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Coumaphos Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions

    • Product Name: Coumaphos Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions
    • Factroy Site: Yudu County, Ganzhou, Jiangxi, China
    • Price Inquiry: sales10@sinochem-nanjing.com
    • Manufacturer: Ascent Petrochem Holdings Co., Limited
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    Specifications
    HS Code 446879
    Productname Coumaphos Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions
    Commonname Coumaphos
    Chemicalname O,O-diethyl O-(3-chloro-4-methyl-2-oxo-2H-chromen-7-yl) phosphorothioate
    Casnumber 56-72-4
    Molecularformula C14H16ClO5PS
    Molecularweight 362.77 g/mol
    Appearance White to off-white crystalline powder
    Odor Mild, characteristic
    Meltingpoint 91 °C
    Solubilityinwater Slightly soluble (1.5 mg/L at 20 °C)
    Solubilityinorganicsolvents Soluble in acetone, chloroform, ethanol, and other organic solvents
    Drugclass Organophosphate acaricide/insecticide
    Mechanismofaction Inhibits acetylcholinesterase
    Veterinaryindications Control of ticks, lice, horn flies, mange mites, and other ectoparasites on livestock; also used against Varroa mites in honey bees
    Targetspecies Cattle, sheep, goats, horses, swine, dogs, honey bees
    Dosageforms Tablets, injections, capsules, powders, granules, premix, solutions
    Routeofadministration Topical, oral, pour-on, spray, dip, dust, or injectable depending on the formulation
    Purity ≥ 98% (veterinary grade)
    Storageconditions Store in a cool, dry, well-ventilated area in tightly closed containers away from light and moisture
    Stability Stable under normal storage conditions; hydrolyzes in alkaline media
    Hazardclassification WHO Class Ib (highly hazardous)
    Toxicity Highly toxic; cholinesterase inhibitor; may be fatal if swallowed, inhaled, or absorbed through the skin
    Antidote Atropine sulfate and pralidoxime (2-PAM) as directed by a veterinarian
    Withdrawalperiod Varies by species and formulation; consult product labeling
    Regulatorystatus Veterinary prescription product in many jurisdictions
    Shelflife 24 months when stored properly
    Environmentaltoxicity Highly toxic to bees, fish, and aquatic invertebrates
    Chemicalfamily Organophosphate
    Usecategory Ectoparasiticide
    Apiform Powder
    Grade Veterinary grade

    As an accredited Coumaphos 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 & Storage
    Packing Coumaphos Veterinary Grade API supplied in 1 kg, 5 kg, and 25 kg double LDPE-lined, UN-approved fiber drums, sealed and labeled.
    Container Loading (20′ FCL) 20′ FCL: Coumaphos Veterinary Grade API for tablets, injections, capsules, powders, granules, premix, solutions; palletized, moisture-protected, labeled, and sealed for export.
    Shipping Coumaphos Veterinary Grade API for Tablets/Injections/Capsules/Powders/Granules/Premix/Solutions is shipped as a toxic organophosphate hazardous material in sealed, leakproof, UN-approved packaging. Label with correct UN number, hazard class, packing group, and veterinary-use warnings. Keep dry, cool, segregated from food/feed; follow DOT/IATA/IMDG rules.
    Storage Store Coumaphos Veterinary Grade API in a cool, dry, well-ventilated, secure area, away from direct sunlight, heat, ignition sources, food, feed, and incompatible materials. Keep containers tightly closed, moisture-protected, and clearly labeled. Protect solutions and injections from freezing. For tablets, capsules, powders, granules, and premix, follow manufacturer’s labeled storage conditions, recommended temperature, local regulations, and restricted-access handling.
    Shelf Life Coumaphos Veterinary Grade API shelf life varies by formulation; typically 2–3 years when stored sealed, cool, dry, dark, per manufacturer.
    Application of Coumaphos Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions

