• 한국분말재료학회지
• /
• 제31권3호
• /
• pp.263-271
• /
• 2024

This study focused on improving the solubility of silodosin, a drug poorly soluble in water, by utilizing solid dispersions. Three types of dispersions were examined and compared against the drug powder: surface-attached (SA), solvent-wetted (SW), and solvent-evaporated (SE). Polyvinyl alcohol (PVA) was identified as the most effective polymer in enhancing solubility. These dispersions were prepared using spray-drying techniques with silodosin and PVA as the polymer, employing solvents such as water, ethanol, and a water-acetone mix. The physicochemical properties and solubility of the dispersions were evaluated. The surface-attached dispersions featured the polymer on a crystalline drug surface, the solvent-wetted dispersions had the amorphous drug on the polymer, and the solvent-evaporated dispersions produced nearly round particles with both components amorphous. Testing revealed that the order of improved solubility was: solvent-evaporated, solvent-wetted, and surface-attached. The results demonstrated that the preparation method of the solid dispersions significantly impacted their physicochemical properties and solubility enhancement.

• Journal of Pharmaceutical Investigation
• /
• 제19권2호
• /
• pp.63-69
• /
• 1989

Dissolution characteristics of indomethacin (IMC) from hydrophobic polymer solid dispersions were investigated. IMC-polyvinyl chloride (PVC) and IMC-ethylcellulose (EC) solid dispersions were prepared. The dissolution patterns of pure IMC, IMC-PVC and IMC-EC solid dispersions prepared at various ratios (1:1, 1:3, 1:5, 1:9 and 1:19 w/w), and those of corresponding physical mixtures were compared. It was found that the dissolution rates of IMC from solid dispersions with PVC or EC decreased in the order of 1:1>1:3>1:5>1:9>1:19 as the drug to polymer ratios decreased. Also the dissolution rates of IMC from EC solid dispersions increased according to flow rate, but PVC solid dispersions were not affected significantly. After all, PVC and EC matrices could be applied in sustained-release preparation of IMC.

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.412.2-413
• /
• 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
• /
• 제32권3호
• /
• pp.191-197
• /
• 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.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1997년도 춘계학술대회
• /
• pp.118-118
• /
• 1997

Solid dispersions were used to increase the dissolution rate of biphenyl dimethyl dicarboxylate (DDB) in water, with the ultimate goal of optimizing its bioavailability when incoporated into pharmaceuticals. Carriers used were Kollidon 30, Kollidon VA 64, 2-hydroxypropyl-${\beta}$-cyclodextrin (HPCD), sodium salicylate or sodium benzoate. DDB solid dispersions were prepared at drug to carrier proportions ranging from 1 : 5 to 1 : 20 (w/w) by solvent evaporation method. DDB tablets (7.5 mg) were prepared by compressing the powder mixture composed of solid dispersions, lactose, corn starch, crospovidone and magnesium stearate using a single-punch press. DDB capsules (7.5 mg) were prepared by filing the mixture into empty hard gelatin capsules (size #1). Dissolution studies of DDB from powdered solid dispersions, tablets and capsules were performed in 900 $m\ell$ of water at 100 rpm and 37$^{\circ}C$ by the paddle method. The dissolved amount was assayed by HPLC and expressed as the mean(%)of three determinations.

• Journal of Pharmaceutical Investigation
• /
• 제29권3호
• /
• pp.227-234
• /
• 1999

Solid dispersions were prepared to increase the dissolution rate of biphenyl dimethyl dicarboxylate (DDB) using water-soluble carriers such as povidone, copolyvidone, $2-hydroxypropyl-{\beta}-cyclodextrin (HPCD)$, sodium salicylate or sodium benzoate by solvent evaporation method. Solid dispersions were characterized by infrared spectrometry, differential scanning calorimetry (DSC) and powder X-ray diffractometry, dissolution and permeation studies. DDB tablets (7.5 mg) were prepared by compressing the powder mixtures composed of solid dispersions, lactose, com starch, crospovidone and magnesium stearate using a single-punch press. DDB capsules (7.5 mg) were also prepared by filling the mixtures in empty hard gelatin capsules (size No.1). From the DSC and powder x-ray diffractometric studies, it was found that DDB was amorphous in the HPCD or copolyvidone solid dispersions. Dissolution rates after 10 min of DDB alone and solid dispersions (1 : 10) in sodium benzoate, sodium salicylate and copolyvidone were 11.8, 23.5, 22.8 and 82.5%, respectively. Dissolution rates of DDB after 30 min from 1 : 10 and 1 : 20 copolyvidone solid dispersions were 80.5 and 95.0%, respectively. For the DDB tablets prepared using solid dispersions (1 : 20), the initial dissolution rate was dependent on carrier material, and was ranked in order, $Kollidon\;30\;{\ll}$ copolyvidone < HPCD. For the HPCD solid dispersion tablets, dissolution rate reached 97.4% after 15 min, but thereafter slowly decreased to 80.7% after 2 hr due to the precipitation of DDB. However, in the case of copolyvidone solid dispersion tablets, dissolution increased linearly and reached 93.4% after 2 hr. Reducing the volume of test medium from 900 to 300 ml markedly decreased the dissolution rate of the tablets containing 1 : 20 HPCD solid dispersions and 1 : 10 copolyvidone solid dispersion. For 1 : 20 copolyvidone solid dispersion tablets, there was no significant change in dissolution rate up to 1 hr with different volumes of test medium. Preparation of the copolyvidone solid dispersion (1 : 20) in capsules markedly delayed the dissolution (31.2 % after 2hr) due to the limited diffusion within capsules. The permeation rate $(13.4\;g/cm^2\;after\;8\;hr)$ of DDB through rabbit duodenal mucosa from copolyvidone solid dispersion (1 : 10) was markedly enhanced, when compared with drug alone or physical mixtures. From overall findings, DDB formulations containing copolyvidone solid dispersions (1 : 20) could be used to remarkably improve the dissolution rate in dosage form of powders and tablets.

