| HS Code | 711934 |
| Product Name | Sulphamerazine Sodium Pharma Grade API |
| Category | Active Pharmaceutical Ingredient |
| Grade | Pharma Grade |
| Dosage Forms | Tablet, Capsule, Granule, Injection |
| Routes Of Administration | Oral, Injectable |
| Cas Number | 127-58-2 |
| Molecular Formula | C11H11N4NaO2S |
| Molecular Weight | 286.29 g/mol |
| Physical State | Crystalline Powder |
| Color | White to Slightly Yellow |
| Solubility | Freely Soluble in Water, Slightly Soluble in Ethanol |
| Assay | 98.0% - 101.0% (on Dried Basis) |
| Storage Conditions | Store in a Cool, Dry Place, Protected from Light and Moisture |
| Shelf Life | Typically 24 Months When Properly Stored |
| Packaging | Sealed Double Polythene Bags Inside HDPE Drum or as per Pharmacopoeia Requirement |
As an accredited Sulphamerazine Sodium 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 | Supplied in sealed, moisture-proof drums with tamper-evident closures. Net quantity 25 kg per drum, suitable for pharmaceutical manufacturing. |
| Container Loading (20′ FCL) | A 20' FCL securely loads palletized drums of Sulphamerazine Sodium Pharma Grade API, ensuring safe, dry transport for oral and injectable formulations. |
| Shipping | Sulphamerazine Sodium Pharma Grade API is shipped in sealed, moisture-proof, double-lined HDPE drums or fiber drums. Transport is arranged by air or sea in temperature-controlled, dry containers. Full documentation including MSDS, COA, and export certificates is provided, ensuring safe, compliant delivery for oral and injectable manufacturing. |
| Storage | Store in tightly sealed, light-resistant containers, away from direct sunlight and moisture. Keep in a cool, dry, well-ventilated area at controlled room temperature (15–30°C). Avoid exposure to excessive heat or humidity. Ensure container remains closed when not in use. For injectable grade, maintain stringent protection from contamination and follow pharmacopoeial storage guidelines. |
| Shelf Life | Shelf life is typically 24 months when stored in tightly closed containers, protected from light, moisture, and excessive heat. |
In poultry and swine operations, sulphamerazine sodium is incorporated into water-soluble oral powders that are dispersed into drinking-water systems. The sodium salt is selected because the free acid form exhibits insufficient aqueous solubility for reliable in-line medication at ambient drinking-water temperatures of 5–15°C. A formulator working with pharma grade API typically controls the addition ratio to 10–35% w/w on dried substance, with the remainder composed of lactose monohydrate, anhydrous glucose, and sodium citrate buffer to hold the solution pH between 8.0 and 9.5 after dilution. The downstream process on production-scale equipment starts with a ribbon blender running at 6–12 rpm for 15–20 min; the API is pre-screened through an 800 µm conical sieve to break soft agglomerates. Because the sodium salt is hygroscopic, blending is conducted at ≤40% RH and packaging is completed within 24 h into foil-lined polyethylene sachets. The terminal product is a 100 g, 500 g, or 1 kg sachet or a 5 kg pail for use in batch tanks or proportioner medicators. Compliance testing follows USP <61>, USP <62>, USP <467>, and ICH Q3C for residual solvents; blend uniformity is evaluated under USP <905> and loss on drying under USP <921> with a target moisture of 1.0–2.0% w/w. A recurrent scale-up bottleneck is bulk density variation of the API from different crystallisation campaigns, which shifts the fill weight of volumetric dosing augers; this is corrected by adjusting screw speed or by using gravimetric fillers. The alkaline solution generated by the sodium salt can also raise the pH of hard water, causing precipitation of calcium carbonate in nipple drinkers if the water system is not buffered or acidified. Field data from CMO batch records indicate that segregation of API-rich fines during long auger transfer is the main source of assay deviation, not the primary blending step itself.