    Cattle plunge-dip vat operations receiving heavy Rhipicephalus microplus, Psoroptes and lice challenge are the primary downstream route for veterinary-grade coumaphos. The API is not introduced as a technical material directly into the dilute bath; it is converted first into a water-dispersible wettable powder or a flowable suspension concentrate. A field-charge concentration of 2.5–5.0 kg of a 25% WP per 1,000 L of water produces an active concentration of 0.625–1.25 g AI/L, with the upper band reserved for multi-host tick eradication protocols. Industry compliance for food-producing species is linked to national residue control and, where beef is exported, to Codex Alimentarius CXL schedules and importer-specific MRL lists; operators referencing U.S. tolerances confirm current status under 40 CFR 180.189 before shipment. Downstream manufacture begins with air-jet milling of technical coumaphos to a median particle size of 5–12 µm; if the technical powder is stored at relative humidity above 60%, pre-drying at 45–50°C is used to prevent mill screen blinding and particle agglomeration. The milled active is blended with sodium lignosulfonate dispersant at 4–8% w/w, precipitated silica anti-caking agent at 1–3% w/w and a nonionic wetting agent at 1–2% w/w, then high-shear mixed and vibratory sieved through a 150 µm mesh. The concentrate is packaged as a 25% WP, 42% aqueous flowable or 50% WP for end-user vat charging. In the field, the dilute suspension is recirculated through a centrifugal pump with a minimum flow of 1,000 L/min per 10,000 L vat to maintain homogeneity; pH is held between 6.0 and 7.5 because alkaline hydrolysis of the phosphorothioate ester accelerates above pH 8.0. Hypochlorite-based disinfectants and strong alkaline cleaners are incompatible with the bath and must be excluded because oxidative sulfoxidation reduces active content and forms unregistered degradation residues. Terminal finished product classes are plunge-dip concentrates, not tablets or injectable presentations; any use in those dosage forms would require an entirely different toxicological and residue assessment.

    Does Replenishment Rate Control Slurry Settling in Sheep Plunge Dips?

    Psoroptic mange control in sheep depends on maintaining a near-constant coumaphos concentration and keeping insoluble carrier particles suspended in the long, narrow dip bath because settled solids form a friction layer that reduces fleece contact. The initial charge for a 50% WP formulation is 1.0 kg per 1,000 L of water, producing 0.5 g AI/L; replenishment after every 200–250 sheep uses 0.4–0.5 kg per 1,000 L of added water when the tank is topped back to volume. The manufacturing route for this product type uses a 50:50 blend of technical coumaphos on an insoluble kaolin or calcium silicate carrier, with an anionic naphthalene sulfonate dispersant at 3–6% w/w to achieve CIPAC suspensibility above 70% after 30 min in standard hard water. Compliance standards for sheep dip antiparasitics include OECD 404 for dermal irritation and OECD 402 for acute dermal toxicity to support hazard classification, while any marketed formulation in the European Union must satisfy the registration dossier requirements under Regulation (EU) 2019/6. End users prepare a slurry in a separate pre-mix vessel with a high-shear rotor-stator mixer running at 1,000–1,500 rpm before transferring it into the main bath; without this pre-dispersion step the wettable powder forms gummy aggregates that blind recirculation screens and cause severe tank concentration gradients. The finished product is a bulk bagged 50% WP for plunge dipping, and the industrial boundary excludes injection or capsule manufacturing because the active is not distributed systemically after topical administration but acts by direct contact with the mite cuticle.

    Spray-race installations applying a high-volume, low-pressure wash to cattle are configured for rapid throughput and require a suspension that remains non-foaming under repeated pump shear. The working solution is prepared by adding 4.0 kg of a 25% WP or 2.4 kg of a 42% flowable per 1,000 L of water to give 1.0 g AI/L, although low-tick-pressure labels in some jurisdictions reduce the charged active to 0.6 g/L. Industry compliance is driven by operator-exposure benchmarks and protective-clothing standards such as ISO 27065:2017 for pesticide spray protective ensembles, while residue clearance in bovine products follows the same 40 CFR 180.189 tolerance framework as vat applications. The downstream manufacturing process converts technical coumaphos into a suspension concentrate by wet milling a 40–45% AI slurry in a horizontal bead mill charged with 0.8–1.2 mm zirconium oxide beads until the D90 particle size is below 20 µm; an ethoxylated tridecyl alcohol wetter at 2–4% w/w lowers air entrainment compared with alkylbenzene sulfonate systems that produce foam in high-velocity spray-race sumps. The terminal product is a 25% WP or 42% flowable spray-race concentrate that is metered through a venturi injector into a holding tank. Spray-race applicators deliver 1.5–2 L of ready-to-use suspension per adult bovine through nozzles operating at 2–4 bar, and the suspension is screened through 50-mesh inline filters to protect nozzle tips from carrier fines. The formulation type is exclusively topical; oral dosage forms are absent from registered spray-race use and would require a different systemic absorption study package.

