Lurasidone Intermediate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable
- Product Name: Lurasidone Intermediate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable
- Factroy Site: Yudu County, Ganzhou, Jiangxi, China
- Price Inquiry: sales10@sinochem-nanjing.com
- Manufacturer: Ascent Petrochem Holdings Co., Limited
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- Lurasidone Intermediate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable is typically used in formulations when particle size distribution, polymorphic form, and bulk density and residual solvent content, moisture content, and impurity profile must be controlled within specific ranges.
| HS Code | 794274 |
| Product Name | Lurasidone Intermediate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable |
| Product Type | Pharmaceutical intermediate/API |
| Cas Number | 367514-87-2 |
| Chemical Formula | C28H36N4O2S |
| Molecular Weight | 492.68 g/mol |
| Grade | Pharma Grade |
| Assay Purity | ≥99.0% |
| Appearance | White to off-white crystalline powder |
| Solubility | Soluble in dimethyl sulfoxide, methanol, ethanol; slightly soluble in water |
| Storage Conditions | Store in a cool, dry, well-ventilated place protected from light; 2-8°C recommended |
| Shelf Life | 24 to 36 months |
| Dosage Form Compatibility | Tablet, Capsule, Granule, Injection |
| Route Of Administration | Oral, Injectable |
| Therapeutic Category | Atypical antipsychotic |
| Mechanism Of Action | Dopamine D2 and serotonin 5-HT2A receptor antagonist |
| Packaging | Double polyethylene bag inside fiber drum |
| Moisture Content | ≤0.5% |
| Heavy Metals | ≤20 ppm |
| Residual Solvents | Complies with ICH Q3C |
| Impurity Profile | Individual impurity ≤0.1%; total impurities ≤0.5% |
| Particle Size | D90 ≤ 50 µm |
| Microbial Limits | Total aerobic microbial count ≤1000 CFU/g |
| Endotoxin | ≤0.5 EU/mg for injectable grade |
| Sterility | Sterile grade available for injectable use |
| Ph | 5.0 to 7.0 for 1% suspension |
| Melting Point | >200°C with decomposition |
| Hygroscopicity | Non-hygroscopic |
| Regulatory Status | Manufactured under cGMP and ICH guidelines |
| Manufacturing Standard | cGMP, ICH Q7 |
| Optical Rotation | -40° to -50° |
| Density | Approx. 1.2 g/cm³ |
As an accredited Lurasidone Intermediate 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 | Lurasidone intermediate pharma-grade API packaged in 25 kg double-lined fiber drums with moisture-barrier bags for tablet, capsule, granule, oral, and injection use. |
| Container Loading (20′ FCL) | 20' FCL container loaded with pharma-grade Lurasidone intermediate API; suitable for tablets, capsules, granules, oral and injectable formulations, securely stowed. |
| Shipping | Lurasidone Intermediate Pharma Grade API is shipped in sealed, inert-lined drums or double-LDPE bags under controlled conditions. Maintain specified temperature, protect from moisture, light, and contamination. Include batch records, MSDS, and temperature monitoring. Follow GDP, IATA/ADR, and customs regulations for oral, injectable, tablet, capsule, granule, and injection applications. |
| Storage | Store Lurasidone Intermediate Pharma Grade API in tightly closed, original containers in a cool, dry, well-ventilated area at controlled room temperature (20–25°C; excursions 15–30°C), protected from light and moisture. Keep away from heat, ignition sources, oxidizers, and incompatible materials. Maintain cGMP segregation, cleanliness, and labeled quarantine status. For injectable use, follow additional sterile/controlled storage requirements. Do not store near food or drink. |
| Shelf Life | Shelf life: generally 24–36 months under recommended storage; protect from light, moisture, and heat in sealed original container. |
Lurasidone hydrochloride is incorporated into immediate-release film-coated tablets at label strengths equivalent to 20 mg, 40 mg, 60 mg, 80 mg, and 120 mg of lurasidone free base per unit. Because the salt-to-base conversion factor is 1.074, the corresponding lurasidone hydrochloride input per tablet is 21.48 mg, 42.96 mg, 64.43 mg, 85.91 mg, and 128.87 mg. The direct-compression matrix combines the API with mannitol, pregelatinized starch, croscarmellose sodium, hypromellose, and magnesium stearate; croscarmellose sodium is held at 2–4% w/w for disintegration, and magnesium stearate is limited to 0.5–1.0% w/w to avoid dissolution retardation. The API is pre-sieved through a 30-mesh stainless steel screen and blended in a V-blender or bin blender with an intensifier bar for 10–15 minutes at 12–18 rpm; magnesium stearate is added in the final 3 minutes. Compression is performed on a rotary tablet press with precompression rolls at precompression force 4–8 kN and main compression force 10–25 kN, targeting tablet hardness 80–120 N, friability ≤1.0% per USP <1216>, and disintegration ≤15 minutes per USP <701>. The aqueous film-coating step uses Opadry II in a perforated pan coater with inlet air temperature 55–70 °C, exhaust air temperature 35–45 °C, and a weight gain of 2–4% w/w. The unit operation sequence follows the RLD inactive composition; press parameters are standard rotary press qualification ranges for mannitol-based immediate-release matrices and require lurasidone-specific confirmation during scale-up. Compliance is verified against USP <905> content uniformity, USP <711> dissolution, FDA 21 CFR 211.165, and ICH Q3D elemental impurities. Terminal product type: film-coated immediate-release tablet.
