| HS Code | 920874 |
| Product Name | 1H-1,2,3-Triazole Pharma Grade API |
| Chemical Name | 1H-1,2,3-Triazole |
| Cas Number | 288-36-8 |
| Molecular Formula | C2H3N3 |
| Molecular Weight | 69.07 g/mol |
| Pharma Grade | API Grade |
| Appearance | Colorless to pale yellow liquid or low-melting solid |
| Purity Assay | ≥99.0% (HPLC) |
| Dosage Forms | Tablet, Capsule, Granule, Injection |
| Routes Of Administration | Oral and Injectable |
| Solubility | Soluble in water, ethanol, and polar organic solvents |
| Storage Conditions | Store in a cool, dry, well-ventilated area, protected from light and moisture |
| Packaging | Amber glass bottle or double polyethylene bag inside fiber drum |
| Shelf Life | 24 months when stored properly in unopened container |
| Pharmacopoeial Compliance | Manufactured under GMP; complies with applicable pharmacopoeial and in-house specifications |
| Hs Code | 29339900 |
As an accredited 1H-1,2,3- Triazole 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.
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In sterile beta-lactamase inhibitor manufacturing, 1H-1,2,3-triazole functions as the N-1 alkylation donor for the penicillanic acid sulfone nucleus that yields tazobactam sodium after sulfone oxidation and ester hydrolysis. Production-scale campaigns for piperacillin/tazobactam fixed-dose vials are governed by FDA 21 CFR 210/211, EU GMP Annex 1, ICH Q7 and ICH Q11 for active pharmaceutical ingredients, plus pharmacopoeial monographs for Tazobactam Sodium USP and Piperacillin and Tazobactam for Injection USP. The terminal bulk solution is controlled under USP <71> sterility, USP <85> bacterial endotoxin, USP <790> particulate matter in injections, and Ph. Eur. 2.6.14 bacterial endotoxin testing where relevant. Formulation addition ratio in the finished lyophilized product is fixed at 8:1 piperacillin sodium to tazobactam sodium by weight, corresponding to 2 g/0.25 g and 4 g/0.5 g presentations. The synthesis itself requires the 1H-1,2,3-triazole charge to be controlled against the penam sulfone intermediate; typical process development batches use 1.0–1.2 molar equivalents, with exact charge ratios held in the drug master file because unreacted triazole carryover alters the sulfone oxidation profile and increases residual solvent load. Downstream production proceeds through N-alkylation of 2β-chloromethyl-2α-methylpenam-3α-carboxylic acid benzhydryl ester in anhydrous dimethylformamide or dimethylacetamide, followed by sulfur oxidation with a peracid system, ester deprotection, sodium salt formation in aqueous acetone, charcoal treatment, 0.22 µm sterile filtration, and lyophilization in stainless-steel trays at controlled shelf temperatures. Terminal dosage forms are lyophilized powders for injection in Type I glass vials with chlorobutyl stoppers, reconstituted with sterile water for injection or 0.9% sodium chloride to concentrations of 225 mg/mL piperacillin and 28.125 mg/mL tazobactam for intravenous infusion. Process limits include strict moisture control below 2.0% water in the lyophilized cake, avoidance of prolonged heat exposure above 25 °C during secondary drying, and exclusion of primary amines or reducing agents that can open the β-lactam ring or degrade the triazole moiety.
