| HS Code | 368769 |
| Chemical Name | Prostaglandin F2α (Dinoprost) |
| Cas Registry Number | 551-11-1 |
| Molecular Formula | C20H34O5 |
| Molecular Weight | 354.48 g/mol |
| Grade | Veterinary grade |
| Appearance | White to off-white crystalline powder |
| Solubility | Soluble in ethanol and DMSO; poorly soluble in water |
| Storage Conditions | Store at -20°C, protected from light and moisture |
| Shelf Life | 24 months when stored unopened under recommended conditions |
| Purity | ≥98% (HPLC) |
| Mechanism Of Action | Luteolytic prostaglandin F2α receptor agonist causing corpus luteum regression |
| Veterinary Indications | Estrus synchronization, luteolysis, induction of parturition, and treatment of reproductive disorders |
| Compatible Dosage Forms | Tablets, injections, capsules, powders, granules, premix, and solutions |
As an accredited Prostaglandin F2α Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions factory, we enforce strict quality protocols—every batch undergoes rigorous testing to ensure consistent efficacy and safety standards.
| Packing | Packaged in 25 kg sealed drums with double polyethylene liners, ensuring stability and purity for veterinary pharmaceutical formulations. |
| Container Loading (20′ FCL) | 20′ FCL: temperature-controlled, moisture-proof, palletized drums of Prostaglandin F2α veterinary API, secured for safe transit. |
| Shipping | Shipments of Prostaglandin F2α Veterinary Grade API are handled under strict temperature-controlled, secure conditions. Product is packaged in sealed, inert containers with desiccant, labeled per hazardous material regulations. Cold-chain logistics and tamper-evident protocols ensure stability, sterility, and safe delivery for pharmaceutical manufacturing use. |
| Storage | Store in the original tightly sealed container in a cool, dry, well-ventilated area, protected from light, moisture, and heat. Maintain temperatures between 2–8°C if supplied refrigerated; otherwise avoid freezing and excessive warmth. Keep away from incompatible substances and ensure the container is securely closed after each use. |
| Shelf Life | Stable for 24 months when stored as directed in unopened containers, protected from light and moisture. |
PGF2α veterinary-grade API is supplied as dinoprost tromethamine crystalline powder and is processed into sterile aqueous injection solutions for luteolysis and uterine evacuation. Oral tablet and capsule formats are excluded from the current downstream matrix because extensive first-pass metabolism and gastrointestinal smooth-muscle effects are not supported by approved veterinary monographs. The following applications are limited to documented parenteral and intrauterine routes in food-producing and companion animal species.
Dinoprost tromethamine powder is dissolved in Water for Injection chilled to 8–12°C inside a jacketed stainless-steel vessel fitted with bottom-mounted magnetic agitation and a nitrogen overlay. The finished injection is compounded to 5.0 mg dinoprost base per mL, with benzyl alcohol as preservative at 9.0 mg per mL and sodium hydroxide or hydrochloric acid used only to trim pH into a 7.0–8.0 control band. At 500 L scale, the tromethamine salt dissolves rapidly without co-solvent, but process hold time between pH adjustment and sterile filtration is limited to 8 h at 2–8°C because prolonged aqueous hold increases pH-dependent degradation products measured as total unspecified impurities. The primary compliance anchors are 21 CFR 522.690 for the cattle indication, 21 CFR 211.42 for aseptic processing design, 21 CFR 211.167 for sterility assurance, and the USP monograph for Dinoprost Tromethamine Injection. In the European Economic Area, the same product is governed by Regulation (EU) 2019/6, and dinoprost is classified in Table 1 of Commission Regulation (EU) No 37/2010 as a substance for which no maximum residue limit is required for bovine and porcine tissues.
