| HS Code | 457969 |
| Productname | Prednisolone Acetate Pharma Grade API |
| Chemicalname | 11β,17α,21-Trihydroxypregna-1,4-diene-3,20-dione 21-acetate |
| Casnumber | 52-21-1 |
| Molecularformula | C23H30O6 |
| Molecularweight | 402.48 g/mol |
| Appearance | White to almost white crystalline powder |
| Solubility | Practically insoluble in water; slightly soluble in alcohol; soluble in chloroform |
| Meltingpoint | Approximately 213°C to 220°C with decomposition |
| Specificopticalrotation | Approximately +112° to +119° |
| Assaybyhplc | 97.0% to 102.0% on dried basis |
| Storageconditions | Store in airtight containers, protected from light, at controlled room temperature |
| Grade | Pharma Grade |
| Suitabledosageforms | Tablet, capsule, granule, and injection |
As an accredited Prednisolone Acetate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable factory, we enforce strict quality protocols—every batch undergoes rigorous testing to ensure consistent efficacy and safety standards.
| Packing | Prednisolone Acetate Pharma Grade API is packaged in 25 kg sealed drums with double polythene lining, ensuring stability for oral and injectable formulations. |
| Container Loading (20′ FCL) | Container Loading (20′ FCL) securely packs Prednisolone Acetate Pharma Grade API in sealed drums/pallets into a 20-foot container for safe transport. |
| Shipping | Prednisolone Acetate Pharma Grade API ships in sealed, inert containers to maintain purity and stability. Shipments follow cold-chain or controlled-temperature guidelines as required, with moisture-proof, light-protective packaging. Handling includes tamper-evident labeling, proper documentation, and strict compliance with international pharmaceutical and hazardous material regulations. |
| Storage | Store in a well-closed container in a cool, dry place, protected from light and moisture. Recommended storage temperature: 15–30°C (room temperature). Keep away from heat, sparks, and incompatible substances. Ensure compliance with pharmacopeial guidelines and maintain integrity of the API for oral and injectable formulations. |
| Shelf Life | Shelf life: 24 months from manufacture when stored below 30°C, protected from light and moisture in original container. |
Direct compression of low-dose prednisolone acetate tablets demands a pre-blend step and controlled API particle size because the API is incorporated at 0.5–5.0% w/w of the core mass, with core masses typically 80–120 mg for 1 mg, 2.5 mg, and 5 mg strengths. The pre-blend is held at 5–10% w/w API in spray-dried lactose monohydrate or microcrystalline cellulose before main blending to reduce segregation. Content uniformity is assessed under USP <905> with an acceptance value not exceeding 15, and dissolution is controlled by USP <711> Apparatus II at 75 rpm in 900 mL of pH 6.8 phosphate buffer containing 0.5% w/v sodium lauryl sulfate. Residual solvents are managed under USP <467>, elemental impurities under ICH Q3D, and in-process controls under 21 CFR 211.110(a). Production-scale compression uses a 45-station rotary tablet press with 9.5 mm round B-tooling, force feeder paddle speed 30–40 rpm, pre-compression 8–12 kN, and main compression 12–20 kN. Tablet hardness is held at 6–10 kp, and friability is kept at ≤1.0% according to USP <1216>. Blending and compression are conducted at ambient relative humidity below 60%; if relative humidity exceeds 60%, excipient pre-drying to moisture below 2.0% is required. Segregation-related content uniformity drift is controlled by limiting blender fill volume to 50–65% of shell capacity and avoiding bin blender discharge rotations below 60 rpm. Field failures in this dosage category are traced to agglomerated API particles with volume-median diameter D90 above 20 µm, which produce localized superpotent granules and release failures at the 2.5 mg strength. The terminal product types are immediate-release tablets in 1 mg, 2.5 mg, and 5 mg strengths, packaged in PVC/aluminium blisters or HDPE bottles with desiccant.
For anhydrous capsule formulations containing prednisolone acetate at 2–15% w/w, roller compaction is preferred over direct fill when bulk density control and flow consistency are critical. The API is dry-blended with pregelatinized starch and anhydrous dicalcium phosphate in a bin blender at 60% fill volume, then compacted on a roller compactor with ribbed rolls at 40–60 bar roll pressure and 2–3 mm roll gap, followed by screening through a 1.0 mm screen. The resulting granules are lubricated with 0.5–1.0% w/w magnesium stearate and filled into hard gelatin or HPMC capsules using a dosator or tamping-pin encapsulator at 30,000–60,000 capsules/h. Capsule fill weights range from 100–300 mg for 5 mg, 10 mg, and 20 mg strengths. Uniformity is verified against USP <905>, dissolution against USP <711> using Apparatus I or II in 900 mL of 0.5% w/v sodium lauryl sulfate in pH 6.8 medium, and residual solvents under USP <467>. The terminal product types are immediate-release hard capsules in 5 mg, 10 mg, and 20 mg strengths, packaged in aluminium/aluminium or PVC/PVDC blisters. Slugging is not recommended for this low-dose corticosteroid because of die-splitting and measurable weight variance exceeding 2.0% RSD in production runs.
