What is Cloxacillin Benzathine?
Cloxacillin Benzathine Powder is a semi-synthetic penicillinase-resistant penicillin antibiotic raw material, formed by the salt formation of two molecules of cloxacillin and one molecule of N,N'-dibenzylethylenediamine. Its molecular formula is 2C₁₉H₁₈ClN₃O₅S·C₁₆H₂₀N₂, with a molecular weight of 1112.11 g/mol. Cloxacillin Benzathine is a white to off-white powder and belongs to the isoxazolidinyl penicillin subclass of β-lactam antibiotics. The cloxacillin component in its core structure has the ability to resist β-lactamases secreted by enzyme-producing strains such as Staphylococcus aureus, thus effectively combating penicillinase-resistant bacteria. As a benzyl benzoate salt, this product has extremely low solubility, allowing it to slowly dissolve at the administration site and continuously release cloxacillin, achieving a long-acting sustained-release effect.
How to treat Gram-positive bacterial infections with Cloxacillin Benzathine?
Cloxacillin Benzathine Powder is primarily used in veterinary anti-infective therapy, with its core application being the treatment and prevention of mastitis in dairy cows during the dry period. Specifically, this active pharmaceutical ingredient (API) is formulated as an intramammary infusion for non-lactating dairy cows suffering from mastitis caused by Gram-positive bacteria such as Staphylococcus aureus and Streptococcus agalactiae. Due to its resistance to penicillinase, it can effectively kill penicillin G-resistant Staphylococci. In pharmaceutical formulation, Cloxacillin Benzathine Powder is a core component in the preparation of long-acting veterinary injections and intramammary infusions, and is widely used in the development of generic veterinary drugs and the formulation of compound antibiotic preparations. In clinical testing, this API is also used as a reference standard for drug susceptibility testing to assess the sensitivity of isolated strains to these drugs.
How does Cloxacillin Benzathine achieve sustained antibacterial effects through long-acting, sustained-release formulation?
Cloxacillin Benzathine Powder molecular structure can resist the degradation and destruction by β-lactamases secreted by Staphylococcus aureus. It can target and bind to key transpeptidases synthesized in bacterial cell walls, inhibiting cell wall cross-linking and causing osmotic imbalance, lysis, and death of pathogenic bacteria. It has specific and potent bactericidal effects against various enzyme-producing drug-resistant Staphylococcus aureus and Staphylococcus epidermidis, and also has inhibitory activity against some hemolytic streptococci. The benzathine group gives the raw material a slow-release, long-acting characteristic, which can maintain an effective antibacterial concentration in human tissues for a long time after administration, significantly extending the dosing interval. It can be used to prepare single-agent long-acting anti-infective agents, or it can be rationally combined with other suitable antibacterial excipients to adjust the treatment plan. It plays an irreplaceable pharmacological value in the long-term prevention and treatment of skin wounds and mild respiratory drug-resistant coccal infections.
MF of Cloxacillin Benzathine
Molecular Formula: 2C19H18ClN3O5S·C16H20N2
Molecular Weight: 885.11
Melting Point: 128～134℃
Precision quality: 884.3605
Density: 1.32g/cm³
PH: 4.8～6.6
Product Specification
| Item | Specification | Result |
| Appearance | White to off-white crystalline powder | Complies |
| Identification | IR/HPLC consistent with standard | Complies |
| Assay | 98.0% ~ 102.0% | 99.63% |
| Purity | ≥ 99.0% | 99.32% |
| Loss on Drying | ≤1.0% | 0.51% |
| Residue on Ignition | ≤0.1% | 0.06% |
| Heavy Metals | ≤ 10 ppm | < 5 ppm |
| Conclusion | Complies with enterprise standard | |
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FAQ：
Q1: Is the antibacterial effect of Cloxacillin Benzathine stable against enzyme-producing resistant Staphylococcus aureus?
A1: Its structure is resistant to β-lactamases and will not be destroyed by enzymes produced by resistant strains. Its bactericidal activity is long-lasting and stable, with consistent antibacterial efficacy across batches of raw materials, ensuring long-lasting anti-infective efficacy in the finished product.
Q2: What are the advantages of Cloxacillin Benzathine's long-acting sustained-release pharmacology?
A2: The carrier delays the release of the active ingredient, maintaining an effective antibacterial concentration in vivo for a longer period, reducing the need for frequent dosing and improving patient adherence.
Q3: What common clinical pathogens does Cloxacillin Benzathine's antibacterial spectrum cover?
A3: It primarily inhibits various enzyme-producing Staphylococcus aureus and Staphylococcus epidermidis, while also exhibiting good inhibitory effects against hemolytic streptococci, making it suitable for the production of preparations related to skin and respiratory tract coccal infections.
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