The downstream process uses sterile filtration through a 0.22 µm PVDF capsule; terminal steam sterilization is not used because prostaglandin F2α degrades under autoclave thermal load. The filtered solution is filled into USP Type I amber borosilicate glass vials at 10 mL, 30 mL, and 100 mL, closed with chlorobutyl stoppers and aluminium crimp caps, then inspected for particulate contamination under USP 788. Finished product types are multi-dose vials labelled as 5 mg/mL dinoprost injection for intramuscular administration at 25 mg per animal. Cold-chain storage at 2–8°C is required, and exposure to direct sunlight or freeze-thaw cycles must be prevented to avoid precipitation and loss of assay.
| Parameter | Reference value |
|---|---|
| Dinoprost base concentration | 5.0 mg/mL |
| Benzyl alcohol content | 9.0 mg/mL |
| Target pH band | 7.0–8.0 |
| Sterile filtration | 0.22 µm PVDF/PES |
| Primary packaging | USP Type I amber glass, 10/30/100 mL |
In sow unit applications, the injection is administered intramuscularly at 10 mg per sow to induce farrowing after day 112 of gestation, with the approved use documented in 21 CFR 522.690 and mirrored in the EU under Regulation (EU) 2019/6. The formulation addition ratio remains unchanged at 5.0 mg dinoprost base per mL with 9.0 mg/mL benzyl alcohol, but the filling line is often configured for 10 mL and 30 mL amber vials because the individual dose volume is only 2 mL. Fill-weight control is maintained within ±3% using peristaltic or rotary piston pumps with single-use silicone tubing. Foaming during compounding is the principal line-scale failure mode when the agitator creates vortex at speeds above 120 rpm; vacuum deaeration is avoided because it strips benzyl alcohol and shifts assay. Instead, low-speed subsurface mixing and headspace nitrogen are maintained until the product reaches the filling hold vessel.
Compliance for this segment includes 21 CFR 211.110 for in-process bioburden control, 21 CFR 211.166 for stability testing, and VICH GL3 for bracketing of container sizes in stability protocols. Sterile filtration uses a 0.22 µm PES or PVDF membrane, selected after product-specific filter validation because some nylon membranes produce low recovery at 5 mg/mL concentration. The terminal finished product is a multi-dose aqueous injection in 10 mL and 30 mL vials; no oral powder, premix, or feed additive form is generated for this approved porcine indication because the luteolytic dose requires parenteral delivery. Batches released for export to tropical markets are sometimes packaged with overwrap and desiccant, but cold-chain handling at 2–8°C is retained as a regulatory condition rather than a distribution recommendation.
In equine reproductive medicine, the 5.0 mg/mL preserved injection is used intramuscularly at 5–10 mg per mare to regress a mature corpus luteum and shorten diestrus. The luteolytic effect is confined to corpora lutea that are at least 5 days post-ovulation; before this threshold, FP receptor responsiveness on luteal cells is insufficient and injection does not reliably shorten the interovulatory interval. Regulatory status is extra-label in the United States under 21 CFR 530 and, in the EU, through the prescribing cascade under Articles 105–107 of Regulation (EU) 2019/6; no horse-specific approval exists for many dinoprost products. The formulation addition ratio remains 5.0 mg dinoprost base per mL with 9.0 mg/mL benzyl alcohol, filled into 10 mL and 30 mL vials by the same aseptic filtration route used for cattle products.
The downstream process for equine-destined product is identical in equipment and raw material inputs, but batch documentation differs: meat withdrawal language is replaced by a pregnant-handler contraindication, and some markets require a tamper-evident shrink-seal on the vial neck. Terminal finished product type is a sterile multi-dose injection stored at 2–8°C and protected from light; in-use stability after first stopper puncture is governed by preservative efficacy testing under USP 51, with a typical in-use limit of 28 days for a preserved multidose container. Published data for equine-specific formal stability at ambient equine clinic conditions are limited, so transport in validated cool-chain packaging is required until point of use.
Pyometra and chronic endometritis in dairy cattle are treated with intramuscular dinoprost injection because the compound lyses the persistent corpus luteum and removes progesterone support from the infected uterus. The finished product concentration is not different from the synchronization presentation: 5.0 mg dinoprost base per mL, 9.0 mg/mL benzyl alcohol, pH 7.0–8.0, Water for Injection q.s. The manufacturing process is therefore the identical aseptic filtration route through 0.22 µm PVDF, but the regulatory submission must include clinical data supporting the pyometra indication and the label must state the dose of 25 mg intramuscularly per cow. In the U.S., the approval is captured under 21 CFR 522.690; in the EU, the product falls under Regulation (EU) 2019/6 and the dinoprost residue classification in Commission Regulation (EU) No 37/2010 Table 1.