    When Polyvinyl Chloride Ear Tag Matrices Are Loaded with Coumaphos

    Where cattle ear tags are manufactured with coumaphos as the contact toxicant, the API is compounded into a plasticized vinyl matrix that must retain sufficient migration of the active to the tag surface for release onto the animal's hair coat. Published data for specific commercial tag configurations is limited; the production benchmark used by compounders is a coumaphos loading of 10–20% w/w in a PVC resin system containing 30–40% w/w di-2-ethylhexyl phthalate or a phthalate-free citric ester plasticizer, with 1–3% w/w calcium-zinc stabilizer and 0.5–1.5% w/w epoxidized soybean oil co-stabilizer. The mechanical and rheological control standards for continuous extrusion are ASTM D638-14 for tensile yield and elongation at break, and ISO 1133-1:2022 for melt mass-flow rate, with a target MFR of 12–25 g/10 min at 190°C under 10 kg load. The compounding route uses a high-intensity mixer pre-blend at 70–80°C to absorb liquid plasticizer into the PVC, followed by twin-screw extrusion at an L/D ratio of 32:1 to 36:1, with melt temperature controlled at 165–175°C because higher temperatures trigger exothermic decomposition of coumaphos and rapid darkening. The melt is strand-pelletized, then injection-molded into ear tag cavities on machines with clamp force of 250–400 metric tons; molded tags are die-cut and assembled with a locking backing plate. The terminal product is a two-tag per animal slow-release device that delivers contact acaricide over a 12–20 week season, and residual release is confirmed by in vitro elution rather than by human pharmaceutical dissolution pharmacopoeia. Formulation as tablets or injectable doses is not a recognized downstream route for this active in ear-tag matrices.

    Backline Pour-On Solvent Systems and Dermal Spreading Behaviour

    Backline pour-ons containing coumaphos are produced as true solutions or microemulsifiable concentrates, not as WP or SC, because the product must spread from the whithers along the backline and onto the flanks without run-off. A typical production formula places the API at 1–3% w/w in a mixed solvent system of 60–80% w/w mineral oil or isopropyl myristate, with a slow-evaporating aliphatic hydrocarbon and a nonionic spreading agent at 5–15% w/w to reduce surface tension below 30 mN/m. The compliance dossier for such topical products includes OECD 402 for acute dermal toxicity, OECD 404 for dermal irritation, and closed-cup flash point classification under ASTM D7094 for flammable solvent risk. Manufacturing dissolves technical coumaphos in the solvent blend under nitrogen blanketing at 35–45°C in a glass-lined or stainless-steel vessel, passes the liquid through a 1.0 µm polypropylene cartridge filter, and then fills it into 500 mL or 1 L high-density polyethylene bottles. Dermal spreading is governed by the solvent evaporation envelope; if the flash-off is too fast, the active crystallizes as a white residue on the hair shaft and does not fully disperse into the sebaceous film. The terminal product is a ready-to-use pour-on for topical administration by pour-on gun or syringe, and the drug is presented as a liquid solution rather than a powder or granule. The industrial boundary is set by the organophosphate's acute toxicity: operations at concentrations above 3% w/w require dedicated closed filling lines and skin-contact monitoring protocols.

    Particle Adhesion Determines Retention of Premise Dust in Housing Litter

    Premise dust formulations containing coumaphos are directed at mite and lice populations in poultry housing and cattle bedded environments, where the active must adhere to litter particles and cracks rather than remain airborne. The formulation addition ratio is 1% or 5% coumaphos on a carrier of kaolin, talc, or diatomaceous earth, with light mineral oil added at 0.5–1.5% w/w to suppress dust drift while maintaining flow through mechanical dusters. The downstream production process dry-blends technical coumaphos with the carrier in a ribbon mixer at 15–20 rpm for 30–45 min, then passes through a 75 µm screen before bagging in 10 kg valve-pack bags; the product is applied at 10–20 g/m² to litter and nest box surfaces according to label. Regulatory compliance is tied to national pesticide registration pathways and any imported-product tolerances in 40 CFR 180.189 where food-producing premises are treated, while user exposure follows the same ISO 27065 protective-clothing framework plus OECD 403 acute inhalation toxicity data to justify label ventilation statements. The terminal product is a ready-to-use dusting powder for mechanical application, not a premix for feed incorporation; any downstream claim involving feed-through therapy would be outside the registered indication. Particle adhesion testing with a cascade impactor or settleable dust chamber is used at the formulation stage because particles below 10 µm remain suspended too long and create inhalation hazard, while particles above 150 µm bounce out of litter pockets and fail to contact resting mites. The industrial boundary for this application is set by the physical performance of the carrier system rather than by coumaphos potency, because the dusting powder's efficacy depends on surface coverage uniformity and residual persistence in the bedding environment.

