| HS Code | 136669 |
| Chemical Name | 6-fluoro-1-(4-fluorophenyl)-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid |
| Cas Number | 98105-99-8 |
| Molecular Formula | C20H17F2N3O3 |
| Molecular Weight | 385.36 g/mol |
| Appearance | White to pale yellow crystalline powder |
| Solubility | Slightly soluble in water; soluble in dilute alkaline solutions and polar organic solvents; hydrochloride salt form is soluble in water |
| Melting Point | Approximately 270°C with decomposition |
| Assay | 98.0% to 101.0% on dried basis |
| Ph | 3.0 to 5.0 for aqueous solution of hydrochloride salt form |
| Shelf Life | 24 months in original tightly closed container |
| Storage | Store in tight, light-resistant containers at controlled room temperature 20°C-25°C, protected from moisture |
| Antibacterial Spectrum | Broad-spectrum activity against Gram-positive and Gram-negative bacteria, including Escherichia coli, Pasteurella, Salmonella, and Mycoplasma |
| Indicated Dosage Forms | Tablets, injections, capsules, powders, granules, premix, and solutions |
As an accredited Sarafloxacin Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions factory, we enforce strict quality protocols—every batch undergoes rigorous testing to ensure consistent efficacy and safety standards.
| Packing | Packaged in sealed, light-protective containers, 25 kg per drum, with tamper-evident closure for stability and safety. |
| Container Loading (20′ FCL) | 20′ FCL container loaded with Sarafloxacin Veterinary Grade API, securely packed in sealed drums, ready for pharmaceutical formulation. |
| Shipping | Sarafloxacin Veterinary Grade API is shipped in sealed, light-resistant, moisture-proof containers to maintain stability and purity. Transport under controlled temperature, avoiding excessive heat and humidity. Properly labeled for veterinary use, with safety data sheets and certificates of analysis included. Handling follows GMP and applicable dangerous goods regulations. |
| Storage | Store Sarafloxacin Veterinary Grade API in a well-closed, light-resistant container in a cool, dry place, ideally below 25°C. Protect from moisture and direct sunlight. Avoid exposure to excessive heat or humidity. Keep container tightly sealed when not in use to maintain stability and potency. Ensure proper labeling and secure storage away from feed, food, and animals. |
| Shelf Life | Shelf life is typically 24 months when stored in a cool, dry, airtight container protected from light. |
Sarafloxacin veterinary-grade API supplied for tablets, injections, capsules, powders, granules, premix, and solutions enters the poultry water-medication stream as a milled hydrochloride salt. In broiler and turkey integrations, sarafloxacin hydrochloride is dry-blended into a water-soluble powder for mass administration through proportional medicators or stock-tank buckets. The API is milled to a D90 below 75 µm to prevent medicator nozzle blockage, then blended in a 200 kg ribbon blender at 20–25 rpm for 10–15 minutes with dextrose monohydrate, citric acid buffer, and 0.5% w/w colloidal silicon dioxide. The citric acid buffer is pre-dispersed to hold final solution pH between 3.5 and 4.5 because sarafloxacin hydrochloride tends to lose solubility above pH 6.5; field water hardness above 500 mg/L CaCO₃ must be corrected with an acidifier or chelating agent before medicator introduction, since calcium and magnesium present a chelation risk that depresses oral absorption. Release testing under Ph. Eur. 5.1.4 for non-sterile oral powders sets total aerobic microbial count below 10³ CFU/g and bile-tolerant Gram-negative bacteria below 10¹ CFU/g; absence of Escherichia coli in 1 g is required. A standard field concentration is obtained with a 10.0% w/w powder: adding 100 g of finished powder to 10 L of stock solution and metering at 1:100 delivers 100 mg/L, while 1:200 delivers 50 mg/L. Batch production passes through a 0.5 mm in-line sieve and is packed under 35% relative humidity in foil-lined LDPE heat-sealed pouches; terminal formats include 1 kg, 5 kg, and 25 kg high-barrier packs with desiccant. Waterline sanitizing with chlorine must be followed by residual free chlorine neutralization below 0.5 mg/L before medication to avoid oxidative degradation.
