I-Dapoxetine hydrochloride powder (129938-20-1) hplc = 98% | I-AASraw
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I-Dapoxetine HCL powder

Isilinganiselwa: SKU: 129938-20-1. Isigaba:

I-AASraw ikwazi ukuhlanganisa nokukhiqiza ikhono kusuka kugramu ukuya ku-Dapoxetine hydrochloride powder (129938-20-1), ngaphansi komthethonqubo we-CGMP kanye nesistimu yokulawula ikhwalithi.

I-Dapoxetine hydrochloride iyinveli esemfushane eyenziwa i-serotonin i-reuptake inhibitor ekhiqizwa ukwelashwa kwe-ejaculation ngaphambi kwesikhathi emadodeni. I-ejaculation esandulele (PE) iyisifo esivamile sesilisa socansi, kulinganiselwa ukuthi siyathinta kuze kufike ku-30% wamadoda. I-Dapoxetine hydrochloride iyi-standard reference reference ehlukaniswa njenge-serotonin e-reuptake inhibitor ekhethiwe. Inikeza ukuthuthukiswa kwemingcele eminingana ehlobene ne-ejaculation engakabiphi ekuvivinyweni kwemitholampilo. Lo mkhiqizo uhloselwe ucwaningo nezinhlelo zokusebenza ze-forensic.

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Product Incazelo

 

I-Dapoxetine hydrochloride i-anesthesia powder ividiyo

 

 


 

I-Dapoxetine ekhululekile i-hydrochloride i-anesthesia powder eziyisisekelo Abalingiswa

 

Igama: I-Dapoxetine hydrochloride
CAS: 129938-20-1
Ifomula Yamamolekhula: C9H7ClN2O5
Isisindo Yamamolekhula: 258.62
I-Melt Point: I-175-179 ° C
Isitoreji Sokugcina: -20 ° C I-Freezer
Umbala: I-powder elimhlophe elimhlophe

 


I-Dapoxetine iyinhlanganisela engokwemvelo yeklasi ye-inhibitors ekhethiwe ye-serotonin reuptake kodwa ngaphandle komphumela wokulwa nokucindezela. Lesi sidakamizwa sithuthukiswe ngokuqondile ukuze siphathe i-ejaculation ngaphambi kwesikhathi kubantu abesilisa abadala phakathi kweminyaka engu-18 no-64 abahlangabezana nalezi zinqubo ezilandelayo:

I-1. Ukujula okuqhubekayo noma okuphindaphindiwe kwe-penis ngaphambi, ngesikhathi, noma ngemva nje kokufakwa emgodini, futhi ngaphambi nje kokuntuleka kokwaneliseka ngokocansi;

I-2. Ukucindezeleka okubalulekile komuntu siqu noma izithiyo ezingezona zomuntu siqu ngenxa ye-ejaculation ngaphambi kwesikhathi (PE);

I-3. Ikhono lokulawulwa kwe-ejaculation elibi.

Izakhi ze-Chemical zeDapoxetine

I-Dapoxetine hydrochloride ithebhulethi yithebhulethi enekhamera elibomvu, elimhlophe noma elimhlophe ngemuva kokususwa kwengubo.

Isithako esikhulu: Dapoxetine hydrochloride.

IUPAC Name: (1S)-N,N-dimethyl-3-naphthalen-1-yloxy-1-phenylpropan-1-amine

 

Isakhiwo se-Dapoxetine HCL powder Chemical

I-1. Isakhiwo se-2D:

I-2. I-3D Conformer:

Ifomula ye-molecular: C21H23NO

Isisindo somzimba: 305.421 g / mol

CAS: 119356-77-3

 

Incazelo elula ye-Dapoxetine

Njengamanje, ayikho imithethonqubo ethize yokwelapha i-ejaculation yesilisa engakafiki ngaphambi kwamaphilisi e-dapoxetine hydrochloride. Akukho mthethonqubo othize ukuthi umuthi usetshenziswa isikhathi esingakanani ukwelashwa. Kuxhomeke ebukhulu bezimpawu ze-ejaculation ngaphambi kwesikhathi. Inkinga yokwelashwa ihlukile. Isikhathi semithi asikwazi ukukhiqizwa. Kodwa-ke, lesi sidakamizwa singathuthukisa izimpawu ze-ejaculation ngaphambi kwesikhathi, ngakho-ke iziguli zingathatha imithi ngokwezimpawu zazo.

