Allopurinol (CAS No.: 315-30-0) - Xanthine Oxidase Inhibitor for Hyperuricemia & Gout
As a professional supplier of pharmaceutical-grade active pharmaceutical ingredients (APIs), we provide high-purity Allopurinol that strictly complies with global pharmacopoeia standards (USP, EP, BP, CP). A selective xanthine oxidase inhibitor (XOI), it is clinically approved for treating hyperuricemia (elevated blood uric acid levels) and its complications-including gout (acute flares and chronic tophaceous gout) and uric acid nephrolithiasis (kidney stones). By reducing uric acid production at the source, Allopurinol prevents the formation of uric acid crystals, making it a cornerstone therapy for long-term management of uric acid-related disorders.
Product Basic Information
| Item | Details |
|---|---|
| Product Name | Allopurinol |
| CAS No. | 315-30-0 |
| Synonyms | 1H-Pyrazolo[3,4-d]pyrimidin-4-ol; Zyloprim® (brand name for oral formulations); Aloprim® (brand name for injectable formulations) |
| Molecular Formula | C₅H₄N₄O |
| Molecular Weight | 136.11 |
| Appearance | White to off-white crystalline powder; Odorless |
| Specification | - Pharmaceutical Grade: Purity ≥99.0% (HPLC); Assay 98.0%–102.0% (anhydrous basis); Loss on drying ≤0.5%; Residue on ignition ≤0.1%; Heavy metals (Pb≤1ppm, Hg≤0.1ppm, Cd≤0.1ppm); Residual solvents (methanol ≤300ppm, ethanol ≤500ppm); pH (1% aqueous solution): 5.5–7.5 |
| Melting Point | 350–356°C (with decomposition) |
| Solubility | Slightly soluble in water (≈0.7 mg/mL at 25°C); Soluble in dilute acids (e.g., 0.1M HCl) and dilute alkalis (e.g., 0.1M NaOH); Practically insoluble in ethanol, chloroform, and ether |
| Storage Conditions | Store in a cool (15–25°C), dry, light-protected container; Sealed to prevent moisture absorption and oxidation; Avoid contact with strong oxidizing agents; Shelf life: 36 months for pharmaceutical grade |
Core Functions & Mechanism of Action
Allopurinol (CAS#315-30-0) acts by inhibiting xanthine oxidase-a key enzyme in the purine metabolism pathway that converts hypoxanthine to xanthine and xanthine to uric acid. Its mechanism is targeted and irreversible, producing two critical effects:
1.Reduces Uric Acid Production
- Pathway Blockade: Uric acid is the end product of purine breakdown in humans. The drug binds irreversibly to xanthine oxidase, blocking the conversion of hypoxanthine and xanthine to uric acid.
- Metabolite Synergy: In the body, it is metabolized to oxypurinol (alloxanthine), a long-acting (half-life ≈18–30 hours) xanthine oxidase inhibitor that extends the therapeutic effect, allowing once-daily dosing.
2.Prevents Uric Acid Crystal Deposition
- Lower Serum Uric Acid (sUA): By reducing uric acid production, it lowers sUA levels below the saturation point (6 mg/dL for adults; <5 mg/dL for patients with tophaceous gout), preventing new uric acid crystals from forming in joints, tendons, and kidneys.
- Dissolves Existing Crystals: Sustained low sUA levels over months to years gradually dissolve pre-formed uric acid crystals (tophi) in chronic gout, reducing joint damage and pain.
Core Applications (Pharmaceutical Field)
CAS#315-30-0 is administered orally (tablets, capsules) or intravenously (IV, for severe cases like tumor lysis syndrome). It is a long-term therapy (not for acute gout flares) and requires dose titration to achieve target sUA levels:
1. Chronic Gout & Hyperuricemia
Initial Dosing: 100 mg once daily (to minimize risk of acute flares); may be increased by 100 mg weekly until sUA reaches target (usually 300–600 mg daily, max 800 mg daily for severe cases).
Key Note: Acute gout flares may occur during the first 6–12 months of treatment (due to crystal mobilization). Concomitant low-dose colchicine (0.5 mg daily) or non-steroidal anti-inflammatory drugs (NSAIDs) are recommended to prevent flares.
2. Uric Acid Nephrolithiasis
Dosing: 200–400 mg daily (adjusted based on sUA levels and kidney function). Reduces uric acid excretion, preventing the formation of uric acid stones and dissolving small existing stones.