If single-dose oral granules are manufactured with prednisolone acetate at 0.2–5.0% w/w of sachet fill weight, the process is normally a top-spray fluidized-bed granulation using an aqueous binder solution of hypromellose at 2–5% w/w of dry granulate mass. The sachet fill weight ranges from 500 mg to 2,000 mg, with API strengths of 1 mg, 2.5 mg, and 5 mg per sachet. Granulation is executed at inlet air temperature 60–70 °C, product temperature 30–35 °C, and spray rate 10–20 g/min/kg of batch mass, with endpoint loss on drying controlled at 1.5–2.5%. Exceeding a product temperature of 35 °C during spray drying yields friable granules and increases residual fines below 0.180 mm, which raises sachet fill weight variability to >3.0% RSD on volumetric fillers. Mass uniformity is verified under Ph.Eur. 2.9.5, dissolution under USP <711>, particle size distribution under USP <786> with sieve stack limits of 0.180–0.850 mm, and elemental impurities under ICH Q3D. The finished goods are single-dose sachet or stick-pack granules for oral administration or reconstitution in water, in 1 mg, 2.5 mg, and 5 mg strengths with a reconstitution volume target of 5–10 mL. Processing-equipment bottlenecks are frequently observed when the filter bag of the fluid bed becomes blinded at loss-on-drying above 2.5%, causing defluidization and non-uniform granule growth.
Sterile aqueous injectable suspensions of prednisolone acetate are manufactured with micronized API at 1.0–5.0% w/w of the finished suspension, equivalent to 10–50 mg/mL prednisolone acetate. The suspension vehicle is typically composed of polysorbate 80 at 0.1–0.2% w/w, polyethylene glycol 3350 at 2–3% w/w, sodium chloride for isotonicity at 0.8–0.9% w/w, and water for injection to volume; antimicrobial preservatives are added only when a multidose presentation is registered under 21 CFR 211.167. The API particle size is reduced by wet milling or high-pressure homogenization to a volume-median diameter D50 of 1–5 µm and D90 below 10 µm, because larger crystal populations cause syringeability failures and settle into cemented cakes. The vehicle is sterilized by terminal steam sterilization at 121 °C for 15 min; the API is aseptically dispersed through a sterile transfer line after dry-heat sterilization at 160 °C for 120 min, and the suspension is filled aseptically into depyrogenated glass vials under EU GMP Annex 1. Terminal steam sterilization of the finished suspension requires revalidation because it can induce aggregate growth and shift D90 above 25 µm, creating visible particulates. Release testing includes sterility per USP <81>, bacterial endotoxins per USP <85> with a limit of NMT 2.5 EU/mg of prednisolone acetate, subvisible particulate matter per USP <788> with limits of ≤6,000 particles/vial at ≥10 µm and ≤600 particles/vial at ≥25 µm, visible particulates per USP <790>, and syringeability through a 21 G needle using a glide force not exceeding 5 N. The terminal presentations are single-dose vials and prefilled syringes at 25 mg/mL and 50 mg/mL; multidose vials are limited to formulations with preservative efficacy validated under USP <51> and a maximum beyond-use period of 28 days.
