: 838: 829: 820: 806: 802: 795: 787: 781: 777: 773: 769: 762: 754: 748: 744: 740: 736: 729: 725: 715: 712: 710: 707: 706: 697: 693: 689: 685: 682: 678: 675: 671: 670: 669: 661: 652: 649: 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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 202:to the 145:tablets 143:(e.g., 83:scholar 1590:fields 1061:  1027:  964:  923:  915:  782:  749:  694:, and 572:analog 446:esters 85:  78:  71:  64:  56:  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 214:and 186:and 133:oral 62:news 1533:: ( 993:doi 952:doi 905:doi 772:doi 739:doi 624:by 505:. 45:by 1919:: 1434:, 1430:, 1426:, 1422:, 1383:, 1379:, 1303:, 987:. 983:. 960:. 948:28 946:. 942:. 919:. 911:. 901:23 899:. 895:. 876:. 872:. 853:. 849:. 803:. 778:. 745:. 690:, 556:. 479:. 218:. 179:. 163:, 159:, 147:, 135:, 1562:) 1558:( 1537:) 1487:) 1483:( 1438:) 1418:( 1387:) 1332:) 1328:( 1307:) 1108:e 1101:t 1094:v 1067:. 1033:. 1006:. 995:: 989:1 968:. 954:: 927:. 907:: 878:1 855:1 813:. 788:. 774:: 755:. 741:: 698:. 683:. 676:. 651:) 645:( 640:) 636:( 632:. 618:. 407:. 382:s 378:C 342:t 339:d 334:W 331:d 300:L 296:) 293:C 285:s 281:C 277:( 274:A 271:D 265:= 259:t 256:d 251:W 248:d 131:( 112:) 106:( 101:) 97:( 87:· 80:· 73:· 66:· 39:.

Index


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"Absorption" pharmacology
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scholar
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route of administration
oral
topical-dermal
dosage form
tablets
capsules
solution
intravenous therapy
intramuscular injection
enteral nutrition
bioavailability
Intravascular
inhalation
drug development
medicinal chemistry
esophagus
stomach
GI tract
liver

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