| HS Code | 395779 |
| Product Name | Kitasamycin (Leucomycin, Kitamycin) Veterinary Grade API |
| Chemical Class | 16-membered-ring macrolide antibiotic |
| Source | Fermentation-derived antibiotic complex produced by Streptomyces kitasatoensis |
| Cas Number | 1392-21-8 |
| Composition Note | Complex mixture of leucomycin components, primarily leucomycins A1-A7 |
| Molecular Formula | Complex mixture; main component leucomycin A1: C40H67NO14 |
| Molecular Weight | Variable for complex; leucomycin A1 is approximately 785.97 g/mol |
| Appearance | White to light-yellow or faintly yellow crystalline or amorphous powder |
| Solubility | Base form is practically insoluble in water and freely soluble in methanol, ethanol, acetone, chloroform, ethyl acetate and ether; water-soluble acid-addition salts are available for soluble formulations |
| Mechanism Of Action | Inhibits bacterial protein synthesis by reversible binding to the 50S ribosomal subunit, blocking peptidyl transfer and peptide elongation |
| Antibacterial Spectrum | Active mainly against Gram-positive bacteria such as Staphylococcus, Streptococcus, Listeria and Erysipelothrix; also active against certain Gram-negative organisms, Mycoplasma, Chlamydia and Rickettsia |
| Therapeutic Indications | Veterinary treatment of respiratory, digestive, soft-tissue and systemic infections caused by susceptible organisms, including mycoplasmosis, swine respiratory disease, avian chronic respiratory disease and fowl cholera |
| Target Species | Poultry, swine, cattle and other veterinary species of herd origin; veterinary use only |
| Dosage Form Compatibility | Suitable as a bulk active pharmaceutical ingredient for tablets, injections, capsules, powders, granules, premixes and oral solutions |
| Storage Conditions | Store in a tightly closed, light-protected container in a cool, dry, well-ventilated place |
| Shelf Life | Typically 24 to 36 months when unopened and stored under recommended conditions |
| Grade | Veterinary-grade bulk API for pharmaceutical formulation use |
As an accredited Kitasamycin (Leucomycin, Kitamycin) 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 | Kitasamycin veterinary grade API is packaged in 25 kg sealed laminated aluminum bags within fiber drums, ensuring stability and safety. |
| Container Loading (20′ FCL) | 20′ FCL container loading of Kitasamycin veterinary-grade API, packaged securely for tablets, injections, capsules, powders, granules, premix, and solutions. |
| Shipping | Kitasamycin Veterinary Grade API ships in sealed, light-resistant containers with tamper-evident seals, complying with international hazardous material regulations. Shipments are temperature-controlled, moisture-protected, and clearly labeled. Documentation includes MSDS, certificate of analysis, and origin certificate. Expedited air or ground freight ensures stability, safety, and regulatory compliance. |
| Storage | Store Kitasamycin veterinary-grade API in a tightly sealed, original container, protected from light, moisture, and heat. Recommended storage: cool, dry, well-ventilated area, ideally below 25°C (77°F). Avoid freezing, direct sunlight, and incompatible substances. Ensure proper labeling and secure area access. For formulated products, follow manufacturer-specific stability and shelf-life instructions. |
| Shelf Life | Shelf life: 36 months in sealed, original container stored below 25°C, protected from light and moisture. |
Dry premix manufacture for swine respiratory disease begins with geometric dilution of kitasamycin tartrate into a carrier matrix of lactose monohydrate and a coarse corn-cob granular carrier. A 5% w/w activity premix is layered in a ribbon blender with working capacity of 500 kg and paddle clearance of 5–8 mm above the trough bottom; the active fraction is pre-sieved through a 60-mesh screen before charging. Residue above 80-mesh is held below 2.0% of total mass to avoid segregation during bulk transfer. Blend uniformity is measured on 10 thief samples drawn according to ISO 6497:2002; acceptance requires RSD ≤ 5.0% and mean assay 95.0–105.0% of label claim. Water content is controlled below 4.0% by Karl Fischer titration because the tartrate salt becomes hygroscopic above 60% relative humidity. Total mixing after final active addition is limited to 12–15 rpm for 15 min; extended mixing increases surface charge on carrier particles and produces measurable de-mixing in the lower quadrant of the ribbon blender. The two-step geometric dilution prevents localized overload of sticky tartrate fines on ribbon blades; a single-step charge has been observed on production-scale ribbon blenders to raise assay RSD above 5.0% in the lower sample ports. The terminal product is a free-flowing 5% premix filled into polyethylene-lined paper sacks with desiccant sachets, metered into finished swine feed at a ratio fixed by the farm prescription; contact surfaces are Type 316L stainless steel to limit iron-catalysed macrolide degradation.
