| HS Code | 368340 |
| Chemical Name | Isoprenaline Hydrochloride (Isoproterenol Hydrochloride) |
| Cas Number | 51-30-9 |
| Molecular Formula | C11H17NO3·HCl |
| Molecular Weight | 247.72 g/mol |
| Appearance | White or almost white crystalline powder |
| Solubility | Freely soluble in water; sparingly soluble in ethanol; practically insoluble in ether |
| Melting Point | 170-175°C with decomposition |
| Storage Conditions | Store in tightly sealed, light-resistant containers in a cool, dry place protected from moisture and air |
| Shelf Life | 24 months when stored under recommended conditions |
| Veterinary Use | Suitable as a veterinary-grade active pharmaceutical ingredient for tablets, injections, capsules, powders, granules, premixes, and solutions; acts as a non-selective beta-adrenergic agonist for bronchodilation and cardiac stimulation |
As an accredited Isoprenaline 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 | Supplied in 25 kg sealed fiber drums with double polyethylene liners, protected from light/moisture, labeled for veterinary API use. |
| Container Loading (20′ FCL) | 20′ FCL container loading of Isoprenaline Veterinary Grade API: packed on pallets in sealed drums, ensuring stability, safety, and efficient transport. |
| Shipping | Ship as a temperature-controlled, tightly sealed, light-protected API. Use double-layered, moisture-barrier packaging with absorbent cushioning. Ensure compliance with veterinary drug transport regulations and proper labeling. Avoid extreme heat or freezing. For powders/granules, minimize static and dust; for solutions, prevent leakage. Include Material Safety Data Sheets and tamper-evident seals. |
| Storage | Store Isoprenaline Veterinary Grade API in a tightly sealed, light-resistant container in a cool, dry, well-ventilated area. Protect from moisture, humidity, and direct sunlight. Maintain controlled room temperature, away from heat sources and incompatible substances like strong oxidizers. Keep container closed when not in use, and follow specific stability guidelines for each formulated dosage form. |
| Shelf Life | Shelf life is typically 24–36 months in unopened, tightly sealed containers, stored protected from light, moisture, and heat. |
In veterinary emergency medicine, isoprenaline hydrochloride is compounded into a sterile injectable solution for temporary rate support in haemodynamically significant bradyarrhythmias, including third-degree atrioventricular block and sinus bradycardia refractory to atropine. Because the catechol ring is susceptible to oxidative degradation, the manufacturing sequence does not include terminal steam sterilisation. The aqueous vehicle is sparged with filtered nitrogen until dissolved oxygen falls below 2 mg/L; sodium metabisulfite is then added at 0.1% w/v as an oxygen scavenger, and disodium edetate at 0.01% w/v chelates trace metal ions that catalyse adrenochrome formation. The solution is adjusted to pH 3.0–4.5 with dilute hydrochloric acid because alkaline conditions accelerate oxidation of the catechol nucleus. The bulk liquid is chilled to 2–8°C and filtered through a 0.45 µm prefilter followed by a 0.22 µm PVDF sterilising-grade membrane into depyrogenated Type I borosilicate glass vials. Vial headspace is overlaid with nitrogen before bromobutyl stopper insertion. On production-scale aseptic fill lines, batch-to-batch colour variability has been traced to residual headspace oxygen and iron contamination in stopper elastomers; stoppers are therefore washed with an EDTA-containing rinse solution to reduce extractable metal ions. Diluted infusions are prepared in PVC-free polyolefin or low-density polyethylene containers because catecholamines may interact with flexible PVC and plasticiser components during extended contact. The diluted admixture is protected from light and is treated as a single-use preparation in the absence of product-specific in-use stability data.