| Release test | Standard designation | Typical target |
|---|---|---|
| Sterility | USP <81> | No growth |
| Bacterial endotoxins | USP <85> | NMT 2.5 EU/mg |
| Subvisible particulate matter | USP <788> | ≤6,000 particles/vial at ≥10 µm; ≤600 particles/vial at ≥25 µm |
| Visible particulates | USP <790> | Free from visible particulates |
| Syringeability | 21 G needle glide force | ≤5 N |
Prednisolone acetate is granulated in a high-shear mixer at 5–20% w/w of the tablet core mass when doses of 10 mg or 20 mg and core masses of 150–400 mg are produced. The binder solution, usually povidone K30 at 2–5% w/w of dry granulate, is added at 3–8% w/w; wet massing proceeds with impeller speed 200–400 rpm and chopper speed 1,500–3,000 rpm for 2–5 min. The wet mass is dried in a fluid-bed dryer at inlet air 60–70 °C to loss-on-drying 1.0–2.0%, then milled through a 0.8 mm conical mill. The milled granulate is lubricated with 0.5–1.0% w/w magnesium stearate and compressed on a rotary press at 10–18 kN main compression, producing tablet hardness 8–12 kp and friability ≤0.8%. Granule particle size is controlled between 0.125 mm and 0.850 mm; fines below 0.125 mm are limited to ≤15% w/w to preserve die-fill consistency. Content uniformity is assessed by USP <905>, dissolution by USP <711> Apparatus II, mass uniformity by Ph.Eur. 2.9.5, and process deviations are recorded under 21 CFR 211.110(a). The finished products are 10 mg and 20 mg immediate-release tablets in HDPE bottles and blister lines with area-integrity testing.
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Prednisolone Acetate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable is supplied as a white to off-white crystalline powder with the chemical identity 21-acetate of 11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione, CAS 52-21-1, molecular formula C23H30O6, and relative molecular mass 402.49 g/mol. The product is assigned three industrial model designations: PRED-A-100 for direct-compression oral solid formulations, PRED-A-200 for wet-granulation and capsule filling, and PRED-A-300 for sterile-milled injectable suspensions. Each model is manufactured under ICH Q7 active pharmaceutical ingredient GMP requirements and is released against the United States Pharmacopeia/National Formulary Prednisolone Acetate monograph and the European Pharmacopoeia Prednisolone Acetate monograph. The acetate ester substitution at C21 reduces aqueous solubility relative to prednisolone base and prednisolone sodium phosphate; this physicochemical difference is the primary formulation determinant for the oral and injectable dosage forms addressed in this document. The API is intended for further pharmaceutical processing and is not supplied as a finished dosage form.
For the USP/NF monograph, assay is determined by high-performance liquid chromatography under USP 〈621〉 and must fall within 97.0% to 103.0% on the dried basis. Optical rotation by USP 〈781S〉 is controlled between +112° and +119° when measured at 25 °C in dioxane; the exact acceptance interval should be verified against the current monograph because compendial revisions may adjust the lower bound. Identification relies on infrared absorption spectrophotometry USP 〈197K〉 or Ph. Eur. 2.2.24, thin-layer chromatographic identity, and the retention time match in the assay chromatogram. Loss on drying is measured at 105 °C for 3 h under USP 〈731〉 and is typically not more than 1.0%. Residue on ignition by USP 〈281〉 is not more than 0.1%. Related substances are controlled by liquid chromatography: specified impurity limits are typically not more than 0.5% for any individual specified impurity and not more than 1.0% total impurities. Elemental impurities are assessed under ICH Q3D, and residual solvents under USP 〈467〉 or Ph. Eur. 5.4, with class 2 solvent limits such as methanol not more than 3000 ppm, ethanol not more than 5000 ppm, and dichloromethane not more than 600 ppm where process solvents are used. The injectable grade requires additional release controls for bacterial endotoxins, sterility, and particulate matter; these are described under the injectable processing section.
Prednisolone acetate exhibits cohesive powder behavior after jet-milling at D90 values below 30 µm, and direct-compression formulations require dry blending with pregelatinized starch, microcrystalline cellulose, or lactose monohydrate to limit segregation. The micronized grade PRED-A-100 is controlled to D90 ≤ 30 µm and D50 3–15 µm to support content uniformity in low-dose tablets under USP 〈905〉; however, published data for this specific model designation is limited, and the particle-size distribution limits are supplied through the manufacturer’s technical dossier. Flow function coefficient measured by annular shear cell may remain below 2.0 if unprocessed, so wet granulation with hypromellose or povidone solution is commonly selected for oral solid manufacture. The granule-grade PRED-A-200 is controlled to D90 ≤ 45 µm after de-agglomeration and is intended for capsule filling and roller-compacted granulation. Loss on drying for all oral grades should be rechecked after exposure to ambient humidity above 60% RH because the crystalline form is not expected to behave as a hydrate; conditioning at 25 °C/60% RH before weighing is standard. On compression lines, flow function coefficients below 2.0 are associated with bridging in gravity-fed hoppers; loss-in-weight feeders with mechanical stirrers are specified for direct-compression blends containing the micronized API.
