| HS Code | 623755 |
| Chemicalname | Carbetocin (deamino-1-monocarba-2-O-methyltyrosine-4-threonine-8-ornithine-oxytocin) |
| Casnumber | 37025-55-1 |
| Molecularformula | C45H69N11O12S |
| Molecularweight | 988.18 g/mol |
| Appearance | White to off-white lyophilized or crystalline powder |
| Solubility | Freely soluble in water; sparingly soluble in ethanol; practically insoluble in ether |
| Meltingpoint | No sharp melting point; decomposes above 200°C |
| Purity | ≥98.0% by HPLC |
| Storageconditions | Store at 2-8°C, protected from light and moisture, in airtight, light-resistant container |
| Shelflife | 24 months from date of manufacture under recommended storage |
| Pharmacologicalaction | Long-acting oxytocin receptor agonist; induces uterine contraction and facilitates milk ejection |
| Veterinaryindications | Post-partum uterine involution, uterine atony, retained placenta, and obstetric management in animals |
| Dosageformcompatibility | Suitable for tablets, injections, capsules, powders, granules, premixes, and solutions |
As an accredited Carbetocin 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 | Carbetocin Veterinary Grade API supplied in sealed, light-protected containers with desiccant. Net weight 1 kg per drum, suitable for formulations. |
| Container Loading (20′ FCL) | A 20′ FCL shipment of temperature-controlled Carbetocin veterinary API, palletized and moisture-protected, safely packed for tablet, injection, capsule, and powder production. |
| Shipping | Carbetocin Veterinary Grade API ships in sealed, light-resistant containers under temperature-controlled conditions to preserve potency and stability. All shipments include certified documentation, SDS, and compliance with international regulations. Secure, tamper-evident packaging ensures safe delivery worldwide for tablet, injection, capsule, powder, granule, premix, or solution formulations. |
| Storage | Store Carbetocin Veterinary Grade API in a tightly sealed, light-resistant container under cool, dry conditions, ideally between 2–8°C. Protect from moisture, heat, and direct sunlight. Keep away from incompatible substances. Use clean equipment during handling. Do not store after expiration date. For manufacturing use only; not for direct veterinary administration. |
| Shelf Life | Shelf life: 24 months from manufacture when stored properly in sealed containers, protected from light and moisture. |
The downstream application scope for carbetocin veterinary-grade API is restricted to sterile injectable and lyophilised sterile preparations. Oral solid dosage forms such as tablets and capsules, granules, and feed or drinking-water premix are excluded from this application section because published pharmacokinetic data in target veterinary species do not demonstrate sufficient oral bioavailability of the modified nonapeptide; gastrointestinal proteolysis and poor mucosal permeability prevent a defensible formulation ratio. The following five downstream tracks are therefore limited to documented parenteral routes.
Farrowing management in commercial sow units uses carbetocin injectable solution at a finished concentration of 70 µg/mL, equivalent to 0.007% w/v active base, for the treatment of uterine inertia; the API is dissolved in Water for Injection and maintained in an acidic pH range because peptide deamidation accelerates above pH 5.0. Compliance for the finished injectable is governed by EU GMP Part II for API manufacture, VICH GL18 residual solvent limits, ICH Q3D(R2) elemental impurities, and sterility assurance under Ph. Eur. 2.6.1 or USP <71>. Downstream production on a sterile filling line requires aseptic filtration through a 0.22 µm PVDF or PES membrane because terminal steam sterilisation is not used for this heat-sensitive peptide; the solution is filled into Type I borosilicate vials under nitrogen overlay to hold dissolved oxygen below 1.0 mg/L and to reduce oxidative degradation. Equipment qualification includes filter integrity testing before and after filtration, extractables profiling under USP <1663>, and visual inspection for subvisible particulates per Ph. Eur. 2.9.19 or USP <788>. Adsorption loss to silicone tubing and stopper elastomers is pH- and concentration-dependent and must be quantified during process validation. Terminal product types are ready-to-use multidose vials of 10 mL, 20 mL, and 50 mL for intramuscular or intravenous administration to sows.