3. Tumor Lysis Syndrome (TLS)
Prophylaxis: Used in patients with hematologic malignancies (e.g., leukemia, lymphoma) undergoing chemotherapy (which causes massive cell death and purine release). IV/oral dose: 600–800 mg daily for 2–3 days before chemotherapy, continued until risk of TLS resolves.
Treatment: IV dose (Aloprim®) for severe TLS with hyperuricemia (when oral intake is not possible), 200–400 mg/m² body surface area daily.
4. Contraindications
Hypersensitivity to Allopurinol or oxypurinol.
Acute gout flares (Allopurinol does not treat acute inflammation and may worsen flares).
Severe hepatic impairment (Child-Pugh Class C) or end-stage renal disease (ESRD, CrCl <10 mL/min) without dialysis.
Quality & Safety Assurance
As a long-term prescription API, Allopurinol requires rigorous quality control to ensure purity, potency, and safety-especially given its risk of hypersensitivity reactions and drug interactions:
1. Manufacturing & Purity Control
Synthesis: Produced via multi-step chemical synthesis (starting from 4,5-diaminopyrimidine-6-ol), with key steps including cyclization (forming the pyrazolo[3,4-d]pyrimidine ring) and purification via recrystallization. The process ensures:
Minimal impurities (e.g., synthetic intermediates, degradation products) ≤0.1% (single impurity) and ≤0.5% (total impurities);
No residual heavy metals or solvents (critical for long-term use, as accumulation could cause toxicity).
GMP Compliance: Manufactured in Grade D cleanrooms (per ICH Q7 guidelines) with strict environmental monitoring (airborne particles, microbial counts) to prevent contamination.
2. Comprehensive Testing Protocol
| Test Item | Method | Acceptance Criterion |
|---|---|---|
| Purity & Assay | HPLC (C18 column, 254 nm detection) | Purity ≥99.0%; Assay 98.0%–102.0% |
| Related Substances | HPLC (gradient elution) | Single impurity ≤0.1%; Total impurities ≤0.5% |
| Heavy Metals | ICP-MS (Inductively Coupled Plasma-Mass Spectrometry) | Pb≤1ppm, Hg≤0.1ppm, Cd≤0.1ppm |
| Residual Solvents | GC (headspace sampling, FID detector) | Class 2 solvents ≤500ppm; Class 1 solvents not detected |
| Loss on Drying | Gravimetric method (105°C for 2 hours) | ≤0.5% |
| Residue on Ignition | Ashing at 600°C | ≤0.1% |
| pH (1% Aqueous Solution) | pH meter | 5.5–7.5 |
3. Safety Reminders
Adverse Effects:
Common (mild): Nausea, diarrhea, rash, and headache (usually resolve with continued use).
Rare but serious: Allopurinol hypersensitivity syndrome (AHS)-a life-threatening reaction characterized by fever, rash (Stevens-Johnson syndrome), liver dysfunction, and renal failure (more common in patients with renal impairment or concurrent diuretic use).
Renal toxicity: Monitor renal function (serum creatinine, eGFR) regularly, as dose adjustments are required for impaired renal function.
Drug Interactions:
Azathioprine/mercaptopurine: Allopurinol inhibits their metabolism, increasing risk of bone marrow suppression-dose reduction (to 25% of usual) is mandatory.
Warfarin: May increase anticoagulant effect-monitor INR (international normalized ratio) closely.
Diuretics (e.g., hydrochlorothiazide): Increase risk of AHS and hyperuricemia-avoid concurrent use if possible.
Cooperation & Contact
We supply pharmaceutical-grade Allopurinol in forms tailored to oral and injectable formulations:
Pharmaceutical Grade: Fine powder (1kg–100kg per order, double-layered aluminum foil bags with desiccants, packed in sealed fiber drums) for tablet, capsule, or IV lyophilized powder production.
Value-added services include:
Providing DMF (Drug Master File) (Type II) and CEP (Certificate of Suitability) to support regulatory filings (ANDA, NDA, MAA) in global markets (U.S., EU, APAC).
Supplying batch-specific COA (Certificate of Analysis) with full testing results (purity, impurities, pH) for compliance.
Technical support for formulation development (e.g., solubility enhancement for IV formulations, stability testing protocols).
If you are a pharmaceutical manufacturer, generic drug company, or contract development and manufacturing organization (CDMO), please contact us for detailed cooperation:
Contact Information:
Email: sales@huarongpharma.com
Phone/WhatsApp: +86 13751168070
We adhere to the principles of "prescription-grade quality, regulatory compliance, and patient safety" and look forward to partnering with global pharmaceutical industries in metabolic and oncology supportive care!
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