| HS Code | 981245 |
| Product Name | Moxifloxacin Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable |
| Pharmacopoeial Grade | USP / EP / IP compliant pharma grade |
| Chemical Name | 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid (free base); corresponding hydrochloride salt for parenteral/oral use |
| Cas Number | 151096-09-2 (free base); 186826-86-8 (hydrochloride) |
| Molecular Formula | C21H24FN3O4 (free base); C21H24FN3O4·HCl (hydrochloride) |
| Molecular Weight | 401.44 g/mol (free base); 437.89 g/mol (hydrochloride) |
| Appearance | White to pale yellow crystalline powder |
| Solubility | Hydrochloride salt is sparingly soluble in water and soluble in dilute acidic media; free base is practically insoluble in water; slightly soluble in ethanol |
| Assay Hplc | 98.0% to 102.0% on dried basis |
As an accredited Moxifloxacin 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 | Moxifloxacin Pharma Grade API packaged in sealed drums with double polythene bags, 25 kg net each, oral/injectable use. |
| Container Loading (20′ FCL) | Moxifloxacin Pharma Grade API (oral/injectable) is packed in drums, palletized, and loaded into one 20′ FCL container for shipment. |
| Shipping | Moxifloxacin Pharma Grade API ships in sealed, moisture-resistant containers under temperature-controlled conditions to preserve purity and stability. Export packaging meets IATA/IMDG regulations for pharmaceutical actives. Documentation includes COA, MSDS, and origin certificate. Delivery is secure, traceable, and compliant with global cold-chain and handling protocols. |
| Storage | Store Moxifloxacin Pharma Grade API in a well-ventilated, cool, dry area below 25°C, protected from light and moisture. Keep in original, tightly closed, labeled containers, away from incompatible materials and heat sources. For manufactured tablets, capsules, granules, or injections, follow labeled storage conditions; use appropriate handling for oral and injectable formulations. |
| Shelf Life | Shelf Life: 36 months when stored in original container below 30°C, protected from light and moisture. |
In oral solid dose manufacture, moxifloxacin hydrochloride is anchored by the conversion of the salt to a 400 mg base-equivalent dose: 436.4 mg of moxifloxacin hydrochloride per tablet core, calculated from a molecular mass ratio of 1.091 between the hydrochloride salt and the free base. For a reference core mass of 700 mg, the drug load is 62.3% w/w, placing the formulation in the high-dose category where filler selection, granulation endpoint, and blend lubrication determine content uniformity and compaction behavior. The process begins with aqueous high-shear granulation in a 300–600 L vertical granulator, with binder solution added at 2–4% w/w of dry mass and water quantity adjusted to reach a target granulate moisture content of 2.0–3.5% w/w before fluid-bed drying. Product temperature is held below 45°C during drying to minimize discoloration and related substance formation, and drying is terminated by near-infrared moisture endpoint rather than time alone. Dried granules are milled through a cone mill with an aperture screen of 0.8–1.2 mm, then blended with croscarmellose sodium as disintegrant, lactose monohydrate as filler, and magnesium stearate added last at 0.5–1.0% w/w; exceeding 2.0% w/w lubricant is avoided because hydrophobic films on granule surfaces can delay dissolution and reduce tablet hardness. Compression on a rotary tablet press with 10- or 12-station tooling uses a compression force range of 8–18 kN; core hardness is maintained at 80–120 N and friability below 1.0%. Aqueous film coating with a hypromellose/titanium dioxide/iron oxide system is applied to a 3–4% weight gain, with pan exhaust temperature held at 40–50°C and spray rate adjusted to prevent edge erosion and bridging. Release and in-process compliance is governed by USP <711> dissolution, USP <905> uniformity of dosage units, USP <701> disintegration, ICH Q3D elemental impurity control, ICH Q3C residual solvent limits, 21 CFR 211.110(a) for blend uniformity, and the USP Moxifloxacin Tablets monograph. Because fluoroquinolones undergo photodegradation, tablet cores are transferred and stored in light-protective containers, and final packs include light-barrier materials. The terminal product type is a 400 mg immediate-release film-coated tablet intended for oral administration.
