DOCSLIB.ORG

Prediction of Human Renal Clearance from Preclinical Species for a Diverse Set of Drugs That Exhibit Both Active Secretion and Net Re- Absorption

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Prediction of Human Renal Clearance from Preclinical Species for a Diverse Set of Drugs That Exhibit Both Active Secretion and Net Re- Absorption Prediction of human renal clearance from preclinical species for a diverse set of drugs that exhibit both active secretion and net re- absorption Stuart W. Paine, Karelle Ménochet, Rebecca Denton, Dermot F. McGinnity, Robert J. Riley Table 1 Compound CLR Unbound CLR References Human Dog Rat Human Dog Rat Ampicillin 1.39 3.25 11.80 1.70 3.61 13.11 Shrewsbury, 1986; Goodman and Gilman, 1996; Griffin, 2002 Carbamazepine 0.13 0.53 0.45 0.42b 1.96b 2.24b Morselli and Frigerio, 1975; Remmel et al., 1990; Griffin, 2002; Goodman and Gilman, 2006 Cefazolin 0.76 3.14 4.92 9.27b 4.23b 41.02b Komiya et al., 1981; Sawada et al., 1984; Goodman and Gilman, 2006 Cefclidin 1.47 2.52 8.20 1.61 2.75 9.15 Nakashima et al., 1989; Kita et al., 1992 Cefmetazole 1.54 3.92 7.98 7.96b 4.36b 14.25 Sawada et al., 1984 Cefodizime 0.50 1.13 0.40 1.84 2.51 2.86 Klesel et al., 1984; Barre, 1990; Matsushita et al., 1992 Cefoperazone 1.20 3.24 3.11 6.82 4.11b 4.17 Sawada et al., 1984 Cefotetan 0.15 2.11 6.65 1.03 2.35b 9.45 Komiya et al., 1981; Goodman and Gilman, 2006 Cefozopran 2.55 2.69 6.99 3.68 3.00 7.47 Kita et al., 1992; Paulfeuerborn et al., 1993 Cefpiramide 0.07 3.62 3.35 1.78 5.17 6.21 Sawada et al., 1985 Cefpirome 1.17 2.63 8.32 1.30 2.83 9.88 Kavi et al., 1988; Kita et al., 1992; Sakamoto et al., 1993 Ceftazidime 0.88 2.29 8.41 1.12 2.56 8.83 Kita et al., 1992; Sakamoto et al., 1993; Araki et al., 2002; Goodman and Gilman, 2006 Cimetidine 5.15 6.53 37.65 6.35 7.73 45.06 Griffin, 2002; Goodman and Gilman, 2006 Dolasetron 5.02 4.83 34.0 10.25 10.98 77.27 Sanwald-Ducray and Dow, 1997 Donepezil 0.31 0.26 1.19 2.36b 0.43b 2.84b Matsui et al., 1999; Goodman and Gilman, 2006 Fluconazole 0.20 0.60 0.72 0.24b 0.67 0.81 Humphrey et al., 1985; Jezequel, 1994; Goodman and Gilman, 2006 Furosemide 1.18 11.9 2.83 84.19b 383.94b 141.50b Lee et al., 1986; Jang et al., 1994; Goodman and Gilman, 2006 Gabapentin 1.06 1.54 9.08 1.09 1.59 9.37 Radulovic et al., 1995; Goodman and Gilman, 2006 Garenoxacin 0.80 0.37 1.65 3.20 1.61 12.60 Gajjar et al., 2003; Hayakawa et al., 2003 Ibuprofen 0.008 0.06a 0.0002a 1.50b 5.83b 0.01b Goodman and Gilman, 2006 Indomethacin 0.21 0.07a 0.001a 22.11b 8.05b 0.50b Goodman and Gilman, 2006 Inogatran 3.05 3.40 15.7 4.01 4.47 20.66 Teger-Nilsson et al., 1995; Eriksson et al., 1998 Levetiracetam 0.63 0.69 2.18 0.70 0.77 2.42 Isoherranen et al., 2001; Benedetti et al., 2004; Goodman and Gilman, 2006 Losartan 0.97 3.03a 0.003a 48.60b 58.72b 0.33b Goodman and Gilman, 2006 Melagatran 1.71 2.98 8.60 2.00 3.33 9.56 Eriksson et al., 1998; Eriksson et al., 2003 Moxalactam 1.25 1.99 7.69 3.13 3.61 15.08 Sawada et al., 1984 Moxifloxacin 0.50 0.37 3.60 0.90 0.52 5.71 Siefert et al., 1999; Goodman and Gilman, 2006 Naproxen 