| Label claim (lurasidone free base) | Lurasidone HCl quantity per unit | USP <905> acceptance value | USP <701> disintegration limit |
|---|---|---|---|
| 20 mg | 21.48 mg | ≤15.0 | ≤15 min |
| 40 mg | 42.96 mg | ≤15.0 | ≤15 min |
| 60 mg | 64.43 mg | ≤15.0 | ≤15 min |
| 80 mg | 85.91 mg | ≤15.0 | ≤15 min |
| 120 mg | 128.87 mg | ≤15.0 | ≤15 min |
Why Does Roller Compaction Require Ribbon Density Above 0.9 g/cm³ for Lurasidone HCl Capsule Fill?
Hard gelatin capsule filling with lurasidone hydrochloride is limited by the API’s low bulk density and cohesive flow, which lead to segregation and fill weight variation when direct powder filling is attempted on dosator or tamping-pin machines. Published data for a commercial lurasidone HCl capsule product is limited; the roller compaction envelope below is derived from equipment capability for low-density poorly compressible APIs and must be verified with lurasidone-specific design-of-experiments. Roller compaction is introduced to produce a densified granulate with ribbon density controlled between 0.9 g/cm³ and 1.2 g/cm³; ribbons below 0.9 g/cm³ generate excessive fines after milling, while ribbons above 1.2 g/cm³ reduce compactability and may prolong disintegration. The roller compactor is operated with roll pressure 30–50 kN, roll speed 5–10 rpm, and an integrated oscillating mill screen size 0.8–1.5 mm. Formula addition ratio: lurasidone HCl equivalent to 20–80 mg lurasidone per capsule, croscarmellose sodium at 2–4% w/w, and magnesium stearate at 0.5–1.0% w/w. The granulate is filled into size 1 or size 0 hard gelatin capsules on a rotary dosator machine running at 60,000–120,000 capsules/hour. Fill weight variation is verified under USP <905>, dissolution under USP <711>, and disintegration under USP <701>, with batch release governed by FDA 21 CFR 211.165. A known failure mode is wear of the tamping pins or dosator tips when magnesium stearate content falls below 0.5% w/w, while levels above 1.0% w/w increase dissolution lag time; both boundaries are tracked through periodic capsule weight and dissolution trend analysis. Terminal product type: hard gelatin capsule.
For granules dispensed in single-dose or multi-dose sachets intended for oral suspension, lurasidone HCl is wet-granulated in a top-spray fluid-bed granulator using a binder solution of 5–8% w/w hypromellose E5 or povidone K30 in purified water. Because published data for lurasidone HCl sachet granules is limited, the process envelope is based on top-spray fluid-bed capability for low-density poorly compressible antipsychotic granulates and requires confirmation by design-of-experiments. The dry blend of API, mannitol, and croscarmellose sodium is fluidized at inlet air temperature 50–65 °C and spray rate 5–15 g/min/kg of dry charge; granulation is continued until the median granule size reaches 150–250 µm and moisture content reaches 1.5–2.5%. The granules are dried to loss on drying ≤2.0% and milled through a 1.0 mm screen. Formula addition ratio: each sachet contains lurasidone HCl equivalent to 20 mg or 40 mg lurasidone base in a total fill weight of 1.0–2.0 g, with croscarmellose sodium 2–4% w/w, hypromellose binder 1.5–3.0% w/w, and magnesium stearate 0.5–1.0% w/w after drying and milling. Terminal product type: granules for oral suspension. Compliance is assessed by USP <711> for drug release from the reconstituted suspension, USP <905> for content uniformity of single-dose sachets, USP <701> for disintegration where a dispersible granule claim is pursued, and FDA 21 CFR 211.165 for batch release. Moisture-sensitive packaging with desiccant is used when stability data show sachet moisture uptake above 2% at 25 °C/60% RH. The main process limitation is binder solution nozzle blockage during top-spray granulation; binder solution is therefore filtered through a 100 µm screen and viscosity is controlled before spraying.
