Caspofungin Acetate Igikorwa cyibinyabuzima
Sobanura | Caspofungin Acetate ni imiti igabanya ubukana ishobora kutabangamira guhuza synthesis ya 1,3-β-d glucan synthase。 |
Bifitanye isanoibyiciro | inzira yerekana ibimenyetso >> Kurwanya kwandura >> Fungus Ibice byubushakashatsi >> Yanduye |
Muri vivoubushakashatsi | Imbeba zatewe na caspofungin nta mpinduka nini zigeze zihinduka mu miterere ya ERG ku gipimo cya 0.41 kugeza kuri 4.1 μM, kandi retina yabo nta mpinduka yagaragaye yagaragaye cyangwa gutakaza selile.Mugihe cya vitreous ya 41 μM, caspofungin yagabanije amplitude yumuraba, b umuraba hamwe na scotopic imbibi za ERG, kandi binagabanya umubare wutugingo ngengabuzima twa selile ya ganglion [1].Carprofungin (8 mg / kg) cyangwa amphotericine B 1 mg / kg, inshinge za intraperitoneal rimwe kumunsi 30 h nyuma yo kwandura iminsi 7 ikurikiranye, ugereranije no kuvura ibinyabiziga, kubaho 100% kumunsi wa 28, bigatuma ku manywa 100% bapfa 11 , nyuma yikibazo cyanduye.Ugereranije no kuvura ibinyabiziga ku munsi wa 5, caspofungin yagabanije gukira kwa Candida nzima mu mpyiko no mu bwonko igihe umutwaro wo kugenzura wageze ku rwego rwo hejuru.Imbeba zavuwe na caspofungine ku gipimo cya mg / kg 2 cyangwa zirenga zaragabanutse cyane ku bwonko ku munsi wa 5 kuruta imbeba zavuwe na amphotericine B. Amphotericine B hamwe no kuvura caspofungin byagabanije umutwaro w’impyiko 1.7 log CFU / g na 2.46 kugeza 3.64 log CFU / g, kimwe [2]。 |
Inyamaswaigerageza | Ubuvuzi bwa antifungal bwatangiye nyuma yamasaha 30 nyuma yikibazo cyanduye kandi butangwa ninshinge ya intraperitoneal (ip) rimwe kumunsi iminsi 7.Imbeba zavuwe hamwe na 1, 2, 4, cyangwa 8 mg / kg / kumunsi caspofungin, mg / kg / kumunsi amphotericine B cyangwa kugenzura ibinyabiziga (amazi meza).Imikorere yicyitegererezo yasuzumwe muburyo butatu: mugukurikirana igipimo cyokubaho kwinyamaswa 10 muri buri tsinda rivura, mugukurikirana umutwaro wa Candida mumpyiko nubwonko bwitsinda rya kabiri ryinyamaswa zavuwe, no gusuzuma amateka yimpyiko.Ubwonko.Itsinda rya gatatu ryinyamaswa zavuwe.Imbeba zashizwemo umwuka na CO 2 no guhumeka mumasaha 30 (kugenzura ibinyabiziga bivurwa gusa) no kumunsi wa 5 (amasaha 24 nyuma yumuti wa 4), 8 (amasaha 24 nyuma yumuti uheruka), namasaha 14, 21 Kandi amateka icyitegererezo.(Gusa kuvura caspofungin), na 28 nyuma yigitero. |
Reba | [1].Mojumder DK, n'abandi.Gusuzuma uburozi bwa retinal bwa intravitreal caspofungin mumaso yimbeba.Shora Ophthalmol Vis Sci.2010 Ugushyingo; 51 (11): 5796-803. [2].Flattery, Amy M. n'abandi.Imikorere ya caspofungin muburyo bwimbeba yimbeba ya santrale yo hagati ya kandidiasis.Imiti igabanya ubukana na chimiotherapie (2011), 55 (7), 3491-3497. |
Ibikoresho bya chimique na physique ya caspofungin acetate
Ingingo yo guteka | 1408.1ºC kuri 760 mmHg |
Inzira ya molekulari | C56H96N10O19 |
Uburemere bwa molekile | 1093.31000 |
Ubwiza | 1092.64000 |
PSA | 412.03000 |
LogP | 0.06150 |
Ibiranga isura | cyera to beige |
Umuvuduko wumwuka | 0mmHg kuri 25 ° C. |
Imiterere yo kubika | 20 ° C. |
Amazi meza | H2O: gushonga15mg / mL (igisubizo gisobanutse) |
Gasutamo ya Caspofungin
Kode ya gasutamo | 2933990099 |
Incamake y'Ubushinwa | 2933990099. Ibindi bikoresho bya heterocyclic birimo azote ya azote gusa.Igipimo cy'umusoro ku nyongeragaciro: 17.0%.Igipimo cyo kugabanyirizwa imisoro: 13.0%.Ibisabwa: Nta na kimwe.Igiciro cyigihugu gikunzwe cyane: 6.5%.Igiciro rusange: 20.0% |