| Stock solution (g/L) | Proportioner setting | Final drinking water concentration (mg/L) |
|---|---|---|
| 50 | 1:100 | 50 |
| 75 | 1:100 | 75 |
| 100 | 1:100 | 100 |
| 100 | 1:200 | 50 |
Feed mills producing therapeutic premixes for poultry integrators face an assay recovery problem if sarafloxacin hydrochloride is simply dry-blended with uncoated limestone or dicalcium phosphate; the free carboxyl and carbonyl groups in the fluoroquinolone complex with calcium and iron, causing batch-to-batch assay recovery drift that exceeds the acceptance criterion of the medicated feed authorization. The accepted corrective step is to pre-coat the carrier with 0.5% w/w soy lecithin or 1.0% w/w refined vegetable oil in a paddle mixer before adding the API. A mid-premix is then standardized at 2.0–10.0% w/w sarafloxacin hydrochloride on coated wheat middlings or lactose monohydrate; final medicated feed is typically incorporated at 0.05–0.10 kg/tonne, depending on the national registration dossier. Granulation is performed on a fluid bed top-spray unit with binder solution containing 3–5% w/w povidone K30, inlet air temperature 55–60 °C, product temperature 35–40 °C, and final moisture not exceeding 2.0%. The feed safety system follows Regulation (EC) No 183/2005 for feed hygiene and Regulation (EU) 2019/4 for medicated feed; stability is supported under VICH GL18. Finished products are filled into 25 kg multiwall paper bags with PE liners; terminal granules or extruded pellets must be protected from direct sunlight and stored below 30 °C. A hard incompatibility exists with high-iron mineral premixes, bentonite carriers, and water-absorbing silicate binders; these materials must be excluded from the same blending sequence because they promote local pH shifts and reduce drug recovery.
Unlike the waterline route used in poultry houses, cold-water finfish therapy does not begin with a field-mixed powder; sarafloxacin hydrochloride is applied as a top-coated therapeutic pellet via vacuum coating, because immersion bath exposure in salmonid smolts produces inconsistent drug intake due to mucus clearance and variable gill perfusion. The formulation addition ratio is built in two steps: a 5.0% w/w oil-phase dispersion of API in fish oil is prepared first, then sprayed onto extruded pellets to reach a final feed concentration of 0.05–0.10% w/w, which corresponds to a 5 mg/kg body weight daily dose when fish consume 1% body weight per day. The coating line operates at 40–50 °C vessel wall temperature and 45 °C oil temperature with 2–3 bar compressed air for atomization; after coating, pellets are cooled to ≤10 °C and immediately packed in 25 kg sealed bags. A 30-minute leaching test in 8 °C artificial seawater should show ≤5% API loss; published data for this specific sarafloxacin hydrochloride coating configuration is limited, so each production line must validate pellet hardness and oil penetration limits. Regulatory use requires a national prescription and residue surveillance under the applicable listing, such as Commission Regulation (EU) No 37/2010 where the substance is listed for the target species; feed mills must maintain medicated feed records under Regulation (EU) 2019/4. Terminal product types are extruded finfish pellets of 2–5 mm diameter with fish oil topcoat; they are not suitable for rainbowing or high-temperature re-extrusion.
