| HS Code | 406671 |
| Product Name | Mezlocillin Sodium (sterile) Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable |
| Chemical Name | Sodium 6-(D-2-(3-methyl-2-oxo-1-imidazolidinecarboxamido)-2-phenylacetamido)penicillanate |
| Cas Number | 42057-22-5 |
| Molecular Formula | C21H24N5NaO8S2 |
| Molecular Weight | 561.56 g/mol |
| Appearance | White to off-white crystalline powder |
| Solubility | Freely soluble in water; sparingly soluble in alcohol; very slightly soluble in acetone |
| Assay | 96.0% to 102.0% on anhydrous basis by HPLC |
| Ph | 5.0 to 7.5 for 1% w/v aqueous solution |
| Sterility | Passes sterility test as a sterile product |
| Storage Condition | Store in airtight, moisture-protected container at 2°C to 8°C, protected from light |
As an accredited Mezlocillin Sodium (sterile) Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable factory, we enforce strict quality protocols—every batch undergoes rigorous testing to ensure consistent efficacy and safety standards.
| Packing | Sterile Mezlocillin Sodium API packaged as 1 kg per sealed aluminium bag, double polyethylene-lined, for oral and injectable formulations. |
| Container Loading (20′ FCL) | 20′ FCL: Sterile Mezlocillin Sodium API packed in sealed drums on pallets, temperature-controlled, protected from moisture, with secure loading and documentation. |
| Shipping | Mezlocillin Sodium (sterile) is shipped in temperature-controlled, tamper-evident containers to maintain potency and sterility. Handling requires dry, protected conditions and compliance with pharmaceutical logistics protocols. Transportation ensures full traceability, with cold-chain options available to preserve the API’s integrity for oral and injectable formulations. |
| Storage | Store in tightly closed, light-resistant containers in a cool, dry place at controlled room temperature (15–30°C). Protect from moisture, heat, and direct sunlight. Keep the sterile Pharma Grade API in its original sealed packaging until use. Avoid exposure to humidity and oxidizing agents to maintain potency, purity, and suitability for oral and injectable formulations. |
| Shelf Life | Shelf life: typically 24 months from manufacture, when stored in sealed containers, protected from moisture, heat, and light. |
Mezlocillin sodium sterile pharma-grade API is supplied as a white to off-white crystalline powder intended for parenteral use. The acylureido penicillin nucleus is hydrolytically unstable in gastric acid; consequently, tablet, capsule, and granule oral dosage formats are not supported by pharmacopoeial monographs or clinical pharmacokinetic data for oral bioavailability. The downstream tracks below are therefore limited to sterile injectable manufacturing, hospital sterile compounding, fixed-dose combination filling, and point-of-care reconstitution.
Aseptic powder filling of sterile mezlocillin sodium into single-dose borosilicate glass vials constitutes the primary large-volume downstream route; this operation is governed by USP <71> Sterility Tests, USP <85> Bacterial Endotoxins Test, USP <788> Particulate Matter in Injections, USP <790> Visible Particulates in Injections, 21 CFR 211.167 special testing requirements, and EU GMP Annex 1 grade A/B environmental criteria. The formulation is excipient-free: the sterile sodium salt is filled as 100% w/w of the dry powder, with label claims of 1 g, 2 g, 3 g, or 4 g expressed as mezlocillin acid equivalent; release potency is typically controlled within 95.0–105.0% of label claim, and residual moisture is held below 2.0% w/w by Karl Fischer titration (USP <921> Method Ic). On a production line, the sterile API is transferred from charge hoppers into a restricted access barrier system or isolator fitted with Class A air supply (ISO 14644-1 Class 5 at-rest); rotary vial washers deliver washed vials to a depyrogenation tunnel operating at 250°C for at least 30 minutes, achieving a validated 3-log endotoxin reduction. Powder filling is performed by auger or vacuum-drum fillers; fill weight drift of ±1.5% per vial is monitored by in-process checkweighers, and static charge generated by low-humidity powder transfer at or below 30% RH can reduce fill consistency on continuous lines. Because terminal steam sterilization is generally unsuitable for the thermolabile β-lactam ring, sterility assurance depends on the incoming bulk API and aseptic filling. After filling, vials receive halogenobutyl rubber stoppers and aluminum flip-off seals under nitrogen purge, with headspace oxygen controlled below 2.0% v/v to limit oxidative degradation. Terminal finished product configurations are single-dose vials of 1 g, 2 g, 3 g, and 4 g for reconstitution and intravenous administration in acute-care settings.
