• Journal of Pharmaceutical Investigation
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• 제29권3호
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• pp.241-245
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• 1999

Bioequivalence study of two cefpodoxime preparations, the test drug ($Banan^{\circledR}$: Hanil Pharmaceutical Co., Ltd.) and the reference drug ($Podox^{\circledR}$: Chong Kun Dang Pharmaceutical Co., Ltd.), was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen healthy male volunteers, $23.8{\pm}2.13$ years old and $63.34{\pm}4.84kg$ of body weight in average, were divided randomly into two groups and administered the drug orally at the dose of 200 mg as cefpodoxime proxetil in a $2{\times}2$ crossover study. Plasma concentrations of cefpodoxime were analysed by HPLC method for 12 hr after administration. The $AUC_{0-12hr}$ was calculated by the linear trapezoidal rule method. The $C_{max}$, and $T_{max}$ were compiled directly from the plasma drug concentration-time data. Student's t-test indicated no significant differences between the formulations in these parameters. Analysis of variance (ANOVA) revealed that there were no differences in AUC, $C_{max}$, and $T_{max}$ between the formulations. The apparent differences between the formulations were far less than 20% (e.g., 4.31, 1.99 and 4.30% for AUC, $C_{max}$, and $T_{max}$, respectively). Minimum detectable differences (%) between the formulations at ${\alpha}=\;0.05$ and $1-{\beta}=\;0.8$ were less than 20% (e.g., 13.89, 13.88, and 16.97% for AUC, $C_{max}$, and $T_{max}$, respectively). The 90% confidence intervals for these parameters were also within ${\times}20%$ (e.g., $-5,58{\sim}14.20$, $-7.89{\sim}11.88$, and $-7.78{\sim}16.38%$ for AUC, $C_{max}$, and $T_{max}$, respectively). These results satisfied the bioequivalence criteria of KFDA guidelines, indicating that the two formulations of cefpodoxime were bioequivalent.

• Archives of Pharmacal Research
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• 제18권4호
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• pp.237-242
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• 1995

For the vioequivalence study of two ceftriaxone injection formulations ($Rocephin{\circledR}$ ; Roche, and Triaxone ; Hanmi0, the HPLC analytical method for the analysis of ceftriaxone in plasma was used. Fourteen healthy volunteers completed the study and each subject were IM in jected signle doses (1 g) of the test and the reference formulations in a two-way crossover design with an one week drug free interval between doses. Following each administration, plasma concentrations of ceftrixone were monitored over a period of 24 h. Bioequivalence parameters $AUC_{24th}, {\;}T_{max}, {\;}C_{max}$ and MRT determined from the data obtained for the two formulations were examined by analyses of variance (ANOVA) and other criteria and tests for bioequivalence. Results of ANOVA and confidence limits of test/reference ratios of $AUC_{24th}, {\;}T_{max}, {\;}C_{max}$ and MRT, and statistical tests indicated the bioequivalence of the two formulations (i.e., test/reference ratio was within $100{\pm}20%$) except for $T_{max}$ The mean of $T_{max}$ showed only 6. 9% difference from the reference but the detection limit was 22.5% which is slightly over the 20% criteria. No pharmacokinetic parameters including Ka, Kel, Vd and Cl indicated significant difference in between the two fomulations. It was concluded that the data yielded fro the two cefriaxone formulations demonstrated that they were bioequivalent.

• Journal of Pharmaceutical Investigation
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• 제41권4호
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• pp.217-225
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• 2011

