• Journal of Pharmaceutical Investigation
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• 제12권3호
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• pp.55-63
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• 1982

The dissolution kinetics for polymorphs of sulpiride, the effect of polyethylene glycol 4000 on the dissolution kinetics of sulpiride polymorphs and the dissolution rate difference between the tablets of polymorph form I and form II were investigated. The results could be summerized as followings: 1. The dissolution rates of two polymorphs of sulpiride were significantly different and the thermodynamic parameters calculated from dissolution kinetics were as follows; transition temperature $98^{\circ}C$, enthalpy change, -2.108 kcal/mole, free energy change, -783 cal/mole $(31.0^{\circ}C)$. 2. The dissolution rates of the two polymorphs of sulpiride containing polyethylene glycol 4000 were significantly diefferent in 0.01N HCl but the effect of polyethylene glycol on the dissolution rates of two polymorphs was not significant at low concentration of polyethylene glycol 4000. The study on the effect by stirring speed showed that at lower stirring speed the promotion rate of dissolution of polymorph form I is greater than that of form II. 3. In the case of tablets the dissolution rates of polymorph form I of sulpiride was two fold as compared with the results obtained from form II.

• Journal of Pharmaceutical Investigation
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• 제25권1호
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• pp.37-46
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• 1995

The experiment was designed to investigate the sustained release dosage form of silymarin (SL) from chitosan (CS) carrier. Solid dispersed system was prepared by mixing the drug with chitosan. This solid dispersed system was cross-linked by glutaraldehyde, formaldehyde, acetaldehyde and butylaldehyde, respectively. The dissolution rates of these preparations were compared with each other in vitro. The silymarin was mired with anionic alginate gel and bead was prepared by dropping this mixture to cationic chitosan solution including calcium chloride. Chitosan encapsulated alginate bead after drying in the oven was investigated for the dissolution rate. The dissolution rate of SL-CS mixture was delayed with increase in the amounts of CS and the concentration of aldehyde. The effect on the delay of dissolution rate was in the increasing order of formaldehyde, glutaraldehyde, acetaldehyde, butylaldehyde. The dissolution rate of chitosan encapsulated alginate bead was parallel with the concentration of chitosan in diluted hydrochloric acid solution and delayed with increase in the concentration of chitosan in phosphate buffer solution.

• Journal of Pharmaceutical Investigation
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• 제20권2호
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• pp.79-88
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• 1990

A numerical model for diffusion and dissolution controlled transport from dispersed matrix is presented. The rate controlling process for transport is considered to be diffusion of drug through a concentration gradient coupled with time-dependent surface change and/or disappearance of the dispersed drug in response to the dissolution. The transport behavior of drug was explained in terms of ${\nu}$ parameter: ${\nu}$ value means a ratio of diffusion time constant and dissolution time constant. This general model has wide range of application from where release is controlled by the diffusion rate to where release is governed by the dissolution rate. Based on this model, theoretical drug concentration, particle size distributions in the polymer matrix system and the resulting release rate were also investigated.

• Archives of Pharmacal Research
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• 제18권1호
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• pp.22-26
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• 1995

The solubility and dissolution rate of naproxen (NPX) complexed with 2-hydroxypropyl-.betha.-cyc-lodextrin (2-HP.betha.CD) using coprecipitation, evaporation, freeze-drying and kneading method were investigated. Solubility of NPX linearly increased (correlation cefficient, 0.995) as $2-HP\betaCD$ concentraction increased, resutling in $A_l$ type phase solubility curve. Inclusion complexes prepared by four different methods were compared by different methods were compared by dfferential scanning calorimetry(DSC). The NPX showed sharp endothemic peak around $156^{\circ}C$ but inclusion complexes by evaporation, freeze-drying and kneading method showed very broad peak without distinct phase transtion temperature. In contrast, inclusion complex prepared by coprecipitation method resulted in detectable peak around $156^{\circ}C$ which is similar to NPX, suggesting incoplete formation of indusion co plex. Dissolution rate of inclusion complexes prepared by evaporation, frezz-drying and kneding except coprecipitation method was largely enhanced in the simultaed gastric and intestinal fluid when compared to NPX powder and commercial $NA-XEN^\registered$tablet. However, about 65% of NPX in gstric fluid. in case of inclusion complex prepared by coprecipitation method, formation of inclusion complex appeared to be incoplete, resulting in no marked enhancement of dissolution rate. From these findings, inclusion complexes of poorly water-soluble NPX with $2-HP\betaCD$ were useful to increase soubility and dissolution rate, resting in enhancement of bioavailability and minimization of gastrointestinal toxicity of drug upon oral administration of inclusion complex.

