Ibuprofen Capsules Research Articles

Effect of preoperative oral ibuprofen on postoperative pain after dental implantation: a randomized controlled trial

Objective: To evaluate the effect of preemptive analgesia with ibuprofen on postoperative pain following single posterior tooth implantation, aiming to provide a clinical reference for its application. Methods: A multicenter, randomized, double-blind, placebo-controlled parallel-group trial was conducted. A total of 82 participants were included in the trial, meeting the eligibility criteria from April 2022 to April 2024 at the Capital Medical University School of Stomatology (40 cases), Beijing TianTan Hospital, Capital Medical University (22 cases), Beijing Chao-Yang Hospital, Capital Medical University (20 cases). Participants were randomly assigned in a 1∶1 ratio to either the ibuprofen group or the control group, with each group comprising 41 individuals. Participants in the ibuprofen group received 300 mg of sustained-release ibuprofen capsules orally 15 min before surgery, while the control group received a placebo. Both groups received the same postoperative analgesic regimen for 3 days. Pain scores were assessed using the Numerical rating scale (NRS) at 30 min, 4 h, 6 h, 8 h, 24 h, 48 h, and 72 h postoperatively, and the additional use of analgesic medication was recorded from days 4 to 6 postoperatively. Results: A total of 82 participants were initially enrolled in the study, with 7 dropouts (4 from the control group and 3 from the ibuprofen group), resulting in 75 participants (37 in the control group and 38 in the ibuprofen group) completing the trial. There were no reports of adverse events such as nausea or vomiting among the participants. The ibuprofen group exhibited significantly lower pain scores at 4 h, 6 h and 8 h [1.0 (0.0, 2.0), 1.0 (0.0, 2.0), 1.5 (0.0, 3.0) ] postoperatively compared to the control group 4 h, 6 h and 8 h [2.0 (1.0, 3.0), 3.0 (1.5, 4.0), 2.0 (1.0, 4.0)] (Z=-1.99, P=0.047; Z=-3.01, P=0.003; Z=2.10, P=0.036). The proportions of patients requiring additional analgesic medication between days 4 and 6 post-surgery were 18.4% (7/38) in the ibuprofen group and 27.0% (10/37) in the control group, with no significant difference (χ2=0.79, P=0.373). The median additional medication usage postoperatively was [0.0 (0.0, 0.0) pills] in the ibuprofen group and [0.0 (0.0, 1.0) pills] in the control group, with no significant difference (Z=-0.78, P=0.439). Conclusions: Preemptive analgesia with ibuprofen effectively reduces postoperative pain following tooth implantation, representing a safe and effective perioperative pain management strategy.

Clinical validation of a fast-acting acetaminophen: a randomized, active and placebo controlled dental pain study

Objectives To address the need for faster pain relief of over-the-counter (OTC) analgesic users, a novel drug delivery technology was developed to achieve faster absorption of orally administered acetaminophen with the goal of delivering earlier onset of pain relief. Previous development studies suggested that a 1000 mg dose of this fast-acting acetaminophen (FA-acetaminophen) formulation provided faster absorption and onset of action versus, commercially available OTC fast-acting analgesics, 1000 mg of extra-strength acetaminophen (ES-acetaminophen) or 400 mg of liquid-filled ibuprofen capsules (LG-ibuprofen). This study was designed as the definitive trial evaluating the onset of pain relief of FA-acetaminophen versus these same OTC comparators. Methods This single-dose, randomized, double-blind, placebo- and active-controlled clinical trial compared analgesic onset, overall efficacy, and safety of FA-acetaminophen 1000 mg, ES-acetaminophen 1000 mg, LG-ibuprofen 400 mg, and placebo over 4 h in a postsurgical dental pain model. Following removal of 3 to 4 impacted third molars, 664 subjects with moderate-to-severe pain were randomized in a 4:4:2:1 ratio to FA-acetaminophen (249), ES-acetaminophen (232), LG-ibuprofen (124), or placebo (59). Mean age was 18.9 years; 45.5% were male; 57.5% had severe baseline pain intensity. Subjects stopped a first stopwatch if/when they had perceptible pain relief and a second stopwatch if/when their pain relief became meaningful to them. Pain intensity difference (PID) and pain relief (PAR) were obtained using an 11-point numerical rating scale. Findings FA-acetaminophen 1000 mg had faster median time to onset of pain relief (15.7 min) compared to ES-acetaminophen 1000 mg (20.2 min, p = 0.035), LG-ibuprofen 400 mg (23.2 min, p < 0.001), and placebo (non-estimable), statistically greater mean PAR and PID scores than other treatment groups at 15 and 30 min, and a statistically greater percentage of subjects with confirmed perceptible pain relief at 15 and 20 min. At 25 min, FA-acetaminophen 1000 mg had a statistically significantly greater percentage of subjects with confirmed perceptible pain relief than LG-ibuprofen 400 mg and placebo. No clinically significant adverse events were reported. Conclusions This study supports previous studies, demonstrating faster onset of analgesia with FA-acetaminophen 1000 mg compared to OTC ES-acetaminophen 1000 mg and OTC LG-ibuprofen 400 mg. ClinicalTrials.gov Identifier NCT03224403 https://clinicaltrials.gov/ct2/show/NCT03224403

