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813 results on '"Lee, Beom-Jin"'

172. Investigation of crystallization and salt formation of poorly water-soluble telmisartan for enhanced solubility

Author

Park, Chulhun, Meghani, Nileshkumar M., Shin, Yongkwan, Oh, Euichaul, Park, Jun-Bom, Cui, Jing-Hao, Cao, Qing-Ri, Tran, TT-D, Tran, Ha Lien Phuong, Lee, Beom-Jin, Park, Chulhun, Meghani, Nileshkumar M., Shin, Yongkwan, Oh, Euichaul, Park, Jun-Bom, Cui, Jing-Hao, Cao, Qing-Ri, Tran, TT-D, Tran, Ha Lien Phuong, and Lee, Beom-Jin

Abstract

The crystal changes and salt formation of poorly water-soluble telmisartan (TEL) in various solvents were investigated for enhanced solubility, stability and crystallinity. Polymorphic behaviors of TEL were characterized by dispersing in distilled water, acetone, acetonitrile, DMSO, or ethanol using Method I: without heat and then dried under vacuum at room temperature; and Method II: with heat below boiling temperature, cooled at 5 °C, and then dried under vacuum at 40 °C. For salt formation (Method III), the following four powdered mixtures were prepared by dispersing in solution of hydrochloric acid (HCl) (pH 1.2), TEL/HCl; in simulated gastric fluid (pH 1.2 buffer), TEL/simulated gastric fluid (SGF); in intestinal fluid (pH 6.8 buffer), TEL/simulated intestinal fluid (SIF); or in NaOH (pH 6.8), TEL/NaOH, respectively, and then dried under a vacuum at room temperature. The structures of powdered mixtures were then studied using a field emission scanning electron microscope (FESEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), FTIR, ¹H nuclear magnetic resonance (¹H-NMR), and LC⁻MS. The solubility of TEL in powdered forms was performed in pH 6.8, pH 1.2, and distilled water. No polymorphic behaviors of TEL were observed in various solvents as characterized by FESEM, DSC, PXRD, and FTIR. However, the structural changes of powdered mixtures obtained from Method III were observed due to the formation of salt form. Moreover, the solubility of salt form (TEL/HCl) was highly increased as compared with pure TEL. There were no significant changes of TEL/HCl compared with TEL in the content assay, PXRD, DSC, and FTIR during stressed storage conditions at 40 °C/75% relative humidity (RH) for 4 weeks under the closed package condition. Therefore, the present study suggests the new approach for the enhanced stability and solubility of a poorly water-soluble drug via salt form.

Published
2019

185. Release Kinetics of Hydroxypropyl Methylcellulose Governing DrugRelease and Hydrodynamic Changes of Matrix Tablet

Author

Park, Chulhun, Lee, Jong Hoon, Jin, Gang, Ngo, Hai Van, Park, Jun-Bom, Tran, Thao T.D., Tran, Phuong H.L., and Lee, Beom-Jin

Abstract

Background: Hydrophilic Hydroxypropyl Methylcellulose (HPMC) matrix tablets arethe standard role model of the oral controlled-release formulation. Nevertheless, the HPMC kineticsfor the mechanistic understanding of drug release and hydrodynamic behaviors are rarely investigated.This study aims to investigate the release behaviors of both HPMC and paracetamol(model drug) from the hydrophilic matrix tablet. Methods: Two different viscosity grades of HPMC were used (Low viscosity: 6 cps, High viscosity:4,000 cps). Three different ratios of drug/HPMC (H:38.08%, M:22.85%, and L:15.23% (w/w)of HPMC amounts in total weight) matrix tablets were prepared by wet granulation technique. Therelease profiles of the drug and HPMC in a matrix tablet were quantitatively analyzed by HPLCand 1H-Nuclear Magnetic Resonance (NMR) spectroscopy. The hydrodynamic changes of HPMCwere determined by the gravimetric behaviors such as swelling and erosion rates, gel layer thickness,front movement data,and distributive Near-Infrared (NIR) chemical imaging of HPMC in amatrix tablet during the dissolution process. Results: High viscosity HPMC tablets showed slower release of HPMC than the release rate ofdrug, suggesting that drug release preceded polymer release.Different hydration phenomenon wasqualitatively identified and corresponded to the release profiles. The release behaviors of HPMCand drug in the tablet could be distinguished with the significant difference with fitted dissolutionkinetics model (Low viscosity HPMC 6cps; Korsmeyer-Peppas model, High viscosity HPMC4000cps; Hopfenberg model, Paracetamol; Weibull model) according to the weight of ingredientsand types of HPMC. Conclusion: The determination of HPMC polymer release correlating with drug release, hydrodynamicbehavior, and NIR chemical imaging of HPMC can provide new insights into the drug release-modulating mechanism in the hydrophilic matrix system.

