| HS Code | 773882 |
| Product Name | Kanamycin Acid Sulfate Pharma Grade API |
| Api Grade | Pharma Grade |
| Therapeutic Category | Aminoglycoside Antibiotic |
| Dosage Forms | Tablet, Capsule, Granule, Injection |
| Administration Route | Oral and Injectable |
| Chemical Name | 4-O-(3-amino-3-deoxy-alpha-D-glucopyranosyl)-6-O-(6-amino-6-deoxy-alpha-D-glucopyranosyl)-2-deoxy-D-streptamine sulfate acid salt |
| Cas Number | 25389-94-0 |
| Molecular Formula | C18H36N4O11·H2SO4 |
| Molecular Weight | 582.58 g/mol |
| Appearance | White or almost white crystalline powder |
| Odor | Odorless or almost odorless |
| Taste | Bitter |
| Solubility | Freely soluble in water; very slightly soluble in ethanol; practically insoluble in ether and chloroform |
| Hygroscopic Nature | Hygroscopic |
| Storage Conditions | Store in a tightly closed container protected from moisture, heat, and light |
| Product Name | Kanamycin Acid Sulfate Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable |
| Api Name | Kanamycin Acid Sulfate |
| Drug Class | Aminoglycoside antibiotic |
| Cas Number | 25389-94-0 |
| Molecular Formula | C18H36N4O11·H2SO4 |
| Molecular Weight | 582.58 g/mol |
| Appearance | White to off-white crystalline powder |
| Solubility | Freely soluble in water; practically insoluble in ethanol, acetone, and ether |
| Melting Point | Decomposes above approximately 250°C |
| Specific Optical Rotation | Approximately +112° to +123° in water |
| Ph | 4.5 to 7.0 for a 1% aqueous solution |
| Storage Conditions | Store in a tightly closed container, protected from light and moisture, below 25°C |
| Route Of Administration | Oral and injectable |
| Dosage Forms | Tablet, capsule, granule, and injection |
As an accredited Kanamycin Acid Sulfate 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 | Packaged in 25 kg sealed drums with double polyethylene liners, protected from moisture and contamination for oral and injectable use. |
| Container Loading (20′ FCL) | A 20' FCL container loaded with Kanamycin Acid Sulfate Pharma Grade API, packed in sealed drums, palletized, secure for oral and injectable use. |
| Shipping | Kanamycin Acid Sulfate Pharma Grade API (for tablet, capsule, granule, oral & injectable formulations) ships in sealed, tamper-evident containers with desiccant. Requires dry, temperature-controlled transport (15–30°C), away from light and moisture. For professional pharmaceutical manufacturing only. Ensure compliant documentation, safety data sheet, and cold-chain integrity per regulatory requirements. |
| Storage | Store Kanamycin Acid Sulfate Pharma Grade API in tightly sealed, light-resistant containers in a cool, dry, well-ventilated area. Maintain controlled room temperature, protect from moisture, humidity, and direct sunlight. Avoid exposure to excessive heat. Ensure container integrity until use to preserve stability for tablet, capsule, granule, and injectable formulations. |
| Shelf Life | Stable for 3 years when stored in a cool, dry place, protected from moisture and light, in its original container. |
Direct compression of kanamycin acid sulfate immediate-release tablets for enteric Gram-negative and anaerobic gut decontamination is constrained by the hygroscopicity of the sulfate salt and its tendency to form adherent compacts under elevated relative humidity. The API is first dry-sieved through a 500 μm screen to remove agglomerates, and residual water content is confirmed at not more than 2.0% w/w by USP <921>. In a representative 250 mg kanamycin acid sulfate tablet, the API addition ratio is 35–65% w/w of the core weight, with microcrystalline cellulose at 20–40% w/w, croscarmellose sodium at 2–5% w/w, colloidal silicon dioxide at 0.5–1.0% w/w, and magnesium stearate at 0.5–1.5% w/w; the actual API weight is adjusted against the assay potency of the incoming lot. Blending is performed in a V-blender or bin blender at 8–12 rpm for 10–15 min, and the blend is compressed on a rotary tablet press equipped with precompression rolls set at 5–8 kN and main compression rolls at 12–18 kN. Tablet hardness is maintained at 80–120 N, friability is controlled to not more than 1.0% w/w, and disintegration time is not more than 15 min in 900 mL water at 37°C under USP <701>. Dissolution release is assessed by USP <711> in 900 mL pH 6.8 phosphate buffer at 50 rpm, with 80% of label claim released within 30 min as a typical acceptance criterion. Compliance for the finished tablet includes USP <905> for content uniformity, 21 CFR 211.165 for batch testing, 21 CFR 211.166 for stability, and ICH Q3D for elemental impurities. The finished product type is an aqueous film-coated immediate-release tablet, with an HPMC-based coating at 2–4% w/w total weight gain, intended for oral intestinal antisepsis.