Preparation of three structurally similar stationary phases with different ionizable terminal groups and evaluation of their retention performances under multiple modes in high performance liquid chromatography

Three structurally similar silane reagents with different terminal groups were prepared and bonded to silica to obtain three structurally similar stationary phases (Sil-Ph-COOH, Sil-Phe and Sil-Ph-NH2). The prepared stationary phases were characterized through elemental analysis (EA) and Fourier Transform Infrared Spectroscopy (FT-IR). These three stationary phases provided acceptable retention repeatability (relative standard deviations between 0.08% and 0.13%) and high column efficiency (7.3 × 104 plates/m for uridine on Sil-Phe). The retention behavior of the three columns was investigated under different chromatographic conditions including different mobile phase ratio, salt concentration, pH etc. The retention mechanisms were explored by linear solvation energy relationships and Van't Hoff plots. Applications in separation under reversed phase liquid chromatography (RPLC), hydrophilic interaction liquid chromatography (HILIC) and ion exchange chromatography (IEC) mode were investigated. The results showed that the retention capacity of the stationary phases with different terminal groups to the analytes is very different, especially for carboxylic acids, because the surface charges of amino groups and carboxyl groups under weakly acidic conditions produce different electrostatic effects with dissociated carboxylic acids. Finally, the Sil-Phe column was employed to detect ibuprofen extracted from pharmaceutical ibuprofen capsules and vitamins extracted from vitamin tablets.

Down the canal or down the gullet - which form of ibuprofen is best for post-endo instrumentation pain?

Study population and design This randomised observational study compared the analgesic efficacy of intra-canal local ibuprofen paste (Odontocide) with systemic ibuprofen capsules. Ninety patients with symptomatic apical periodontitis scheduled to undergo endodontic therapy were randomised to receive either local ibuprofen, systemic ibuprofen, or no ibuprofen (control). Using a visual analogue scale, pain scores were measured at set time points in the first 48 hours after endodontic instrumentation. The endodontic instrumentation procedures were standardised to use the same endodontic files, sodium hypochlorite, and EDTA irrigants. Canals were dressed with either Odontocide (local ibuprofen paste) or calcium oxide in the systemic ibuprofen and control groups.Data analysis Friedman and Wilcoxon tests were used to compare groups. A power calculation was listed in the methods of the paper which is an important and appropriate step.Results Systemic ibuprofen gave statistically significant better pain relief compared with local ibuprofen paste applied to root canals but only in the first 24 hours after root canal instrumentation. After the 24-hour mark, the systemic ibuprofen had a lower mean pain score but this was not statistically significant. Systemic ibuprofen was always statistically better at providing pain relief than the control.

