• Journal of Pharmaceutical Investigation
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• 제32권3호
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• pp.215-221
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• 2002

Cephradine is a first generation cephalosporin and has broad spectrum antibacterial activity against gram-positive and gram-negative microorganisms, through inhibition of bacterial cell wall synthesis. Cephradine is useful for treatment of infections of the urinary and respiratory tract, skin and soft tissues. The purpose of the present study was to evaluate the bioequivalence of two cephradine capsules, Cefradine Yuhan (YuHan Corporation) and Broadcef (Ilsung Pharmaceuticals Co. Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The cephradine release from the two cephradine capsules in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty normal male volunteers, $23.10{\pm}2.90$ years in age and $67.69{\pm}8.04\;kg$ in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one capsule containing 500 mg as cephradine was orally administered, blood was taken at predetermined time intervals and the concentrations of cephradine in serum were determined using HPLC method with UV detector. The dissolution profiles of two cephradine capsules were very similar at all dissolution media. Besides, the pharmacokinetic parameters such as $AVC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AVC_t\;and\;C_{max}$ and untransformed $T_{max}$. The results showed that the differences in $AVC_t,\;C_{max}\;and\;T_{max}$ between two capsules based on the Cefradine Yuhan were -2.87%, -0.96% and -4.85%, respectively. There were no sequence effects between two capsules in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of 1og(0.8) to log(1.25) $(e.g.,\;log(0.93){\sim}log(1.02)\;and\;log(0.88){\sim}log(1.13)\;for \;AVC_t\;and\;C_{max},\;respectively)$. The 90% confidence interval using untransformed data was within ${\pm}20%$ $(e.g., \;-17.54{\sim}7.78\;for\;T_{max})$. All parameters met the criteria of KFDA guideline for bioequivalence, indicating that Broadcef capsule is bioequivalent to Cefradine Yuhan capsule.

• Journal of Pharmaceutical Investigation
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• 제35권3호
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• pp.193-199
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• 2005

Gabapentin is an antiepileptic drug that is structurally similar to ${\gamma}-aminobutyric$ acid (GABA), but does not interact with the GABA receptor. It does not bind significantly to plasma proteins, and is excreted to unchanged form in the urine. The purpose of the present study was to evaluate the bioequivalence of two gabapentin capsules, $Neurontin^{TM}$ capsule 300 mg (Pfizer Pharm. Co., Ltd.) and Kuhnil $Gabapentin^{TM}$ capsule 300 mg (Kuhnil Pharm. Co., Ltd), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of gabapentin from the two gabapentin formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty six healthy male subjects, $22.46{\pm}1.86$ years in age and $67.64{\pm}7.24$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After a single capsule containing 300 mg as gabapentin was orally administered, blood samples were taken at predetermined time intervals and the concentrations of gabapentin in serum were determined using HPLC with fluorescence detector. The dissolution profiles of two formulations were similar at all dissolution media. In addition, the pharmacokinetic parameters such as $AUC_t$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test 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, $Neurontin^{TM}$ capsule 300 mg, were -2.03, -0.43 and 4.29% 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 $(e.g.,\;log\;0.89{\sim}log\;1.09\;and\;log\;0.91{\sim}log\;1.09$ for $AUC_t$ and $C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Kuhnil $Gabapentin^{TM}$ capsule 300 mg was bioequivalent to $Neurontin^{TM}$ capsule 300 mg.

