Ingcaciso yeMveliso
Iimpawu ezisisiseko zeSemaglutide
| Igama lemveliso: | Semaglutide |
| Inombolo ye-CAS: | 910463-68-2 |
| I-molecular Formula: | C187H291N45O59 |
| Isisindo somzimba: | 4113.58g / mol |
| Melt Point: | 34-39 ° C |
| umbala: | Mhlophe |
| Isitoreji sokugcina: | Gcina kwi-8 ° C-20 ° C, ukhusele kumswakama kunye nokukhanya |
Yintoni iSemaglutide?
I-Semaglutide yi-glucagon-like peptide-1 receptor agonist esetyenziswa kubantu abanesifo sikashukela sohlobo lwe-2 njengesongezo sokutya kunye nokuzivocavoca ukuphucula ulawulo lwe-glycemic..I-Semaglutide yi-GLP-1 yokufanisa ene-94% yokulandelelana kwe-homology kwi-GLP-1 yomntu. agonist.Ngaphezu koko, i-semaglutide inokusebenza kwindlela yokugaya ngokulibazisa ukukhupha isisu ukuze kubangele ukugcwala; ebuchotsheni ngokucinezela umdla wokutya; kunye nakwinkqubo yokujikeleza kwegazi ngokulungisa i-intima eyonakalisiweyo kunye nokuphucula umsebenzi we-endothelial.
Isebenza njani iSemaglutide?
Semaglutide powder i-agonist ye-glucagon-like peptide-1 receptor.Ikhuthaza ukuveliswa kwe-insulin, ihomoni enciphisa amanqanaba eswekile yegazi, ngokuxelisa umphumo we-incretin glucagon-like peptide-1 (GLP-1) . ukukhuthaza ukwanda kweeseli ze-pancreatic beta, ezijongene nokuveliswa kwe-insulin kunye nokukhululwa.Ngaphezu koko, i-AASraw semaglutide inamandla okunciphisa ukuveliswa kwe-glucagon, i-hormone evuselela i-glycogenolysis (ukukhululwa kwe-carbs egcinwe kwisibindi) kunye ne-gluconeogenesis ( ukudalwa kweglucose entsha).Inciphisa ukutya ngokucinezela indlala kwaye icothise ukucolwa kwesisu esiswini, nto leyo enceda ekunciphiseni umzimba.Icinezela umdla wokutya, iminqweno yokutya, kunye nokugcinwa kwamafutha.
Uphando lweSemaglutide
①Intshayelelo
I-Semaglutide yonyango eyenziwa ekuqaleni ukunyanga isifo sikashukela.Nangona kunjalo, iye yafumana ukuthandwa njengeyeza lokulahlekelwa kwesisindo emva kokuba ifunyenwe ukunceda ngokufanelekileyo abantu ukuba balahlekelwe isisindo, kubandakanywa nomntu wesibini osisityebi emhlabeni, u-Elon Musk.Kutshanje, isifundo--Kanye-ngeVeki ye-Semaglutide kwi-Adolescents nge-Obesity—-ipapashwe kwi Ijenali yeNew England yezoNyango (NEJM) uye wafumanisa ukuba i-semaglutide inokunceda ulutsha olutyebileyo lunciphise ubunzima kunye nokukhuthaza impilo yentliziyo.
②Iziphumo eziphambili
- Ulutsha olutyebileyo oluthatha i-semaglutide ngeveki lubone ukunyuka kwe-16.1% kwi-index mass body (BMI) kwinqanaba lamazwe ngamazwe le-3a yolingo lwekliniki, xa kuthelekiswa nokunyuka kwe-0.6% kwiqela le-placebo.
- I-Semaglutide yi-glucagon-like peptide 1 (GLP-1) i-receptor agonist enokunciphisa ukutya, ukutya, kunye nokutya kwekhalori, okwenza kube lula ukulahleka kwesisindo.
- Ulingo olukhulu lwekliniki lubonise ukuba i-semaglutide inefuthe elimangalisayo njengeyeza lokulahlekelwa kwesisindo, kunye neqela eliphathwayo elilahlekelwa ngumyinge we-15.3 kg.