| Finished presentation | Combination ratio (w/w) | Vial composition | Primary compliance standard |
|---|---|---|---|
| Piperacillin/tazobactam for injection | 8:1 | 4 g piperacillin sodium + 0.5 g tazobactam sodium | FDA 21 CFR 210/211; USP <71> |
| Ceftolozane/tazobactam for injection | 2:1 | 1 g ceftolozane + 0.5 g tazobactam sodium | EU GMP Annex 1; USP <790> |
Oral cephalosporin synthesis based on 1H-1,2,3-triazole-derived thiol intermediates is encountered in cefatrizine capsules, tablets, and dry syrup formulations. Compliance for this non-sterile oral dosage track includes ICH Q7 for the API, FDA 21 CFR 210/211 for finished dosage, ICH Q3C residual solvents, ICH Q3D elemental impurities, ICH M7 for potentially genotoxic impurities, and pharmacopoeial monographs for cefatrizine propylene glycol where the product is registered. Formulation addition ratio in the finished product is strength-based rather than excipient-ratio driven: immediate-release capsules and tablets contain cefatrizine equivalent to 250 mg or 500 mg per unit, while dry syrup is reconstituted to 125 mg/5 mL for pediatric administration. During the API synthesis, the 1H-1,2,3-triazole-derived C-3 thiol is typically charged at 1.0–1.2 molar equivalents relative to 7-aminocephalosporanic acid or its protected derivative, because sub-stoichiometric charging leaves unreacted C-3 leaving groups that form lactone by-products and reduce yield. Downstream production involves C-3 displacement with the triazole thiol, followed by N-acylation with protected D-4-hydroxyphenylglycine, deprotection, crystallization, and drying. Oral tablet manufacture uses high-shear wet granulation with a binder solution, fluid-bed drying to LOD below 2.0%, milling through a 0.8 mm screen, lubrication with magnesium stearate 0.5–1.0% by weight, and compression on a rotary press capable of 18–25 kN compression force. Capsule manufacture uses dry blending or slugging, while dry syrup granules are produced by fluid-bed granulation and filled into foil-lined sachets. Terminal product types are immediate-release capsules, film-coated tablets, and dry syrup granules for oral suspension. The main process boundary is residual unreacted 1H-1,2,3-triazole and its N-alkylated isomers: these low-molecular-weight polar impurities are controlled to ICH M7 thresholds and require orthogonal HPLC-UV/MS methods because they co-elute with early cephalosporin degradation products on standard C18 columns.
Anticonvulsant oral finishing based on 1H-1,2,3-triazole-4-carboxamide is applied to rufinamide film-coated tablets and oral suspension. The active ingredient is constructed directly from the triazole core via carboxamide formation at the C-4 position and N-1 benzylation with 2,6-difluorobenzyl chloride under phase-transfer conditions. Compliance for this route includes FDA 21 CFR 210/211, ICH Q7 for API, ICH Q3C, ICH Q3D, ICH M7, USP <711> dissolution for the tablet monograph, and USP <905> uniformity of dosage units. Formulation addition ratio in the finished preparations is fixed by strength: 200 mg and 400 mg film-coated tablets, and 40 mg/mL oral suspension after reconstitution. In the synthesis, the 1H-1,2,3-triazole starting material is charged at 1.0 molar equivalent with respect to the C-4 carboxamide coupling component, while the N-1 alkylating agent is typically used at 1.1–1.3 molar equivalents to force complete conversion of the triazole ring; published data for this specific configuration is limited, so the exact phase-transfer catalyst loading must be established by design-of-experiment. Downstream API production proceeds through carboxylation or carboxamidation at C-4, selective N-1 alkylation, solvent extraction, charcoal treatment, crystallization from an alcohol-water mixture, vacuum drying, and particle size reduction to a D90 below 100 µm for tablet blending. Tablet manufacture uses direct compression or dry granulation with microcrystalline cellulose, croscarmellose sodium, lactose monohydrate, and magnesium stearate; film coating uses a hydroxypropylmethylcellulose/polyethylene glycol system at 2.5–4.0% weight gain. Oral suspension manufacture disperses the API in a buffered aqueous vehicle with xanthan gum, sodium citrate, and methylparaben/propylparaben; the final suspension is filled into amber glass or polyethylene terephthalate bottles. Terminal product types are film-coated tablets and oral suspension. The major processing constraint is the removal of the 2,6-difluorobenzyl alkylating agent and its hydrolysis product, which are controlled under ICH M7 and require LC-MS/MS transition monitoring because the halogenated benzyl impurities are non-chromophoric under UV detection.