• 분석과학
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• 제26권1호
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• pp.99-105
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• 2013

염모제품 중 유효성분의 품질검사는 식품의약품안전청의 "의약외품에 관한 기준 및 시험방법"에 따라 제품에 표기된 산화염료들을 박층크로마토그래프법(TLC방법)으로 확인시험을 하도록 되어있다. 그러나 TLC방법은 원료분량이 미량이거나, $R_f$ 값이 비슷한 성분들이 존재하면 확인시험이 어려운 문제점이 있다. 본 연구에서는 미량성분 검출이 용이하며 분석시간이 짧다고 보고된 UPLC를 이용하기 위한 시료 전처리 및 분석조건을 탐색하였다. 유효성분들을 분석할 수 있는 검출한계는 6.7-77.9 ${\mu}g/L$, 정량한계는 22.3-259.7 ${\mu}g/L$ 이었으며, 회수율은 ${\alpha}$-naphthol를 제외하고는 96.2-101.5%로 양호하였다. 유효성분 추출하기 위한 시료 전처리에는 헥산-증류수를 사용하였다. 시료 전처리 시 복잡한 추출과정을 거치지 않고, UPLC방법은 빠르고 정확하게 염모제품에 함유되어 있는 유효성분들을 동시에 분석 할 수 있었다.

• The Korean Journal of Physiology and Pharmacology
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• 제17권5호
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• pp.469-477
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• 2013

This study investigated effect of extract containing quercetin-3-O-${\beta}$-D-glucuronopyranoside from Rumex Aquaticus Herba (ECQ) against chronic gastritis in rats. To produce chronic gastritis, the animals received a daily intra-gastric administration of 0.1 ml of 0.15% iodoacetamide (IA) solution for 7 days. Daily exposure of the gastric mucosa to IA induced both gastric lesions and significant reductions of body weight and food and water intake. These reductions recovered with treatment with ECQ for 7 days. ECQ significantly inhibited the elevation of the malondialdehyde levels and myeloperoxidase activity, which were used as indices of lipid peroxidation and neutrophil infiltration. ECQ recovered the level of glutathione, activity of superoxide dismutase (SOD), and expression of SOD-2. The increased levels of total NO concentration and iNOS expression in the IA-induced chronic gastritis were significantly reduced by treatment with ECQ. These results suggest that the ECQ has a therapeutic effect on chronic gastritis in rats by inhibitory actions on neutrophil infiltration, lipid peroxidation and various steps of reactive oxygen species (ROS) generation.

• Journal of Pharmaceutical Investigation
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• 제32권2호
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• pp.127-133
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• 2002

Levosulpiride is the 1evo-enantiomer form of racemic sulpiride, a benzamide derivative selectively inhibiting dopaminergic $D_2$ receptors at the trigger zone both in the central nervous system and in the gastrointestinal tract. The purpose of the present study was to evaluate the bioequiva1ence of two levosulpiride tablets, Levopride (SK Pharmaceutical Co., Ltd.) and Levopid (Dae Won Pharmaceutical Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The levosulpiride release from the two levosulpiride tablets in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty eight normal male volunteers, $23.82{\pm}3.26$ years in age and $69.13{\pm}8.58$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 25 mg of levosulpiride was orally administered, blood was taken at predetermined time intervals and the concentrations of levosulpiride in serum were determined using HPLC method with fluorescence detector. The dissolution profiles of two levosulpiride tablets were very similar at all dissolution media. Besides, the pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t\;and\;C_{max}$ and untransformed $T_{max}$. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets based on the Levopride were -1.17%, 1.20% and -1.09%, respectively. There were no sequence effects between two tablets in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) $(e.g.,\;log(0.93){\sim}log(1.07)\;and\;log(0.90){\sim}log(1.14)\;for\;AUC_t\;and\;C_{max}$, respectively). The 90% confidence interval using untransformed data was within ${\pm}20%$ $(e.g.,\;-19.47{\sim}16.20\;for\;T_{max})$. All parameters met the criteria of KFDA guideline for bioequivalence, indicating that Levopid tablet is bioequivalent to Levopride tablet.