Aseptic filtration rather than terminal autoclaving is selected for low-pH sarafloxacin hydrochloride solutions because the formulation contains benzyl alcohol and is packaged in amber Type I glass vials; final autoclaving can accelerate oxidative discoloration in the presence of trace iron. The solution is compounded at 5.0–10.0% w/v sarafloxacin hydrochloride, adjusted with hydrochloric acid or sodium hydroxide to pH 4.0–4.5, preserved with 1.0–2.0% v/v benzyl alcohol in multi-dose presentations, and made to volume with water for injection. Bulk holding under nitrogen overlay maintains dissolved oxygen below 0.5 ppm; the liquid is passed through a 0.22 µm PVDF sterilizing filter with 100% integrity testing and then filled into siliconized Type I glass vials under laminar airflow. Sterility is tested according to Ph. Eur. 5.1.1 and the finished product must meet the particulate and fill-volume requirements of USP <1>. Terminal formats are 10 mL, 50 mL, and 100 mL vials with synthetic rubber stoppers and flip-off seals. The injection is incompatible with aluminum hydroxide adjuvants and should not be admixed with magnesium- or calcium-containing diluents because precipitation occurs. Production-scale filling often includes automatic weight-check rejection; the filled vials are packed in amber cartons and stored below 25 °C.
For psittacine and raptor patients under veterinary care, sarafloxacin hydrochloride is compounded into capsules or tablets when licensed oral liquids are not available in a small enough dose; this is a non-food species application governed by USP <795> and FDA 21 CFR 530.13 extralabel use rules. The pharmacist prepares a 1:10 or 1:100 trituration with microcrystalline cellulose by geometric dilution; final capsule strengths range from 5 mg to 20 mg in size 3 to 5 capsules. A 100-hole manual capsule filling machine is used for batch sizes above 100 units, with weight variation checks on 10 units and HPLC content uniformity limits of 90.0–110.0% of label claim. Tablet production from the same trituration uses a single-punch press with 50 mg total tablet mass, 5% w/w crospovidone, 0.5% w/w magnesium stearate, and 1% w/w talc; friability is tested on 10 tablets. The finished capsules are packaged in opaque HPMC or gelatin shells and blister-sealed under low humidity; tablets are scored and stored below 25 °C. Because sarafloxacin is a fluoroquinolone, the preparation must be protected from light and stored in amber vials after trituration; use in food-producing species is not permitted under this compounding route.
Stabilizing sarafloxacin hydrochloride in a ready-to-use oral solution requires strict control of light exposure, headspace oxygen, and metal ion contamination. The liquid is formulated at 10.0% w/v API with 2.0–4.0% w/v citric acid monohydrate, 0.1% w/v disodium edetate, and, where justified by multi-dose use, 1.0% v/v benzyl alcohol; the pH is set at 3.8–4.2 to keep the hydrochloride in solution. The manufacturing process uses a closed stainless steel mixing vessel under vacuum, followed by 0.45 µm clarification and filling into amber HDPE jerry cans with nitrogen headspace. Dilution in the field is 1 L of the 10% solution to 1000 L drinking water, yielding 100 mg/L. Preservative effectiveness is assessed under USP <51>; stability is bracketed under VICH GL18. Terminal formats are 5 L and 20 L amber HDPE or fluorinated HDPE containers, stored below 30 °C and protected from sunlight. The solution is incompatible with aluminum hydroxide, soluble calcium salts, and strong oxidizing agents; scaling in waterlines must be removed before medication to prevent local drug binding to iron oxide deposits.
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Sarafloxacin hydrochloride (CAS 91296-87-6) is the hydrochloride salt of sarafloxacin base (CAS 98105-99-8), a 6-fluoro-4-oxo-7-(piperazin-1-yl)quinoline-3-carboxylic acid derivative with a 4-fluorophenyl substituent at N-1. The veterinary-grade active pharmaceutical ingredient is supplied as a white to pale yellow crystalline powder with a hydrochloride molecular mass of 421.83 g/mol and a base molecular mass of 385.36 g/mol. Two commercial particle-size designations are available: a standard crystalline grade with D90 not exceeding 100 µm for tablet, capsule, and granulation operations, and a micronized grade with D90 not exceeding 20 µm for aqueous solutions, water-soluble powders, and medicated feed premixes where rapid dispersion and homogeneous suspension are required. The API is released under specifications aligned with ICH Q7 good manufacturing practice for active pharmaceutical ingredients, ICH Q3C residual solvent guidance, and ICH Q3D elemental impurity guidance. The product is intended for veterinary finished dosage forms of sarafloxacin hydrochloride; it is not a sterile finished medicine and must be further processed before administration. Published data for some formulation configurations is limited; therefore, each finished product dossier should confirm route-specific release limits and stability behavior.
