• YAKHAK HOEJI
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• v.44 no.6
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• pp.578-587
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• 2000

The purpose of the present study was to design and prepare the optimum formulation for the oral administration of titrated extract of the unsaponifiable fraction of Zea mays L. (ETIZM). For this purpose, we simulated the blood concentration of ETIZM after its oral administration, changing the dissolution rate constants $(0.05{\sim}20\;hr^{-1})$. In vivo parameters, such as absorption rate constant $(k_a)$, elimination rate constant (k) and volume of distribution (Vd), were incorporated in the simulation on the basis of the experiments and literatures. When the dissolution rate constant $(k_r)$ is over $5\;hr^{-1}$, the absorption process appears to be the rate limiting step for the transport of ETIZM from the G.I. ract to the blood circulation. While less than $5\;hr^{-1}$, the dissolution rate considered to be the rate limiting step. Moreover, the optimum blood concentration was shown in the range from 1 to $5\;hr^{-1}$ of $k_r$ in the simulation. To design and prepare the tablets on the basis of the above results, 7 formula containing HPMC, PEG 4000 and PEG 6000 (1-5%, respectively) were prepared and evaluated. The tablets containing PEG 4000 (1%), PEG 6000 (1%) or PEG 4000 (5%) satisfy the optimum $k_r$ range ($1-5\;hr^{-1}$). These formulations, therefore, will be able to show the more effective blood concentration, compared with the commercial products after the oral administration.

• YAKHAK HOEJI
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• v.57 no.3
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• pp.226-233
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• 2013

Although the dissolution test can serve as an effective tool for quality control and predictor of in vivo performance, there are a number of drugs with no established dissolution specification in Korean Pharmaceutical Codex (KPC). So, with each reference and test drugs, the dissolution test method and an analytical procedure by HPLC were developed and validated to establish dissolution specification for acebrophylline capsules and bromhexine hydrochloride tablets. The dissolution condition was determined based on the "Guidelines on Specifications of Dissolution tests for Oral dosage forms" of Ministry of Food and Drug Safety (MFDS). The analytical method of HPLC was validated in specificity, linearity, precision and accuracy. Final dissolution test was performed with commercially available samples of 3 lots to establish specification. In addition, no difference was observed by the inter-laboratory evaluation. Dissolution specifications and conditions will be used for revising the monograph of acebrophylline capsules and bromhexine hydrochloride tablets in next supplement of KPC.

• Polymer(Korea)
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• v.36 no.3
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• pp.332-337
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• 2012

The primary objective of this work is to find the properties of sustained release dissolution pattern depending on solubility of drugs, so venlafaxine HCl and carbamazepine tablets were made by using polymer wich various particle size. Hydroxy propyl methyl cellulose (HPMC) has been utilized in this study as an excipient that is one of the most widely used polymers for an oral sustained release formulation, and drug release pattern was strongly influenced by swelling rate depending on particle size of HPMC. Scanning electron microscope (SEM) was employed to investigate the surface of tablets with various HPMC particle size, and differential scanning calorimeter (DSC) was employed to investigate the crystallization of drugs in tablets. The release model equation was applied to analyze the main mechanism of drug release pattern. The results demonstrate that drug release pattern is controlled by the drug solubility and HPMC particle size.

• Archives of Plastic Surgery
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• v.41 no.5
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• pp.571-575
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• 2014

Background Disulfiram implantation is a widely used treatment alternative for alcohol abuse, yet reports on the surgical aspect of disulfiram implantation with respect to patient and drug-related treatment efficacy and wound complications are very limited. We present our clinical experiences with disulfiram implantation and discuss the surgical outcomes obtained with different anatomical planes for implantation. Methods Medical records of all patients referred to our clinic from the psychiatry department between 2007 and 2013 for disulfiram implantation were retrospectively analyzed. Implantation was carried out using 10 sterile Disulfiram tablets (WZF Polfa S.A.), each tablet containing 100 mg of disulfiram. The procedure was carried out by implanting the tablets randomly in either a subcutaneous or an intramuscular plane. The location and the plane of implantation and the complications were recorded for each patient and compared to determine the differences in the outcomes. Results A total of 32 implantation procedures were evaluated for this study. Twenty-five implants were placed in the intramuscular plane (78.2%), while seven implants were placed subcutaneously (21.8%). Exposure was encountered in three of the seven subcutaneous implants (42.9%), while no exposure was seen with the intramuscular implants. Incomplete absorption of the tablets was encountered in one patient with a previous subcutaneous implant who presented 1 year later for re-implantation as part of the continuation of therapy. Conclusions To overcome the issue of treatment continuation in the case of disulfiram therapy, which may be ceased due to frequently encountered wound complications, we believe that implantation in the subscapular intramuscular plane allows both uneventful healing and an out-of-reach implant location.

