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Interactions during aqueous film coating of ibuprofen with aquacoat ECD.

Schmid S, Muller-Goymann CC, Schmidt PC.

Department of Pharmaceutical Technology, Eberhard-Karls-University Tubingen, Auf der Morgenstelle 8, 72076, Tubingen, Germany.

During the development of a coated ibuprofen formulation a sticking tendency occurred when applying Aquacoat ECD. This interaction indicated the formation of a eutectic mixture. The compatibility of the components of Aquacoat ECD with ibuprofen was investigated by differential scanning calorimetry. Cetyl alcohol, a stabilizing excipient in Aquacoat, was found to form a eutectic system with ibuprofen. It was characterized by the construction of a phase diagram with 33 mol% ibuprofen and an onset temperature of 40.5 degrees C. Wide-angle X-ray diffraction was used to identify the polymorphic forms of cetyl alcohol. The results confirmed the amorphous state in the aqueous dispersion in contrast to the beta(0)- and gamma(4)-polymorphs of solid cetyl alcohol.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10704791&dopt=Abstract ibuprofen Motrin



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Polyamidoamine Starburst dendrimers as solubility enhancers.

Milhem OM, Myles C, McKeown NB, Attwood D, D'Emanuele A.

School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Manchester, UK.

The solubility of the hydrophobic drug ibuprofen has been compared in an aqueous solution of polyamidoamine (PAMAM) G4 dendrimer and sodium dodecyl sulphate (SDS). The PAMAM G4 dendrimer solution significantly enhanced the solubility of ibuprofen compared to 2% SDS solution. It was found that the solubility of ibuprofen in dendrimer solution was directly proportional to dendrimer concentration and inversely proportional to temperature. The influence of dendrimer solution pH on the solubility enhancement of ibuprofen suggests that it involves an electrostatic interaction between the carboxyl group of the ibuprofen molecule and the amine groups of the dendrimer molecule.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10704811&dopt=Abstract ibuprofen Motrin



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Comparison of analgesic effects of khat (Catha edulis Forsk) extract, D-amphetamine and ibuprofen in mice.

Connor J, Makonnen E, Rostom A.

Department of Pharmacology, The Pennsylvania State University College of Medicine, Hershey 17033, USA.

We have compared the analgesic properties of khat (Catha edulis Forsk) extract, amphetamine and ibuprofen in mice. After intragastric administration of the drugs analgesia was measured relative to water-injected controls using the hot-plate, the tail-flick, and abdominal-constriction tests. At the highest doses examined (amphetamine 1.8 mg kg(-1), ibuprofen 90 mg kg(-1), khat extract 1800 mg kg(-1)), all three substances produced analgesia, but the order of efficacy varied with the test. Khat and ibuprofen were significantly different from the control in the hot-plate assay at three or more time points post-injection. In the tail-flick test, khat and amphetamine were efficacious; ibuprofen means were somewhat lower but still significantly different from control. Higher doses of the drugs decreased the number of responses in the acetic acid-induced abdominal-constriction assay. We conclude that khat, like amphetamine and ibuprofen, can relieve pain. Differences in assay results may reflect differences in modes and sites of action, as well as in the type of pain generated by the chemical and thermal stimuli for nociception.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10716611&dopt=Abstract ibuprofen Motrin



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Use of aspirin and ibuprofen compared with aspirin alone and the risk of myocardial infarction.

Patel TN, Goldberg KC.

Department of Internal Medicine, Duke University Medical Center, Durham, NC 27710, USA.