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    Certification & Compliance
    More Introduction

    Coumaphos Veterinary Grade API is the unformulated active substance O-(3-chloro-4-methyl-2-oxo-2H-1-benzopyran-7-yl) O,O-diethyl phosphorothioate, CAS 56-72-4. The compound is an organophosphate acetylcholinesterase inhibitor used for non-systemic ectoparasite control in veterinary medicine. Commercial grade designations for the API are manufacturer-specific and commonly encode particle-size distribution, residual solvent profile, and packaging configuration; no harmonized pharmacopeial model number exists. A milled grade for dry premix blending may be supplied with a D90 of approximately 100 µm, whereas a micronized grade for suspension concentrates may carry a D90 of 25 µm or lower. These numerical values are not compendial acceptance limits and must be verified against the batch certificate of analysis.

    Physicochemical identity and characterization data for Coumaphos Veterinary Grade API
    PropertyValue or descriptorTypical test method or standard
    CAS number56-72-4Chemical Abstracts Service
    IUPAC nameO-(3-chloro-4-methyl-2-oxo-2H-1-benzopyran-7-yl) O,O-diethyl phosphorothioate—
    Molecular formulaC14H16ClO5PS—
    Molecular weight362.77 g/mol—
    Melting point91–92 °COECD TG 102, Ph. Eur. 2.2.14
    Water solubility1.5 mg/L at 20 °COECD TG 105
    Octanol-water partition coefficientlog Kow 4.13OECD TG 117
    Vapor pressure0.013 mPa at 20 °COECD TG 104
    Appearancewhite to off-white crystalline powdervisual inspection

    The coumarin chromophore confers strong ultraviolet absorbance, permitting HPLC detection without derivatization. This characteristic distinguishes coumaphos from organophosphate active substances that lack an aromatic coumarin moiety and require gas chromatography with flame photometric detection or mass-selective detection for trace analysis.

    What specification and impurity-control framework applies to a multi-dosage-form API?

    Because a dedicated monograph for coumaphos is not harmonized across the major veterinary pharmacopeias, release specifications are typically assembled from the manufacturer’s validated HPLC method, ICH Q3A, ICH Q3C, ICH Q3D, and VICH GL18. A certificate of analysis should include appearance, identification by infrared spectroscopy and retention-time match, assay on the dried basis, related substances, loss on drying, residue on ignition, elemental impurities, residual solvents, and particle-size distribution where solid dosage forms are intended. Assay by HPLC is commonly requested as not less than 98.0% on the anhydrous, solvent-free basis; total related substances are frequently controlled at not more than 2.0%; loss on drying not more than 0.5%; and sulfated ash not more than 0.1%. These are common supplier defaults for veterinary organophosphate active substances, not harmonized pharmacopeial acceptance limits; end users must validate acceptance criteria against the intended dosage form and target species. Residual solvent control should follow ICH Q3C classes; elemental impurity control should follow ICH Q3D rather than a total heavy metals test alone. The toxicologically relevant oxygen analogue, coumaphos oxon, and the hydrolytic cleavage product 3-chloro-4-methyl-7-hydroxycoumarin should be separated and quantified by HPLC because both may affect potency and safety. Method validation should follow ICH Q2(R1) or an equivalent VICH validation guideline.

    Particle-size distribution is not a single-value specification. For tablet or capsule blends, a D90 of 100 µm may be acceptable for direct compression if flow and segregation risks are addressed; for aqueous suspension concentrates, D90 should be lower, typically 25 µm or less, to reduce sedimentation and improve content uniformity. Particle-size methods should be stated in the certificate of analysis as laser diffraction under ISO 13320 or analytical sieving under Ph. Eur. 2.9.38.

    Across the seven listed dosage-form routes, coumaphos presents two controlling constraints: low water solubility and a narrow therapeutic index. Dry solid forms are technically preparable, but approved oral tablet and capsule products are not established in most jurisdictions. For investigational tablets or capsules, the API is best handled as a milled powder with controlled particle size. Direct compression blends may require moisture-proof packaging and desiccant; microcrystalline cellulose and lactose monohydrate are compatible diluents, but amine-functional excipients should be avoided because alkaline microenvironments accelerate hydrolysis. Wet granulation water or binder solution should be maintained at pH 5.0–6.5; high-shear granulators with jacketed bowl cooling below 45 °C prevent heat-mediated cohesion and particle-size instability near the melting point. The resulting premix should be tested for blend uniformity by Ph. Eur. 2.9.40 or USP <905>, and powder flow should be characterized by USP <1174> when direct compression is attempted.