Where registered for cattle, the commercial carbetocin injection is prepared as an aqueous solution at 0.07 mg/mL, corresponding to 0.007% w/v, and a single 1 mL dose delivers 70 µg per animal by intramuscular or intravenous injection. Industry compliance for a multidose injectable in this application includes antimicrobial preservative efficacy testing under Ph. Eur. 5.1.3 or USP <51>, bacterial endotoxin limits under Ph. Eur. 2.6.14 or USP <85>, and container closure integrity under USP <1207>. The downstream manufacturing process differs from the sow presentation principally in the use of a preservative—chlorobutanol at pharmacopoeial concentrations between 0.25% and 0.5% w/v where a multidose presentation is required—and in the need to validate preservative partitioning into halobutyl rubber stoppers, because partitioning can reduce both preservative efficacy and peptide assay after long-term contact. Rotary piston filling with ceramic pistons is preferred over peristaltic tubing to limit shear-induced aggregation, and the filler speed is qualified to maintain subvisible particle counts below pharmacopoeial acceptance limits. Cold-chain distribution and storage at 2 °C to 8 °C with continuous temperature logging is required; freeze-thaw cycles are avoided because ice-crystal-induced aggregation reduces assay and increases particulate burden. Terminal products are 50 mL and 100 mL multidose vials of 70 µg/mL solution used in postpartum dairy cattle for retained placenta or uterine atony.
| Control point | Standard designation | Measurement condition / acceptance principle |
|---|---|---|
| API manufacture and process validation | ICH Q7 / EU GMP Part II | Documented process validation for peptide purity by stability-indicating HPLC |
| Residual solvents | VICH GL18 / ICH Q3C | Class 2 and Class 3 solvent limits applied to bulk solution and excipients |
| Elemental impurities | ICH Q3D(R2) | PDE-based control for parenteral route of administration |
| Sterility of finished injectable | Ph. Eur. 2.6.1 / USP <71> | Membrane filtration or aseptic fill validation with media fills |
| Bacterial endotoxins | Ph. Eur. 2.6.14 / USP <85> | Endotoxin limit derived from maximum dose per animal |
| Container closure integrity | USP <1207> | Deterministic or probabilistic leak test method validated to package configuration |
| Subvisible particulate matter in injectable | Ph. Eur. 2.9.19 / USP <788> | Light obscuration and microscopic count after reconstitution or filling |
Lyophilised carbetocin powder for veterinary hospital and ambulatory compounding is produced from a bulk solution containing carbetocin at 0.1 mg/mL to 0.5 mg/mL and mannitol or trehalose as a bulking agent at 2% to 5% w/v; the API-to-bulking agent ratio is therefore between 1:40 and 1:500, depending on the final vial strength. Published data for carbetocin-specific lyophilisation cycle parameters is limited, so cycle design follows general peptide freeze-drying practice: primary drying at a shelf temperature of -30 °C to -20 °C with chamber pressure 0.1 mbar to 0.3 mbar, followed by secondary drying at 20 °C to 30 °C until residual moisture by Ph. Eur. 2.5.12 or USP <921> method Ic is not more than 3.0% water. Collapse of the lyophilised cake occurs when product temperature exceeds the glass transition temperature of the amorphous excipient phase; for mannitol-containing formulations, crystallisation of mannitol during freezing must be controlled because incomplete crystallisation can result in vial breakage or cake collapse. Compliance requires subvisible particulate matter testing after reconstitution under Ph. Eur. 2.9.19 and USP <788>, and closure integrity under USP <1207>. Terminal product types are single-dose vials of 70 µg, 100 µg, and 200 µg carbetocin, reconstituted with 1 mL or 2 mL sterile Water for Injection.
Bulk carbetocin solution used as an intermediate for licensed finished injectable manufacture is commonly prepared at 0.5 mg/mL or 1.0 mg/mL, and an antioxidant such as L-methionine may be added at 0.05% to 0.2% w/v only where forced degradation studies demonstrate oxidation in the peptide; the antioxidant-to-API ratio is therefore variable and must be justified by stability-indicating HPLC peak purity. Industry standards for this manufacturing step are ICH Q7 / EU GMP Part II for API handling, VICH GL18 for residual solvents, and ICH Q1A(R2) for stability protocols. The production process in a 316L stainless-steel jacketed vessel includes nitrogen sparging through a sintered sparger to maintain dissolved oxygen below 1.0 mg/L, and the solution is transferred through 0.45 µm pre-filtration followed by 0.22 µm sterilising-grade filtration into gamma-irradiated single-use bags or Type I glass bottles. Adsorption to filter membranes and silicone tubing is pH-dependent; recovery loss is evaluated across the range pH 3.5 to pH 5.0, and a rinse volume plus in-process assay after filtration is required. Terminal product types are sterile bulk concentrate packages of 100 mL, 500 mL, and 1 L supplied to finished-dose manufacturers under controlled 2 °C to 8 °C storage.