- NgoJuni ka-2021, i-USFood kunye noLawulo lweDrugs (i-FDA) yavuma ukuthengiswa kwe-semaglutide (i-Semaglutide), ichiza lokunciphisa umzimba elinegama lokurhweba lika-Wegovy.
- Uphononongo lwakutsha nje lufumene ukuba i-semaglutide igqithise i-placebo ngokumalunga nokuncipha kobunzima kunye nokuphuculwa kwezinto ezinobungozi be-cardiometabolic kulutsha olutyebileyo.
- Emva kokuthatha i-semaglutide, izinto ezinobungozi be-cardiovascular ezifana ne-waist circumference, i-blood glucose index HbA1c, i-cholesterol epheleleyo, i-low-density lipoprotein cholesterol, i-triglycerides, kunye ne-triglycerides iphuculwe.
- Iqela le-semaglutide ligqithise iqela le-placebo kumgangatho onxulumene nobunzima bokulinganisa ubomi, ngenxa yobuninzi bezinto eziphezulu zokuthuthuzela ngokomzimba.
③Isiphelo
I-Semaglutide ibonakaliswe njengeyeza elisebenzayo lokulahlekelwa kwesisindo, kwaye uphando olutshanje luye lwabonisa ukuba lunokuba luncedo kulutsha olutyebileyo.Nangona iyeza lidibene nemiphumo emibi yesisu, ifunyenwe ukuphucula imingcipheko ye-cardiovascular risk factor and quality of imilinganiselo yobomi.
Imvelaphi yomthombo:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9997064/
Izibonelelo zokusebenzisa Semaglutide
I-Semaglutide yonyango olusebenzayo olunika uluhlu lweenzuzo kubantu abaneemeko ezahlukeneyo zonyango.Ezinye zeemeko eziqhelekileyo ezinokuthi zizuze ekusebenziseni i-AASraw Semaglutide kuquka uhlobo lwe-2 yesifo sikashukela i-Mellitus, iingozi ze-caidiovascular, ukukhuluphala kunye ne-Alzheimer.
①Ukwehliswa kweGlucose yeGazi
I-Semaglutide i-GLP-1 i-receptor agonist esebenzayo ekunciphiseni amanqanaba e-glucose yegazi kubantu abanesifo sikashukela sohlobo lwe-2 ngeendlela ezininzi. I-Semaglutide iphinda icinezele i-glucagon secretion, eyanciphisa ukuveliswa kwe-glucose ngesibindi.Ukwengeza, iyancipha ukukhupha isisu, esinciphisa izinga apho i-glucose ingena egazini emva kokutya.
Kwizilingo zeklinikhi, i-semaglutide ibonakaliswe ukunciphisa kakhulu amanqanaba e-HbA1c, eyisalathisi sokulawula i-glucose yegazi ixesha elide.Kwilingo lwe-SUSTAIN-1, i-semaglutide yanciphisa amanqanaba e-HbA1c nge-1.5% xa kuthelekiswa ne-placebo, kunye ne-SUSTAIN-10 uvavanyo, lwanciphisa amanqanaba e-HbA1c nge-1.8% xa kuthelekiswa ne-placebo.I-Semaglutide nayo ibonakaliswe ukuba iyasebenza ekunciphiseni i-plasma glucose ngokukhawuleza kunye ne-postprandial glucose excursions.
②Ukunciphisa umngcipheko weziganeko ze-Cardiovascular
I-Semaglutide ibonakaliswe ukunciphisa umngcipheko weziganeko ezimbi kakhulu ze-cardiovascular (MACE) ezifana nokufa kwe-cardiovascular death, i-nonfatal myocardial infarction, kunye ne-stroke engapheliyo kubantu abadala abane-2 yesifo sikashukela kunye nesifo se-cardiovascular disease. Le nzuzo yabonwa kwi-SUSTAIN-6 kunye ne-PIONEER -Izilingo ze-6, ezibonise ukunciphisa okukhulu kwe-MACE kunye nonyango lwe-semaglutide xa kuthelekiswa ne-placebo.Ngaphezu koko, i-Semaglutide ibonakaliswe ukuphucula izinto ezininzi ezinobungozi benhliziyo ezifana noxinzelelo lwegazi, iphrofayili ye-lipid, kunye namanqaku okuvuvukala kubantu abanesifo sikashukela sohlobo lwe-2. uvavanyo lwe-SUSTAIN-6, i-semaglutide yadibaniswa nokunciphisa okukhulu kwixinzelelo lwegazi le-systolic kunye nokuphuculwa kweprofayili ye-lipid, kubandakanywa nokunciphisa i-cholesterol epheleleyo, i-cholesterol ye-LDL kunye ne-triglycerides.
