The present invention relates to the hemi sulfuric acid salt of D-phenylglycine methyl ester, to a method for the preparation of said salt and to the use of said salt in the enzymatic synthesis of antibiotics and of D-phenylglycine methyl ester free base.

The present invention relates to amoxicillin trihydrate compositions having a surface area of from 1.0 to 2.5 m.sup.2.Math.g.sup.−1 that are free of organic contaminants such as dichloromethane, isopropanol, pivalic acid and triethyl amine and that have a purity of from 97.0% to 99.99%. Furthermore, the present invention relates to a method for the preparation of said amoxicillin trihydrate compositions and to the use of said compositions for the treatment of a bacterial infection.

The present invention relates to amoxicillin trihydrate compositions having a surface area of from 1.0 to 2.5 m.sup.2.Math.g.sup.−1 that are free of organic contaminants such as dichloromethane, isopropanol, pivalic acid and triethyl amine and that have a purity of from 97.0% to 99.99%. Furthermore, the present invention relates to a method for the preparation of said amoxicillin trihydrate compositions and to the use of said compositions for the treatment of a bacterial infection.

An object of the present invention is to provide a compound and a pharmaceutical composition which exhibit strong antibacterial activity against Gram-negative bacteria and drug-resistant Gram-negative bacteria. According to the present invention, a compound represented by General Formula [1] (the reference signs in the formula have the same definitions as those described in the present specification) or a salt thereof has strong antibacterial activity against Gram-negative bacteria such as Pseudomonas aeruginosa and drug-resistant Gram-negative bacteria including multidrug-resistant Pseudomonas aeruginosa, and the pharmaceutical composition containing the compound or a salt thereof is useful as an antibacterial agent. ##STR00001##

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.

An object of the present invention is to provide a compound and a pharmaceutical composition which exhibit strong antibacterial activity against Gram-negative bacteria and drug-resistant Gram-negative bacteria. According to the present invention, a compound represented by General Formula [1] (the reference signs in the formula have the same definitions as those described in the present specification) or a salt thereof has strong antibacterial activity against Gram-negative bacteria such as Pseudomonas aeruginosa and drug-resistant Gram-negative bacteria including multidrug-resistant Pseudomonas aeruginosa, and the pharmaceutical composition containing the compound or a salt thereof is useful as an antibacterial agent.

##STR00001##

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.