When High-Shear Wet Granulation Replaces Direct Compression for Dose-Proportional Tablet Cores
High-shear wet granulation is selected when direct compression generates unacceptable segregation or tablet weight variability at scale. Published data for lurasidone HCl high-shear granulation parameters is limited; the ranges below derive from high-shear granulator capability for low-dose poorly compactable drugs and require verification during technical transfer. In a 150–600 L high-shear granulator equipped with main impeller and side chopper, lurasidone HCl, mannitol, pregelatinized starch, and a portion of croscarmellose sodium are dry-mixed at impeller speed 100–200 rpm and chopper speed 1,500–3,000 rpm for 3–5 minutes; purified water or an aqueous binder solution is added at 15–25% w/w of dry charge while maintaining impeller power draw equivalent to a torque increase of 8–12 Nm. The wet mass is passed through a 1.5 mm screen and dried in a fluid-bed dryer at inlet air temperature 55–65 °C until loss on drying is 1.0–2.5%. Dried granules are milled through a 0.8 mm screen, blended with croscarmellose sodium 2–4% w/w and magnesium stearate 0.5–1.0% w/w, and compressed on a rotary press to hardness 80–120 N and friability ≤1.0%. Formula addition ratio: lurasidone HCl equivalent to 20 mg, 40 mg, 60 mg, 80 mg, or 120 mg lurasidone per tablet core; tablet core mass is adjusted in proportion to strength to maintain comparable compaction pressure. Terminal product type: film-coated tablet. Compliance standards include USP <905>, USP <711>, USP <701>, FDA 21 CFR 210/211, and ICH Q3C for residual solvents when an organic granulating solvent is used. The critical process constraint is moisture below 2.5% at compression; higher moisture causes picking on the tablet tooling, while over-drying below 1.0% increases granule friability and die-fill variation.
For injectable dosage form development, lurasidone HCl is a practically water-insoluble weak base requiring particle size reduction by high-pressure homogenization or wet bead milling to create a nanosuspension suitable for intramuscular or subcutaneous administration. Published data for a commercial lurasidone injectable product is limited; formulation development therefore applies a risk-based process anchored to USP <1> Injections, USP <71> sterility, USP <788> particulate matter in injections, USP <790> visible particulates, USP <791> pH, and USP <785> osmolality. Formula addition ratio: drug load in the aqueous nanosuspension is evaluated between 5% w/w and 20% w/w relative to total suspension mass; the vehicle contains a stabilizer such as polysorbate 20 or poloxamer 188 at 0.2–1.0% w/v, sodium chloride at 0.6–0.9% w/v for tonicity, and a pH-adjusting agent to maintain pH 5.0–6.0. Process: wet bead milling is performed with yttria-stabilized zirconia beads of 0.2–0.5 mm diameter in a recirculation mill at 2,000–4,000 rpm, with chamber temperature maintained at 5–15 °C; the target particle size is D90 ≤500 nm and D50 ≤250 nm by laser diffraction. Terminal product type: aseptically filled injectable suspension in single-dose vials or pre-filled syringes; sterility assurance follows 21 CFR 211.167 and USP <71>. The operational boundary is that terminal steam sterilization is generally incompatible with nanoparticulate suspensions because of particle agglomeration risk; the vehicle is therefore sterilized by 0.22 µm filtration before aseptic milling and filling, and the API suspension is processed in an isolator or restricted access barrier system. Aggregation tendency must be rechecked after storage at 2–8 °C unless accelerated stability data indicate otherwise.
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- Lurasidone Intermediate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable is manufactured under an ISO 9001 quality system and complies with relevant regulatory requirements.
- COA, SDS/MSDS, and related certificates are available upon request. For certificate requests or inquiries, contact: sales10@sinochem-nanjing.com.
