Techniques for measuring gastrointestinal pH and transit, and their application in drug development

International Journal of Pharmaceutical Medicine

Volumn 13, Issue 3, 1999, Pages 147-154

  Zimmermann, T ^a   Laufen, H ^a   Yeates, R A ^a   Lammerich, A ^a   Wildfeuer, A ^a  

^a PFIZER INC   (United States)

Author keywords

Drug absorption; Gastrointestinal pH; Gastrointestinal transit time; Measurement techniques; Pharmaceutical development

Indexed keywords

ANTIBIOTIC AGENT; DILTIAZEM; FLUCONAZOLE; ISOSORBIDE 5 NITRATE; ITRACONAZOLE; OMEPRAZOLE; PARACETAMOL; PYRIDINE DERIVATIVE; SALIZYLAZOSULFAPYRIDINE; UNCLASSIFIED DRUG;

ARTICLE; DIGESTIVE SYSTEM PERFORATION; DIGESTIVE TRACT INTUBATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DEVELOPMENT; DRUG FORMULATION; GASTROINTESTINAL ABSORPTION; GASTROINTESTINAL TRANSIT; HUMAN; HUMAN EXPERIMENT; HYDROGEN BREATH TEST; MAJOR CLINICAL STUDY; NORMAL HUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; STOMACH EMPTYING; STOMACH PH;

EID: 0032800251     PISSN: 13649027     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (60)