BACKGROUND: Laboratory investigations suggest that the simultaneous use of aspirin and ibuprofen may attenuate the antiplatelet effect of aspirin, making it less useful for cardioprotection. To determine if there is clinical evidence of this potentially harmful interaction, we conducted a retrospective matched case-control study. METHODS: All patients issued outpatient prescriptions for aspirin or ibuprofen from January 1, 1990, to December 31, 2000, at the Durham Veterans Affairs Medical Center pharmacy were included in the study. Patients who used aspirin and ibuprofen concurrently were matched against those who used aspirin only by race, sex, age within 10 years, and cholesterol levels (either low-density lipoprotein or total cholesterol) to within 30 mg/dL (0.78 mmol/L). The rate ratio of experiencing a myocardial infarction per patient-month of drug exposure was then determined. RESULTS: Some 3859 patients received both aspirin and ibuprofen, for a total of 52 139 patient-months of medication use. This group experienced 138 infarctions. The 10 239 patients receiving aspirin only, for a total of 156 417 patient-months of use, experienced 684 infarctions. The rate ratio of having an infarction was 0.61 (95% confidence interval, 0.50-0.73) (P <.001), favoring the group that took aspirin and ibuprofen simultaneously. An analysis of diabetic patients found a rate ratio of 0.48 (95% confidence interval, 0.34-0.66) (P <.001). An examination of patients who spent time in both groups at different times resulted in a rate ratio of infarction during combined use of 0.70 (95% confidence interval, 0.59-0.83) (P <.001). CONCLUSION: There does not seem to be an increased risk of myocardial infarction among patients simultaneously consuming aspirin and ibuprofen compared with aspirin alone.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=15111370&dopt=Abstract ibuprofen Motrin



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Ibuprofen modulates tissue perfusion in partial-thickness burns.

Barrow RE, Ramirez RJ, Zhang XJ.

Department of Surgery, University of Texas Medical Branch and Shriners Hospitals for Children, 815 Market Street, Galveston 77550, USA.

INTRODUCTION: The anti-inflammatory and anticoagulant effects of ibuprofen and heparin may enhance skin perfusion in cutaneous scald burns. To test this hypothesis, skin perfusion and edema formation in scald burned rabbit ears were measured. METHOD: Eighteen rabbits (3.5-4.5 kg) received partial-thickness scald burns to one ear and then were given normal saline, n = 6, 20 mg/kg ibuprofen, n = 6, or 700 IU/kg heparin, n = 6. Skin perfusion, blood flow and edema formation in the burned ear were measured with laser Doppler, ultrasound flowmeter and skin calipers, respectively. Statistical analysis was performed using repeated measures ANOVA with post hoc Scheffe's test for comparison between groups. RESULTS: Blood flow to the scald burned ear increased 10-15 times that of baseline with tissue perfusion increasing by 70% within 0.5 h compared to pre-burn. Ibuprofen maintained the elevated tissue perfusion for 5 h while the heparin and saline groups showed decreases to 95 and 35% of pre-burn values, respectively. The heparin and ibuprofen groups demonstrated significant increases in ear perfusion at 4 and 5 h postburn. Ibuprofen also showed a significant difference within the first hour postburn, p<0.01. Wet to dry weight ratios in burned ear tissue were greater in rabbits receiving saline or heparin compared to ibuprofen at 3.6+/-0.2 and 2.9+/-0.3 vs. 2.1+/-0.1, respectively (p<0.001). CONCLUSION: Ibuprofen increases tissue perfusion and reduces edema formation in scald burned rabbit ears.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10751701&dopt=Abstract ibuprofen Motrin



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Alternating antipyretics: is this an alternative?

Mayoral CE, Marino RV, Rosenfeld W, Greensher J.

Department of Pediatrics, Winthrop University Hopsital, Mineola, New York, USA. kalenamd aol.com

OBJECTIVES: To identify current fever management strategies and their basis, and to assess the frequency of alternating acetaminophen and ibuprofen. BACKGROUND: Practicing pediatricians confront the dilemma of elevated temperature and the anxiety this creates for parents. An informal survey of pediatricians revealed a variety of management strategies, including alternating acetaminophen and ibuprofen. There are no scientific data regarding alternating these 2 products. Design. During professional meetings, pediatricians voluntarily filled out a 15-item questionnaire. RESULTS: One hundred sixty-one completed surveys were reviewed. Respondents were mostly general pediatricians (67.7%), with >/=20 years in practice (55.9%). Most respondents chose a temperature of 101(o)F to start antipyretic treatment (61.9%). A small percentage used discomfort alone as the indication (13%). The antipyretic of choice was temperature-dependent in 50% of respondents; 57% used ibuprofen for temperature >/=102 degrees F. Fifty percent of respondents advised parents to alternate acetaminophen and ibuprofen. The method of alternation varied. The most common answers given for choosing a particular antipyretic regime were recommendations of the American Academy of Pediatrics (29%) and opinions of colleagues and mentors (25%). Physicians with <5 years of practice were significantly more likely to alternate antipyretics (69.7%). CONCLUSION: Acetaminophen and ibuprofen are commonly being used in an alternating manner for management of fever. There is presently no scientific evidence that this combination is safe or achieves faster antipyresis than either agent alone. There is evidence that the improper use of these agents may cause harm. Despite 29% of participants citing American Academy of Pediatrics recommendations as the basis for fever management, no such policy or recommendations exist. The observation that this practice is more common in younger practitioners may reflect their continued anxiety about fever (fever phobia). Until properly controlled studies have assessed the risk of combining these 2 products, practitioners should proceed with caution.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10790455&dopt=Abstract ibuprofen Motrin



