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Development and Validation of a UHPLC-UV Method for The
Development and validation of a UHPLC-UV method for the detection and quantification of erectile dysfunction drugs and some of their analogues found in counterfeit medicines. Pierre-Yves Sacré a,b, Eric Deconinck a, Patrice Chiap c, Jacques Crommen b, François Mansion b, Eric Rozet d, Patricia Courselle a, Jacques O. De Beer a,* a Laboratory of Drug Analysis, Scientific Institute of Public Health, Brussels, Belgium b Department of Analytical Pharmaceutical Chemistry, Institute of Pharmacy, University of Liège, Liège, Belgium. c Advanced Technology Corporation (A.T.C.), University Hospital of Liège, Liège, Belgium d Department of Analytical Chemistry, Institute of Pharmacy, University of Liège, Liège, Belgium. Abstract Pharmaceutical counterfeiting is a permanently growing problem. Control laboratories are constantly analysing counterfeit medicines. In industrialised countries, one of the main counterfeited class of medicines are erectile dysfunction drugs. This paper describes the development and validation of a fast method to detect and quantify the three authorised phosphodiesterase type 5 inhibitors and five analogues. The method is based on the use of a sub-2 microns polar-embedded column with a gradient using acetonitrile as organic modifier and 10 mM ammonium formate buffer (pH 3.5) as aqueous component of the mobile phase. The separation was achieved in less than 4.5 min. The method has also been compared to the registered HPLC method for the assay of Viagra ® which was considered as the reference method. The method is also compatible with on-line coupling mass spectrometry and will significantly reduce analysis times and solvent consumption. Keywords: Phosphodiesterase type 5 inhibitors; UHPLC; method validation, analogues, counterfeit drugs, accuracy profiles. -
Screening of Phosphodiesterase-5 Inhibitors and Their Analogs in Dietary Supplements by Liquid Chromatography–Hybrid Ion Trap–Time of Flight Mass Spectrometry
molecules Article Screening of Phosphodiesterase-5 Inhibitors and Their Analogs in Dietary Supplements by Liquid Chromatography–Hybrid Ion Trap–Time of Flight Mass Spectrometry 1,2, 1,3, 4 5 3 Unyong Kim y, Hyun-Deok Cho y, Myung Hee Kang , Joon Hyuk Suh , Han Young Eom , Junghyun Kim 6, Sumin Seo 1, Gunwoo Kim 1, Hye Ryoung Koo 1, Nary Ha 1, Un Tak Song 1 and Sang Beom Han 1,* 1 Department of Pharmaceutical Analysis, College of Pharmacy, Chung-Ang University, 84 Heukseok-ro, Dongjak-gu, Seoul 06974, Korea; [email protected] (U.K.); [email protected] (H.-D.C.); [email protected] (S.S.); [email protected] (G.K.); [email protected] (H.R.K); [email protected] (N.H.); [email protected] (U.T.S.) 2 Biocomplete Co., Ltd., 272 Digital-ro, Guro-gu, Seoul 08389, Korea 3 Bioanalysis and Pharmacokinetics Study Group, Korea Institute of Toxicology, 141 Gajeong-ro, Yuseong-gu, Daejeon 34114, Korea; [email protected] 4 Agro-Livestock and Fishery Products Division, Busan Regional Korea Food and Drug Administration, 222 Geoje-daero, Yunje-gu, Busan 47537, Korea; [email protected] 5 Department of Food Science and Human Nutrition, Citrus Research and Education Center, University of Florida, 700 Experiment Station Rd, Lake Alfred, FL 33850, USA; joonhyuksuh@ufl.edu 6 Forensic Toxicology Division, National Forensic Service, 10 Ipchoon-ro, Wonju, Gangwon-do 26460, Korea; [email protected] * Correspondence: [email protected]; Tel.: +82-2-820-5596 These authors contributed equally to this work. y Received: 22 May 2020; Accepted: 9 June 2020; Published: 12 June 2020 Abstract: An accurate and reliable method based on ion trap–time of flight mass spectrometry (IT–TOF MS) was developed for screening phosphodiesterase-5 inhibitors, including sildenafil, vardenafil, and tadalafil, and their analogs in dietary supplements. -
Call for Methods