0.004 0.02 0.06 4.00b 7.87b 22.64b Runkel et al., 1972; Sugawara et al., 1978; Griffin, 2002; Goodman and Gilman, 2006 Ramatroban 1.36 1.65a 0.64 56.67b 30.44b 12.57b Insight., ; Boberg et al., 1997 Ranitidine 7.18 10.1 7.78 8.44 14.43 8.64 Boom et al., 1998; Griffin, 2002; Goodman and Gilman, 2006 Sematilide 3.33 6.10 17.41 3.92b 6.78b 19.34b Hinderling et al., 1993 Sulfinpyrazone 0.08 0.37 0.05 12.02b 6.27b 20.35b Dieterle and Faigle, 1981; Pedersen et al., 1982 Sulfisoxazole 0.13 0.33 0.06 1.15b 0.55 6.00b Yacobi and Levy, 1979; Suber et al., 1981; Oie et al., 1982 Theophylline 0.12 0.82 0.57 0.27 1.46 1.43 Kuze et al., 1988; Poulin and Theil, 2002; Goodman and Gilman, 2006 UK-224,671 0.41 0.90 6.58 0.99 3.21 19.35 Beaumont et al., 2000 UK-240,455 3.66 5.33 6.84 28.15 35.53 228.00 Webster et al., 2003 a: Renal clearances measured in-house. b: Plasma protein binding measured in-house. Araki H, Ogake N, Tsuneda R, Minami S, Watanabe Y, Tamai I and Tsuji A (2002) Muscle distribution of antimicrobial agents after a single intravenous administration to rats. Drug Metab Pharmacokinet 17:237-244. Barre J (1990) Pharmacokinetics of cefodizime: a review of the data on file. J Antimicrob Chemother 26 Suppl C:95-101. Beaumont K, Harper A, Smith DA and Abel S (2000) Pharmacokinetics and metabolism of a sulphamide NK2 antagonist in rat, dog and human. Xenobiotica 30:627-642. Benedetti MS, Coupez R, Whomsley R, Nicolas JM, Collart P and Baltes E (2004) Comparative pharmacokinetics and metabolism of levetiracetam, a new anti-epileptic agent, in mouse, rat, rabbit and dog. Xenobiotica 34:281-300. Boberg M, Ahr HJ, Beckermann B, Buhner K, Siefert HM, Steinke W, Wunsche C and Hirayama M (1997) Pharmacokinetics and metabolism of the new thromboxane A2 receptor antagonist ramatroban in animals. 1st communication: absorption, concentrations in plasma, metabolism, and excretion after single administration to rats and dogs. Arzneimittelforschung 47:928-938. Boom SP, Meyer I, Wouterse AC and Russel FG (1998) A physiologically based kidney model for the renal clearance of ranitidine and the interaction with cimetidine and probenecid in the dog. Biopharm Drug Dispos 19:199-208. Dieterle W and Faigle JW (1981) Species differences in the disposition and metabolism of sulfinpyrazone. Xenobiotica 11:559-568. Eriksson UG, Bredberg U, Hoffmann KJ, Thuresson A, Gabrielsson M, Ericsson H, Ahnoff M, Gislen K, Fager G and Gustafsson D (2003) Absorption, distribution, metabolism, and excretion of ximelagatran, an oral direct thrombin inhibitor, in rats, dogs, and humans. Drug Metab Dispos 31:294-305. Eriksson UG, Renberg L, Bredberg U, Teger-Nilsson AC and Regardh CG (1998) Animal pharmacokinetics of inogatran, a low-molecular-weight thrombin inhibitor with potential use as an antithrombotic drug. Biopharm Drug Dispos 19:55-64. Gajjar DA, Bello A, Ge Z, Christopher L and Grasela DM (2003) Multiple-dose safety and pharmacokinetics of oral garenoxacin in healthy subjects. Antimicrob Agents Chemother 47:2256-2263. Goodman LS and Gilman AG (1996) The Pharmacological Basis of