1. 1. Hebbard GS, Sun WM, Bochner F, Morowitz M. Pharmacokinetic considerations in gastrointestinal motor disorders. Clin Pharmacokinet 1995; 28:41-66.
2. 2. Macheras P, Argyrakis P. Gastrointestinal drug absorption: is it time to consider heterogeneity as well as homogeneity? Pharm Res 1997; 14:842-847.
3. 3. Möller H. Gastro-intestinal absorption and transport kinetics. In: Gundert R, Möller H editors. Oral controlled release products. Therapeutic and biopharmaceutic assessment, Vol. 22. Stuttgart: Wissenschaftl, 1990.
4. 4. Wilding IR, Davis SS, Pozzi F, Furlani P, Gazzaniga A. Enteric coated timed release systems for colonic targeting. Int J Pharm 1994; 111:99-102.
5. 5. Breimer DD. An integrated pharmacokinetic and pharmacodynamic approach to controlled drug delivery. J Drug Target 1996; 3:411-415.
6. 6. Swenson ES, Curatolo WJ. Intestinal permeability enhancement for proteins, peptides and other polar drugs: mechanisms and potential toxicity. Adv Drug Deliv Rev 1992; 8:39-92.
7. 7. Tsuji A, Tamai J. Carrier-mediated intestinal transport of drugs. Pharm Res 1996; 13:963-977.
8. 8. Connell AM, Waters TE. Assessment of gastric function by pH telemetering capsule. Lancet 1964; 227-230.
9. 9. Yarbrough DR, McAlhany JC, Cooper N, Weidner MG. Evaluation of the Heidelberg pH capsule. Method of tubeless gastric analysis. Am J Surg 1969; 117:185-192.
10. 10. Emde C, Garner A, Blum A. Technical aspects of intraluminal pH-metry in man: current status and recommendations. Gut 1987; 28:1177-1188.
11. 11. Evans DF, Pye G, Bramley R, Clark AG, Dyson TJ, Hardcastle JD. Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut 1988; 29:1035-1043.
12. 12. Zimmermann T, Leitold M. The influence of food intake on gastrointestinal pH and gastric emptying time. Int J Clin Pharmacol Ther 1992; 30:477-478.
13. 13. Ewe K, Press AG, Dederer W. Gastrointestinal transit of undigestible solids measured by metal detector EASII. Eur J Clin Invest 1989; 19:291-297.
14. 14. Ewe K, Press AG, Bollen S, Schuhn I. Gastric emptying of indigestible tablets in relation to composition and time of ingestion of meals studied by metal detector. Digest Dis Sci 1991; 36:146-152.
15. 15. Ewe K, Ueberschaer B, Press AG, Kurrek C, Klump M. Effect of lactose, lactulose and bisacodyl on gastrointestinal transit studied by metal detector. Aliment Pharmacol Ther 1995; 9:69-73.
16. 16. Read NW, Miles CA, Fisher D, Holgate AM, Kime ND, Mitchell MA et al. Transit of a meal through the stomach, small intestine, and colon in normal subjects and its role in the pathogenesis of diarrhea. Gastroenterol 1980; 79:1276-1282.
17. 2) measurements. J Lab Clin Med 1975; 85:546-555.
18. 18. Sciarretta G, Furno A, Mazzoni M, Gagagnani B, Malaguti P. Lactulose hydrogen breath test in orocecal transit assessment. Critical evaluation by means of scintigraphic method. Digest Dis Sci 1994, 39:1505-1510.
19. 19. Heading RC, Nimmo J, Prescott LF, Tothill P. The dependence of paracetamol absorption on the rate of gastric emptying. Br J Pharmacol 1973; 47:415-421.
20. 20. Petring OU, Flachs H. Inter-and intrasubject variability of gastric emptying in healthy volunteers measured by scintigraphy and paracetamol absorption. Br J Clin Pharmacol 1990; 29:703-708.
21. 21. Kennedy M, Chinwah P, Wade DN. A pharmacological method of measuring mouth caecal transit time in man. Br J Clin Pharmacol 1979; 8:372-373.
22. 22. Staniforth DH. Comparison of orocaecal transit times assessed by the lactulose/breath hydrogen and the sulphasalazine/sulphapyridine methods. Gut 1989; 30:978-982.
23. 23. Kerlin P, Tucker R, Phillips SF. Rapid intubation of the ileo-colonic region of man. Aust NZ J Med 1983; 13:591-593.
24. 24. Gleiter CH, Antonin KH, Bieck P, Godbillon J, Schönleber W, Malchow H. Colonoscopy in the investigation of drug absorption in healthy volunteers. Gastrointest Endoscopy 1985; 31:71-73.
25. 25. Schuster O, Hugemann B. Course of development of the HF-capsule -variations and method-related typical findings. Meth Clin Pharmacol 1987; 7:28-32.
26. 26. Fordtran JS, Rector FC, Ewton MF, Soter N, Kinney J. Permeability characteristics of the human small intestine. J Clin Invest 1965; 44:1935-1944.
27. 27. Cooper HC, Levitan R, Fordtran JS, Ingelfinger FJ. A method for studying absorption of water and solute from the human small intestine. Gastroenterol 1966; 50:1-7.
28. 28. Whalen GE, Harris JA, Geenen JE, Soergel KH. Sodium and water absorption from the human small intestine. The accuracy of the perfusion method. Gastroenterol 1966; 51:975-984.
29. 29. Modigliani R, Rambaud JC, Berner JJ. The method of intraluminal perfusion of the human small intestine. Digestion 1973; 9:176-192.
30. 30. Parsons RL. Drug absorption in gastrointestinal disease. Clin Pharmacokinet 1977; 2:45-60.