Ibuprofen and Acetaminophen Versus Intranasal Ketorolac (Sprix) in an Untreated Endodontic Pain Model: A Randomized, Double-blind Investigation

IntroductionPreviously, ketorolac was available for primary use only via intravenous and intramuscular routes. Its availability in intranasal form offers an alternative route of administration that patients can self-administer. The purpose of this study was to compare the efficacy of intranasal ketorolac (Sprix; Egalet US Inc, Wayne, PA) with a combination of ibuprofen/acetaminophen in an acute pain model of untreated endodontic patients experiencing moderate to severe pain and symptomatic apical periodontitis. MethodsSeventy patients experiencing moderate to severe pain, a pulpal diagnosis of symptomatic irreversible pulpitis or necrosis, and a periapical diagnosis of symptomatic apical periodontitis participated. Patients were randomly divided into 2 groups and received either 31.5 mg intranasal ketorolac and placebo capsules or 1000 mg acetaminophen/600 mg ibuprofen capsules and a mock nasal spray. Patients recorded perceived pain scores on a visual analog scale every 15 minutes from drug administration up to 240 minutes. The time to 50% pain relief, the first sign of pain relief, and meaningful pain relief were recorded, and the data were analyzed. ResultsA decline in reported pain was observed until 120 minutes after dosing, after which reported pain remained relatively constant. There was no significant difference between the 2 groups for the time to 50% pain relief, the first sign of pain relief, or meaningful pain relief. ConclusionsThe effectiveness of intranasal ketorolac was not significantly different from that of a 1000 mg acetaminophen/600 mg ibuprofen combination. Intranasal ketorolac provides a nonnarcotic alternative and an additional route of medication administration to practicing clinicians.

The effectiveness of ibuprofen and lorazepam combination therapy in treating the symptoms of acute Migraine: A randomized clinical trial.

BackgroundMigraine is a common, episodic and debilitating disease. The migraineur not only suffers from pain, but also lives with a diminished to poor quality of life. Several medicinal therapies are used to abate the debilitating symptoms of this disease.ObjectiveThe present study was conducted to determine the effectiveness of Ibuprofen and Lorazepam combination therapy in treating the symptoms of acute migraine.MethodsThe present randomized clinical trial study used the pretest-posttest design with three comparison treatments, to examine 90 patients with an average of two to six attacks per month and an initial diagnosis of migraine based on the International Headache Society (HIS) criteria. The study was conducted on patients during the first half of 2014 with a diagnosis of acute migraine attack who were referred to Babol Ayatollah Rouhani Hospital in Iran. The patients were randomly divided into three groups of 30. The first group was administered 200 mg Ibuprofen capsules, the second group 400 mg Ibuprofen capsules and the third group a combination of 200 mg Ibuprofen capsules and 1 mg Lorazepam tablets. The medications were taken in the presence of the researcher. A checklist was used to assess the severity of headache and other migraine symptoms such as nausea, vomiting, photophobia and phonophobia in the patients, before and two hours after the intervention. Data were analyzed in SPSS-18 using the Mann-Whitney test, the McNemar test, Wilcoxon’s test, the NOVA and the Chi-squared test at the significance level of p<0.05, and power analysis with 30 patients in each group to perform this study was 0.8(1-β).ResultsThe mean age of participants was reported as 52±8 years and the condition was more frequent in women (56%). All three treatment regimens reduced the severity of headache significantly in the patients (p<0.001); nevertheless, the combination therapy used, produced the lowest mean severity of headache (p<0.001). The highest reduction in nausea and vomiting was (3.3%). None of the patients in either of the three groups reported phonophobia after the intervention, but only the patients in the combination therapy group reported no instance of photophobia.ConclusionsGiven the greater effectiveness of combination therapy with Ibuprofen and Lorazepam in alleviating the symptoms of acute migraine compared to single-drug treatments with Ibuprofen, Lorazepam is recommended to be used as a first line treatment for acute migraine.Clinical trial registrationThe trial was registered at the Thai Clinical Trials Registry (TCTR) (http://www.clinicaltrials.in.th/) with the ID: TCTR20160927003.FundingThe authors received no financial support for the research, authorship, and/or publication of this article.