Therapeutics. McGraw-Hill Publishers, New York. Goodman LS and Gilman AG (2006) The Pharmacological Basis of Therapeutics. McGraw-Hill Publishers, New York. Griffin SJ (2002) Evaluation of rat hepatocyte models for the prediction of in vivo clearance. PhD Thesis, University of Manchester. Hayakawa H, Fukushima Y, Kato H, Fukumoto H, Kadota T, Yamamoto H, Kuroiwa H, Nishigaki J and Tsuji A (2003) Metabolism and disposition of novel des-fluoro quinolone garenoxacin in experimental animals and an interspecies scaling of pharmacokinetic parameters. Drug Metab Dispos 31:1409-1418. Hinderling PH, Dilea C, Koziol T and Millington G (1993) Comparative kinetics of sematilide in four species. Drug Metab Dispos 21:662-669. Humphrey MJ, Jevons S and Tarbit MH (1985) Pharmacokinetic evaluation of UK- 49,858, a metabolically stable triazole antifungal drug, in animals and humans. Antimicrob Agents Chemother 28:648-653. Insight. ARD. http://www.adisinsight.com// Isoherranen N, Yagen B, Soback S, Roeder M, Schurig V and Bialer M (2001) Pharmacokinetics of levetiracetam and its enantiomer (R)-alpha-ethyl-2-oxo- pyrrolidine acetamide in dogs. Epilepsia 42:825-830. Jang SH, Lee MG and Kim ND (1994) Pharmacokinetics and pharmacodynamics of furosemide after intravenous and oral administration to spontaneously hypertensive rats and DOCA-salt-induced hypertensive rats. Biopharm Drug Dispos 15:185-206. Jezequel SG (1994) Fluconazole: interspecies scaling and allometric relationships of pharmacokinetic properties. J Pharm Pharmacol 46:196-199. Kavi J, Andrews JM, Ashby JP, Hillman G and Wise R (1988) Pharmacokinetics and tissue penetration of cefpirome, a new cephalosporin. J Antimicrob Chemother 22:911-916. Kita Y, Yamazaki T and Imada A (1992) Comparative pharmacokinetics of SCE- 2787 and related antibiotics in experimental animals. Antimicrob Agents Chemother 36:2481-2486. Klesel N, Limbert M, Seeger K, Seibert G, Winkler I and Schrinner E (1984) Cefodizime, an aminothiazolylcephalosporin. II. Comparative studies on the pharmacokinetic behavior in laboratory animals. J Antibiot (Tokyo) 37:901-909. Komiya M, Kikuchi Y, Tachibana A and Yano K (1981) Pharmacokinetics of new broad-spectrum cephamycin, YM09330, parenterally administered to various experimental animals. Antimicrob Agents Chemother 20:176-183. Kuze T, Miyazaki H and Taneike T (1988) [Theophylline: pharmacokinetics, metabolism and urinary excretion in dogs]. Nippon Yakurigaku Zasshi 91:325-334. Lee MG, Li T and Chiou WL (1986) Effect of intravenous infusion time on the pharmacokinetics and pharmacodynamics of the same total dose of furosemide. Biopharm Drug Dispos 7:537-547. Matsui K, Taniguchi S and Yoshimura T (1999) Correlation of the intrinsic clearance of donepezil (Aricept) between in vivo and in vitro studies in rat, dog and human. Xenobiotica 29:1059-1072. Matsushita H, Suzuki H, Sugiyama Y, Sawada Y, Iga T, Kawaguchi Y and Hanano M (1992) Effect of benzylpenicillin on the disposition of cefodizime in rats: no net effect on total clearance due to decreased hepatobiliary clearance and increased renal clearance.
