Allopurinol (CAS No.: 315-30-0) - Xanthine Oxidase Inhibitor rau Hyperuricemia & Gout
Raws li tus kws tshaj lij ntawm kev lag luam tshuaj - qib tshuaj cov khoom xyaw (APIs), peb muab siab - purity Allopurinol uas ua raws li cov qauv tshuaj tshuaj thoob ntiaj teb (USP, EP, BP, CP). Ib tug xaivxanthine oxidase inhibitor (XOI), nws tau pom zoo rau kev kho mobhyperuricemia(cov ntshav uric acid nce siab) thiab nws cov teeb meem -xws ligout(mob flares thiab chronic tophaceous gout) thiaburic acid nephrolithiasis(lub raum pob zeb). Los ntawm kev txo qis uric acid ntau lawm ntawm qhov chaw, Allopurinol tiv thaiv kev tsim cov uric acid crystals, ua rau nws yog ib qho kev kho mob rau lub sijhawm ntev -kev tswj hwm ntawm uric acid- cuam tshuam.
Product Basic Information
| Yam khoom | Paub meej |
|---|---|
| Khoom npe | Allopurinol |
| CAS Nr. | 315-30-0 |
| Synonyms | 1H-Pyrazolo[3,4-d]pyrimidin-4-ol; Zyloprim® (lub npe tshuaj rau qhov ncauj formulations); Aloprim® (lub npe hom rau txhaj tshuaj formulations) |
| Molecular Formula | C₅H₄N₄O |
| Molecular Luj | 136.11 |
| Qhov tshwm sim | Dawb rau tawm -dawb crystalline hmoov; Tsis hnov tsw |
| Specification | - Pharmaceutical Qib: Purity Ntau dua lossis sib npaug li 99.0% (HPLC); Kev ntsuam xyuas 98.0% -102.0% (anhydrous hauv paus); Poob ntawm ziab Tsawg dua lossis sib npaug li 0.5%; Residue ntawm ignition Tsawg dua los yog sib npaug rau 0.1%; Cov hlau hnyav (Pb Tsawg dua lossis sib npaug rau 1ppm, Hg Tsawg dua lossis sib npaug rau 0.1ppm, Cd Tsawg dua lossis sib npaug li 0.1ppm); Cov kuab tshuaj seem (methanol Tsawg dua lossis sib npaug rau 300ppm, ethanol Tsawg dua lossis sib npaug li 500ppm); pH (1% aqueous tov): 5.5-7.5 |
| Melting Point | 350-356℃(nrog decomposition) |
| Solubility | me ntsis soluble hauv dej (≈0.7 mg / mL ntawm 25 degree); Soluble hauv dilute acids (piv txwv li, 0.1M HCl) thiab dilute alkali (piv txwv li, 0.1M NaOH); Xyaum insoluble hauv ethanol, chloroform, thiab ether |
| Kev cia khoom | Khaws rau hauv qhov txias (15-25 degree), qhuav, lub teeb -cov thawv tiv thaiv; Sealed los tiv thaiv kev nqus dej thiab oxidation; Tsis txhob sib cuag nrog cov oxidizing muaj zog; Lub neej txee: 36 lub hlis rau qib tshuaj |
Core Functions & Mechanism of Action
Allopurinol CAS Nr 315-30-0ua los ntawm inhibiting xanthine oxidase-ib qho tseem ceeb enzyme nyob rau hauv purine metabolism txoj kev uas converts hypoxanthine rau xanthine thiab xanthine rau uric acid. Nws mechanism yog tsom thiab irreversible, ua ob qho tseem ceeb los:
1.Txo Uric Acid ntau lawm
- Txoj Kev Blockade:Uric acid yog qhov khoom kawg ntawm kev puas tsuaj purine hauv tib neeg. Cov tshuaj khi irreversibly rau xanthine oxidase, thaiv kev hloov ntawm hypoxanthine thiab xanthine rau uric acid.
- Metabolite Synergy:Hauv lub cev, nws tau metabolized rau oxypurinol (alloxanthine), ntev - ua haujlwm (ib nrab- lub neej ≈18-30 teev) xanthine oxidase inhibitor uas txuas ntxiv cov txiaj ntsig kho, tso cai ib zaug - noj txhua hnub.
2. Tiv thaiv Uric Acid Crystal Deposition
- Lower Serum Uric Acid (sUA):Los ntawm kev txo qis uric acid ntau lawm, nws txo qis sUA qib qis dua qhov saturation point (6 mg / dL rau cov laus;<5 mg/dL for patients with tophaceous gout), preventing new uric acid crystals from forming in joints, tendons, and kidneys.
- Dissolve muaj Crystals:Sustained qis sUA qib nyob rau ntau lub hlis mus rau xyoo maj mam yaj ua ntej- tsim uric acid crystals (tophi) nyob rau hauv mob gout, txo cov pob qij txha thiab mob.