The fixed-dose injectable combination of mezlocillin sodium and sulbactam sodium, where registered, is manufactured as a sterile dry powder for solution for injection or infusion; the compliance framework includes the pharmacopoeial monographs for both components, USP <905> Uniformity of Dosage Units for blend homogeneity, USP <71> Sterility Tests, USP <85> Bacterial Endotoxins Test, USP <788> Particulate Matter in Injections, and ICH Q3D elemental impurity limits. The formulation addition ratio is 4:1 w/w on an active acid basis: a 1.25 g vial contains 1.0 g mezlocillin equivalent and 0.25 g sulbactam; 2.5 g and 3.75 g vials contain 2.0 g/0.5 g and 3.0 g/0.75 g, respectively. Production-scale dry blending of the two sterile sodium salts is performed in double-cone blenders or V-blenders under low-humidity nitrogen-blanketed conditions; powders are sieved through a 0.5 mm stainless steel screen prior to blending to reduce agglomerates, and the primary process conflict is segregation of the two compounds during hopper discharge into the filling line because their particle size distributions and bulk densities differ. Blend uniformity is verified at minimum and maximum fill depths with high-performance liquid chromatographic assay, and filling is typically performed with rotary auger equipment at line speeds of 60–180 vials/min depending on vial diameter; in-process checkweighing rejects vials outside ±3% of target weight. Terminal product types are 1.25 g, 2.5 g, and 3.75 g combination vials intended for intravenous infusion after reconstitution.
In centralized pharmacy sterile compounding, bulk vials are converted into ready-to-use intravenous admixtures for hospital formularies under USP <797> Pharmaceutical Compounding—Sterile Preparations. The dilution ratio is a two-stage process: a 2 g vial is reconstituted with 40 mL sterile water for injection to yield 50 mg/mL, then transferred into an infusion bag of 0.9% sodium chloride injection or 5% dextrose injection to achieve a final concentration of 20 mg/mL; for peripheral administration, concentrations above 50 mg/mL are avoided due to osmotic irritation. Automated compounding devices with gravimetric accuracy of ±1% and integrated barcode verification operate in ISO Class 5 laminar airflow workbenches or compounding aseptic isolators; batch-to-batch variance in reconstitution time is influenced by the bulk API particle size, because highly electrostatic powders adhere to vial walls and require longer vortex agitation on peristaltic mixing stations. Beyond-use dating is assigned according to USP <797> risk categories: low-risk preparations without sterility testing may be assigned up to 14 days at 2–8°C, while immediate-use preparations in ward environments are limited to 4 hours at room temperature unless continuous infusion with published stability data supports longer dating. Terminal finished product types include 50 mL and 100 mL ready-to-use infusion bags, elastomeric reservoir devices for outpatient parenteral antimicrobial therapy, and syringes for intravenous push administration.
The intramuscular route for mezlocillin sodium is an established but lower-volume application, typically reserved for moderate infections where intravenous access is not available; the regulatory framework relies on USP <1> Injections, USP <71> Sterility Tests, and the approved product package insert for diluent compatibility. The formulation addition ratio for intramuscular reconstitution is 1 g in 4 mL of sterile water for injection or 0.5% lidocaine hydrochloride injection; powder displacement yields approximately 5 mL of solution, corresponding to 200 mg/mL. A single intramuscular injection site should not receive more than 3 mL, which limits practical single-site dosing to 600 mg under standard protocols. Downstream production in this pathway is point-of-care reconstitution rather than industrial processing: the vial contents are injected with diluent using a 21-gauge or 22-gauge needle connected to a 10 mL syringe, followed by gentle inversion until dissolution is complete; the resulting solution must be inspected for visible particulates before administration. Terminal finished products are 1 g and 2 g single-dose vials labelled for intramuscular and intravenous use, with the intramuscular route usually restricted to short courses because of limited injection volume tolerance in adult deltoid and gluteal sites.