③Ukunciphisa Ubunzima
I-Semaglutide i-agent enamandla yokulahlekelwa kwesisindo, nakubantu abangenayo isifo sikashukela.I-Semaglutide isebenza ngokunciphisa ukutya kunye nokutya kwekhalori, okukhokelela ekunciphiseni ubunzima bomzimba.Oku kufezekiswa ngemiphumo yayo kwinkqubo ye-nervous central kunye ne-gastrointestinal tract.I-Semaglutide isebenza i-hypothalamus, elawula ukulamba kunye nokuhlutha, kunye nokunciphisa umnqweno wokutya ngokunyusa iimvakalelo zokuzala.Ukongezelela, i-semaglutide iyancipha ukukhupha isisu, oko kwandisa ukuvakalelwa kokuhlutha emva kokutya kunye nokunciphisa umnqweno wokutya.
Izilingo zeklinikhi zibonise inzuzo yokulahlekelwa kwesisindo se-semaglutide.Kwinkqubo ye-STEP, eyavavanya ukusetyenziswa kwe-semaglutide yokulawula ubunzima kubantu abangenayo isifo sikashukela, i-semaglutide yayidityaniswa nokulahlekelwa kwesisindo esibalulekileyo xa kuthelekiswa ne-placebo. umyinge we-15% yobunzima bomzimba wabo kwiiveki ezingama-68, ngelixa abo bafumana i-placebo balahlekelwe yi-2.4% kuphela.
Kubantu abanesifo sikashukela sohlobo lwe-2, i-semaglutide inokukhokelela kwiinzuzo ezongezelelweyo zokulahlekelwa kwesisindo.Kwilingo lwe-SUSTAIN 7, oluvavanya ukusebenza kunye nokukhuseleka kwe-semaglutide kubantu abanesifo sikashukela sohlobo lwe-2, i-semaglutide yadibaniswa nokuncipha okukhulu kobunzima bomzimba xa kuthelekiswa ne-placebo. .Abathathi-nxaxheba abafumana i-semaglutide balahlekelwa ngumyinge we-4.6 kg, ngelixa abo bafumana indawo ye-placebo balahlekelwa yi-1.2 kg kuphela.
④Ukunyanga i-Alzheimer's Symptom
Izifundo ezininzi ze-preclinical zibonise ukuba i-semaglutide ineempawu ze-neuroprotective ezichasene ne-amyloid-β plaques kwi-cell line ye-neuroblastoma (SH-SY5Y), ebonisa ukuba i-semaglutide inokunciphisa iimpawu zesifo se-Alzheimer. Ngokutsho kwesaziso sikaNovo Nordisk, isibonakaliso seepilisi ze-semaglutide ze-Alzheimer's disease (AD) kwinqanaba leklinikhi.Izilingo ezimbini zehlabathi zeSigaba se-III, i-EVOKE kunye ne-EVOKE plus, ziyaqhubeka, kwaye malunga namavolontiya angama-3,700 kulindeleke ukuba aqeshwe.Kulu cwaningo. , xa kuthelekiswa ne-placebo, uvavanya ukuphakama kwamacwecwe e-semaglutide kumsebenzi wokuqonda kwizifundo ezinokukhubazeka okuncinci kwengqondo (MCI) okanye ukuphazamiseka kwengqondo okubangelwa yi-AD.
Izilumkiso:Kuyinto ebalulekileyo ekuthengeni i-semaglutide kwimithombo ehloniphekileyo, ngaphandle koko, awukwazi ukufumana i-semaglutide efanelekileyo kakhulu.Njengomenzi we-semaglutide oyingcali kunye nomthengisi, i-AASraw inenjongo yokubonelela nge-semaglutide ecocekileyo emhlabeni jikelele. yeyakho.