Bulk veterinary API sampling follows reduced sampling plans under ANSI/ASQ Z1.4, with representative draws from top, middle, and bottom of each drum. Fourier-transform infrared spectroscopy and HPLC are used for identity confirmation. In multi-product API facilities, sarafloxacin hydrochloride is segregated from beta-lactam and sulfonamide APIs through dedicated or validated cleaned equipment. Cleaning validation limits are calculated from toxicological acceptable daily exposure and analytical determination by HPLC with a limit of quantitation not greater than 0.1 µg/cm² for shared contact surfaces. Production personnel use respiratory protection because fluoroquinolone dust is a potential phototoxic and respiratory irritant.
The hydrochloride salt exhibits pH-dependent aqueous solubility. Solutions prepared at pH 3.0 to 5.0 maintain clear, assay-stable conditions; as pH approaches 6.5 to 7.0, the free base precipitates, producing filtration loss and nonuniform dosing in metering pumps. Injectable solutions are therefore adjusted to the approved finished-product pH, commonly below 5.5, and filtered through 0.22 µm PVDF or PES membranes. Nylon membranes and depth filters with charged surfaces may adsorb fluoroquinolone carboxylate species and reduce assay recovery; filtration validation should measure sarafloxacin binding against the selected membrane. Oral solutions and water-soluble powders should be prepared with buffered acidulant systems where the final drinking-water pH remains below 7.0. Use of hard water containing Ca²⁺ and Mg²⁺ above 200 mg/L as CaCO₃ equivalents may form chelated species and reduce bioavailable drug; addition of citric acid at 0.5% w/v to 1.0% w/v is commonly used to lower pH and chelate hardness ions. Published data for this specific API in hard-water administration is limited; the finished product label should state the maximum acceptable water hardness.
Metering pump lines for water medication should be flushed after use because residual sarafloxacin hydrochloride can precipitate when the water pH rises above 7.5 during cleaning with alkaline detergents. Stock solutions held at ambient temperature are assigned a 24 h use period; solutions stored beyond 24 h require re-assay and pH documentation before administration.
Release acceptance for the veterinary-grade API includes identification, assay, purity, solvents, elemental impurities, particle size, and microbial quality. The following parameters are applied to each batch unless otherwise specified on the certificate of analysis. Analytical methods use high-performance liquid chromatography, gas chromatography, laser diffraction, and compendial limit tests.
| Parameter | Acceptance criterion | Reference method |
|---|---|---|
| Appearance | White to pale yellow crystalline powder | Visual inspection |
| Identification by HPLC | Retention time matches sarafloxacin hydrochloride reference standard | HPLC, USP <621> |
| Assay on dried basis | 98.0–102.0% as C₂₀H₁₈ClF₂N₃O₃ | HPLC, USP <621> |
| Loss on drying | ≤0.5% | USP <731> |
| Residue on ignition | ≤0.1% | USP <281> |
| Elemental impurities | Complies with ICH Q3D route limits | USP <232> / <233> |
| Residual solvents | Complies with ICH Q3C Option 1 | USP <467> |
| Related substances | Any individual impurity ≤0.5%; total impurities ≤2.0% | HPLC, USP <621> |
| Bacterial endotoxins, parenteral grade | ≤0.15 EU/mg or as justified by finished product dose | USP <85> |
| Particle size, micronized grade | D90 ≤20 µm; D50 ≤10 µm | ISO 13320-1:2020 |
| Particle size, standard grade | D90 ≤100 µm | ISO 13320-1:2020 |
Polymorphic identity is controlled by X-ray powder diffraction. The micronized grade may develop amorphous surface content during jet milling. If amorphous content exceeds 10%, moisture uptake increases and chemical stability can decline; therefore, nitrogen-assisted jet milling with inlet temperature not above 40 °C is used to keep amorphous content below 5%. Powder X-ray diffraction is performed according to USP <941>; crystalline peaks must match the approved reference diffractogram. Microbiological quality for oral powder and premix grades is confirmed by total aerobic microbial count not more than 10³ CFU/g, total yeast and mold count not more than 10² CFU/g, and absence of Escherichia coli. Parenteral grade material is controlled further for bioburden and endotoxin.
