Ibuprofen formulation

Chan KLA, Kazarian SG. High-throughput study of poly(ethylene glycol)/ibuprofen formulations under controlled environment using FTIR imaging. J Comb Chem 2006 8(1) 26-31. 

FIGURE 14 Raman spectra of three ibuprofen formulations. Ibuprofen formulations solution (dimer 3), solid line extrudate (PVP), dashed line crystalline powder, dotted line. The ibuprofen extrudate and solution are shifted compared to the crystalline form of ibuprofen. (Reprinted with permission from ref. 25, Copyright 1999, Plenum.)... 

From the above reports, it would appear prudent to use an enantiospecific assay when comparing bioavailability of ibuprofen formulations, especially when the formulations are designed to have modified drug release characteristics. 

Roberts, M Ford, JL MacLeod, GS Fell, JT Smith, GW Rowe, P Dyas, AM. Effect of lubricant type and concentration on the punch tip adherence of model ibuprofen formulations. J Pharm Pharmacol, 2004, 56, 299-305. 

Serajuddin ATM (1999) Solid dispersion of poorly water-soluble drugs etirly promises, subsequent problems, and recent breakthroughs. J Pharm Sd 88(10) 1058-1065 Shen SC, Ng WK, Chia L, Hu J, Tan RB (2011) Physical state and dissolution of ibuprofen formulated by co-spray drying with mesoporous silica effect of pore and particle size. Int J Pharm 410 188-195... 

A. Das, S. Wadhwa, and A. Srivastava, Cross-linked guar gum hydrogel discs for colon-specific delivery of ibuprofen Formulation and in vitro evaluation. Drug Delivery, 13 (2),... 

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. 

Figure 4 Dissolution of ibuprofen from the pure drug and several formulations available on the European market under the pH 6.8 test conditions shown in Table 3.

An MEKC method for the determination of ibuprofen, codeine phosphate hemihydrate, their nine potential degradation products, and impurities in a commercial tablet formulation was developed, optimized, and fully validated according to ICH guidelines and submitted to the regulatory authorities. The optimized system containing ACN as organic modifier allowed baseline separation of ibuprofen, codeine, and nine related substances within 12 min. 

FIG. 12. Permeability of ibuprofen from different formulations via excised human stratum comeum. Redrawn from Stoye, L, Permeabilitdtsverdnderung von humanem Stratum corneum nach Applikation nicht-steroidaler Antirheumatika in verschiedenen kolloidalen Trdgersystemen, Ph.D. Thesis TU Braunschweig, 1997. 

Bioactive compounds from Blumea gariepina salicin, salicylic acid, tenoxicam, ketorolac, piroxicam, tolmetin, naproxen, flurbiprofin, diclofenac, and ibuprofen in pharmaceutical formulations and biological samples ... 

S) ) formulation has been tested. Ibuprofen cream was more effective than placebo cream in the treatment of primary knee osteoarthritis. 

An early example of Raman mapping by Breitenbach et al. [52] showed that when crystalline ibuprofen is formulated in a hot melt extrudate the API changes to the amorphous form. Ibuprofen is a sparingly water-soluble compound, so this formulation provides a route to better bioavailability via the more soluble amorphous form. Using confocal Raman mapping the form of the API was determined at the time of manufacture and under stress conditions and was used to assess the stability of the amorphous form. These studies also showed that the API was homogeneously distributed throughout the formulation based on the relative band intensities of the amorphous API and a formulation excipient, polyvinylpyrrolidone (PVP). 

L.M. Oberoi, K.S. Alexander, A.T. Riga, Study of interaction between ibuprofen and nicotinamide using differential scanning calorimetry, spectroscopy, and microscopy and formulation of a fast-acting and possibly better ibuprofen suspension for osteoarthritis patients, J. Pharm. Sci. 94 (2005) 93-101. 

Oral ibuprofen is often prescribed in lower doses (< 2400 mg/d), at which it has analgesic but not anti-inflammatory efficacy. It is available over the counter in low-dose forms under several trade names. A topical cream preparation appears to be absorbed into fascia and muscle an (S)( ) formulation has been tested. Ibuprofen cream was more effective than placebo cream for the treatment of primary knee osteoarthritis. A liquid gel preparation of ibuprofen 400 mg provided faster relief and superior overall efficacy in postsurgical dental pain. In comparison with indomethacin, ibuprofen decreases urine output less and also causes less fluid retention than indomethacin. Ibuprofen has been shown to be effective in closing patent ductus arteriosus in preterm infants, with much the same efficacy and safety as indomethacin. Oral ibuprofen is as effective as intravenous administration in this condition. 

Ibuprofen is available in liquid, sachet, capsule, melt and tablet form. The licensed age range for ibuprofen depends on the product formulation. Ibuprofen is only indicated for children over six months of age over the counter. It has additional anti-inflammatory properties which may be helpful in conditions such as otitis media. Ibuprofen has the potential to cause gastrointestinal disturbances, although if given with food this is unlikely. Note Caution if using in a child with history of severe asthma or renal disease. 

Flurbiprofen, 100 mg three times daily, is a well-established first-line NSAID providing there is no evidence of vascular closure or scleral destruction on biomicroscopy. Flurbiprofen should provide pain relief within 2 days and improvement in clinical signs within 1 week. Indomethacin SR fiarmulation, 75 mg twice daily, is a well-established second-choice drug when flurbiprofen is not effective but has also been used as first line. NSAIDs that have shown efficacy and are now available in over-the-counter formulations include naproxen, 500 mg twice daily, and ibuprofen, 600 mg four times daily. If a simplified dosing schedule is a consideration, then pirox-icam, 20 mg/day, may be considered. Once effective control is established, a lower maintenance dose may suffice until the scleritis enters remission. To reduce the risk of gastrointestinal side effects, patients should be instructed to take NSAIDs with food or antacids. 

The relative concentration of the pharmacologically active S enantiomer of ibuprofen (S R ratio) increases with prolongation of the gastrointestinal transit time of racemic formulations due to a corresponding increase in chiral inversion of the R to S enantiomer in the gut (25). Administration of S-ibuprofen, therefore, reduces the formulation-dependent variability in the concentration of the active enantiomer in the body. 

From physicochemical viewpoints, enantiomers and racemates are often very different from one another. For example, it has been shown that individual enantiomers of ibuprofen have greater water solubility and faster dissolution than their racemates (30). A formulation of S-ibuprofen, therefore, may have more rapid absorption and consequently a shorter onset of analgesia. This is important, as evidence exists in the literature in support of a meaningful relationship between ibuprofen serum concentrations and its analgesic effects (31). Hence, a more rapidly absorbed formulation may provide shorter onset of action, Therefore, as a pain reliever, stereochemically pure NSAIDs may be preferable to their respective race-mates. Furthermore, one may take advantage of the single enantiomer s greater solubility to prepare various soluble formulations of NSAIDs and products with an accelerated dissolution rate. 

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). 

Packman, B. Packman, E. Doyle, G. Cooper, S. Ashraf, E. Koronkiewicz, K. Jayawardena, S. Solubilized ibuprofen evaluation of onset, relief, and safety of a novel formulation in the treatment of episodic tension-type headache. Headache 2000, 40 (7), 561-567. 

Fig. 12 Permeability of ibuprofen from different formulations via excised human stratum corneum. (Redrawn from RefP l)...

The bioavailability of an effervescent ibuprofen tablet was compared to a sugar-coated tablet. Ibuprofen was absorbed more rapidly from the effervescent tablet but both formulations were bioequivalent in... 

In-die temperature can be monitored for heat-sensitive formulation, such as ibuprofen. " ... 

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