Bioavailability of ibuprofen from hot-melt extruded mini-matrices

Brabander, C De; Vervaet, Chris; Bortel, Luc Van; Remon, Jean‐Paul

doi:10.1016/j.ijpharm.2003.10.029

Cited by 39 publications

(15 citation statements)

References 12 publications

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“…Effective treatment of chronic painful arthritic conditions requires daily doses between 1.6 and 2.4 g [1]. When used in the treatment of rheumatoid arthritis, ibuprofen has relieved pain and stiffness, reduced swelling, and improved grip strength and joint flexion.…”

Section: Introductionmentioning

confidence: 99%

Comparative Bioavailability Study of Two Ibuprofen Preparations after Oral Administration in Healthy Volunteers

Bienert¹,

Szkutnik-Fiedler²,

Dyderski³

et al. 2011

Arzneimittelforschung

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The bioavailability of a new ibuprofen (2-(p-isobutylphenyl)propionic acid, CAS 15687-27-1) preparation was compared with a reference preparation of the drug in 23 healthy male volunteers, aged between 19 and 27. A single dose of 400 mg was given orally in the fasted state, using a randomized two-way crossover study. A washout period of two weeks separated both treatment periods. Ibuprofen plasma levels were determined by means of a validated HPLC method (UV detector). Values of 154.48 +/- 53.27 microg x h/ml (95 % confidence interval CI: 133.50-177.03) for the test, and 140.86 +/- 44.82 microg x h/ml (95% CI: 122.53-159.16) for the reference preparation AUC(0-infinity) demonstrate a nearly identical extent of drug absorption. Maximum plasma concentrations Cmax of 39.53 +/- 7.11 microg/ml (95 % CI: 35.97-41.78) and 37.71 +/- 8.67 microg/ml (95% CI: 33.37-40.46) achieved for the test and reference preparations did not differ significantly. AUC(0-infinity) and Cmax ratios (90% CI) were within the 80-125% interval required for bioequivalence as stipulated in the current international regulations of the European Agency for the Evalution of Medicinal Products and the Food and Drug Administration. Therefore it is concluded that the new ibuprofen preparation is therapeutically equivalent to the reference preparation for both, the extent and the rate of absorption, after single dose administration in healthy volunteers.

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Section: Introductionmentioning

confidence: 99%

Comparative Bioavailability Study of Two Ibuprofen Preparations after Oral Administration in Healthy Volunteers

Bienert¹,

Szkutnik-Fiedler²,

Dyderski³

et al. 2011

Arzneimittelforschung

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“…In addition to the enhancement of the solubility (and hence bioavailability) of poorly soluble BCS Class II therapeutic agents, there are several pharmaceutical applications for extrusion and injection moulding. These include, the production of controlled release/modified release solid dosage forms (Andrews et al, 2008;De Brabander et al, 2000;De Brabander C. et al, 2004;Yang M. et al, 2004;Young et al, 2002), targeted drug release (Andrews et al, 2008;Miller D.A. et al, 2008) and films for transdermal/buccal drug delivery Mididoddi PK.…”

Section: Extrusion Has Been Investigated As a Methods To Enhance The Smentioning

confidence: 99%

Characterisation and modelling of the thermorheological properties of pharmaceutical polymers and their blends using capillary rheometry: Implications for hot melt processing of dosage forms

Jones

Margetson

McAllister

et al. 2015

International Journal of Pharmaceutics

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“…Brabender et al investigated the bioavailability of ibuprofen from hot-melt extruded mini-matrices based on ethyl cellulose and a hydrophilic excipient, xanthum gum (De Brabander et al, 2004). During in vivo evaluation an oral dose of 300 mg ibuprofen was administered in hard gelatin capsules to healthy volunteers (n = 9) in a randomized cross-over study and compared with a commercially available sustained release product (Ibuslow ® ).…”

Section: Granules Pellets and Spheresmentioning

confidence: 99%

Pharmaceutical Applications of Hot-Melt Extrusion: Part II

Repka

Battu

Upadhye

et al. 2007

Drug Development and Industrial Pharmacy

317

158

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The advent of high through-put screening in the drug discovery process has resulted in compounds with high lipophilicity and poor solubility. Increasing the solubility of such compounds poses a major challenge to formulation scientists. Various approaches have been adopted to address this including preparation of solid dispersions and solid solutions. Hot-melt extrusion is an efficient technology for producing solid molecular dispersions with considerable advantages over solvent-based processes such as spray drying and co-precipitation. Hot-melt extrusion has been demonstrated to provide sustained, modified, and targeted drug delivery. Improvements in bioavailability utilizing the hot-melt extrusion technique demonstrate the value of the technology as a potential drug delivery processing tool. The interest in hot-melt extrusion technology for pharmaceutical applications is evident from the increasing number of patents and publications in the scientific literature. Part II of this article reviews the myriad of hot-melt extrusion applications for pharmaceutical dosage forms including granules, pellets, tablets, implants, transmucosal, and transdermal systems.

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Bioavailability of ibuprofen from hot-melt extruded mini-matrices

Cited by 39 publications

References 12 publications

Comparative Bioavailability Study of Two Ibuprofen Preparations after Oral Administration in Healthy Volunteers

Comparative Bioavailability Study of Two Ibuprofen Preparations after Oral Administration in Healthy Volunteers

Characterisation and modelling of the thermorheological properties of pharmaceutical polymers and their blends using capillary rheometry: Implications for hot melt processing of dosage forms

Pharmaceutical Applications of Hot-Melt Extrusion: Part II

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