When capsule filling is required for clinical development, regional registration, or patients requiring a non-tablet oral solid, direct compression of moxifloxacin hydrochloride is usually rejected because of poor powder flow and segregation risk in the 50–150 µm particle-size range. Dry granulation by roller compaction resolves flow without introducing moisture or thermal stress. A reference fill mass of 600 mg for a 400 mg base-equivalent content requires 436.4 mg of moxifloxacin hydrochloride per capsule, corresponding to 72.7% w/w; the remaining 27.3% w/w consists of microcrystalline cellulose, pregelatinized starch, croscarmellose sodium, and magnesium stearate. Roller compaction is conducted on a pharmaceutical roller compactor with roll pressure 30–50 kN and roll speed 2–8 rpm; ribbon density is controlled in the range 0.85–1.10 g/cm³ to achieve granulate flow and recompaction potential. Ribbon milling through an oscillating granulator with a 1.0 mm screen produces a granulate fraction between 180 µm and 710 µm; fines below 180 µm are recycled at no more than 25% of granulate mass to prevent density over-compaction and loss of recompactability. Encapsulation on a tamping-pin or dosator capsule filling machine is selected based on granulate flow; tamping-pin machines are preferred when Carr’s index exceeds 25%. Capsule fill weight is verified by in-line net weight checkweigher, content uniformity is controlled by USP <905>, and dissolution follows USP <711> with medium and acceptance criteria aligned to the reference tablet monograph. Capsule shells must be stored at 40–50% RH at 20–25°C to prevent brittleness or deformation, and filled capsules are packed in light-protective materials. The terminal product type is a 400 mg moxifloxacin hydrochloride hard capsule; because this is not the reference product in major markets, dissolution and bioequivalence bridging data are generally required in the filing sequence.
Ready-to-use intravenous moxifloxacin hydrochloride infusion is compounded as a sterile, nonpyrogenic solution in which each 250 mL polyolefin bag contains moxifloxacin hydrochloride equivalent to 400 mg moxifloxacin, giving a base concentration of 1.6 mg/mL and a salt concentration of 1.746 mg/mL. Compounding is carried out in stainless steel or glass-lined vessels, with sodium chloride added at 8.0 mg/mL to achieve isotonicity; pH is adjusted with dilute hydrochloric acid or sodium hydroxide to a target range of 4.0–4.6, outside which moxifloxacin can precipitate or oxidative degradation accelerates. The solution is filtered through a 0.22 µm sterilizing-grade membrane and aseptically filled into polyolefin infusion bags under EU GMP Annex 1 grade A/B conditions; if terminal steam sterilization is applied, the selected F0 must be justified by photostability and related substance data because fluoroquinolones are sensitive to prolonged heat and light. Filled bags are checked for visible particulates per USP <790> and subvisible particulates per USP <788>, and each batch is tested for sterility per USP <71>, bacterial endotoxins per USP <85>, and pH. Container closure integrity is verified by vacuum decay or dye penetration and aligned to USP <1207>; aseptic process validation follows ISO 13408-1:2023 and 21 CFR 211.113(b). The infusion must not be refrigerated or frozen because low-temperature storage can initiate precipitation, and the overwrapped bag must be protected from light during warehouse transfer and hospital storage. Incompatibility with multivalent cations requires dedicated filling lines and prohibits co-infusion with magnesium-, calcium-, or zinc-containing admixtures; chelation can reduce free drug and produce visible particulates. The terminal product type is a 400 mg/250 mL ready-to-use intravenous infusion bag for hospital and home-care administration.