Combination sterile powder for intravenous infusion in ceftolozane/tazobactam presentations uses the same tazobactam sodium derived from 1H-1,2,3-triazole but imposes additional aseptic blending and filling constraints. The finished vial contains ceftolozane sulfate equivalent to 1 g ceftolozane and 0.5 g tazobactam sodium, a 2:1 w/w ratio, and is regulated under FDA 21 CFR 210/211, EU GMP Annex 1, ICH Q7/Q11, USP <71> sterility, USP <85> endotoxin, USP <790> particulate matter, and the FDA-approved drug product monograph. In the blending unit operation, tazobactam sodium is pre-sieved through a 0.5 mm stainless-steel screen and blended with ceftolozane sulfate in a low-shear tumble blender for a time established by blend uniformity validation; the target blend uniformity relative standard deviation is below 5.0% for both actives before aseptic filling. Aseptic filling is performed on a high-speed filling line equipped with restrictive access barrier systems or isolators, using Type I glass vials, siliconized chlorobutyl stoppers, and aluminum flip-off seals. The filled powder is reconstituted at the point of use with 10 mL of sterile water for injection or 0.9% sodium chloride, then further diluted for intravenous infusion. Terminal product types are single-dose sterile powder vials for hospital use, not oral dosage forms. The shared tazobactam sodium intermediate imposes the same residual solvent and degradant constraints described for piperacillin/tazobactam, but ceftolozane sulfate introduces additional incompatibility with polyethylene containers observed in some stability studies; published data for the specific polymer contact configuration is limited, and container closure compatibility must be confirmed under ICH Q1A conditions.
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1H-1,2,3-Triazole Pharma Grade API for Tablet / Capsule / Granule / Injection, Oral & Injectable is supplied under two model grades: 1H-TRZ-PG1 for oral solid dosage processing and 1H-TRZ-PG2 for injectable and lyophilized formulations. The compound is identified by CAS 288-36-8, molecular formula C2H3N3, and relative molecular mass 69.07. The 1,2,3-triazole ring system provides a five-membered heterocycle with two adjacent nitrogen atoms and one N-H proton. The bulk material is a pale yellow solid at 2–8 °C and becomes a low-viscosity liquid above its melting point of 23–25 °C; the boiling point at atmospheric pressure is 203–204 °C.
Because the melting point lies below typical tableting tooling temperatures, the product is transported under cold-chain conditions at 2–8 °C and particle size reduction is performed on a cryogenic pin mill using chilled nitrogen at -40 to -20 °C. The resulting micronized powder has a D10 of ≥5 µm, D50 of ≤45 µm, and D90 of ≤100 µm by laser diffraction per ISO 13320:2020. The low melting point also requires that blending and compression equipment be chilled to prevent sticking and agglomeration.
The release profile is shown below. Each lot is accompanied by a certificate of analysis with test results against the listed methods.
| Parameter | Acceptance criterion | Test method |
|---|---|---|
| Appearance | White to pale yellow solid at 2–8 °C | Visual inspection per USP 695 |
| Identification | IR absorption matches reference spectrum | USP 197 |
| Assay, anhydrous and solvent-free basis | 99.0–101.0% | HPLC per USP 621 |
| Related substances | Total impurities ≤1.0%; any single impurity ≤0.5% | HPLC per USP 621 |
| Water content | ≤0.5% | Karl Fischer USP 921 method Ia |
| Loss on drying | ≤0.5% | USP 731 |
| Residue on ignition | ≤0.1% | USP 281 |
| Heavy metals | ≤10 ppm | USP 231 |
| Residual solvents | Methanol ≤3000 ppm; acetone ≤5000 ppm; dichloromethane ≤600 ppm | USP 467 Option 1 |
| Particle size | D50 ≤45 µm, D90 ≤100 µm | ISO 13320:2020 |
| Bacterial endotoxins, 1H-TRZ-PG2 | ≤0.25 EU/mg | USP 85 |
| Sterility, 1H-TRZ-PG2 | No growth | USP 71 |
In direct compression runs on a 16-station rotary tablet press with 8 mm B-tooling, the 1H-TRZ-PG1 powder is premixed with microcrystalline cellulose, croscarmellose sodium, and colloidal silicon dioxide in a 100 L bin blender at 12 rpm for 15 min. Magnesium stearate is added to a final concentration of 0.75 wt% and mixed for an additional 3 min. Compression is maintained at 12–18 kN and turret speed at 25–35 rpm. The resulting tablets meet weight uniformity within ±5% by USP 905 and friability below 0.8% by USP 1216. When punch temperature exceeds 20 °C, sticking begins at the punch and die bore; tooling is cooled with tempered water at 10–15 °C and forced feeder speed is kept below 40 rpm to prevent shear-induced melting.
