Pdc to carboxylic acid
Discovery and development of first in class antifungal caspofungin (CANCIDAS(R))-a case study. US4100274A (May 11, 1976), Imperial Chemical Industries Ltd., 1976.īalkovec JM, Hughes DL, Masurekar PS, Sable CA, Schwartz RE, Singh SB. Generation of T cell responses targeting the reactive metabolite of halothane in mice. Antibodies raised against trifluoroacetyl-protein adducts bind to N-trifluoroacetyl-phosphatidylethanolamine in hexagonal phase phospholipid micelles. Effects of peptide fraction and counter ion on the development of clinical signs in experimental autoimmune encephalomyelitis. 2020 13(12):442.īoullerne AI, Polak PE, Braun D, Sharp A, Pelligrino D, Feinstein DL. The role of counter-ions in peptides-an overview. Sikora K, Jaskiewicz M, Neubauer D, Migon D, Kamysz W. The bioavailability of erythromycin stearate versus enteric-coated erythromycin base when taken immediately before and after food.
Xilobam: effect of salt form on pharmaceutical properties. Walkling WD, Reynolds BE, Fegely BJ, Janicki CA. Milestone 1: discovery and purification of heparin. Two new factors in blood coagulation-heparin and pro-antithrombin. Recent developments in pharmaceutical salts: FDA approvals from 2015 to 2019. A controlled double blind comparative study of single dose administration of imipramine pamoate and divided dose of imipramine hydrochloride in depressive illness. An integrated approach to the selection of optimal salt form for a new drug candidate. Morris KR, Fakes MG, Thakur AB, Newman AW, Singh AK, Venit JJ, et al. Salt formation to improve drug solubility. Pharmaceutical salts: a summary on doses of salt formers from the Orange book. Trends in active pharmaceutical ingredient salt selection based on analysis of the Orange book database. The technical advantage of carboxylate salts over free-base or other counterions is also discussed. The decade-wise analysis indicates that 1991–2000 contributed a maximum number of carboxylate salts (24) and least (3) in 1939–1950. This review provides an account of FDA-approved carboxylate salts from 1939 to 2020. Overall, the analysis shows that fifteen carboxylic acid counterions are present in FDA-approved pharmaceutical salts with a major share of acetate (18 drugs). Hydrocodone tartrate is the first FDA-approved carboxylate salt approved in 1943. A total of 94 pharmaceutical salts discovered during 1943–2020 comprises carboxylic acids as counterions with a major contribution of acetate, maleate, tartrate, fumarate, and succinate. Among various cationic and anionic counterions used in FDA-approved pharmaceutical salts, the carboxylic acids have significantly contributed. The FDA’s eighty-year trajectory of new drug approvals depicts around one-third of the drugs clinically used as their pharmaceutical salts. Salification is one of the powerful and widely employed approaches to improve the biopharmaceutical properties of drugs.