DOCSLIB.ORG

(12) United States Patent (10) Patent No.: US 8,097,607 B2 Cabana Et Al

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
(12) United States Patent (10) Patent No.: US 8,097,607 B2 Cabana Et Al USO08097607B2 (12) United States Patent (10) Patent No.: US 8,097,607 B2 Cabana et al. (45) Date of Patent: *Jan. 17, 2012 (54) LOW DOSE RIFALAZIL COMPOSITIONS Emori et al., “Evaluation of in Vivo Therapeutic Efficacy of a New Benzoxazinorifamycin, KRM-1648, in SCID Mouse Model for Dis (76) Inventors: Bernard E. Cabana, Montgomery seminated Mycobacterium avium Complex Infection.” International Village, MD (US); Arthur F. Michaelis, Journal of Antimicrobial Agents 10(1):59 (1998). Devon, PA (US); Gary P. Magnant, Fujii et al., “In Vitro and In Vivo Antibacterial Activities of KRM Topsfield, MA (US); Chalom B. 1648 and KRM-1657, New Rifamycin Derivatives.” Antimicrobial Sayada, Luxembourg (LU) Agents and Chemotherapy 38: 1118, (1994). Gidoh et al., “Bactericidal Action at Low Doses of a New Rifamycin (*) Notice: Subject to any disclaimer, the term of this Derivative, 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl) patent is extended or adjusted under 35 Benzoxazinorifamycin (KRM-1648) on Mycobacterium leprae U.S.C. 154(b) by 447 days. Inoculated into Ffootpads of Nude Mice.” Leprosy Review 63(4):319 This patent is Subject to a terminal dis (1992). claimer. Heep et al., “Detection of Rifabutin Resistance and Association of rpoB Mutation S with Resistance to Four Rifamycin Derivatives in Helicobacter pylori.” Journal of Clinical Microbiology & Infectious (21) Appl. No.: 10/668,792 Diseases 21:143 (2002). Hirara et al., “In Vitro and in Vivo Activities of the (22) Filed: Sep. 23, 2003 Benezoxazinorifamycin KRM-1648 Against Mycobacterium tuber (65) Prior Publication Data culosis,” Antimocrobial Agents and Chemotherapy 39 (10):2295 (1995). US 2004/O15784.0 A1 Aug. 12, 2004 Hosoe et al., “Identification and Antimicrobial Activity of Urinary Metabolites of a Rifamycin Derivative in Dog,” Xenoblotica Related U.S. Application Data 26(3):321 (1996). Hosoe et al., “Pharmacokinetics of KRM-1648, a New (60) Provisional application No. 60/412,958, filed on Sep. Benzoxazinorifamycin, in Rats and Dogs.” Antimicrobial and Che 23, 2002. motherapy 40(12):2749 (1996). Ji et al., “How Effective is KRM-1648 in Treatment of Disseminated (51) Int. Cl. Mycobacterium avium Complex Infections in Beige Mice?.” Antimi A6 IK3I/33 (2006.01) crobial Agents and Chemotherapy 40(2):437 (1996). (52) U.S. Cl. ....................................................... S14f183 Kelly et al., “Low-Dose Aerosol Infection Model for Testing Drugs (58) Field of Classification Search ........................ None for Efficacy Against Mycobacterium tuberculosis,” Antimicrobial See application file for complete search history. Agents and Chemotherapy 40(12):2809 (1996). Klemens et al., “Activity of KRM-1648 in Comination with Isoniazid (56) References Cited Against Mycobacterium tuberculosis in a Murine Model.” Antimi crobial Agents and Chemotherapy 40(2):298 (1996). U.S. PATENT DOCUMENTS Lenaerts et al., “Evaluation of Rifalazil in a Combination Treatment 4,983,602 A 1/1991 Yamane et al. ............ 514,229.5 Regimen as an Alternative to Isoniazid-Rifampin Therapy in a Mouse 5,547,683 A 8, 1996 Yano et al. ..... ... 