Critical care protocols for mezlocillin sodium frequently use extended or continuous infusion to maximize the time above MIC for susceptible Gram-negative pathogens; this downstream application is governed by USP <797> sterile compounding requirements, institutional antimicrobial stewardship guidelines, and, where continuous infusion pumps are used, IEC 60601-2-24 for infusion pump performance. The addition ratio for continuous infusion is typically 20 mg/mL in 0.9% sodium chloride injection, with daily doses of 12 g to 24 g diluted into 500 mL or 600 mL reservoirs; the limiting process parameter is hydrolytic degradation of the β-lactam ring in aqueous solution, which accelerates above 25°C and imposes shorter beyond-use dating than refrigerated storage. Production-scale preparation in hospital pharmacies uses automated compounding devices to transfer reconstituted mezlocillin sodium into elastomeric infusion devices or syringe pump cassettes; batch-to-batch variance in cold-chain storage is monitored with temperature loggers because excursions above 8°C during transport can reduce the acceptable administration window. Terminal finished dosage configurations include 100 mL to 600 mL elastomeric infusion reservoirs, 50 mL syringe cassettes for syringe drivers, and ready-to-use infusion bag formats labelled with beyond-use dates of 24 hours at 2–8°C where validated stability data exist.
In pediatric and neonatal wards, the same sterile powder vials are repackaged or diluted into lower-concentration minibags because label concentrations exceed the dosing accuracy required for patients under 40 kg; this application sits within USP <797> and hospital pharmacy guidelines, with additional compliance to ICH Q3D because elemental impurity exposure per kilogram of body weight shifts when small vial fractions are used. The addition ratio is a two-step dilution: a 1 g vial is reconstituted to 50 mg/mL with 0.9% sodium chloride injection, then further diluted to 10 mg/mL or 20 mg/mL for intermittent infusion over 30 minutes; dose rounding is typically performed to 0.1 mL increments on syringes with 1 mL graduation. Downstream processing in the pharmacy uses sterile vial-to-bag transfer devices, syringe pumps, and infusion pump drug libraries calibrated against the specific barrel diameter of the syringe used; the main production bottleneck is the retention of undissolved particles in the vial neck after reconstitution, requiring filtration through a 5-micron filter needle if visible matter persists. Terminal product types are 10 mg/mL and 20 mg/mL pediatric minibags, 10 mL and 20 mL syringes for injection into intravenous lines, and syringe pump cassettes for weight-based dosing.
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Mezlocillin sodium (CAS 59798-30-0) is a sterile pharma-grade acylureido penicillin API, chemically sodium (2S,5R,6R)-3,3-dimethyl-6-[(2R)-2-[(3-methylsulfonyl-2-oxoimidazolidine-1-carbonyl)amino]-2-phenylacetyl]amino-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate, with molecular formula C21H24N5NaO8S2 and molecular weight 561.56 g/mol. The powder is supplied as a white to off-white crystalline solid with high aqueous solubility, and the sterile injectable grade is controlled under pharmacopeial monographs where recognized. Manufacturer-specific product codes usually designate sterile injectable, sterile micronized, and non-sterile oral solid grades. The molecule is a β-lactam antibiotic with an acylureido side chain; it is primarily used as a dry powder for reconstitution into intravenous or intramuscular injection. Claims for tablet, capsule, granule, or oral use require a non-sterile oral grade with different bioburden and endotoxin specifications, but the β-lactam ring is acid-labile and reliable human oral bioavailability is not established. The product differs from piperacillin and azlocillin in side-chain substitution, β-lactamase susceptibility, and clinical formulation strategy. The sodium salt form requires particular attention to sodium load in infusion electrolyte calculations.
Release criteria for the sterile injectable grade are tighter than those for non-sterile oral grades in bioburden, bacterial endotoxins, and particulate cleanliness. Pharmacopeial monographs for mezlocillin sodium, where applicable, define assay on anhydrous basis, pH of a 10% aqueous solution, specific optical rotation, water, residual solvents, sterility, and endotoxin limits. The table below lists typical release limits aligned with USP general chapters and ICH Q3C/Q3D. Batch certificates also include particle-size data by laser diffraction using ISO 13320; for the injectable grade, dissolution of the dry powder is controlled mainly by crystal habit and surface area, not by a USP particle-size monograph.