Clinical observation of blood-letting to reduce pressure plus electroacupuncture for acute scapulohumeral periarthritis

To evaluate the clinical effect of blood-letting to reduce pressure combined with electro-acupuncture for acute scapulohumeral periarthritis and to explore its mechanism. Sixty-six patients were randomly assigned into an observation group (34 cases) and a control group (32 cases).Electroacupuncture (EA) was used at Jianyu (LI 15), Jianliao (TE 14), Jianqian (Extra), Jianzhen (SI 9), Quchi (LI 11) and ashi points in the two groups, once a day for 9 days. Besides, blood-letting to reduce pressure was applied at ashi points in the observation group, namely cupping therapy after blood-letting puncture 3 times, 3-10 mL a time,once 3 days. Ibuprofen capsules were prescribed orally for 9 days in the control group, 0.3 g a time,twice a day. 5-hydroxy-tryptamine (5-HT) and prostaglandin E2 (PGE2) of blood in the cups were tested by enzyme linked immunosorbent assay after the first and third blood-letting in the observation group. The changes of numerical rating scale (NRS) grades for pain and shoulder joint movements were observed. The comprehensive effects of the two groups were evaluated. The contents of 5-HT and PGE2 after the third blood-letting apparently decreased compared with those after the first operation in the observation group (both P<0.001). The grades of NRS and shoulder movements were obviously improved after treatment in the two groups (all P<0.001),with better results in the observation group (both P<0.05). The result of 4 cured cases, 20 apparently effective cases, 9 effective cases and 1 noneffective case in the observation group was superior to that of 1, 10, 15, 6 in the control group (P<0.05). Blood-letting therapy combined with EA can ease pain and improve shoulder joint function of scapulohumeral periarthritis,and the effect is better than that of ibuprofen combined with EA. The mechanism may be related to directly discharging the inflammatory substances in local blood of the affected shoulder.

Preparation of Micronized Ibuprofen Substance and Assessment of Its Bioavailability

A Buchi B-290 mini spray dryer (Switzerland) designed to dry aqueous solutions or suspensions was used to prepare micronized ibuprofen substance, which differed from the starting substance in terms of decreased crystal size. The bioavailability of ibuprofen given as oral capsules containing micronized ibuprofen substance (crystal size 30 μm) and capsules containing commercial ibuprofen substance (crystal size 150 μm) was studied in Chinchilla rabbits. Concentrations of unaltered ibuprofen were measured by reverse-phase HPLC with spectrophotometric detection at 220 nm. Ibuprofen was extracted from rabbit serum by liquid:liquid extraction and averaged 78 %. The detection limit was 0.1 μg/ml. The bioavailability of micronized ibuprofen was more than twice that of the commercial substance (mean crystal size 150 μm). There were no differences in the rates of absorption or elimination of ibuprofen from the systemic circulation.

Comparison between Soft Gelatin Capsule Containing Ibuprofen and Ibuprofen Regular Tablet in Pain Control Following Scaling and Root Planing

Aim: Scaling and root planing (SRP) is a major component of periodontal therapy which is often accompanied by painful experiences for the patient. The objective of the present study is to evaluate the pain control of two available types of ibuprofen, soft gelatin capsules and tablets, following SRP in patients with chronic periodontitis.&#x0D; Methodology: 75 patients with chronic periodontitis, undergoing routine periodontal SRP were selected. Following probing the amount of pain perceived was recorded as the baseline pain using visual analog scale (VAS). Further, they received either 800 mg ibuprofen tablet, 800 mg ibuprofen capsule or placebo and the pain level was measured thirty minutes thereafter. Participants underwent SRP procedure and the pain levels were recorded immediately and then at 30 and 60 minutes after SRP.&#x0D; Results: The mean VAS pain scores assessed immediately, thirty minutes and an hour after SRP for both ibuprofen and ibuprofen capsule groups were lower than placebo. Significant difference in the pain parameter only immediately after SRP between three groups were observed (p=0.012).The mean VAS pain score difference after thirty minutes and an hour upon SRP with baseline was insignificant in all study groups (p≤0.0001). However, the mean VAS pain score measured an hour after SRP showed significant difference between both NSAID groups and placebo group (p=0.012)&#x0D; Conclusions: Soft gelatin ibuprofen capsules are well suitable for pain management during SRP procedure in patients with chronic periodontitis due to reported rapid onset of action and less gastrointestinal intolerance. &#x0D; How to cite this article: Jenabian N, Naderi E, Moghadamnia AA, Zahedpasha S. Comparison between Soft Gelatin Capsule Containing Ibuprofen and Ibuprofen Regular Tablet in Pain Control Following Scaling and Root Planing. Int Dent Res 2011;2:42-47.&#x0D; Linguistic Revision: The English in this manuscript has been checked by at least two professional editors, both native speakers of English.