Published
2022
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186. Evaluation of the effects of food on levodropropizine controlled-release tablet and its pharmacokinetic profile in comparison to that of immediate-release tablet

Author

Lee,Soyoung, Nam,Kyu-Yeol, Oh,Jaeseong, Lee,SeungHwan, Cho,Sang-Min, Choi,Youn-Woong, Cho,Joo-Youn, Lee,Beom-Jin, Hong,Jang Hee, Lee,Soyoung, Nam,Kyu-Yeol, Oh,Jaeseong, Lee,SeungHwan, Cho,Sang-Min, Choi,Youn-Woong, Cho,Joo-Youn, Lee,Beom-Jin, and Hong,Jang Hee

Abstract

Soyoung Lee,1,* Kyu-Yeol Nam,2,3,* Jaeseong Oh,1 SeungHwan Lee,1 Sang-Min Cho,3 Youn-Woong Choi,3 Joo-Youn Cho,1 Beom-Jin Lee,2,4,* Jang Hee Hong5,* 1Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, Republic of Korea; 2College of Pharmacy, Ajou University, Suwon, Republic of Korea; 3Korea United Pharm Inc., Seoul, Republic of Korea; 4Institute of Pharmaceutical Science and Technology, Ajou University, Suwon, Republic of Korea; 5Department of Pharmacology, Chungnam National University Hospital and College of Medicine, Daejeon, Republic of Korea *These authors contributed equally to this work Background: Levodropropizine is a non-opioid antitussive agent that inhibits cough reflex by reducing the release of sensory peptide in the peripheral region. To improve patients’ compliance, a controlled-release (CR) tablet is under development. The aim of this study was to compare the pharmacokinetic (PK) profiles of the CR and immediate-release (IR) tablets of levodropropizine. In addition, the effect of food on the PK properties of levodropropizine CR tablet in healthy subjects was evaluated.Subjects and methods: A randomized, open-label, multiple-dose, three-treatment, three-period, six-sequence, crossover study was conducted on 47 healthy subjects. All subjects were randomly assigned to one of the six sequences, which involve combinations of the following three treatments: levodropropizine IR 60 mg three times in the fasted state (R), levodropropizine CR 90 mg two times in the fasted state (T), and levodropropizine CR 90 mg two times in the fed state (TF). Serial blood samples were collected up to 24 h after the first dose. Tolerability was assessed based on the vital signs, adverse events (AEs), and clinical laboratory tests.Results: Levodropropizine CR showed lower maximum drug concentration (Cmax) and similar total exposure compared to levodropropizine IR

Published
2018

187. Protein corona: a new approach for nanomedicine design

Author

Nguyen,Van Hong and Lee,Beom-Jin

Subjects
International Journal of Nanomedicine
Abstract

Van Hong Nguyen, Beom-Jin Lee Department of Pharmacy, Bioavailability Control Laboratory, College of Pharmacy, Ajou University, Suwon, Republic of Korea Abstract: After administration of nanoparticle (NP) into biological fluids, an NP–protein complex is formed, which represents the “true identity” of NP in our body. Hence, protein–NP interaction should be carefully investigated to predict and control the fate of NPs or drug-loaded NPs, including systemic circulation, biodistribution, and bioavailability. In this review, we mainly focus on the formation of protein corona and its potential applications in pharmaceutical sciences such as prediction modeling based on NP-adsorbed proteins, usage of active proteins for modifying NP to achieve toxicity reduction, circulation time enhancement, and targeting effect. Validated correlative models for NP biological responses mainly based on protein corona fingerprints of NPs are more highly accurate than the models solely set up from NP properties. Based on these models, effectiveness as well as the toxicity of NPs can be predicted without invivo tests, while novel cell receptors could be identified from prominent proteins which play important key roles in the models. The ungoverned protein adsorption onto NPs may have generally negative effects such as rapid clearance from the bloodstream, hindrance of targeting capacity, and induction of toxicity. In contrast, controlling protein adsorption by modifying NPs with diverse functional proteins or tailoring appropriate NPs which favor selective endogenous peptides and proteins will bring promising therapeutic benefits in drug delivery and targeted cancer treatment. Keywords: protein-nanoparticle interaction, protein corona, exchange of adsorbed protein, toxicity reduction, predictive modeling, targeting drug delivery

Published
2017

192. Vaccinium bracteatum Leaf Extract Reverses Chronic Restraint Stress-Induced Depression-Like Behavior in Mice: Regulation of Hypothalamic-Pituitary-Adrenal Axis, Serotonin Turnover Systems, and ERK/Akt Phosphorylation

Author

Oh, Dool-Ri, primary, Yoo, Ji-Seok, additional, Kim, Yujin, additional, Kang, Huwon, additional, Lee, Hunmi, additional, Lm, So J., additional, Choi, Eun-jin, additional, Jung, Myung-A, additional, Bae, Donghyuck, additional, Oh, Kyo-Nyeo, additional, Hong, Ji-Ae, additional, Jo, Ara, additional, Shin, Jawon, additional, Kim, Jaeyong, additional, Kim, Young R., additional, Cho, Seung S., additional, Lee, Beom-Jin, additional, and Choi, Chul yung, additional

Published
2018
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