| Parameter | Typical release limit | Method designation |
|---|---|---|
| Appearance | White to off-white crystalline powder | Visual |
| Assay (anhydrous basis) | 91.0–100.5% | HPLC per USP monograph |
| pH of 10% aqueous solution | 5.0–7.5 | USP <791> |
| Water | ≤ 6.0% | Karl Fischer, USP <921> |
| Specific optical rotation | +170° to +200° (c = 1, water) | USP <781> |
| Bacterial endotoxins, sterile grade | ≤ 0.10 EU/mg | USP <85>, Ph. Eur. 2.6.14 |
| Sterility | No growth | USP <71>, Ph. Eur. 2.6.1 |
| Residual solvents | methanol ≤ 3000 ppm, acetone ≤ 5000 ppm, dichloromethane ≤ 600 ppm | ICH Q3C Option 1 |
| Elemental impurities | Class 1 elements at or below ICH Q3D limits; Class 2A/2B batch-specific | USP <232>, <233> |
The bacterial endotoxin limit of ≤ 0.10 EU/mg for the sterile grade is not a fixed safety margin for every intended dose; it must be evaluated against the maximum adult daily dose and the finished product label. Sterility testing is performed on each batch using membrane filtration or direct inoculation, and the sterility assurance concept relies on aseptic manufacture rather than terminal sterilization because aqueous heat treatment degrades the β-lactam ring. The residual solvent profile reflects the crystallization and drying sequence; manufacturers using methanol, acetone, or dichloromethane must demonstrate that lot release values remain at or below the ICH Q3C Option 1 limits. Elemental impurity data are supplied per ICH Q3D and USP <232>/<233>; for injectable grade, Class 1 elements such as cadmium, lead, arsenic, and mercury are controlled at the finished-product limit, not at a diluted bulk intermediate level. The product should be stored in well-closed containers with desiccant and protected from moisture; re-sampling from open containers in humid production rooms should be minimized if relative humidity exceeds 60%.
In aseptic manufacturing, the sterile powder is double-bagged in polyethylene and aluminum foil and transferred into a Grade A filling line under EU GMP Annex 1 conditions. Glass vials are washed and depyrogenated in a tunnel at temperatures at or above 300°C, and stoppers are steam-sterilized at 121°C for 15 min or an equivalent F0 cycle. Mezlocillin sodium is not subjected to terminal steam sterilization; the β-lactam ring opens rapidly in aqueous solution at elevated temperature, and dry heat can cause discoloration. The principal processing bottleneck is hygroscopicity. Campaigns run in facilities without controlled humidity show caking, poor weight control, and visible aggregates when the powder is exposed to relative humidity above 60%. Because the API is crystalline and flowable only within a narrow moisture window, incoming lots are qualified by bulk density, angle of repose, and residual solvent profile before manufacturing. Drying after crystallization is typically performed under vacuum at temperatures not exceeding 40°C. Residual acetone and methanol desorb slowly as the powder approaches 2% water; equipment-specific drying curves show extended secondary drying for agglomerates larger than approximately 500 μm. Batch-to-batch crystal habit differences also affect reconstitution time; producers of injectable vials often specify a maximum reconstitution time after adding diluent, but published pharmacopeial standards for reconstitution time are limited.
Sterile filtration of the bulk solution before crystallization is performed with 0.2 μm sterilizing-grade membranes, and filter integrity is tested by bubble point, diffusive flow, or water intrusion per ASTM F838. Container closure integrity of the filled vials is evaluated by dye ingress or vacuum decay under USP <1207>. Degradation products include the hydrolyzed β-lactam ring-opened acid and carbonyl fragmentation products; HPLC methods require resolution of the main peak from the hydrolyzed impurity. For sterile injectable grade, total unspecified impurities are controlled against the monograph limits; published photostability data for mezlocillin sodium are limited, and the product should be protected from light. Particulate matter in the finished injectable is controlled per USP <788>; for API powder, subvisible particulate is not directly specified, so the manufacturer relies on controlled crystallization and filtration before drying.
Development of oral tablet and capsule forms is constrained by acid-catalyzed hydrolysis of the β-lactam ring in gastric fluid and by the absence of reliable oral bioavailability data for mezlocillin sodium. If oral solid dosage development is undertaken, dry granulation or roller compaction is preferred over aqueous high-shear granulation; water contact at elevated temperature accelerates ring opening and increases degradation products. Residual moisture in granules should be held below 2.0% by Karl Fischer before compression, and enteric polymer coatings such as hypromellose acetate succinate or methacrylic acid-ethyl acrylate copolymer are required to reduce gastric acid contact. Powder blends for capsules require laser-diffraction particle-size control per ISO 13320, with D10/D50/D90 reported on the certificate of analysis; fines below 10 µm can cause sticking and flow defects, while coarse particles reduce content uniformity in low-dose blends. The API should not be blended with acidic fillers or effervescent couples because acid liberation accelerates β-lactam degradation. For granule or dry syrup formats, the vehicle should be buffered near pH 5.0–7.0 and used immediately after reconstitution; published data on extemporaneous oral suspension stability are limited. Process selection for tablet and capsule work should also account for the sodium content of the API, because tablet disintegration and osmotically driven release can be altered by the soluble salt. Non-sterile oral grades may have a higher bioburden limit than sterile injectable grades, but they must still meet ICH Q3C, ICH Q3D, and the same assay and impurity specifications unless a compendial monograph for an oral solid dosage form is established.