424,501 Tuberculosis Model.” Antimicrobial Agents and Chemotherapy 5,786,349 A 7, 1998 Yamashita et al. ............ 514/183 44(11):3167 (2000). 5,981.522 A 11/1999 Yamashita et al. ......... 514/224.5 Mae et al., “Effect of a New Rifamycin Derivative, Rifalazil, on Liver 6,316,433 B1 1 1/2001 Rose et al. .. ... 514, 183 Microsomal Enzyme Induction in Rat and Dog,” Xenoblotica 6,486,161 B1 1 1/2002 Fujii et al. ............. 514,252.13 6,566,354 B1 5/2003 Montgomery et al. ....... 514, 183 28(8):759 (1998). 2003/0203903 A1 10, 2003 Rose et al. ................. 514,229.8 Mae et al., “Isolation and Identification of Major Metabolites of 2003/0236265 A1* 12/2003 Sayada .................... 514,252.13 Rifalazil in Mouse and Human.” Xenobiotica 29:1073 (1999). 2004/00 14750 A1 1/2004 Michaelis et al. ......... 514,224.5 Roblin et al., “In Vitro Activities of Rifamycin Derivatives ABI-1648 2004.0034021 A1 2/2004 Michaelis et al. 514/310 (Rifazil, KRM-1648), ABI-1657, and ABI-1131 Against Chlamydia 2004/OO77533 A1 4/2004 Sayada ............................. 5148 trachomatis and Recent Clinical Isolates of Chlamydia 2004/0106590 A1* 6/2004 Eisenstein 514, 183 pneumoniae," Antimicrobial Agents and Chemotherapy 47: 1135 2004/O126414 A1 7/2004 Michaelis .................. 514,224.5 (2003). 2004/0176404 A1 9/2004 Sayada .......... 514,252.13 Sano et al., “Therapeutic Effects of Benzoxazinorifamycin KRM 2005, 01371.89 A1* 6, 2005 Van Duzer et al. 514,224.5 1648 Administered Alone or in Combination with a Half-sized Secre 2005/0143409 A1* 6/2005 Michaelis et al. ............ 514,291 tory Leukocyte Protease Inhibitor or the Nonsteroidal Anti-inflam OTHER PUBLICATIONS matory Drug Diclofenac Sodium against Mycobacterium avium Complex Infection in Mice.” Antimicrobial Agents and Chemo Lithander et al., British Journal of Ophthalmology, 2001, 85:371.* therapy 43(2):360 (1999). Remington's Pharmaceutical Sciences, (1975) 15" edition, p. 703.* “Rifalazil PathoGenesis Plans Phase II Studies.” R&D Focus Drug (Continued) News. Jun. 9, 1997. Bermudez et al., “Activity of KRM 1648 Alone or in Combination Primary Examiner — Phyllis G. Spivack with Ethambutolor Clarithromycin Against Mycobacterium avium in (74) Attorney, Agent, or Firm — David Bradin: Steven J. Beige Mouse Model of Disseminated Infection.” Antimicrobial Hultquist; Hultquist IP Agents and Chemotherapy 38(8): 1844 (1994). Dietzeet al., “Safety and Bactericidal Activity of Rifalazil in Patients (57) ABSTRACT with Pulmonary Tuberculosis.” Antimicrobial Agents and Chemo therapy 45(7): 1972 (2001). The invention features low-dosage rifalazil compositions Dhople AM, “In Vivo Susceptibility of Mycobacterium ulcerans to which are useful for the treatment of bacterial infections. KRM-1648, A New Benzoxazinorifamycin, in Comparison with Rifampicin.” Arzneimiiffelforschung 51(6):501 (2001). 4 Claims, 7 Drawing Sheets US 8,097,607 B2 Page 2 OTHER PUBLICATIONS Tomioka et al., “Therapeutic Efficacy of KRM-1648 in Combination with Other Antimicrobials Against M. leprae Infection Induced in Sato et al., “Antimicrobial Activities of Benzoxazinorifamycin Nude Mice.” International Journal of Leprosy and Other Mycobacte KRM-1648, Clarithromycin and Levofloxacin Against Intracellular rial Diseases 61:77A (1993). Mycobacterium avium Complex Phagocytosed by Murine Peritoneal Tomioka et al., “Intramacrophage Passage of