CALL FOR METHODS Methods for Identification, Determination, or Screening Methods for PDE5 Inhibitors AOAC INTERNATIONAL invites method developers to submit methods for consideration and possible evaluation through the AOAC Official MethodsSM program. Prospective methods may be qualitative, identification methods, and/or screening methods for phosphodiesterase type 5 inhibitors (PDE5 inhibitors) in dietary ingredients and supplements. OBJECTIVE: The objective of this call for methods is to select and evaluate methods that can be used for routine surveillance of dietary ingredients. Acceptable methods must be reliable and reproducible when used by trained analysts in accredited laboratories. Interested method developers should provide a description of their proposed method and data characterizing the analytical performance of the proposed method. For the purpose of this Call-for-Methods, PDE5 inhibitors are defined as avanafil, lodenafil carbonate, mirodenafil, sildenafill, tadalafil, udenafil, or vardenafil; or any of their analogs. Any analytical technique that measures the analytes of interest and meets the method performance requirements specified in the SMPR will be considered. It is acceptable to have a different analytical method for each class of analytes. Applicable SMPRs: • View AOAC 2014.010 – Methods for the Identification of PDE5 Inhibitors • View AOAC SMPR 2014.011 – Methods for the Determination of PDE5 Inhibitors • View AOAC SMPR 2014.012 – Screening Methods for PDE5 Inhibitors Submit Your Method AOAC INTERNATIONAL METHOD SUBMISSION PROCESS: AOAC invites method authors to submit their methods with no fee required. Interested method authors or developers should provide a copy of their proposed method, as well as any available data characterizing the analytical performance and scientific validity of the method in AOAC format. -
2251 Adulteration of Dietary Supplements with Drugs
BRIEFING 2251 Adulteration of Dietary Supplements with Drugs and Drug Analogs. This new general chapter provides tools for detection of dietary supplement adulteration with ⟨extraneously⟩ added synthetic compounds. The illegal addition of synthetic substances to products marketed as dietary supplements constitutes a significant threat to consumer health, considering that these products, administered without medical supervision, may contain toxic constituents or substances whose safety has never been examined, and whose interaction with medications may be unpredictable or lethal. The proposed chapter suggests multiple methods for detection of adulteration. It is advisable to use several screening techniques to maximize the potential for adulteration detection, because no single methodology is universally applicable. Presently, the chapter targets supplements adulterated with phosphodiesterase type 5 inhibitors; subsequent revisions will include methodologies specific to analysis of adulterated weight loss and sports performance enhancement products. It is anticipated that this chapter will be updated regularly. (GCCA: A. Bzhelyansky.) Correspondence Number—C144928 Add the following: ▪ 2251 ADULTERATION OF DIETARY SUPPLEMENTS WITH DRUGS AND DRUG ANALOGS ⟨ ⟩ INTRODUCTION The illegal addition of undeclared synthetic compounds to products marketed as dietary supplements1 (DS) is a serious problem. This fraud is practiced to impart therapeutic effects that cannot be achieved by the supplement constituents alone. Increasingly, synthetic intermediates and structural analogs of the pharmaceuticals and drugs that have been discontinued or withdrawn from the market due to unsatisfactory safety profiles are being used as adulterants. Multiple adulterating compounds may be added to a single DS, frequently in erratic amounts. The proposed test methodologies facilitate screening of DS for synthetic adulterants. No individual technique is capable of addressing all potential analytes; thus, a combination of orthogonal approaches adds certainty to the analytical outcome. -
Phosphodiesterase (PDE)