31. 31. Wacher VJ, Wu C-Y, Banet LZ. Overlapping substrate specifities and tissue distribution of cytochrom P450 3A and ρ-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Molecul Carcinogen 1995; 13:129-134.
32. 32. Benet LZ, Wu C-Y, Hebert MF, Wacher VJ. Intestinal drug metabolism and antitransport processes: A potential paradigm shift in oral drug delivery. J Contr Rel 1996; 39:139-143.
33. 33. Lennernäs H. Human intestinal permeability. J Pharm Sci 1998; 87:403-410.
34. 34. Russel TL, Berardi RR, Barnett JL, Dermentzoglou LC, Jarvenpea KM, Schmaltz SP, et al. Upper gastrointestinal pH in seventy-nine healthy, elderly, North American men and women. Pharm Res 1993; 10:187-196.
35. 35. Dressman JB, Bass P, Rithschel WA, Friend DR, Rubinstein A. Gastrointestinal parameters that influence oral medications. E Ziv Pharma Sci 1993; 82:857-872.
36. 36. Zimmermann T, Yeates RA, Riedel KD, Lach P, Laufen H. The influence of gastric pH on the oral pharmacokinetics of fluconazole: The effect of omeprazole. Int J Clin Pharmacol Therap 1994; 32:491-496.
37. 37. Blum RA, D'Andrea DT, Florentino BM et al. Increased gastric pH and the bioavailability of fluconazole and ketoconazole. Ann Intern Med 1991; 114:755-757.
38. 38. Davis SS, Hardy JG, Fara JW. Transit of pharmaceutical dosage forms through the small intestine. Gut 1986; 27:886-892.
39. 39. Nimmo WS. Drugs, diseases and altered gastric emptying. Clin Pharmacokinet 1976; 1:189-203.
40. 40. BurksTF. Actions of pharmacological agents on gastrointestinal function. In: Kumar D, Gustavsson S editors. An illustrated guide to gastrointestinal motility. Chichester: John Wiley, 1988, pp. 272-289.
41. 41. Greiff JMC, Rowbotham D. Pharmacokinetic drug interactions with gastrointestinal motility modifying agents. Clin Pharmacokinet 1994; 27:447-461.
42. 42. Sanchez J, Martinez L, Garcia-Barbal J, Roser R, Bartlett A, Sagarra R. The influence of gastric emptying on droxicam pharmacokinetics. J Clin Pharmacol 1989; 29:739-745.
43. 43. Itoh Z, Aizawa I, Sekiguchi T. The interdigestive migration complex and its significance in man. Clin Gastroenterol 1982; 11:497-521.
44. 44. Mojaverian P, Ferguson RK, Vlasses PH, Rocci ML, Oren A, Fix JA et al. Estimation of gastric residence time of the Heidelberg capsule in humans: effect of varying food composition. Gastroenterol 1985; 89:392-397.
45. 45. Zimmermann T, Yeates RA, Laufen H, Pfaff G, Wildfeuer A. Influence of concomitant food intake on the oral absorption of two triazole antifungal agents, itraconazole and fluconazole. Eur J Clin Pharmacol 1994; 46:147-150.
46. 46. Elkind AH. Alternative delivery systems for management of migraine pain. Headache Quarterly 1993; 4(suppl 3): 14-16.
47. 47. Eadie MJ. Neurological diseases. In: Splight TM editor. Avery's drug treatment, 3rd ed. Auckland: Adis Press, 1987.
48. 48. Rao TRK, Naido MVR, Shooha JC, Sekhar KR, Rani PV, Sekhar EC. Effect of a single oral dose of sumatriptan on paracetamol pharmacokinetics. Clin Drug Invest 1995; 10:242-246.
49. 49. Wyman JB, Heaton KW, Manning AP, Wicks ACB. Variability of colonic function in healthy subjects. Gut 1978; 19:146-150.
50. 50. Atkin DA, Davis SS, Sparrow RA, Wilding IR. Colonic transit of different sized tablets in healthy subjects. J Contr Rel 1993; 23:147-156.
51. 51. Wilding IR. Pharmacoscintigraphic evaluation of oral delivery systems: Parts I and II. Pharm Tech Eur 1994; 19-26 and 32-38.
52. 52. Zimmermann T, Riedel KD, Laufen H. Gastrointestinal transit time measured by metal detector and pharmacokinetics of a controlled release dosage form of diltiazem [abstract]. Eur J Clin Pharmacol 1996; 50:557.
53. 53. Epstein M. Calcium antagonists and hypertension: evolving perspectives. Cardiovasc Rev Rep 1996; 17:30-42.
54. 54. Laufen H, Wildfeuer A. Absorption of isosorbide-5-nitrate from the gastrointestinal tract. Meth Clin Pharmacol 1987; 7:76-81.
55. 55. Gramatté T, El Desoky E, Klotz U. Site-dependent small intestinal absorption of ranitidine. Eur J Clin Pharmacol 1994; 46:253-259.
56. 56. Gramatté T, Oertel R, Terhaag B, Kirch W. Direct demonstration of small intestinal secretion and site-dependent absorption of the β-blocker talinolol in humans. Clin Pharmacol Ther 1996; 59: 541-549.
57. 57. Sörgel F, Naber KG, Jaehde U et al. Gastrointestinal secretion of ciprofloxacin. Am J Med 1989; 87:63S-65S.
58. 58. Griffiths NM, Hirst BH, Simmons NS. Active intestinal secretion of the fluoroquinolone antibacterials ciprofloxacin, norfloxacin and pefloxacin; a common secretory pathway? J Pharmacol Exp Ther 1994; 269:496-502.
59. 59. DeBoer AG, Moolenaar F, DeLeede LGJ, Breimer DP. Rectal drug administration: clinical pharmacokinetic considerations. Clin Pharmacokin 1982; 7:285-311.
60. 60. Pfaff G, Zimmermann T, Lach P, Yeates R, Simon G, Wildfeuer A. Pharmacokinetics and tolerance of fluconazole suppositories in healthy volunteers. Arzneim-Forsch/Drug Res 1993; 43:391-395.