Mycobacterium Macrophages,” Journal of Antimicrobial Chemotherapy 41(1):77 tuverculosis and M. avium Complex Alters the drug susceptibilities of te organisms as determined by intracellular SuSeptivility Testing (1998). using Macrophages and Type II Alveolar Epithelial Cells.” Antimi Shimizu et al., “Effects of the Chinese Traditional Medicine Mao crobial Agents and Chemotherapy 46:519 (2002). bushi-saishin-to on Therapeutic Efficacy of a New Wallis et al., “Inhibition of Isoniazid-induced Expression of Benzoxazinorifamycin, KRM-1648, Against Mycobacterium avium Mycobacterium tuberculosis Antigen 85 in Sputum: Potential Surro Infection in Mice.” Antimicrobial Agents and Chemo gate Marker in Tuberculosis Chemotherapy Trials.” Antimicrobial therapy:43(3):514 (1999). Agents and Chemotherapy 45(4): 1302 (2001). Shoen et al., “Evaluation of Rifalazil in Long-term Treatment Regi Yamamoto et al., “In Vitro Bactericidal and in Vivo Therapeutic mens for Tuberculosis in Mice.” Antimicrobial Agents and Chemo Activities of a New Rifamycin Derivative, KRM-1648, Against therapy 44(6): 1458 (2000). Mycobacterium tuberculosis,” Antimicrobial Agents and Chemo Tomioka et al., “Effects of Benzoxazinorifamycin KRM-1648 on therapy 40(2):426 (1996). Cytokine Production at Sites of Mycobacterium avium Complex Yamamoto et al., “Activity of KRM-1648 Alone or in Combination Infection Induced in Mice.” Antimicrobial Agents and Chemotherapy with Both Ethambutol and Kanamycin or Clanthromycin Against 41(2):357 (1997). Mycobacterium intracellulare Infections in Beige Mice.” Antimicro Tomioka et al., “In Vivo Antileprosy Activity of the Newly Synthe bial Agents and Chemotherapy 40(2):429 (1996). sized Benzoxazinorifamycin, KRM-1648.” International Journal of Leprosy 61:255-258 (1993). * cited by examiner U.S. Patent Jan. 17, 2012 Sheet 1 of 7 US 8,097,607 B2 O Observed Values Predicted Values FIG. A O 24 48 72 96 120 144 168 192 216 240 264. 288 312 336 Time (hr) 1 O t = 139 hours FIG. B O 24 48 72 96 120 144 168 192 216 240 264. 288 312 336 Time (hr) U.S. Patent Jan. 17, 2012 Sheet 2 of 7 US 8,097,607 B2 FIG. 2 TWO.COMPARTMENT OPEN MODEL Ka Gract -0. Plasma Compartment Tissue Compartment Drug Elimination (Metabolism & Excretion) U.S. Patent Jan. 17, 2012 Sheet 3 of 7 US 8,097,607 B2 FIG. 3 1 O O - - Amount in Plasma (ng/g) --- Amount in Tissues (ng/g) 10 ' ' ' ' ' ' MIC for C. trachomatis (ng/mL) 0.1 0.01 O 48 96 144 192 240 288 336 384 432 480 Time (hr) U.S. Patent Jan. 17, 2012 Sheet 4 of 7 US 8,097,607 B2 FIG. 4 100 - Amount in Plasma (ng/g) --- Amount in Tissues (nglg) 10 MIC for C. trachomatis (ng/mL) - s r s s - - - * s s s - A. s • *w - a • * * r * - - - a a • - - - - - - - - - - - - - - - - - creas aas - - - - • * r s r * * r * a • - as - - - 0.1 O 48 96 144 192 240 288 336 384. 432 480 Time (hr) U.S. Patent Jan. 17, 2012 Sheet 5 Of 7 US 8,097,607 B2 FIG. 5 Amount in Plasma (ng/g) 0.6 -- Amount in Tissues (ng/g) 0.5 - / MIC for C. Trachomatis (ng/mL) 1G - Series 1 2 0.4 re- Series3 R 5 0.3 /N E E3 0.2 e 0.1 O.O -- --- O 48 96 144 192 240 288 336 384 432 480 Time (h) U.S. Patent Jan. 17, 2012 Sheet 6 of 7 US 8,097,607 B2 FIG. 6 100 - Amount in Plasma (ng/g) --- Amount in Tissues (ng/g) - - - - - - - - - - MIC for C. trachomatis (ng/mL) 10 - tw. a s s - w - - - t a s - - ". 0.1 0.01 O 48 96 144 192 240 288 336 384 432 480 Time (hr) U.S.