Veterinary sulfonamide boluses produced by high-shear wet granulation use sulphamerazine sodium as the primary active load in formulations that commonly range from 25–55% w/w. The API alone has poor flow and compactability, so the manufacturing route is not direct compression; a high-shear mixer with an impeller speed of 200–300 rpm and chopper speed of 1200–1800 rpm granulates the blend with povidone K30 at 2–4% w/w dry granulation mass. Granulation endpoint is controlled by impeller torque, with a target window of 35–55 N·m on a 100 L bowl, corresponding to a wet mass density suitable for transfer to a fluid-bed dryer. Drying is performed at inlet air temperature of 55–65°C until loss on drying reaches 1.5–2.5% w/w; over-drying below 1.0% w/w increases dust and reduces tablet hardness, while residual moisture above 3.0% w/w causes sticking on the tablet press. The dried granules are milled through a 0.8–1.25 mm screen and blended with crospovidone 2–4% w/w and magnesium stearate 0.5–1.0% w/w. Compression is carried out on a rotary tablet press with precompression force of 3–5 kN and main compression force of 10–18 kN, producing 500 mg and 1 g veterinary boluses with a hardness range of 80–150 N. In-process control includes USP <905> uniformity of dosage units and USP <1216> friability; release testing includes USP <711> dissolution in phosphate buffer pH 7.2. Terminal products include single-dose blister packs and bulk bottles of 100 or 500 boluses for veterinary distribution. The process is sensitive to API particle size; a D90 above 250 µm produces granule porosity that lowers tablet hardness, while a D50 below 50 µm can raise granulation liquid requirement by 10–15% and increase drying time.
The manufacture of an injectable sulphamerazine sodium preparation is constrained by the narrow pH window between complete dissociation of the free acid and alkaline degradation of the sulfonamide ring. In aqueous solution at 20–25°C, the sodium salt is typically formulated at 5–20% w/v active substance, with pH adjusted to 9.0–10.5 using 0.1 M hydrochloric acid or 0.1 M sodium hydroxide as needed. Below pH 8.5, precipitation of the poorly soluble free acid can occur on standing, and the resulting particles generate 21 CFR 211.167 visual inspection failures. Above pH 10.8, hydrolysis of the sulfonamide bond becomes measurable after 30 days at 25°C in stability samples. Production-scale dissolution is performed in 316L stainless steel vessels under nitrogen blanketing to limit oxygen ingress; dissolution time at 100–200 rpm is 20–40 min depending on API particle size. The solution is cooled to 2–8°C before filtration and then passed through a 0.45 µm clarifying filter followed by a 0.22 µm sterilising-grade polyethersulfone membrane cartridge with a filtration area of 0.6 m² per 100 L batch. Terminal sterilisation by autoclave at 121°C for 15 min is used only when the marketing authorisation demonstrates thermal stability; otherwise aseptic filtration and filling are mandatory. Filling is performed in a Grade A laminar-flow zone with Type I borosilicate glass vials of 50 mL, 100 mL, or 250 mL capacity, closed with bromobutyl rubber stoppers. The terminal product is an injectable solution for intramuscular or slow intravenous administration after dilution in 5% dextrose or 0.9% sodium chloride injection; multi-dose vials may require an antimicrobial preservative, but any preservative must be tested for compatibility with the alkaline pH. The main batch-to-batch failure observed on filling lines is filter flux decay caused by insufficient pre-filtration when API particle size D90 exceeds 150 µm, leading to loading of the sterilising filter and pressure drops above 1.0 bar.