| Quality attribute | Compendial method | Typical criterion | Process observation |
|---|---|---|---|
| Appearance | Visual inspection | Clear, colourless to faint yellow | Yellow-brown colour indicates adrenochrome formation |
| pH | Ph. Eur. 2.2.3 / USP <791> | 3.0–4.5 | Above 4.5 oxidation increases; below 3.0 injection site irritation is possible |
| Osmolality | Ph. Eur. 2.2.35 / USP <785> | 280–320 mOsmol/kg | Adjusted with sodium chloride |
| Particulate contamination | Ph. Eur. 2.9.19 / USP <788> | Compendial SVI/LVP limits | Serial filtration through 0.45 µm and 0.22 µm membranes |
| Sterility | Ph. Eur. 2.6.1 / USP <71> | No growth after 14 days | Aseptic fill with nitrogen overlay |
| Bacterial endotoxins | Ph. Eur. 2.6.14 / USP <85> | Dose-based limit | Depyrogenated vial and stopper components |
| Assay | HPLC with UV detection | 95.0–105.0% label claim | Related substances must be integrated and reported |
Equine recurrent airway obstruction (RAO, severe equine asthma) is managed with bronchodilator aerosols delivered through high-output equine nebuliser systems that generate tidal-breathing-compatible aerosols. Isoprenaline hydrochloride solution for nebulisation is compounded at a concentration selected by the prescribing veterinarian and is typically buffered to pH 4.0 with citrate or acetate buffer because pH drift toward neutral water in unadjusted formulations accelerates oxidative discolouration within the administration period. Sodium metabisulfite at 0.05% w/v is included only where the horse has no documented sulfite hypersensitivity; the solution is filled into amber multi-dose nebuliser reservoirs and used within 24 h of first puncture when no preservative efficacy data are available. The aerodynamic droplet size must fall between 2 µm and 5 µm for lower airway deposition; this is verified by cascade impaction according to Ph. Eur. 2.9.44 or USP <601> where regulatory filing is required. Mixing with alkaline mucolytics such as acetylcysteine is avoided because the resulting pH rise accelerates catechol degradation. In equine practice, compressed-air nebulisers operated at 6–8 L/min may produce condensation or heating in the administration circuit, shifting the droplet distribution toward larger particles that impact in the upper airways; the resulting heart-rate response must be monitored because isoprenaline is non-selective and can produce significant beta-1 mediated tachycardia.
Tablets and capsules for veterinary oral use are prepared as low-dose, dose-titrated forms, but systemic bioavailability after oral administration is reduced by intestinal and hepatic conjugation. The oral route is therefore reserved for protocols in which a β-adrenergic effect is desired over a short dosing interval under direct veterinary supervision, and published clinical data for this specific configuration is limited. Direct compression is preferred over wet granulation because the addition of water in a high-shear granulator increases the amorphous surface area of the API and accelerates oxidative decomposition; a dry blend of isoprenaline hydrochloride, lactose monohydrate, microcrystalline cellulose and pregelatinised starch is processed in a low-shear tumble blender. The API is first preblended by geometric dilution at a 1:10 ratio with a portion of carrier to reduce segregation caused by particle size differences. Production-scale blending records show that over-filling the blender above 60% of nominal capacity reduces mixing efficiency and increases assay variance, so the batch size is matched to the working volume. Capsule filling on semi-automated machines requires pin height and slide plate settings to be validated per capsule size; tablets are compressed at 5–10 kN with a precompression step to prevent capping of low-hardness tablets. Excipients with alkaline microenvironments, such as dibasic calcium phosphate, are avoided because they raise the local pH on the API surface and accelerate discolouration. If wet granulation is unavoidable, drying is performed at a product temperature not exceeding 40°C under vacuum to limit thermal degradation. The finished units are packaged in cold-seal or foil-laminated blister packs with desiccant and stored at 2–8°C; beyond-use dating is justified only by validated stability data.
| Quality attribute | Compendial method | Practitioner control |
|---|---|---|
| Blend uniformity | Ph. Eur. 2.9.40 / USP <905> | Geometric dilution, low-shear tumble blending |
| Uniformity of mass | Ph. Eur. 2.9.5 | Validated pin height and slide plate settings |
| Disintegration | Ph. Eur. 2.9.1 / USP <701> | Direct compression with disintegrant selection |
| Dissolution | Ph. Eur. 2.9.3 / USP <711> | Water or 0.1 M HCl as medium; sink conditions maintained |
| Water content | Ph. Eur. 2.5.12 / USP <921> Method Ia | Moisture-proof packaging with desiccant |
| Assay / related substances | HPLC with UV detection | Protection from heat, light and alkaline excipients |
Lyophilised presentations of isoprenaline hydrochloride are manufactured when a dry powder for reconstitution is required to reduce hydrolysis and oxidation during storage in veterinary hospital pharmacies. The pre-lyophilisation solution is prepared at 2–8°C and contains isoprenaline hydrochloride, mannitol as a bulking crystallising excipient, disodium edetate, and sodium metabisulfite in water for injection. The solution is filled into Type I glass vials and loaded onto lyophiliser shelves pre-cooled to 5°C. The freezing step is carried out at −40°C for at least 2 h to ensure complete solidification; primary drying is then initiated at a shelf temperature of −20°C and a chamber pressure of 0.2 mbar, with the product temperature maintained below the collapse temperature of the formulation. If mannitol crystallisation is incomplete during freezing, the lyophilisate may contain amorphous regions that expand during primary drying and cause cake shrinkage or meltback on the shelf; an annealing step at −10°C for 1–2 h is therefore used when the mannitol content exceeds 10% w/v. The end of primary drying is confirmed by comparative pressure measurement using Pirani and capacitance manometer gauges. Secondary drying is performed at 25°C until the residual moisture determined by Ph. Eur. 2.5.12 or USP <921> Method Ia is below 1.0%. Reconstitution with sterile water for injection or 0.9% w/v sodium chloride produces a clear to faint yellow solution that is administered by constant rate infusion after further dilution; any unused reconstituted solution is discarded after 24 h when stored at 2–8°C unless specific in-use stability data support a longer period.
