| HS Code | 297048 |
| Product Name | Ergometrine Veterinary Grade API |
| Suitable Dosage Forms | Tablets, Injections, Capsules, Powders, Granules, Premix, Solutions |
| Chemical Name | (6aR,9R)-N-((S)-1-hydroxypropan-2-yl)-7-methyl-4,6,6a,7,8,9-hexahydroindolo[4,3-fg]quinoline-9-carboxamide |
| Cas Number | 60-79-7 |
| Molecular Formula | C19H23N3O2 |
| Molecular Weight | 325.41 g/mol |
| Appearance | White to off-white crystalline powder |
| Solubility | Slightly soluble in water; soluble in alcohol and acetone |
| Melting Point | Approximately 162°C |
| Assay Purity | 97.0% to 101.0% on dried basis |
| Storage Conditions | Store in tightly closed containers, protected from light, in a cool and dry place |
| Shelf Life | 24 months when stored under recommended conditions |
As an accredited Ergometrine 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 | Available in 25 kg net, packaged in double-lined, sealed drums/bags, protected from light and moisture for various formulations. |
| Container Loading (20′ FCL) | One 20′ FCL of Ergometrine Veterinary Grade API, packed in sealed drums, palletized and secured, for pharmaceutical production use. |
| Shipping | Ergometrine Veterinary Grade API ships in sealed, light-resistant, tamper-proof containers with proper hazard labeling. Requires temperature-controlled, secure transport away from moisture and direct sunlight. Full documentation, SDS, and cold-chain compliance included. International shipments follow strict pharmaceutical regulations to ensure purity, potency, and safety throughout transit. |
| Storage | Store Ergometrine Veterinary Grade API in tightly sealed, light-resistant containers in a cool, dry, well-ventilated area, ideally between 2–8°C. Protect from moisture, heat, and direct sunlight. Keep away from oxidizing agents and incompatible materials. Ensure container remains closed when not in use to maintain stability and potency for all finished formulations. |
| Shelf Life | Shelf life is typically 24 months when stored in airtight, light-resistant containers at controlled room temperature, protected from moisture and heat. |
In veterinary obstetric therapeutics, ergometrine maleate is processed into sterile injectable solutions when rapid uterine contraction is indicated after dystocia, retained placenta, or postpartum uterine atony in cattle, horses, and sows. The maleate salt is preferred over the free base because its aqueous solubility permits low-concentration injections without organic co-solvents. A batch is prepared by dissolving the active substance in Water for Injection, adjusting to pH 3.0–3.5 with dilute hydrochloric acid, and sterile-filtering through a 0.22 µm PVDF or PES membrane. Terminal moist-heat sterilisation is generally avoided because ergometrine is thermolabile and forms the stereoisomer ergometrinine under alkaline or thermal stress. Aseptic filling therefore takes place in a Grade A zone within a Grade B cleanroom under ISO 14644-1 and EU GMP Annex 1, using rotary piston or peristaltic filling pumps. Fill volume is checked gravimetrically every 5 minutes on a multi-head checkweigher, and amber Type I borosilicate glass vials conforming to ISO 4802-1 are used with nitrogen overlay to limit oxidative headspace oxygen.
| Control point | Method / standard | Typical release limit | Observed process failure mode |
|---|---|---|---|
| Fill volume | Ph. Eur. 2.9.17 gravimetric | ±5% of label fill | peristaltic tube wear and drift after 4 h |
| Solution pH | Ph. Eur. 2.2.3 | 3.0–3.5 | pH rise from vial glass leaching if unbuffered |
| Sterility | Ph. Eur. 2.6.1 | no growth | filter integrity failure or pinhole |
| Bacterial endotoxins | Ph. Eur. 2.6.14 | product-specific, often <0.25 EU/mL for low-volume injections | vial washer depyrogenation failure |
| Assay | HPLC-UV per Ph. Eur. monograph | 95.0–105.0% label claim | filter adsorption above 2% |
| Ergometrinine | HPLC-UV per Ph. Eur. monograph | not more than pharmacopoeial limit | light exposure during fill |
Filter validation is not optional at low-concentration fill volumes. A product-specific bacterial retention study is conducted on the selected 0.22 µm membrane, and adsorption is measured by assaying the first 50 mL, middle fraction, and last 50 mL of filtrate. If the first fraction assay falls below 95% of target, the filter is pre-flushed with the same vehicle or switched to a low-binding polyethersulfone membrane. Extractables are reviewed under ISO 10993-18, and the final rinse volume must be justified. In-process light exposure is limited to 100 lux for manual interventions, and amber vial light transmission between 290 nm and 450 nm should remain below 10% by container light-transmission testing. Aqueous ergometrine maleate solutions degrade more rapidly above pH 5.0, so weak acid buffers are preferred, and phosphate buffers are avoided unless a specific stability study supports their use.