Veterinary compounding pharmacies preparing carbetocin injections from lyophilised powder or bulk concentrate generally dilute to final concentrations of 10 µg/mL, 35 µg/mL, or 70 µg/mL in sterile sodium chloride 0.9% or Water for Injection, with active ingredient addition at 0.001% to 0.007% w/v under ISO 5 laminar airflow. Compliance follows USP <797> principles for compounded sterile preparations, USP <85> bacterial endotoxin limits, and, in the United States, extralabel animal use must satisfy 21 CFR 530 under AMDUCA. The production process involves reconstitution of the powder with a sterile diluent using gentle rotation rather than vigorous shaking to avoid aggregation, followed by withdrawal through a 5 µm filter needle into sterile amber glass vials or polypropylene syringes. API powder used in compounding is sieved through a 100 µm mesh where supplied as powder to ensure complete dissolution, and batch-to-batch moisture above 1.0% requires desiccated storage at 2 °C to 8 °C before weighing. Because these are preservative-free preparations, terminal products are single-dose syringes or vials labelled with beyond-use dates not exceeding 24 h at room temperature or 72 h under refrigeration unless site-specific stability data supports longer storage.
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Carbetocin Veterinary Grade API is the acetate salt of 1-deamino-1-carba-2-O-methyltyrosine-oxytocin, registered under CAS 37025-55-1. The free-base molecular formula is C45H69N11O12S, corresponding to an anhydrous molecular weight of 988.2 g/mol. The veterinary-grade material is released as a white to off-white lyophilized powder or spray-dried powder and is controlled for formulation into tablets, injections, capsules, powders, granules, premix, and solutions. The structural difference from native oxytocin is the replacement of one cystine sulfur atom by a methylene bridge, producing a thioether-stabilized cyclic peptide that retains oxytocin-receptor agonist activity while reducing disulfide-exchange inactivation in aqueous formulation environments. Release documentation for the veterinary grade includes reversed-phase HPLC assay, related substance profiling, residual solvent testing under VICH GL18/ICH Q3C, and elemental impurity screening under VICH GL19/ICH Q3D; bacterial endotoxin and bioburden data are added when the API is designated for injectable manufacture.
Native oxytocin is degraded rapidly by aminopeptidases and undergoes disulfide-exchange inactivation; this shortens the interval of uterine contractility and can increase the number of injections needed during farrowing and postpartum management in swine and cattle. On large sow units, repeated handling of farrowing sows is a recognized labour bottleneck, particularly when retained placenta or uterine atony is diagnosed. Carbetocin is designed to resist aminopeptidase cleavage and disulfide-exchange scrambling because the N-terminus is deaminated and the remaining thioether linkage is not reducible under physiological redox conditions. Published veterinary field data report a prolonged uterotonic response from carbetocin compared with oxytocin, but the response is dose-, parity-, and species-dependent and should not be extrapolated between formulations without pharmacokinetic confirmation. The practical difference in the veterinary pharmacy is therefore a reduction in injection frequency when the clinical setting requires sustained uterine contraction; however, no universal dose-spacing interval is valid across all food-producing species.
| Comparison parameter | Native oxytocin | Carbetocin Veterinary Grade API |
|---|---|---|
| Structural stabilization | Disulfide bridge; aminopeptidase-sensitive N-terminus | Thioether-stabilized carba analogue; N-terminal deamino modification |
| Aqueous degradation route | Disulfide exchange and hydrolysis | Disulfide exchange reduced; pH-dependent hydrolysis and oxidation remain |
| Released dosage formats | Injection and solution | Injection, solution, oral powder, granule, premix, tablet and capsule intermediates where validated |
| Processing constraint | Terminal sterilization possible only with formulation-specific validation | Aseptic filtration preferred; terminal heat sterilization avoided unless forced-degradation data support it |
| Quality release panel | HPLC and pharmacopoeial injection monograph tests | HPLC assay, related substances, residual solvents VICH GL18, elemental impurities VICH GL19 |
The pharmacodynamic distinction between carbetocin and oxytocin is not limited to duration of action. Native oxytocin injection requires strict pH control and protection from light to limit disulfide scrambling, whereas carbetocin can be formulated in aqueous solution with a broader pH stability window because the sulfur-containing bridge is less redox-labile. This does not eliminate the need for pH control, because deamidation and hydrolysis remain pH- and temperature-dependent. Manufacturer forced degradation studies define the buffer system, not the pharmacopoeial monograph alone.
