• Journal of Pharmaceutical Investigation
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• 제40권5호
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• pp.285-289
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• 2010

Manufacturing a multi-layered tablet such as Xatral XL$^{(R)}$ is more complex and expensive than monolayered tablets, but mono-layered tablets may have less favorable release properties depending on the pharmacodynamics and pharmacokinetics of the active ingredient. We therefore sought to develop a monolayer tablet with a similar dissolution profile to the commercial alfuzosin sustained-release triple layered tablet (Xatral XL$^{(R)}$). We prepared four different mono-layered alfuzosin tablets with different concentrations of hydroxypropyl methycellulose and PVP K-90. Fomulation III with alfuzosion/mg-stearate/ HPMC/ PVP K-90 (10/5/110/95 mg/tab) has a similar dissolution rate to Xatral XL$^{(R)}$, with a similarity factor score of 81.4. However, the swelling and erosion rates of the two formulations were different, and NIR analysis showed differences in the mechanisms of drug release. Thus, although formulation III and Xatral XL$^{(R)}$ show similar dissolution rates, the mechanisms of drug release are different.

• Journal of Pharmaceutical Investigation
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• 제29권3호
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• pp.205-210
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• 1999

To formulate the parenteral delivery of a new cephalosporin derivative, 7-${\beta}$-[(2)-2-(2-arninothiazol-4-yl)-2methoxyiminoacetamido]- 3- [(2,3-cyclopenteno-4-carbamoyl-l-pyridinium)methyl]- 3-cephem-4-carboxylate sulfate( CKD604), the stability and solubility of CKD-604 in various aqueous media were investigated. The degradation kinetics of CKD-604 in aqueous solutions (ionic strength 0.1, pH 1-8) were studied at $37^{\circ}C$. The observed degradation rates followed pseudo first order kinetics. The pH-rate profile exhibited a minimum degradation rate at pH 5. The Arrhenius activation energy was 14.2 kcal/mol in pH 5 buffer solution. Excellent agreement between the cephalosporins' theoretical pH-rate profile and the experimental data indicated that the degradation pathway of CKD-604 could be predicted according to the general pathway of cephalosporins. The solubility of CKD-604 was 8.16 mg/ml at $25^{\circ}C$. To enhance the solubility and adjust the suitable pH, CKD-604 was solubilized by using sodium ascorbate, ascorbic acid and urea. The compositions were obtained to satisfy optimum pH and concentration, and the total amount of additives was several times of the active ingredient, CKD-604.

• 약학회지
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• 제54권4호
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• pp.240-243
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• 2010

High-performance liquid chromatography (HPLC) screening method revealed that a propolis product marketed as a functional food contained an undeclared substance similar to tadalafil, the active ingredient of the prescription drug Cialis$^{(R)}$ approved for the treatment of male erectile dysfunction. In order to identify the illegal additive, the propolis product was extracted with methylene chloride, and the extract was purified further using semipreparative HPLC. The chemical structure of the isolated substance was elucidated based on IR, LC/MS-ESI, and $^1H$- and $^{13}C$-NMR spectroscopy, which showed the characteristics similar to tadalafil. The only difference was the substitution of the methyl group at the piperazinedione ring of tadalafil to the amino group of the identified illegal additive.

• Bulletin of the Korean Chemical Society
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• 제32권1호
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• pp.109-112
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• 2011

A new derivative of tacrolimus was evaluated for its molecular weight, using LC-MS of the tacrolimus bulk active pharmaceutical ingredient (API) recovered through the purification of crude tacrolimus produced by Streptomyces clavuligerus CKD-1119. In addition, the molecular weight of the new derivative of tacrolimus was found to be at m/z 818 and was identified by $^{13}C$-NMR with peak assignments based on the differences in methyl group location resulting from the chemical structure. The structure of the new derivative, an unknown impurity of tacrolimus, was found to be 18-methyltacrolimus through comparison of the spectral data of the structural differences between ascomycin, tacrolimus, and the new derivative 18-methyltacrolimus.

