Procaine penicillin G synthesis

Yield:-

Reaction Conditions:

with nipasol;Plasdone C-30;rongalite;sodium citrate;methyl 4-hydroxylbenzoate;lecithin;carboxymethylcellulose in water for 1 h;

Steps:

1
Example 1; To prepare a 2000L batch the following ingredients are used:QuantityPenicillin G Potassium*Methlyparaben2.6kgPropylparaben400gSodium Citrate (dihydrate)20kgCarboxymethylcellulose2.0kgPlasdone C-30 (Povidone)10.0kgLecithin12.0kgNa Formaldehyde Sulfoxylate400gProcaine Hydrochloride40.0kg+*Water for injectionQ.S.* to provide penicillin G procaine, 300,000 U/ml.Preparation of BulkMixing Tank 1 (MT-1): Mix designated inactive ingredients (Methylparaben,Propylparaben, Povidone C-30, Lecithin and Na Carboxylcellulose) in water for injection and heat the solution to 60°C. Sample the solution for visual observation, pH and bioburden. Adjust the pH if required and SIP sterilise the solution.Mixing Tank A (MT-A): Mix Sodium Citrate, Sodium Formaldehyde Sulfoxylateand Procaine Hydrochloride in 400 L of water for injection. Take sample for visual observation and bioburden. Transfer into the mixing tank MT1 through 0.2 micron sterile filter.Mixing Tank B (MT-B): Mix Penicillin G Potassium in 400 L of water for injection.Sample the solution for visual observation and bioburden. Transfer into the mixing tank MT1 through 0.2 micron sterile filter.Reaction ProcessOnce all ingredients have been added to mixing tank MT-1, the solution is Q.S.ed to the desired quantity and mixed for a period of not less than 1 hour. At this point the chemical reaction between the ingredients Penicillin G Potassium and Procaine Hydrochloride takes place to produce the active ingredient penicillin G procaine. The mixed solution is the Penicillin G Procaine bulk suspension.

References:

CROSS VETPHARM GROUP LIMITED WO2006/16347, 2006, A1 Location in patent:Page/Page column 4-6

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