Phosphodiesterase (PDE) Phosphodiesterase (PDE) is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases, as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules. www.MedChemExpress.com 1 Phosphodiesterase (PDE) Inhibitors, Activators & Modulators (+)-Medioresinol Di-O-β-D-glucopyranoside (R)-(-)-Rolipram Cat. No.: HY-N8209 ((R)-Rolipram; (-)-Rolipram) Cat. No.: HY-16900A (+)-Medioresinol Di-O-β-D-glucopyranoside is a (R)-(-)-Rolipram is the R-enantiomer of Rolipram. lignan glucoside with strong inhibitory activity Rolipram is a selective inhibitor of of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM phosphodiesterase. and 240 nM for PDE4A, PDE4B, and PDE4D, respectively. Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg (R)-DNMDP (S)-(+)-Rolipram Cat. No.: HY-122751 ((+)-Rolipram; (S)-Rolipram) Cat. No.: HY-B0392 (R)-DNMDP is a potent and selective cancer cell (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, AMP(cAMP)-specific phosphodiesterase (PDE) binds PDE3A directly. -
The Use of Stems in the Selection of International Nonproprietary Names (INN) for Pharmaceutical Substances
WHO/PSM/QSM/2006.3 The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances 2006 Programme on International Nonproprietary Names (INN) Quality Assurance and Safety: Medicines Medicines Policy and Standards The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 © World Health Organization 2006 All rights reserved. Publications of the World Health Organization can be obtained from WHO Press, World Health Organization, 20 Avenue Appia, 1211 Geneva 27, Switzerland (tel.: +41 22 791 3264; fax: +41 22 791 4857; e-mail: [email protected]). Requests for permission to reproduce or translate WHO publications – whether for sale or for noncommercial distribution – should be addressed to WHO Press, at the above address (fax: +41 22 791 4806; e-mail: [email protected]). The designations employed and the presentation of the material in this publication do not imply the expression of any opinion whatsoever on the part of the World Health Organization concerning the legal status of any country, territory, city or area or of its authorities, or concerning the delimitation of its frontiers or boundaries. Dotted lines on maps represent approximate border lines for which there may not yet be full agreement. The mention of specific companies or of certain manufacturers’ products does not imply that they are endorsed or recommended by the World Health Organization in preference to others of a similar nature that are not mentioned. Errors and omissions excepted, the names of proprietary products are distinguished by initial capital letters. -
Designer Drugs: a Review
WORLD JOURNAL OF PHARMACY AND PHARMACEUTICAL SCIENCES Chavan et al. World Journal of Pharmacy and Pharmaceutical Sciences SJIF Impact Factor 5.210 Volume 4, Issue 08, 297-336. Review Article ISSN 2278 – 4357 DESIGNER DRUGS: A REVIEW Dr. Suyash Chavan,MBBS*1 and Dr. Vandana Roy2 1MD, Resident Doctor, Department of Pharmacology, Maulana Azad Medical College, New Delhi. 2MD, PhD Professor, Department of Pharmacology, Maulana Azad Medical College, New Delhi. ABSTRACT Article Received on 25 May 2015, Designer drugs‟ are psychoactive substances that mimic the effects of Revised on 16 June 2015, other banned illicit drugs but evade detection by law enforcing Accepted on 07 July 2015 agencies. This is because of modifications in the structure of the original psychoactive molecule. Originally developed as a way to *Correspondence for evade existing drug laws in the late 1960s, the synthesis and use of Author designer drugs has increased dramatically. They are advertised with Dr. Suyash Chavan innocuous names and are sold mostly over the internet, discreet outlets MD, Resident Doctor, Department of and at entertainment clubs. Victims may exhibit symptoms similar to Pharmacology, Maulana the effects of the illegal drug that these synthetic drugs mimic, Azad Medical College, however, the exact culprit drug is not detected due to structural New Delhi. modifications in the new drug. Overdose of these drugs may lead to serious adverse effects that can be life threatening. Understanding the pharmacology and toxicology of these agents is essential to facilitate their detection and to provide better medical care for patients suffering from adverse effects due to their consumption. -
The Effects of the Combined Use of a PDE5 Inhibitor and Medications for Hypertension, Lower Urinary Tract Symptoms and Dyslipidemia on Corporal Tissue Tone
