• Journal of Pharmaceutical Investigation
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• 제33권3호
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• pp.245-253
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• 2003

Dissolution profile comparsions can be done by virtue of the similarity factor $(f_2)$. It is a logarithmic reciprocal square root transformation of the sum of squared error of % dissolution differences between two profiles at several time points. It gives information on the degree of similarity between the two profiles: An $f_2$ value between 50 and 100 suggests the similarity/equivalence of the two dissolution curves being compared. The objective of this report was to provide a careful examination on the $f_2$ metrics in detail. It was shown that $f_2$ values exceeded 50, when relative differences in % dissolved between two products were less than 15% at all time points. The similarity factor value was also found to be greater than 50, in cases when absolute % dissolution differences were below 10% at all time points. Interestingly, the $f_2$ value was changed by the number of the time points selected for calculation. In particular, $f_2$ tended to have higher values, when the $f_2$ metrics used a large number of time points in which % dissolved reached plateau. Finally, since the similarity factor was a sample statistics, it was impossible to infer type I/II errors and sampling error. Despite certain limitations inherited in the $f_2$ metrics, it was easy and convenient to evaluate how similar the two dissolution profiles were.

• 약학회지
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• 제44권5호
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• pp.424-431
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• 2000

A biopharmaceutics drug classification system for correlation between in vitro dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling the rate and extent of drug absorption. The objective of this study was to assess whether in vitro dissolution profiles of immediate-release beta-blocker tablets can be correlated with intestinal membrane permeability and/or in vivo bioavailability In vitro dissolution of the beta-blocker tablets was examined using KP VII Apparatus II methods at various pH. Intestinal membrane permeability was determined in vitro using the diffusion chamber method. Bioavailablity parameters were cited from literatures. The dissolution profiles did not accurately represent the in vivo bioavailablity However there were good correlations between intestinal membrane permeability and log P (noctanol/buffer). The correlations obtained in this study indicated that in vitro diffusion chamber method could be used to predict intestinal absorption in vivo.

• Journal of Pharmaceutical Investigation
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• 제14권3호
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• pp.122-130
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• 1984

The dissolution profiles of the seven branded prednisolone tablets were determined by means of available compendium. Those tablets were stored at $40^{\circ}C,\;50^{\circ}C\;and\;60^{\circ}C$ for 15, 30 and 60 days respectively. Under the stress conditions, the dissolution efficiency showed significant changes. It is considered that the determination of shelf life of drug from these aging effects is possible because the dissolution data followed a logarithmic distribution. There were no substantial differences of dissolution between two prednisolone formulations with different particle size not larger than $100\;{\mu}m$. The effect of two starches (corn and potato) on the rate of dissolution of prednisolone from dosage form was also investigated. All marketed tablets met the requirement of the established compendium.

• 약학회지
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• 제39권6호
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• pp.593-599
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• 1995

Erythromycin was formulated as enteric-coated pellets in order to reduce degradation in stomach and gastromtestmal irritation, and to maximize the absorption in intestine followmg its oral administration. Core pellets were prepared using fluid-bed granulator with two different methods (powder layering and solvent spraying) and enteric-coated with two different coating polymers (HPMCP and Eudragit E30D). Physical characteristics md dissolution rates of core pellets and enteric-coated pellets were evaluated to optimize the formulation. Powder layering method resulted in shorter initial dissolution time than solvent spraying method, but physicochmical properties of the product were worse than solvent spraying method with respect to hardness, ftiability and density. The dissolution rate of the drug was increased with the addition of surfactants, showing concentration-dependence. The scanning electron microscopic observation of pellets revealed significant differences on the surface appearances prepared with solvent spraying method. The core pellet made with powder layering method had crystals on the surface, which resulted in poor physical properties of the pellets. The dissolution profiles of erythromycin pellets coated with HPMCP or Eudragit L30D were close to that of commercially available erythromycin enteric-coated product.

• Journal of Pharmaceutical Investigation
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• 제30권2호
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• pp.85-91
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• 2000

We have studied the dissolution kinetics of two fast releasing tablets in four media, and the similarity of dissolution profiles was compared using 3 methods. Two of the methods were introduced from statistical algorithm of distance methods, which are maximum distance and Mahalanobis distance. The dissolution kinetics were also analysed using FDA method for similarity evaluation, and the results were compared with those obtained using the distance methods.

• 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.

• Journal of Pharmaceutical Investigation
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• 제32권3호
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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.

• 약학회지
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• 제56권4호
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• pp.211-216
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• 2012

Drug dissolution test has been used for the purpose of both quality control of solid oral dosage forms and predicting in vivo drug release profiles. In this study, the dissolution profiles of buflomedil hydrochloride tablets and ticlopidine hydrochloride tablets were investigated according to the "Guidelines on Specifications of Dissolution tests for Oral dosage forms" of Korean Pharmacopoeia (KP). The analytical method using HPLC was validated. The validation was performed in terms of specificity, linearity, accuracy, precision and limit of quantitation.

• Archives of Pharmacal Research
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• 제24권6호
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• pp.568-571
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• 2001

The purpose of this work was to study the effect of storage time and temperature on the in vitro release kinetics of a commercial sustained-release dosage form of theophylline, at different pHs of the dissolution medium. The formulation was stored at $35^{\circ}C$ for 16 months and at $45^{\circ}C$ for 8 months, with a relative humidity of 60%. The in vitro release tests were performed at pHs 2, 4, 6 and 7.4. The mean values of the transport coefficient n, were close to 0.5 in all the conditions tested, which indicates that the transport system is not modified after storage of the formulation at $35^{\circ}C$ and $45^{\circ}C$. The mean values of the dissolution rate constant ranged from 0.036 to 0.043 $min^{-n}$, under all the conditions tested. Significant differences (${\alpha}=0.05$) were found between pHs 2, 4 and 6, 7.4 for all the model-independent parameters studied. When the formulation was kept at $35^{\circ}C$ for 16 months, the mean percentage of drug dissolved at 8 hours was 25.61% (pHs 2, 4) and, 36.12% (pHs 6, 7.4), representing a 26% and 24% reduction, respectively. Simitar results were obtained after storing the formulation at $45^{\circ}C$ for 8 months, corresponding to 33.3% (pHs 2, 4) and, 22.5% (pHs 6, 7.4) diminution, respectively. The values of the similarity factory $f_2$, obtained were lower than 50, which indicates the lack of similarity among the dissolution profiles, after storing the formulation under the experimental Conditions tested.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.309.1-309.1
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• 2003

The purposes of this study were to evaluate bioequivalence (BE) using In-transformed pharmacokinetic parameters obtained from two risperidone products and to develop the analytical methods for the quantitative determination of risperidone in human serum. In addition, the in vitro dissolution profiles of the two risperidone products in various dissolution media: pH 1.2, 4.0, 6.8 and water (KP VII Apparatus II method) were assesed. (omitted)