Influência do processo de mistura de pós na preparação magistral de cápsulas de ibuprofeno

O objetivo do presente trabalho foi avaliar a influência do processo de mistura de pós na preparação magistral de cápsulas contendo ibuprofeno. Para a mistura dos pós foram utilizados o misturador e triturador automático e mistura manual em saco plástico. Depois de estabelecidos os tempos ótimo de mistura, cápsulas de ibuprofeno foram preparadas (3 lotes de 40 cápsulas), nas doses de 100 e 200 mg. O controle de qualidade das cápsulas foi realizado através da determinação do peso médio, doseamento e uniformidade de doses unitárias. Através dos resultados, diferenças entre os dois processos de mistura foram observadas, especialmente para a mistura de pós contendo ibuprofeno na dose de 100 mg. Os lotes obtidos pela mistura manual, neste caso, não cumpriram com as especificações em relação à uniformidade de doses. Para as cápsulas contendo ibuprofeno na dose de 200 mg os resultados foram satisfatórios.

A Validated Enantioselective Assay for the Determination of Ibuprofen in Human Plasma Using Ultra Performance Liquid Chromatography with Tandem Mass Spectrometry (UPLC-MS/MS)

A modified ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method was developed and validated for the quantitation of ibuprofen enantiomers in human plasma. Ibuprofen and flurbiprofen (internal standard) were extracted from human plasma at acidic pH, using a single-step liquid-liquid extraction with methyl-tert-butyl ether. The enantiomers of ibuprofen and flurbiprofen were derivatized to yield the corresponding diastereomers. Chromatographic separation was achieved using a phenyl column with a run time of 20 min. (R)- and (S)-ibuprofen were quantitated at the multiple reaction monitoring (MRM) transition of m/z 360.2 ? 232.1, and (R)- and (S)-flurbiprofen were monitored at the MRM transition of m/z 398.3 ? 270.1. The method was validated for accuracy, precision, linearity, range, limit of quantitation (LOQ), limit of detection (LOD), selectivity, absolute recovery, matrix effect, dilution integrity, and evaluation of carry-over. Accuracy for (R)-ibuprofen ranged between –11.8% and 11.2%, and for (S)-ibuprofen between –8.6% and –0.3%. Precision for (R)-ibuprofen was ≤ 11.2%, and for (S)-ibuprofen ≤ 7.0%. The calibration curves were weighted (1/X2, n = 7) and were linear with r2 for (R)-ibuprofen ≥ 0.988 and for (S)-ibuprofen ≥ 0.990. The range of the method was 50 to 5000 ng/mL with the LOQ of 50 ng/mL, and LOD of 1 ng/mL, for (R)- and (S)-ibuprofen requiring 100 µL of sample. The method was applied successfully to a pharmacokinetic study with the administration of a single oral dose of ibuprofen capsules to human subjects.

Oesophageal perforation following ingestion of over-the-counter ibuprofen capsules

We present a rare case of oesophageal perforation following ingestion of over-the-counter ibuprofen capsules. Case report and literature review of pill oesophagitis. A previously well, 18-year-old man presented with sudden onset, severe, retrosternal pain, dysphagia and odynophagia following ingestion of over-the-counter ibuprofen capsules. Plain X-ray films and a contrast-enhanced computed tomography scan indicated the diagnosis. The patient was successfully treated with non-operative management. To our knowledge, this is the first report in the world literature concerning oesophageal perforation with ibuprofen. We discuss pill-induced oesophageal injury and its prevention. Manufacturers, clinicians and patients can all take steps to avoid this potentially life-threatening complication.