For granulated moxifloxacin hydrochloride supplied to a direct-compression or capsule-filling line, the terminal product type is not a finished pharmacopoeial dosage form but a non-sterile granulated API intermediate that enters a customer’s compression or encapsulation process. The granulated stream itself contains 90–98% w/w moxifloxacin hydrochloride, with the balance composed of binder, disintegrant, and a lubricant; this ratio permits downstream dilution to 400 mg base per tablet at a final core mass of 450–700 mg. Particle-size distribution is controlled by laser diffraction or air-jet sieving, with a targeted D50 between 150 µm and 300 µm and a D90 not exceeding 850 µm to ensure uniform die filling and acceptable segregation behavior. Bulk density and tapped density are measured per USP <616>; a tapped density ratio below 1.35 is preferred to maintain tablet weight relative standard deviation below 2.0% at press speeds of 60–100 rpm. Residual moisture is held below 3.0% w/w because higher moisture increases punch-face sticking and accelerates photodegradation during storage. Granulated API is packed in double polyethylene bags inside light-protective aluminum pouches with desiccant, and the material should be equilibrated in the compression room at 20–25°C and below 50% RH for 12–24 h before use; failure to equilibrate can increase static charge and cause picking during prolonged tablet runs. Release testing is controlled under 21 CFR 211.165, in-process testing under 21 CFR 211.110, specification setting under ICH Q6A, elemental impurity control under ICH Q3D, residual solvents under ICH Q3C, and good manufacturing practice for API intermediates under ICH Q7. Because this intermediate is not a registered drug product, each downstream formulator must establish its own dissolution, impurity, and stability acceptance criteria against the intended tablet or capsule finished dosage form.
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Moxifloxacin Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable is supplied as moxifloxacin hydrochloride monohydrate. The molecular formula is C21H24FN3O4·HCl·H2O, the relative molecular mass is 455.9 g/mol, and the CAS registry number is 192927-63-2 for the monohydrate; the anhydrous hydrochloride form carries CAS 151096-09-2 and the base form CAS 354812-41-2. Manufacturer-specific model designations for this API distinguish direct compression grades, fine-milled capsule grades, granulation grades, and sterile injectable grades. These model codes are not pharmacopoeial identifiers; they encode particle-size distribution, bulk density, residual solvent profile, and microbiological qualification status. The API is a white to pale yellow crystalline powder supplied under current good manufacturing practice controls and is tested against the United States Pharmacopeia and European Pharmacopoeia monographs for moxifloxacin hydrochloride. Release testing includes identification, assay, related substances, water content, residue on ignition, residual solvents, elemental impurities, and microbial limits. The product is used as the active ingredient in film-coated tablets, hard gelatin or hypromellose capsules, granules for oral suspension, and sterile injectable preparations. The oral and injectable grades differ principally in bioburden, endotoxin, and particulate controls rather than in chemical identity.
| Parameter | Method/Standard Designation | Typical Release or Pharmacopoeial Control |
|---|---|---|
| Appearance | Visual inspection | White to pale yellow crystalline powder |
| Identification | IR absorption spectrophotometry; Ph. Eur. 2.2.24, USP <197> | Matches reference spectrum; HPLC retention time match |
| Water content | Karl Fischer titration; Ph. Eur. 2.5.12, USP <921> | 3.0%–4.5% for monohydrate form |
| Related substances | Liquid chromatography; Ph. Eur. 2.2.29, USP <621> | Individual unspecified impurity commonly controlled at ≤0.10%; total impurities commonly ≤0.5% |
| Assay | HPLC; Ph. Eur. 2.2.29, USP <621> | 98.0%–102.0% calculated on the dried basis |
| Residue on ignition | Ph. Eur. 2.4.14, USP <281> | ≤0.1% |
| Residual solvents | Headspace gas chromatography; USP <467>, Ph. Eur. 5.4 | Class 1 solvents absent; Class 2 solvents below ICH Q3C options |
| Elemental impurities | ICP-MS; USP <232>/<233>, ICH Q3D | Within oral and parenteral permitted daily exposure values |
| Microbial limits | Ph. Eur. 5.1.4, USP <61>/<62> | Non-sterile oral grade: total aerobic microbial count ≤100 CFU/g; total yeasts and moulds ≤20 CFU/g |