Load more

Recommended publications
  • The Evolving Role of Direct Thrombin Inhibitors in Acute Coronary
    View metadata, citation and similar papers at core.ac.uk brought to you by CORE Journal of the American College of Cardiology providedVol. by 41, Elsevier No. 4 - SupplPublisher S Connector © 2003 by the American College of Cardiology Foundation ISSN 0735-1097/03/$30.00 Published by Elsevier Science Inc. PII S0735-1097(02)02687-6 The Evolving Role of Direct Thrombin Inhibitors in Acute Coronary Syndromes John Eikelboom, MBBS, MSC, FRACP, FRCPA,* Harvey White, MB, CHB, DSC, FRACP, FACC,† Salim Yusuf, MBBS, DPHIL, FRCP (UK), FRCPC, FACC‡ Perth, Australia; Auckland, New Zealand; and Hamilton, Ontario, Canada The central role of thrombin in the initiation and propagation of intravascular thrombus provides a strong rationale for direct thrombin inhibitors in acute coronary syndromes (ACS). Direct thrombin inhibitors are theoretically likely to be more effective than indirect thrombin inhibitors, such as unfractionated heparin or low-molecular-weight heparin, because the heparins block only circulating thrombin, whereas direct thrombin inhibitors block both circulating and clot-bound thrombin. Several initial phase 3 trials did not demonstrate a convincing benefit of direct thrombin inhibitors over unfractionated heparin. However, the Direct Thrombin Inhibitor Trialists’ Collaboration meta-analysis confirms the superiority of direct thrombin inhibitors, particularly hirudin and bivalirudin, over unfractionated heparin for the prevention of death or myocardial infarction (MI) during treatment in patients with ACS, primarily due to a reduction in MI (odds ratio, 0.80; 95% confidence interval, 0.70 to 0.91) with little impact on death. The absolute risk reduction in the composite of death or MI at the end of treatment (0.8%) was similar at 30 days (0.7%), indicating no loss of benefit after cessation of therapy.
    [Show full text]
  • )&F1y3x PHARMACEUTICAL APPENDIX to THE
    )&f1y3X PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE )&f1y3X PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 3 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. Product CAS No. Product CAS No. ABAMECTIN 65195-55-3 ACTODIGIN 36983-69-4 ABANOQUIL 90402-40-7 ADAFENOXATE 82168-26-1 ABCIXIMAB 143653-53-6 ADAMEXINE 54785-02-3 ABECARNIL 111841-85-1 ADAPALENE 106685-40-9 ABITESARTAN 137882-98-5 ADAPROLOL 101479-70-3 ABLUKAST 96566-25-5 ADATANSERIN 127266-56-2 ABUNIDAZOLE 91017-58-2 ADEFOVIR 106941-25-7 ACADESINE 2627-69-2 ADELMIDROL 1675-66-7 ACAMPROSATE 77337-76-9 ADEMETIONINE 17176-17-9 ACAPRAZINE 55485-20-6 ADENOSINE PHOSPHATE 61-19-8 ACARBOSE 56180-94-0 ADIBENDAN 100510-33-6 ACEBROCHOL 514-50-1 ADICILLIN 525-94-0 ACEBURIC ACID 26976-72-7 ADIMOLOL 78459-19-5 ACEBUTOLOL 37517-30-9 ADINAZOLAM 37115-32-5 ACECAINIDE 32795-44-1 ADIPHENINE 64-95-9 ACECARBROMAL 77-66-7 ADIPIODONE 606-17-7 ACECLIDINE 827-61-2 ADITEREN 56066-19-4 ACECLOFENAC 89796-99-6 ADITOPRIM 56066-63-8 ACEDAPSONE 77-46-3 ADOSOPINE 88124-26-9 ACEDIASULFONE SODIUM 127-60-6 ADOZELESIN 110314-48-2 ACEDOBEN 556-08-1 ADRAFINIL 63547-13-7 ACEFLURANOL 80595-73-9 ADRENALONE
    [Show full text]
  • PHARMACEUTICAL APPENDIX to the TARIFF SCHEDULE 2 Table 1
    Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2020) Revision 19 Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names INN which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service CAS registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known.