• 대한화학회지
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• 제60권4호
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• pp.235-238
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• 2016

Mt. Jiri located in the southwestern part of Korea is a treasure trove of wild medicinal plants. More than 1200 species currently classified as herbs are grown or cultivated in the area. Recently, safflower has attracted interest because of its ability to control fine wrinkle formation on the neck. The objective of this study therefore was to determine whether the active ingredient of safflower could be used in the form of an extract to reduce wrinkle formation in individuals aged 30 to 59 years. In particular, this study was aimed at determining the extract’s elastase activity and anti-oxidant effect by using DPPH assay in vitro and evaluating the anti-wrinkle efficacy of different types of safflower extracts in improving fine wrinkles on the neck. This study will provide a basis for future studies to develop safflower extracts using advanced composition technology and contribute to the development of the herbal cosmetics industry.

• Journal of Ginseng Research
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• 제46권1호
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• pp.39-53
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• 2022

Ginsenoside Rb₁ (Rb₁), one of the most important ingredients in Panax ginseng Meyer, has been confirmed to have favorable activities, including reducing antioxidative stress, inhibiting inflammation, regulating cell autophagy and apoptosis, affecting sugar and lipid metabolism, and regulating various cytokines. This study reviewed the recent progress on the pharmacological effects and mechanisms of Rb₁ against cardiovascular and nervous system diseases, diabetes, and their complications, especially those related to neurodegenerative diseases, myocardial ischemia, hypoxia injury, and traumatic brain injury. This review retrieved articles from PubMed and Web of Science that were published from 2015 to 2020. The molecular targets or pathways of the effects of Rb₁ on these diseases are referring to HMGB1, GLUT4, 11β-HSD1, ERK, Akt, Notch, NF-κB, MAPK, PPAR-γ, TGF-β1/Smad pathway, PI3K/mTOR pathway, Nrf2/HO-1 pathway, Nrf2/ARE pathway, and MAPK/NF-κB pathway. The potential effects of Rb₁ and its possible mechanisms against diseases were further predicted via Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway and disease ontology semantic and enrichment (DOSE) analyses with the reported targets. This study provides insights into the therapeutic effects of Rb₁ and its mechanisms against diseases, which is expected to help in promoting the drug development of Rb₁ and its clinical applications.

• Bulletin of the Korean Chemical Society
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• 제34권9호
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• pp.2760-2764
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• 2013

Geniposide is a biologically active ingredient of gardenia fruit. A liquid chromatography-tandem mass spectrometric method was developed and validated for the determination of geniposide in rat plasma. The plasma samples were pretreated by solid-phase extraction and introduced into a BDS Hypersil $C_{18}$ column ($50{\times}2.1mm$, $5{\mu}m$) for chromatographic separation. The mobile phase consisted of 0.1% formic acid and 0.1% formic acid in acetonitrile, and gradient elution was performed at a flow rate of 0.25 mL/min. For mass spectrometric detection, multiple reaction monitoring was performed via an electrospray ionization source in positive mode. The calibration curve for geniposide was linear ($r^2=0.997$) in the concentration range of $0.005-1{\mu}g/mL$. The intra- and inter-day accuracies and precisions fulfilled the required criteria (${\pm}15%$). The developed method was subsequently used for pharmacokinetic analysis of geniposide after oral administration to rats at a dose of 50 mg/kg. The mean maximum plasma concentration of geniposide was $0.68{\pm}0.29{\mu}g/mL$ at $0.44{\pm}0.13h$, and the mean area under the plasma concentration versus time curve was $1.46{\mu}g{\cdot}h/mL$.

• 한국미생물·생명공학회지
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• 제39권3호
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• pp.266-273
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• 2011