Load more

Recommended publications
  • (12) United States Patent (10) Patent No.: US 9,662.400 B2 Smith Et Al
    USOO9662400B2 (12) United States Patent (10) Patent No.: US 9,662.400 B2 Smith et al. (45) Date of Patent: *May 30, 2017 (54) METHODS FOR PRODUCING A (2013.01); C08B 37/003 (2013.01); C08L 5/08 BODEGRADABLE CHITOSAN (2013.01); A6 IK 38/00 (2013.01); A61 L COMPOSITION AND USES THEREOF 2300/404 (2013.01) (58) Field of Classification Search (71) Applicant: University of Memphis Research CPC ...... A61K 47/36; A61K 31/00; A61K 9/7007; Foundation, Memphis, TN (US) A61K 9/0024; A61 L 15/28: A61L 27/20; A61L 27/58: A61L 31/042; C08B 37/003 (72) Inventors: James Keaton Smith, Memphis, TN USPC ................................ 514/23, 40, 777; 536/20 (US); Ashley C. Parker, Memphis, TN See application file for complete search history. (US); Jessica A. Jennings, Memphis, (56) References Cited TN (US); Benjamin T. Reves, Memphis, TN (US); Warren O. U.S. PATENT DOCUMENTS Haggard, Bartlett, TN (US) 4,895,724. A * 1/1990 Cardinal .............. A61K9/0024 424,278.1 (73) Assignee: The University of Memphis Research 5,541,233 A 7/1996 Roenigk Foundation, Memphis, TN (US) 5,958,443 A 9/1999 Viegas et al. 6,699,287 B2 3/2004 Son et al. (*) Notice: Subject to any disclaimer, the term of this 6,989,157 B2 1/2006 Gillis et al. patent is extended or adjusted under 35 7,371.403 B2 5/2008 McCarthy et al. 2003, OO15825 A1 1/2003 Sugie et al. U.S.C. 154(b) by 0 days. 2003/0206958 A1 11/2003 Cattaneo et al.
    [Show full text]
  • Transdermal Drug Delivery Device Including An
    (19) TZZ_ZZ¥¥_T (11) EP 1 807 033 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61F 13/02 (2006.01) A61L 15/16 (2006.01) 20.07.2016 Bulletin 2016/29 (86) International application number: (21) Application number: 05815555.7 PCT/US2005/035806 (22) Date of filing: 07.10.2005 (87) International publication number: WO 2006/044206 (27.04.2006 Gazette 2006/17) (54) TRANSDERMAL DRUG DELIVERY DEVICE INCLUDING AN OCCLUSIVE BACKING VORRICHTUNG ZUR TRANSDERMALEN VERABREICHUNG VON ARZNEIMITTELN EINSCHLIESSLICH EINER VERSTOPFUNGSSICHERUNG DISPOSITIF D’ADMINISTRATION TRANSDERMIQUE DE MEDICAMENTS AVEC COUCHE SUPPORT OCCLUSIVE (84) Designated Contracting States: • MANTELLE, Juan AT BE BG CH CY CZ DE DK EE ES FI FR GB GR Miami, FL 33186 (US) HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI • NGUYEN, Viet SK TR Miami, FL 33176 (US) (30) Priority: 08.10.2004 US 616861 P (74) Representative: Awapatent AB P.O. Box 5117 (43) Date of publication of application: 200 71 Malmö (SE) 18.07.2007 Bulletin 2007/29 (56) References cited: (73) Proprietor: NOVEN PHARMACEUTICALS, INC. WO-A-02/36103 WO-A-97/23205 Miami, FL 33186 (US) WO-A-2005/046600 WO-A-2006/028863 US-A- 4 994 278 US-A- 4 994 278 (72) Inventors: US-A- 5 246 705 US-A- 5 474 783 • KANIOS, David US-A- 5 474 783 US-A1- 2001 051 180 Miami, FL 33196 (US) US-A1- 2002 128 345 US-A1- 2006 034 905 Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations.
