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Compositions and Formulations Based on Swellable Matrices for Sustained Release of Poorly Soluble Drugs Such As Clarithromycin
(19) & (11) EP 2 283 824 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 16.02.2011 Bulletin 2011/07 A61K 9/20 (2006.01) A61K 31/00 (2006.01) (21) Application number: 09166824.4 (22) Date of filing: 30.07.2009 (84) Designated Contracting States: (72) Inventors: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR • Camponeschi, Claudio HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL 00040, Pomezia (IT) PT RO SE SI SK SM TR • Colombo, Paolo Designated Extension States: 43100, Parma (IT) AL BA RS (74) Representative: Palladino, Saverio Massimo et al (71) Applicants: Notarbartolo & Gervasi S.p.A. • Special Products Line S.p.A. Corso di Porta Vittoria, 9 00040 Pomezia (IT) 20122 Milano (IT) • So. Se. Pharm S.r.l. 00040 Pomezia (IT) (54) Compositions and formulations based on swellable matrices for sustained release of poorly soluble drugs such as clarithromycin (57) The present invention concerns the discovery uct, capable to provide a quasi-constant prolonged re- of a new formulation for oral drug sustained release prod- lease of poorly soluble drugs whose solubility depends on the pH. EP 2 283 824 A1 Printed by Jouve, 75001 PARIS (FR) EP 2 283 824 A1 Description FIELD OF THE INVENTION 5 [0001] The present invention concerns the discovery of new compositions and formulations for oral drug modified release products, capable to provide a sustained release of poorly soluble drugs whose solubility depends on the pH. BACKGROUND OF THE INVENTION 10 [0002] New drug dosage forms facilitating the human therapeutic practice are needed for making efficient the treatment of several diseases. -
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. -
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 . -
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). -
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. -
(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. -
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 -
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 -
European Surveillance of Healthcare-Associated Infections in Intensive Care Units
TECHNICAL DOCUMENT European surveillance of healthcare-associated infections in intensive care units HAI-Net ICU protocol Protocol version 1.02 www.ecdc.europa.eu ECDC TECHNICAL DOCUMENT European surveillance of healthcare- associated infections in intensive care units HAI-Net ICU protocol, version 1.02 This technical document of the European Centre for Disease Prevention and Control (ECDC) was coordinated by Carl Suetens. In accordance with the Staff Regulations for Officials and Conditions of Employment of Other Servants of the European Union and the ECDC Independence Policy, ECDC staff members shall not, in the performance of their duties, deal with a matter in which, directly or indirectly, they have any personal interest such as to impair their independence. This is version 1.02 of the HAI-Net ICU protocol. Differences between versions 1.01 (December 2010) and 1.02 are purely editorial. Suggested citation: European Centre for Disease Prevention and Control. European surveillance of healthcare- associated infections in intensive care units – HAI-Net ICU protocol, version 1.02. Stockholm: ECDC; 2015. Stockholm, March 2015 ISBN 978-92-9193-627-4 doi 10.2900/371526 Catalogue number TQ-04-15-186-EN-N © European Centre for Disease Prevention and Control, 2015 Reproduction is authorised, provided the source is acknowledged. TECHNICAL DOCUMENT HAI-Net ICU protocol, version 1.02 Table of contents Abbreviations ............................................................................................................................................... -
Standing Order for Tularemia Prophylaxis
OREGON HEALTH AUTHORITY PUBLIC HEALTH DIVISION ACUTE AND COMMUNICABLE DISEASE PREVENTION SECTION Tularemia Prophylaxis I. OREGON MODEL PROTOCOL 1. Follow the nursing assessment of individuals presenting for prophylactic treatment to a known or potentially harmful biological agent. 