인도산 울금 분말을 bifidobacteria와 lactobacilli를 포함한 프로바이오틱 유산균으로 발효한 시료들의 소염활성 정도를 세포 내 염증성 인자들의 발현양을 관찰함으로써 평가하였다. 그 중 L. johnsonii IDCC 9203으로 발효한 시료의 소염 활성이 가장 뛰어났다. 이를 바탕으로 울금 분말을 포함한 본배양 배지에서 L. johnsonii IDCC 9203으로 21시간 동안 배양 후 얻은 상등액으로 발효 울금 원료를 제조하였고, 제조된 발효 울금 원료에 대한 소염활성 효능을 테스트하기 위해 LPS로 활성화된 raw 264.7 세포주에 처리하고 COX-2와 iNOS의 발현양을 확인하였다. 그 결과 발효 울금 원료 250 ${\mu}g$/mL까지 농도 의존적으로 COX-2와 iNOS의 발현을 감소시켰으며, 그 저해 활성은 동일 농도의 비발효 울금 원료보다 강하였다. NC/Nga 아토피 피부염 동물모델과 PCA 동물모델에서 발효 울금 원료의 효능 확인 결과 대조군에 비해 아토피 피부염의 초기 증상 개선효과와 급작형 과민반응에 대한 예방효과가 뛰어남을 확인하였다. 발효 울금 원료의 유효성분 함량을 분석했을 때 커큐민의 함량은 비발효 울금 원료에 비해 2.5배 증가했으며, 수용성 커큐민의 함량 역시 증가하였다. 또한 비스디메톡시커큐민이나 디메톡시커큐민의 함량도 증가되었을 뿐 아니라 전체 커큐미노이드 중에서 이들 유도체의 비중이 높아짐을 확인하였다. 모든 결과들을 종합하면, 울금 분말을 L. johnsonii IDCC 9203을 이용하여 발효함으로써 유효성분인 커큐미노이드들의 성분비가 변화하고 수용성 커큐미노이드의 증가에 의한 생체 이용율 증가로 울금의 소염 및 항알레르기 활성이 증가된다. 본 연구를 통해 L. johnsonii IDCC 9203으로 발효한 울금 원료는 급성기 피부염에 대한 예방 및 치료 목적으로 사용 가능할 것으로 예상된다.

• ALGAE
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• 제29권4호
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• pp.333-341
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• 2014

In this study, four compounds isolated from the red alga Laurencia snackeyi were evaluated for their potential anti-inflammatory effect in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. These compounds were tested for their inhibitory effects on nitric oxide (NO) production in LPS-stimulated RAW 264.7 cells. Since $5{\beta}$-hydroxypalisadin B showed the best activity it was further tested for the production of prostaglandin-$E_2$ ($PGE_2$), expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), the release of pro-inflammatory cytokines tumor necrotic factor-alpha (TNF-${\alpha}$), interleukin-$1{\beta}$ (IL-$1{\beta}$), and interleukin-6 (IL-6). $5{\beta}$-Hydroxypalisadin B significantly reduced the $PGE_2$ release and suppressed the iNOS and COX-2 expression in LPS-stimulated RAW 264.7 cells. It also significantly reduced the release of pro-inflammatory cytokines TNF-${\alpha}$, IL-$1{\beta}$, and IL-6. These findings provide the first evidence of anti-inflammatory potential of $5{\beta}$-hydroxypalisadin B isolated from the red alga L. snackeyi and hence, it could be exploited as an active ingredient in pharmaceutical, nutraceutical and functional food applications.

• 한국식품위생안전성학회지
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• 제30권3호
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• pp.258-264
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• 2015

본 연구는 윈터체리 추출물의 미백 활성을 검증하여 기능성 미백 소재로서의 가능성을 확인하였다. 먼저, DPPH, ABTS, FRAP를 이용한 항산화 활성 검증에서 윈터체리 추출물은 매우 높은 항산화 효과를 보였으며, 티로시나아 제의 활성에도 농도 의존적인 억제 효과를 보여주었다. 마우스 유래 B16-F10 멜라노마 세포를 이용한 멜라닌 생성에서 윈터체리 추출물이 미치는 영향을 확인한 결과, 세포 내에서 생합성 되는 멜라닌의 양이 상당히 감소하고 있음을 확인하였다. 또한, 멜라닌 생성을 더욱 유도하는 ${\alpha}-MSH$를 세포에 처리하였을 때, 윈터체리 추출물은 농도 의존적인 억제 효능을 보여주었다. 이러한 윈터체리 추출물의 멜라닌 생성 억제는 MITF 전사인자의 발현을 억제함으로써 일어나고, 결과적으로 멜라닌 생합성과 관련된 티로시나아제와 Tyrp-1 등의 단백질 발현을 감소시킴으로써 일어나게 됨을 확인하였다. 이러한 결과들로 볼 때, 윈터체리 추출물은 기존의 미백 원료들을 대체할 수 있을 뿐만 아니라 함께 사용할 경우 상승 효과를 낼 수 있는 새로운 미백 소재로 활용될 수 있을 것이다.