    Parenteral solution or suspension dosage forms are constrained by the compound’s water solubility of approximately 1.5 mg/L at 20 °C. Achieving therapeutic concentrations in an aqueous injection would require substantial co-solvent fractions, with risk of precipitation on dilution and injection-site irritation. Because coumaphos acts by contact with surface ectoparasites rather than by systemic distribution, injectable administration is generally not developed. Published data for coumaphos injectable configurations are limited; any injectable development should be preceded by target animal safety studies under VICH GL43 and residue depletion studies under VICH GL48.

    Non-aqueous solutions are feasible because coumaphos dissolves readily in acetone, chloroform, and ethyl acetate. These solvents are not suitable for direct injection but can serve as manufacturing solvents for pour-on products or emulsifiable concentrates. Aqueous dip solutions should be prepared from emulsifiable concentrates or wettable powders, with pH maintained below 8 to reduce alkaline hydrolysis. Suspensions require particle-size control to prevent sediment caking; D90 below 25 µm is typical for aqueous suspension concentrates, with viscosity-modifying suspending agents added to maintain redispersibility.

    Approved veterinary uses of coumaphos center on contact ectoparasiticide applications. In cattle, coumaphos is used in plunge dip and spray formulations for control of Rhipicephalus microplus, Amblyomma spp., lice, and mite populations. In sheep, coumaphos has been employed against psoroptic mange mites, although label availability depends on national marketing authorization. In honeybee colonies, coumaphos-impregnated polymer strips are used for control of Varroa destructor and Aethina tumida. The API for these strips must be dissolved and incorporated into a polymer matrix; release rate is controlled by plasticizer level, strip thickness, and polymer type. Manufacturers should confirm strip content uniformity and residual solvent levels prior to hive placement. Removal during honey flow is a label restriction in many jurisdictions to prevent honey residue violations.

    Comparative differentiation against other organophosphate and non-organophosphate ectoparasiticides

    Coumaphos differs from trichlorfon in systemic potential and solvent partitioning. Trichlorfon is a water-soluble organophosphate prodrug that converts to dichlorvos and can be used in oral or parenteral formulations in some species; coumaphos is non-systemic and lipophilic, making direct substitution inappropriate in high-water-content injection or oral solution applications. Compared with phosmet, coumaphos exhibits lower vapor pressure and greater retention in lipid-rich hair coat and polymer matrices; however, both share a common cholinesterase inhibition mode and should not be rotated as if they had distinct target sites. Against diazinon, coumaphos has higher log Kow and lower water solubility, which reduces wash-off from hair coat but increases sediment partitioning in aquatic systems; environmental risk assessment for dip vat discharge should follow national or OECD guidance.

    Compared with pyrethroids and macrocyclic lactones, coumaphos belongs to a different mode-of-action group. Macrocyclic lactones such as ivermectin act on glutamate-gated chloride channels and are systemic; coumaphos does not provide systemic control of endoparasites. Amitraz is a formamidine with a different neuropharmacological target; cross-resistance is not automatic, but dual-resistance populations in Rhipicephalus microplus have been reported in published acaricide resistance surveillance. Any claim of resistance-breaking activity should be supported by FAO or polymerase chain reaction-based bioassay data, not by product class alone.

    Qualitative differentiation of coumaphos from selected veterinary ectoparasiticides
    Comparative propertyCoumaphosTrichlorfonDiazinonAmitraz
    Chemical classorganophosphateorganophosphate prodrugorganophosphateformamidine
    Systemic activitynon-systemicsystemicnon-systemictopical acaricide
    Water solubilitylow, 1.5 mg/Lhighlow to moderatevery low
    Primary veterinary presentationdip, spray, pour-on, hive striporal/parenteral solution, pour-ondip, spray, ear tagdip, spray, collar
    Hydrolytic limitationalkaline hydrolysis, photolysisconversion to dichlorvos under alkaline conditionsalkaline hydrolysisoxidation, high pH

    Handling and formulation incompatibilities are governed by the phosphorothioate ester bond. Alkaline hydrolysis is rapid at pH above 8; therefore, dip vat pH should be monitored and adjusted with non-alkaline buffers. The API is susceptible to photolysis, and bulk containers should be opaque or stored in the dark. Contact with strong oxidizers, acid chlorides, or amine-functional excipients should be avoided. Personnel handling the API must use nitrile gloves and dust extraction because organophosphate dust can rapidly inhibit plasma cholinesterase; medical surveillance should include red blood cell and plasma cholinesterase baselines before work starts. These controls are operational boundaries required to maintain API integrity and worker safety.

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