Excipient compatibility studies should include forced degradation with water, magnesium stearate, lactose, microcrystalline cellulose, and croscarmellose sodium; published data specific to mezlocillin sodium in roller-compacted matrices are limited, so powder blend stability must be generated under ICH Q1A(R2) stress conditions. For capsule filling, dosator or tamping-pin machines may require granulation to improve flow; if the powder is dry granulated, the granule size should be controlled by sieve analysis in addition to laser diffraction. Direct compression of the untreated API is generally not practical because the crystalline powder has high bulk density but variable flow; for low-dose oral solid forms, pre-filling the API into a dry-blended carrier with colloidal silicon dioxide is used to reduce segregation. The absence of published human oral bioavailability data is a limitation for any oral solid dosage claim, and a tablet or capsule specification cannot be transferred directly from an injectable monograph.
The distinguishing structural feature of mezlocillin is the 3-methylsulfonyl-2-oxoimidazolidine-1-carbonyl substituent on the penicillin side chain. This polar side chain improves Gram-negative outer-membrane penetration relative to benzylpenicillin, but the resulting anti-Pseudomonas activity is generally lower than that of piperacillin when measured by CLSI M07 broth microdilution or EUCAST broth microdilution. Piperacillin carries a 4-ethyl-2,3-dioxo-1-piperazinecarbonyl side chain and is available as a co-formulation with tazobactam; mezlocillin sodium has no marketed β-lactamase inhibitor combination. Azlocillin carries a 2-oxo-1-imidazolidinecarbonyl side chain without the methylsulfonyl group, and its commercial use has declined in many regions. Compared with carboxypenicillins such as ticarcillin, mezlocillin shows a broader Enterobacteriaceae spectrum but remains hydrolyzed by class A extended-spectrum β-lactamases and by chromosomal AmpC enzymes. Differences in sodium load also affect infusion compounding: piperacillin sodium is reported in US labeling as containing 1.85 mEq of sodium per gram; mezlocillin sodium product information from older finished-product labels lists a sodium value in a similar range, but current compendial monographs do not uniformly specify sodium content, so the batch certificate should be consulted for electrolyte calculations. In susceptibility reporting, MIC interpretive criteria must follow current CLSI M100 or EUCAST breakpoints; published MIC distributions for mezlocillin against Pseudomonas aeruginosa are method- and collection-dependent and should not be extrapolated across regions without local antibiograms.
| Compound | Side-chain substituent | β-Lactamase inhibitor co-formulation | Primary route |
|---|---|---|---|
| Mezlocillin sodium | 3-methylsulfonyl-2-oxoimidazolidine-1-carbonyl | None | IV/IM |
| Piperacillin sodium | 4-ethyl-2,3-dioxo-1-piperazinecarbonyl | Tazobactam | IV |
| Azlocillin sodium | 2-oxo-1-imidazolidinecarbonyl | None | IV |
For sterile injectable compounding, mezlocillin sodium is reconstituted with water for injection or compatible diluent and administered as an intravenous infusion under aseptic technique per USP <797>. The reconstituted solution is not terminally sterilized, and in-use stability is governed by concentration, diluent pH, and storage temperature. Published data for related acylureido penicillins indicate that β-lactam hydrolysis is slowest in the pH 5.0–7.0 range and accelerates at pH below 4.0 or above 8.0. The API should not be combined with aminoglycoside antibiotics in the same infusion container or in the same intravenous line without compatible flushing, because aminoglycoside amino groups can open the β-lactam ring and form inactive adducts. The dry sterile powder is stored at controlled room temperature in tight containers protected from light and moisture. In manufacturing dispensaries, repeated opening of bulk containers should be avoided at relative humidity above 60%; if an opened container must be held, it should be re-sealed with a fresh desiccant sachet and the holding time qualified by in-house stability data under ICH Q1A(R2). For tablet and capsule operations, the operational boundary is residual moisture; aqueous granulation is not recommended, and direct compression or dry granulation with moisture-resistant packaging is the only practical oral solid-dose route.