I-Dapoxetine ngokuyinhloko ihloswe ukwelashwa kwe-18 kuya ku-64 ubudala ubudala wesilisa engaphambi kwesikhathi ejaculation (PE) iziguli ezihlangabezana nazo zonke izimo ezilandelayo, kuhlanganise:

I-1. I-penis iyingcosana ngaphambi, ngesikhathi, noma ngemva nje kokufakwa emgodini, nangaphambi kokwaneliseka ngokocansi. Isisusa sokuhlukunyezwa ngokobulili kuqhutshwa ngokuqhubekayo noma okuphindaphindiwe;

I-2. Ukucindezeleka okubalulekile komuntu siqu noma izithiyo ezingezona zomuntu siqu ngenxa ye-ejaculation ngaphambi kwesikhathi (PE);

I-3. Ukulawulwa okungahambi kahle kokuzikhandla.

 

I-Dapoxetine isivele ivunyiwe njengemithi yokwelapha eYurophu nase-United States njengokuba nomthelela omkhulu ekwelapheni kwe-ejaculation ngaphambi kwesikhathi. Uma uthatha i-dapoxetine, i-serotonin, into ekhona ebuchosheni, ifihliwe. Le serotonin yinto evutha injabulo yobuchopho noma iveza umphumela wokuphumula. Ukukhathazeka nokuthokozeka kuxazululwa, umphumela we-adrenaline uphinde wehlise, ukuze isikhathi sokujula sikwazi ukubambezeleka.

I-Dapoxetine hydrochloride ingakwazi ukuvimbela ngokuphumelelayo ukuphindaphinda kabusha kwe-5-HT futhi ukwandise ukuhlushwa kwe-5-HT kusihluthulelo se-synaptic ngokuvimbela i-5-HT transporter. Ucwaningo luye lwabonisa ukuthi i-dapoxetine ivimbela i-ejaculation reflex ngokuyinhloko, futhi i-nucleus yesigcawu se-giant isisindo esibalulekile sezobuchopho. Lapho ukuhlushwa kwe-dapoxetine kuphakeme, uhlelo lwe-monoamine lwamaprotheni yokuthutha lungavinjelwa, futhi ukuphindwa kabusha kwe-dopamine nakho kuvinjelwe. I-Dapoxetine yenza ukwanda kwe-pudendal motor neuron reflexes futhi kuthuthukise umsebenzi wezocansi.

Kuthatha isikhathi esingakanani ukuthi amaphilisi e-dapoxetine hydrochloride asebenze ayenziwa ngokujwayelekile. Ukwelashwa kuxhomeke ekubambeni kwezimpawu zokuthi u-ejaculation ngaphambi kwesikhathi. Inkinga yokwelashwa ihlukile, kanti isikhathi sokuthatha imithi kuhlukile.

 

Indlela yokusebenza ye-Dapoxetine

Indlela yokwenza i-dapoxetine ekwelapheni kwe-ejaculation engakafiki ingase ihlobene nokuvimbela ukubuyiswa kabusha kwe-serotonin nge-neurons, ngaleyo ndlela kuthinte umehluko ongase ube we-neurotransmitters osebenza kuma-receptors ngaphambi nangemva kwe-cell synapses.

I-Dapoxetine isebenza kahle nge-ejaculation ngaphambi kwesikhathi ngoba inomthelela wokwandisa ukuhlushwa kwe-serotonin okuvimbela ukuxolisa ebuchosheni.

I-Serotonin ivame ukubuyiselwa kabusha kusukela ku-synapse, kodwa ngokuthatha i-dapoxetine inqanda ukubuyiselwa kabusha nokuphazamisa i-serotonin.

I-Serotonin igxilisa i-dopamine ekhulisa ukuthokoza, ukukhathazeka, kanye ne-adrenaline ephuma uma ukhathazekile, ngakho ungandisa isikhathi sokuthi u-ejaculate.I-Dapoxetine iphumelele ejaculation ngaphambi kwesikhathi ngoba inomthelela wokwandisa ukuhlushwa kwe-serotonin okuvimbela ukuxolisa ubuchopho.