For hard gelatin and HPMC capsule filling of kanamycin acid sulfate, roller compaction is used instead of direct powder filling because the API sieve fraction and electrostatic charge can cause tamping-pin or dosator fill weight drift on high-speed encapsulation lines. The granulated composition consists of kanamycin acid sulfate at 40–70% w/w, pregelatinized starch or microcrystalline cellulose at 15–35% w/w, crospovidone at 2–4% w/w, and colloidal silicon dioxide at 0.5–1.0% w/w. Roller compaction is run at roll pressure 30–50 bar, roll gap 1.5–2.5 mm, and roll speed 3–8 rpm; the compacted ribbons are milled through a 1.0 mm screen to yield granules with bulk density 0.45–0.65 g/mL, tapped density 0.55–0.80 g/mL, and Carr index not more than 25. Capsule filling is performed on a tamping-pin or dosator machine at 60,000–120,000 capsules/hour, with fill weight control within ±5% of target and segregation checks every 30 min. In-process blend uniformity is verified under 21 CFR 211.110, while the finished capsules are tested for content uniformity per USP <905> and dissolution per USP <711> under aqueous conditions because the API is freely soluble in water. The finished product types are hard gelatin or HPMC capsules in size 0 or 1, containing the equivalent of 250 mg or 500 mg kanamycin acid sulfate, used for susceptible enteric infections and presurgical bowel antisepsis.
When oral granules are produced by high-shear wet granulation in a top-driven mixer, kanamycin acid sulfate is loaded at 45–75% w/w dry basis with lactose monohydrate and povidone K30; the binder solution is purified water or a 5% w/v povidone K30 solution, added at 10–15% w/w of the dry powder mass. Granulation endpoint is controlled by impeller power consumption rather than fixed time alone; impeller speed is maintained at 150–250 rpm and chopper speed at 1000–1500 rpm until the power curve reaches a plateau indicative of dense granule growth. The wet mass is screened through a 2000 μm sieve and dried in a fluid-bed dryer at inlet air temperature 55–65°C, product temperature not exceeding 40°C, and endpoint moisture not more than 1.5% w/w. The dried granules are passed through a 1000 μm mill and sifted to retain not more than 20% w/w below 150 μm, because a high fine fraction raises segregation risk during sachet filling. Sachets are filled on vertical form-fill-seal equipment with relative humidity below 35%, fill weight tolerance ±5%, and seal integrity tested at 50–100 mm Hg vacuum decay. Compliance includes USP <711> dissolution testing in 900 mL pH 6.8 phosphate buffer with paddle speed 50 rpm, USP <905> for unit-dose uniformity, and 21 CFR 211.165 for release. The terminal finished product type is a single-dose oral granule in sachet form, either placed on the tongue and swallowed with water or dispersed in 30–50 mL water immediately before administration for intestinal antisepsis.