    [Show full text]
  • 1 Oral Anticoagulants and Risk of Dementia: a Systematic Review
    Oral Anticoagulants and Risk of Dementia: A Systematic Review and Meta-analysis of Observational Studies and Randomized Controlled Trials Pajaree Mongkhon, PharmD1,2,3; Abdallah Y. Naser, MBA3; Laura Fanning, BPharm (Hons) MPH4; Gary Tse, PhD FACC FRCP5,6; Wallis C.Y. Lau, PhD3; Ian C.K. Wong, PhD3,7,8; Chuenjid Kongkaew, PhD1,3,9 1Centre for Safety and Quality in Health, Department of Pharmacy Practice, Faculty of Pharmaceutical Sciences, Naresuan University, Thailand 2School of Pharmaceutical Sciences, University of Phayao, Thailand 3Research Department of Practice and Policy, School of Pharmacy, University College London, London, United Kingdom 4Eastern Health Clinical School, Faculty of Medicine, Nursing and Health Sciences, Monash University, Melbourne, Australia 5Department of Medicine and Therapeutics, Faculty of Medicine, Chinese University of Hong Kong, Hong Kong, SAR, P.R. China 6Li Ka Shing Institute of Health Sciences, Faculty of Medicine, Chinese University of Hong Kong, Hong Kong, SAR, P.R. China 7Centre for Safe Medication Practice and Research Department of Pharmacology and Pharmacy University of Hong Kong 8Centre for Medication Optimisation Research and Education (CMORE), University College London Hospital, United Kingdom 9Center of Excellence for Environmental Health & Toxicology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok, Thailand 1 Corresponding author Chuenjid Kongkaew, Ph.D. Department of Pharmacy Practice, Faculty of Pharmaceutical Sciences, Naresuan University 99 Moo 9, Phitsanulok-Nakhon Sawan Road, Tha Pho, Mueang Phitsanulok, Phitsanulok 65000, Thailand. Tel: 66 55 961825 Fax: 66 55 963731 E-mail: [email protected] Word count: 4320 words (excluding title page, abstract, references, figures and tables) Number of references: 42 references Number of figures: 3 figures Number of tables: 3 tables 2 Abstract Atrial fibrillation (AF) is a documented risk factor for dementia.
    [Show full text]
  • WO 2010/025328 Al
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date 4 March 2010 (04.03.2010) WO 2010/025328 Al (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 31/00 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, (21) International Application Number: CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, PCT/US2009/055306 DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, 28 August 2009 (28.08.2009) KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (25) Filing Language: English NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, (26) Publication Language: English SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (30) Priority Data: 61/092,497 28 August 2008 (28.08.2008) US (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (71) Applicant (for all designated States except US): FOR¬ GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, EST LABORATORIES HOLDINGS LIMITED [IE/ ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, —]; 18 Parliament Street, Milner House, Hamilton, TM), European (AT, BE, BG, CH, CY, CZ, DE, DK, EE, Bermuda HM12 (BM).
    [Show full text]
  • Computational Antibiotics Book
    Andrew V DeLong, Jared C Harris, Brittany S Larcart, Chandler B Massey, Chelsie D Northcutt, Somuayiro N Nwokike, Oscar A Otieno, Harsh M Patel, Mehulkumar P Patel, Pratik Pravin Patel, Eugene I Rowell, Brandon M Rush, Marc-Edwin G Saint-Louis, Amy M Vardeman, Felicia N Woods, Giso Abadi, Thomas J. Manning Computational Antibiotics Valdosta State University is located in South Georgia. Computational Antibiotics Index • Computational Details and Website Access (p. 8) • Acknowledgements (p. 9) • Dedications (p. 11) • Antibiotic Historical Introduction (p. 13) Introduction to Antibiotic groups • Penicillin’s (p. 21) • Carbapenems (p. 22) • Oxazolidines (p. 23) • Rifamycin (p. 24) • Lincosamides (p. 25) • Quinolones (p. 26) • Polypeptides antibiotics (p. 27) • Glycopeptide Antibiotics (p. 28) • Sulfonamides (p. 29) • Lipoglycopeptides (p. 30) • First Generation Cephalosporins (p. 31) • Cephalosporin Third Generation (p. 32) • Fourth-Generation Cephalosporins (p. 33) • Fifth Generation Cephalosporin’s (p. 34) • Tetracycline antibiotics (p. 35) Computational Antibiotics Antibiotics Covered (in alphabetical order) Amikacin (p. 36) Cefempidone (p. 98) Ceftizoxime (p. 159) Amoxicillin (p. 38) Cefepime (p. 100) Ceftobiprole (p. 161) Ampicillin (p. 40) Cefetamet (p. 102) Ceftoxide (p. 163) Arsphenamine (p. 42) Cefetrizole (p. 104) Ceftriaxone (p. 165) Azithromycin (p.44) Cefivitril (p. 106) Cefuracetime (p. 167) Aziocillin (p. 46) Cefixime (p. 108) Cefuroxime (p. 169) Aztreonam (p.48) Cefmatilen ( p. 110) Cefuzonam (p. 171) Bacampicillin (p. 50) Cefmetazole (p. 112) Cefalexin (p. 173) Bacitracin (p. 52) Cefodizime (p. 114) Chloramphenicol (p.175) Balofloxacin (p. 54) Cefonicid (p. 116) Cilastatin (p. 177) Carbenicillin (p. 56) Cefoperazone (p. 118) Ciprofloxacin (p. 179) Cefacetrile (p. 58) Cefoselis (p. 120) Clarithromycin (p. 181) Cefaclor (p.