Iimpembelelo eziPhambili zeSemaglutide?
I-Semaglutide, njengawo nawaphi na amayeza, inokubangela iziphumo ezibi.
①Iziphumo ebezingalindelekanga eziqhelekileyo ziquka:
- I sizathu
- Ukuvutha
- Uhudo
- Intlungu zesisu
- Ukuphelelwa kwesidlo
- Ukutyunjwa
- intloko ebuhlungu
- Ukukhathala
- Utywala
②Iziphumo ebezingalindelekanga ezingaxhaphakanga kakhulu kodwa ezibi kakhulu zinokubandakanya:
- Pancreatitis
- I-Hypoglycemia (iswekile yegazi ephantsi)
- Ukwenzakala okuqatha kwezintso
- Iingxaki ze-Diabetic retinopathy
- Isifo seGallbladder
- Ukuphendulwa kwemizwa
- Amathumba edlala lengqula
Amanqaku: Ubude bemiphumo emibi ye-semaglutide inokuhluka ngokuxhomekeke kumntu kunye nobukhulu bemiphumo emibi.Kwiimeko ezininzi, imiphumo emibi ye-semaglutide yesikhashana kwaye iya kuphucula njengoko umzimba wakho ulungelelanisa amayeza.Iimpembelelo eziqhelekileyo eziqhelekileyo ezifana ne isicaphucaphu, isifo sohudo, ukuhlanza, ukuqunjelwa, kunye nentloko ebuhlungu ngokuqhelekileyo ixazulula kwiintsuku ezimbalwa ukuya kwiveki.Ukuba ufumana nayiphi na imiphumo engavamile okanye enzima xa uthatha i-semaglutide, yiya kugqirha ngokukhawuleza. njenge-AASraw, ibalulekile.
Umthamo kunye noLawulo lwe-Semaglutide yokuReference
Umthamo kunye nolawulo lwe-semaglutide lunokwahluka ngokuxhomekeke kwisalathisi sokusetyenziswa.Nazi izikhokelo eziqhelekileyo:
①Isalathiso: Uhlobo lwesi-2 seswekile iMellitus
· Isitofu esingaphantsi kwesikhumba
Iveki 1-4: 0.25 mg / ngeveki
Iveki ye-5 nangaphezulu: 0.5 mg / ngeveki
√ Ukuba kuyimfuneko, emva kweeveki ezi-4 ubuncinane kwi-dose ye-0.5-mg, yongeza kwi-1 mg ngaphantsi kwe-subcutaneous kanye ngeveki.
√ Ukuba kuyimfuneko, emva kweeveki ze-4 ubuncinane kwi-dose ye-1-mg, yongeza kwi-2 mg ngaphantsi kwe-subcutaneously kanye ngeveki; ungadluli kwi-2 mg / ngeveki.
· Icwecwe lomlomo
Usuku 1-30: 3 mg / ngosuku
Usuku lwe-31 nangaphezulu: 7 mg / ngosuku
√ Ukuba kuyimfuneko, emva ubuncinane beentsuku ze-30 kwi-dose ye-7-mg, yongeza kwi-14 mg ngomlomo kanye yonke imihla.
√ Qaphela: Sukuthatha iipilisi ezimbini ze-7-mg ukufumana idosi ye-14-mg
②Isalathiso:Ulawulo lobunzima obungapheliyo
· Isitofu esingaphantsi kwesikhumba
Iveki 1-4: 0.25 mg / ngeveki
Iveki 5-8: 0.5 mg / ngeveki
Iveki 9-12: 1 mg / ngeveki
Iveki 13-16: 1.7 mg / ngeveki
Iveki ye-17 ukuya phambili: 2.4 mg / ngeveki (idosi yesondlo)
√ Qalisa ngedosi ephantsi kwaye ngokuthe ngcembe unyukele kwidosi yolondolozo ukunciphisa ukusabela okubi emathunjini.
√ Ukuba awukwazi ukunyamezela ithamo ngexesha lokunyuka, cinga ngokulibazisa ukunyuka kwethamo kwiiveki ezi-4.