| Oral solid form | Kanamycin acid sulfate addition | Critical excipient ratio | Key process control | Terminal product |
|---|---|---|---|---|
| Immediate-release tablet | 35–65% w/w | MCC 20–40% w/w; croscarmellose sodium 2–5% w/w; magnesium stearate 0.5–1.5% w/w | Hardness 80–120 N; disintegration <15 min; residual water <2.0% w/w | Film-coated tablet |
| Hard gelatin/HPMC capsule | 40–70% w/w | Pregelatinized starch 15–35% w/w; crospovidone 2–4% w/w; colloidal silicon dioxide 0.5–1.0% w/w | Roll pressure 30–50 bar; Carr index <25; fill weight ±5% | Hard capsule |
| Oral granule in sachet | 45–75% w/w | Lactose monohydrate; povidone K30 2–5% w/w; granulation water 10–15% w/w | Product temperature <40°C; moisture <1.5% w/w; sachet fill ±5% | Single-dose sachet |
Terminal steam sterilization of kanamycin acid sulfate injection solutions is limited by pH drift and color formation during thermal exposure, which are accelerated above pH 5.5 and by residual oxygen in headspace. The bulk solution is compounded with kanamycin acid sulfate equivalent to 50–250 mg/mL kanamycin base; a tonicity agent, when required, is added to target osmolality 280–320 mOsmol/kg; the solution pH is adjusted to 3.5–5.5 with 0.1 N sulfuric acid or sodium hydroxide. After dissolution and mixing, the solution is sparged with nitrogen to reduce dissolved oxygen below 0.5 mg/L, then clarified through 0.45 μm and sterilized through 0.22 μm filters. Filling into Type I glass ampoules or vials is performed under ISO 14644-1 Class 5 environmental conditions with continuous particle monitoring per EU GMP Annex 1. Steam-air or superheated water terminal sterilization at 121°C for 15 min with minimum F0 ≥ 8 is validated by container mapping and biological indicator inhibition. The finished injectable solution is tested under USP <1> Injections for volume and package integrity, USP <71> Sterility Tests, USP <85> Bacterial Endotoxins Test with a container-specific limit derived from maximum dose, and USP <787> Subvisible Particulate Matter for ≥10 μm and ≥25 μm particle counts. Published data for the terminal sterilization of high-concentration kanamycin sulfate formulations is limited; therefore, each container-closure system must undergo thermal challenge studies to establish assay loss, pH drift, and extractables under maximum load. The terminal finished product types are aqueous injectable ampoules or vials for intramuscular administration or intravenous infusion after dilution in sodium chloride injection or dextrose injection.
| Finished product form | Core processing standard | Critical release test | Process boundary |
|---|---|---|---|
| Oral immediate-release tablet | 21 CFR 211.165; ICH Q3D | USP <905>; USP <711> | Residual water <2.0% w/w; processing RH <35% |
| Hard capsule | 21 CFR 211.110 | USP <905>; USP <711> | Fill weight ±5%; Carr index <25 |
| Oral granule sachet | 21 CFR 211.165 | USP <905>; USP <711> | Product temperature <40°C; moisture <1.5% w/w |
| Aqueous injection | EU GMP Annex 1; ISO 14644-1 Class 5 | USP <71>; USP <85>; USP <787> | Lethality F0 ≥ 8; pH 3.5–5.5 |
| Lyophilized injection | EU GMP Annex 1 | USP <71>; USP <85>; USP <921> | Residual water <1.0% w/w; chamber pressure 80–120 μbar |
Once the sterile filtered solution reaches the lyophilizer chamber, collapse and subvisible particle formation are the primary process constraints because kanamycin acid sulfate lyophiles can exhibit low glass transition temperature in the amorphous fraction if bulking agent concentration is inadequate. The fill solution is prepared with kanamycin acid sulfate equivalent to 50–150 mg/mL kanamycin base, mannitol or glycine at 5–10% w/v as a crystalline bulking agent, and water for injection adjusted to pH 3.5–5.5. The solution is aseptically filtered through 0.22 μm filters, filled into 10 mL Type I glass vials at 2–10 mL fill volume, and partially stoppered with elastomeric closures. Lyophilization begins with freezing at shelf temperature -40°C for 2–4 h, followed by primary drying at shelf temperature -20°C and chamber pressure 80–120 μbar for 18–36 h, then secondary drying at shelf temperature 25–30°C for 6–12 h to residual moisture not more than 1.0% w/w by USP <921>. The vials are stoppered under vacuum or sterile nitrogen at 50–70 kPa, with moisture ingress prevented by closure integrity testing using vacuum decay or helium leak. Compliance is demonstrated under USP <1> Injections for reconstitution time and particulate content, USP <71>, USP <85>, USP <787>, and EU GMP Annex 1 for loading, partial stoppering, and capping. Operational boundaries include shelf temperature not exceeding the collapse temperature during primary drying and residual moisture not above 1.5% w/w in stored product; however, published data on the collapse temperature of this specific kanamycin acid sulfate formulation is limited, so lyophilization cycle design requires thermal characterization by freeze-drying microscopy and modulated DSC. The terminal finished product type is a lyophilized powder in a Type I glass vial, reconstituted with sterile water for injection to a clear solution before intramuscular or intravenous infusion.
