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Adeyeye, Christianah Moji; Price, James C.

doi:10.1023/a:1018931002991

Cited by 66 publications

(12 citation statements)

References 6 publications

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“…This results in a reduction of hydrophilic pathways for water molecules to access drug crystals inside the pellet. The same phenomenon was also observed by Adeyeye and Price (29). …”

Section: In Vitro Release Studiessupporting

confidence: 86%

Formulation and evaluation of mefenamic acid sustained release matrix pellets

Ibrahim

2013

Acta Pharmaceutica

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Interest in pellets as dosage forms has been increasing continuously. Several therapeutic advantages could be achieved by using pellets as a drug delivery system, over the single-unit regimen, such as less irritation of the gastrointestinal tract and a lowered risk of side effects due to dose dumping (1 The objective of the study was to prepare mefenamic acid (MA) sustained release matrix pellets and investigate the formulation parameters affecting pellet attributes and drug release in vitro. A mixer torque rheometer (MTR) was used to characterize the rheological properties of wet mass used in pellet formulation. Mefenamic acid pellets were prepared by extrusion/spheronization techniques using microcrystalline cellulose (MCC) in combination with lactose as pellet forming agents and water as the binding liquid. Also, the prepared pellets were characterized for their particle size and in vitro drug dissolution. The results revealed that the increase in lactose weight ratio to MCC resulted in a significant reduction of both maximum torque and binder ratios, while the addition of 2 % (m/m) polyvinyl pyrolidone (PVP) to MCC-lactose influenced only the mean torque rather than the wetting liquid (water). Particle size ranged from 945 to 1089 mm and had small span values (0.56-0.67). Furthermore, an inverse relation was observed between the rheological character of pellet wet masses (expressed by peak torque) and in vitro release rate. Increasing MA loading from 2.5 to 5 and 10 % was accompanied by a decrease in dissolution rates. In conclusion, properties of MA matrix pellets could be successfully monitored by controlling the wet mass characteristics by measuring torque.

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“…This results in a reduction of hydrophilic pathways for water molecules to access drug crystals inside the pellet. The same phenomenon was also observed by Adeyeye and Price (29). …”

Section: In Vitro Release Studiessupporting

confidence: 86%

Formulation and evaluation of mefenamic acid sustained release matrix pellets

Ibrahim

2013

Acta Pharmaceutica

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“…The quicker drug release at low wax loads can be due to increased drug crystals positioned on the liposphere surface that remained exposed to the dissolution fluid (3). At higher drug loads, drug dissolution resulted in a subsequent increase in the number of channels and pores within the wax matrix, which decreased the diffusional path length through the drug depleted zone and enhanced drug release (20).…”

Section: Resultsmentioning

confidence: 99%

Design and statistical optimization of glipizide loaded lipospheres using response surface methodology

Shivakumar

Patel²,

Desai³

et al. 2007

Acta Pharmaceutica

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A 32 factorial design was employed to produce glipizide lipospheres by the emulsification phase separation technique using paraffin wax and stearic acid as retardants. The effect of critical formulation variables, namely levels of paraffin wax (X1) and proportion of stearic acid in the wax (X2) on geometric mean diameter (dg), percent encapsulation efficiency (% EE), release at the end of 12 h (rel12) and time taken for 50% of drug release (t50), were evaluated using the F-test. Mathematical models containing only the significant terms were generated for each response parameter using the multiple linear regression analysis (MLRA) and analysis of variance (ANOVA). Both formulation variables studied exerted a significant influence (p < 0.05) on the response parameters. Numerical optimization using the desirability approach was employed to develop an optimized formulation by setting constraints on the dependent and independent variables. The experimental values of dg, % EE, rel12 and t50 values for the optimized formulation were found to be 57.54 +/- 1.38 mum, 86.28 +/- 1.32%, 77.23 +/- 2.78% and 5.60 +/- 0.32 h, respectively, which were in close agreement with those predicted by the mathematical models. The drug release from lipospheres followed first-order kinetics and was characterized by the Higuchi diffusion model. The optimized liposphere formulation developed was found to produce sustained anti-diabetic activity following oral administration in rats.

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“…Dissolution thus becomes the rate limiting step for absorption, and the quick release of ibuprofen in the gastrointestinal tract following oral administration is desirable. 1) Various formulations such as prodrugs, 2) inclusion complexes, 3) microcapsules, 4) etc. of ibuprofen were developed.…”

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confidence: 99%

Enhancement of Solubility, Dissolution and Bioavailability of Ibuprofen in Solid Dispersion Systems

et al. 2008

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To improve its solubility, dissolution, and bioavailability; Ibuprofen-polyethylene glycol 8000 (PEG 8000) solid dispersions (SDs) with different drug loadings were prepared, characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for solubility, in-vitro release, and oral bioavailability of ibuprofen in rats. Loss of individual surface properties during melting and solidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of drug-polymer interactions. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and C max , and a significant decrease in T max over pure ibuprofen. Preliminary results of this study suggested that the preparation of ibuprofen SDs using PEG 8000 as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution and bioavailability of ibuprofen.

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Cited by 66 publications

References 6 publications

Formulation and evaluation of mefenamic acid sustained release matrix pellets

Formulation and evaluation of mefenamic acid sustained release matrix pellets

Design and statistical optimization of glipizide loaded lipospheres using response surface methodology

Enhancement of Solubility, Dissolution and Bioavailability of Ibuprofen in Solid Dispersion Systems

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