Sarafloxacin hydrochloride is sensitive to ultraviolet and visible light; photolytic degradation produces defluorinated and oxidized impurities that increase total related substances. Bulk API and finished premixes should be stored in amber glass or opaque high-density polyethylene containers with closures tested for light transmission under USP <671>. The recommended storage condition is 15 °C to 25 °C with desiccant. Bulk retest interval is 36 months from the manufacture date when stored at 25 °C and 60% RH in double low-density polyethylene liners inside a sealed HDPE drum. At relative humidity above 60%, the hydrochloride salt adsorbs moisture; pre-drying at 60 °C under vacuum until loss on drying returns to ≤0.5% is required before dry blending. Open processing in high-humidity rooms should be limited to 4 h to avoid moisture uptake above 1.0% and subsequent granule sticking on tablet punches.
Thermal stress during drying should not exceed 60 °C for aqueous granulations. Higher drying temperatures can increase total related substances and shift surface pH. Process experience indicates that tray drying at 65 °C for more than 8 h can produce color change from white to pale yellow and increase total impurities beyond the release limit. Fluid-bed drying with inlet air temperature not exceeding 60 °C and product temperature not exceeding 45 °C is preferred for granules intended for tablet compression or premix filling.
Injectable-grade sarafloxacin hydrochloride is not identical to oral powder grade. The parenteral designation requires reduced bioburden, controlled endotoxin, low particle counts, and full elemental impurity confirmation for the parenteral route. Aqueous solutions for injection should be prepared in a Grade C or Grade D environment with terminal aseptic filtration into depyrogenated vials. Filter compatibility trials should compare PVDF and PES membranes at 0.22 µm; nylon membranes may produce assay loss due to adsorption. The solution pH is maintained at 3.5 to 4.5 to preserve solubility and reduce injection-site irritation. Buffering agents should not include phosphate above 20 mmol/L if calcium or magnesium from the vial elastomer can leach, because insoluble quinolone-metal complexes may form. Published data for this specific configuration is limited; compatibility studies should be performed on the finished container-closure system.
Terminal moist-heat sterilization of sarafloxacin hydrochloride aqueous solutions has limited published stability data. Aseptic filtration is therefore the preferred sterilizing operation for injectable solutions unless the finished product dossier demonstrates adequate stability under thermal sterilization. If terminal sterilization is pursued, hold-time studies at 121 °C for 15 min must confirm assay retention and impurity profile. The injectable product should be protected from light during filling, because photodegradation can occur in clear glass under visible light exposure exceeding 1000 lux.
Relative to enrofloxacin, the N-1 substituent is a 4-fluorophenyl group rather than a cyclopropyl group. This substitution increases the base molecular mass from 359.39 g/mol for enrofloxacin to 385.36 g/mol for sarafloxacin and alters partition behavior. Enrofloxacin undergoes hepatic de-ethylation to ciprofloxacin in many target species; sarafloxacin is not a metabolic precursor of ciprofloxacin. Difloxacin hydrochloride, also a veterinary fluoroquinolone, shares the 4-fluorophenyl N-1 substituent but carries a 4-methylpiperazin-1-yl group at C-7, which further modifies distribution and elimination. The structural differences do not establish therapeutic equivalence; dose selection for each species must follow the approved label or species-specific pharmacokinetic data. Published direct comparative efficacy data for sarafloxacin, enrofloxacin, and difloxacin across all formulations is limited; therefore, interchange is not recommended without bridging safety and residue depletion data.
