Tadalafil (CAS No.: 171596-29-5) - Long-Acting PDE5 Inhibitor for Erectile Dysfunction & Pulmonary Arterial Hypertension
Raws li tus kws tshaj lij kev lag luam ntawm cov kws kho mob - qib cov khoom xyaw tshuaj (APIs), peb muab siab -Tadalafil purity uas ua raws li cov qauv tshuaj tshuaj thoob ntiaj teb (USP, EP, BP, CP). Ib qho kev xaiv thiab ntev - ua yeeb yam phosphodiesterase type 5 (PDE5) inhibitor, nws raug pom zoo los khoerectile kawg (ED), benign prostatic hyperplasia (BPH), thiabpulmonary arterial hypertension (PAH). Nws qhov tshwj xeeb pharmacokinetic profile-nrog ib nrab- lub neej ntawm ~ 17.5 teev- ua kom yoog raws (ntawm-xav tau lossis txhua hnub qis- koob tshuaj) thiab txuas ntxiv cov teebmeem kev kho mob, ua rau nws yog qhov kev xaiv zoo tshaj plaws hauv cov txiv neej kev noj qab haus huv thiab kev kho mob plawv.
Product Basic Information
| Yam khoom | Paub meej |
|---|---|
| Khoom npe | Tadalafil |
| CAS Nr. | 171596-29-5 |
| Synonyms | (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione; Cialis® (hom npe rau ED / BPH formulations); Adcirca® (hom npe rau PAH formulations) |
| Molecular Formula | C₂₂H₁₉N₃O₄ |
| Molecular Luj | 389.40 |
| 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 ntawm 300ppm, acetonitrile Tsawg dua lossis sib npaug ntawm 410ppm, ethyl acetate Tsawg dua lossis sib npaug li 500ppm); Optical purity (ee) Ntau dua lossis sib npaug li 99.5% |
| Melting Point | 302-305℃(nrog decomposition) |
| Solubility | Xyaum insoluble hauv dej (≈0.02 mg / mL ntawm 25 degree); me ntsis soluble hauv ethanol (≈0.8 mg / mL) thiab methanol; Soluble hauv dimethyl sulfoxide (DMSO) thiab dilute acids (piv txwv li, 0.1M HCl) |
| Kev cia khoom | Khaws rau hauv qhov txias (2-8 degree), qhuav, lub teeb -cov thawv tiv thaiv; Muab ntim rau hauv nitrogen los tiv thaiv oxidation thiab noo noo nqus; Tsis txhob sib cuag nrog cov acids muaj zog / bases thiab oxidizing agents; Lub neej txee: 36 lub hlis rau qib tshuaj |
Core Functions & Mechanism of Action
Tadalafil exerts nws cov teebmeem kho los ntawmxaiv inhibiting PDE5-ib qho enzyme uas rhuav tshem cyclic guanosine monophosphate (cGMP), ib qho tseem ceeb taw qhia molecule hauv cov leeg nqaij:
1. Rau Erectile Dysfunction (ED)
Physiological Trigger: Kev sib deev stimulation ua rau tso tawm nitric oxide (NO) nyob rau hauv lub corpus cavernosum ntawm noov.
cGMP Cov khoom: TSIS MUAJ activates guanylate cyclase, uas nce cGMP ntau lawm. Tadalafil inhibits PDE5, tiv thaiv cGMP degradation thiab cia nws qib nce.
Smooth Muscle Relaxation: Ua kom siab cGMP relaxes cov leeg du ntawm cov hlab ntsha ntawm penile, ua rau cov ntshav ntws mus rau hauv lub cev corpus cavernosum- ua rau erection.
Qhov tseem ceeb Advantage: Tsis zoo li luv luv - ua yeeb yam PDE5 inhibitors (xws li, sildenafil), CAS#171596-29-5 ntev ib nrab-lub neej tso cai rau erections tshwm simtus kheejtsis pub dhau 24-36 teev tom qab noj tshuaj (tsis xav tau lub sij hawm raug txheeb ze rau kev sib deev).
2. Rau Benign Prostatic Hyperplasia (BPH)
Pathology Link: BPH cuam tshuam nrog cov nqaij mos prostate loj compressing cov zis, ua rau cov tsos mob tso zis (piv txwv li, tso zis ntau zaus, tsis muaj zog). PDE5 kuj tau qhia nyob rau hauv prostate thiab zais zis caj dab du nqaij.
So kom txaus: yog inhibits PDE5 nyob rau hauv lub prostate thiab zais zis, so cov leeg du, txo cov urethral obstruction, thiab txhim kho zis ntws. Nws feem ntau siv rau cov neeg mob uas muaj ob qho tib si ED thiab BPH (dual indication).
Core Applications (Pharmaceutical Field)
Tadalafil CAS#171596-29-5 yog siv los ntawm qhov ncauj (cov ntsiav tshuaj, cov ntsiav tshuaj tsis sib haum hauv qhov ncauj) thiab yog cov tshuaj nruj me ntsis-tsuas yog vim muaj peev xwm ua rau cov hlab plawv. Dosing nws txawv los ntawm kev qhia:
1. Erectile Dysfunction (ED)
Ntawm -Dom Dosing: 10 mg noj tsawg kawg 30 feeb ua ntej kev sib deev; Tej zaum yuav raug hloov mus rau 5 mg (rau cov neeg mob me ED lossis cov neeg laus) lossis 20 mg (rau qhov hnyav ED), nrog ntau zaus ntawm ib hnub.
