Preclinical safety pharmacological studies on the amorphous formulation of celecoxib

Arzneimittel-Forschung/Drug Research

Volumn 59, Issue 5, 2009, Pages 254-262

  Sharma, Shyam Sunder ^a   Srinivasan, Sathish Kumar ^a   Krishnamoorthy, Srinivasan ^a   Kaushal, Aditya Mohan ^a   Bansal, Arvind Kumar ^a  

^a NATIONAL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RESEARCH NIPER   (India)

Author keywords

CAS 169590 42 5; Celecoxib, amorphous formulation; Core battery safety pharmacology; COX 2 inhibitors; Functional observation battery; Non steroidal anti inflammatory drugs

Indexed keywords

CELECOXIB;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BLOOD PRESSURE MONITORING; CONTROLLED STUDY; DRUG DOSAGE FORM COMPARISON; DRUG DOSE COMPARISON; DRUG FORMULATION; DRUG MEGADOSE; DRUG SAFETY; FUNCTIONAL ASSESSMENT; HEART ARRHYTHMIA; HEART RATE; LOCOMOTION; MALE; MAXIMUM TOLERATED DOSE; MOTOR COORDINATION; NONHUMAN; QT INTERVAL; QT PROLONGATION; RAT; REPEATED DRUG DOSE; RISK ASSESSMENT; SINGLE DRUG DOSE; STOMACH INJURY; STOMACH SECRETION;

EID: 67149111789     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1296394     Document Type: Article

References (29)