| Release Test | Standard Designation | Typical Limit |
|---|---|---|
| Sterility | USP <71> | Sterile |
| Bacterial endotoxins | USP <85> | ≤0.5 EU/mg |
| Subvisible particulate matter | USP <788> | For 100 mL: NMT 6000 particles > 10 µm and 600 particles > 25 µm |
| Visible particles | USP <790> | No visible particles |
| Residual solvents | USP <467>, ICH Q3C | Per authorised specification |
When a dry oral solid dosage form is required for precision unit dosing in small animals or for extemporaneous dispensing, sulphamerazine sodium is filled into hard gelatin or HPMC capsules after roller compaction. The addition ratio is usually 20–40% w/w on dried basis, with the remainder composed of microcrystalline cellulose, pregelatinised starch, croscarmellose sodium 2–4% w/w, and magnesium stearate 0.5–1.0% w/w. The process begins with dry blending in a 300 L bin blender at 10–15 rpm for 20 min, followed by roller compaction at a hydraulic pressure of 40–80 bar and a gap of 2–3 mm; the compacted ribbons are milled through a 1.0 mm screen to form granules with a target D50 of 200–350 µm. The granules are then filled into size 0 or size 1 hard gelatin capsules on a tamping-pin capsule machine at 60,000–100,000 capsules/h, with an in-process weight variation limit of ±5.0% or tighter. Environmental control is critical: processing is maintained at 20–25°C and ≤40% RH because the sodium salt absorbs moisture above 40% RH and the gelatin shell becomes brittle below 30% RH. The terminal products are 250 mg and 500 mg capsules for veterinary oral administration, packaged in PVC/PVDC blisters with desiccant. Quality methods include USP <905> for capsule weight variation, USP <711> dissolution using apparatus 1 at 100 rpm in 900 mL of pH 7.4 buffer, and USP <921> for moisture. A known production failure is capsule shell crosslinking when storage temperature exceeds 30°C and moisture from the formulation migrates into the shell; this is reduced by pre-drying the granules to 1.0–2.0% w/w at 40°C in a vacuum dryer before filling.
For oral granules that dissolve rapidly in drinking water, fluid-bed spray granulation is an alternative to dry blending when the target addition ratio is 15–45% w/w sulphamerazine sodium and the finished product must have a controlled granule size of 150–250 µm D50. In top-spray mode, a lactose monohydrate or mannitol carrier is charged to the fluid bed, and an aqueous solution of the API is sprayed through a 1.2 mm two-fluid nozzle at atomisation air pressure of 1.0–1.5 bar, spray rate of 8–15 g/min/kg, and inlet air temperature of 45–55°C. The API solution concentration is held at 20–30% w/w because above 30% w/w the sodium salt solution becomes viscous and leads to nozzle fouling; below 20% w/w the spray run time extends beyond 90 min and causes excessive attrition of the carrier granules. The process is stopped when the product temperature reaches 35°C or the loss on drying falls to 1.0–1.8% w/w. Granules are then discharged through a 0.8 mm sieve and packed into 5 g, 20 g, or 100 g sachets with a trilaminate barrier film. Release testing for this granule form includes USP <711> dissolution with a 15-min specification of ≥80% released, USP <61>/USP <62> microbial limits, and ISO 13320 laser diffraction for particle size. The terminal product is used by mixing one sachet into a predetermined volume of drinking water in a stock tank; the uniform granule size prevents segregation and floating. The principal processing limit is that the sodium salt solution pH above 10.0 can plasticise certain hydroxypropylmethylcellulose film coatings if a coated granule is required; uncoated granules are therefore preferred unless a pH-stable polymer is selected.
Fixed-dose tablet lines that combine sulphamerazine sodium with other sulfonamides, such as sulfadiazine and sulfamethazine, present a formulation challenge because the sodium salt contributes alkalinity that can accelerate hydrolytic degradation of co-active substances. The sulphamerazine sodium addition ratio in such fixed-dose blends is generally limited to 10–25% w/w, while total sulfonamide load may be 40–70% w/w; the sodium salt is pre-mixed with dibasic calcium phosphate dihydrate and croscarmellose sodium 2–4% w/w before the other actives are added to avoid localised high pH spots. Granulation is performed in a high-shear mixer with an impeller speed of 250 rpm and chopper at 1500 rpm; the binder solution is prepared with 50% ethanol/50% water to reduce solubilisation of the sodium salt during granulation, and the wet mass is dried at 40–50°C to a final moisture of 1.5–2.5% w/w. The dried granules are milled to a D50 of 150–300 µm and compressed at 12–16 kN on a rotary press to 800 mg or 1 g tablets. Compendial compliance requires USP <905>, USP <1216>, and USP <711> dissolution in 0.1 M hydrochloric acid or phosphate buffer, depending on the marketing authorisation; residual solvent levels are controlled under USP <467> and ICH Q3C. Terminal products include foil-wrapped veterinary tablets and, in jurisdictions where such fixed-dose human formulations remain authorised, hospital unit-dose strips. Published data for the three-active blend stability is limited, but batch records from compounding facilities indicate that the free acid form of sulfamerazine is preferred when the pH of the granulating fluid falls below 6.0 because the sodium salt raises the equilibrium pH and changes the dissolution profile of the fixed-dose combination.