Premix and granule formulations containing isoprenaline are prepared as dry, ready-to-dilute intermediates for non-food companion animals and equine patients, not as medicated feed premixes for animals entering the human food chain. Published residue depletion data for isoprenaline in food-producing species is limited; therefore routine use of such premixes in production animals is excluded from formulation. For a companion animal oral liquid, isoprenaline hydrochloride is adsorbed onto a neutral carrier such as microcrystalline cellulose or lactose monohydrate by low-shear blending; the drug-carrier mixture is then filled into double polyethylene bags with an outer foil laminate and a desiccant sachet. The blend is tested for uniformity of dosage units according to Ph. Eur. 2.9.40 or USP <905> on samples taken from the beginning, middle and end of the blending discharge because low-dose APIs segregate during discharge from V-blenders. If granulation is required to reduce dust, a dry granulation step with roller compaction is preferred over wet granulation because residual moisture above 2.0% w/w can plasticise the carrier and destabilise the catechol. The premix is reconstituted into an oral liquid only at the point of dispensing by the compounding pharmacist or veterinary practitioner; the liquid vehicle is selected to maintain pH below 4.5 and is protected from light. Published data for this specific configuration is limited, so each batch must be assigned a beyond-use date on the basis of product-specific stability studies rather than extrapolation from injectable or nebuliser formulations.
Compounded oral solutions containing isoprenaline hydrochloride are dispensed for small animal patients when a liquid dosage form improves dose adjustment in animals that cannot be safely tablet-dosed. The oral solution is prepared from a concentrated stock under continuous stirring, with the vehicle buffered to pH 3.5–4.5 using citrate buffer and protected from light in amber glass or high-density polyethylene bottles. Because isoprenaline is susceptible to oxidative losses in the presence of trace copper and iron from tap water, purified water rather than potable water is used as the diluent; edetate disodium is added at 0.01% w/v to reduce metal-catalysed degradation. The product is not suitable for mixing with alkaline syrups, antacids, or high-pH flavouring bases that raise the microenvironment pH and cause rapid discolouration. A calibrated oral dosing syringe is supplied with the dispensed formulation, and the label states the exact milligram strength per 0.1 mL to prevent dosing errors; use of a household teaspoon is not acceptable. When dilution from a stock solution occurs at the clinic, the diluted product is assigned a default beyond-use date of 14 days under refrigeration according to general compounding standards, but a longer or shorter period may be justified only by stability-indicating assay data from the specific formulation.
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Isoprenaline veterinary grade API for tablets, injections, capsules, powders, granules, premix, and solutions is supplied as the hydrochloride salt of 4-[1-hydroxy-2-(isopropylamino)ethyl]benzene-1,2-diol, CAS 51-30-9, molecular formula C11H17NO3·HCl, molecular weight 247.72 g/mol. The product is designated VET-ISP-HCl API for compendial-grade supply. The substance is a white or almost white, odourless crystalline powder; the hydrochloride salt is freely soluble in water, sparingly soluble in ethanol, and practically insoluble in methylene chloride. The catechol group imposes specific handling constraints because oxidation is accelerated in alkaline solution, by light exposure, by dissolved oxygen, and by trace transition-metal ions. The API is therefore controlled for appearance, clarity and colour of solution, pH, loss on drying, related substances by HPLC, residual solvents, sulfated ash, and assay on the anhydrous basis. Typical release specifications require assay between 98.0–101.0% w/w on the anhydrous basis and water content not exceeding 0.5%. Residual solvent and elemental impurity limits are aligned with Ph. Eur. 2.4.24 and ICH Q3D where the intended route is parenteral.