| Release parameter | Acceptance criterion | Test method or standard |
|---|---|---|
| Appearance | Off-white to pale yellow free-flowing powder | Visual examination, ISO 6498:2012 sampling plan |
| Water content | ≤ 4.0% by Karl Fischer | USP <921> |
| Particle size | 95% passes 60-mesh, residue on 80-mesh ≤ 2.0% | ASTM E11 |
| Blend uniformity | RSD ≤ 5.0% across 10 samples | USP <905> |
| Assay | 95.0–105.0% label claim | HPLC validated per VICH GL2 |
In a high-shear wet-granulation process, kitasamycin tartrate for oral granules is processed with impeller tip speed 3–5 m/s and chopper at 1500 rpm. A binder solution of 5% w/w povidone K30 in purified water is sprayed at 10–15 mL/min per kg of dry blend; the granulation endpoint is defined by a moisture content of 12–14% w/w and a hand-squeeze bolus that fractures cleanly. Drying in a fluid-bed dryer is limited to inlet air 45–50°C and product temperature below 38°C; the residual moisture specification after drying is 2.0–3.0%. Lower than 1.5% residual water increases fines below 0.15 mm, which causes poor flow into sachet dosing equipment; higher than 3.5% results in clumping inside aluminum-foil sachets during tropical storage. Wet mass holding time before transfer to the dryer is limited to 15 min; extended holding leads to binder migration to the granule surface and produces hard, poorly dispersible granules. Granule sizing through a cone mill with round impeller at 1000 rpm yields 0.25–0.85 mm granules with fines <15% w/w. Assay is performed by HPLC after extraction with acetonitrile-phosphate buffer at pH 6.0, with method transfer validated under VICH GL2. Residual solvent compliance is assessed under VICH GL18(R2). The terminal product is a 10% kitasamycin activity oral granule in sachets for direct top-dressing or reconstitution in drinking water.
When direct compression is selected for a 100 mg activity tablet, the dry blend is assembled at 31.25% w/w spray-dried kitasamycin tartrate (80% active), 58.25% microcrystalline cellulose PH102, 5.0% croscarmellose sodium, 4.0% sodium starch glycolate, 1.0% colloidal silicon dioxide, and 0.5% magnesium stearate. Magnesium stearate is blended for 3 min at 20 rpm in a V-blender; over-lubrication beyond 5 min depresses tensile strength by coating the active-carrier particles. Compression on a 16-station rotary press uses 12–18 kN compression force, target hardness 6–8 kp, and friability <1.0% after 100 rotations under USP <1216>. Aqueous film coating with hydroxypropyl methylcellulose is applied at 3–5% weight gain with inlet air dew point below 10°C and bed temperature 38–42°C, because re-humidification of the tartrate core above 60% RH increases sticking. Capsule filling uses size 0 hard gelatin capsules at 400 mg fill weight, with the same dry blend optimized for flow; the terminal products are aluminum-aluminum blistered tablets and HDPE bottle-packed capsules. Dissolution testing for tablets is conducted under USP <711> with a validated discriminatory medium.