Line-scale experience in dairy veterinary channels shows that pyometra treatment demand is seasonal and batch sizes are often smaller, which introduces changeover validation concerns on multiproduct sterile fill lines. Residual API carryover from the filling needle manifold is controlled by flushing with Water for Injection and verifying total organic carbon below the site acceptance limit. The terminal finished products are 10 mL and 30 mL multi-dose vials with the same chlorobutyl closure system; single-dose syringes are not commonly produced because the approved dose is 5 mL per animal and multi-dose vials allow repeated use under farm conditions. In-use storage after first puncture is limited by sterility risk and preservative challenge testing under USP 51, and farm-level training must state that penetration of the vial with unsterile needles is a preventable source of bacterial contamination.
In small ruminant breeding systems, dinoprost injection is used off-label for luteolysis in ewes and does to synchronise oestrus, terminate pseudopregnancy, or manage missed oestrus under veterinary prescription. The compounded product is not a dedicated oral powder or granular premix; it remains the aqueous sterile injection at 5.0 mg dinoprost base per mL with 9.0 mg/mL benzyl alcohol, filled in 10 mL multi-dose vials. In the United States, extra-label use in sheep and goats as food-producing species is constrained by 21 CFR 530.20 and 21 CFR 530.41; in the EU, cascade use follows Articles 105–107 of Regulation (EU) 2019/6. The downstream manufacturing process for this segment is usually repackaging or secondary labelling rather than a dedicated small ruminant formula, because the approved cattle injection is used at reduced doses. Terminal product type remains a parenteral sterile solution; oral solid-dose formats are unsuitable due to extensive metabolism and gastrointestinal side effects. Published residue depletion data for sheep and goats are limited, so withdrawal intervals must be assigned by the prescribing veterinarian based on food-producing species data and applicable extra-label rules.
Competitive Prostaglandin F2α Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions prices that fit your budget—flexible terms and customized quotes for every order.
For samples, pricing, or more information, please contact us at +8615365186327 or mail to admin@ascent-chem.com.
We will respond to you as soon as possible.
Tel: +8615365186327
Email: admin@ascent-chem.com
Flexible payment, competitive price, premium service - Inquire now!
Prostaglandin F2α Veterinary Grade API is supplied as the endogenous prostaglandin dinoprost (CAS 551-11-1) and as the water-soluble dinoprost tromethamine salt (CAS 38562-01-5). The model designation PGF2α-VET-01 identifies the reference grade in this document; manufacturer-specific product codes may be appended for salt form, micronization grade, residual solvent class, and container size. The base has molecular formula C20H34O5 and molar mass 354.48 g/mol. The tromethamine salt contains 2-amino-2-(hydroxymethyl)propane-1,3-diol and has molar mass 475.60 g/mol. Salt-to-base conversion is performed using the factor 0.745. Identity is controlled by infrared spectroscopy and HPLC retention time against a qualified reference standard. Assay is performed by a stability-indicating HPLC procedure validated according to ICH Q2(R1) or the corresponding VICH guidance.
The API is a white to off-white crystalline powder when supplied as the tromethamine salt. The base is more lipophilic and may require low-temperature storage. Release specifications commonly include water content not more than 0.5% by Karl Fischer titration, residual solvents controlled to ICH Q3C or VICH GL18, and elemental impurities controlled to ICH Q3D daily exposure limits. Non-sterile API microbial quality is typically controlled with a total aerobic microbial count not more than 10² CFU/g and a total yeast and mold count not more than 10 CFU/g under USP <61>, with absence of Escherichia coli under USP <62>. Parenteral grades are not terminal-sterilized; the API is supplied with bioburden data and, where required, bacterial endotoxin data based on the finished product maximum dose.
Direct compression of dinoprost tromethamine tablets is constrained by low-dose content uniformity, the poor flow of micronized drug substance, and the moisture sensitivity of the prostaglandin skeleton. For a 5 mg base-equivalent tablet, the required unit dose of tromethamine salt is approximately 6.7 mg. At this level, a micronized grade with D90 not exceeding 20 µm is typically selected to reduce segregation. Pre-blending by geometric dilution in steps not exceeding 1:10 by mass is performed before final blending. Blending and compression rooms are maintained at relative humidity not more than 40%, and excipients are pre-dried when ambient RH exceeds 60%. The final blend is controlled to water activity below 0.3 to limit hydrolytic degradation. Content uniformity is evaluated according to USP <905>; process suitability is supported by blend uniformity sampling with acceptance at not more than 2.0% relative standard deviation for the active peak. Wet granulation with aqueous binders is generally avoided because low-pH granulating fluids accelerate dehydration to PGA2-type impurities. Dry granulation by roller compaction may be used if compaction force and residence time are controlled, but published data for this specific configuration is limited.