The molecule is a zwitterionic 8-methoxyfluoroquinolone with ionisation constants near pKa1 6.25 and pKa2 9.29. Aqueous solubility is pH-dependent: solubility is higher under acidic conditions where the C-7 diazabicyclo substituent is protonated and decreases as pH approaches the isoelectric region. This pH-solubility behaviour affects dissolution, wet granulation, and injection formulation. Moxifloxacin hydrochloride monohydrate shows limited hygroscopicity at ambient storage conditions, but exposure to high humidity or unbound water during processing should be controlled to avoid localised hydration and agglomeration. The substance is light-sensitive; forced degradation studies demonstrate photolytic degradation in solution and in the solid state. Storage in airtight containers protected from light is required by the pharmacopoeial monograph. The 8-methoxy substituent reduces phototoxicity compared with older 6-fluoroquinolones, but photochemical stability of the API itself is not equivalent to low light sensitivity. Formation of chelates with multivalent cations such as Al3+, Mg2+, Ca2+, Fe2+/3+, and Zn2+ is a known incompatibility; direct contact with metal-containing excipients, antacids, or minerals in solution can reduce oral absorption or generate turbidity in injectable preparations. Dry blending with dibasic calcium phosphate or magnesium-containing fillers should therefore be screened for dissolution stability and appearance.
Particle-size specifications for moxifloxacin hydrochloride monohydrate are supplier-specific and route-dependent. For low-dose direct compression or dry powder capsule filling, milling to a d90 below 75 µm can improve blend uniformity and content uniformity, but particle-size reduction tends to increase electrostatic charging and reduce flow. A milled API with d50 in the range of 10–25 µm may require higher levels of colloidal silicon dioxide, typically 0.2%–0.5%, and magnesium stearate at 0.5%–1.0% in capsule formulations. Over-lubrication from extended blending or excessive magnesium stearate can reduce tablet tensile strength and retard dissolution. For wet granulation, a coarser API with d90 up to 250 µm may be acceptable because wet massing and subsequent milling control the final granule size. Published compaction and ejection data for moxifloxacin hydrochloride monohydrate at production scale are limited; processing parameters are manufacturer-specific and should be established using instrumented tablet presses and compaction simulation rather than transferred from other fluoroquinolones.
For aqueous high-shear wet granulation, the quantity of purified water must be controlled because the drug substance is sparingly soluble in water and can act as a secondary binder. Local overwetting can produce hard agglomerates that require additional dry milling and shift the final particle-size distribution. Top-spray fluid-bed granulation with a low-viscosity binder solution, hydroxypropyl methylcellulose or povidone at 3%–5% solids, is an alternative when lower granule density and faster drying are needed. Roller compaction is used where moisture exposure is undesirable or where direct compression is not feasible because of poor flow; critical process parameters include roll force, roll speed, and screen size, but no universal values apply to all formulations. Tablets containing moxifloxacin hydrochloride monohydrate are generally film-coated for light protection and taste masking, with coating weight gain typically 2%–4% of core tablet weight.
Injectable-grade moxifloxacin hydrochloride monohydrate is manufactured with lower bioburden and endotoxin load than oral-grade material. For a large-volume parenteral solution, the commercial infusion presentation is commonly a clear yellow-green solution containing moxifloxacin hydrochloride equivalent to 1.6 mg/mL moxifloxacin in 0.8% sodium chloride, with pH adjusted to 4.1–4.6 and osmolality in the range of 270–300 mOsmol/kg. Sterile filtration through 0.22 µm filters or terminal sterilisation may be used depending on process validation; heat exposure should be justified by degradation studies because the molecule can undergo photolytic and oxidative degradation. The injectable formulation must comply with particulate matter limits under USP <788> or Ph. Eur. 2.9.19, bacterial endotoxins under USP <85> or Ph. Eur. 2.6.14, and sterility under USP <71> or Ph. Eur. 2.6.1. Any diluent containing divalent cations, including certain Ringer’s or parenteral nutrition admixtures, is incompatible or requires compatibility data because of chelation and possible precipitation. If a lyophilised product is developed, the freeze-drying cycle should account for the crystallisation tendency of moxifloxacin hydrochloride and the pH shift during freezing; mannitol or glycine may be used as bulking agents, but calcium-containing bulking agents are not appropriate.