1. Frampton JE, Keating GM. Celecoxib: a review of its use in the management of arthritis and acute pain. Drugs 2007;67:2433-2472. (Pubitemid 350080285)
2. Barden J, Edwards JE, McQuay HJ, Moore RA. Single dose oral celecoxib for postoperative pain. Cochrane Database Syst Rev. 2008;CD004233:1-11.
3. Arber N, Eagle CJ, Spicak J, Racz I, Dite P, Hajer J et al . Celecoxib for the prevention of colorectal adenomatous polyps. N Engl J Med. 2006;355:885-895. (Pubitemid 44315981)
4. Paulson SK, Vaughn MB, Jessen SM, Lawal Y, Gresk CJ, Yan B et al . Pharmacokinetics of celecoxib after oral administration in dogs and humans: effect of food and site of absorption. J Pharmacol Exp Ther. 2001;297:638-645. (Pubitemid 32377995)
5. Hancock BC, Parks M. What is the true solubility advantage for amorphous pharmaceuticals? Pharm Res. 2000;17:397-404.
6. Bansal AK, Gupta P, Kakumanu VK. Ternary amorphous systems for improving aqueous solubility of poorly water soluble drugs. Indian Pat. Appl. 2008. IN 2002DE00682.1-10.
7. Gupta P, Bansal AK. Oral bioavailability advantage from stabilized amorphous systems of celecoxib. J Pharm Res. 2006;5:1-9.
8. Andersohn F, Suissa S, Garbe E. Use of first- and second-generation cyclooxygenase-2-selective nonsteroidal antiinflammatory drugs and risk of acute myocardial infarction. Circulation. 2006;113:1950-1957. (Pubitemid 43754197)
9. Solomon SD, McMurray JV, Pfeffer MA, Wittes J, Fowler R, Finn P et al . Cardiovascular risk associated with celecoxib in a clinical trial for colorectal adenoma prevention. N Engl J Med. 2005;352:1071-1080. (Pubitemid 40365348)
10. Silverstein FE, Faich G, Goldstein JL, Simon LS, Pincus T, Whelton A et al . Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: a randomized controlled trial. JAMA. 2000;284:1247-1255. (Pubitemid 30691365)
11. Center for Drug Evaluation and Research (CDER), US FDA. Guidance for industry: S7A safety pharmacology studies for human pharmaceuticals. July 2001. Available at http://www.fda.gov/CDER/GUIDANCE/4461fnl.pdf
12. Hübler N, Gottschling B, Jacobs M, von Landenberg F, Hewicker-Trautwein M. Functional observational battery and motor activity in rats after single administration of two NHE 1 inhibitors. Toxicol Appl Pharmacol. 2005;208:266-276. (Pubitemid 41457228)
13. Moser VC. Neurobehavioral screening in rodents. Mahin M, Costa LG, Reed DJ, Shigeru SI, Glenn S, eds. Curr Protoc Toxicol. New Jersey: John Wiley & Sons, Inc; 2000.
14. Gupta S, Sharma SS. Neuroprotective effects of trolox in global cerebral ischemia in gerbils. Biol Pharm Bull. 2006;29:957-961.
15. Kim EJ, Lee RK, Suh JE, Han SS, Kim JK. Safety pharmacology of CKD-602, a novel anticancer agent. Arzneimittelforschung. 2003;53:272-279. (Pubitemid 36535383)
16. Arun KHS, Kaul CL, Ramarao P. AT1 receptors and L-type calcium channels: functional coupling in supersensitivity to angiotensin II in diabetic rats. Cardiovasc Res. 2005;65:374-386. (Pubitemid 40082479)
17. Hamlin RL, Kijtawornrat A, Keene BW, Hamlin DM. QT and RR intervals in conscious and anesthetized guinea pigs with highly varying RR intervals and given QTc-lengthening test articles. Toxicol Sci . 2003;76:437-442. (Pubitemid 38035437)
18. Hamlin RL. Non-drug-related electrocardiographic features in animal models in safety pharmacology. J Pharmacol Toxicol Methods . 2005;52:60-76. (Pubitemid 41008630)
19. Luo JC, Shin VY, Liu ESL, So WHL, Ye YN, Chang FY et al. Non-ulcerogenic dose of dexamethasone delays gastric ulcer healing in rats. J Pharmacol Exp Ther . 2003;307:692-698. (Pubitemid 37310685)
20. Ito K, Kinoshita K, Tomizawa A, Inaba F, Morikawa-Inomata Y, Makino M et al . Pharmacological profile of novel acid pump antagonist 7-(4-Fluorobenzyloxy) -2,3-dimethyl-1-{[(1S,2S)-2-methyl cyclopropyl]methyl}-1H-pyrrolo[2,3-d]- pyridazine (CS-526). J Pharmacol Exp Ther. 2007;323:308-317. (Pubitemid 47443260)
21. Arisawa H, Fukui K, Imai E, Fujise N, Masunaga H. General pharmacological profile of the novel muscarinic receptor agonist SNI-2011, a drug for xerostomia in Sjogren's syndrome. 4th communication: effects on gastrointestinal, urinary and reproductive systems and other effects. Arzneimittelforschung. 2002;52:225-232.
22. Center for Drug Evaluation and Research (CDER), US FDA. Guidance for industry: S7B nonclinical evaluation of the potential for delayed ventricular repolarization (QT interval prolongation) by human pharmaceuticals. Rockville, October 2005. Available at http://www.fda.gov/CDER/GUIDANCE/6885fnl.pdf.
23. Monro A, Mordenti J. Expression of exposure in negative carcinogenicity studies: dose/body weight, dose/body surface area, or plasma concentrations? Toxicol Pathol. 1995;23:187-198.
24. Voisin EM, Ruthsatz M, Collins JM, Hoyle PC. Extrapolation of animal toxicity to humans: interspecies comparisons in drug development. Regul Toxicol Pharmacol. 1990;12:107-116. (Pubitemid 20337293)
25. Sakaguchi Y, Sugiyama A, Takao S, Akie Y, Takahara A, Hashimoto K. Halothane sensitizes the guinea-pig heart to pharmacological IKr blockade: comparison with urethane anesthesia. J Pharmacol Sci . 2005;99:185-190. (Pubitemid 41524457)
26. + channel blocker-induced QT-interval prolongation. Biol PharmBull. 2006;29:827-829.
27. Netzer R, Ebneth A, Bischoff U, Pongs O. Screening lead compounds for QT interval prolongation. Drug Discov Today. 2001;6:78-84. (Pubitemid 32101509)
28. Peskar B. Role of cyclooxygenase isoforms in gastric mucosal defense and ulcer healing. Inflammopharmacology . 2005;13:15-26. (Pubitemid 41607366)
29. Takahashi S, Shigeta J, Inoue H, Tanabe T, Okabe S. Localization of cyclooxygenase-2 and regulation of its mRNA expression in gastric ulcers in rats. Am J Physiol Gastrointest Liver Physiol. 1998;275:G1137-1145. (Pubitemid 28538968)