The API is supplied with a certificate of analysis that includes loss on drying determined by Ph. Eur. 2.2.32, Karl Fischer water content by Ph. Eur. 2.5.12, sulfated ash by Ph. Eur. 2.4.14, related substances and assay by HPLC under Ph. Eur. 2.2.29, and UV identification under Ph. Eur. 2.2.25. Residual solvents are reported against the current general chapter Ph. Eur. 2.4.24. For injectable applications, the vendor specification adds bacterial endotoxins by Ph. Eur. 2.6.14 and a declared limit based on the maximum veterinary dose. The product is not a finished veterinary medicine and is supplied only for further pharmaceutical processing or compounding into authorised or legally prepared veterinary dosage forms.
For tablets, capsules, powders, granules, and premixes, particle-size distribution is the primary material attribute controlling blend uniformity and dose precision. Isoprenaline hydrochloride is a low-density, cohesive powder with poor native flow. Laser diffraction under Ph. Eur. 2.9.31 is used to control D10, D50, and D90; a D90 of 150 µm or below is a common applicant specification for direct compression and capsule filling, while a micronised grade with D90 below 25 µm is required for low-dose tablets with acceptable content uniformity. Bulk and tapped density values obtained by Ph. Eur. 2.9.34 typically yield a Hausner ratio above 1.35 for unmilled material, indicating that wet or dry granulation is necessary to stabilise die filling and tablet weight control. On production-scale rotary tablet presses, batch-to-batch flow variation is reduced by adding colloidal silicon dioxide at 0.1–0.5% w/w, but high-shear pre-blending is avoided because the low-density API may be entrained in dust extraction systems.
Capsule filling with this API requires a free-flowing granulate or powder blend to avoid weight variation and punch-die segregation. Direct-filled capsules are feasible only when the API is pre-dispersed at low concentration in a carrier of suitable particle size and low electrostatic charge, such as lactose monohydrate or microcrystalline cellulose. Granulation is conducted in a high-shear granulator or fluid-bed processor; the granulation liquid is a non-alkaline binder solution because alkaline pH accelerates catechol oxidation. Drying temperature is limited to an inlet air temperature not exceeding 50 °C in fluid-bed drying unless forced degradation data support a higher limit. The dried granulate is screened through a 0.8–1.2 mm sieve and lubricated with magnesium stearate at 0.25–1.0% w/w. Blend homogeneity is assessed by sampling at multiple positions; an RSD of not more than 5.0% for assay is applied for potent low-dose blends, although acceptance limits should be justified by the applicant from the finished-product specification.
Direct compression and dry granulation are preferred for moisture-sensitive processing because the catechol group degrades in the presence of free water. Dry granulation by roller compaction can be applied when the powder is pre-blended with a dry binder, but the equipment roll force and screen size must be controlled to avoid excessive fines and loss of flowability. The ribbon density is monitored because low-density ribbons produce granules that dissolve too slowly in wet mass or cause segregation during tablet compression. Published data for the size-reduction energy requirements of this API are limited; therefore, micronisation is performed only to the minimum particle size needed for content uniformity rather than as a general processing step.
Isoprenaline hydrochloride is incorporated into sterile aqueous solutions at concentrations typically between 0.02 mg/mL and 1.0 mg/mL, although published data for specific veterinary licensed formulations is limited. The hydrochloride salt is selected for sterile aqueous presentations because of its water solubility. The solution pH is adjusted to 3.5–4.5 with a suitable acid to stabilise the catechol and reduce oxidative degradation. Sodium metabisulfite or a comparable antioxidant is added in a declared concentration; the antioxidant content is controlled in the finished-product specification because sulfite loss during processing can reduce protection. The solution is protected from light and oxygen by using amber glass containers and nitrogen overlay during compounding and filling. The API solution should not be combined with alkaline buffer systems or strongly oxidising agents, and contact with iron, copper, or other transition-metal ions is minimised because trace metals catalyse oxidative discolouration.
Injectable manufacture uses aseptic filtration rather than terminal steam sterilisation as the primary sterilisation method because isoprenaline hydrochloride can degrade under moist heat. A sterilising-grade filter of 0.22 µm pore size is used under a Grade A environment with Grade B background, consistent with current EU GMP Annex 1. The sterilised solution is filled into depyrogenated amber glass vials or ampoules. Terminal sterilisation may be considered only if supplemented by forced degradation and thermal mapping data; otherwise, aseptic processing is mandatory. Release testing includes clarity and degree of opalescence by Ph. Eur. 2.2.1, degree of colour by Ph. Eur. 2.2.2, pH, assay and related substances, sterility by Ph. Eur. 2.6.1, bacterial endotoxins by Ph. Eur. 2.6.14, and particulate contamination by Ph. Eur. 2.9.19. The finished injectable should be stored protected from light and under conditions that limit oxidation; any change in solution colour or clarity is treated as an out-of-specification indicator.