    [Show full text]
  • Rifalazil | Medchemexpress
    Inhibitors Product Data Sheet Rifalazil • Agonists Cat. No.: HY-105099 CAS No.: 129791-92-0 Molecular Formula: C₅₁H₆₄N₄O₁₃ • Molecular Weight: 941.07 Screening Libraries Target: DNA/RNA Synthesis; Bacterial Pathway: Cell Cycle/DNA Damage; Anti-infection Storage: 4°C, sealed storage, away from moisture * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) SOLVENT & SOLUBILITY In Vitro DMSO : 8.33 mg/mL (8.85 mM; Need ultrasonic) Mass Solvent 1 mg 5 mg 10 mg Concentration Preparing 1 mM 1.0626 mL 5.3131 mL 10.6262 mL Stock Solutions 5 mM 0.2125 mL 1.0626 mL 2.1252 mL 10 mM --- --- --- Please refer to the solubility information to select the appropriate solvent. In Vivo 1. Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline Solubility: ≥ 2.2 mg/mL (2.34 mM); Clear solution 2. Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.2 mg/mL (2.34 mM); Clear solution BIOLOGICAL ACTIVITY Description Rifalazil (KRM-1648; ABI-1648), a rifamycin derivative, inhibits the bacterial DNA-dependent RNA polymerase and kills bacterial cells by blocking off the β-subunit in RNA polymerase[1]. Rifalazil (KRM-1648; ABI-1648) is an antibiotic, exhibits high potency against mycobacteria, gram-positive bacteria, Helicobacter pylori, C. pneumoniae and C. trachomatis with MIC values from 0.00025 to 0.0025 μg/ml[3]. Rifalazil (KRM-1648; ABI-1648) has the potential for the treatment of Chlamydia infection, Clostridium difficile associated diarrhea (CDAD), and tuberculosis (TB)[2].
    [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]
  • EMA/CVMP/158366/2019 Committee for Medicinal Products for Veterinary Use
    Ref. Ares(2019)6843167 - 05/11/2019 31 October 2019 EMA/CVMP/158366/2019 Committee for Medicinal Products for Veterinary Use Advice on implementing measures under Article 37(4) of Regulation (EU) 2019/6 on veterinary medicinal products – Criteria for the designation of antimicrobials to be reserved for treatment of certain infections in humans Official address Domenico Scarlattilaan 6 ● 1083 HS Amsterdam ● The Netherlands Address for visits and deliveries Refer to www.ema.europa.eu/how-to-find-us Send us a question Go to www.ema.europa.eu/contact Telephone +31 (0)88 781 6000 An agency of the European Union © European Medicines Agency, 2019. Reproduction is authorised provided the source is acknowledged. Introduction On 6 February 2019, the European Commission sent a request to the European Medicines Agency (EMA) for a report on the criteria for the designation of antimicrobials to be reserved for the treatment of certain infections in humans in order to preserve the efficacy of those antimicrobials. The Agency was requested to provide a report by 31 October 2019 containing recommendations to the Commission as to which criteria should be used to determine those antimicrobials to be reserved for treatment of certain infections in humans (this is also referred to as ‘criteria for designating antimicrobials for human use’, ‘restricting antimicrobials to human use’, or ‘reserved for human use only’). The Committee for Medicinal Products for Veterinary Use (CVMP) formed an expert group to prepare the scientific report. The group was composed of seven experts selected from the European network of experts, on the basis of recommendations from the national competent authorities, one expert nominated from European Food Safety Authority (EFSA), one expert nominated by European Centre for Disease Prevention and Control (ECDC), one expert with expertise on human infectious diseases, and two Agency staff members with expertise on development of antimicrobial resistance .