Competitive Sulphamerazine Sodium Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable prices that fit your budget—flexible terms and customized quotes for every order.
For samples, pricing, or more information, please contact us at +8615365186327 or mail to admin@ascent-chem.com.
We will respond to you as soon as possible.
Tel: +8615365186327
Email: admin@ascent-chem.com
Flexible payment, competitive price, premium service - Inquire now!
Sulphamerazine Sodium Pharma Grade API is the sodium salt of N-(4-methylpyrimidin-2-yl)sulfanilamide, supplied as a white to off-white crystalline powder with molecular formula C11H11N4NaO2S and CAS 127-58-2. The product is released in two grade designations for oral solid and injectable manufacture: SMRZ-Na-PG-M75, a micronized oral-grade powder with D90 ≤ 75 µm, and SMRZ-Na-PG-I, an injection-grade material with bacterial endotoxin and subvisible particulate controls suitable for aqueous filling and terminal filtration. The sodium salt form is freely soluble in water and yields an alkaline solution, which makes it suitable for tablet, capsule, granule, oral suspension, and injectable solution or lyophilized dosage forms where the free acid cannot provide the required dissolution rate. The counterion contributes approximately 8.0% w/w sodium, and the dry powder is sufficiently hygroscopic to require low-humidity handling below RH 40% in oral solid dispensing suites. Sulphamerazine sodium is used as a sulfonamide antibacterial active pharmaceutical ingredient; the choice of grade depends on the manufacturing route and the allowable sodium load in the finished formulation.
Dispensing and sampling of SMRZ-Na-PG-M75 require defined ambient controls because the micronized API exhibits charge-induced adhesion to polypropylene and aluminium contact surfaces. Observed operational experience on production-scale drum lifters shows that relative humidity above 45% creates partial surface hydration and leads to inconsistent gravimetric feeding from twin-screw loss-in-weight feeders. The API is therefore transferred through polyethylene-lined drums and charged into the granulation suite under nitrogen overlay when prolonged residence time is expected. Bulk density of the micronized grade typically ranges from 0.28 g/mL to 0.42 g/mL, and the powder should not be compacted by extended storage in deep containers; consolidation increases the force required for initial screw feeder rotation and can produce mass-flow variability in tablet and capsule lines. Particle-size distribution is confirmed by laser diffraction according to Ph. Eur. 2.9.31, with the oral-grade D50 typically controlled between 25 µm and 45 µm.
Release of SMRZ-Na-PG-M75 includes identification by infrared absorption and sodium flame test, assay by validated HPLC or pharmacopoeial nitrite titration, loss on drying, pH of a 50 g/L aqueous solution, related substances, residual solvents per USP <467>, and elemental impurities per ICH Q3D. The injection-grade SMRZ-Na-PG-I is additionally controlled for bacterial endotoxins using Ph. Eur. 2.6.14 or USP <85>, and for subvisible particles using Ph. Eur. 2.9.19 or USP <788>. Because the sodium salt contains no organic counterion, the sulfated ash test provides a further check on sodium stoichiometry. Acceptable quality for parenteral manufacture requires that individual specified related substances remain below 0.2%, the total related substance burden remain below 0.5%, and residual solvents be controlled to ICH Q3C limits. Water content in the injectable grade is typically held below 0.5%; higher water content accelerates sintering and discolouration during storage and can complicate gravimetric dispensing into closed processing systems. Bacterial endotoxin acceptance is calculated from the intended maximum human dose using Ph. Eur. 5.1.10; for injectable material, an upper control of 0.30 EU/mg is commonly applied unless the dosage and route require a lower limit.