√ Ukuba awukwazi ukunyamezela umthamo wokulondoloza we-2.4 mg kanye ngeveki, unokuhla okwethutyana ukuya kwi-1.7 mg kanye ngeveki ubuninzi beeveki ezi-4; emva kweeveki ezi-4, ukunyusa umva kwisondlo se-2.4 mg kanye ngeveki; yeka ukuba ayinyamezelwa emva komzamo wesibini.
√ Qaphela: I-dosage kunye nolawulo lwe-semaglutide lunokwahluka ngokuxhomekeke kwisalathisi sokusetyenziswa.Landela imiyalelo enikezwe ngugqirha wakho okanye njengoko kuboniswe kwilebula yeyeza.Ngaphezu koko, zama konke okusemandleni akho ukuthenga i-semaglutide ecocekileyo ukufezekisa ukusebenza kakuhle.
Ungayithenga phi iSemaglutide?
I-Semaglutide, iyeza elifunwa kakhulu kunyango lwe-2 yesifo sikashukela, liye laziwa kakhulu phakathi kwezigulane ezifuna izisombululo ezisebenzayo zokulawula imeko yabo.Ngenxa yoko, iimarike ze-intanethi ziye zavela njengeqonga elilungele abantu ukuba bathenge i-semaglutide kwi-intanethi. iiplatifti zedijithali zinika abathengi ithuba lokuthelekisa amaxabiso, ukufunda ukuphononongwa, kunye nokufikelela kuluhlu olubanzi lokukhetha ukuhambelana neemfuno zabo.Nangona kunjalo, kubalulekile kubathengi ukuba balumke xa kuthengwa i-semaglutide kwi-intanethi, njengoko iimveliso zomgunyathi okanye ezikumgangatho ophantsi zinokubanakho. ukuphazamisa impilo yabo.Ngokuqhuba uphando olunzulu kunye nokukhetha umthengisi ohloniphekileyo kunye noqinisekisiweyo, abantu ngabanye banokuthenga ngokuzithemba i-semaglutide kwi-intanethi kwaye balawule ngokufanelekileyo isifo sikashukela ngokukhululeka.
AASraw ejolise ekuveliseni i-abd yokubonelela ngamachiza aphakathi kunye nezithako ezisebenzayo zamachiza (APIs), ngumnikezeli othembekileyo we-semaglutide ephezulu kunye nezinye iimveliso ezinxulumene nazo. Ukuzibophezela kwabo ekulawuleni umgangatho ongqongqo kunye nokuthotyelwa kwemigangatho yoshishino kuqinisekisa ukuba abathengi bafumana kuphela iimveliso ezilungileyo kakhulu zabo. impilo kunye nokuphila kakuhle.Ngokuthenga kwi-AASraw, abantu abafuna i-semaglutide banokunandipha amava okuthenga afanelekileyo, akhuselekileyo, athembekileyo, ngelixa bexhamla kulwazi lwabo olubanzi kunye nobuchule kwintsimi.
Ingxelo yoVavanyo lwe-Semaglutide-HNMR
Yintoni i-HNMR kwaye ikuxelela ntoni i-spectrum ye-HNMR?H I-Nuclear Magnetic Resonance (NMR) ispectroscopy bubuchule bohlalutyo lwekhemistri esetyenziswa kulawulo lomgangatho kunye nophando ukumisela umxholo kunye nokusulungeka kwesampulu kunye nobume bayo bemolekyuli.Umzekelo, i-NMR inokuhlalutya ngokobungakanani imixube equlethe iikhompawundi ezaziwayo. Kwiikhompawundi ezingaziwayo, i-NMR inokusetyenziselwa ukutshatisa iilayibrari ezibonwayo okanye ukucingela ubume obusisiseko ngokuthe ngqo. Xa ulwakhiwo olusisiseko lwaziwa, i-NMR inokusetyenziselwa ukumisela ukuhambelana kwemolekyuli. kwisisombululo kunye nokufunda iipropathi ezibonakalayo kwinqanaba leemolekyuli ezifana notshintshiselwano oluhambelanayo, utshintsho lwesigaba, ukunyibilika, kunye nokusasazwa.
Semaglutide-COA
I-Semaglutide (910463-68-2)-COA
Indlela yokuthenga i-Semaglutide kwi-AASraw?