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Kanamycin Acid Sulfate Pharma Grade API is a fermentation-derived aminoglycoside antibiotic supplied as the sulfate salt of kanamycin A. The salt has the molecular formula C18H36N4O11·H2SO4, CAS 25389-94-0, and a molecular weight of 582.58 g/mol; the free base molecular weight is 484.50 g/mol. Manufacturer model codes differentiate sterile injectable powder, non-sterile oral powder, micronized granulation-grade material, and compacted direct-compression material. These codes are not pharmacopoeial identifiers; they are assigned in the certificate of analysis and regulatory dossier to link the physical grade to specific downstream processing requirements. The product is intended for oral and injectable dosage forms, including tablets, capsules, granules, and sterile injection preparations. In aqueous media the acid sulfate is freely soluble, whereas ethanol, chloroform, and ether are practically insoluble. This solubility differential governs formulation selection: injectable concentrates rely on complete dissolution, while oral solid dosage forms use the crystalline or spray-dried powder after blending with excipients.
Route-specific pharmacopoeial alignment follows the current USP Kanamycin Sulfate monograph, the European Pharmacopoeia monograph for Kanamycin monosulfate, and the Japanese Pharmacopoeia where applicable. A finished-dose application must distinguish between oral and injectable API grades because the microbial and particulate requirements are not identical. Oral grades are controlled for potency, related substances, water content, and residual solvents. Injectable grades additionally require bacterial endotoxin testing according to USP <85>, sterility testing according to USP <71> when a sterile claim is made, and particulate matter testing according to USP <788>. Relevant general chapters include USP <791> for pH, USP <731> for loss on drying, USP <781> for specific optical rotation, and USP <281> for residue on ignition.
| Parameter | Representative acceptance criterion | Method / chapter |
|---|---|---|
| Appearance | White to almost white powder | Visual inspection |
| Identification | Infrared spectrum matches reference; chromatographic retention time matches standard | USP <197>, EP 2.2.24 |
| pH of 10% aqueous solution | 6.5–8.0 | USP <791> |
| Specific optical rotation | +112° to +123°, anhydrous basis | USP <781> |
| Loss on drying | NMT 1.5%; hygroscopic grades NMT 3.0% | USP <731> |
| Residue on ignition | NMT 0.5% | USP <281> |
| Potency | 750–850 µg/mg on dried basis | HPLC or microbial assay |
| Related substances | Total impurities NMT 2.0%; any individual impurity NMT 1.0% | HPLC |
| Bacterial endotoxins | Injectable grade ≤0.67 EU/mg | USP <85> |
| Sterility | Sterile grade complies | USP <71> |
| Particulate matter | Meets injectable limits | USP <788> |
| Residual solvents | Class 3 solvents NMT 0.5% | USP <467> |
For oral solid dosage forms, particle size distribution is controlled because it influences granulation end point, flow, compaction, and content uniformity. Laser diffraction is performed under ISO 13320:2020 or USP <429>. A direct-compression acid sulfate grade may be specified with D90 ≤ 200 µm and bulk density 0.45–0.65 g/mL; a spray-dried wet-granulation grade may be delumped to D50 20–40 µm to permit even wetting by binder solution. For injectable use, the dissolved API no longer possesses a particle size distribution, but the manufacturing process must still meet subvisible particulate limits. Filtration of the bulk solution through 0.22 µm polyvinylidene fluoride or polyethersulfone membrane filters is validated with the specific solution viscosity, pH, and temperature; published data for this specific configuration is limited to the applicant's filter compatibility studies.
In high-shear wet granulation, kanamycin acid sulfate is blended with microcrystalline cellulose and pregelatinized starch before addition of purified water or a 5% w/w povidone binder. The granulation end point is monitored by loss on drying; a target of 1.5–2.5% w/w moisture before compression is maintained because residual moisture above 3.0% w/w raises the risk of picking and sticking on rotary tablet tooling. Roller compaction at roll pressure 40–80 kN and roll gap 2–4 mm is preferred for moisture-sensitive or high-dose formulations, followed by milling to a granule D50 of 150–250 µm. Capsule filling uses tamping or dosator systems; weight variation is monitored according to USP <905> with acceptance criteria derived from the finished dosage form.
Wet granulation at pilot scale uses a 25 L high-shear granulator with impeller tip speed 5–10 m/s, wet massing time 4–8 min, and fluid-bed drying at inlet air temperature 50–60°C. These parameters are not pharmacopoeial; they are equipment-dependent and should be re-established for each production line. The granulation is milled through a 1.0–1.5 mm screen and blended with disintegrant and lubricant. Tablet compression is performed on a rotary press with precompression force 4–8 kN and main compression force 12–20 kN to achieve hardness 60–120 N depending on tablet size. Capsule filling uses tamping pins at 60–80% of maximum compaction to control weight variation.