I-Serotonin ivame ukubuyiselwa kabusha kusukela ku-synapse, kodwa ngokuthatha i-dapoxetine inqanda ukubuyiselwa kabusha nokuphazamisa i-serotonin.
I-Serotonin icindezela i-dopamine ekhulisa injabulo, ukukhathazeka, kanye ne-adrenaline ephuma uma usaba, ngakho ungakwandisa isikhathi sokuba u-ejaculate.

Ukujula kwabantu ngokuyinhloko kuxoxisana nesistimu yomzwelo ezwelayo. I-reflex pathway ejaculation itholakala esikhungweni se-splex reflex, esixhunywe yi-brainstem, eqala ukuthinteka yizinzwa eziningi ze-brain nuclei (i-nucleus yangaphambi komzimba kanye ne-nucleus ye-hypoventricular paraventricular).

 

I-Dapoxetine HCL Pharmacokinetics

Ngemuva kokulawulwa komlomo, i-dapoxetine iyancipha ngokushesha futhi ifinyelele ukugxilongwa okuphezulu kwe-plasma (i-Cmax) ngemuva kwamahora angu-1-2. I-bioavailability ngokuphelele i-42% (ibanga le-15-176%). Ngemuva kokuphathwa komlomo okulodwa kwe-30 mg no-60 mg we-dapoxetine esimweni sokuzila, ukuphakama kwe-plasma (297 ng / ml ne-498 Ng / ml, ngokulandelana) kwafinyelelwa emva kwe-1.01 namahora we-1.27, ngokulandelana. Ukungena kokudla okunamafutha aphezulu kunganciphisa ngokulinganisela i-Cmax (10%) ye-dapoxetine futhi kwandiswe ngokulingana i-AUC (12%), kuyilapho iphinde ilinde ukuhlushwa okukhulu kwe-dapoxetine; Kodwa-ke, amafutha aphezulu adla ukudla akuthinti izinga lokumunca. Ayikho yalezi zinguquko ezinokubaluleka komtholampilo. I-Bentley ingakhonzwa noma ngaphandle kokudla.

Ngemuva kokuphathwa komzimba womuntu nge-injection engumgogodla, ukulinganiswa kokuqala, okuphakathi, kanye nokuphela kokuphila-i-dapoxetine yi-0.10, 2.19, namahora we-19.3, ngokulandelana.

I-metabolites ye-dapoxetine exreted ngokuyinhloko isulwe umchamo esimweni conjugate. Ayikho into esebenzayo eyatholakala emcinini. I-Dapoxetine isuliwe ngokushesha, futhi ubufakazi bungaphansi kwezindleko zegazi amahora angu-24 ngemuva kokuphathwa (ngaphansi kwe-5% yezinga lokuhlushwa). Umthamo wansuku zonke we-dapoxetine usemncane kakhulu. I-half-life terminal yokuphathwa komlomo cishe amahora angu-19. Ukuphila kwengxenye ye-desmethyl dapoxetine kufana neka-dapoxetine.

 

Ukusetshenziswa kwe-Dapoxetine

Ukwelashwa kweziguli zesilisa ezine-ejaculation ngaphambi kwesikhathi (PE)

Amaphilisi e-Dapoxetine hydrochloride angaphumelela ekuthuthukiseni ikhono lokulawula i-ejaculation; ngokuphawulekayo kuthuthukisiwe ukwaneliseka kokuphila ngokocansi ukwandisa kahle i-ejaculation latency.

Ngenkathi usebenzisa imithi, iziguli zingasebenzisa izinyathelo ezincane zokuthuthukisa izimpawu zokuthi u-ejaculation ungakafiki, ulungise isimo sengqondo, uqinise ukuxhumana phakathi komyeni nomfazi, ukudla okunengqondo, ukuqinisa ukuzivocavoca umzimba, ukugijima nsuku zonke, nokuhlanganyela emsebenzini wokuzivocavoca njalo ngesonto. Kungcono futhi ukukhetha ukudlala ibhola kanye nokudlala ibhola basketball ukuze uthuthuke ngokomzimba futhi unciphise ukucindezeleka kwengqondo.