Because the API may be used in sterile injectable manufacture, the release specification is written to the most conservative downstream use. Acceptance ranges are harmonized with pharmacopoeial general chapters and VICH guidance; where a formal carbetocin veterinary monograph is not published, acceptance criteria are derived from ICH Q3C, ICH Q3D, and general peptide API controls. The specification table below summarizes the release panel used for veterinary-grade material supplied to finished-dose manufacturers.
| Test parameter | Analytical basis | Typical acceptance range |
|---|---|---|
| Appearance | Visual inspection, Ph. Eur. 2.2.1 | White to off-white powder or lyophilized cake |
| Identification | HPLC retention time and infrared absorption | Consistent with carbetocin reference standard |
| Assay | Reversed-phase HPLC, Ph. Eur. 2.2.29, on anhydrous basis | 98.0–102.0% w/w |
| Related substances | HPLC area normalization | Total ≤ 1.0%; any unspecified impurity ≤ 0.5% |
| Water content | Karl Fischer coulometric titration, Ph. Eur. 2.5.32 | ≤ 5.0% w/w for acetate hydrate |
| Residual solvents | Headspace gas chromatography, VICH GL18/ICH Q3C | Class 1 solvents absent; Class 2 and Class 3 within permitted daily exposure |
| Elemental impurities | ICP-MS or ICP-OES, VICH GL19/ICH Q3D | Parenteral-exposure limits for Pb, Cd, As, Hg; other elements by risk assessment |
| Bacterial endotoxins | Ph. Eur. 2.6.14 kinetic chromogenic LAL | 0.50 EU/mg or tighter for injection-grade API |
| Microbial enumeration | Ph. Eur. 2.6.12 and Ph. Eur. 2.6.13 | TAMC ≤ 103 CFU/g; TYMC ≤ 102 CFU/g; absence of E. coli in 1 g |
Sterility is not assigned to the bulk API; sterile status is established during finished-drug manufacturing by aseptic filtration through a 0.22 µm sterilizing-grade membrane and validated fill-line operation. Endotoxin limits above are typical for a parenteral-grade peptide API; actual values are contract-defined and may be tightened based on the intended injection volume per kg body weight.
During low-dose blending of carbetocin into powders, granules, and premix intermediates, direct addition of the active to a final blend is not recommended because carbetocin is present at microgram-to-milligram levels per gram of diluent and requires staged dilution to control assay variability. A standard GMP veterinary plant approach is a 1:10 or 1:100 preblend in lactose monohydrate or microcrystalline cellulose, passed through a 0.8 mm screen before transfer to a V-shell blender with an intensifier bar. Blend uniformity is monitored according to Ph. Eur. 2.9.40 or USP <905>, with acceptance limits of 90.0–110.0% of target assay and relative standard deviation not more than 5.0%. For granulated premixes, fluid-bed granulation with an aqueous binder is used; inlet air temperature, spray rate, and product dew point are controlled to avoid localized overwetting and peptide hydrolysis. Tablets and capsules produced from carbetocin-containing granulations require content uniformity testing under Ph. Eur. 2.9.6 and USP <905>, because low-dose peptide segregation during compression or encapsulation is a production-scale failure mode. If the processing environment exceeds 60% relative humidity, pre-drying of the API and excipients is required before weighing.