    [Show full text]
  • Anew Drug Design Strategy in the Liht of Molecular Hybridization Concept
    www.ijcrt.org © 2020 IJCRT | Volume 8, Issue 12 December 2020 | ISSN: 2320-2882 “Drug Design strategy and chemical process maximization in the light of Molecular Hybridization Concept.” Subhasis Basu, Ph D Registration No: VB 1198 of 2018-2019. Department Of Chemistry, Visva-Bharati University A Draft Thesis is submitted for the partial fulfilment of PhD in Chemistry Thesis/Degree proceeding. DECLARATION I Certify that a. The Work contained in this thesis is original and has been done by me under the guidance of my supervisor. b. The work has not been submitted to any other Institute for any degree or diploma. c. I have followed the guidelines provided by the Institute in preparing the thesis. d. I have conformed to the norms and guidelines given in the Ethical Code of Conduct of the Institute. e. Whenever I have used materials (data, theoretical analysis, figures and text) from other sources, I have given due credit to them by citing them in the text of the thesis and giving their details in the references. Further, I have taken permission from the copyright owners of the sources, whenever necessary. IJCRT2012039 International Journal of Creative Research Thoughts (IJCRT) www.ijcrt.org 284 www.ijcrt.org © 2020 IJCRT | Volume 8, Issue 12 December 2020 | ISSN: 2320-2882 f. Whenever I have quoted written materials from other sources I have put them under quotation marks and given due credit to the sources by citing them and giving required details in the references. (Subhasis Basu) ACKNOWLEDGEMENT This preface is to extend an appreciation to all those individuals who with their generous co- operation guided us in every aspect to make this design and drawing successful.
    [Show full text]
  • Pharmaceutical Appendix to the Harmonized Tariff Schedule
    Harmonized Tariff Schedule of the United States Basic Revision 2 (2021) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States Basic Revision 2 (2021) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names INN which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service CAS registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known.
    [Show full text]
  • Pharmaceutical Appendix to the Tariff Schedule 2
    Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9
    [Show full text]
  • The Antibiotics Composition Comprising Beta-Lactam
    (19) & (11) EP 2 062 581 A1 (12) EUROPEAN PATENT APPLICATION published in accordance with Art. 153(4) EPC (43) Date of publication: (51) Int Cl.: 27.05.2009 Bulletin 2009/22 A61K 31/545 (2006.01) A61K 31/546 (2006.01) A61K 31/43 (2006.01) A61K 31/431 (2006.01) (2006.01) (2006.01) (21) Application number: 07785338.0 A61K 31/424 A61K 31/7036 A61K 47/18 (2006.01) A61K 47/12 (2006.01) (2006.01) (2006.01) (22) Date of filing: 14.08.2007 A61K 47/02 A61K 47/04 A61K 9/08 (2006.01) A61K 9/19 (2006.01) A61K 9/72 (2006.01) A61P 31/04 (2006.01) A61P 31/00 (2006.01) (86) International application number: PCT/CN2007/002438 (87) International publication number: WO 2008/025226 (06.03.2008 Gazette 2008/10) (84) Designated Contracting States: (71) Applicant: Tianjin Hemey Bio-Tech Co., Ltd. AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Tianjin 300457 (CN) HU IE IS IT LI LT LU LV MC MT NL PL PT RO SE SI SK TR (72) Inventor: ZHANG, Hesheng Designated Extension States: Tianjin 300457 (CN) AL BA HR MK RS (74) Representative: Hryszkiewicz, Danuta et al (30) Priority: 25.08.2006 CN 200610015437 Kancelaria Patentowa ul. Jana z Kolna 38 PL-75-204 Koszalin (PL) (54) THE ANTIBIOTICS COMPOSITION COMPRISING BETA-LACTAM ANTIBIOTICS AND IONIC CHELATING AGENTS (57) The antibiotics composition comprising at least tors and buffers simultaneously. The composition can be one of beta-lactam antibiotics and at least one of ionic formulated with at least one of aminoglycoside antibiotics chelating agents used for inhibiting particulate formation, into solution for controlling microbial infection in a con- further comprising at least one of beta-lactamase inhib- tainer.