For powders, granules, and premixes used in veterinary feed or oral mixing, the API is commonly dispersed in a non-alkaline carrier such as lactose monohydrate, mannitol, or microcrystalline cellulose. Calcium carbonate and other basic carriers are avoided because contact with alkaline surfaces accelerates catechol oxidation. Dry mixing is performed in twin-shell, double-cone, or ribbon blenders; for low-dose premixes, a staged geometric dilution is used to prevent segregation and to ensure that assay values across the batch remain within 90.0–110.0% of label claim. Homogeneity is tested at multiple sampling points by HPLC and the coefficient of variation is controlled to not more than 5.0% for a premix intended for subsequent feed dilution. If the premix is added to pelleted feed, the thermal and moisture exposure of the pelleting process should be evaluated because published data for this specific configuration is limited.
The dry powder is hygroscopic enough to require low-humidity handling. At relative humidity above 60%, the powder may agglomerate and flow properties deteriorate; therefore, rooms are maintained at controlled relative humidity, and open handling is minimised. Packaging is aluminium-laminated foil with a desiccant to limit moisture uptake. Storage conditions are controlled at 15–25 °C unless the applicant’s stability data support alternative conditions. The powder must not be stored in contact with oxidising agents or under direct sunlight. For capsules and powder sachets, the finished product should be tested for related substances and assay after storage to confirm that the antioxidant system, if present, remains sufficient for the intended shelf life.
Isoprenaline is a synthetic non-selective beta-adrenoceptor agonist with direct beta1 and beta2 activity and comparatively weak alpha-adrenergic activity. This distinguishes it from adrenaline, which activates alpha- and beta-adrenoceptors and therefore produces vasoconstriction at alpha1 receptors, and from noradrenaline, which is predominantly alpha-adrenergic with beta1 activity. In veterinary use, isoprenaline has been used for its positive chronotropic and inotropic effects in selected bradyarrhythmias and high-grade atrioventricular block; its beta2 activity also produces bronchodilation. In contrast, salbutamol is a selective beta2 agonist with less beta1-mediated tachycardia at therapeutic doses. The non-selective profile of isoprenaline can provoke excessive heart rate, hypotension due to beta2-mediated vasodilation, and arrhythmia; therefore, it is not interchangeable with salbutamol or adrenaline in formulations or clinical protocols. Published species-specific veterinary pharmacokinetic data is limited, so dose and dosage-form choices are based on clinical monitoring and existing pharmacopoeial quality standards rather than on a single veterinary regulatory monograph.
The same API can be used across tablets, injections, capsules, powders, granules, premixes, and solutions, but the release testing emphasis changes with the dosage-form matrix. The following compliance matrix summarises the primary API-related controls for solid oral, sterile, and premix applications.
| Dosage-form matrix | Critical API-derived control | Method or standard reference |
|---|---|---|
| Tablets and capsules | Particle-size distribution, bulk/tapped density, loss on drying, related substances, assay, residual solvents | Ph. Eur. 2.9.31, Ph. Eur. 2.9.34, Ph. Eur. 2.2.32, Ph. Eur. 2.2.29, Ph. Eur. 2.4.24 |
| Injections and solutions | Clarity, colour, pH, related substances, bacterial endotoxins, sterility, particulate contamination | Ph. Eur. 2.2.1, Ph. Eur. 2.2.2, Ph. Eur. 2.2.29, Ph. Eur. 2.6.14, Ph. Eur. 2.6.1, Ph. Eur. 2.9.19 |
| Powders, granules, and premixes | Blend homogeneity, loss on drying, related substances, assay, microbial enumeration | Ph. Eur. 2.2.32, Ph. Eur. 2.2.29, Ph. Eur. 2.6.12, Ph. Eur. 2.6.13 |
The API is released only after all specified parameters meet the applicant-approved specification. Deviations in water content, related substances, or solution colour are not accepted into sterile processing because these shifts indicate oxidative degradation or moisture ingression. Batch-to-batch reproducibility is monitored against reference chromatograms and solid-state reference samples. The manufacturer’s certificate of analysis is cross-checked by the receiving facility using incoming identification and water content testing before use in production.