For capsule presentations, the tromethamine salt is blended with pregelatinized starch or lactose-based fillers and filled into hard gelatin or hydroxypropyl methylcellulose capsules. Enteric coating may be applied to retard acid-catalyzed degradation in the gastric environment, but oral administration is not the primary route because dinoprost undergoes extensive pulmonary and hepatic first-pass metabolism after absorption. Dissolution testing, where developed, is performed under USP <711>; method conditions must be product-specific because sink conditions for the base are difficult to maintain in aqueous media. Published data for oral capsule or tablet bioavailability in target species is limited; therefore, demonstration of clinical relevance would require additional species-specific pharmacokinetic studies.
Injectable solution manufacture uses Water for Injection as vehicle, with sodium chloride added for isotonicity. A nominal 5 mg/mL dinoprost base-equivalent solution is compounded using 6.71 mg of dinoprost tromethamine per mL. The pH is adjusted to 6.5–7.5; buffering is minimized because high buffer concentrations can accelerate the base-catalyzed epimerization pathway. The solution is sterilized by aseptic filtration through a 0.22 µm polyvinylidene fluoride or polysulfone membrane, after filter compatibility and product adsorption studies are performed. Terminal moist-heat sterilization is not preferred for this API because exposure to autoclave conditions increases dehydration impurities. Filling is conducted under nitrogen; headspace oxygen is maintained below 1.0% v/v. Primary containers are Type I borosilicate glass vials meeting USP <660>, with chlorobutyl stoppers. Storage at 2–8°C with protection from light is specified for the tromethamine salt; exposure to temperatures above 25°C should be limited to qualified excursions.
Therapeutic use in veterinary medicine is based on luteolytic action on the corpus luteum. The API reduces progesterone, allowing follicle maturation, estrus synchronization, and parturition induction in cattle and swine; it is also used in equine programs for luteolysis. Administration route and dose are finished-product-specific and species-specific; label data must be used because the API itself does not carry a therapeutic dose. For food-producing species, withdrawal periods are assigned through residue depletion studies conducted on the specific formulation and are not inferred from the API’s endogenous nature.
Dry presentations require protection from humidity, oxygen, and light. Powder and granule intermediates are produced by geometric dilution with a direct compression vehicle such as mannitol, lactose monohydrate, or microcrystalline cellulose. The active substance is added as a micronized or co-milled fraction; sieving through a 500 µm screen before blending reduces agglomerates. Premix manufacture for feed incorporation is controlled by first producing a concentrated premix, typically at 100 g/kg or 10% w/w, followed by sequential dilution to the target concentration. Homogeneity is verified by sampling at multiple locations after defined mixing intervals; acceptance criteria for coefficient of variation not exceeding 5.0% may be used for the premix assay, but the finished feed method must be validated for the specific matrix. Packaging for dry intermediates consists of double polyethylene liners inside an HDPE drum, vacuum-sealed under nitrogen with desiccant. Loaded containers are stored at 2–8°C for the tromethamine salt; the base form requires -20°C storage because it is more oxidation-prone. Handling operations exceeding 60% RH require pre-conditioning of the room to 35–40% RH before opening the container.
