Pharmaceutical raw material Sulfamethazine

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Sulfamethazine Powder Usage and Synthesis.

Sulfadimethoxine is a broad-spectrum bacteriostatic agent, and its p-aminobenzoic acid (PABA), which can act competitively with PABA on the enzyme of folate synthase in the bacterial body, thus preventing the process of synthesising folic acid required by the bacteria as a raw material of PABA, and decreasing the amount of the metabolically active tetrahydrofolate, which is necessary for the bacterial synthesis of purine, thymine nucleoside and deoxyribonucleic acid (DNA). Sulfadimethoxine therefore inhibits the growth and reproduction of bacteria.

The effect of sulfadimethoxine is antagonised by PABA and its derivatives (procaine, bupivacaine), as well as by the presence of pus and decomposition products of the tissues, which provide essential substances for bacterial growth.

Uses and functions of Sulfamethazine.

An antimicrobial sulfonamide; induces CYP3A4 expression, as well as acetylation via N-acetyltransferase; exhibits sex-dependent pharmacokinetics, generating metabolic changes via the male-specific isoform CYP2C11; inhibits dihydrofolate synthase, with the effect of blocking folate synthesis.

It is used for the prevention and treatment of staphylococcus and Streptococcus solani infections, and has an inhibitory effect on haemolytic streptococcus and pleurodynamic coccus, mainly used for the treatment of avian cholera, avian typhoid fever, and coccidiosis of chickens.

It has inhibitory effect on haemolytic streptococcus, pneumococcus and meningitis.

Synthetics of Sulfamethazine.

A mixture of p-acetamidobenzenesulfonyl chloride (1.0 mmol) and cyclic amine (1.5 mmol) in water (1 mL) was stirred for 5 min and the resulting precipitate was collected by filtration.

It was transferred to a round-bottomed flask and 2 mL of concentrated solution was added. hydrochloric acid and 4 mL of water. The reaction mixture was gently boiled at 100°C for one hour.

The solution obtained in an ice bath was cooled and alkalised using saturated aqueous NaHCO3. The granular precipitate was filtered, washed with water and dried in air to give the product sulfadimethoxine.

Production Methods of Bulk Sulfamethazine Powder.

Sulfaguanidine by cyclisation with acetylacetone.

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