 

Isilinganiso se-Dapoxetine

Ukulinganisa kwamathebulethi e-dapoxetine hydrochloride ngomlomo, futhi amaphilisi kufanele agonywe kahle; iziguli zeluleka ukuba zithathe indebe eyodwa egcwele yamanzi imithi; iziguli kufanele zizame ukugwema ukulimala okubangelwa izimpawu ze-prodromal ezifana ne-syncope noma isiyezi.

Inani lamaphilisi e-dapoxetine hydrochloride anconyiwe kuwo wonke iziguli kubantu abadala (i-18 kuya ku-64 ubudala ubudala) ngu-30 mg futhi kudingeka athathwe mayelana ne-1 kumahora angu-3 ngaphambi kokuphila ngokocansi. Uma umphumela ungawanelisi ngemuva kokuthatha i-30mg nemiphumela emibi isengaphakathi kwebanga elimukelekile, umthamo unganyuswa ube ngu-60mg wezinga eliphakanyisiwe eliphakanyisiwe.

I-dose ephakanyisiwe ephakanyisiwe isetshenziselwa njalo amahora we-24.
Abantu asebekhulile (abaneminyaka engu-65 nangaphezulu) Lo mkhiqizo awuhlolwanga eminyakeni engu-65 nokuphepha nokusebenza kweziguli phezu kwesixuku esisetshenzisiwe, isizathu esiyinhloko sedatha kulo mkhiqizo okusetshenziselwa kulesi sibalo sinomkhawulo kakhulu kuziguli ezinomnene ukukhubazeka komzimba noma iziguli ezinomonakalo wezinso akudingeki ukuba ulungise umthamo uma uthatha lo mkhiqizo, kodwa kufanele uziphathe ngokucophelela. Lo mkhiqizo awukhuthazwa iziguli ezinokulimala kwezinso ezinzima.

 

Izinkomba ze-Dapoxetine:

Lo mkhiqizo uhloselwe ukwelashwa kweziguli zesilisa ezine-ejaculation engakafiki (PE) phakathi kweminyaka yobudala ye-18 ne-64 ehlangabezana nalezi zimo ezilandelayo: i-penis iyaqhubeka ize ifakwe emkhathini, ngesikhathi noma ngemva kokufakiwe, nangaphambi ukuzithokozisa ngokocansi kufinyelelwe, kuphela ngenxa yokucasula okuncane. Ukuphindaphinda okuphindaphindiwe; kanye nokucindezeleka okuphawulekayo komuntu siqu noma izithintelo ezingekho ngaphansi komuntu ngenxa ye-ejaculation ngaphambi kwesikhathi (PE); nokulawulwa okuncane kokuzikhandla.

(1) Amadoda amadala (18 kuya eminyakeni engu-64 ubudala)

Ncoma umthamo wokuqala we-30 mg kuzo zonke iziguli futhi kudingeka uthathe mayelana ne-1 kumahora we-3 ngaphambi kocansi. Uma umphumela ungawanelisi ngemuva kokuthatha i-30mg nemiphumela emibi isengaphakathi kwebanga elimukelekile, umthamo unganyuswa ube ngu-60mg wezinga eliphakanyisiwe eliphakanyisiwe. I-dose ephakanyisiwe ephakanyisiwe isetshenziselwa njalo amahora we-24. Lo mkhiqizo ungathathwa ngaphambi noma emva kokudla.

Uma udokotela ekhetha lo mkhiqizo ukwelapha i-ejaculation ngaphambi kwesikhathi, kufanele ahlole ubungozi nenzuzo ebikiwe yesiguli emasontweni okuqala ayi-4 ngemuva kokusetshenziswa komuthi, noma ahlole ibhalansi yenzuzo yesiguli ngemuva kokusebenzisa umthamo wokwelashwa wesikhathi esingu-6 bese ethatha isinqumo ukuqhubeka nokusebenzisa umkhiqizo.