Direct compression is rarely the first choice for ergometrine maleate tablets because the active substance is typically present at less than 0.5 mg per unit in veterinary oral formulations. At this concentration, segregation during hopper discharge and die filling creates content uniformity failure under Ph. Eur. 2.9.40. A robust direct compression process uses a pre-blend of ergometrine maleate in lactose monohydrate 200 mesh at a ratio between 1:9 and 1:19, prepared by geometric dilution in a V-blender running at 25 rpm for 15–20 minutes. Microcrystalline cellulose 20–35% w/w and crospovidone 2–5% w/w are added in a second blending stage, followed by magnesium stearate at 0.25–0.5% w/w for 3–5 minutes. Over-lubrication beyond 5 minutes reduces tablet hardness and slows dissolution in 0.1 M hydrochloric acid.
Compression on a rotary tablet press with B-tooling at 4–10 kN produces tablets with hardness 40–70 N and friability not more than 1.0% when measured by Ph. Eur. 2.9.7. If blend segregation is observed, the formulation is switched to wet granulation rather than increasing magnesium stearate. Granulation disperses the pre-dissolved active substance and reduces punch filming. Moisture is controlled to LOD ≤2.0% before compression; higher residual water causes picking, sticking, and localised discolouration. Tablets are packed into amber glass bottles or alu-alu blisters with desiccant because light and humidity accelerate degradation. Published veterinary target-species bioequivalence data for oral ergometrine maleate tablets are limited, so release testing follows contract specifications based on pharmacopoeial general chapters.
Hard gelatin and HPMC capsule filling of ergometrine maleate is generally limited to extemporaneous veterinary pharmacy compounding because published stability data for capsule presentations in target species are sparse. Where a capsule is required for oral dosing in small ruminants or companion animals, the blend is prepared by geometric dilution of ergometrine maleate with lactose monohydrate or pregelatinised starch. The target capsule fill weight is usually 100–150 mg in size 3 or size 4 capsules, and the active fraction is kept below 1% w/w to permit accurate dispensing. Powder flow is measured by Ph. Eur. 2.9.36; an angle of repose above 42° is corrected by adding colloidal silicon dioxide at 0.5–1.0% w/w. A tamping-pin capsule machine or a manual hand-filling device is used for batch sizes below 5,000 capsules, and content uniformity is tested by Ph. Eur. 2.9.40 on a composite sample of 10 capsules. Dissolution testing under Ph. Eur. 2.9.3 may require pepsin or HPMC capsules if gelatin cross-linking occurs in accelerated storage above 30°C and 65% RH. Capsule-specific stability data should be generated for each target species because gastrointestinal pH differences alter drug release and absorption.
Granulation is selected when direct compression cannot sustain blend uniformity and when dust containment is required for operator safety. A top-spray fluid-bed granulator with a bowl capacity between 5 kg and 100 kg is charged with a pre-blend of ergometrine maleate, microcrystalline cellulose, and lactose monohydrate. The binder solution, 5% w/w hypromellose 5 mPa·s or 3–5% w/w povidone K30 in purified water, is sprayed at 4–8 g/min per kilogram of dry powder. Inlet air temperature is maintained at 50–65°C, product temperature at 30–40°C, and atomisation air pressure at 1.5–2.0 bar. Inlet temperatures above 65°C risk thermal degradation of ergometrine maleate and surface hardening of granules; below 50°C the spray wets the bed unevenly and forms lumps larger than 1.0 mm.