Ibimenyesha | Izina ryibicuruzwa, ibiyigize, koresha, hexamethylene chloride, nyamuneka werekane isura, 6-caprolactam, nyamuneka werekane isura, itariki yo gusinya |
Incamake | 2933990090. ibice bya heterocyclic hamwe na azote hetero-atom (s) gusa.TVA: 17.0%.Igipimo cyo kugabanyirizwa imisoro: 13.0%..Igiciro cya MFN: 6.5%.Igiciro rusange: 20.0% |
Inzira yumusaruro
Caspofungin igomba gutegurwa na tekinoroji ya fermentation.Ibicuruzwa bitarondoreka byimpeta nyamukuru bigomba kuboneka hifashishijwe ikoranabuhanga rya fermentation, hanyuma ibicuruzwa bigereranywa bikaboneka mugutandukana no kwezwa, hanyuma ibicuruzwa bigaciriritse bikoreshwa nkibikoresho byo gutangira kurangiza urunigi rwuruhande rwifashishije ikorana buhanga kugirango amaherezo abone intego Intego.Kuberako ibicuruzwa "fermented semi-synthique" bigomba kunyura muburyo bwa tekinike nka fermentation, gutandukana no kwezwa, synthesis, nibindi, inzira ya tekiniki hamwe no kugenzura ibipimo biragoye cyane mubitabo bya Chemical.Byongeye kandi, ibisabwa n'amategeko agenga iyandikwa rya caspofungin, ibicuruzwa biva mu gice cya sintetike, nabyo biri hejuru cyane.Inyandiko zisaba zigomba gutangirira kumasoko ya fermentation, ntabwo ari ukwiga gusa gahunda yo guhinga amoko, tekinoroji ya fermentation, hamwe nikoranabuhanga ryo kweza, ariko kandi no gushakisha inzira ya synthesis.Inzira, imiterere, hamwe no kugenzura umwanda mubikorwa, kubera ko ibicuruzwa byanyuma byoroshye cyane, uburangare ubwo aribwo bwose buzahanagura imbaraga zose zabanjirije iyi, kandi ingorane za tekiniki nigiciro ntabwo ari bike.
Ni ukubera ko inzitizi zo mu rwego rwo hejuru hamwe n’ahantu heza ho guhatanira Hengrui Caspofungin yagumanye umwanya mwiza ugereranije nyuma yo kurutonde.
Kurinda patenti byarangiye muri 2014
Kugurisha inshinge za caspofungin mu bigo nderabuzima bya Leta y'Ubushinwa (igice: ibihumbi icumi)
Kugeza ubu, imiti rusange y’imiti ya Hengrui, Chia Tai Tianqing, Pharmaceuticals ya Borui, na Haisco niyo yonyine yemewe kurutonde.Ubuvuzi bwa Huadong?
Isosiyete yambere yubushakashatsi bwa caspofungin acetate ni Merck, kandi ibyifuzo byurutonde rwibigo 6 birasuzumwa kandi byemejwe, aribyo Qilu Pharmaceutical, Nanjing Yinxing Pharmaceutical, Sihuan Pharmaceutical, Osaikang Pharmaceutical, Sino-US Huadong Pharmaceutical, na Tian Wei Biopharmaceuticals.
JIN DUN Ubuvuzi bufiteImpamyabumenyi ya ISO kandi yujuje ubuziranenge bwa GMP, yakoresheje inzobere mu kuvura ibiyobyabwenge mu gihugu no mu mahanga bifite uburambe bukomeye bwo kuyobora R&D ya sosiyete.
TECHNOL OGY INYUNGU
Pressure Umuvuduko mwinshi Catalytic Hydrogenation.Umuvuduko mwinshi Hydrogenolysis reaction.Imyitwarire ya Cryogenic (<-78% C)
● Synthesis ya Aromatic Heterocyclic
Re reaction Kuvugurura
Res Igisubizo cya Chiral
Heck, Suzuki, Negishi, Sonogashira.Gignard
Ibikoresho
Laboratwari yacu ifite ibikoresho bitandukanye byo kugerageza no kugerageza, nka: NMR (Bruker 400M) 、 HPLC 、 chiral-HPLC 、 LC-MS 、 LC-MS / MS (API 4000) 、 IR 、 UV 、 GC 、 GC-MS, Chromatografiya, Microwave Synthesizer, Parallel Synthesizer, Calorimeter itandukanye (DSC), Electron Microscope ...
Itsinda R&D
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Urubanza rwa Customzation Urubanza rwa mbere:
Cas No.: 110351-94-5
Urubanza rwa Customzation Urubanza rwa kabiri:
Cas No.: 144848-24-8
Urubanza rwa Customzation Urubanza rwa gatatu:
Cas No.: 200636-54-0
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