• Analytical Science and Technology
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• v.30 no.1
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• pp.32-38
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• 2017

In attempt to contribute in official monographs of Korean Pharmacopoeia, an HPLC method was developed and fully validated for the determination of tolperisone hydrochloride in tablets which have never been published in other forgein Pharmacopoeia. Analysis was carried out in an ODS column ($250{\times}4.6mm$ I.D., $5{\mu}m$) with common solvents include acetonitrile and ammonium hydrophosphate buffer as mobile phase. The assay was validated according to International Conference on Harmonization (ICH) guidelines. The method has good linearity in the range of $5-200{\mu}g/mL$ tolperisone. Intra-day precision varied between 0.04 and 0.10 %. Relative standard deviations of inter-day precision ranged between 0.43 and 1.24 % for peak area. The percentage recovery of the tolperisone ranged between 99.8 and 101.2 % in material. Recoveries in tablets were ranged between 98.7 and 100.8 %, thus confirmed the suitability of method for estimation of tolperisone hydrochloride in tablet dosage form.

• Journal of Pharmaceutical Investigation
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• v.25 no.3
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• pp.205-211
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• 1995

To increase the solubility of iodine and iodine releasing agents, which are used widely as a topical broad spectrum antiseptics and disinfectant sanitizers, its inclusion complexes were prepared and studied. Inclusion complexes of iodine with ${\beta}-cyclodextrin$ were prepared by coprecipitation method and complex formation was acertained by differential scanning calorimetry and microscopic observation. Iodine content of inclusion complex was determined by means of iodometry. Tablets containing inclusion complex were manufactured with sugar, citric acid, magnesium stearate, dextrose. Stability of inclusion complexes and tablets was evaluated by accelerated stability test, and comparing with PVP-iodine. During preparation, use of 50% ethanol solution is preferable to water as the medium because the former resulted in more stable complex for a month under accelerated storage conditions. Solubility of iodine in KI aqueous solution was 0.048 g/ml and lower than in 50% ethanol solution. Inclusion complex and its tablets were very stable at severe condition for one month, and comparable to PVP-iodine in the aspect of stability. Inclusion complex tabletswere not affected with citric acid, sugar, dextrose, and direct tableting method was recommendable because wet granulation using ethanol gave some release of included iodine during process.

• Archives of Pharmacal Research
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• v.18 no.5
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• pp.340-345
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• 1995

A nebumetone tablet in development $(Navuton^R)$ was tested for its bioequivalence to the erference tablet $(Uniton^R)$. Seventeen healthy Korean male subjects participated in this study. Each subject received a 1-g dose of nabumetone (2tables each) in an unbalanced, randomized, two-way crossover investigation. Serum concentrations of 6-methoxy-2-na-phthylacetic acid (6-MNA), a major metabolite of nebumetone, were measured over 120 hr interval by a high-performance liquid chromatography. The maximum serum concentration $(C_{max})$ and time to reach the maximum concentration$(T_{max})$ were read directly, but area under the serum concentration time curve from time 0 to 120 hr (AUC) and mean residence time serum curves showed multiple peaks of 6-MNA in most subjects, and the $C_{max}$ and $T_{max}$ were read from the highest serum peaks. calculated bioavailability parameters for test and reference tablets were 148.6 : 1377.9 $\mug \cdot hr/ml$ for AUC; 25.2:23.1 $\mu/ml$ for $C_{max}$; 11.8:16.4 hr for $T_{max}$, and 42.6 : 43.8 hr for MRT, respectively. The paired t-test revealed no significant differences in all the parameters between the two tablets. Analysis ofl variance (ANOVA) revealed no significant differences between groups and formulations in all the parameters ($C_{max}$ and $T_{max}$, AUC and MRT) indicating the crossover design of the experiment was properly performed. But significant differences (p<0.05) between subject/groups and periods were found for all the parameters indicating substantial intersubject and interperiodic variations for these parameters.