When carbetocin is formulated into oral premixes, tablets, capsules, or granules, the oral bioavailability cannot be inferred from injectable data. Carbetocin, like other short-chain peptides, is susceptible to gastric and intestinal proteolysis; therefore, tablet and capsule formats require enteric protection, an absorption enhancer, or a buccal/gingival retention strategy if systemic activity is intended. Published data for these specific oral configurations is limited, and in most jurisdictions carbetocin is approved as an injectable veterinary medicine rather than as an oral premix. Premix formulations are therefore usually constrained to development and research batches, not established pharmacopoeial drug product monographs. In contrast, injectable solutions are supported by pharmacopoeial quality chapters and require aseptic processing because terminal autoclaving is not assumed to be compatible with peptide stability; a 0.22 µm polyethersulfone or PVDF sterilizing-grade filter is used before filling into Type I glass vials. Finished injection storage is specified at 2–8°C with protection from light to limit oxidation and hydrolysis.
Aqueous carbetocin injection solutions are typically prepared with mannitol or sodium chloride as tonicity adjusters and an acetate or citrate buffer system in an acidic pH range selected by forced degradation studies. Nitrogen sparging of the bulk solution and nitrogen overlay during filling reduce oxidative degradation in the vial headspace. Production lines that handle carbetocin solutions should use 316L stainless steel or borosilicate glass contact surfaces; prolonged contact with untreated elastomeric closures may cause sorption losses, and siliconized closure surfaces are specified to limit surface adsorption. Lyophilized injection formulations are reconstituted with water for injection before use and are manufactured on freeze-dryer shelves with controlled ramps because the amorphous API cake can collapse if the primary drying temperature exceeds the formulation-specific collapse temperature. For non-sterile powders and granules, storage at 25°C or below is typical; excursions above 30°C require batch-specific stability data and are not covered by routine storage specifications unless formal bracketing studies are available.
In tablet and capsule development, carbetocin presents the same low-dose peptide challenges as other synthetic peptide APIs: poor direct compressibility, electrostatic adhesion to metal punches, and content uniformity drift at high press speeds. Pilot-scale compression runs with ≤ 2.0% API loading have shown increased relative standard deviation when hopper residence time is extended; for this reason, feed-frame level control and tablet press turret speed are treated as critical process parameters. Capsule filling of low-dose carbetocin granules on automatic dosator machines may require pin adjustment to control plug density and avoid overfilling with fines, which can shift assay delivery outside 90.0–110.0% of label claim. These process parameters are established during technical transfer and are not specified in the API certificate of analysis; they are, however, part of the finished-dose manufacturing development package that a veterinary drug manufacturer must compile before process validation.
For injectable solutions, the filling line is typically a restricted-access barrier or isolator system with automatic stopper insertion. The fill volume is based on the target dose per kg body weight and the final assay; in-process checks include fill volume by weight, filter integrity by bubble point or diffusion test, and optical inspection for visible particles according to Ph. Eur. 2.9.20. Terminal heat sterilization is not substituted for aseptic filtration unless the formulation developer provides data showing ≤ 0.5% related substance increase and full assay retention after the thermal cycle. Endotoxin reduction is not a substitute for filtration, because depyrogenation of the bulk peptide is rarely feasible without thermal destruction.
The release and stability-indicating method for carbetocin separates the parent peptide from desamido, sulfoxide, and other hydrolytic products generated during forced degradation. Reversed-phase HPLC on a C18 column with UV detection at 220 nm is a common configuration for peptide API assay and related substance profiling. Forced degradation conditions include acidic hydrolysis, alkaline hydrolysis, oxidative stress with dilute hydrogen peroxide, thermal stress, and photolysis; the analytical method is considered stability-indicating when peak purity is demonstrated and mass balance is between 95.0% and 105.0% of the unstressed control. Water content is controlled because excess moisture accelerates deamidation and hydrolytic cleavage in the solid state; the Karl Fischer limit in the specification table is therefore a critical quality attribute for solid dosage manufacturing. For injectable solutions, pH and buffer species are confirmed as part of formulation development because carbetocin degradation follows pH-dependent kinetics, with maximum solution stability typically observed in an acidic buffer range near pH 4.0–5.0. The pH rate profile is verified experimentally for each formulation rather than assumed from oxytocin data, because the thioether-stabilized analogue does not share the same redox degradation pathway.
Carbetocin veterinary API is not compatible with strong oxidizing agents, acidic solutions below the formulation-specific stability boundary, or untreated metal surfaces that catalyze peptide adsorption. It should not be blended with hygroscopic deliquescent excipients without moisture-control studies. Powder, granule, and premix intermediates are intended for veterinary use only and require validated withdrawal periods in food-producing animals when administered through any route.