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Controlled release injectable liposomal gel of ibuprofen for epidural analgesia.

Paavola A, Kilpelainen I, Yliruusi J, Rosenberg P.

Department of Pharmacy, Pharmaceutical Technology Division, Biocenter 2, PO Box 56, University of Helsinki, Helsinki, Finland. anne.paavola helsinki.fi

The epidural administration is used commonly in the treatment of pain. Nonsteroidal anti-inflammatory drugs, especially ibuprofen, would have potential in epidural use. Like many epidurally useful drugs it, however, has a short duration of action, which is a limiting factor. To improve epidural pain treatment, a long-acting, single-dose gel injection is being developed. In the present study, the possibility of using liposomal systems to control the release and dural permeation of ibuprofen was investigated in vitro. Liposomal solutions of ibuprofen.Na (20 mg/ml) were prepared by high-pressure homogenization from egg phosphatidylcholine. The liposomal gel consisted of poloxamer 407 and the liposomal solution. No signs in the 1H-NMR spectroscopy of line broadenings or chemical shifts were observed. The liposomal formulations were reproducible and stable. Ibuprofen release in phosphate buffer, pH 7.4, at 37 degrees C from the liposomal solution and the liposomal gel were prolonged significantly compared with their respective solution and gel controls. The liposomal gel controlled ibuprofen release and dural permeation in vitro and showed a permeation pattern favourable for maintaining constant drug levels. The liposomal poloxamer gel represents a new formulation approach to increase the local epidural availability of ibuprofen. It appeared to be a promising injectable controlled-release drug delivery system.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10794930&dopt=Abstract ibuprofen Motrin



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Development and validation of an indirect enzyme-linked immunosorbent assay (ELISA) for the nonsteroidal anti-inflammatory drug S-ibuprofen.

Grafe KA, Hoffmann H.

Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, Frankfurt, Germany. K.Graefe pharmchem.uni-frankfurt.de

An indirect enzyme-linked immunosorbent assay (ELISA) was developed for the nonsteroidal anti-inflammatory drug (NSAID) S-ibuprofen. Conjugates for immunization were prepared by linking S-ibuprofen via the spacer 4-aminobutyric acid to bovine serum albumin as well as to a novel synthetic lipopeptide using the N-hydroxysuccinimide/dicyclohexylcarbodiimide method. Immunization with these immunogens was carried out in New Zealand rabbits. A poly-L-lysine-S-ibuprofen conjugate was used as a hapten-carrier for coating the surface of the microtiter plates with the hapten. Horse-radish peroxidase labeled anti-rabbit IgG served as secondary antibody using hydrogen peroxide and ABTS as substrates. The characterization of the polyclonal antiserum with compounds of analogous structure demonstrated that the antiserum possesses a very high specificity for S-ibuprofen (cross-reactivity < 0.14-1.4%). Additional cross-reactivity experiments using R-ibuprofen (cross-reactivity 50.5%), ibufenac (58%) and isopropylphenylacetic acid (6.4%) were carried out to obtain more detailed information about the antigenic recognition concerning the chiral center. The results indicated that the polyclonal antiserum possesses an additional antibody population, whose antigenic recognition did not contain the chiral center. The upper and lower limits of quantification of the developed ELISA were defined as 362 and 3.62 ng S-ibuprofen/ml, respectively, based on a 90% confidence interval.

Online source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10798242&dopt=Abstract ibuprofen Motrin