• Journal of Pharmaceutical Investigation
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• 제32권2호
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• pp.135-140
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• 2002

Cefadroxil is a semi-synthetic cephalosporin active against many Gram-positive and Gram-negative bacteria. The drug has been used for the treatment of the urinary and respiratory tract infections when caused by susceptible strains of the designated microorganism. The purpose of the present study was to evaluate the bioequivalence of two cefadroxil capsules, Duricef (Bo Ryung Pharmaceutical Co. Ltd.) and Hanacef (Korean Pharmaceutical Co. Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The cefadroxil release from the two cefadroxil capsules in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty four normal male volunteers, $21.58{\pm}2.43$ years in age and $70.74{\pm}10.29$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one capsule containing 500 mg as cefadroxil was orally administered, blood was taken at predetermined time intervals and the concentrations of cefadroxil in serum were determined using HPLC with UV detector. The dissolution profiles of two cefadroxil capsules were very similar at all dissolution media. The pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t\;and\;C_{max}$ and untransformed $T_{max}$. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two capsules based on the Duricef were 0.05%, -5.29% and 4.53%. There were no sequence effects between two capsules in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) $(e.g.,\;log(0.95){\sim}log(1.05)\;and\;log(0.87){\sim}log(1.02)$ for $AUC_t\;and\;C_{max}$, respectively). The 90% confidence interval using untransformed data was within ${pm}20%$ $(e.g.,\;-6.75{\sim}15.74\;for\;T_{max})$. All parameters met the criteria of KFDA guideline for bioequivalence, indicating that Hanacef capsule is bioequivalent to Duricef capsule.

• Journal of Pharmaceutical Investigation
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• 제36권2호
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• pp.143-148
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• 2006

Finasteride $[N-(1, 1-dimethylethyl)-3-oxo-4-aza-5{\alpha}-androst-1-ene-17{\beta}-carboxamide]$ is a 4-aza-3-oxosteroidal inhibitor of human $5{\alpha}-reductase$. The purpose of the present study was to evaluate the bioequivalence of two finasteride tablets, $Proscar^{\circledR}$ (MSD Korea Ltd.) and Procare (Hana Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of finasteride from the two finasteride formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty six healthy male subjects, $23.7\;{\pm}\;2.24$ years in age and $67.2\;{\pm}\;8.55\;kg$ in body weight, were divided into two groups and a randomized $2\;{\time}\;2$ cross-over study was employed. After two tablets containing 5 mg as finasteride was orally administered, blood samples were taken at predetermined time intervals and the concentrations of finasteride in serum were determined using HPLC with UV 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 ANOVA test 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, $Proscar^{\circledR}$, were 6.39, 4.65 and -13.9% 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 0.800 to log 1.25 $(e.g.,\;log\;0.990{\sim}log\;1.14\;and\;log\;0.977{\sim}log\;1.13 for\;AUC_t\;and\;C_{max},\;respectively)$. Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Procare tablet was bioequivalent to $Proscar^{\circledR}$ tablet.

• 한국산학기술학회논문지
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• 제18권1호
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• pp.295-301
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• 2017

보툴리눔 신경독소는 콜린성 신경말단(부)을 선택적으로 공격하여 신경마비를 일으키는 신경독소로서, 그람양성을 띠고 내성포자를 형성하는 절대혐기성 세균인 보툴리눔 균(Clostridium botulinum)이 만들어낸다. 이 중 보툴리눔 A형 독소(BoNT/A)는 음식물과 물을 오염시킬 수 있으며 생물 무기나 생물 협박물질로 사용될 수도 있다. 이 때문에 독성을 탐지할 수 있는 예민한 분석방법과 중독을 치료할 수 있는 효능 있는 항독소를 개발해낼 필요성이 제기되어 왔다. 본 연구에서는 BoNT/A를 중화할 수 있는 단일클론 항체(mAb)를 생산하기 위하여 BoNT/A로 면역된 토끼의 항혈청에서 유래한 scFv 라이브러리를 인간 IgG와 융합시켰다. 그렇게 재조합된 scFvIgG 항체 단백질을 안정된 세포주에서 발현시켰고 항체 친화 크로마토그래피를 사용하여 scFvIgG mAb 단백질을 정제하였다. ELISA로 정제된 scFvIgG mAb 단백질의 효율성을 확인하였고, in vivo 실험으로 BoNT/A에 대한 중화능을 시험하였다. 독성 중화능 실험은 마우스를 사용하여 수행하였는데, 그 결과 scFvIgG 항체(10 ug)는 BoNT/A(100,000 $LD_{50}$)의 독성이 주입된 마우스를 완전히 방어하지는 못하지만 마우스의 생존 기간을 현격하게 연장시키는 것이 확인되었다. 이러한 결과들은 이 scFvIgG mAb가 BoNT/A를 중화하는 효능을 가지고 있다는 점을 제시한다.