The aim of this work was to prepare porous osmotic pump tablets for controlled delivery of Aceclofenac. Aceclofenac solid dispersion was prepared to improve the solubility by using the drug - carrier (Mannitol) ratio of 1:1. The osmotic pump tablets were prepared using the solid dispersed product of Aceclofenac. The formulation contains potassium chloride as osmotic agent, cellulose acetate as semipermeable membrane, poly ethylene glycol (PEG 4000) as pore former and sodium lauryl sulphate (SLS) as solubility enhancer. The formulations were designed by the general factors such as osmotic agent and pore former. All formulations were evaluated for various physical parameters and, the in vitro release studies were conducted as per USP. The drug release kinetic studies such as zero order, first order, and Higuchi and Korsmeyer peppas were determined and compared. All the formulations gave more controlled release compared to the marketed tablet studied. Numerical optimization techniques were applied to found out the best formulation by considering the parameter of in vitro drug release kinetics and dissolution profile standards. It was concluded that the porous osmotic pump tablets (F7) composed of Aceclofenac solid dispersion/Potassium chloride/Lactose/Sodium lauryl sulphate/Magnesium Stearate (400/40/95/10/5, mg/tab) and coating composition with Cellulose acetate/ PEG 4000 (60/40 %w/w) is the most satisfactory formulation. The porous osmotic pump tablets provide prolonged, controlled, and gastrointestinal environment-independent drug release.

• Journal of Pharmaceutical Investigation
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• 제40권3호
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• pp.187-192
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• 2010

We aimed to evaluate the effect of temperature, pH, and light conditions on the stability of porcine placental extract (PPE)-loaded liposomes with different surface charges. The size distribution profiles and in vitro release patterns were investigated by dynamic light scattering method and spectrophotometry. The stability of PPE-loaded liposomes was affected by the surface charges of the liposomes. As compared to neutral and anionic liposomes, cationic liposome formulations showed significantly lower physical stability. At the test storage conditions of different temperatures and pHs, the mean sizes of cationic PPE-loaded liposomes substantially increased. In contrast, neutral and anionic liposomes did not reveal significant changes in mean sizes upon various storage conditions. The neutral and anionic liposomes showed no significant differences in the release profiles of PPE after storage at various temperatures and pHs. Our results indicate that anionic and neutral liposome compositions might be more suitable for the formulations of PPE providing the higher stability.

• Journal of Pharmaceutical Investigation
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• 제40권1호
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• pp.51-57
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• 2010

Losartan potassium, 2-butyl-4-chloro-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]imidazole-5-methanol mono-potassium salt, is a new class of antihypertensive agents, and is an antagonist in angiotensin receptor. The purpose of the present study was to evaluate the bioequivalence of two Losartan potassium tablets, Cozaar tablet (MSD Pharmaceutical Co., Ltd.) and Losata tablet (Kyung Dong Pharmaceutical Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of losartan from the two losartan potassium formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media. Twenty eight healthy male subjects, $23.86{\pm}1.80$ years in age and $67.27{\pm}6.60\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single tablet containing 50 mg as losartan potassium was orally administered, blood samples were taken at predetermined time intervals, and the concentrations of losartan in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar in all tested dissolution media. The pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated, and Equiv Test/K-BE Test 2002 was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Cozaar, were -2.70%, 1.45% and 2.31% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 (e.g., log 0.8852~log 1.0655 and log 0.8319~log 1.2342 for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Losata tablet was bioequivalent to Cozaar tablet.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.411.2-411.2
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• 2002

In order to develope an optimum formulation for iontophoretic delivery of vitamine-C-2 phosphate. we have prepared 3 different formulations using hydrophilic polymers, such as poloxamer, carbo pol and HPMC and iontophoretic flux through skin from these hydrogel formulations was carried out. The effect of current density, drug concentration and current profile on flux was investigated. In-vitro flux study was performed at 36.5$^{\circ}C$, using side-by-side diffusion cell. Full-thickness hairless mouse skin was used for this work. (omitted)

• Journal of Pharmaceutical Investigation
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• 제31권3호
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• pp.197-200
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• 2001

Lectin-conjugated ellagitannin (LET), a newly introduced melanoma-specific antitumor agent which has been synthesized by conjugation of wheat germ agglutinin as a lectin with praecoxin A as an ellagitannin, was encapsulated into sterically stabilized liposomes (SSL). Modified Folin phenol method was established for the quantitation of LET contents in liposomal formulations protein employing the standard calibration curve with bovine serum albumin. After removal of phospholipid by organic solvent extraction, which interferes the specific selectivity of the Folin-Ciocalteu reagent with the protein, recovery of LET was $94.5{\pm}2.3%$ and the encapsulation efficiency was revealed as $37.8{\pm}5.9%$ for 2.5 mg/ml LET solution.

