{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,16]],"date-time":"2025-10-16T09:52:48Z","timestamp":1760608368954,"version":"3.28.0"},"reference-count":24,"publisher":"Oxford University Press (OUP)","issue":"11","license":[{"start":{"date-parts":[[2006,11,1]],"date-time":"2006-11-01T00:00:00Z","timestamp":1162339200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/academic.oup.com\/journals\/pages\/open_access\/funder_policies\/chorus\/standard_publication_model"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2006,11,1]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:p>The biopharmaceutical properties of an in-house developed new crystal modification of torasemide (Torasemide N) were investigated in comparison with the most well known crystal modification form of torasemide (Torasemide I) in order to classify the drug according to the Biopharmaceutics Classification System (BCS), and to evaluate the data in line with current US Food and Drug Administration (FDA) guidance (with biowaiver provision for Class I drugs) to determine if the biowaiver provision could be improved. The solubility profiles of Torasemide I and Torasemide N were determined, and tablets prepared from both forms of the drug were studied for in-vitro release characteristics in media recommended by the current FDA guidance for biowaiver of generic products, and in other media considered more appropriate for the purpose than the ones recommended by the FDA. Two separate bioequivalence studies in healthy humans (following oral administration) were performed with two test products (both prepared from Torasemide I) against a single reference product (prepared from Torasemide N). The absorption profiles of the drug from the tablets were determined by deconvolution for comparison with the in-vitro release profiles to determine the appropriateness of some dissolution media for predicting in-vivo performance and to determine the comparative rate and extent of absorption. The drug was absorbed from the tested products quickly and almost completely (about 95% within 3.5 h of administration). However, one test product failed to meet the bioequivalence criteria and had a significant initial lower absorption rate profile compared with the reference product (P \u2264 0.05), whereas the other product was bioequivalent and had a similar absorption profile to the reference product. A dissolution medium at pH 5.0, in which torasemide has minimum solubility, was found to be more discriminatory than the media recommended by the FDA. Torasemide has been classified as a Class I drug according to the BCS up to a maximum dose of 40 mg and the data suggest that the current FDA guidance could be improved by giving more emphasis to selection of appropriate dissolution media than is given in its current form for approving biowaiver to generic products of Class I drugs.<\/jats:p>","DOI":"10.1211\/jpp.58.11.0008","type":"journal-article","created":{"date-parts":[[2006,11,14]],"date-time":"2006-11-14T00:24:43Z","timestamp":1163463883000},"page":"1475-1482","source":"Crossref","is-referenced-by-count":8,"title":["Classification of torasemide based on the Biopharmaceutics Classification System and evaluation of the FDA biowaiver provision for generic products of Class I drugs"],"prefix":"10.1093","volume":"58","author":[{"given":"M Zahirul I","family":"Khan","sequence":"first","affiliation":[{"name":"PLIVA Research and Development Ltd , Prilaz baruna Filipovi\u0107a 29, 10 000 Zagreb,","place":["Croatia"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Dragica","family":"Rau\u0161l","sequence":"additional","affiliation":[{"name":"PLIVA Research and Development Ltd , Prilaz baruna Filipovi\u0107a 29, 10 000 Zagreb,","place":["Croatia"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Senka","family":"Rado\u0161evi\u0107","sequence":"additional","affiliation":[{"name":"PLIVA Research and Development Ltd , Prilaz baruna Filipovi\u0107a 29, 10 000 Zagreb,","place":["Croatia"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Darko","family":"Fili\u0107","sequence":"additional","affiliation":[{"name":"PLIVA Research Institute Ltd , Prilaz baruna Filipovi\u0107a 29, 10 000 