    [Show full text]
  • Antithrombotic Agents in the Management of Sepsis
    Antithrombotic Agents in the Management of Sepsis !"#$ Loyola University Medical Center, Maywood, Illinois-60153, USA ABSTRACT Sepsis, a systemic inflammatory syndrome, is a response to infection and when associated with mul- tiple organ dysfunction is termed, severe sepsis. It remains a leading cause of mortality in the critically ill. The response to the invading bacteria may be considered as a balance between proinflammatory and antiinflammatory reaction. While an inadequate proinflammatory reaction and a strong antiinflammatory response could lead to overwhelming infection and death of the patient, a strong and uncontrolled pro- inflammatory response, manifested by the release of proinflammatory mediators may lead to microvas- cular thrombosis and multiple organ failure. Endotoxin triggers sepsis by releasing various mediators inc- luding tumor necrosis factor-alpha and interleukin-1(IL-1). These cytokines activate the complement and coagulation systems, release adhesion molecules, prostaglandins, leukotrienes, reactive oxygen speci- es and nitric oxide (NO). Other mediators involved in the sepsis syndrome include IL-1, IL-6 and IL-8; arachidonic acid metabolites; platelet activating factor (PAF); histamine; bradykinin; angiotensin; comp- lement components and vasoactive intestinal peptide. These proinflammatory responses are counterac- ted by IL-10. Most of the trials targeting the different mediators of proinflammatory response have failed due a lack of correct definition of sepsis. Understanding the exact pathophysiology of the disease will enable better treatment options. Targeting the coagulation system with various anticoagulant agents inc- luding antithrombin, activated protein C (APC), tissue factor pathway inhibitor (TFPI) is a rational appro- ach. Many clinical trials have been conducted to evaluate these agents in severe sepsis.
    [Show full text]
  • Center for Drug Evaluation and Research Application
    CENTER FOR DRUG EVALUATION AND RESEARCH APPLICATION NUMBER: 22-512 PHARMACOLOGY REVIEW(S) Tertiary Pharmacology Review By: Paul C. Brown, Ph.D., ODE Associate Director for Pharmacology and Toxicology OND IO NDA: 22-307 Submission date: 4/19/2010 Drug: Pradaxa™ (Dabigatran etexilate mesylate) Sponsor: Boehringer Ingelheim Pharma GmbH & Co. KG Indication: Prevention of stroke and systemic embolism in patients with atrial fibrillation Reviewing Division: Division of Cardiovascular and Renal Products Comments: The pharm/tox reviewer and supervisor found the nonclinical information submitted for dabigatran to be sufficient to support the proposed use. The reviewer proposes pregnancy category C for the labeling. Dabigatran induced some reproductive toxicity in rats manifest as a decreased number of implantations, decreased number of viable fetuses, increase in the resorption rate, increase in post-implantation loss, and an increase in the number of dead offspring when given at doses of 70 mg/kg (about 2.6 to 3 times the MRHD of 300 mg/day on a mg/m2 basis). Dabigatran also induced some fetal structural variations but did not induce fetal malformations in rats or rabbits. Dabigatran was evaluated for carcinogenicity in 2-year rat and mouse studies. The Executive Carcinogenicity Assessment Committee concluded that these studies were adequate and there were no drug-related tumors in either study. Conclusions: I concur with the Division pharm/tox conclusion that the nonclinical data support approval of this NDA. No additional nonclinical studies are recommended at this time. The proposed Established Pharmacologic Class for dabigatran is "direct thrombin inhibitor". This is appropriate because it is consistent with other moieties of this class.
    [Show full text]