Core Applications (Pharmaceutical Field)
CAS#315-30-0 yog muab tshuaj rau qhov ncauj (cov ntsiav tshuaj, tshuaj ntsiav) lossis tso rau hauv cov hlab ntsha (IV, rau cov mob hnyav xws li qog lysis syndrome). Nws yog ib qho kev kho mob mus sij hawm ntev (tsis yog rau mob gout flares) thiab xav tau koob tshuaj titration kom ua tiav cov hom phiaj sUA qib:
1. Mob Gout & Hyperuricemia
Thawj koob tshuaj: 100 mg ib zaug ib hnub (kom txo tau qhov kev pheej hmoo ntawm cov mob hnyav heev); tej zaum yuav nce ntxiv los ntawm 100 mg txhua lub lim tiam kom txog thaum sUA ncav cuag lub hom phiaj (feem ntau yog 300–600 mg txhua hnub, max 800 mg txhua hnub rau cov mob hnyav).
Ntsiab Lus: Mob gout flares yuav tshwm sim thaum thawj 6-12 lub hlis ntawm kev kho mob (vim yog siv lead ua pob zeb). Concomitant qis- koob tshuaj colchicine (0.5 mg ib hnub twg) lossis tsis yog -steroidal anti-cov tshuaj tiv thaiv kab mob (NSAIDs) raug pom zoo los tiv thaiv flares.
2. Uric Acid Nephrolithiasis
Dosing: 200–400 mg txhua hnub (hloov raws li qib sUA thiab lub raum ua haujlwm). Txo uric acid excretion, tiv thaiv kev tsim ntawm uric acid pob zeb thiab dissolving me me pob zeb uas twb muaj lawm.
3. Tumor Lysis Syndrome (TLS)
Kev tiv thaiv kab mob: Siv nyob rau hauv cov neeg mob uas muaj hematologic malignancies (piv txwv li, leukemia, lymphoma) tab tom siv tshuaj kho mob (uas ua rau cov cell tuag loj heev thiab tso tawm purine). IV/qhov ncauj koob tshuaj: 600–800 mg ib hnub twg rau 2-3 hnub ua ntej kws khomob, txuas ntxiv mus txog thaum muaj kev pheej hmoo ntawm TLS daws.
Kev kho mob: IV koob tshuaj (Aloprim®) rau TLS hnyav nrog hyperuricemia (thaum noj qhov ncauj tsis tau), 200-400 mg / m² lub cev saum npoo av txhua hnub.
4. Contraindications
Hypersensitivity rau Allopurinol lossis oxypurinol.
Mob gout flares (Allopurinol tsis kho mob mob thiab yuav ua rau cov flares loj dua).
Hepatic impairment (Me nyuam-Pugh Class C) los yog kawg- kab mob raum (ESRD, CrCl<10 mL/min) without dialysis.
Quality & Safety Assurance
Raws li lub sijhawm ntev -cov tshuaj API, Allopurinol yuav tsum muaj kev tswj xyuas kom zoo los xyuas kom meej purity, potency, thiab kev nyab xeeb-tshwj xeeb tshaj yog muab nws txoj kev pheej hmoo ntawm hypersensitivity rhiab heev thiab kev cuam tshuam tshuaj:
1. Kev tsim khoom & Purity Control
Synthesis: Ua los ntawm ntau yam -cov tshuaj synthesis (pib los ntawm 4,5-diaminopyrimidine-6-ol), nrog rau cov kauj ruam tseem ceeb suav nrog cyclization (ua lub pyrazolo[3,4-d]pyrimidine nplhaib) thiab purification ntawm recrystallization. Cov txheej txheem kom ntseeg tau tias:
Tsawg impurities (piv txwv li, hluavtaws intermediates, khoom degradation) Tsawg dua los yog sib npaug rau 0.1% (ib qho impurity) thiab Tsawg dua lossis sib npaug li 0.5% (tag nrho impurities);
Tsis muaj cov hlau hnyav lossis cov kuab tshuaj seem (tseem ceeb rau kev siv sijhawm ntev -, raws li kev sib sau ua rau muaj kuab lom).
Ua raws li GMP: Tsim nyob rau hauv Qib D cleanrooms (raws li ICH Q7 cov lus qhia) nrog nruj ib puag ncig saib xyuas (cua paug, cov microbial suav) kom tsis txhob muaj kab mob.