International Journal of Impotence Research (2012) 24, 221 -- 227 & 2012 Macmillan Publishers Limited All rights reserved 0955-9930/12 www.nature.com/ijir ORIGINAL ARTICLE The effects of the combined use of a PDE5 inhibitor and medications for hypertension, lower urinary tract symptoms and dyslipidemia on corporal tissue tone JH Lee1,2, MR Chae1,2, JK Park1,3, JH Jeon1,4 and SW Lee1,2 ED is closely associated with its comorbidities (hypertension, dyslipidemia and lower urinary tract symptoms (LUTS)). Therefore, several drugs have been prescribed simultaneously with PDE5 inhibitors. If a specific medication for ED comorbidities has enhancing effects on PDE5 inhibitors, it offers alternative combination therapy in nonresponders to monotherapy with PDE5 inhibitors and allows clinicians to treat ED and its comorbidities simultaneously. To establish theoretical basis of choosing an appropriate medication for ED and concomitant disease, we examined the effects combining a PDE5 inhibitor with representative drugs for hypertension, dyslipidemia and LUTS on relaxing the corpus cavernosum of rabbits using the organ- bath technique. The effect of mirodenafil on relaxing phenylephrine-induced cavernosal contractions was significantly enhanced À4 À6 À6 À7 À9 by the presence of 10 M losartan, 10 M nifedipine, 10 M amlodipine, 10 M doxazosin and 10 M tamsulosin (Po0.05). The maximum relaxation effects were 47.2±3.8%, 57.6±2.6%, 64.0±3.7%, 76.1±5.7% and 71.7±5.4%, respectively. Enalapril and simvastatin had no enhancing effects. The relaxation induced by sodium nitroprusside alone (39.0±4.0%) was significantly À4 enhanced in the presence of the 10 M losartan (66.0±6.0%, Po0.05). -
207/2015 3 Lääkeluettelon Aineet, Liite 1. Ämnena I
207/2015 3 LÄÄKELUETTELON AINEET, LIITE 1. ÄMNENA I LÄKEMEDELSFÖRTECKNINGEN, BILAGA 1. Latinankielinen nimi, Suomenkielinen nimi, Ruotsinkielinen nimi, Englanninkielinen nimi, Latinskt namn Finskt namn Svenskt namn Engelskt namn (N)-Hydroxy- (N)-Hydroksietyyli- (N)-Hydroxietyl- (N)-Hydroxyethyl- aethylprometazinum prometatsiini prometazin promethazine 2,4-Dichlorbenzyl- 2,4-Diklooribentsyyli- 2,4-Diklorbensylalkohol 2,4-Dichlorobenzyl alcoholum alkoholi alcohol 2-Isopropoxyphenyl-N- 2-Isopropoksifenyyli-N- 2-Isopropoxifenyl-N- 2-Isopropoxyphenyl-N- methylcarbamas metyylikarbamaatti metylkarbamat methylcarbamate 4-Dimethyl- ami- 4-Dimetyyliaminofenoli 4-Dimetylaminofenol 4-Dimethylaminophenol nophenolum Abacavirum Abakaviiri Abakavir Abacavir Abarelixum Abareliksi Abarelix Abarelix Abataceptum Abatasepti Abatacept Abatacept Abciximabum Absiksimabi Absiximab Abciximab Abirateronum Abirateroni Abirateron Abiraterone Acamprosatum Akamprosaatti Acamprosat Acamprosate Acarbosum Akarboosi Akarbos Acarbose Acebutololum Asebutololi Acebutolol Acebutolol Aceclofenacum Aseklofenaakki Aceklofenak Aceclofenac Acediasulfonum natricum Asediasulfoni natrium Acediasulfon natrium Acediasulfone sodium Acenocoumarolum Asenokumaroli Acenokumarol Acenocumarol Acepromazinum Asepromatsiini Acepromazin Acepromazine Acetarsolum Asetarsoli Acetarsol Acetarsol Acetazolamidum Asetatsoliamidi Acetazolamid Acetazolamide Acetohexamidum Asetoheksamidi Acetohexamid Acetohexamide Acetophenazinum Asetofenatsiini Acetofenazin Acetophenazine Acetphenolisatinum Asetofenoli-isatiini -
Illicit Erectile Dysfunction Products in the Netherlands Dysfunction a Decade of Trends and a 2007-2010 Product Update Products
Illicit erectile Illicit erectile dysfunction products in the Netherlands dysfunction A decade of trends and a 2007-2010 product update products Illicit erectile dysfunction products in the Netherlands A decade of trends and a 2007-2010 product update RIVM Report 370030003/2010 RIVM Report 370030003 Colophon © RIVM 2010 Parts of this publication may be reproduced, provided acknowledgement is given to the 'National Institute for Public Health and the Environment', along with the title and year of publication. B.J. Venhuis, National Institute for Public Health and the Environment M.E. Zwaagstra, Dutch Customs Laboratory J.D.J. van den Berg, Netherlands Forensic Institute A.J.H.P. van Riel, National Poisons Information