Journal of Pharmaceutical Science and Technology, Japan最新文献

Click Therapy: Novel Concept in Pretargeting Drug Delivery 点击疗法:预靶向药物递送的新概念

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 2017-11-01 DOI: 10.14843/JPSTJ.77.306

S. Hapuarachchige

{"title":"Click Therapy: Novel Concept in Pretargeting Drug Delivery","authors":"S. Hapuarachchige","doi":"10.14843/JPSTJ.77.306","DOIUrl":"https://doi.org/10.14843/JPSTJ.77.306","url":null,"abstract":"Click therapy is a pretargeted therapeutic strategy that utilizes bioorthogonal click chemistry for treating cancers that overexpress cell surface receptors. In this strategy, pretargeting component and the drug delivery component undergo click reaction on the cell surface. Click chemistry is a concept of rapid and selective reactions between two functional groups under mild, convenient and reliable conditions1). This synthetic approach is now widely used in the drug development because of high yielding, wide in scope and producing only byproducts that can be removed without chromatography. Click reactions which can be performed in biological systems without interfering regular biochemical and physiological in the living systems are called bioorthogonal click chemistry. Examples of bioorthogonal click chemistry reactions and their reaction rates are shown in the Fig. 1 2). However, only few click reactions can be used as bioorthogonal click reactions in living systems, since they should be biocompatible, fast and feasible in physiological conditions. In click therapy, target-specific mAbs are delivered first to pretarget the cancer cells and are followed by the functionalized drug-carrier nanoplatform (Fig. 2). Two components react chemoselectively on the target cell surface via azide (Az) and dibenzylcyclooctyne (DBCO) (Click-1) or trans-cyclooctene (TCO) and tetrazine (Tt) (Click-2) bioorthogonal click reactions3,4). Due to the close proximity, multiple click reactions between two components are possible on cells with high receptor density on the cell surface. These reactions result in the formation of nanoclusters, which generate tension in the cell membrane and lead to rapid internalization via receptor-mediated endocytosis5).","PeriodicalId":241592,"journal":{"name":"Journal of Pharmaceutical Science and Technology, Japan","volume":"37 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2017-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"120972289","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

The American Pharm.D. Parkour 美国药学博士。跑酷

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 2017-04-01 DOI: 10.14843/JPSTJ.77.118

Jacob Wesley, A. Nkobena

引用次数: 0

Development and Characterization of a Suspension Containing Nanoparticulated Rebamipide for a Mouth Wash for Stomatitis 含纳米关节利巴米胺的口腔炎漱口水悬浮液的研制与表征

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 2017-03-01 DOI: 10.14843/JPSTJ.77.104

Yayoi Kawano, N. Ishii, Yuichiro Shimizu, T. Hanawa

引用次数: 4

A RENEWED PHARMACY FOR A NEW SOCIETY 一个新社会的新药房

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 2016-09-01 DOI: 10.14843/JPSTJ.76.356

C. López

引用次数: 0

Phase Solution and Solution Recrystallization Equilibrium Constants of Hydroxypropyl-β-cyclodextrin Complexes with Nifedipine and Nicardipine Hydrochloride 羟丙基-β-环糊精与硝苯地平和盐酸尼卡地平配合物的相、溶液和溶液重结晶平衡常数

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 2016-07-01 DOI: 10.14843/JPSTJ.76.267

Yingpeng Li, S. Goto, Yohsuke Shimada, K. Makino

{"title":"Phase Solution and Solution Recrystallization Equilibrium Constants of Hydroxypropyl-β-cyclodextrin Complexes with Nifedipine and Nicardipine Hydrochloride","authors":"Yingpeng Li, S. Goto, Yohsuke Shimada, K. Makino","doi":"10.14843/JPSTJ.76.267","DOIUrl":"https://doi.org/10.14843/JPSTJ.76.267","url":null,"abstract":"The calcium-channel blockers nifedipine (NIF) and nicardipine (NIC) hydrochloride (Scheme 1) are ester derivatives of 4-aryl-1,4-dihydropyridine-3,5-dicarboxylate, and they are widely used for the treatment of moderate hypertension and cerebral disease1,2). Because NIF and neutral NIC have low solubility in aqueous solutions and high permeability across biomembranes, they are categorized as class-II drugs on the Biopharmaceutics Classi cation System (BCS) catalog 3). The poor solubility of class-II drugs decreases both their absorption and distribution; therefore, an improvement in their solubility is required to enhance the bioavailability and transportability toward their cellular targets. Cyclodextrin (CD) is a cyclic (α-1,4)-linked oligosaccharide of α-D-glucopyranose. It is widely used to increase the aqueous solubility, stability, and bioavailability of drugs; in addition, it is used to convert crystalline drugs into microcrystalline powders, prevent drug-drug or drug-additive interactions, decrease gastrointestinal irritation, and eliminate unpleasant taste4). These applications exploit the ability of CD and its derivatives to capture insoluble drugs, either by inclusion in the hydrophobic central cavity or by adsorption at the hydrophilic outer surface5). Hydroxypropyl-β-cyclodextrin (HP-β-CD) is a CD alternative, and shows improved aqueous solubility of drugs and resistance to chemical and photodegradation6~8). Moreover, HP-β-CD is utilized in medicines approved for clinical use in oral and intravenous products and suppositories in the United States, Belgium, and Switzerland9). In a previous study, we investigated the physicochemical properties of NIF/HP-β-CD and NIC/ HP-β-CD complexes by differential scanning calorimJ. Pharm. Sci. Technol., Jpn., 76 (4), 267-273 (2016)","PeriodicalId":241592,"journal":{"name":"Journal of Pharmaceutical Science and Technology, Japan","volume":"37 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2016-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"123123686","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 6

