Pharmacokinetics of gabapentin in a novel gastric-retentive extended-release formulation: Comparison with an immediate-release formulation and effect of dose escalation and food

Journal of Clinical Pharmacology

Volumn 51, Issue 3, 2011, Pages 346-358

  Chen, Cuiping ^a   Cowles, Verne E ^a   Hou, Eddie ^b  

^a Pharmacokinetics Depomed Inc   (United States)

^b NONE

Author keywords

dose proportionality; extended release; food effect; gabapentin; gastric retentive; Pharmacokinetics

Indexed keywords

GABAPENTIN;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DIZZINESS; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSAGE FORM COMPARISON; DRUG DOSE ESCALATION; DRUG FATALITY; DRUG FORMULATION; DRUG RELEASE; DRUG TOLERABILITY; EXTENDED DRUG RELEASE; FAT CONTENT; FEMALE; FOOD; FOOD DRUG INTERACTION; HUMAN; HUMAN EXPERIMENT; IMMEDIATE DRUG RELEASE; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PHASE 1 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL; SOMNOLENCE; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADULT; AMINES; ANALGESICS, NON-NARCOTIC; ANTICONVULSANTS; BIOLOGICAL AVAILABILITY; CALCIUM CHANNEL BLOCKERS; CROSS-OVER STUDIES; CYCLOHEXANECARBOXYLIC ACIDS; DELAYED-ACTION PREPARATIONS; DIETARY FATS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; FOOD-DRUG INTERACTIONS; GAMMA-AMINOBUTYRIC ACID; GASTRIC EMPTYING; HALF-LIFE; HUMANS; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; STOMACH; YOUNG ADULT;

EID: 79953826630     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270010368411     Document Type: Article

References (28)

1. Kong VK, Irwin MG. Gabapentin: a multimodal preoperative drug? Br J Anaesth. 2007;99:775-786.
2. Nicholson B. Gabapentin use in neuropathic pain syndromes. Acta Neurol Scand. 2000;101:359-371. (Pubitemid 30337416)
3. Curran MP, Wagstaff AJ. Gabapentin: in postherpetic neuralgia. CNS Drugs. 2003;17:975-982. (Pubitemid 37410071)
4. Hwang JH, Yaksh TL. Effect of subarachnoid gabapentin on tactile-evoked allodynia in a surgically induced neuropathic pain model in the rat. Reg Anesth. 1997;22:249-256. (Pubitemid 27217143)
5. Gee NS, Brown JP, Dissanayake VU, Offord J, Thurlow R, Woodruff GN. The novel anticonvulsant drug, gabapentin (Neurontin), binds to the alpha2delta subunit of a calcium channel. J Biol Chem. 1996;271:5768-5776. (Pubitemid 26083915)
6. Alden KJ, Garcia J. Differential effect of gabapentin on neuronal and muscle calcium currents. J Pharmacol Exp Ther. 2001;297:727-735. (Pubitemid 32378006)
7. Neurontin [package insert]. New York, NY: Parke-Davis, Division of Pfizer; April 2009.
8. Rowbotham M, Harden N, Stacey B, Bernstein P, Magnus-Miller L. Gabapentin for the treatment of postherpetic neuralgia: a randomized controlled trial. JAMA. 1998;280:1837-1842. (Pubitemid 28544424)
9. Rice ASC, Maton S; Postherpetic Neuralgia Study Group. Gabapentin in postherpetic neuralgia: a randomized, double blind, placebo controlled study. Pain. 2001;94:215-224.
10. McLean MJ. Clinical pharmacokinetics of gabapentin. Neurol. 1994;44:S17-S22.
11. Boyd RA, Türck D, Abel RB, Sedman AJ, Bockbrader HN. Effects of age and gender on single dose pharmacokinetics of gabapentin. Epilepsia. 1999;40:474-479. (Pubitemid 29164860)
12. Bockbrader HN. Clinical pharmacokinetics of gabapentin. Drugs Today. 1995;31:613-619. (Pubitemid 26048983)
13. Stewart BH, Kugler AR, Thompson PR, Bockbrader HN. A saturable transport mechanism in the intestinal absorption of gabapentin is the underlying cause of the lack of proportionality between increasing dose and drug levels in plasma. Pharm Res. 1993;10:276-281. (Pubitemid 23041744)
14. Parsons B, Tive L, Huang S. Gabapentin: a pooled analysis of adverse events from three clinical trials in patients with postherpetic neuralgia. Am J Geriatr Pharmacother. 2004;2:157-162. (Pubitemid 39618440)
15. Cundy KC, Sastry S, Luo W, Zou J, Moors TL, Canafax DM. Clinical pharmacokinetics of XP13512, a novel transported prodrug of gabapentin. J Clin Pharmacol. 2008;48:1378-1388.
16. Hou SYE, Cowles VE, Berner B. Gastric retentive dosage forms: a review. Crit Rev Ther Drug Carrier Syst. 2003;20:459-497.
17. Cowles VE, Gusler G, Chen TF, et al. Gastric emptying and intestinal transit of gastroretentive tablets in the fed state: effect of meal content and tablet size. Gastroenterol. 2004;126:A489-A490.
18. Shojaei AH, Berner B. Gastric retentive dosage forms. In: Li X, Jasti B, eds. Design of Controlled Release Drug Delivery Systems, New York, NY: McGraw-Hill; 2005;175-203.
19. Berner B, Cowles V. Case studies in swelling polymeric gastric retentive tablets. Expert Opin Drug Deliv. 2006;3:541-548.
20. Keats TE, Sistrom C. Gastrointestinal system. In: Atlas of Radiologic Measurement. St Louis, Mo: Mosby; 2001:400-403.
21. Chien YW. Oral drug delivery and delivery systems. In: Novel Drug Delivery Systems. New York, NY: Marcel Dekker; 1992:159-163.
22. Smith BP, Vandenhence FR, DeSante KA, et al. Confidence interval criteria for assessment of dose proportionality. Pharm Res. 2000;17:1278-1283.
23. Gusler GM, Hou E, Berner B, et al. Single dose pharmacokinetics of gabapentin gastric retentive (GR) tablets in healthy volunteers. Paper presented at: Controlled Release Society 31st Annual Meeting; June 12-16, 2004; Honolulu, HI.Abstract 54.
24. Gu R, Gusler GM, Hou E, et al. Extended release and dose proportionality of a novel gabapentin formulation. Paper presented at: Endocrine Society 88th Annual Meeting; June 24-26, 2006; Boston, Mass. Abstract 1194.
25. Gordi T, Savic R, Hou E, Karlsson MO, Berner B. A mechanistic model for gabapentin pharmacokinetics after immediate release and extended release formulations. AAPS J. 2006;S2:8.
26. Gordi T, Hou E, Berner B. Effect of food on the bioavailability of gabapentin delivered from extended release tablets. Paper presented at: Endocrine Society 89th Annual Meeting; June 2-5, 2007; Toronto, Canada. Abstract P4-152.
27. Vollmer KO, Turck D, Bockbrader HN, et al. Summary of Neurontin (gabapentin) clinical pharmacokinetics (abstract). Epilepsia. 1992;33(suppl 3):77.
28. Gordi T, Hou E, Sreeneeranj K, Berner B. Pharmacokinetics of gabapentin after a single day and at steady state following the administration of gastric-retentive-extended-release and immediate-release tablets: a randomized, open-label, multiple-dose, three-way crossover, exploratory study in healthy subjects. Clin Ther. 2008;30:909-916. (Pubitemid 351799872)