• Korean Chemical Engineering Research
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• 제48권3호
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• pp.342-349
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• 2010

젖산은 식품, 화학 및 의약 산업에서 널리 이용되며 생분해성 고분자인 폴리젖산(poly lactic acid)의 원료로서 요구량이 증대되고 있다. 합성에 의한 생산 방법에서 환경 친화적이고 경제적인 발효에 의한 생산 방법으로 바뀌는 추세이다. 그러나 발효에 의해 생성된 생산물은 과량의 물과 고비점 부산물을 포함하고 있다. 고비점 물질의 존재와 젖산의 비휘발성은 젖산 분리 및 정제를 어렵게 만든다. 또한 정제 및 분리 공정은 많은 투자 비용과 에너지 소모를 요구한다. 반응증류 공정은 기존 공정과 비교하여 높은 선택도와 수율을 얻을 수 있다. 분리벽형 반응 증류탑과 같이 새롭게 통합된 공정은 투자 비용과 에너지 비용을 줄일 수 있고 순수한 젖산을 회수할 수 있다. 본 연구에서는 젖산의 분리 및 정제를 위한 설계구조들을 제안하였다. 제안된 설계구조들은 SQP 방법에 의해 최적화되었으며 최적화된 설계 구조들 사이의 에너지 소모량 및 생산물 순도를 비교하였다. 그리고 공정 성능과 최적화된 공정에 대한 주요 공정 변수들의 영향을 조사하였다.

• 생명과학회지
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• 제19권9호
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• pp.1245-1250
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• 2009

패모는 한국, 일본, 중국 지역에 분포하는 백합과 인경식물로 오래전부터 진해, 거담제 및 편도염, 기관지염에 이용되어 왔다. 그러나, 오랫동안 진행되어 온 기내배양, 휴면타파, 성분분석에 대한 연구와 달리 생리활성에 대한 연구는 거의 없는 실정이다. 본 연구에서는 패모로부터 메탄올 추출물을 조제하고, 이로부터 다양한 유기용매 분획물을 조제하여 이들의 항균, 항혈전 및 항산화 활성을 평가하였다. 패모의 메탄을 추출물은 다량의 수용성 당을 포함하고 있으며(물 잔류물 58.98%), 지용성 오일도 상당량 포함하였다(헥산 분획물 14.85%). 항균활성의 경우, 에틸아세테이트 및 부탄올 분획물 $500{\mu}g$/disc에서 E. coli를 제외한 실험세균 모두에서 우수한 항세균 활성이 나타났으며, 항진균 활성은 모든 시료에서 나타나지 않았다. 항혈전 활성은 메탄올 추출물에서 우수하였으며, 헥산, 에틸아세테 이트 및 부탄올 분획물은 2.4 mg/ml 농도에서 모두 300초 이상의 연장된 트름빈 타임을 나타내었고, 특히 에틸아세테이트 분획은 1.2 mg/ml 농도에서 95.4초를 나타내어 항혈전제인 아스피린 활성과 유사하였다. 메탄올 추출물 및 분획물의 항산화 활성 평가 결과, 에틸아세테이트 분획 및 부탄올 분획이 368.2 및 $344.0{\mu}g$/ml의 $IC_{50}$를 나타내어 우수한 DPPH 소거능을 나타내었으며, SOD 유사활성은 $55{\sim}63%$로, vitamin C의 20-25%, 환원력의 경우 BHT의 51-54%를 나타내어 우수한 항산화 활성을 가짐을 확인하였다.