• Journal of Pharmaceutical Investigation
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• 제13권3호
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• pp.100-103
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• 1983

Coprecipitates of sulpiride and polyethylene glycol (PEG) decrease the dissolution rate of sulpiride and the degree of decrease is reversely proportional to molecular size of PEG and proportional to increase of PEG ratios in coprecipitates. The physical mixtures of sulpiride and PEG increase the dissolution rate of sulpiride.

• Journal of Pharmaceutical Investigation
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• 제20권2호
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• pp.65-71
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• 1990

Some studies reported physicochemical factors of drugs affecting solubility and dissolution rate. However, few have been reported about pharmaceutical application of crystal forms (habits). Therefore, using acetylsalicylic acid and phenacetin as model substances, we monitored the effects of crystal forms on the dissolution rates.

• Journal of Pharmaceutical Investigation
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• 제19권1호
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• pp.1-7
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• 1989

Coprecipitates of ibuprofen (IPF)-sodium deoxycholate (DC-Na) were prepared at various mixing ratios of IPF to DC-Na. X-ray diffraction measurments indicated that IPF in 1:3 and 1:5 IPF-DC-Na coprecipitate did not exist in the crystal form, however in the 1:8 coprecipitate, IPF remained its crystalline form. The dissolution rate was tested in pH 7.4 phosphate buffer by the paddle method of dissolution test of KP V. The dissolution rates of IPF from 1:1, 1:3, 1:5, 1:8 and 1:10(w/w) IPF-DC-Na coprecipitates and physical mixtures were compared with that of IPF alone. It was found that the dissolution rate of 1:5(w/w) coprecipitate was greater than that of pure IPF, coprecipitate and physical mixture at any other ratios of the two components. The concentration of IPF released from the IPF-DC-Na coprecipitates reached a plateau within 10 min, and thereafter gradually decreased indicating that IPF released from the coprecipitate was recrystallized due to the transient supersaturation.

• Journal of Pharmaceutical Investigation
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• 제28권4호
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• pp.267-274
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• 1998

Biphenyl dimethyl dicarboxylate (DDB) has been used for the treatment of acute and chronic hepatitis. However, its poor solubility in water, $2.5\;{\mu}g/ml$, caused low bioavailability of the drug after its oral administration. In order to increase the dissolution of DDB in gastrointestinal tracts, consequently to increase the bioavailability of the drug, DDB tablet was prepared with solid dispersion of DDB with poloxamer 338 or 407 using a direct compression method. To improve the flowability of the solid dispersion, Aerosil was used as an adsorbent. The effect of formulation variables (poloxamer and Aerosil contents) on the dissolution rate of DDB from tablets was investigated using an analysis of variance. The dissolution rate of DDB from tablets was evaluated with KP II (paddle) method. The dissolution patterns of the drug from the tablet prepared with poloxamer 407 were affected significantly by the contents of poloxamers and Aerosil over the range employed, but those of the drug from the tablet prepared with poloxamer 338 were not. The optimum formulation of the DDB tablet, showed the same dissolution pattern as that of the reference, was obtained after polynomial equations of drug dissolution profiles for each formula were fitted to contour plots. The optimum formulation ratios of DDB:poloxamer 407:Aerosil were 1:2.5:2.5 and 1:5:5.

• 설비공학논문집
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• 제19권12호
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• pp.850-856
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• 2007

In a supercooled or capsule type ice storage system, aqueous solution (or water) may have trouble with non-uniform dissolution though the system contributes to the simplicity of system and ecological improvement. The non-uniform dissolution increases the instability of the system because it may cause an ice blockage in pipe or cooling part. In order to observe the supercooled state, a cooling experiment was performed with pressurization to an ethylene glycol(EG) 3 mass% solution in stationary state. Also, the effect of the pressurization from 101 to 505 kPa to the dissolution of supercooled aqueous solution was measured with the dissolution time of the supercooled aqueous solution at a fixed cooling rate of brine. At results, the dissolution of supercooled point decreased as the pressure of the aqueous solution in the vessel increased. Moreover, the dissolution point increased as the heat flux for cooling increased.

• Journal of Pharmaceutical Investigation
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• 제38권1호
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• pp.51-55
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• 2008

To develop a novel metformin HCl-loaded GR type tablet, various tablets were compressed with poly acrylic acid (PAA) and hydroxypropylmethyl cellulose (HPMC) using a wet granulation, and their physical properties such as swelling rate, hardness and dissolution were then investigated. Among the formulae tested in this study, the tablet prepared with PAA 971 and 974 as disintegrants showed fastest dissolution rate and swelling rate. Furthermore, the tablets prepared with PAA and HPMC improved the swelling rate, hardness and dissolution compared to those prepared with only HPMC. Our results suggested that the tablets prepared with PAA 971, 974 and HPMC might be a potential candidate for gastric retention type tablets.