The impurity profile of moxifloxacin hydrochloride monohydrate is controlled by liquid chromatography with ultraviolet detection. ICH Q3A thresholds apply to new impurities; for a maximum daily dose of 400 mg, the reporting threshold is 0.05%, the identification threshold is 0.10%, and the qualification threshold is 0.15% unless a more stringent pharmacopoeial limit is specified. Degradation products observed in stress studies include acid, base, oxidative, and photolytic products; the relative retention times and response factors are method-specific and should not be transferred across columns or mobile phases without verification. Residual solvents are measured by headspace gas chromatography against USP <467> and Ph. Eur. 5.4; common process solvents such as methanol, ethanol, isopropanol, and ethyl acetate are monitored, with acceptance criteria derived from ICH Q3C. Elemental impurities are controlled by ICP-MS using USP <232>/<233> and ICH Q3D permitted daily exposure limits. For a product intended for both oral and injectable use, the lower parenteral limits for cadmium, lead, arsenic, mercury, cobalt, vanadium, and nickel typically govern the specification. The API manufacturer should provide a risk assessment covering raw materials, catalysts, processing equipment, and packaging components.
When compared with ciprofloxacin hydrochloride and levofloxacin hemihydrate, moxifloxacin hydrochloride monohydrate differs in the C-8 methoxy substituent and the C-7 diazabicyclononane ring. These structural features confer enhanced activity against Streptococcus pneumoniae, atypical respiratory pathogens, and many anaerobes, while activity against Pseudomonas aeruginosa is reduced relative to ciprofloxacin. The changes also affect photodegradation kinetics, chelation behaviour, and physicochemical handling. The comparative attributes relevant to formulation and clinical pharmacokinetics are summarised in Table 2.
| Attribute | Moxifloxacin hydrochloride monohydrate | Ciprofloxacin hydrochloride | Levofloxacin hemihydrate |
|---|---|---|---|
| Molecular formula | C21H24FN3O4·HCl·H2O | C17H18FN3O3·HCl | C18H20FN3O4·½H2O |
| Relative molecular mass | 455.9 g/mol | 367.8 g/mol | 370.38 g/mol |
| Oral bioavailability | Approximately 90% | Approximately 70% | Approximately 99% |
| Plasma protein binding | 30%–50% | 20%–40% | 24%–38% |
| Elimination half-life | 11–15 h | 3–5 h | 6–8 h |
| Key spectrum difference | Enhanced Gram-positive, atypical, and anaerobic activity; reduced Pseudomonas activity | Highest Pseudomonas aeruginosa activity among the group | Intermediate Gram-positive and Gram-negative activity |
| Formulation-related caution | Light sensitivity; multivalent cation chelation; pH-dependent solubility | Multivalent cation chelation; photosensitivity; variable solubility | Multivalent cation chelation; photosensitivity; solution pH control |
Selection between these fluoroquinolones in product development is driven by the target indication, route of administration, and required antimicrobial spectrum. For moxifloxacin-containing products, the 8-methoxy substituent alters photodegradation kinetics and chelation behaviour relative to older fluoroquinolones. Substitution of moxifloxacin for ciprofloxacin or levofloxacin at equivalent dose is not appropriate without revalidation of assay, dissolution, related substances, and in-process controls because molecular mass, salt stoichiometry, and powder handling characteristics differ.