    [Show full text]
  • Ehealth DSI [Ehdsi V2.2.2-OR] Ehealth DSI – Master Value Set
    MTC eHealth DSI [eHDSI v2.2.2-OR] eHealth DSI – Master Value Set Catalogue Responsible : eHDSI Solution Provider PublishDate : Wed Nov 08 16:16:10 CET 2017 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 1 of 490 MTC Table of Contents epSOSActiveIngredient 4 epSOSAdministrativeGender 148 epSOSAdverseEventType 149 epSOSAllergenNoDrugs 150 epSOSBloodGroup 155 epSOSBloodPressure 156 epSOSCodeNoMedication 157 epSOSCodeProb 158 epSOSConfidentiality 159 epSOSCountry 160 epSOSDisplayLabel 167 epSOSDocumentCode 170 epSOSDoseForm 171 epSOSHealthcareProfessionalRoles 184 epSOSIllnessesandDisorders 186 epSOSLanguage 448 epSOSMedicalDevices 458 epSOSNullFavor 461 epSOSPackage 462 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 2 of 490 MTC epSOSPersonalRelationship 464 epSOSPregnancyInformation 466 epSOSProcedures 467 epSOSReactionAllergy 470 epSOSResolutionOutcome 472 epSOSRoleClass 473 epSOSRouteofAdministration 474 epSOSSections 477 epSOSSeverity 478 epSOSSocialHistory 479 epSOSStatusCode 480 epSOSSubstitutionCode 481 epSOSTelecomAddress 482 epSOSTimingEvent 483 epSOSUnits 484 epSOSUnknownInformation 487 epSOSVaccine 488 © eHealth DSI eHDSI Solution Provider v2.2.2-OR Wed Nov 08 16:16:10 CET 2017 Page 3 of 490 MTC epSOSActiveIngredient epSOSActiveIngredient Value Set ID 1.3.6.1.4.1.12559.11.10.1.3.1.42.24 TRANSLATIONS Code System ID Code System Version Concept Code Description (FSN) 2.16.840.1.113883.6.73 2017-01 A ALIMENTARY TRACT AND METABOLISM 2.16.840.1.113883.6.73 2017-01
    [Show full text]
  • NOTES in Vitro Activities of Norfloxacin and Ciprofloxacin Against
    ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, July 1984, p. 94-96 Vol. 26, No. 1 0066-4804/84/070094-03$02.00/0 Copyright C 1984, American Society for Microbiology NOTES In Vitro Activities of Norfloxacin and Ciprofloxacin Against Mycobacterium tuberculosis, M. avium Complex, M. chelonei, M. fortuitum, and M. kansasii J. DOUGLAS GAY, DONALD R. DEYOUNG, AND GLENN D. ROBERTS* Section of Clinical Microbiology, Department of Laboratory Medicine, Mayo Clinic and Mayo Foundation, Rochester, Minnesota 55905 Received 28 November 1983/Accepted 4 April 1984 The activities of ciprofloxacin and norfloxacin against 100 mycobacteria isolates were studied in vitro by the 1% standard proportion method. Ciprofloxacin was more active against M. tuberculosis and M. fortuitum with MICs of 1.0 and 0.25 ,ug/ml, respectively, against 90% of isolates; norfloxacin had MICs of 8.0 and 2.0 ,ug/ml, respectively, against 90% of isolates. Nalidixic acid and other heterocyclic carbonic acid deriva- studied. The organisms were taken from the Mayo Clinic tives have been used primarily in the treatment of urinary stock culture collection, which included recent clinical iso- tract infections for many years. The compounds of this lates. Stock cultures were maintained on Middlebrook 7H10 general group include nalidixic acid, oxolinic acid, pipemidic agar slants (Difco Laboratories, Detroit, Mich.) and were acid, cinoxacin, and rosoxacin. Two new substances in this subcultured monthly. The identification of isolates was series which have been recently synthesized are norfloxacin based on standard biochemical tests (17) and gas-liquid (6) (1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-[ 1-piperazinyl ]-3- chromatography (16).