Zagreb,","place":["Croatia"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Aleksandar","family":"Danilovski","sequence":"additional","affiliation":[{"name":"PLIVA Research and Development Ltd , Prilaz baruna Filipovi\u0107a 29, 10 000 Zagreb,","place":["Croatia"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Miljenko","family":"Dumi\u0107","sequence":"additional","affiliation":[{"name":"PLIVA Research and Development Ltd , Prilaz baruna Filipovi\u0107a 29, 10 000 Zagreb,","place":["Croatia"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zdravka","family":"Kne\u017eevi\u0107","sequence":"additional","affiliation":[{"name":"PLIVA Research and Development Ltd , Prilaz baruna Filipovi\u0107a 29, 10 000 Zagreb,","place":["Croatia"]}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"286","published-online":{"date-parts":[[2006,11,1]]},"reference":[{"key":"2024103109343097400_cit1","first-page":"15","article-title":"Comparison of bioavailability, pharmacokinetics and pharmacodynamics of torasemide in young and elderly healthy volunteers","volume":"8","author":"Barr","year":"1990","journal-title":"Prog. Pharmacol. Clin. Pharmacol."},{"key":"2024103109343097400_cit2","first-page":"29","article-title":"Torasemide dose-proportionality of pharmacokinetics and pharmacodynamics","volume":"8","author":"Barr","year":"1990","journal-title":"Prog. Pharmacol. Clin. Pharmacol."},{"key":"2024103109343097400_cit3","first-page":"227","article-title":"Methods for the characterization of polymorphs and solvates","volume-title":"Polymorphism in pharmaceutical solids.","author":"Brittain","year":"1999"},{"volume-title":"Guidance for industry: immediate-release solid oral dosage forms. Scale-up and post-approval changes: chemistry, manufacturing and controls, in vitro dissolution testing and in vivo bioequivalence documentation","year":"1995","author":"CDER","key":"2024103109343097400_cit4"},{"volume-title":"Guidance for industry: waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a biopharmaceutics classification system","year":"2000","author":"CDER","key":"2024103109343097400_cit5"},{"volume-title":"Draft guidance for industry: ANDAs: pharmaceutical solid polymorphism; chemistry, manufacturing and control information","year":"2004","author":"CDER","key":"2024103109343097400_cit6"},{"key":"2024103109343097400_cit7","first-page":"103","article-title":"Chemistry of torasemide: molecular and crystal structure of new polymorph N","volume":"74","author":"Danilovski","year":"2001","journal-title":"Croatica Chemica Acta."},{"key":"2024103109343097400_cit8","doi-asserted-by":"crossref","first-page":"1304","DOI":"10.1107\/S0567740878005403","article-title":"Structure cristalline et moleculaire d'un diuretique derive de l'alkyl-1[(ph\u00e9nylamino-4-pyridyl-3)sulfonyl]-3 ur\u00e9e: la Toras\u00e9mide (C15H20N4SO3)","volume":"B34","author":"Dupont","year":"1978","journal-title":"Acta Crystallogr."},{"key":"2024103109343097400_cit9","doi-asserted-by":"crossref","first-page":"2659","DOI":"10.1107\/S0567740878008900","article-title":"Structure d'une seconde variete de la Toras\u00e9mide","volume":"B34","author":"Dupont","year":"1978","journal-title":"Acta Crystallogr."},{"key":"2024103109343097400_cit10","doi-asserted-by":"crossref","first-page":"1035","DOI":"10.1136\/gut.29.8.1035","article-title":"Measurement of gastrointestinal pH profiles in normal ambulant human subjects","volume":"29","author":"Evans","year":"1988","journal-title":"Gut"},{"volume-title":"Crystal modification of torasemide","year":"2002","author":"Fili\u0107","key":"2024103109343097400_cit11"},{"volume-title":"Process for the preparation of modification I of N-(1-methylethylaminocarbonyl)-4-(3-methylphenylamino)-3-pyridinesulfonamide","year":"2004","author":"Fili\u0107","key":"2024103109343097400_cit12"},{"key":"2024103109343097400_cit13","doi-asserted-by":"crossref","first-page":"698","DOI":"10.1023\/A:1011910801212","article-title":"Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs","volume":"15","author":"Galia","year":"1998","journal-title":"Pharm. Res."},{"key":"2024103109343097400_cit14","doi-asserted-by":"crossref","first-page":"1537","DOI":"10.1007\/s11095-005-6247-7","article-title":"Impact of excess solids on apparent solubility","volume":"22","author":"Kawakami","year":"2005","journal-title":"Pharm. Res."