2. Provide patient information about tularemia and the preventive antibiotics prior to administration, answering any questions 3. Dispense antibiotic prophylaxis in accordance with prophylactic treatment guidelines (Table 1) and within the restrictions of the guidelines of the Strategic National Stockpile program. ________________________________________________________ Signature, Health Officer Date II. Persons for whom prophylaxis may be dispensed The World Health Organization recommends post-exposure prophylaxis in the following settings: 1. Exposure of laboratory personnel to Francisella tularensis in the absence of proper infection control measures; 2. Exposure to an aerosolized release of Francisella tularensis. Tularemia Page 2 of 15 Table 1 Recommendations for Treatment of Patients with Tularemia in a Mass Casualty Setting and for Post-exposure Prophylaxis a Preferred Choices Adults Doxycycline, 100 mg orally twice daily b Ciprofloxacin, 500 mg orally twice daily Preferred Choices Doxycycline; if ≥45 kg, give 100 mg orally twice daily; Children Doxycycline, if <45 kg, give 2.2 mg/kg orally twice daily; Ciprofloxacin, 10–15 mg/kg orally twice daily c Preferred Choices Pregnant women Ciprofloxacin, 500 mg orally twice daily b Doxycycline, 100 mg orally twice daily a One antibiotic, appropriate for patient age, should be chosen from among alternatives. The duration of all recommended therapies in Table 1 is 14 days. b Not a US Food and Drug Administration–approved use. c Ciprofloxacin dosage should not exceed 1g/d in children. -
Isolation and Characterization of Norfloxacin-Resistant Mutants Of
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, Aug. 1986, p. 248-253 Vol. 30, No. 2 0066-4804/86/080248-06$02.00/0 Copyright © 1986, American Society for Microbiology Isolation and Characterization of Norfloxacin-Resistant Mutants of Escherichia coli K-12 KEIJI HIRAI,'* HIROSHI AOYAMA,1 SEIGO SUZUE,1 TSUTOMU IRIKURA,1 SHIZUKO IYOBE,2 AND SUSUMU MITSUHASHI3 Central Research Laboratories, Kyorin Pharmaceutical Co. Ltd., Nogi-machi, Shimotsuga-gun, Tochigi,l Department of Microbiology, School ofMedicine, Gunma University, Maebashi, Gunma,2 and Episome Institute, Fujimi, Gunma,3 Japan Received 30 December 1985/Accepted 19 May 1986 We isolated spontaneous mutants from Escherichia coli K-12 with low-level resistance to norfloxacin. These mutants were classified into the following three types on the basis of their properties: (i) NorA appeared to result for mutation in the gyrA locus for the A subunit of DNA gyrase; (ii) NorB showed low-level resistance to quinolones and other antimicrobial agents (e.g., cefoxitin, chloramphenicol, and tetracycline), and the norB gene was considered to map at about 34 min on the E. coli K-12 chromosome; (iii) NorC was less susceptible to norfloxacin and ciprofloxacin but was hypersusceptible to hydrophobic quinolones such as nalidixic acid and rosoxacin, hydrophobic antibiotics, dyes, and detergents. Susceptibility to bacteriophages and the hydropho- bicity of the NorC cell surface also differed from that of the parent strain. The norC gene was located near the lac locus at 8 min on the E. coli K-12 chromosome. Both NorB and NorC mutants had a lower rate of norfloxacin uptake, and it was found that the NorB mutant was altered in OmpF porin and that the NorC mutant was altered in both OmpF porin and apparently in the lipopolysaccharide structure of the outer membrane. -
Development of Novel Antibiotic Classes
60 years ago… The changes in antibiotic research as shown by patent publications Development of Novel Antibiotic Classes 1930 1940 1950 1960 1970 1980 1990 2000 2003 Daptomycin 1999 Linezolid 1962 Quinolones 1962 Streptogramins 1958 Glycopeptides 1952 Macrolides 1950 Aminoglycosides 1949 Chloramphenicol 1949 Tetracyclines 1940 Beta-Lactams 1936 Sulfonamides Harald Labischinski Products in the Pipeline Product Class Main Segment Status ABT 492 Quinolone Community Ph II DK507k Quinolone Community Ph I Daptomycin Lipopeptide Hospital Reg. Oritavancin Glycopeptide Hospital Ph III Dalbavancin Glycopeptide Hospital Ph III Tigecycline Glycylcycline Hospital Ph III AR 100 Trimethoprime Hospital Ph II BAL 9141 Cephalosporin Hospital Ph II BB-83698 PDF-inhibitor Community Ph I CS-023 Carbapenem Hospital Ph II Until 2008 very few antibiotics will reach the market ! Harald Labischinski 60 years ago… 1942 Gardner and Chain discover a substance with antibacterial activity, produced by a strain of Proactinomyces (later Streptomyces gardneri), which they name proactinomycin A. Macrolide structure • Macrolides are lipophilic molecules with a characteristic central lactone ring bearing 12 to 17 atoms, few if any double bonds and no nitrogen athoms (until the advent of the azalides). • Several amino and/or neutral sugars can bind to the lactone ring. MACROLIDE ANTIBIOTICS 12-membered-ring 14-membered-ring 15-membered-ring 16-membered-ring 17-membered-ring Methymycin Natural Semi-synthetic Azithromycin Natural Semi-synthetic Lankacidin Neomethymycin compounds derivatives compounds derivatives complex YC-17 Litorin Erythromycin A to F Roxithromycin Josamycin Rokitamycin Oleandomycin Dirithromycin Kitasamycin Miokamycin Sporeamicin Flurithromycin Spiramycin Clarithromycin Midecamycin • The macrolides narrow the entrance of the tunnel through which the nascent polypeptide chain is extruded from the ribosome.