Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Ketoprofen

Шохин, И. Е.; Kulinich, Julia I.; Ramenskaya, G. V.; Abrahamsson, Bertil; Kopp, Sabine; Langguth, Peter; Polli, James E.; Shah, Vinod P.; Groot, D.W.; Barends, D. M.; Dressman, Jennifer B.

doi:10.1002/jps.23233

Cited by 85 publications

(69 citation statements)

References 31 publications

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“…Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. In several pharmacopeias ketoprofen is considered as practically insoluble in water [14,15]. The solubility of the crystalline form of ketoprofen in pure water at room temperature (22-24 • C) was reported to be 0.010 mg/mL [15].…”

Section: Methodsmentioning

confidence: 99%

“…After dissolution, the microcontainers were observed with an optical microscope (Zeiss, Germany, 10× magnitude) to confirm complete emptying. The amount of drug loaded per chip was estimated by the final concentration measured in the dissolution test at 16 h. Solubility of ketoprofen at 37 • C in aqueous solutions changes significantly with pH between 1 and 7 [14]. However, even in the test with the highest drug loading, the pH of the dissolution medium drop below 5.5 as ketoprofen is a weak acid (pK a 4.5).…”

Section: In Vitro Drug Dissolution Studiesmentioning

confidence: 99%

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Supercritical impregnation of polymer matrices spatially confined in microcontainers for oral drug delivery: Effect of temperature, pressure and time

Marizza

Pontoni

Rindzevicius

et al. 2016

The Journal of Supercritical Fluids

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The present study is aimed to enhance the oral bioavailability of ketoprofen by inserting it into the matrixof poly(vinylpyrrolidone) (PVP) K10 spatially confined into microcontainers, by means of supercriticalCO2-aided impregnation. Microcontainers are cylindrical reservoirs, with typical sizes in the micrometerrange, with a cavity open on one side, where the drug formulation is loaded. Differently to traditionaltablets, microcontainers have a higher surface area per unit volume, and release the drug only in onedirection. This design is meant to enhance the absorption of problematic drugs, like those with poor sol-ubility in water. In a previous study we introduced a novel technique for drug loading of microcontainers,based on inkjet printing and supercritical impregnation (SCI). We showed that SCI produces accurate andreproducible drug loading for large arrays of microcontainers. In the attempt of enhancing the throughputof the loading methods, we propose the replacement of polymer inkjet printing with an easier man-ual compression of the PVP powder into the microcontainers. As the second step, the polymer powderfilled-microcontainers were submitted to SCI. The separate role of different impregnation parameters(temperature, pressure, time, drug concentration in the supercritical phase) was elucidated with respectto the loading capacity. The microcontainer filling was observed by means of optical macroimaging, X-ray microtomography and scanning electron microscopy. The physical state of the drug was investigatedby means of Raman spectroscopy and compared with selected representative PVP-ketoprofen physicalmixtures. Finally, the drug loading was estimated by means of in vitro dissolution tests.The characterization study shows that the present loading method is a valuable alternative to the onepreviously described. The drug loading can be controlled with high accuracy and reproducibility andthe impregnated drug is in amorphous state. These results demonstrate that SCI can be used as a highthroughput loading technique for microfabricated devices for oral drug delivery

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Section: Methodsmentioning

confidence: 99%

Section: In Vitro Drug Dissolution Studiesmentioning

confidence: 99%

Supercritical impregnation of polymer matrices spatially confined in microcontainers for oral drug delivery: Effect of temperature, pressure and time

Marizza

Pontoni

Rindzevicius

et al. 2016

The Journal of Supercritical Fluids

View full text Add to dashboard Cite

show abstract

“…Therefore, formulation strategies for compounds of this class target a solubility improvement in an effort to optimize their biopharmaceutical profiles [1,16,17]. Consequently, we selected the BCS 2 APIs Diclofenac, Ibuprofen, Ketoprofen, Naproxen, Sulfadiazine, Sulfamethoxazole and Tolbutamide for this study [18][19][20][21][22]. Frequently, solubility improvement of ionizable APIs is subject to salt screening, with sodium being the most commonly used counterion for acidic APIs [1] and therefore, sodium salts were used as a control group.…”

Section: Discussionmentioning

confidence: 99%

Transformation of acidic poorly water soluble drugs into ionic liquids

Balk

Wiest

Widmer

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…Ketoprofen is a widely known product with good indices of effectiveness in the treatment of conditions associated with inflammatory and painful processes such as rheumatic diseases, musculoskeletal conditions, postoperative surgery, dysmenorrhea, renal colic and traumatic affections [1] [7].…”

Section: Introductionmentioning

confidence: 99%

Bioequivalence of 150 mg Extended-Release Ketoprofen from Laboratories LETI S.A.V. Test, vs ProfenidBI of Laboratories Sanofi-Aventis Pharmaceuticals LTDA, Prolonged Release, Reference, in Healthy Volunteers*

Annunziato¹,

Yibirín²,

Alfredo³

et al. 2018

OALib

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Objective: To evaluate the bioequivalence between two formulations of ketoprofen after administration of a 150 mg extended release tablet (L.P. ProfenidBI®), 150 mg modified release tablets. Methods: A single-dose cross-over, randomized study was performed under fasting conditions with two treatments, two periods, two sequences (2 × 2) with a 7-day washout period between each dose in 28 healthy volunteers. Subjects were randomly assigned to each of the administration sequences. The pharmacokinetic parameters evaluated were: C max , AUC 0-t and AUC 0-∞ . For the bioequivalence analysis, the AUC 0-t was calculated from the time of administration to the 12 th hour, posology requested for the medication test, by the trapezoidal method; Software: Excel. The means and Confidence Intervals were compared between 80% -125% for the quotient of C max , T max , AUC 0-t and AUC 0-∞ . Results: C max 8.3529 ± 1.9176 μg/mL vs. 7.7175 ± 2.1751 μg/mL, T max 0.75 h vs. 1.25 h, AUC 0-12 25.9560 ± 4.9846 μg/mL/hr vs. 24.9015 ± 5.1507 μg/mL/ hr and AUC 0-∞ 27.0147 ± 5.1099 μg/mL/hr vs. 25.6400 ± 5.1144 μg/mL/h, respectively. 95% IC: C max 106.26% -107.85%, AUC 0-12 101.11% -101.78% and AUC 0-∞ 100.53% -102.94%. Conclusion: The test formulation Ketoprofen 150 mg LP, manufactured by LETI S.A.V. Laboratories, is bioequivalent with respect to the reference product ProfenidBI® 150 mg controlled release tablets, manufactured by Sanofi-Aventis Pharmaceuticals LTDA Laboratories, as the Values obtained from AUC and C max were maintained in the range of 80% -125%.

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Biowaiver Monographs for Immediate-Release Solid Oral Dosage Forms: Ketoprofen

Cited by 85 publications

References 31 publications

Supercritical impregnation of polymer matrices spatially confined in microcontainers for oral drug delivery: Effect of temperature, pressure and time

Supercritical impregnation of polymer matrices spatially confined in microcontainers for oral drug delivery: Effect of temperature, pressure and time

Transformation of acidic poorly water soluble drugs into ionic liquids

Bioequivalence of 150 mg Extended-Release Ketoprofen from Laboratories LETI S.A.V. Test, vs ProfenidBI of Laboratories Sanofi-Aventis Pharmaceuticals LTDA, Prolonged Release, Reference, in Healthy Volunteers*

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