After spraying, the granules are dried to LOD 1.5–2.5% and sized over a 710 µm screen. The fraction below 150 µm is limited to 15% w/w because fines reduce flow and promote segregation during subsequent capsule filling or tableting. Particle-size distribution is verified by Ph. Eur. 2.9.38. Bulk density of the final granules is typically 0.45–0.65 g/mL, with tapped density 0.55–0.80 g/mL, and compressibility index should remain below 25% for smooth die filling. Granules may be packed as single-dose sachets or further processed into tablets. The sachet material must be light-opaque and moisture-barrier, with alu-alu laminate preferred over clear film. Stability of ergometrine maleate granules in veterinary-specific packaging requires photostability and moisture-uptake studies because the active substance degrades by light-induced isomerisation and hydrolytic ring opening.
| Parameter | Tablet | Capsule | Granules |
|---|---|---|---|
| Active fraction in blend | 0.1–0.5% w/w | 0.1–1.0% w/w | 0.1–0.5% w/w |
| Bulk density | 0.50–0.70 g/mL | 0.45–0.65 g/mL | 0.45–0.65 g/mL |
| LOD before processing | 1.5–2.5% | 1.5–2.5% | 1.5–2.5% |
| Critical process limit | compression force 4–10 kN | tamping pin depth 2–3 mm | inlet air 50–65°C |
| In-process test | hardness 40–70 N, friability ≤1.0% | fill weight ±5%, content uniformity | sieve fraction 150–710 µm, LOD |
For oral powder dosing in large animals, ergometrine maleate is triturated with a water-soluble carrier such as glucose monohydrate or lactose monohydrate to produce a free-flowing powder. The active concentration is usually adjusted so that a single dose is contained in 1–5 g of powder, which reduces weighing errors on farm or in clinic. A double-cone blender or V-blender is operated at 60–70% fill volume for 10–20 minutes, and the uniformity of the mix is confirmed by assay of 10 thief samples with relative standard deviation not more than 5%. Because ergometrine maleate is light-sensitive, the powder is packed in amber glass jars or opaque polyethylene pouches with desiccant. The powder is reconstituted with potable water immediately before administration; the resulting solution is protected from light and discarded after 24 hours unless a longer use period is supported by in-house stability data. Published aqueous stability data for ergometrine maleate oral powders under farm conditions are limited, so conservative use periods are applied.
Premix applications for ergometrine maleate are constrained less by mixing technology than by residue legislation. Under EU Regulation (EC) No 1831/2003, ergometrine maleate is not authorised as a feed additive, and under Regulation (EC) No 470/2009 no harmonised maximum residue limit is established for edible tissues. Accordingly, a premix for medicated feed is not a lawful presentation in the EU for food-producing species. Extemporaneous preparation is limited to non-food-producing animals or to national derogations where a veterinarian assumes direct responsibility and residue avoidance is documented. Equivalent national cascade rules include 21 CFR 530 in the United States. Where a premix is legally produced for non-food-producing animals, the active ingredient is dispersed into corn starch or lactose carrier by geometric dilution in a ribbon blender with an intensifier bar. Particle-size reduction to D90 ≤100 µm improves homogeneity, but micronisation can increase static charge and light exposure. Homogeneity is tested by assay of 10 sampling points across the blender with acceptance RSD ≤5%. Pelleted feed is not a suitable carrier because pelleting temperatures of 70–85°C degrade ergometrine maleate and produce low assay values.
Aqueous oral solutions are compounded from ergometrine maleate when intravenous or intramuscular injection is impractical or when a veterinarian prescribes an oral drench for a small number of animals. The solution is commonly prepared in purified water with a target pH of 3.2–3.6, because the protonated alkaloid form is more stable and more soluble than the free base. Citrate or tartrate buffers are used rather than phosphate buffers, which may alter pH with dilution or create incompatibility with divalent cations in hard water. Preservative efficacy must be demonstrated by Ph. Eur. 5.1.3; methyl paraben at 0.18% w/w and propyl paraben at 0.02% w/w are common but must be validated in the specific vehicle. The solution is filled into amber Type III glass or amber PET bottles with a child-resistant closure; clear containers are unacceptable because ambient light accelerates isomerisation to ergometrinine within hours.
