Product Information Report: Amoxicillin

It belongs to a class of medications called penicillin-like (beta-lactam) antibiotics and is used to treat certain infections caused by gram-positive bacteria, such as pneumonia, bronchitis, and gonorrhea, as well as some gram-negative bacteria. The chemical structure of amoxicillin is characterized by its formula, IUPAC name, and physicochemical properties, including moisture sorption and solubility data. Various spectroscopic techniques, such as FTIR, NMR, Mass, and UV Visible, have been used to characterize amoxicillin. The 6-amino penicillanic acid is a key material for the synthesis of amoxicillin, and different synthetic and enzymatic routes and their mechanisms are discussed in the report. Amoxicillin has been reported to exist as amoxicillin base, sodium salt, and trihydrate, with amoxicillin trihydrate being the most stable form. The report highlights the stability of amoxicillin in aqueous and solid states, including the mechanism of degradation and the degradation products formed. Amoxicillin is included in the penicillin group of compounds, which are well-documented as sensitizing agents, causing anaphylaxis-type allergic responses in susceptible patients. Dedicated manufacturing equipment and manufacturing sites are recommended for amoxicillin production. The report provides qualitative formulae for amoxicillin dispersible tablet formulations, including DisperMox and Flemoxin Solutab, along with proposed functions of the excipients and US Food and Drug Administration (FDA) inactive ingredient database (IID) limits for the individual excipients. The manufacturing process for amoxicillin trihydrate dispersible tablets involves the dry granulation process, and requirements for manufacturing equipment and the proposed manufacturing process are outlined. Possible scale-up recommendations are included in accordance with US FDA's Scale Up and Post Approval Changes Guidance for Immediate Release formulations. Toxicology information for amoxicillin includes acute toxicity values, such as oral LD50 in mice of 25 g/kg and in rats of 15 g/kg. Amoxicillin is not listed as a known carcinogen in any groups of the International Agency for Research on Cancer (IARC). Amoxicillin is an FDA pregnancy category B drug, and the occupational exposure limit (OEL) value and acceptable daily exposure (ADE) of amoxicillin are discussed in the report. The report provides a comprehensive analysis of the physicochemical, biopharmaceutics, and toxicological properties of amoxicillin, as well as its API synthesis, analytical, formulation, and manufacturing. The information presented is based on an extensive literature review of data available in the public domain and the opinion of several experts in the field.