    [Show full text]
  • WHO Report on Surveillance of Antibiotic Consumption: 2016-2018 Early Implementation ISBN 978-92-4-151488-0 © World Health Organization 2018 Some Rights Reserved
    WHO Report on Surveillance of Antibiotic Consumption 2016-2018 Early implementation WHO Report on Surveillance of Antibiotic Consumption 2016 - 2018 Early implementation WHO report on surveillance of antibiotic consumption: 2016-2018 early implementation ISBN 978-92-4-151488-0 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution- NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons. org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non- commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. WHO report on surveillance of antibiotic consumption: 2016-2018 early implementation. Geneva: World Health Organization; 2018. Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [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 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]
  • Pharmaceuticals As Environmental Contaminants
    PharmaceuticalsPharmaceuticals asas EnvironmentalEnvironmental Contaminants:Contaminants: anan OverviewOverview ofof thethe ScienceScience Christian G. Daughton, Ph.D. Chief, Environmental Chemistry Branch Environmental Sciences Division National Exposure Research Laboratory Office of Research and Development Environmental Protection Agency Las Vegas, Nevada 89119 [email protected] Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada Why and how do drugs contaminate the environment? What might it all mean? How do we prevent it? Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada This talk presents only a cursory overview of some of the many science issues surrounding the topic of pharmaceuticals as environmental contaminants Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada A Clarification We sometimes loosely (but incorrectly) refer to drugs, medicines, medications, or pharmaceuticals as being the substances that contaminant the environment. The actual environmental contaminants, however, are the active pharmaceutical ingredients – APIs. These terms are all often used interchangeably Office of Research and Development National Exposure Research Laboratory, Environmental Sciences Division, Las Vegas, Nevada Office of Research and Development Available: http://www.epa.gov/nerlesd1/chemistry/pharma/image/drawing.pdfNational
    [Show full text]
  • Surveillance of Antimicrobial Consumption in Europe 2013-2014 SURVEILLANCE REPORT
    SURVEILLANCE REPORT SURVEILLANCE REPORT Surveillance of antimicrobial consumption in Europe in Europe consumption of antimicrobial Surveillance Surveillance of antimicrobial consumption in Europe 2013-2014 2012 www.ecdc.europa.eu ECDC SURVEILLANCE REPORT Surveillance of antimicrobial consumption in Europe 2013–2014 This report of the European Centre for Disease Prevention and Control (ECDC) was coordinated by Klaus Weist. Contributing authors Klaus Weist, Arno Muller, Ana Hoxha, Vera Vlahović-Palčevski, Christelle Elias, Dominique Monnet and Ole Heuer. Data analysis: Klaus Weist, Arno Muller and Ana Hoxha. Acknowledgements The authors would like to thank the ESAC-Net Disease Network Coordination Committee members (Marcel Bruch, Philippe Cavalié, Herman Goossens, Jenny Hellman, Susan Hopkins, Stephanie Natsch, Anna Olczak-Pienkowska, Ajay Oza, Arjana Tambić Andrasevic, Peter Zarb) and observers (Jane Robertson, Arno Muller, Mike Sharland, Theo Verheij) for providing valuable comments and scientific advice during the production of the report. All ESAC-Net participants and National Coordinators are acknowledged for providing data and valuable comments on this report. The authors also acknowledge Gaetan Guyodo, Catalin Albu and Anna Renau-Rosell for managing the data and providing technical support to the participating countries. Suggested citation: European Centre for Disease Prevention and Control. Surveillance of antimicrobial consumption in Europe, 2013‒2014. Stockholm: ECDC; 2018. Stockholm, May 2018 ISBN 978-92-9498-187-5 ISSN 2315-0955
    [Show full text]