Storage is typically at 2–8°C for compounded oral solutions, and a shelf-life longer than 30 days is not assigned unless supported by a stability protocol under ICH Q1A. The fill line uses a peristaltic pump with silicone tubing and a 1 mL oral syringe graduated in 0.1 mL increments; for large-animal drenching, a 10–50 mL drench gun is calibrated daily. Homogeneity during filling is maintained by a magnetic stirrer at 200–300 rpm; excessive stirring can introduce oxygen and increase oxidative degradation. Published pharmacokinetic and target-species stability data for oral ergometrine maleate solutions are limited, so the formulation and packaging limits above derive from pharmacopoeial principles and compounding practice rather than from veterinary-specific registration dossiers.
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Ergometrine maleate veterinary-grade API is supplied as the water-soluble maleate salt of the ergot alkaloid ergometrine, also known as ergonovine. The active entity has the molecular formula C19H23N3O2·C4H4O4 and a relative molecular mass of 441.48 g/mol; the maleate salt CAS registry number is 129-51-1, and the free base CAS number is 60-79-7. The substance is controlled against the current European Pharmacopoeia monograph for ergometrine maleate and, where applicable, the USP Ergonovine Maleate monograph. Release data include assay on the dried or anhydrous basis, specific optical rotation, related substances, residual solvents, particle-size parameters, and microbiological quality attributes appropriate to the intended dosage form. The material is supplied in two physical grades: a standard milled grade for tablets, capsules, granules, and premix manufacture, and a micronized grade for sterile aqueous suspensions and solutions. The grade designation does not define a separate chemical entity; it defines particle-size control, packaging configuration, and the documentation required for downstream processing. In food-producing species, suitability of use is determined by the approved marketing authorization, applicable maximum residue limit or withdrawal period, and national residue control requirements.
The primary veterinary use of ergometrine maleate is in formulations intended for the management of uterine atony and postpartum hemorrhage when included in an authorized product. The API is not dispensed directly as a finished dosage form. Tablets, capsules, granules, and oral powders are used where oral administration is required; injectable solutions and suspensions are used where rapid onset is necessary; premix and medicated feed formats are used only where authorized for the target species. The dosage form changes the required particle-size specification, excipient compatibility, and stability program.
For solid dosage forms, particle-size distribution is characterized by laser diffraction using Ph. Eur. 2.9.31 or USP <429>. The standard milled grade is released against an agreed D10/D50/D90 envelope matched to the unit operation, because no universal compendial particle-size limit applies to ergometrine maleate. In direct compression, low-dose blends are prepared by geometric dilution in a bin blender or V-blender; blend uniformity is evaluated using Ph. Eur. 2.9.40 or USP <905>. A processing risk is segregation when the active particle size is much smaller than the direct-compression diluent. This is controlled by matching carrier particle size and by maintaining relative humidity below the point at which static charge increases. For capsule filling, flow through dosator or tamping-pin equipment is assessed by bulk density, Carr index, and Hausner ratio using Ph. Eur. 2.9.36 and USP <1174>. Where particle-size reduction is required, air-jet milling or pin milling with nitrogen cooling is used to limit heat exposure. After milling, the powder is sampled at multiple points and analyzed for D10/D50/D90; a D90 limit is set to avoid slow dissolution in tablets and capsules. The particle shape also influences flow; needle-shaped or cohesive powders may require dry granulation before compression.
Compendial control of ergometrine maleate is based on assay, optical rotation, and chromatographic purity. The assay is controlled between 97.0% and 102.0% on the dried or anhydrous basis. Specific optical rotation is controlled between +48° and +57°, determined on the dried substance; this test provides an identity and chiral purity check because the inactive epimer ergometrinine and related degradation products have different optical rotation values. Related substances are determined by high-performance liquid chromatography using the stationary phase, mobile phase, detection wavelength, and system suitability conditions described in the pharmacopoeial monograph. The product is released only when total impurity and specified impurity thresholds meet the monograph limits. Loss on drying is determined by the method and conditions described in the monograph. Residual solvents are controlled according to VICH GL18 and Ph. Eur. 5.4, with class 1 solvents absent or below limits and class 2 solvents reported in the certificate of analysis. Identity is confirmed by infrared absorption spectrophotometry concordant with the reference standard and by HPLC retention time comparison. The substance is also evaluated against the general monograph Ph. Eur. 2034 for substances for pharmaceutical use.
