Sulbactam Sodium is a β-lactamase inhibitor used in combination with β-lactam antibacterial agents to overcome bacterial resistance mediated by β-lactamase enzymes. It is a semi-synthetic penicillanic-acid derivative and is commonly formulated with antibiotics such as ampicillin and cefoperazone.
The Indian Pharmacopoeia Commission defines Sulbactam Sodium as sodium (2S,5R)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate 4,4-dioxide. It is described as a white or almost white, hygroscopic crystalline powder.
Sulbactam Sodium has the molecular formula C₈H₁₀NNaO₅S and molecular weight 255.22 g/mol. Its CAS number is 69388-84-7 and FDA UNII is DKQ4T82YE6.
The active moiety, Sulbactam, has the formula C₈H₁₁NO₅S, CAS 68373-14-8, and molecular weight 233.24 g/mol.
Sulbactam Sodium is the sodium salt of Sulbactam. The molecule contains a β-lactam structure and sulfone functionality characteristic of penicillanic-acid sulfone derivatives.
The IP specification requires 97.0%–102.0% Sulbactam Sodium on an anhydrous basis. USP instead expresses the definition as 886–941 µg of Sulbactam per mg of Sulbactam Sodium, calculated on an anhydrous basis.
Sulbactam acts primarily as a β-lactamase inhibitor. It irreversibly interacts with susceptible β-lactamase enzymes, reducing their ability to hydrolyze β-lactam antibiotics.
When combined with a β-lactam antibiotic, this inhibition can restore or enhance antibacterial activity against organisms producing susceptible β-lactamases.
Sulbactam Sodium is used in combination pharmaceutical products, particularly with:
It is used in injectable formulations for treatment of susceptible bacterial infections.
Sulbactam Sodium has established pharmacopoeial controls. The IP monograph specifies:
The IP related-substances procedure controls several named Sulbactam impurities as well as total secondary peaks.
Sulbactam Sodium is a semi-synthetic pharmaceutical ingredient derived from a fermentation product. The manufacturing process involves controlled chemical conversion, purification, salt formation and crystallization followed by drying and analytical quality control. The BP/Ph. Eur. definition likewise describes it as a semi-synthetic product derived from a fermentation product.
Sulbactam Sodium is a white or almost white, hygroscopic crystalline powder. It is freely soluble in water, sparingly soluble in ethyl acetate and very slightly soluble in ethanol (96%). It is also freely soluble in dilute acids.
The IP specification gives a pH range of 4.5–7.2 for the aqueous solution, or 5.2–7.2 when the substance is sterile. Specific optical rotation is +219.0° to +233.0° in a 1% w/v aqueous solution.
Sulbactam Sodium should be protected from moisture. The IP monograph specifies storage protected from moisture and, for sterile material, in a sterile, airtight, tamper-proof container.
A pharmaceutical-grade Sulbactam Sodium API documentation package may include:
Sulbactam Sodium has established IP, USP and Ph. Eur. quality standards, allowing pharmaceutical manufacturers to control assay, impurities, water, pH, optical rotation and microbiological quality using recognized pharmacopoeial methods. The Indian Pharmacopoeia Commission specifically establishes a 97.0–102.0% anhydrous-basis content requirement.
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 97.0–102.0% anhydrous basis |
| pH (1% Solution) | 4.5–7.2 |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |
| Specific Rotation | +219.0° to +233.0° |
| Melting Point | 190°C |