Lurasidone intermediate pharma grade API is supplied as the hydrochloride salt, CAS 367514-87-2, molecular formula C28H36N4O2S·HCl, and molecular weight 529.14 g/mol. The designation refers to a purified lurasidone hydrochloride substance that is released to drug substance specifications and is suitable as a downstream formulation intermediate for tablet, capsule, granule, and injectable products. It is not a crude chemical intermediate; the release panel includes polymorph identity, assay, related substances, residual solvents, and elemental impurities. No universal commercial model number is assigned under the product title; the material is identified by chemical name, CAS, manufacturer lot number, and certificate of analysis. Standard pack configurations of 1 kg, 5 kg, and 25 kg net weight in double polyethylene bags within an aluminium-lined drum are typical but manufacturer-specific. Because oral and injectable applications impose different impurity and particulate constraints, the material is controlled to allow downstream selection for the intended route. The product is not released as sterile and is not intended for direct patient administration.
Polymorph identity and particle-size distribution are locked by the release specification
Control of solid-state form is achieved through X-ray powder diffraction against the approved reference diffractogram. Differential scanning calorimetry is used as an orthogonal identification tool; the melting endotherm is recorded, but acceptance is based on the reference pattern. Particle-size distribution is measured by laser diffraction per ISO 13320:2020; reportable values include d10, d50, and d90. For low-dose tablets, d90 is the critical parameter for content uniformity and dissolution rate because a coarse fraction may delay release and increase sampling error. The product is pre-screened through a 0.5 mm sieve during tableting and capsule operations. In injectable solution processing, the API must dissolve completely before sterilizing-grade filtration; therefore, particle size is less critical for true solutions but remains critical for suspension-based injectables. The material is not a sterile API and is not a submicron suspension.
| Release attribute | Method designation | Application-critical control |
|---|---|---|
| Polymorph identity | XRPD reference diffractogram | Must match approved form; amorphous content monitored in micronized lots |
| Particle size distribution | ISO 13320:2020 | d90 limit set by dissolution and content uniformity; exact limit on certificate of analysis |
| Water content | USP <921> | Limit prevents hydrolytic degradation during aqueous granulation or hot-melt processing |
| Residual solvents | USP <467>, ICH Q3C | Class 1 not used; Class 3 ≤ 5000 ppm; Class 2 at PDE-based limits |
| Elemental impurities | USP <232>/<233>, ICH Q3D | Oral PDE panel for solid oral; parenteral PDE panel for injectable |
For tablet and capsule manufacture, the API is commonly incorporated after roller compaction or high-shear wet granulation when direct compression flow is insufficient. A high-shear granulator with main impeller and chopper speeds controlled by torque, or a twin-screw granulator with a defined length-to-diameter ratio, is used to wet-mass the blend. The granulation is dried in a fluid-bed dryer to a loss-on-drying endpoint specified in the batch record; moisture content is determined by USP <731>. The dried granule is milled and sized over 0.5 mm and 0.25 mm screens; the target size fraction is formulation-specific. Compression is performed on a rotary tablet press with precompression and main compression force selected to achieve hardness and disintegration per USP <701>; no universal compression force is stated because it depends on tablet geometry and tooling. Capsule filling is controlled by in-process weight variation under USP <905>, and blend uniformity is verified before release. For granule-filled sachets, the product is blended with a suitable excipient base after sieving; content uniformity is controlled by USP <905>. Powder flow is assessed by USP <1174> or equivalent angle-of-repose method. Direct compression is feasible only after flow and compressibility are demonstrated on the intended production press.
If the formulation requires solubility enhancement, the API may be incorporated into a hot-melt extruded solid dispersion or spray-dried intermediate. Such operations require thermal stability data and glass transition temperature control; no universal hot-melt extrusion processing window is assigned because the polymer matrix and plasticizer alter viscosity and degradation kinetics. The API release alone does not guarantee dissolution equivalence; finished dosage performance is verified by USP <711> dissolution testing.
Which impurity, solvent, and elemental panels determine oral versus injectable acceptance?