• KSBB Journal
• /
• 제26권4호
• /
• pp.283-292
• /
• 2011

Solid dispersion is one of well-established pharmaceutical techniques to improve the dissolution and consequent bioavailability of poorly water soluble drugs. It is defined as a dispersion of drug in an inert carrier matrix. Solid dispersions can be classified into three generations according to the carrier used in the system. First and second generations consist of crystalline and amorphous substances, respectively. Third generation carriers are surfactant, mixture of polymer and surfactants, and mixture of polymers. Solid dispersions can be generallyprepared by melting method and solvent method. While melting method requires high temperature to melt carrier and dissolve drug, solvent method utilizes solvent to dissolve the components. The improvement in dissolution through solid dispersions is attributed to reduction in drug particle size, improvement in wettability, and/or formation of amorphous state. The primary characteristics of solid dispersions, the presenceof drug in amorphous state, could be determined by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and fourier-transformed infrared spectroscopy (FTIR). In spite of the significant improvement in dissolution by solid dispersion technique, some drawbacks have limited the commercial application of solid dispersions. Thus, further studies should be conducted in a direction to improve the congeniality to commercialization.

• 천문학회보
• /
• 제36권2호
• /
• pp.62.2-62.2
• /
• 2011

The correlation between black hole mass and stellar velocity dispersion provides an important clue on the black hole growth and galaxy evolution. In the case of AGN, however, it is extremely difficult to measure stellar velocity dispersions in the optical since AGN continuum dilutes stellar absorption features. In contrast, stellar velocity dispersions of active galaxies can be measured in the near-IR, where AGN-to-star flux ratio is much smaller. Expecting that more stellar velocity dispersion measurements will be available using future near-IR facilities, it is crucial to test whether the stellar velocity dispersions measured from the near-IR spectra are consistent with those measured from the optical spectra. For a sample of 35 nearby galaxies, for which optical stellar velocity dispersion measurements and dynamical black hole masses are available, we obtained high quality H-band spectra, using the TripleSpec at the Palomar 5-m Telescope, in order to calibrate the stellar velocity dispersions and define the $M_{BH}-sigma_*$ relation in the near-IR. Based on the spatially resolved kinematics, we correct for the rotation component and determine the luminosity-weighted stellar velocity dispersion of the spheroid component in each galaxy. In this presentation, we will show the comparison between optical and near-IR stellar velocity dispersion measurements and define the $M_{BH}-sigma_*$ relation based on uniformly measured stellar velocity dispersion in the near-IR.

• Journal of Pharmaceutical Investigation
• /
• 제26권1호
• /
• pp.23-28
• /
• 1996

The dissolution characteristics of DDB were markedly enhanced by preparing solid dispersions of drug with polyethylene glycol 6000. Solid dispersions of various weight fraction were formed by a melting method. And various tablets$(A{\sim}E)$ were prepared from these solid dispersions with excipients (lactose, com starch, Avicel and PVP) by wet granulation method. There were no significant differences in dissolution rates between physical mixture and DDB alone. But dissolution rates of solid dispersions were $1.4{\sim}2.0$ times greater than that of DDB alone and $1.2{\sim}1.8$ times greater than those of a commercial tablet.

• 한국도로학회논문집
• /
• 제18권4호
• /
• pp.77-82
• /
• 2016

PURPOSES : This paper proposes a reliability index for the safety evaluation of freeway sections. It establishes a reliability index as a safety surrogate on freeways considering speeds and speed dispersions. METHODS : We collated values of design elements including radii, curve lengths, vertical slopes (absolute values), superelevations, and vertical slopes from seven freeway sections in Korea. We also collected data about driving speeds, traffic accidents, and their deviations. We established a reliability index using these variables. RESULTS : The average radii, curve lengths, and superelevations are highly correlated with the incidence of traffic accidents. Deviations in radius and curve lengths show an especially high correlation. The reliability index, derived from speed and speed dispersions of the seven freeway sections, also correlated highly with accidents with a correlation index of 0.63. CONCLUSIONS : Since the reliability index obtained from speed and speed dispersions are highly correlated with traffic accidents, we conclude that a reliability index can be a safety surrogate on freeways considering speeds and speed dispersions together in terms of design and operational levels.