Because the free base is insoluble in water at neutral pH, parenteral administration of kitasamycin tartrate requires a buffered aqueous vehicle containing 10% w/v active, 0.9% w/v sodium chloride, and phosphate-citrate buffer adjusted to pH 6.0–6.5 with 0.1 M sodium hydroxide or hydrochloric acid. Below pH 4.0, lactone ring hydrolysis accelerates during storage; above pH 7.5, the free base precipitates and blocks 0.22 μm sterilizing filters. The bulk solution is sparged with nitrogen to reduce headspace oxygen below 1.0% v/v, then passed through a 0.22 μm PVDF membrane under aseptic conditions. Terminal steam autoclaving is not recommended for this macrolide, and published data on kitasamycin-specific terminal moist-heat resistance is limited; sterile filtration followed by aseptic filling into amber Type I glass vials is the standard manufacturing route. Finished product sterility is confirmed by USP <71>, bacterial endotoxin by USP <85>, and particulate matter by USP <788>. Osmolality is adjusted to 280–320 mOsm/kg before filtration. The product is stored at 2–8°C; after first opening, in-use pH is maintained at 5.5–7.0 for up to 6 h at 25°C. Terminal presentations are 10 mL and 50 mL single-dose vials.
| Parameter | Target range | Monitoring point |
|---|---|---|
| Bulk solution pH | 6.0–6.5 | Before sterile filtration |
| Saturation storage temperature | 2–8°C | Finished product quarantine |
| In-use pH after first opening | 5.5–7.0 | 6 h at 25°C |
| Headspace oxygen | ≤ 1.0% v/v | After nitrogen sparging |
| Sterility | No growth | USP <71> |
Daily production of a 50% w/w water-soluble powder for drinking-water administration is built on a three-component dry blend of kitasamycin tartrate, anhydrous dextrose, and citric acid–trisodium citrate dihydrate at a carrier ratio of 1:0.90:0.10; buffer salts maintain reconstituted water at pH 6.0–7.5 and reduce carbonate precipitation in hard water. The powder is mixed in a double-cone blender at 60–70% working volume, 10 rpm, for 20 min; the final product passes through a 40-mesh screen and is filled into foil-lined sachets of 100 g, 500 g, and 1 kg. Sachet filling is carried out at 30–40% RH; static adherence to foil at RH below 25% is a common line-loss mode. Stock solution at 5% w/v is prepared by adding powder to water under continuous circulation, not by adding water to powder, to prevent localized acidic hydrolysis. In a 1:50 proportioning pump, stock solution is metered into drinking water at a rate calibrated daily against the actual water flow-meter; pH is measured at the end drinker line and maintained at 6.0–7.5. Hard water above 180 mg/L CaCO3 should be softened or treated with a chelating agent because divalent cations can reduce the apparent solubility of the tartrate salt in the stock tank; published data for kitasamycin-specific cation interactions in drinking water is limited. Medicated water is consumed within 24 h; the terminal product is a freely soluble powder for use in poultry and swine flock treatment, with an in-use expiry not exceeding 24 h after reconstitution.
After the conditioned mash leaves the pellet mill, thermal degradation becomes the dominant stability boundary for kitasamycin tartrate. In a standard ring-die pellet mill with die compression ratio 1:10–1:12, mash enters the conditioner at 80–85°C for 20–40 s at 15–16% moisture; these conditions are acceptable only when the 10% premix is protected by a thermally stable carrier or when a post-pelleting liquid addition system is used. High-shear die pressure raises pellet surface temperature above the conditioner set point for a short interval; recovery below 90% label claim can occur when pellets are held in the cooler inlet above 40°C for more than 5 min. Published studies on kitasamycin-specific pelleting loss at 85°C are limited, so each feed mill should validate potency on finished pellets using a VICH GL2-validated assay and compare to the mash sample before pelleting. Process adjustments include reducing conditioner residence time to 15–20 s for poultry feed, setting cooler air temperature 5–10°C below ambient, and achieving final moisture below 12% within 10 min after extrusion. Post-pellet liquid spraying of protected kitasamycin premix avoids the high-temperature conditioner entirely but requires calibration of spray nozzle flow to pellet bed residence time. The terminal product is a 3–4 mm pelleted feed with the 10% premix diluted to the prescribed inclusion, packed in woven polypropylene bags with a low-water-vapour-transmission liner.