| API | CAS registry | Base molecular mass | N-1 substituent | C-7 substituent |
|---|---|---|---|---|
| Sarafloxacin hydrochloride | 91296-87-6 | 385.36 g/mol | 4-fluorophenyl | piperazin-1-yl |
| Enrofloxacin | 93106-60-6 | 359.39 g/mol | cyclopropyl | piperazin-1-yl |
| Difloxacin hydrochloride | 91296-86-5 | 399.39 g/mol | 4-fluorophenyl | 4-methylpiperazin-1-yl |
The micronized grade of sarafloxacin hydrochloride is intended for water-soluble powders and premixes. In ribbon blenders and double-cone blenders, micronized fluoroquinolones can segregate when the excipient bulk density differs by more than 0.3 g/cm³. Wet granulation with aqueous binder solutions containing povidone or starch at 3% w/w to 5% w/w binder solids locks the API into granules and reduces segregation. Drying temperature should not exceed 60 °C for aqueous granules because higher temperatures can increase related substances. Final blend uniformity is tested by sampling 10 locations and comparing assay relative standard deviation; acceptance is not more than 5.0% RSD. For dry premixes, the carrier should be selected for neutral pH and low ash; attapulgite, bentonite, and kaolin may bind fluoroquinolones and are not suitable unless a bioequivalence study demonstrates adequate release.
In tablet and capsule manufacture, the standard crystalline grade is preferred. Direct compression may be used for low-dose formulations, but process experience indicates that sarafloxacin hydrochloride is cohesive and may adhere to upper punch faces when lubricant magnesium stearate exceeds 0.75% w/w. Wet granulation with lactose monohydrate, microcrystalline cellulose, and crospovidone provides acceptable tablet hardness from 5 kP to 12 kP and disintegration below 15 min in 0.1 M hydrochloric acid. Capsule blends should be compacted or granulated to improve flow; direct-filled capsules may exhibit weight variability above 5% RSD if the micronized grade is used without densification. Roller compaction with sieve granulation at 1.0 mm to 1.5 mm retains polymorphic identity and avoids solvent exposure. Dissolution testing for finished tablets and capsules uses compendial apparatus under USP <711>; acceptance criteria are established in the approved veterinary product dossier.
Premix processing in mineral-dense feed matrices requires attention to chelation and pH. Calcium carbonate, magnesium oxide, and ferrous sulfate should not be co-mixed with sarafloxacin hydrochloride unless the finished premix is evaluated for drug release. High-shear mixing of premixes should be limited to 3 min after API addition to avoid excessive electrostatic segregation. Sampling of medicated feed should follow VICH quality guidelines; assay variability in finished feed should not exceed 10% RSD for routine manufacturing. The API should not be dry-blended with sodium bicarbonate, sodium citrate dihydrate, or strongly alkaline amine excipients, because localized pH elevation can precipitate the free base and reduce uniformity. Incompatibility with aluminum hydroxide, magnesium trisilicate, and calcium phosphate should be evaluated by content uniformity and dissolution testing in the target formulation.
Sarafloxacin Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions should be used only in veterinary applications under applicable regulatory approval. Handling personnel should wear respiratory protection and impervious gloves because fluoroquinolone dust may cause phototoxic skin reactions. Spills are collected by HEPA-filtered vacuum or wet wiping; dry sweeping is not used because of dust exposure. The API is not released for human use; the difference between veterinary and human product requires separate supply-chain segregation and cleaning validation in multi-product facilities. The operational boundary for the API includes avoidance of co-milling with alkaline excipients such as sodium bicarbonate or amine-containing binders, which may raise local pH and induce free-base precipitation or chemical hydrolysis. When formulation questions arise beyond the available technical data, the supplier certificate of analysis and a qualified finished-product development report remain the controlling documents.