| Quality attribute | Method reference | Controlled parameter | Release criterion anchor |
|---|---|---|---|
| Chemical identity | Ph. Eur. 2.2.24; USP <197K> | Infrared spectrum concordance | Concordant with reference standard |
| Assay | HPLC per monograph | Ergometrine maleate content | 97.0–102.0% dried or anhydrous basis |
| Specific optical rotation | Ph. Eur. 2.2.7; USP <781> | Chiral purity indicator | +48° to +57° |
| Related substances | HPLC per monograph | Total and specified impurities | Monograph thresholds |
| Loss on drying | Ph. Eur. 2.2.32; USP <731> | Moisture content | Monograph limit |
| Residual solvents | VICH GL18; Ph. Eur. 5.4 | Class 1 and class 2 solvents | Class-specific limits |
| Particle size | Ph. Eur. 2.9.31; USP <429> | D10/D50/D90 | Quality target product profile |
| Microbial quality | Ph. Eur. 5.1.4; USP <1111> | TAMC/TYMC or sterility | Route-specific |
In aqueous injection compounding, the manufacturing line typically uses a high-shear mixer for vehicle preparation followed by nitrogen sparging through a sintered stainless steel sparger. Dissolved oxygen is monitored with a polarographic probe until the target is reached; the solution is then brought to final volume with Water for Injection and pH-adjusted with a suitable acidic buffer to maintain the maleate salt in the ionized form and to minimize epimerization. Storage of the finished sterile solution is commonly specified at 2–8 °C with protection from light, because the ergoline chromophore undergoes photodegradation. Solutions are filtered through 0.22 µm polyethersulfone or polyvinylidene fluoride membranes when terminal moist-heat sterilization is not justified by stability data. For injectable suspensions, the micronized grade is dispersed in an aqueous vehicle that may include a wetting agent and viscosity modifier. Syringeability is evaluated by force-to-plunge tests using the intended needle size and by particle-size retention after stress. Bacterial endotoxin testing by Ph. Eur. 2.6.14 or USP <85> is applied with a limit calculated from the maximum dose and species body weight. The API and the finished injection are not autoclaved unless stability data demonstrate acceptable degradation of the ergoline ring at the selected F0 value.
The decision to use sterile filtration instead of terminal moist-heat sterilization is based on thermal degradation data, solution pH, and container headspace oxygen. Ergometrine maleate in unbuffered or weakly buffered aqueous solution is sensitive to elevated temperature and light; therefore, aseptic processing is preferred unless terminal sterilization is validated. Sterile filtration through a 0.22 µm membrane does not remove endotoxin; the upstream water, raw materials, and API must meet endotoxin limits before filtration. Filter compatibility is tested by measuring API recovery, visible particle formation, and membrane integrity after filtration. The container-closure system is typically a Type I borosilicate glass vial with a butyl or halobutyl rubber stopper; the glass is washed and depyrogenated by dry heat. Nitrogen overlay in the headspace or vacuum filling is used to reduce oxidative degradation. Particulate matter in the finished injection is controlled by light obscuration using Ph. Eur. 2.9.19 or USP <788>. For freeze-sensitive solution products, storage must remain above the freezing point; freeze-thaw stress is tested only if the label permits freezing. Stability data are generated in the final packaging because the closure can contribute extractables that affect solution pH and color.
Unlike the nonapeptide oxytocin, ergometrine maleate is a small-molecule ergot alkaloid salt that is not degraded by gastrointestinal peptidases; this supports oral solid dosage forms such as tablets, capsules, granules, and oral powders in addition to parenteral solutions. The receptor profile also differs: ergometrine exerts oxytocic and vasopressor activity through α-adrenergic and serotonergic receptor pathways, while oxytocin acts through the oxytocin receptor. The difference is relevant in species-specific use and in the assessment of vascular adverse effects. The two molecules require different stabilization strategies: oxytocin is commonly supplied as a sterile solution or injection and is sensitive to pH and heat, whereas ergometrine maleate can be processed into non-sterile oral solids if the dosage form controls light, moisture, and oxidative exposure. Methylergometrine and other ergot alkaloids differ in their potency, adverse-effect spectrum, and regulatory status in animal health; the formulator should not substitute one ergot alkaloid for another without compendial and clinical data. The term “veterinary grade” does not imply equivalence to oxytocin or to methylergometrine.