Related substances are quantified by high-performance liquid chromatography using a C18 stationary phase and a detection wavelength appropriate for lurasidone hydrochloride. The acceptance criteria are stratified according to ICH Q3A; because approved adult doses are 40–160 mg/day for schizophrenia and 20–120 mg/day for bipolar I depression, the maximum daily dose remains below 2 g/day, and the corresponding unspecified impurity threshold is 0.10% with qualification above 0.15%. Actual lot-specific limits are recorded on the certificate of analysis. Residual solvents are determined by headspace gas chromatography per USP <467> and assigned according to ICH Q3C; Class 3 solvents are controlled to not more than 5000 ppm, Class 2 solvents are limited to their PDE-based concentrations, and Class 1 solvents are not used. Elemental impurities are screened by inductively coupled plasma mass spectrometry per USP <232>/<233> and ICH Q3D. Palladium, platinum, nickel, chromium, and lead are included in the routine panel if the synthetic route uses the corresponding catalysts or reagents. For injectable use, the parenteral PDE values are applied; a lot acceptable for oral use may fail injectable elemental impurity limits. Mutagenic impurities are evaluated under ICH M7; route-specific purge factors and analytical control data are provided in the quality dossier.
In injectable compounding, the API is dissolved in a parenterally acceptable vehicle and filtered through a sterilizing-grade polyethersulfone membrane with nominal pore size 0.22 µm. Membrane compatibility with the solvent system and pH is assessed before scale-up; no filter type is assigned without compatibility data. The solution is transferred to a filling line under unidirectional air, and the container-closure system is selected to limit oxygen and light exposure. Endotoxin control is exercised at the API and water system level because sterilizing-grade filtration does not remove endotoxins. If the API is used in a lyophilized injectable format, the solution is filtered before lyophilization; the resulting cake is tested for moisture by USP <921>. The material described here is not released as sterile, and the default lot release does not include USP <71> sterility testing; terminal sterilization or aseptic filtration must be applied downstream.
When terminal sterilization or aseptic filtration is applied
Terminal sterilization of lurasidone hydrochloride solutions is acceptable only when formulation pH and buffer species do not accelerate hydrolytic degradation. Autoclave mapping trials are performed with biological indicators and validated load configurations; no single time-temperature cycle is fixed because heat penetration depends on fill volume, container, and viscosity. If the solution is heat-sensitive, aseptic filtration through a 0.22 µm membrane is used. Filtration does not remove dissolved endotoxins and cannot compensate for inadequate upstream bioburden control. The API's insoluble particle burden before dissolution must be aligned with finished-product particulate matter limits per USP <788> for large-volume parenterals or USP <789> for small-volume parenterals, because filtration may not remove all particles if source particle load is high. For suspension injectables, the API must be micronized under conditions that avoid amorphization; particle-size distribution after micronization is measured by ISO 13320:2020, and the suspension is tested for syringeability, sedimentation rate, and particle-size stability over shelf life. Published data for terminal sterilization of lurasidone hydrochloride injectable formulations is limited; formulation-specific stability and compatibility studies are required before routine production.
Comparative release profile against non-pharma and alternative-salt materials
The comparative release profile is based on GMP documentation and analytical results. Technical-grade lurasidone base may contain residual synthetic intermediates, catalyst metals, and uncrystallized amorphous fractions; pharma-grade lurasidone hydrochloride is released with a defined assay range, related-substance profile, and polymorph identity. The hydrochloride salt provides controlled stoichiometry for oral solid dosage forms; alternative salts or free base forms may differ in hygroscopicity, solubility, and millability. The table summarizes key differences.
| Differentiating parameter | Pharma-grade lurasidone hydrochloride | Technical-grade or non-pharma intermediate | Milled oral-only grade |
|---|---|---|---|
| Elemental impurity panel | ICH Q3D oral and parenteral PDE reported | May omit Pd/Pt confirmation | Oral PDE only |
| Endotoxin/bioburden trending | Assessed for injectable use | Not assessed | Not assessed |
| Particle-size control | d90 controlled by ISO 13320:2020 | Wide distribution | Milled but may lack parenteral particulate control |
| Residual solvent control | ICH Q3C Class 2/3 limits | May contain process solvents | Class 3 only |
| Intended downstream use | Tablet, capsule, granule, injectable after terminal sterilization | Synthesis/exploratory only | Oral solid dose only |
Batch-to-batch variance in residual palladium and particle-size distribution is monitored by statistical process control; lots outside the validated range are not released for injectable use. Storage conditions are assigned from long-term and accelerated stability data under ICH Q1A(R2); the material is protected from light and moisture in double polyethylene bags within an aluminium-lined drum. If controlled cold storage is required, the label states 2–8 °C; controlled room temperature storage is permitted only when supported by stability studies. The API is intended for further pharmaceutical processing under 21 CFR 210/211 and ICH Q7 GMP. Published data for this specific configuration—particularly injectable suspension and terminal sterilization behavior—is limited; downstream validation remains formulation-specific.