Scrutinizing Global Short-Term Medical Outreach

Scrutinizing Global Short-Term Medical Outreach Matthew DeCamp (bio) About five years ago, I was among a dozen or so medical and nursing students involved in a short-term medical outreach trip to Honduras. By "short-term medical outreach trip," I mean those brief trips to developing countries taken by medical professionals and often organized by health professional schools in the United States. The idea behind them is that they expose students and faculty to people in developing countries, often for the first time, and bring much-needed care to the countries. The visitors run an acute care clinic or ambulatory surgery center, distribute donated medications, engage in health education, and learn about health care in the developing world. At the time, I assumed that what I was doing was "ethical" and maybe even commendable. I thought it was altruistic. No doubt many with me shared this belief. But as time passes, the value of what the Hondurans gave me, in moral and educational terms, seems to surpass the value of the acute medical care I helped deliver. I did not intend this; in fact, I thought my participation would help Hondurans much more than it would help me. But if I was wrong, and the benefit went mainly to someone outside the local community, then was the trip fundamentally different from the international AIDS clinical trials that years before received such scrutiny? If so, why did our trip—and others like it—escape the ethical scrutiny applied to clinical research in developing countries? Not Research? I wondered at first if my questions were misguided: perhaps global short-term medical outreach is just clinical care, and not "research" at all. From the perspective of those who go on these trips, how best to understand it is less than obvious.1 Health care personnel from a developed country organize a visit with local contacts in a developing one. The team travels to a community. With them are medical supplies, including medications and educational materials. They stay for a short period and operate something resembling a clinic or surgical center in their home country. Many individuals (though of course not all in need) receive some basic medical care. The team departs. Some time later, the medications and supplies run out (unless another team arrives and brings more). More or less continuing contact exists. Does this situation describe research or clinical care? If this scenario were research, it might have gone through ethical review by institutional review boards in the developed and developing country. In addition, the researchers would have obtained informed consent (written or oral) from the study participants. If the scenario were a short-term medical outreach trip, neither would have happened. This lack of oversight might not be a problem if short-term outreach is unequivocally good or does not raise any interesting ethical issues. However, once we move beyond the trivial claim that outreach is different from research simply because it is handled differently, interesting ethical issues arise. Appeals to Benefits For example, I wondered if the crucial difference between research and clinical practice might lie in outreach's goal. Unlike research, the goal of global short-term medical outreach is not to gain "generalized knowledge" but to provide tangible medical benefits to individuals in the community (a distinction between research and clinical care equally applicable in the United States). This is probably what many people think when they consider outreach. I thought this, too, before my trip to Honduras. But there are a couple of problems with this view. First, well-designed clinical research often provides medical benefit as well. Second, in outreach, we tend to avoid spelling out exactly what we mean by "benefit." In fact, we are tempted to act as if any benefit counts ethically in favor of the trip, or that simply intending to provide benefit is enough. Both are too permissive. The former would endorse a short-term medical outreach whose only goal, for example, was to administer ten ibuprofen capsules to each individual in a community (even as we scrutinize a clinical trial that helps sustain a local pharmacy merely because it involves research). The latter is philosophically challenging, and it would...

Novel approach for determination of correlation between in vivo and in vitro dissolution using the optimization technique.