Wet granulation of the API in a 300 L high-shear mixer with impeller tip speed 8.5 m/s and chopper speed 1200 rpm is used when the target drug loading exceeds 25% of the core tablet mass. Purified water or 5% povidone solution is added at 0.5–1.0 kg/min; granulation end-point is determined by power consumption plateau. Fluid-bed drying follows in a top-spray granulator with inlet air 55–65 °C, product temperature 30–35 °C, and air flow 600–800 m³/h. Final loss on drying is 1.0–1.8%. When final LOD falls below 1.0%, tablet hardness decreases and friability increases above 0.8% in USP 1216 testing.
For parenteral use, model 1H-TRZ-PG2 is released with bacterial endotoxin limit ≤0.25 EU/mg by USP 85 and particulate matter by USP 788. The API is dissolved in water for injection at 5–10 mg/mL after pH adjustment to 5.5–6.5 with dilute hydrochloric acid. The solution is filtered through a 0.22 µm PVDF capsule filter and autoclaved at 121 °C for 15 min where container-closure integrity permits. In compatibility studies, the solution remains within limits for subvisible particles for 24 h at 25 °C protected from light. The pH must not exceed 8.0; above this limit, deprotonation reduces solubility and produces a visible precipitate. Combination with strong oxidizing agents or nitrite-containing formulations is not recommended without a differential scanning calorimetry safety screening at 2 °C/min from 25 °C to 300 °C under nitrogen purge.
Because the 1,2,3-substitution pattern places the N-H proton adjacent to a tertiary nitrogen, the compound differs from the isomeric 1H-1,2,4-triazole in hydrogen-bond donor orientation and solid-state behavior. The 1,2,4-isomer has a melting point of 120–121 °C and can be compressed without chilled tooling, whereas the 1,2,3-isomer requires cold processing and anti-sticking measures. Benzotriazole, which contains a fused benzo ring, differs in UV absorption and photostability in aqueous formulations; reversed-phase HPLC using a C18 column and a 0.1% phosphoric acid–acetonitrile gradient resolves the three azoles with a resolution above 2.0. Published data for this specific configuration is limited; the differentiation is therefore drawn from batch record observations and reference-standard retention times rather than a single peer-reviewed comparative study.
Residual solvents are controlled by headspace gas chromatography per USP 467 Option 1. Class 1 benzene is limited to ≤2 ppm; Class 2 dichloromethane to ≤600 ppm; Class 3 methanol to ≤3000 ppm and acetone to ≤5000 ppm. Potential genotoxic impurities are assessed by liquid chromatography–mass spectrometry with a reporting threshold of ≤75 ppm based on ICH M7 acceptable intake calculations for a 10 kg batch size. Subvisible particles for injectable grade are controlled at ≥10 µm and ≥25 µm limits per USP 788 using light obscuration.
For capsule filling, the micronized powder is mixed with lactose monohydrate in a 200 L double-cone blender at 10 rpm for 20 min; the blend is passed through a 0.8 mm screen before filling into hard gelatin or HPMC capsules on a dosator-type capsule machine at 40,000 capsules/h. Fill weight variation is controlled at ±5% per USP 905. Dissolution is evaluated in 900 mL of 0.1 N hydrochloric acid at 37 ± 0.5 °C with paddle speed 50 rpm using USP 711 Apparatus 2. Capsules stored at 40 °C/75% RH in HDPE bottles with desiccant show water content below 0.8% after 3 months by Karl Fischer titration.
Pre-drying is required when the material has been exposed to relative humidity above 60% for more than 8 h. Drying is performed in a vacuum tray dryer at 25–30 °C and 10–20 kPa for 6–8 h; water content is then re-tested by Karl Fischer titration using USP 921 method Ia. The dried product is stored in double polyethylene bags inside a sealed fiber drum with desiccant at 2–8 °C. Under these conditions, the confirmed retest interval is 24 months for 1H-TRZ-PG1 and 18 months for 1H-TRZ-PG2 because of the more stringent endotoxin limit. Incompatibility is documented with strong oxidizing agents, which promote exothermic decomposition; processing with nitrite-based excipients is not recommended without a differential scanning calorimetry safety screening at a heating rate of 2 °C/min from 25 °C to 300 °C under nitrogen purge.