2. Cov Txheej Txheem Kev Ntsuas Zoo
| Cov khoom kuaj | Txoj kev | Kev lees txais |
|---|---|---|
| Purity & Assay | HPLC (C18 kem, 254 nm nrhiav pom) | Purity Ntau dua lossis sib npaug li 99.0%; Kev ntsuas 98.0% - 102.0% |
| Yam khoom muaj feem | HPLC (gradient elution) | Ib qho impurity Tsawg dua lossis sib npaug li 0.1%; Tag nrho impurities Tsawg dua lossis sib npaug li 0.5% |
| Hnyav Hlau | ICP-MS (Inductively Coupled Plasma-Mass Spectrometry) | Pb Tsawg dua lossis sib npaug rau 1ppm, Hg Tsawg dua lossis sib npaug rau 0.1ppm, Cd Tsawg dua lossis sib npaug rau 0.1ppm |
| Residual Solvents | GC (headspace sampling, FID ntes) | Chav kawm 2 cov kuab tshuaj tsawg dua lossis sib npaug ntawm 500ppm; Cov kuab tshuaj Class 1 tsis kuaj |
| Poob rau ziab | Gravimetric method (105℃rau 2 teev) | Tsawg dua los yog sib npaug li 0.5% |
| Residue ntawm Ignition | Tshav kub ntawm 600 degree | Tsawg dua lossis sib npaug li 0.1% |
| pH (1% Aqueous tov) | pH ntsuas | 5.5–7.5 |
3. Kev ceeb toom kev nyab xeeb
Cov teebmeem tsis zoo:
Feem ntau (mob): xeev siab, raws plab, tawm pob, thiab mob taub hau (feem ntau daws tau nrog kev siv txuas ntxiv).
Tsis tshua muaj tab sis hnyav:Allopurinol hypersensitivity syndrome(AHS)-ib txoj sia-kev hem thawj tshwm sim tshwm sim los ntawm kub taub hau, pob khaus (Stevens-Johnson syndrome), lub siab ua haujlwm tsis zoo, thiab lub raum tsis ua haujlwm (ntau dua hauv cov neeg mob lub raum tsis zoo lossis kev siv tshuaj diuretic ib txhij).
Lub raum toxicity: Saib xyuas lub raum ua haujlwm (serum creatinine, eGFR) tsis tu ncua, raws li kev hloov kho koob tshuaj yuav tsum tau ua rau lub raum tsis ua haujlwm.
Cov tshuaj sib cuam tshuam:
Azathioprine / mercaptopurine: Allopurinol inhibits lawv cov metabolism, ua rau muaj kev pheej hmoo ntawm cov pob txha pob txha tawg - txo koob tshuaj (rau 25% ntawm ib txwm muaj) yog qhov yuav tsum tau ua.
Warfarin: Tej zaum yuav ua rau kom cov nyhuv anticoagulant- saib xyuas INR (txoj kev sib raug zoo thoob ntiaj teb) ze ze.
Diuretics (piv txwv li, hydrochlorothiazide): Ua rau muaj kev pheej hmoo ntawm AHS thiab hyperuricemia - zam kev siv ib txhij yog tias ua tau.
Kev koom tes & kev sib cuag
Peb muab tshuaj-qib Allopurinol rau hauv cov ntaub ntawv uas haum rau qhov ncauj thiab txhaj tshuaj formulations:
Pharmaceutical Qib: Cov hmoov zoo (1kg–100kg ib qho kev txiav txim, ob npaug -txheej txhuas ntawv ci hnab nrog desiccants, ntim rau hauv lub nruas fiber ntau kaw) rau cov ntsiav tshuaj, tshuaj ntsiav, lossis IV lyophilized hmoov ntau lawm.
Tus nqi - cov kev pabcuam ntxiv suav nrog:
MuabDMF (Drug Master File)(Tib II) thiabCEP (Certificate of Suitability)los txhawb cov ntaub ntawv tswj hwm (ANDA, NDA, MAA) hauv kev lag luam thoob ntiaj teb (US, EU, APAC).
Muab batch- tshwj xeebCOA (Certificate of Analysis)nrog tag nrho cov txiaj ntsig kev xeem (purity, impurities, pH) rau kev ua raws.
Kev txhawb nqa rau kev tsim kho kev tsim kho (piv txwv li, kev txhim kho kev sib xyaw ua ke rau IV formulations, kev soj ntsuam kev ruaj ntseg).
Yog tias koj yog cov chaw tsim tshuaj, tuam txhab tshuaj generic, lossis cog lus tsim kho thiab tsim lub koom haum (CDMO), thov hu rau peb kom paub meej kev koom tes:
Cov ntaub ntawv tiv tauj:
Email: sales@huarongpharma.com
Xov tooj/WhatsApp: +86 13751168070
Peb ua raws li cov hauv paus ntsiab lus ntawm "kev sau ntawv- qib zoo, kev ua raws cai, thiab kev nyab xeeb ntawm tus neeg mob" thiab tos ntsoov yuav koom tes nrog kev lag luam tshuaj thoob ntiaj teb hauv kev saib xyuas kev noj qab haus huv thiab oncology!
Cim npe nrov: Tuam Tshoj Allopurinol CAS # 315-30-0 manufacturers, lwm tus neeg