A new approach to determination of good correlations between in vivo and in vitro dissolution was studied using the optimization technique. Ibuprofen, which exhibits dissolution rate-limiting absorption, was used as a model drug. Ibuprofen capsules of two different release types were prepared, and their in vivo dissolution profiles were obtained from measurements of plasma concentration following oral administration of the capsules to beagle dogs by the mathematical deconvolution method using solution data of oral administration as a weight function. For the dissolution test to correspond to the in vivo dissolution profiles, the test was carried out at 12 levels (9 different sets of conditions) and results were analyzed with the optimization technique to deal with two factors. The first-order rate constant (kappa d) and the dissolution time at 50% (t50%) of the in vivo dissolution were selected for use as the response variables. Regression analysis was performed to describe the in vitro dissolution characteristics as functions of the pH of dissolution medium and paddle rotation speed in the paddle method. The in vivo/in vitro correlation obtained from the kappa d was better than that obtained from the t50%. The optimum conditions for dissolution testing corresponding to the in vivo kappa d were determined to be a pH 6.6 for the dissolution medium and a 56 rpm paddle rotation rate. The experimental data obtained by dissolution testing was well fit by the predicted curve derived from in vivo and in vitro dissolution profiles. This dissolution test is applicable to the formulations containing ibuprofen of particle size within the experimental range.

Bioavailability of ibuprofen from hard gelatin capsules containing different viscosity grades of hydroxypropylmethylcellulose and sodium carboxymethylcellulose

The effect of viscosity grade (molecular weight group) of the polymer diluent on the bioavailability of ibuprofen from hard gelatin capsules was evaluated in two single-dose (400 mg) cross-over studies in healthy volunteers following an overnight fast. The polymers studied were nonionic hydroxypropylmethylcellulose (HPMC) K100 and K15M, and anionic sodium carboxymethylcellulose (NaCMC) LV, MV and HV. Plain ibuprofen capsules were used for reference. Use of HPMC K15M led to markedl3 sustained drug absorption from the capsules. The t max and C max values differed significantly ( P < 0.001) from the reference values. The sustaining effect of the lower viscosity grade, K 100, was less pronounced. NaCMC-based capsules exhibited sustained-release properties similar to those of the HPMC K 100 capsules. In the case of NaCMC, the molecular weight of the polymer had no significant effect on drug absorption. No differences in the extent of bioavailability of ibuprofen between the formulations studied were evident.

The filling of molten ibuprofen into hard gelatin capsules

The dissolution rate of melt-filled ibuprofen capsules is markedly affected by low (10% or less) levels of a variety of excipients. Thus, a high fill weight can be achieved and virtually any in vitro dissolution profile obtained. For any particular system of interest the effect of processing conditions can be readily determined.

Relative Bioavailability of Commercially Available Ibuprofen Oral Dosage Forms in Humans

Two human bioavailability studies were conducted to assess the in vivo performances of recently marketed 200-, 300-, and 400-mg ibuprofen capsules relative to the innovator's 300- and 400-mg tablets when administered as single oral 300- or 400-mg doses. An ibuprofen oral solution was also administered in each trial. Within each study, the products were equivalent to each other and to the oral solution with respect to the extent of ibuprofen absorption. Absorption rates, however, differed markedly among the products studied. Ibuprofen was more slowly absorbed from the 300- and 400-mg capsules than from the respective strength tablets. The 200-mg capsule exhibited an absorption rate comparable to the 400-mg tablet but more rapid than the 400-mg capsule. It was concluded that two of the duplicator's 200-mg capsules were bioequivalent to one of the innovator's 400-mg tablet. The duplicator's 300- and 400-mg capsules were bioinequivalent to the innovator's 300- and 400-mg tablets, respectively, due to their slower rates of absorption.

Gastro-Intestinal Blood Loss during Administration of Indoprofen, Aspirin and Ibuprofen

The acute effect of three non-steroidal anti-inflammatory drugs, ibuprofen, acetylsalicylic acid (ASA) and indoprofen, on faecal blood loss was investigated in 15 subjects by means of 51Cr-labelled erythrocytes. Ibuprofen (900 mg/day for 5 days) and indoprofen capsules and tablets (300 mg and 600 mg/day for 5 days, respectively) slightly increased the amount of blood eliminated in faeces. The increase was of the same order of magnitude for both doses of indoprofen. ASA (1,500 mg/day for 5 days) caused about a 6-fold increase in blood loss. Four days after withdrawal of ASA, faecal blood was still about twice as high as in faeces of subjects given ibuprofen and indoprofen. The method appears sensitive and reliable for comparison of the immediate effect of anti-inflammatory drugs on gastro-intestinal mucosa.