❶Ukuqhagamshelana nathi ngenkqubo yethu yokubuza nge-imeyile, okanye usishiyele inombolo yakho ka-whatsapp, ummeli wethu wenkonzo yabathengi (CSR) uya kuqhagamshelana nawe kwiiyure ezili-12.
❷Ukusinika ubungakanani obubuziweyo kunye nedilesi.
❸I-CSR yethu iya kukubonelela ngekoteyishini, ixesha lokuhlawula, inombolo yokulandelela, iindlela zokuthunyelwa kunye nomhla wokufika oqikelelweyo (ETA).
❹Intlawulo yenziwe kwaye iimpahla ziya kuthunyelwa kwiiyure ezili-12.
❺Impahla efunyenweyo kwaye unike izimvo.
Umbhali weli nqaku:
UGqr Monique UHong uthweswe isidanga kwiKholeji yase-UK Imperial yaseLondon kwiFakhalthi yezoNyango
Umbhali wephepha leJenali yeNzululwazi:
1. Aihua Li
Department of Pharmacy, Zhujiang Hospital, Southern Medical University, Guangzhou 510282, Guangdong, China
2. Tae Suk Lee
School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi 16419, Republic of Korea
3. Saullo Queiroz Silveira MD
Department of Anesthesiology, Vila Nova Star Hospital / Rede D’Or – CMA Anesthesia group, São Paulo, SP, Brazil
4. Fabiane Ferreira Martins
Laboratory of Morphometry, Metabolism, and Cardiovascular Diseases, Biomedical Center, Institute of Biology, The University of the State of Rio de Janeiro, Rio de Janeiro, Brazil
Lo gqirha/ingcali yenzululwazi ayinakuvuma okanye ithethelele ukuthengwa, ukuthengiswa, okanye ukusetyenziswa kwale mveliso nangasiphi na isizathu. I-Aasraw ayinayo indibaniselwano okanye ubudlelwane, ichazwa okanye ngenye indlela, kunye nalo gqirha. Injongo yokucaphula lo gqirha kukuvuma, ukuvuma kunye nokuncoma uphando olupheleleyo kunye nomsebenzi wophuhliso owenziwe ngoososayensi abasebenza kule nto.
Imbekiselo:
[1] UGhusn W,De la Rosa A,Sacoto D,Cifuentes L,Campos A,Feris F,Hurtado MD,Acosta A.Iziphumo zokuLahla kobunzima obuNxulunyaniswe ne-Semaglutide yoNyango lweZigulana ezinobunzima obukhulu okanye ukutyeba.JAMA Netw Vula.2022 Sep 1;5(9):e2231982.
[2] Wilding JPH,Batterham RL,Davies M,Van Gaal LF,Kandler K,Konakli K,Lingvay I,McGowan BM,Oral TK,Rosenstock J,Wadden TA,Wharton S,Yokote K,Kushner RF; INYATHELO 1 IQela lokufunda.Ukubuyisela ubunzima kunye nemiphumo ye-cardiometabolic emva kokuhoxiswa kwe-semaglutide: Ulwandiso lwesilingo se-STEP 1.Diabetes Obes Metab.2022 Aug;24(8):1553-1564.
[3] Garvey WT,Batterham RL,Bhatta M,Buscemi S,Christensen LN,Frias JP,Jódar E,Kandler K,Rigas G,Wadden TA,Wharton S; ISINYATHELO 5 Iqela lokufunda. Imiphumo yeminyaka emibini ye-semaglutide kubantu abadala abanobunzima okanye ukukhuluphala: isilingo se-STEP 5.Nat Med.2022 Oct; 28 (10): 2083-2091.
[4] I-Knudsen LB, uLau J. Ukufunyanwa kunye noPhuhliso lweLiraglutide kunye neSemaglutide.Front Endocrinol (Lausanne) .2019 Apr 12; 10: 155.
[5] I-Mahapatra MK, iKaruppasamy M, i-Sahoo BM. I-Therapeutic Potential ye-Semaglutide, i-GLP-1 entsha ye-Receptor Agonist, kwi-Abating Obesity, i-Non-Alcoholic Steatohepatitis kunye nezifo ze-Neurodegenerative: Ukuphononongwa kwe-Narrative.Pharm Res.2022 Jun; ): 39-6.