Feed premix stability is influenced by moisture, trace metals, and feed matrix components. Moisture ingress above 0.5% in premix can mobilize acid sites from mineral carriers and accelerate prostaglandin degradation. Trace iron and copper above 50 ppm in the premix may catalyze oxidation; chelating agents or antioxidants are sometimes added, but compatibility must be studied. Homogeneity is assessed with a sampling thief at not less than 10 points per blender. Feed processing at temperatures above 80°C is generally avoided because thermal generation of dehydration impurities becomes measurable. If published data for a specific feed matrix is unavailable, a matrix-specific stability study under VICH GL3 or regional equivalent is used.
| Parameter | Method or standard | Acceptance criterion |
|---|---|---|
| Appearance | Visual examination | White to off-white crystalline powder |
| Identification | Infrared spectroscopy and HPLC retention time | Positive against reference standard |
| Assay, anhydrous basis | Stability-indicating HPLC | 95.0%–105.0% for tromethamine salt |
| Water content | Karl Fischer titration per USP <921> | ≤ 0.5% |
| Related substances | HPLC | Total impurities ≤ 2.0%; any single unspecified impurity ≤ 0.5% |
| Residual solvents | VICH GL18 / ICH Q3C | Class 1 solvent limits as specified; methanol ≤ 3000 ppm if used |
| Elemental impurities | ICH Q3D or VICH equivalent | Daily exposure limits; no dedicated limit without finished product dose |
| Microbial limits | USP <61> / USP <62> | TAMC ≤ 10² CFU/g; TYMC ≤ 10 CFU/g; E. coli absent |
| Bacterial endotoxins, parenteral grade | USP <85> | Calculated from finished product maximum dose and route |
The principal difference between PGF2α and synthetic veterinary prostaglandins concerns metabolic fate and dose. PGF2α is endogenously present and is rapidly inactivated by 15-hydroxyprostaglandin dehydrogenase in pulmonary and hepatic tissue. Cloprostenol sodium, a synthetic 16-aryloxy analogue, is resistant to this pathway, which allows a lower administered mass per animal for equivalent luteolytic effect. Consequently, dinoprost and cloprostenol are not interchangeable on a milligram-for-milligram basis; product-specific residue, safety, and efficacy data are required before switching. Another difference is aqueous solubility: the tromethamine salt of dinoprost is freely soluble, whereas the base is not, and therefore the salt is selected for injectable and solution formulations. Solid oral presentations of PGF2α are limited by extensive first-pass metabolism, and published data for oral tablet or capsule bioavailability in target species is limited compared with parenteral data. Powders, granules, and premixes are used largely as production intermediates rather than final feed-grade products because the API is potent and light-sensitive.
| Product or class | Key structural feature | Aqueous solubility behavior | Formulation consequence |
|---|---|---|---|
| PGF2α base | Endogenous prostanoic acid | Low water solubility | Requires organic solvent or cyclodextrin for solution; store cold |
| Dinoprost tromethamine | 1:1 salt with tromethamine | Freely soluble in water | Standard for injection; use 0.745 salt-to-base factor |
| Cloprostenol sodium | Synthetic 16-aryloxy analogue | Water-soluble | Lower dose, metabolically stable; not interchangeable |
| Luprostiol / alfaprostol | Synthetic prostaglandin analogues | Variable solubility | Limited comparative public data for solid dosage |
pH is the most critical solution variable during aseptic manufacture. When the solution pH exceeds 7.5, the rate of C-15 epimerization increases, and storage can generate 15-epi dinoprost, a stereoisomer with reduced biological activity. When pH falls below 4.0, acid-catalyzed dehydration forms PGA2- and PGB2-type impurities. The specification window is therefore set at 6.5–7.5 for most injectable presentations; pH adjustment is performed with dilute hydrochloric acid or tromethamine solution. Terminal steam sterilization at 121°C for 15 min is not used because thermal degradation exceeds the impurity threshold. Aseptic filtration through a 0.22 µm membrane remains the standard method. During scale-up, temperature during high-shear mixing should be kept below 25°C, and nitrogen blanketing should be maintained until the vials are sealed. Incorrect pH adjustment is a known batch failure mode in commercial production because degradation kinetics are rapid outside the stated window, especially when oxygen is present. The API is incompatible with strong oxidizing agents, acid chlorides, and alkaline earth salts; formulation contact surfaces should be stainless steel 316L or borosilicate glass.
The veterinary API is manufactured under EudraLex Volume 4 Part II and supported by a drug master file or active substance master file. Finished dosage forms are prepared under 21 CFR 211 or corresponding national rules. Stability studies follow VICH GL3; photostability follows VICH GL5, which corresponds to ICH Q1B. Specifications are justified against the compendial monograph for dinoprost tromethamine where applicable, and batch-to-batch consistency is controlled through trend analysis of assay, related substances, water content, and particle size.
