Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant-containing microparticles

Wong, Sze; Kellaway, I.W.; Murdan, Sudaxshina

doi:10.1016/j.ijpharm.2006.03.001

Cited by 177 publications

(99 citation statements)

References 20 publications

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“…16 So, increasing the solubility of bosentan can improve its pharmacokinetics and dose reduction and variability in drug exposure among individuals can be solved. 17 One of the strategies in solubility enhancement is particle size reduction. 18 Nanoparticle are colloidal drug delivery systems usually between 10-1000 nm in size.…”

Section: Introductionmentioning

confidence: 99%

D-optimal Design for Preparation and Optimization of Fast Dissolving Bosentan Nanosuspension

Ghasemian¹,

Motaghian²,

Vatanara³

2016

Adv Pharm Bull

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Section: Introductionmentioning

confidence: 99%

D-optimal Design for Preparation and Optimization of Fast Dissolving Bosentan Nanosuspension

Ghasemian¹,

Motaghian²,

Vatanara³

2016

Adv Pharm Bull

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“…Microspheres with greater diameters resulted upon increasing the proportion of carbopol which could be attributed to the increment in viscosity of feed dispersion imparted by it. Higher viscosity results into the formation of larger droplets (14). Particle size of F4 and F5 was significantly smaller than the other batches (one-way ANOVA, p<0.05).…”

Section: Characterization Of the Prepared Microspheresmentioning

confidence: 89%

“…Osmotic effect, induced by them, helps in pore formation and contributes to effective drug mobility within the hydrated matrix (11). Moreover, microsphere formulation of the complexed drug would further enhance the solubility of drug, reduce the likelihood of dose dumping, minimize dose-related variations, and improve patient compliance (12)(13)(14).…”

Section: Introductionmentioning

confidence: 99%

Bioadhesive Microspheres for Bioavailability Enhancement of Raloxifene Hydrochloride: Formulation and Pharmacokinetic Evaluation

2011

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Abstract. Raloxifene hydrochloride (R-HCl), a BCS class II drug, remains a mainstay in the prevention and pharmacologic therapy of osteoporosis. Its absolute bioavailability, however, is 2% due to poor solubility and extensive first pass metabolism. The present study describes two simultaneous approaches to improve its bioavailability, complexation of R-HCl with cyclodextrin(s), and formulation of mucoadhesive microspheres of the complex using different proportions of carbopol and HPMC. Microspheres were pale yellow in color, free-flowing, spherical, and porous in outline. The particle size ranged between 3 and 15 μm, and entrapment efficiency was found to be within 81.63% to 87.73%. A significant improvement in the solubility of R-HCl was observed, and it differed with the combination of excipients used. X-ray diffraction and differential scanning calorimetry studies revealed that enhancement in drug solubility was resulted due to a change in its crystallinity within the formulation. Microspheres possessed remarkable mucoadhesion and offered controlled drug release, lasting up to 24 h. They produced a sharp plasma concentration-time profile of R-HCl within 30 min postadministration to Wistar rats.[AUC] 0-24 h was found to be 1,722.34 ng h/ml, and it differed significantly to that of pure drug powder (318.28 ng h/ml). More than fivefold increase in AUC and more than twofold increase in MRT were observed. FT-IR studies evidenced no interaction among drug and excipients. The results of this study showed that mucoadhesive microspheres could be a viable approach to improve the pharmacokinetic profile of R-HCl.

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“…It remainsas the most favorable and preferred route of drug administration both by patient and physicians. 1 The major challenge with the design of oral dosage forms lies with their poor bioavailability compared to injectable and implants. Pharmaceutical products intended for oral administration are cheaper and currently greater than sixty percent of drugs are marketed as oral products.…”

Section: Introductionmentioning

confidence: 99%

Design and Development of Bi-layered Sustained Release Azithromycin Tablets

Islam

Moghal

Bari

et al. 2017

Dhaka Univ. J. Pharm. Sci

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ABSTRACT:The objective of the current study was to develop a bilayer tablet of Azithromycin containing both immediate and sustained layer and evaluate the effect of formulation variables on drug release. Thirty different formulations (F-1 to F-30) were prepared by direct compression. When the fraction of polymer was increased from 5.55% to 10%, the rate of drug release was found to be slower. Maximum release of Azithromycin was from F-11 (within 8 hours), which contained 50 mg (5.55%) of HPMC 50 cps. Slowest release was observed from F-30 containing 90 mg (10%) of Carbopol 974 P. The IR spectral analysis revealed that all rate regarding agents and excipients used in this study are compatible with the active Azithromycin.

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Enhancement of the dissolution rate and oral absorption of a poorly water soluble drug by formation of surfactant-containing microparticles

Cited by 177 publications

References 20 publications

D-optimal Design for Preparation and Optimization of Fast Dissolving Bosentan Nanosuspension

D-optimal Design for Preparation and Optimization of Fast Dissolving Bosentan Nanosuspension

Bioadhesive Microspheres for Bioavailability Enhancement of Raloxifene Hydrochloride: Formulation and Pharmacokinetic Evaluation

Design and Development of Bi-layered Sustained Release Azithromycin Tablets

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