Because kanamycin acid sulfate can degrade under alkaline conditions and is hygroscopic, formulations avoid moisture-retentive excipients at high levels. The powder blend is dried to LOD 1.5–2.0% w/w before dry granulation; ribbons are compacted at 4–8 mm thickness and milled with 1.0 mm screen. The granule fraction between 125 µm and 850 µm is retained for compression; fines below 125 µm are recycled at a rate not exceeding 20% w/w to avoid variability in granule porosity.
Hygroscopicity imposes an operational boundary. Kanamycin acid sulfate should be handled in a conditioned suite at 20–25°C and RH below 60%; above this threshold, moisture uptake changes flow function and can cause clumping in the feed hopper. Containers are double polyethylene bags inside sealed aluminium foil with desiccant; after opening, the material should be reconditioned or used promptly. If a batch is exposed to RH > 60% for more than 4 h, re-testing of water content and flowability is recommended before compression.
Kanamycin acid sulfate injection concentrates are prepared at strengths up to 333 mg/mL. Terminal sterilization in an air-over-pressure autoclave at 121°C for 15 min may be employed if the drug product remains within color and impurity limits. Autoclaving at 250 mg/mL solution strength and pH 4.5–5.5 requires heat penetration and F0 data; published data for this specific configuration is limited, but the applicant must submit terminal sterilization validation. If the related substance increase exceeds the monograph limit, aseptic filtration is selected. Filtration is performed with a 0.22 µm polyethersulfone filter at a flux of 100–300 L/m²/h and differential pressure below 1.0 bar. Filter integrity is tested by bubble point or diffusion per manufacturer specifications.
For parenteral administration, the endotoxin limit is calculated from the maximum intended dose and the route; a common injectable kanamycin sulfate API specification is ≤0.67 EU/mg. The filtered solution is filled under nitrogen in amber Type I glass vials or prefilled syringes. Depyrogenation of vials is performed at 250°C for not less than 30 min according to validated tunnel parameters. The final product must meet osmolality and pH ranges defined in the dossier, and visible particles are assessed under light per USP <790>. Kanamycin acid sulfate must not be mixed with beta-lactam antibiotics in the same infusion container. Aminoglycosides react with penicillins and cephalosporins in aqueous solution, reducing potency of both active moieties. If coadministration is required, separate intravenous lines should be used.
Kanamycin acid sulfate is produced by fermentation of Streptomyces kanamyceticus and purification of the sulfate salt; amikacin sulfate is a semisynthetic aminoglycoside prepared by acylation of kanamycin A. The difference in origin changes the impurity profile. Fermentation-derived kanamycin acid sulfate must control residual kanamycin B and kanamycin C homologues as well as processing impurities, whereas amikacin sulfate must also control acylating reagents and semisynthetic by-products. Compared with neomycin sulfate, kanamycin acid sulfate is used systemically as well as orally; neomycin sulfate is more frequently restricted to topical or oral local therapy due to a more pronounced nephrotoxic and ototoxic burden. Published data for cross-product equivalence is limited; substitution between aminoglycosides is determined by susceptibility testing and the approved label.
Kanamycin base is practically insoluble in water; acid sulfate salt formation provides freely soluble ionizable species that dissolve rapidly in aqueous fluids. This difference is critical for injectable formulations, where complete dissolution at target concentration must occur without precipitation. The acid sulfate form also differs from kanamycin base in pH of solution and hygroscopicity; the sulfate salt is hygroscopic, requiring moisture-protective packaging and humidity-controlled handling.
Dissolution of kanamycin sulfate tablets is commonly tested with USP <711> apparatus II at 50 rpm in 900 mL of water at 37°C; sampling intervals at 10, 20, 30, 45 min are used to define the release profile. For granules, a similar medium may be used after filling into sachets. The Q value published in the finished product monograph must be met; release profiles are compared using similarity factor f2 where alternative formulations are proposed.
Oral kanamycin sulfate is poorly absorbed through intact gastrointestinal mucosa; systemic bioavailability is generally below 3% of an administered oral dose. Oral tablets, capsules, and granules are therefore used for local intestinal suppression or as an adjunct in hepatic encephalopathy; injectable products are required for systemic therapy. The acid sulfate salt provides rapid dissolution in water and simulated gastric fluid, but the oral product should not be assumed interchangeable with injectable material because the sterile and endotoxin controls are different. The user must verify that the selected API grade matches the intended dosage form and target market monograph.