| Attribute | Oral-grade SMRZ-Na-PG-M75 | Injectable-grade SMRZ-Na-PG-I |
|---|---|---|
| Particle-size specification | D90 ≤ 75 µm; D50 25–45 µm | Dissolves to clear solution at 100 g/L; particulate content controlled |
| Loss on drying | ≤ 0.5% | ≤ 0.5% |
| pH of 50 g/L solution | 9.0–10.5 | 9.0–10.5 |
| Bacterial endotoxins | Not routinely tested | ≤ 0.30 EU/mg unless otherwise justified |
| Subvisible particles | Not applicable | Meets Ph. Eur. 2.9.19 after dissolution and filtration |
| Reference methods | HPLC/UV, USP <731>, Ph. Eur. 2.2.32, USP <467> | Plus Ph. Eur. 2.6.14, USP <85>, Ph. Eur. 2.9.19 |
Tablet and capsule manufacture using SMRZ-Na-PG-M75 is characterized by cohesiveness and a tendency toward electrostatic retention in non-grounded mixing vessels. Flowability measured as Hausner ratio is commonly above 1.40 before granulation, so direct compression is replaced by wet granulation or roller compaction when the API fraction exceeds 40% w/w. In a high-shear granulator with a 10 L bowl and chopper speed of 1500 rpm, the wet mass endpoint is reached at a liquid-to-solids ratio of 0.25–0.35 L/kg when purified water is sprayed onto a preblend of the sodium salt, microcrystalline cellulose, and pregelatinized starch. Torque-rise endpoint detection is attenuated because the sodium salt partially dissolves in the binder, reducing the viscosity contrast between wet granules and dry powder. Drying in a fluid-bed dryer with inlet air at 55–65 °C and exhaust relative humidity below 20% brings granule moisture to 1.5–2.5%; moisture above 3.0% produces picking on rotary presses and increases ejection force by more than 15% in 8.0 mm standard concave tooling. Roller compaction with ribbed rolls at 30–50 kN/cm and screen milling to D50 150–250 µm produces granules with sufficient bulk density; excessive compaction pressure may induce particle-surface amorphization and increase dissolution variability.
Direct compression is feasible only when the total drug load is low and the excipient platform is designed with high-flow co-processed fillers such as spray-dried lactose, microcrystalline cellulose, and dibasic calcium phosphate anhydrous. Even then, the sodium salt should be premixed with a magnesium stearate-free portion of the intragranular phase before lubrication because the alkaline particle surface can deprotonate fatty acid boundary lubricants and reduce their shear-thinning capacity at the die wall. In a tableting run using a rotary press at 40 rpm and a compression force of 12–18 kN, ejection force fluctuations of more than 10% have been reduced by adding 0.5% w/w sodium stearyl fumarate and by maintaining punch-face surface roughness below 0.10 µm Ra. If the formulation contains croscarmellose sodium, the disintegrant is dry-mixed as the final intragranular additive to prevent localized alkalinity from initiating the formation of coloured sulfonamide oxidation products during accelerated storage. In-process control includes tablet hardness, friability, and disintegration time according to USP <701> and Ph. Eur. 2.9.1.
Parenteral processing with SMRZ-Na-PG-I begins with dissolution in Water for Injections at 25–35 °C under nitrogen purge. A 100 g/L solution reaches a pH of 9.0–10.0; adjustment with sterile hydrochloric acid is used to maintain the pH in the target range because pH values below 8.0 can reduce the proportion of ionized sulfonamide and risk precipitation of the poorly soluble free acid during terminal sterilization or storage. The solution is passed through a 0.45 µm clarifying filter followed by a 0.22 µm sterilizing-grade filter; filter compatibility should be confirmed because some positively charged nylon membranes can retain the anionic sulfonamide species and decrease delivered potency. Filled vials are terminally sterilized at 121 °C for 15 minutes only when the maximum temperature loading in the chamber has been mapped in the presence of maximum fill volume; unprotected solutions may develop yellow-brown discolouration, so headspace oxygen is reduced to below 2.0% by nitrogen overlay before capping. For lyophilized products, the sodium salt is dissolved and freeze-dried with a crystalline bulking agent such as mannitol; chamber pressure and shelf temperature are controlled to avoid collapse of the alkaline solution during primary drying.
