Effect of the melt granulation technique on the dissolution characteristics of griseofulvin

Yang, Dong; Kulkarni, Rajesh; Behme, Robert J.; Kotiyan, P.N

doi:10.1016/j.ijpharm.2006.08.029

Cited by 66 publications

(38 citation statements)

References 19 publications

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“…6 It has been reported that PEG has the ability to increase the wettability and dispersibility of the mixture directly after contact with water. 29, 30 Therefore, PEG 3350 was incorporated into the HME process to facilitate the extrusion process as well as improve drug release by increasing the capability of the matrix to absorb more media and increase drug-polymers dispersibility, leading to increased drug release. Adding PEG 3350 to the formulations enhances the drug release dissolution to 10–30% of the binary mixture by inhibiting aggregation and agglomeration.…”

Section: Resultsmentioning

confidence: 99%

Investigation of the combined effect of MgO and PEG on the release profile of mefenamic acid prepared via hot-melt extrusion techniques

Alshehri

Tiwari

Alsulays

et al. 2016

Pharmaceutical Development and Technology

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This study aimed to investigate the combined effect of magnesium oxide (MgO) as an alkalizer and polyethylene glycol (PEG) as a plasticizer and wetting agent in the presence of Kollidon® 12 PF and 17 PF polymer carriers on the release profile of mefenamic acid (MA), which was prepared via hot-melt extrusion (HME) technique. Various drug loads of MA and various ratios of the polymers, PEG 3350, and MgO were blended using a V-shell blender and extruded using a twin-screw extruder (16-mm Prism EuroLab, ThermoFisher Scientific) at different screw speeds and temperatures to prepare a solid dispersion system. Differential scanning calorimetry and X-ray diffraction data of the extruded material confirmed that the drug existed in the amorphous form, as evidenced by the absence of corresponding peaks. MgO and PEG altered the micro-environmental pH to be more alkaline (pH 9) and increased the hydrophilicity and dispersibility of the extrudates to enhance MA solubility and release, respectively. The in vitro release study demonstrated an immediate release for 2 h with more than 80% drug release within 45 min in matrices containing MgO and PEG in combination with PVP, when compared to the binary mixture, physical mixture, and pure drug.

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Section: Resultsmentioning

confidence: 99%

Investigation of the combined effect of MgO and PEG on the release profile of mefenamic acid prepared via hot-melt extrusion techniques

Alshehri

Tiwari

Alsulays

et al. 2016

Pharmaceutical Development and Technology

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show abstract

“…Polyethylene glycol is widely used as a molten binder due to its complimentary solution properties, low melting point, rapid solidification rate, low toxicity and little cost. The increase in dissolution rate can be ascribed to the hydrophilic character of the system due to the presence of water-soluble carriers and the fact that the drug forms monotectic mixtures with PEG 71,72 .…”

Section: Inclusion Complexesmentioning

confidence: 99%

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2011

IJPSR

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Most of the drugs in the developmental pipeline are emerging from the HighThroughput Screening methodology resulting in increased molecular weights and thus consequential bioavailability problems. The bioavailability issue can be due to insufficient solubility of permeability. Most compounds face the solubility problems. Hence, with the advancement of chemical science, the need of development of pharmaceutical technologies is also increasing. Pharmaceutical approaches to correct the bioavailability are definitely being cost-effective in comparison with chemical approaches which are also timeconsuming. Hence various methods of solubility enhancement are being developed. Each technique is with several merits and demerits. To tackle the disadvantages of conventional approaches, newer techniques are developed by many researchers. In this review, an attempt of comparing the conventional and novel techniques is done.

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“…There are many technologies currently used to prepare solid dispersion systems, which include solvent casting, spray drying and hot melt extrusion (HME) [11–13]. It is argued by many, among all of these techniques, that HME,[14] or melt extrusion, is the most promising techniques, which include advantages such as continuous processing, easy to scale up, solvent free fabrication and lower production costs [2,8,15–17]…”

Section: Introductionmentioning

confidence: 99%

“…[5,[7][8][9][10] There are many technologies currently used to prepare solid dispersion systems, which include solvent casting, spray drying and hot melt extrusion (HME). [11][12][13] It is argued by many, among all of these techniques, that HME, [14] or melt extrusion, is the most promising techniques, which include advantages such as continuous processing, easy to scale up, solvent free fabrication and lower production costs. [2,8,[15][16][17] For most of the HME formulations, polymer carriers entail a large proportion of all of the components, which performs the role of recrystallization inhibitor, as well as that of the dissolution controller.…”

Section: Introductionmentioning

confidence: 99%

The effects of polymer carrier, hot melt extrusion process and downstream processing parameters on the moisture sorption properties of amorphous solid dispersions

Feng

Patil

et al. 2016

Journal of Pharmacy and Pharmacology

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Objective The aim of this study was to evaluate the effect of polymer carrier, hot melt extrusion (HME) and downstream processing parameters on the water uptake properties of amorphous solid dispersions. Methods Three polymers and a model drug were used to prepare amorphous solid dispersions utilizing HME technology. The sorption-desorption isotherms of solid dispersions and their physical mixtures were measured by the Dynamic Vapor Sorption system, and the effect of polymer hydrophobicity, hygroscopicity, molecular weight and the HME process were investigated. FTIR imaging was performed to understand the phase separation driven by the moisture. Key findings Solid dispersions with polymeric carriers with lower hydrophilicity, hygroscopicity, and higher molecular weight could sorb less moisture under the high RH conditions. The water uptake ability of polymer-drug solid dispersion systems were decreased compared to the physical mixture after HME, which might be due to the decreased surface area and porosity. The FTIR imaging indicated the homogeneity of the drug molecularly dispersed within the polymer matrix was changed after exposure to high RH. Conclusion Understanding the effect of formulation and processing on the moisture sorption properties of solid dispersions is essential for the development of drug products with desired physical and chemical stability.

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Effect of the melt granulation technique on the dissolution characteristics of griseofulvin

Cited by 66 publications

References 19 publications

Investigation of the combined effect of MgO and PEG on the release profile of mefenamic acid prepared via hot-melt extrusion techniques

Investigation of the combined effect of MgO and PEG on the release profile of mefenamic acid prepared via hot-melt extrusion techniques

Untitled

The effects of polymer carrier, hot melt extrusion process and downstream processing parameters on the moisture sorption properties of amorphous solid dispersions

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