(2) Abantu asebekhulile (iminyaka engu-65 nangaphezulu)

Ucwaningo alukaqapheli ukuphepha nokusebenza kwalo mkhiqizo kuziguli ezineminyaka engu-65 nangaphezulu. Isizathu esiyinhloko salokhu ukuthi idatha ekusetshenzisweni kwalo mkhiqizo kulesi sibalo sinciphile ngokweqile.

(3) Izingane kanye nabantu abasha

Lo mkhiqizo awuhloselwe ukusetshenziswa ngabantu abangaphansi kweminyaka engu-18.

Ithebhulethi eyodwa ngasikhathi ingathathwa ngokungapheli. Isidakamizwa sidinga ukuphuza esiswini esingenalutho. Kungcono ukuphuza itiye ngaphambi kokuyisebenzisa kahle ngaphambi kokuba lo muthi wenze uhlelo olunzulu lokuhlola, kuya ngokugula kwabo kudokotela noma kukasokhemisi abatshele futhi ukuphepha kuhlelwe umuthi ukuze kugwenywe ukusetshenziswa kwezidakamizwa ngendlela engafanele, kepha kunganyuki ngokungafanele imvamisa yokusetshenziswa kwezidakamizwa ngesikhathi Kumele ulandele amalungiselelo kadokotela namahloni.

 

Ukudlula ngokweqile kwe-Dapoxetine

Ngokuvamile, izimpawu zokudlula ngokweqile kwe-serotonin e-reuptake inhibitor ezikhethayo zihlanganisa imiphumela emibi ephakathi kwe-serotonin efana nokuqeda amandla, ukungasebenzi kwamathumbu njengokunambitheka kwesisu nokuhlanza, injabulo, ukuthuthumela, isiyezi kanye ne-tachycardia. Endabeni yokudlula ngokweqile, izinyathelo zokusekela ezijwayelekile kufanele zithathwe njengoba kudingeka. Okwamanje akukho-antidote ethize kulo mkhiqizo.

 

I-Dapoxetine HCL Yokuqapha

1. Izinyathelo zokuqapha ezivamile. I-Dapoxetine isetshenziselwa kuphela iziguli zesilisa ezine-ejaculation ngaphambi kwesikhathi. Ukuphepha kwe-Dapoxetine emadodeni angenayo i-ejaculation ngaphambi kwesikhathi akucaci. Ngasikhathi sinye, akukho datha ngomphumela we-Dapoxetine ekubambezelekeni kwe-ejaculation kulesi sibalo. Kunconywa ukuthi iziguli akufanele zithathe iBeverly kanye "nezidakamizwa zokuzijabulisa" ngasikhathi sinye ngoba umphumela awaziwa futhi kungenzeka izehlakalo ezimbi kakhulu.

I-2. Iziguli zeluleka ukuba zingathathi izidakamizwa ezithinta inhliziyo ngenkathi zithatha.

I-3. Gwema ukuthatha utshwala uma uthatha i-Dapoxetine.

I-4. Sebenzisa i-Dapoxetine ingabangela i-syncope noma isizungu

I-5. Futhi thatha i-cytochrome ejwayelekile ye-P450 3A4 inhibitors njengo-erythromycin, i-clarithromycin, i-fluconazole, i-verapamil ne-diltiazem.

I-6. Thatha i-cytochrome ejulile ye-cytochrome PNNUMX 450D2 inhibitor noma i-cytochrome eyaziwa yi-P6 450D2 Iziguli ezine-metabolism ebuthakathaka kufanele ziqaphele lapho ukwandisa umthamo ku-6 mg, njengoba lokhu kungaholela ekuvezeni okukhudlwana, okuzogcina kuholele ekuphenduleni okungathandeki komthelela omkhulu.

I-7. Okuwusizo akufanele kusetshenziselwe imania / iziguli ezinomlando we-hypomanic noma i-bipolar disorder, ngesikhathi esifanayo, noma yisiphi isiguli esinampawu zesifo esishiwo ngenhla kufanele siphethwe nge-Dapoxetine.

I-8. Ngenxa yokuthi i-serotonin e-reyptake inhibitor ekhethiwe ingase ihlehlise umkhawulo wokufiphala. Inani, noma yisiphi isiguli esinokuqothulwa kufanele sigwetshwe, futhi iziguli ezinesifo sokuqubuka kufanele zigweme ukusebenzisa i-Dapoxetine.