Stability of aqueous SMRZ-Na-PG-I solutions is controlled by dissolved oxygen, trace-metal load, light exposure, and pH. In-process polarographic oxygen measurement is used to reject batches with dissolved oxygen above 1.0 mg/L before filling; this limit reduces the rate of oxidative chromophore generation. The solutions are filled into amber borosilicate vials or covered with light-protective secondary packaging because the aromatic sulfonamide chromophore is photolabile under ICH Q1B stress conditions. Compatibility with normal saline should be confirmed at the intended final concentration; published data for this specific configuration are limited. Calcium-containing infusions are avoided unless specifically tested because the free acid may precipitate when the local pH is reduced below 8.0. Long-term stability programmes follow ICH Q1A(R2) and include pH, assay, related substances, subvisible particulate matter, and colour; intermediate and accelerated stations are used only after confirming that glass delamination is not accelerated by the alkaline drug solution. Terminal sterilization validation includes heat distribution, heat penetration, and biological indicators with Geobacillus stearothermophilus according to Ph. Eur. 5.1.1 or equivalent compendial sterility assurance requirements.
Sulphamerazine sodium differs from sulfadiazine sodium and sulfamethazine sodium in the number of methyl substituents on the pyrimidine ring; the single methyl group of sulphamerazine provides an intermediate polarity between the unmethylated sulfadiazine sodium and the dimethylated sulfamethazine sodium. This affects aqueous solubility, partition coefficient, and the solubility of the acetylated metabolite in urine; clinical use therefore requires attention to hydration status rather than assuming interchangeability with other sulfonamide salts. The sodium contribution of 8.0% w/w is lower than the corresponding sulfadiazine sodium salt and higher than sulfamethazine sodium salt, and this must be included in the sodium-load calculation for parenteral infusions. The free acid is only slightly soluble in water, so replacement of the sodium salt with the free acid in an injectable formulation is not a simple stoichiometric adjustment: it eliminates the alkalinity and may require a micronized suspension or pH adjustment that is not always suitable for intravenous administration. Compared with the free acid, the sodium salt removes the dissolution-rate barrier in oral solid formulations but introduces greater hygroscopicity, alkaline surface chemistry, and a direct effect on tablet ejection force.
| Parameter | Sulphamerazine Sodium | Sulphamerazine Free Acid | Sulfadiazine Sodium |
|---|---|---|---|
| Molecular mass | 286.29 g/mol | 264.31 g/mol | 272.27 g/mol |
| Sodium content | 8.0% w/w | 0 | 8.4% w/w |
| Aqueous solubility class | Freely soluble | Slightly soluble | Soluble |
| Primary processing route | Wet granulation, fluid-bed granulation, aqueous injection | Micronized suspension, dry granulation where sodium intake must be limited | Aqueous injection, oral liquid |
Granulation of SMRZ-Na-PG-M75 for coated tablets commonly uses a binder solution containing povidone K30 at 3–5% w/w in purified water. The formulation is designed to avoid acid-sensitive film coatings based on methacrylic acid copolymers, because the alkaline surface of the sodium salt can neutralize the enteric-polymer acid groups and compromise delayed-release functionality. Immediate-release tablets containing 250 mg of sulphamerazine sodium can be coated with a hypromellose-based film system at a weight gain of 2–3% w/w, provided the inlet-air dew point is maintained below 10 °C and the tablet bed temperature is kept between 38 °C and 42 °C. Capsule filling is performed with a dosator or tamping-style machine under RH 35% or lower; higher humidity increases powder adherence to the interior of gelatin capsules and may increase brittleness of the capsule shell during banding. For granules intended for oral suspension, reconstitution behaviour is tested in water at 25 °C, and the granule fraction is controlled to avoid fine particles that float on the meniscus and coarse particles that settle rapidly; the target dry granule distribution is typically D10 ≥ 75 µm and D90 ≤ 710 µm.