Translational Research の実践を目指して Translational Research的实践

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 2004-07-01 DOI: 10.4993/wwaves1995.11.27

山下伸二

引用次数: 0

感染症時における腸管 P-glycoprotein の発現変動感染时肠道P-glycoprotein的表达变化

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 2002-03-05 DOI: 10.14896/JSSXMEETING.17.0.94.0

敦上林, 幹雄富田, 正弘林

引用次数: 0

アスコルビン酸誘導体, disodium 2-O-octadecyl-5, 6-di-O-sulfoascorbate (CV-11464) の水溶液中でのマルトシル-β-シクロデキストリンによる安定化抗坏血酸衍生物，disodium 2-O-octadecyl-5，在6-di-O-sulfoascorbate (CV-11464)的水溶液中通过糖醇-β-环糊精进行稳定

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 1998-06-20 DOI: 10.14843/JPSTJ.58.83

宇田良明, 小川泰亮

引用次数: 0

Effects of the Physicochemical Properties of Oil Vehicles on the Skin Penetration of Poor Skin-Penetrable Materials under Finite Dose Conditions In Vitro 有限剂量条件下油类载具理化性质对皮肤穿透性差材料的影响

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 1900-01-01 DOI: 10.14843/JPSTJ.74.84

O. Sakata, M. Fujii, N. Koizumi, M. Nakade, K. Kameyama, Yoshiteru Watanabe

{"title":"Effects of the Physicochemical Properties of Oil Vehicles on the Skin Penetration of Poor Skin-Penetrable Materials under Finite Dose Conditions In Vitro","authors":"O. Sakata, M. Fujii, N. Koizumi, M. Nakade, K. Kameyama, Yoshiteru Watanabe","doi":"10.14843/JPSTJ.74.84","DOIUrl":"https://doi.org/10.14843/JPSTJ.74.84","url":null,"abstract":"The topical delivery of active ingredients is based on partition and diffusion into the skin; the penetration of active ingredients into the skin depends on their partition coeffi cient (P) and molecular weight. In general, chemical compounds that have high or low P values or a molecular weight over 500 Da are poorly absorbed through the skin1–3). Therefore, drugs used as transdermal therapeutic systems must have appropriate P values (log P=1–3) and low molecular weight (<500 Da) 4). The evaluation of the skin penetration or absorption of these drugs has been performed under infinite conditions in many cases, because this approach facilitates theoretical analyses. However, often, topical agents and cosmetics are used in small amounts, which represent fi nite dosing. There is a possibility that fi nite dosing will change the donor concentration of active ingredients during experiments. One report has addressed the diffi culties of performing measurements and predictions based on fi nite dose conditions5). However, several trials have predicted the behaviors of chemical compounds in these conditions6–8). The OECD Test Guideline 428 also indicates the application of test substances at a concentration of up to 10 mL/cm2; in most cases, this application amount represents a fi nite dose condition9). Active ingredients with characteristics that are inappropriate for skin penetration (e.g., with a high molecular weight and high or low lipophilicity) are often used in skin therapeutics and cosmetics. J. Pharm. Sci. Technol., Jpn., 74 (1), 84-92 (2014)","PeriodicalId":241592,"journal":{"name":"Journal of Pharmaceutical Science and Technology, Japan","volume":"46 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"1900-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"114535967","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Pharmacy and Pharmaceutical Sciences 药学与制药科学

Journal of Pharmaceutical Science and Technology, Japan Pub Date : 1900-01-01 DOI: 10.14843/JPSTJ.75.383

W. Charman

引用次数: 30