• YAKHAK HOEJI
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• v.47 no.4
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• pp.239-243
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• 2003

Metformin is an oral antihyperglycemic agent used in the therapy of noninsulin-dependent diabetes mellitus and does not cause hypoglycemia at the therapeutic dose. The purpose of the present study was to evaluate the bioequivalence of two metformin hydrochloride tablets, Glucophage tablet (DaeWoong Pharmaceutical Co., reference drug) and Dybis tablet (Shinpoong Pharmaceutical Co., test drug), according to the guidelines of Korea Food and Drug Administration(KFDA). Twenty-four normal volunteers, 26.6$\pm$4.01 years in age and 60.6$\pm$9.80 kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 500 mg of metformin hydrochloride was orally administered, blood was taken at predetermined time intervals and the concentrations of metformin hydrochloride in serum were determined using HPLC with UV detector. The pharmacokinetic parameters such as AUCt, Cmax and Tmax were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in AUCt, Cmax and Tmax between two products were -1.05％, -6.76％ and -4.51％, respectively, when calculated against the reference drug. The 90％ confidence intervals using logarithmically transformed data were within the acceptance range of log0.8$\leq$$\delta$$\leq$log1.25 (e.g., log0.9082$\leq$$\delta$$\leq$log1.0906 and log0.8188$\leq$$\delta$$\leq$log1.0392 for $AUC_{t}$ and $C_{max}$, respectively). The 90％ confidence intervals using untransformed data was within $\pm$20％ (e.g., -17.66％$\leq$$\delta$$\leq$8.63％ for $T_{max}$). All parameters met the criteria of KFDA for bioequivalence, indicating that Dybis tablets (Shinpoong Pharmaceutical Co.) is bioequivalent to Glucophage tablets (DaeWoong Pharmaceutical Co.).

• Korean Journal of Clinical Pharmacy
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• v.8 no.2
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• pp.101-106
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• 1998

A bioequivalence study of the Kerola tablets (Dongkwang Pharmaceutical Co., Korea) to the Tarasyn tablets (Roche Co., Korea), formulations of ketorolac trometamine(KTR), was conducted. Sixteen healthy Korean male subjects received each formulation at the dose of 10 mg as KTR in a $2\times2$ crossover study. There was a 1-week washout period between the dose. Plasma concentrations of KTR were monitored by an HPLC method for over a period of 12 hr after each administration. AUC (area under the plasma concentration-time curve) was calculated by the linear trapezoidal method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma drug concentration-time data. Analysis of variance (ANOVA) revealed that there are no differences in AUC, $C_{max}\;and\;T_{max}$ between the formulations. The apparent differences between the formulations in these parameters were all far less than $20\%$ (i.e., 2.31, 8.19 and $0\%$ for AUC, $C_{max}\;and\;T_{max}$, respectively). Minimum detectable differences $(\%)\;at\;\alpha=0.1\;and\;1-\beta=0.8$ were all less than $20\%$ difference in these parameters between the formulations were all over 0.8. The $90\%$ confidence intervals for these parameters were also within $20\%$. These results satisfy the bioequivalence criteria of the Korea Food and Drug Administration (KFDA) guidelines (No. 1998-86). Therefore, these results indicate that the 2 formulations of KTR are bioequivalent and, thus, may be prescribed interchangeably.

• Journal of the Korea Society of Computer and Information
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• v.19 no.2
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• pp.49-56
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• 2014

This thesis proposes CBIRS/TB method that uses a tablet's color distribution information and form distinctive in content-based search. CBIRS/TB can avoid misuses and improper tablet uses by conducting content-based search in commonly prescribed tablets. The existing FE-CBIRS system is limited to recognizing only the image of color and shape of the tablet, that leads to applying insufficient form-specific information. While CBIRS/TB utilizes average, standard deviation, hue and saturation of each tablets in color, brightness, and contrast, FE-CBIRS has partial-sphere application problem; only applying the typical color of the tablet. Also, in case of the shape-specific-information, Invariant Moment is mainly used for the extracted partial-spheres. This causes delayed processing time and accuracy problems. Therefore, to improve this setback, this thesis indexed color-specific-information of the extracted images into categorized classification for improved search speed and accuracy.