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Kitasamycin (Leucomycin, Kitamycin) Veterinary Grade API for Tablets / Injections / Capsules / Powders / Granules / Premix / Solutions is a fermentation-derived 16-membered macrolide antibiotic obtained from Streptomyces kitasatoensis. The active substance is a multi-component mixture of leucomycin A-class homologues rather than a single chemical entity; potency is therefore assigned in units per milligram relative to a pharmacopoeial reference standard. A common veterinary-grade release limit is ≥1300 units/mg on the dried basis. The product model designation covers the same API identity and purity profile for oral solids, injectable liquids, medicated feed premixes, and drinking-water solutions; distinction between the listed dosage forms is achieved by particle-size control, bulk-density selection, bioburden status, and downstream manufacturing unit operations rather than by a change in molecular identity. The compound is practically insoluble in water and freely soluble in methanol, ethanol, acetone, and chloroform. These solubility properties directly restrict aqueous granulation and solution formulations and determine the manufacturing routes used for each presentation.
The release specification is not identical for every listed dosage form. For tablets and capsules, assay and related substances are primary release parameters; for injectable solutions, bacterial endotoxin, sub-visible particulate matter, and pH-stability data become critical; for premix and dry powder products, blend uniformity and particle-size compatibility with feed carriers often determine whether the API can be used without further micronisation or classification. Fermentation-derived residual solvent profiles are controlled by gas chromatography with headspace sampling under ICH Q3C(R8) or the regional veterinary registration file. Heavy metals are measured by ICP-MS, and the acceptance limit follows the current CVP 2020 monograph.
| Control parameter | Method or standard | Dosage-form relevance | Release basis |
|---|---|---|---|
| Potency/assay | HPLC against reference standard, CVP 2020 | All forms | ≥1300 units/mg dried basis |
| Related substances | HPLC area normalisation, CVP 2020 | Tablets, injectables | Registered total limit |
| Residual solvents | GC-headspace, ICH Q3C(R8) | Injectables, oral solids | Class-specific limits |
| Loss on drying | Vacuum oven, CVP 2020 | Granules, powders | Manufacturer maximum |
| Particle-size distribution | Laser diffraction, ISO 13320:2020 | Premix, powders | Application-dependent D10/D50/D90 |
| Heavy metals | ICP-MS, CVP 2020 | Feed premix | Compendial limit |
For sterile injections, the API is not necessarily sterile at release; downstream aseptic filtration through a 0.22 µm membrane is required, and the finished product must satisfy the sterility and bacterial endotoxin requirements of the applicable pharmacopoeia. For medicated feed premixes, laser diffraction is preferred over simple sieve analysis because the fine tail can govern segregation during discharge and transport. Bulk density, tapped density, and Hausner ratio are supplied on batch certificates and are used to set bin flow, auger metering, and direct-compression excipient selection.
Because the API is a fermentation multi-component mixture, the ratio of leucomycin A3 to A5 and other homologues may vary between batches. This component ratio can change the retention-time profile in HPLC but the pharmacopoeial assay sums the active homologues for potency. Manufacturers of premix and soluble powders should set internal component-ratio limits if downstream blend uniformity or dissolution is sensitive to the physical properties of individual homologues. Published data for this specific configuration is limited, especially for the link between component ratio and finished-product dissolution.
For low-dose premix, the number of active particles per unit feed mass must remain sufficient to avoid random sampling error. If a fine grade with D90 below 150 µm is selected, blend homogeneity may improve, but dusting and electrostatic adhesion increase; if a coarse grade is selected, segregation during transfer and uneven feed distribution may occur. The optimum D90 is therefore established by blend studies using the actual mixer and carrier, not by simple sieve classification alone. Laser diffraction analysis according to ISO 13320:2020 characterises the fine tail below 10 µm, which can be disproportionately responsible for segregation.
In medicated feed premix and dry powder production, the limiting unit operation is low-concentration blend homogeneity. Kitasamycin is usually pre-blended with a carrier such as lactose monohydrate or ground corncob before final feed dilution, and carrier selection is guided by API particle-size distribution rather than simple bulk density. Ribbon blenders of 1–2 m³ working volume can provide adequate shear for geometric dilution at inclusion rates established by the approved feed licence, but post-blend segregation often contributes more to assay variability than mixer type. Samples drawn from blender discharge are assayed by HPLC; a coefficient of variation of ≤5.0% is a common industry acceptance level for a validated blend, while the formal limit remains in the registered product file. Processing under relative humidity above 60% RH may increase adhesion of fine API to stainless steel surfaces and reduce blend recovery; environmental control is therefore applied when static charge or agglomeration is observed. If dry granulation is necessary to improve flow, roller compaction is preferred over slugging because it preserves a narrower particle-size distribution and avoids prolonged tray-drying thermal exposure. For drinking-water solutions, a cosolvent or carrier system is required because the API is practically insoluble in water, and the stability of the resulting stock solution is pH-dependent; published data for this specific configuration is limited, so formulation-specific stability studies are used to set the in-use shelf life.