I-9. I-Dapoxetine akufanele isetshenziswe kubantu abangaphansi kweminyaka engu-18.

I-10. Akunconywa Iziguli ezinomonakalo omkhulu wezinso, iziguli ezinokukhubazeka okunomsoco noma okulinganayo kufanele zisetshenziswe ngokuqapha. Njengenye i-serotonin e-reuptake inhibitors ekhethiwe, ukusebenzisa i-Dapoxetine kuhlotshaniswa nokunye ukuphendula kwamehlo. Isibonelo, ukuphuza umfundi nokuhlungu kweso. Iziguli ezinomsindo ophezulu we-intraocular noma ingozi yokugunda i-glaucoma kufanele isetshenziswe ngokuqapha.

 

I-Dapoxetine HCL powder ivinjelwe

I-1. I-Dapoxetine ayenqatshelwe iziguli eziyaziwa ukuthi ziyingozi kwi-dapoxetine hydrochloride noma yiziphi izidakamizwa.

I-2. I-Dapoxetine inqatshelwe iziguli ezinezimo ezibonakalayo ezingenasifo senhliziyo enhliziyweni [isib. Ukwehluleka kwenhliziyo (i-NYHA II-IV), akukho ukuqhutshwa okungavamile okwenziwa nge-pacemaker therapy (ibanga le-2 noma i-3 atrioventricular block noma isifo se-sinus syndrome), i-myocardial ischemia nesifo se-valvular]

I-3. I-Dapoxetine ayinayo i-monoamine oxidase inhibitors (MAOIs) Akufanele isetshenziswe ndawonye phakathi nezinsuku ze-14 ngemuva kokwelashwa kwe-monoamine oxidase inhibitors kumisiwe. Ngokufanayo, i-monoamine oxidase inhibitors akumele isetshenziswe ngaphakathi kwezinsuku ezingu-7 zokunqamuka kwe-Bili (bheka ukusebenzisana kwezidakamizwa).

I-4. I-Dapoxetine ayikwazi ukusetshenziswa nge-thioridazine noma ngemuva kokwelashwa kwe-thiodazine. Isetshenziswa ngaphakathi kwezinsuku. Ngokufanayo, i-thioridazine akufanele ithathwe phakathi kwezinsuku ze-7 ngemuva kokuqeda i-Dapoxetine (bheka isigaba sokusebenzisana kwezidakamizwa).

I-5. I-Dapoxetine ivinjelwe ukuthatha i-ketoconazole, itraconazole, i-ritonavir, i-saquin Iziguli ezine-cytochrome ezinamandla i-P450 3A4 inhibitors njenge-nave, i-telithromycin, i-nefazodone, i-naffenavir, ne-atazanavir.

I-6. I-Dapoxetine inqatshelwe iziguli ezinokulimala okulinganayo nesibindi esinobungozi.

 

Isiphetho se-Dapoxetine HCL

Uma usebenzisa amathebulethi e-dapoxetine hydrochloride, kufanele alawulwe ngaphansi kokuqondiswa udokotela, okungathuthukisa izimpawu zesifo futhi ngesikhathi esifanayo kusetshenziswe kangcono imithi.


 

Indlela yokuthenga I-Dapoxetine hydrochloride powder (129938-20-1) kusuka ku-AASraw

 

1.Ukuxhumana nathi nge-imeyili yethu uhlelo lokubuza, noma i-skype eku-inthanethiummeleli wenkonzo yamakhasimende (CSR).
I-2.Ukusihlinzekela ngobuningi bakho kanye nekheli lakho elibuziwe.
I-3.I-CSR yethu izokunikeza ikhothethini, isikhathi sokukhokha, inombolo yokulandelela, izindlela zokulethwa kanye nosuku lokufika olulinganisiwe (i-ETA).
I-4.Inkokhelo eyenziwe futhi izimpahla zizothunyelwa kumahora we-12 (Ukuhleleka ngaphakathi kwe-10kg).
Ama-5.Goods athola futhi anikeze imibono.