Comparison of polyethylene glycol and polyoxyethylene stearate as excipients for solid dispersion systems of griseofulvin and tolbutamide II

Kaur, Rabinder; Grant, David J.W.; Eaves, T.

doi:10.1002/jps.2600691122

Cited by 42 publications

(17 citation statements)

References 13 publications

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“…Technically, a cooling curve exhibiting eutectic halt is the best method for constructing eutectic phase diagram;29 however, PEGs are viscous, and most drugs, including fenofibrate, exhibit high degree of supercooling, making the generation of the cooling curves difficult. The heating method used to construct Figure 2 has been accepted in the field of pharmaceutics 30,31…”

Section: Resultsmentioning

confidence: 99%

Properties of Rapidly Dissolving Eutectic Mixtures of Poly(ethylene glycol) and Fenofibrate:The Eutectic Microstructure

Law

Wang

Schmitt

et al. 2003

Journal of Pharmaceutical Sciences

115

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Section: Resultsmentioning

confidence: 99%

Properties of Rapidly Dissolving Eutectic Mixtures of Poly(ethylene glycol) and Fenofibrate:The Eutectic Microstructure

Law

Wang

Schmitt

et al. 2003

Journal of Pharmaceutical Sciences

115

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“…Many workers have reported increased drug release owing to addition of hydrophilic excipient to lipid carriers. [21][22][23] Granules containing Gelucire:EC mixture (1:0.5) have shown significant retardation of drug release without hampering the floatability. The surface hydrophobicity imparted to the drug particle by the hydrophobic lipid coat was responsible for floating behavior.…”

Section: Resultsmentioning

confidence: 99%

Preparation and evaluation of diltiazem hydrochloride-gelucire 43/01 floating granules prepared by melt granulation

et al. 2004

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The basic objective of this study was to explore the application of Gelucire 43/01 for the design of multi-unit floating systems of a highly water-soluble drug diltiazem HCl. Diltiazem HCl-Gelucire 43/01 granules were prepared by melt granulation technique. The granules were evaluated for in vitro and in vivo floating ability, surface topography, and in vitro drug release. Aging effect on storage was evaluated using scanning electron microscopy, hot stage polarizing microscopy (HSPM), differential scanning calorimetry (DSC), and in vitro drug release. Granules were retained in stomach at least for 6 hours. Approximately 65% to 80% drug was released over 6 hours with initial fast release from the surface. Surface topography, HSPM, DSC study of the aged samples showed phase transformation of Gelucire. The phase transformation also caused significant increase in drug release. In conclusion, hydrophobic lipid, Gelucire 43/01, can be considered as an effective carrier for design of a multi-unit floating drug delivery system of highly water-soluble drugs such as diltiazem HCl.

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“…The authors observed that the dissolution rate of tablet was highly sensitive to compression pressure. The sticking of solid dispersion to dies and punches might become so problematic that Kaur et al 38 resorted to placing small pieces of grease-proof paper between metal surfaces and granules before the compression of tablets.…”

Section: Reproducibility Of Physicochemical Propertiessmentioning

confidence: 98%

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

Serajuddin

1999

Journal of Pharmaceutical Sciences

1,431

780

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Although there was a great interest in solid dispersion systems during the past four decades to increase dissolution rate and bioavailability of poorly water-soluble drugs, their commercial use has been very limited, primarily because of manufacturing difficulties and stability problems. Solid dispersions of drugs were generally produced by melt or solvent evaporation methods. The materials, which were usually semisolid and waxy in nature, were hardened by cooling to very low temperatures. They were then pulverized, sieved, mixed with relatively large amounts of excipients, and encapsulated into hard gelatin capsules or compressed into tablets. These operations were difficult to scale up for the manufacture of dosage forms. The situation has, however, been changing in recent years because of the availability of surface-active and self-emulsifying carriers and the development of technologies to encapsulate solid dispersions directly into hard gelatin capsules as melts. Solid plugs are formed inside the capsules when the melts are cooled to room temperature. Because of surface activity of carriers used, complete dissolution of drug from such solid dispersions can be obtained without the need for pulverization, sieving, mixing with excipients, etc. Equipment is available for large-scale manufacturing of such capsules. Some practical limitations of dosage form development might be the inadequate solubility of drugs in carriers and the instability of drugs and carriers at elevated temperatures necessary to manufacture capsules.

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Comparison of polyethylene glycol and polyoxyethylene stearate as excipients for solid dispersion systems of griseofulvin and tolbutamide II

Cited by 42 publications

References 13 publications

Properties of Rapidly Dissolving Eutectic Mixtures of Poly(ethylene glycol) and Fenofibrate:The Eutectic Microstructure

Properties of Rapidly Dissolving Eutectic Mixtures of Poly(ethylene glycol) and Fenofibrate:The Eutectic Microstructure

Preparation and evaluation of diltiazem hydrochloride-gelucire 43/01 floating granules prepared by melt granulation

Solid dispersion of poorly water‐soluble drugs: Early promises, subsequent problems, and recent breakthroughs

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