Center H.W.G. Wagenaar, Royal Dutch Association for the Advancement of Pharmacy K. van Grootheest, National Pharmacovigilance Centre Lareb D.M. Barends, National Institute for Public Health and the Environment D. de Kaste, National Institute for Public Health and the Environment Contact: Dries de Kaste Centre for Quality of Chemical Pharmaceutical Products [email protected] This investigation was commissioned by The Netherlands Health Care Inspectorate (IGZ), and carried out within the framework of V/370030/10/PC Page 2 of 73 RIVM Report 370030003 Abstract Illicit erectile dysfunction products in the Netherlands A decade of trends and a 2007-2010 product update Illicit erectile dysfunction (ED) products often contain experimental medicines. The acute health risks of using such illicit ED products, however, appear to be relatively low – at least to date. Less health damage has been reported than expected based on the presumed use of these products, although their long-term effects on human health are unknown. -
Validation of an HPLC-MS Method for the Determinatin of Vardenafil in Rat Urine
Journal of Applied Pharmaceutical Science Vol. 9(08), pp 079-085, August, 2019 Available online at http://www.japsonline.com DOI: 10.7324/JAPS.2019.90811 ISSN 2231-3354 Validation of an HPLC-MS method for the determinatin of vardenafil in rat urine Liudmila Osypchuk*, Iryna Halkevych, Sophia Davydovych, Yuriy Bidnychenko Department of Toxicological and Analytical Chemistry, Danylo Halytsky Lviv National Medical University, Lviv, Ukraine. ARTICLE INFO ABSTRACT Received on: 24/04/2019 A simple and accurate technique of high-performance liquid chromatography with mass spectrometry was developed Accepted on: 05/06/2019 for the quantitative determination of vardenafil and its metabolites in urine. Extraction of vardenafil and internal Available online: 03/08/2019 standard (sildenafil) was performed from 5 ml of urine with 1,2-dichloroethane at pH = 7.5, followed by purification of samples on Oasis HLB cartridges. Chromatographic separation was carried out on a Zorbax SB-C18 reversed- phase column (50 mm × 2.1 mm) in linear gradient mode, at a rate of 0.4 ml/minute. Mobile phase composition: 0.1% Key words: aqueous formic acid solution and 0.1% formic acid solution in acetonitrile. Detection of vardenafil and sildenafil in vardenafil, HPLC, mass samples was performed using a single quadrupole mass spectrometer with electrospray ionization. Mass spectral spectrometry, urine. analysis was performed in the m/z range: 50–500 with the fragmentation of 50 m/z under positive ionization. The linear dependence for vardenafil was in the range of 7–500 ng/ml; limit of detection and limit of quantification were 5 and 7 ng/ml, respectively. -
Sildenafil 4.0—Integrated Synthetic Chemistry, Formulation And
pharmaceuticals Review Sildenafil 4.0—Integrated Synthetic Chemistry, Formulation and Analytical Strategies Effecting Immense Therapeutic and Societal Impact in the Fourth Industrial Era Andreas Ouranidis 1,2,*, Anastasia Tsiaxerli 1, Elisavet Vardaka 1 , Catherine K. Markopoulou 3, Constantinos K. Zacharis 3 , Ioannis Nicolaou 4, Dimitris Hatzichristou 5, Anna-Bettina Haidich 6 , Nikolaos Kostomitsopoulos 7 and Kyriakos Kachrimanis 1,* 1 Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece; [email protected] (A.T.); [email protected] (E.V.) 2 Department of Chemical Engineering, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece 3 Laboratory of Pharmaceutical Analysis, Department of Pharmaceutical Technology, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece; [email protected] (C.K.M.); [email protected] (C.K.Z.) 4 Laboratory of Pharmaceutical Chemistry, Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece; [email protected] Citation: Ouranidis, A.; Tsiaxerli, A.; 5 Department of Urology, Medical School, Aristotle University of Thessaloniki, 54635 Thessaloniki, Greece; Vardaka, E.; Markopoulou, C.K.; [email protected] 6 Zacharis, C.K.; Nicolaou, I.; Department of Hygiene, Social-Preventive Medicine and Medical Statistics, Medical School, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece; [email protected]