• Journal of Pharmaceutical Investigation
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• v.40 no.spc
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• pp.97-102
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• 2010

A novel surface-attached solid dispersion is designed to improve the solubility and oral bioavailability of poorly water-soluble drugs without crystalline change. Accordingly, it draws increasing interest because of excellent stability and no pollution for accomplishing enhanced solubility and bioavailability, which have recently been highlighted in connection with a number of higher value-added poorly water-soluble drugs. In addition, excellent stability can be attained when the poorly water-soluble drugs are not dissolved but dispersed in water and provide no crystallinity change. This solid dispersion is given by means of attaching the dissolved carriers such as hydrophilic polymer and surfactant to the surface of dispersed drug particles followed by changing the hydrophobic drug to hydrophilic form. The aim of the present review is to outline the preparation, physicochemical property and bioavailability of novel surface-attached solid dispersion with improved solubility and bioavailability of poorly water-soluble drugs without crystalline change.

• Journal of Pharmaceutical Investigation
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• v.32 no.3
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• pp.191-197
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• 2002

Polymer based physical mixtures or solid dispersions containing solubilizing compositions[OA, tween80 and SLS] were prepared using a spray-dryer. Lovastatin(LOS), simvastatin(SIMS), aceclofenac(AFC) and cisapride(CSP) were selected as poorly water-soluble drugs. Dextrin, poly(vinylalcohol) (PVA), poly(vinylpyrrolidone)(PVP) and polyethylene glycol(PEG) were chosen as solubilizing carriers for solid dispersions. The solid dispersions containing solubilizing compositions without drug were prepared without using organic solvents or tedious changes of formulation compositions. This system could be used to quickly screen the dissolution profiles of poorly water-soluble drugs by simply mixing with drugs thereafter. In case of solid dispersion containing drug, organic solvent systems could be used to solubilize model drugs. The dissolution rates of the drugs were higher when mixed with drug and solid dispersions containing solubilizing compositions. However, solid dispersions of LOS, AFC, and CSP simultaneously containing drug and solubilizing compositions in organic solvent systems were more useful than physical mixtures of drug and solid dispersions without drug except SIMS. Based on solubilizing capability of polymer based physical mixtures in gelatin hard capsules, optimal solid dispersion system of poorly water-soluble drugs could be formulated. However, it should be noted that dissolution rate of poorly water-soluble drugs were highly dependent on drug properties, solubilizing compositions and polymeric carriers.

• Proceedings of the PSK Conference
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• 2003.10a
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• pp.50-53
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• 2003

Aceclofenac (AFC) as a model has poor solubility in water, resulting in lower dissolution rate and bioavailability. A solid dispersion (SD) is one of effective methods to enhance the solubility or dissolution rate of various poorly water-soluble drugs. Polyvinylpyrrolidone (PVP) that is a nontoxic, water-soluble and generally applicable pharmaceutical excipient has been widely used as a carrier in the preparation of solid dispersions. (omitted)

• Journal of Pharmaceutical Investigation
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• v.20 no.4
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• pp.193-198
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• 1990

To increase the dissolution rate of furosemide, cogrinding or coprecipitating of furosemide with povidone was carried out. The ground mixture of furosemide with povidone was prepared by cogrinding in a ceramic ball mill and the coprecipitate was prepared by solvent method using methanol. The povidone ground mixture and the coprecipitate showed a faster and more enhanced dissolution rate than the physical mixture or intact furosemide. The IR, DTA and TGA studies showed the physicochemical modifications of furosemide from the ground mixture and the coprecipitate. An interaction, in the ground mixture and in the coprecipitate, such as association between the functional groups of furosemide and povidone might occur in the molecular level. The coprecipitating and cogrinding techniques with povidone provided a promising way to increase the dissolution rate of poorly soluble drugs.

• Carbon letters
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• v.27
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• pp.18-25
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• 2018

In this study, graphene oxide(GO) was used as drug carriers to amorphize poorly watersoluble drugs via a co-spray drying process. Two poorly water-soluble drugs, fenofibrate and ibuprofen, were investigated. It was found that the drug molecules could be in the graphene nanosheets in amorphous or nano crystalline forms and thus have a significantly enhanced dissolution rate compared with the counterpart crystalline form. In addition, the dissolution of the amorphous drug enwrapped with the graphene oxide was higher than that of the amorphous drug in activated carbon (AC) even though the AC possessed a larger specific surface area than that of the graphene oxide. The amorphous formulations also remained stable under accelerated storage conditions ($40^{\circ}C$ and 75% relative humidity) for a study period of 14 months. Therefore, graphene oxide could be a potential drug carrier and amorphization agent for poorly water-soluble drugs to enhance their bioavailability.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.412.2-413
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• 2002

Purpose. To prepare polymer based physical mixtures or solid dispersions containing solubilizing compositions using a spray-dryer. Methods. Lovastatin.simvastatin.aceclofenac and cisapride were selected as poorly water-soluble drugs. Dextrin. poly(vinylalcohol). poly(vinylpyrrolidone)and polyethylene glycol were chosen as solubilizing carriers for solid dispersions. The solid dispersions containing solubilizing compositions without drug were prepared without using organic solvents or tedious changes of formulation compositions. (omitted)

• Journal of Pharmaceutical Investigation
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• v.25 no.1
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• pp.31-36
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• 1995

Solid dispersions and inclusion complex were prepared for the enhancement of solubility and dissolution rate of poorly water-soluble ibuprofen(IPF) as a model drug. Polyethylene glycol 4000(PEG4000) and polyvinylpyrrolidone(PVP) were used for the preparation of solid dispersion. $2-Hydroxypropyl-{\beta}-cyclodextrin(2-HP{\beta}CD)$ was also used for the preparation of inclusion complex. The solubility of IPF increased as the concentration of PEG4000, PVP and $2-HP{\beta}CD$ increased. Solubilization capacity of $2-HP{\beta}CD$ was increased about 10 times when compared to PEG 4000 and PVP. The dissolution rate of drug from solid dispersions and inclusion complex in the simulated gastric fluid was enhanced when compared to pure IPF and commercial $BR4^{\circledR}$ tablet as a result of improvement of solubility. In case of solid dispersions, dissolution rate of drug was proportional to polymer concentration in the formulation. The marked enhancement of dissolution rate of drug by inclusion complexation with $2-HP{\beta}CD$ was noted. However, dissolution rate of drug from solid dispersions and inclusion complex in the simulated intestinal fluid was not significant because IPF was readily soluble in that condition. From these findings, water-soluble polymers and cyclodextrin were useful to improve solubility and dissolution rate of poorly water-soluble drugs. However, easiness and reliability of preparation method, scale-up and cost of raw materials must be considered for the practical application of solid dispersion and inclusion complex in pharmaceutical industry.

• Proceedings of the PSK Conference
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• 2001.04a
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• pp.229.2-230
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• 2001

• Proceedings of the PSK Conference
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• 2001.10a
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• pp.295.3-296
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• 2001

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.225.2-226
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• 2003

The prolonged mechanical grinding process may enhance the bioavailability of the drugs due to the change of solid state such as micronization and decrease of crystallinity. A series of attempts to enhance the bioavailability of insoluble drugs have been made by the fine grinding technique using a planetary mill. The objective of the present study is to investigate the possibility of improving the dissolution properties of poorly water- soluble drugs such as diphenyl hydrantoin (phenytoin) and diphenyl dimethyl dicarboxylate (DDB) based on the molecular interaction between drug and additives during pharmaceutical processing to be related with the bioavailability behavior. (omitted)