The principal veterinary indications are respiratory and systemic infections caused by Mycoplasma and susceptible Gram-positive organisms in swine and poultry. Medicated feed premixes and water-soluble powders are used for group treatment, with inclusion rates defined by the approved product label; injectable solutions and oral solids are intended for individual treatment where the route is supported by bioavailability and tissue residue studies. Capsules are less common in food-producing animals but may be authorised in companion-animal formulations or non-food species where feed-based dosing is impractical. Bulk API storage is normally specified below 25°C in tightly closed containers protected from light, with retest dates assigned from formal stability data. Moisture uptake can produce caking and loss of flow; the certificate of analysis includes loss on drying to detect such exposure. Residual solvent levels from fermentation recovery are reported because they affect feed and food safety where the API is used in food-producing species.
Aqueous injectable formulations are constrained by pH-dependent hydrolysis of the macrolide lactone ring. The finished solution is normally buffered to pH 6.5–7.5; acidic buffers are avoided because acid-catalysed cleavage increases related substances detected by the CVP 2020 HPLC method. Steam sterilisation at 121°C is generally unsuitable for heat-sensitive macrolides unless thermal stability is demonstrated for the specific formulation; aseptic filtration through a 0.22 µm polyethersulfone membrane into sterile vials is the standard alternative. The API lot for injectable manufacture is controlled for bioburden before filtration to prevent membrane blinding and endotoxin carryover. Sub-visible particulate testing follows the pharmacopoeial light obscuration method, and the bacterial endotoxin limit is derived from the maximum dose and species-specific route. Non-aqueous vehicles may be required for poorly water-soluble macrolide injection products; when used, their viscosity, peroxide content, and container compatibility are included in the stability protocol.
Direct compression is feasible only when the API is pre-blended with a directly compressible filler because the native powder may have insufficient flow and compression characteristics. Higher-dose tablets typically require dry granulation by roller compaction or solvent-based wet granulation using ethanol rather than water, given the low aqueous solubility of the compound. Granule drying temperature and time are controlled by assay and related substances; thermal stress can reduce potency if the drying cycle exceeds the validated target. Capsule filling is usually performed on tamping-pin or dosator machines, and the powder blend is adjusted to a target bulk density to meet fill-weight specifications. The main processing incompatibility is with strongly acidic aqueous environments that promote lactone hydrolysis; prolonged contact with wet acidic granulating fluids should be avoided. Tablet dissolution is evaluated by pharmacopoeial apparatus, and the registered dissolution medium may contain a surfactant to maintain sink conditions.
Compared with tylosin, another veterinary 16-membered macrolide, kitasamycin differs in the composition of the fermentation-derived leucomycin A homologues and in the number of peaks that must be resolved by HPLC. Tylosin is typically quantified as a single main component, whereas kitasamycin requires summation of multiple active homologues; this difference directly affects assay system suitability and related substances limits. Structural differences include substitution on the macrolactone and the presence of different sugar residues; these alter basicity, lipid solubility, and tissue distribution relative to tilmicosin, a semisynthetic 16-membered macrolide. Compared with erythromycin, a 14-membered macrolide, kitasamycin does not share the 14-membered acid-degradation hemiketal pathway but still requires pH-controlled liquid formulations to limit lactone hydrolysis. Cross-resistance with macrolides, lincosamides, and streptogramin B should be assumed in isolates carrying constitutive or inducible erm methylase resistance determinants; susceptibility testing should follow CLSI VET01S where interpretive criteria exist, and published breakpoints for kitasamycin are limited in several regions. The compound is used in veterinary medicine primarily against Gram-positive cocci and Mycoplasma species, but treatment indications, dose rates, and withdrawal periods are species-specific and must be taken from approved product labels or regional regulatory monographs.