In aqueous solutions, the main degradation pathways of ergometrine maleate are epimerization to the inactive ergometrinine, oxidation of the ergoline ring, and photodegradation. pH is the most influential variable: the API is more stable under acidic conditions, and the formulation pH is usually maintained below 5.0 unless buffering capacity or tonicity constraints require otherwise. Photostability is evaluated according to VICH GL5, and long-term stability studies are conducted according to VICH GL3. Solutions are protected from light; amber glass containers are commonly required. Oxygen headspace is displaced with nitrogen. For oral solutions and drench formulations, preservative compatibility is tested because some preservatives can increase oxidative degradation. The API is not stable in alkaline media; alkaline buffer systems are avoided. For powders and granules, moisture sorption is controlled by packaging in aluminium foil or high-barrier laminated sachets. When the API is dry, the degradation rate is lower, but the substance should be stored in airtight containers protected from light, at controlled room temperature or as specified in the certificate of analysis.
Roller compaction of ergometrine maleate with microcrystalline cellulose, lactose monohydrate, and crospovidone is used for moisture-sensitive formulations. The ribbon is milled through an oscillating granulator fitted with a screen; granule density is correlated with tablet tensile strength and disintegration time. Dry granulation minimizes the aqueous exposure that accelerates epimerization. For wet granulation, an aqueous binder solution containing povidone is acceptable only if the granulation and drying time are short and the pH is acidic. The wet mass is dried in a fluid-bed dryer at an inlet air temperature below levels that induce chemical instability. Drying endpoints are determined by loss-on-drying using Ph. Eur. 2.2.32 or USP <731>. Compression profiles are established by hand-held or instrumented tablet press; tablet hardness is correlated with disintegration and dissolution using Ph. Eur. 2.9.3 or USP <711>. The API is not micronized for wet granulation unless dissolution failure requires it.
Premix and medicated feed operations use lactose monohydrate, dextrose, or corn starch as carriers. The API is first mixed with a small quantity of carrier in a high-shear or ribbon blender, then diluted stepwise; the final blend is discharged into bulk containers lined with food-compatible polyethylene. Blend uniformity is tested by HPLC at multiple sampling points using Ph. Eur. 2.9.40 or USP <905>; acceptance is based on content uniformity and relative standard deviation. In feed mills, carryover into subsequent batches is controlled by sequencing and by validated cleaning of mixers, conveyors, and dust extraction systems. Because ergometrine maleate is light-sensitive, premix packaging uses light-blocking laminates. Storage conditions are specified on the label; published data for this specific configuration is limited when the premix contains reducing sugars or minerals, so site-specific stability studies are recommended.
Cross-contamination control for this alkaloid is performed by HPLC assay of rinse and swab samples from product-contact surfaces. The acceptance limit is derived from the permitted daily exposure of the target species and the batch size of the next product. Dedicated or campaign manufacturing may be required where the API is handled in open powder form. Aqueous cleaning is more effective than dry cleaning for soluble residues, but contact time and temperature must be controlled to avoid degradation to adhesive or colored residues on stainless steel. Failure modes observed in production include incomplete removal from rotary tablet press punch bodies and capsule dosator bushings, which require specific disassembly and rinse procedures.
Documentation for each batch includes a certificate of analysis, certificate of conformance, and where applicable a certificate of suitability to the European Pharmacopoeia for the active substance. The batch record includes synthesis or purification route details, particle-size data, residual solvent results, and elemental impurity data assessed in line with ICH Q3D principles applied to veterinary products. The supply chain is qualified for starting materials, and the packaging is labeled for veterinary use only where required. All test methods are validated for specificity, linearity, accuracy, and precision before use in release testing.