| Model designation | Target process | Particle-size control | Additional release controls |
|---|---|---|---|
| PRED-A-100 | Tablet direct compression | D90 ≤ 30 µm; D50 3–15 µm | USP 〈621〉, USP 〈731〉, USP 〈281〉, USP 〈467〉 |
| PRED-A-200 | Capsule/granule | D90 ≤ 45 µm; D50 5–20 µm | USP 〈905〉, USP 〈711〉, USP 〈621〉 |
| PRED-A-300 | Injectable suspension | D90 ≤ 20 µm; D50 2–5 µm | USP 〈788〉, USP 〈85〉, USP 〈71〉, USP 〈621〉 |
Where sterile-milled PRED-A-300 is used in injectable suspensions, the API is not rendered soluble by terminal heat; the formulation is a sterile aqueous suspension containing a wetting agent, a suspending agent such as sodium carboxymethylcellulose, and an isotonicity agent. Endotoxin limits follow USP 〈85〉, with a typical acceptance criterion of not more than 0.50 EU/mg for intra-articular or intralesional administration, and sterility is confirmed by USP 〈71〉 membrane filtration. Particulate matter in the final injection is controlled under USP 〈788〉; visible particles must be absent in the constituted suspension and subvisible particle counts must meet the large- and small-volume parenteral thresholds. The API particle-size distribution for injectable suspensions is typically controlled to D90 ≤ 20 µm to prevent needle occlusion through 21-gauge or smaller needles and to minimize sedimentation caking. Syringeability studies on production batches with 25-gauge needles have shown that D50 above 20 µm increases obstruction risk; hence the D90 limit is enforced rather than D50 alone. Aqueous suspension pH is targeted between 5.0 and 7.5 to minimize ester hydrolysis; hydrolytic degradation of prednisolone acetate in aqueous suspension follows pseudo-first-order kinetics and accelerates above pH 7.5. Terminal moist-heat sterilization of the final suspension is not a first-line choice because it may accelerate acetate ester cleavage and cause particle agglomeration; aseptic processing is therefore standard.
Selection between prednisolone acetate and prednisolone sodium phosphate is controlled by aqueous solubility and release duration. Prednisolone sodium phosphate is freely water-soluble and can be formulated as an aqueous solution for intravenous or intramuscular injection; prednisolone acetate is practically insoluble in water and forms a suspension depot after intramuscular, intra-articular, or intralesional injection. The acetate ester hydrolyzes at the injection site and releases prednisolone over a prolonged interval, whereas the phosphate ester provides rapid systemic availability. Differences in finished-product specifications follow: aqueous solution products require clarity and pH controls under USP 〈1〉 and USP 〈791〉, while suspension products require resuspendability, sedimentation volume, and particulate-size controls under USP 〈788〉. For oral solid dosage forms, prednisolone acetate is chosen when dissolution-controlled delivery is required; the practically insoluble acetate form slows in vitro release compared with prednisolone base or prednisolone sodium phosphate, and dissolution testing under USP 〈711〉 with surfactant-containing media is used to distinguish formulation variants. Prednisone is not interchangeable without considering hepatic conversion, because prednisone requires 11β-hydroxysteroid dehydrogenase type 1 reduction to prednisolone; prednisolone acetate supplies the active glucocorticoid after ester hydrolysis. Methylprednisolone acetate is a different glucocorticoid ester with higher lipophilicity and different salt-retaining activity; it is not a milligram-equivalent substitute.
Long-term and accelerated stability studies for prednisolone acetate API are conducted according to ICH Q1A(R2) at 25 °C/60% RH and 40 °C/75% RH. The API is packaged in double polyethylene liners inside fiber drums or in aluminum-laminated bags; the primary moisture barrier must limit water vapor transmission to not more than 0.1 g/m²/day to prevent moisture uptake above the loss-on-drying specification. Under accelerated storage, related substances may increase through hydrolytic cleavage of the 21-acetate ester to prednisolone; the specified degradation product prednisolone is quantified in the related-substances method. Forced degradation studies under 0.1 M hydrochloric acid, 0.1 M sodium hydroxide, 3% hydrogen peroxide, and thermal stress identify ester hydrolysis as the major degradation pathway. Photostability is evaluated under ICH Q1B; the solid is protected from light because light exposure may promote oxidation at the dihydroxyacetone side chain. Bulk storage temperature is controlled at 15–25 °C with excursions permitted only within the labeled range; humidity exposure during sampling is minimized by dry-box handling when ambient RH exceeds 60%. Retest periods are assigned based on statistically analyzed long-term data, typically 24 to 36 months for unopened containers. Aqueous suspension stability is evaluated separately from the dry API because the dispersion medium introduces pH-dependent hydrolysis and sedimentation behavior.