• Journal of Pharmaceutical Investigation
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• 제23권4호
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• pp.213-216
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• 1993

${\kappa}-Carrageenan$, an anionic polysaccharide, was employed in tablet formulations and its function as a drug release sustaining agent was investigated. Tablets composed of ${\kappa}-carrageenan$ and hydroxypropyl methylcellulose were fabricated by using direct compression method. Lactose and sodium alginate were utilized as controls for ${\kappa}-carrageenan$. Drug release experiments performed at pHs 1.2 and 7.4 revealed that ${\kappa}-carrageenan$ retains pH-dependent sustained release effects due to its anionic characteristics. Also, the ionic interaction between ${\kappa}-carrageenan$ and drugs exerted significant affects on drug release kinetics. ${\kappa}-Carrageenan$ was found out to be a useful additive for sustained release tablet formulations.

• Journal of Pharmaceutical Investigation
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• 제38권3호
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• pp.157-162
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• 2008

The aim of the study was to formulate the stable amlodipine maleate tablet by selecting and combining of suitable ingredients. Amlodipine tablets were designed by using different manufacturing methods or formulations. Dissolution rate at 30 min of newly formulated tablets was over 98% in 0.1 M HCl medium. After 4 months storage under accelerated condition, the changes of appearance, loss on drying, content and total impurity were investigated. For long-term stability tests, two formulations of K017 (direct compressed tablets consisting of microcrystalline cellulose and pregelatinized starch) and K018 (wet granulated tablets by OpadryAMB) were stored under $25^{\circ}C$, 60% RH for 24 months. Under the accelerated condition, moisture content in K017 formulation was increased as 5.96% for 4 months, while other formulations with anhydrous monobasic phosphoric potassium or by wet granulation showed higher increase in moisture content compared to K017. In addition, K017 formulation showed a low decrease in contents and total relative substance as 0.8% and 0.7%, respectively. Similar stability of amlodipine in K017 was obtained under the long-term stability test. These results indicate that the K017 combined with microcrystalline cellulose and pregelatinized starch as ingredients is very stable formulation to protect active substance from moisture contact and sustain stability. Therefore, suitable combination of ingredients such as microcrystalline cellulose and pregelatinized starch could attribute to enhance the stability of moisture-labile drug such as amlodipine maleate.

• 약학회지
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• 제45권2호
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• pp.220-226
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• 2001

A bioequivalence study of Lovastati $n^{TM}$ tablets (Dong Sung Pharmaceutical Co., Korea) to Mevaco $r^{TM}$ tablets (Choong Wae Pharmaceutical Co., Korea) was conducted according to the guidelines (No. 98-56) of Korea Food and Drug Administration (KFDA). Each tablet contained 20 mg of lovastatin. Eighteen healthy Korean male subjects received each formulation at a lovastatin dose of 80 mg (i.e., four tablets) in a 2 $\times$ 2 crossover study. There was a washout period of a week between the dose of the two formulations. Plasma concentrations of lovastatin acid were monitored by a GC/MS method for over a period of 12hr after each administration. The area under the plasma concentration-time curve from time zero to 12hr (AUC) was calculated by a linear trapezoidal method. The maximum plasma drug concentration ( $C_{max}$) and the time to reach $C_{max}$ ( $T_{max}$) were compiled from the plasma drug concentration-time data. Analysis of variance (ANOVA) of these parameters revealed that there are no differences in AUC and $C_{max}$ between the formulations. The apparent differences between the formulations in these parameters were 4.87 and 8.03% for AUC and $C_{max}$, respectively. Minimum detectable differences (%) at $\alpha$=0.1 and 1-$\beta$=0.8 were 17.84 and 15.36% for AUC and $C_{max}$ respectively. The 90% confidence intervals were -15.30~5.56 and -17.02-0.95% for AUC and $C_{max}$, respective1y. Thus, the criteria of the KFDA guidelines for the bioequivalence was satisfied, indicating Mevaco $r^{TM}$ tablets and Dong Sung Lovastati $n^{TM}$ tablets are bioequivalent.ivalent.ent.alent.ent.