Ibuprofen pharmacokinetics

Kearns GL, Murry DJ, Oermann C, Gaedigk A, Sock-nider M, Seilheimer DK et al. Ibuprofen pharmacokinetics in cystic fibrosis association with CYP2C9 genotype. Pediatr Pulmonol 1999 28 S19 208. 

Greenblatt, D.J. Arendt, R.M. Locniskar, A. Ibuprofen pharmacokinetics use of liquid chromatography with radial compression separation. Arzneimittelforschung, 1983, 33, 1671-1673... 

Stephenson DW, Small RE, Wood JH, Willis HE, Johnson SM Karnes HT, Rajasekharaiah K. Effect of ranitidine and cimetidine on ibuprofen pharmacokinetics. Clin Pharm (1988) 7, 317-21. 

Small RE, Wilmot-Pater MG, McGee BA, Willis HE, Effects of misoprostol or ranitidine on ibuprofen pharmacokinetics. Clin Pharm (1991) 10, 870-2. 

Ibuprofen. A study in 8 healthy subjects investigating the effects of diazepam on ibuprofen pharmacokinetics found that the ibuprofen half-life was increased from 2.39 to 3.59 hours and the clearance was reduced by about one-third when diazepam and ibuprofen were given at 10 pm, but no effect was seen with morning dosing. The clinical importance of this is uncertain. 

Wilson CG, Washington N, Greaves JL, Kamali F, Rees JA, Sempik AK, Lampard JF. Bimodal release of ibuprofen in a sustained-release formulation—a scintigraphic and pharmacokinetic open study in healthy volunteers under different conditions of food-intake. Int J Pharm 1989 50 155—161. 

The use of polymeric nanoparticles in the eye has gained considerable interests in recent years. Ocular disposition, safety, efficacy, and pharmacokinetic profiles of various nanoparticles offer a wide range of application for the delivery of many drugs used to treat common ocular disorders. Polymeric nanoparticles have been utilized to enhance the performance of ibuprofen and cyclosporine, while reducing systemic side effect of carteolol compared with... 

E. Samara, D. Avnir, D. Ladkani, M. Bialer, Pharmacokinetic Analysis of Diethyl-carbonate Prodrugs of Ibuprofen and Naproxen , Biopharm. Drug Dispos. 1995, 16, 201-210. 

Gillespie, W.R. and Veng-Pedersen, P., A polyexponential deconvolution method evaluation of the gastrointestinal bioavailability and mean in vivo dissolution time of some ibuprofen dosage forms, /. Pharmacokinet. Biopharm., 13, 289-307, 1985. 

Despite the problems posed by the pharmacokinetic and physicochemical characteristics of ibuprofen (small therapeutic window, erratic absorption owing to its poor solubility, etc.), this pulsed release system results in good separation of the two plasma peaks (indicating that there is in fact delayed release of the second drug dose) at the desired concentrations. 

Ibuprofen is a simple derivative of phenylpropionic acid (Figure 36-1). In doses of about 2400 mg daily, ibuprofen is equivalent to 4 g of aspirin in anti-inflammatory effect. Pharmacokinetic characteristics are given in Table 36-1. 

Davies, N. M. Clinical pharmacokinetics of ibuprofen. The first 30 years, Clin. Pharmacokinet. 1998a, 34, 101-154. 

In tables of pharmacokinetic data of drugs, one can readily find information on 11/2 and fmax for oral drugs. Although klih may not always be provided, klih can be determined from fi/2 and fmax. Ibuprofen (7.b) has a half-life of 2 h and t,llla of 1.6 h. Estimate the klih of ibuprofen. 

K. Walter, G. WeiB, A. Laicher, F. Stanislaus, Pharmacokinetics of ibuprofen following single administration of a suspension containing enteric-coated microcapsules, Drug Res 45 886-890 (1995). 

Bapuji AT, Rambhau D, Srinivasu P, Rao BR, Apte SS. Time dependent influence of diazepam on the pharmacokinetics of ibuprofen in man. Drug Metabol Drug Interact 1999 15(1) 71-81. 

This chapter concentrates on some drug choices in acute rather than chronic pain, but the same principles can be used to determine the appropriateness of other types of analgesic. The drugs considered in this section are paracetamol, non-steroidal anti-inflammatories (NSAIDs specifically diclofenac, ibuprofen, indometacin, naproxen, sulindac and tenoxicam) and opioids (codeine, dihydrocodeine, morphine, pethidine and tramadol). Unless otherwise stated, all pharmacokinetic data originate from standard reference sources [1-5] and apply to adults only. 

In a single-dose study examining the pharmacokinetics of sulindac and ibuprofen in 15 patients with alcoholic liver disease, no statistically significant effects were noted for ibuprofen elimination, half-life or AUC compared to the controls. However, there appeared to be delayed absorption in some patients [25]. 

Taking into account pharmacokinetics, adverse effects and clinical studies, ibuprofen may be considered the best choice in this patient, for the following reasons ... 

Li G, Treiber G, Maier K, et al. (1993) Disposition of ibuprofen in patients with liver cirrhosis. Clin Pharmacokinet 25 154-163. 

Aranda J, Varvarigou A, Beharry K, Bansal R, Bardin C, Modanlou H et al. Pharmacokinetics and protein binding of intravenous ibuprofen in premature newborn infant. Acta Paediatr 1997 86 289-93. 

F. Jamali, N. N. Singh, E M. Easutto, R. T. Courts, and A. S. Russell, "Pharmacokinetics of ibuprofen enantiomers in man following oral administration of tablets with different absorption rates," Pharm. Res., 5 40-43 (1988), R. T. Foster, E Jamali, A. S. Russell, and S. R. AlbeUa, "Pharmacokinetics of ketoprofen enantiomers in young and elderly arthritic patients following single and multiple doses," ]. Pharm. ScL, 77 191-195 (1988). 

E Jamali, R. Mehvar, A. S. Russell, S, Sattari, W. W. Yakimets, and J, Koo, "Human pharmacokinetics of ibuprofen enantiomers following different doses and formulations Intestinal chiral inversion,"/, Pharm. Sci., 81 221-225 (1991). 

For the clinical pharmacologist, neither of these racemic drug mixtures is problematic for drug therapy in the clinic if a pharmacodynamic endpoint (e.g., decrease in blood pressure with propranolol or improvement in arthritic pain with ibuprofen) is used to establish drug dose. However, to effectively characterize the pharmacokinetics of the active isomer, an endeavor that may be useful during drug development, administration, and/or specific determination of the active isomer is required. Such data... 

Saano, V. Paronen, P. Peura, P. Vidgen, M. Relative pharmacokinetics of three oral 400 mg ibuprofen dosage forms in healthy volunteers. Int. J. Clin. Pharmacol. Ther. Toxicol. 1991, 29 (10), 381-385. 

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