Txhua Hnub Tsawg-Kev Siv Tshuaj: 2.5 mg lossis 5 mg noj ib zaug ib hnub (tsis hais txog kev sib deev), zoo tagnrho rau cov neeg mob nrhiav kev ua haujlwm ntawm kev sib deev lossis cov neeg uas muaj BPH comorbidity.
2. Benign Prostatic Hyperplasia (BPH)
Monotherapy: 5 mg ib zaug ib hnub ( txhim kho cov tsos mob tso zis hauv 1-2 lub lis piam).
Kev Kho Mob Ua Ke: 5 mg ib hnub ib zaug nrog alpha-blockers (piv txwv li, tamsulosin) rau BPH hnyav (tsis txhob ntxiv hypotension vim yog qhov cuam tshuam tsawg rau ntshav siab ntawm koob tshuaj tsawg).
3. Pulmonary Arterial Hypertension (PAH)
Branded Formulation (Adcirca®): 40 mg ib zaug ib hnub (ntau dua ED / BPH, raws li PAH xav tau ntau dua PDE5 inhibition hauv pulmonary vasculature).
Qhov taw qhia: Pom zoo rau PAH (WHO Pawg 1) txhawm rau txhim kho kev tawm dag zog lub cev thiab ncua kev kho mob tsis zoo.
Quality & Safety Assurance
Raws li cov tshuaj API tseem ceeb, CAS#171596-29-5 yuav tsum muaj kev tswj xyuas kom zoo los xyuas kom meej purity, potency, thiab kev nyab xeeb-tshwj xeeb tshaj yog muab nws lub peev xwm rau kev sib cuam tshuam tshuaj thiab kev mob plawv:
1. Kev tsim khoom & Purity Control
Synthesis: Ua los ntawm ntau yam -qib tshuaj synthesis (pib los ntawm 1,3-benzodioxole derivatives), nrog rau cov kauj ruam tseem ceeb xws li cyclization, chiral daws teeb meem (kom paub tseeb tias kho qhov muag purity), thiab crystallization. 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);
High optical purity (ee Ntau dua lossis sib npaug li 99.5%), raws li (R, R) -enantiomer yog daim ntawv nquag (lwm cov enantiomers tsis muaj PDE5 inhibitory kev ua haujlwm).
Ua raws li GMP: Ua nyob rau hauv Qib B/C cleanrooms (raws li ICH Q7 cov lus qhia) nrog kev saib xyuas ib puag ncig nruj (cov khoom hauv huab cua, suav cov microbial) los tiv thaiv kev sib kis.
2. Cov Txheej Txheem Kev Ntsuas Zoo
| Cov khoom kuaj | Txoj kev | Kev lees txais |
|---|---|---|
| Purity & Assay | HPLC (C18 kem, 230nm kuaj pom) | Purity Ntau dua lossis sib npaug li 99.0%; Kev ntsuas 98.0% - 102.0% |
| Optical Purity | Chiral HPLC (cellulose{0}}raws li kem) | Enantiomeric tshaj (ee) Ntau dua lossis sib npaug li 99.5% |
| 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% |
3. Kev ceeb toom kev nyab xeeb
Contraindications:
Hypersensitivity rau Tadalafil lossis PDE5 inhibitors.
Kev siv nitrates (piv txwv li, nitroglycerin, isosorbide dinitrate) -kev pheej hmoo ntawm txoj sia - hem hypotension.
Cov kab mob plawv hnyav (piv txwv li, tsis ntev los no myocardial infarction / stroke, tsis ruaj khov angina, tsis tswj ntshav siab).
Hepatic impairment (Me nyuam-Pugh Class C) los yog kawg- kab mob raum (ESRD, CrCl<30 mL/min).
Cov teebmeem tsis zoo:
Feem ntau (mob, ib ntus): Mob taub hau, dyspepsia (mob plawv), mob nraub qaum, mob nqaij, thiab dej ntws.
Rare but serious: Priapism (erection lasting >4 teev-xav tau kev kho mob xwm txheej ceev kom tsis txhob muaj cov ntaub so ntswg puas), tsis pom kev tam sim ntawd (tsis yog-arteritic anterior ischemic optic neuropathy, NAION), lossis tsis hnov lus tam sim ntawd.
Kev koom tes & kev sib cuag
Peb muab cov kws kho mob -qib Tadalafil hauv cov ntaub ntawv uas haum rau kev tsim tshuaj:
Pharmaceutical Qib: Cov hmoov zoo (1kg–100kg rau ib qho kev txiav txim, ob npaug- txheej aluminium foil hnab nrog desiccants, ntim rau hauv cov nruas fiber ntau kaw) rau cov ntsiav tshuaj, tshuaj ntsiav, los yog cov ntsiav tshuaj disintegrating qhov ncauj (ODT) 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, optical purity, impurities) rau kev ua raws.
Kev txhawb nqa kev tsim kho kev tsim kho (xws li, kev txhim kho kev sib xyaw ua ke rau cov ntaub ntawv ntawm qhov ncauj, 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 kws tshuaj thoob ntiaj teb hauv kev noj qab haus huv ntawm cov txiv neej thiab cov hlab plawv!
Cim npe nrov: Tuam Tshoj tadalafil cas#171596-29-5 manufacturers, lwm tus neeg