},{"key":"2024103109343097400_cit15","doi-asserted-by":"crossref","first-page":"1","DOI":"10.2165\/00003088-199834010-00001","article-title":"Clinical pharmacokinetics and pharmacodynamics of torasemide","volume":"34","author":"Knauf","year":"1998","journal-title":"Clin. Pharmacokinet."},{"key":"2024103109343097400_cit16","first-page":"107","article-title":"Torasemide pharmacokinetics and pharmacodynamics in patients with renal insufficiency","volume-title":"Diuretics IV: chemistry, pharmacology and clinical applications.","author":"Kramer","year":"1993"},{"key":"2024103109343097400_cit17","first-page":"382","article-title":"Pharmacokinetic study of torasemide in humans: an overview of its diuretic effect","volume":"20","author":"Lesne","year":"1982","journal-title":"Int. J. Clin. Pharmacol. Ther. Toxicol."},{"key":"2024103109343097400_cit18","first-page":"160","article-title":"Comparison of the pharmacokinetics and pharmacodynamics of torasemide and furosemide in healthy volunteers","volume":"38","author":"Lesne","year":"1988","journal-title":"Arzneim. Forsch. Drug Res."},{"key":"2024103109343097400_cit19","first-page":"164","article-title":"Pharmacokinetics and metabolism of torasemide in man","volume":"38","author":"Neugebauer","year":"1988","journal-title":"Arzneim. Forsch. Drug Res."},{"key":"2024103109343097400_cit20","doi-asserted-by":"crossref","first-page":"406","DOI":"10.1023\/A:1022652004114","article-title":"The mean dissolution time depends on the dose\/solubility ratio","volume":"20","author":"Rinaki","year":"2003","journal-title":"Pharm. Res."},{"key":"2024103109343097400_cit21","doi-asserted-by":"crossref","first-page":"1917","DOI":"10.1023\/B:PHAM.0000008037.57884.11","article-title":"Quantitative biopharmaceutics classification system: the central role of dose\/solubility ratio","volume":"20","author":"Rinaki","year":"2003","journal-title":"Pharm. Res."},{"key":"2024103109343097400_cit22","doi-asserted-by":"crossref","first-page":"1567","DOI":"10.1023\/B:PHAM.0000041450.25106.c8","article-title":"Identification of biowaivers among Class II drugs: theoretical justifications and practical examples","volume":"21","author":"Rinaki","year":"2004","journal-title":"Pharm. Res."},{"key":"2024103109343097400_cit23","doi-asserted-by":"crossref","first-page":"293","DOI":"10.1023\/B:PHAM.0000016242.48642.71","article-title":"The \u201chigh solubility\u201d definition of the current FDA guidance on bio-pharmaceutical classification system may be too strict for acidic drugs","volume":"21","author":"Yazdanian","year":"2004","journal-title":"Pharm. Res."},{"key":"2024103109343097400_cit24","doi-asserted-by":"crossref","first-page":"921","DOI":"10.1023\/A:1016473601633","article-title":"Biopharmaceutics classification system: the scientific basis for biowaiver extensions","volume":"19","author":"Yu","year":"2002","journal-title":"Pharm. Res."}],"container-title":["Journal of Pharmacy and Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.wiley.com\/onlinelibrary\/tdm\/v1\/articles\/10.1211%2Fjpp.58.11.0008","content-type":"unspecified","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/academic.oup.com\/jpp\/article-pdf\/58\/11\/1475\/60254925\/jpp.58.11.0008.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"syndication"},{"URL":"https:\/\/academic.oup.com\/jpp\/article-pdf\/58\/11\/1475\/60254925\/jpp.58.11.0008.pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2024,10,31]],"date-time":"2024-10-31T09:36:36Z","timestamp":1730367396000},"score":1,"resource":{"primary":{"URL":"https:\/\/academic.oup.com\/jpp\/article\/58\/11\/1475\/6147874"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2006,11,1]]},"references-count":24,"journal-issue":{"issue":"11","published-online":{"date-parts":[[2006,11,1]]},"published-print":{"date-parts":[[2006,11,1]]}},"URL":"https:\/\/doi.org\/10.1211\/jpp.58.11.0008","relation":{},"ISSN":["0022-3573","2042-7158"],"issn-type":[{"type":"print","value":"0022-3573"},{"type":"electronic","value":"2042-7158"}],"subject":[],"published-other":{"date-parts":[[2006,11]]},"published":{"date-parts":[[2006,11,1]]}}}