Mk -2866 ntsiav tshuaj(Ostarine ntsiav tshuaj) yog qhov siv tau qhov ncauj thiab cov ntsiav tshuaj muaj txiaj ntsig zoo rau cov leeg ua kom zoo nkauj, xws li cov leeg nqaij tawv, thiab muaj zog tshaj tawm cov curves, thiab kev muab tshuaj ntau dua Cov Qauv Txheej Txheem . mk-2866 Cov qauv kev nqus tau zoo li ntau dua 80 teev, ua rau nws haum rau ib zaug Cov thawj coj .} Tsis tau pom zoo los ntawm FDA, ua rau muaj kev nyab xeeb ntau, thiab kev tiv thaiv lub siab ntev thiab ua kom muaj kev phom sij ntev thiab ua kom muaj kev phom sij ntev heev Cov tuam txhab cov tuam txhab uas tau raug tshawb xyuas nws cov ntawv thov kev kho mob, xws li Cancexia thiab laus sarcopenia .
|
|
|
Ostarine (Mk -2866}) hmoov coa
Pharmacological bety thiab ib nrab-lub neej muaj zog ntawm mk -2866
Mk -2866 (Ostarine) yog ib qho kev xaiv And19} {}} Cov tshuaj exert xaiv kev ua haujlwm hauv cov ntaub so ntswg hauv anabolic (e {{. g}}, leeg, pob txha) nrog cov ntaub so ntswg tsis muaj txiaj ntsig zoo li cov prostate.
RAW ib nrab-lub neej cov ntaub ntawv
Kev tshawb nrhiav thaum ntxov:Tom qab ib qho kev txhaj tshuaj ib zaug ntawm 10 mg / kg, ntshav siab ua kom tsawg dua biphasically nrog rau kev pib ua haujlwm ib nrab-lub neej tsis qhia meej tshaj tawm.
Qhov ncauj tsim kev ua kom zoo dua:Tom qab kev txhim kho los ntawm micronizalial thev naus laus zis tau nce ntxiv thiab ib nrab-lub neej tau txuas ntxiv mus rau 24 teev ib zaug noj tshuaj ib zaug {}}
Chaw ua yeeb yam zoo
Cov nqaij expality:Hauv ib qho qauv ua piv txwv, qhov koob tshuaj ntawm 0 {{}}}}} 03%, prostate lub cev rov qab los ntawm kev xaiv qhov hnyav rau cov nqaij mos siab rau anabolic.
Metabolic stability:Qhov tsis yog-c17-}} echaly alkylated qauv zam kev cuam tshuam hepatotoxicity, nyob rau hauv sib piv rau cov khoom noj khoom haus kua zaub.
EXTended-Tso Tawm Ntsiav Tshuaj Tshuab thiab Cov Ntawv Qhia
Kev Tso Tawm Ntxiv-Tso Tawm Txo cov kev tswj hwm ntau zaus los ntawm kev tswj hwm tus nqi ntawm kev saib xyuas ntawm cov ntshav ntawm cov tshuaj tiv thaiv ntshav. cov thev naus laus zis xws li:
Txheej Tshuab Tshuab
Enteric txheej:
Cov Khoom Siv: HydroxyPropylropylroylal Cellulose phthalate (HPMCP), cellulose acetate phthalate (cor), thiab lwm yam.
Mechanism: insoluble hauv cov acidic ib puag ncig ntawm lub plab (pH<5.5), dissolved after entering the intestines (pH>6 {. 0), kom ua tiav txoj hnyuv hauv zos tso tawm.
Daim ntawv thov: Zam kev ywg dej rau lub plab zom mov, muab cov pa roj acid acid acid acid didadation (e {}} {{1} {{3}
Qeeb-tso txheej:
Cov khoom siv: Ethyl cellulose, polymethacrylate, thiab lwm yam.
Mechanism: tswj cov tshuaj diffusion tus nqi los ntawm kev tswj cov txheej txheej txheej tuab lossis porosity .
Daim Ntawv Thov: Exolong Tshuaj Tso Tawm Sijhawm (E {{{} g. Metrofrolol Ncua-tso cov ntsiav tshuaj).
Lub cev ua tshuab
Hydrophilic gel skeleton:
Cov khoom siv: hydroxyprropylropylsylcelylulose (HPMC), carbomer, thiab lwm yam .
Mechanism: Tsim cov gel txheej hauv kev sib cuag nrog dej, thiab cov tshuaj raug tso los ntawm kev sib txawv los ntawm kev sib txawv los ntawm gel txheej .
Daim Ntawv Thov: Haum rau Dej-Soluble Yeeb Tshuaj (E .}}} {PropafEne Ncua-tso cov ntsiav tshuaj).
Insoluble pob txha pob zeb:
Cov khoom siv: Polyethylene, polypropylene, thiab lwm yam .
Mechanism: cov tshuaj raug tso tawm los ntawm kev sib txawv los ntawm cov hws ntawm lub cev pob txha skees ntawm lub cev pob txha pob ntseg
Daim Ntawv Thov: Rau cov tshuaj tsis muaj tshuaj tiv thaiv (xws li nifedipine txuas ntxiv-tso cov ntsiav tshuaj).
Micro-ntsiav tshuaj thev naus laus zis
Kev npaj: cov tshuaj tau sib xyaw nrog kev zam kom muaj cov tshuaj micro-ntsiav tshuaj ({mm hauv cov ntsiav tshuaj lossis sau rau hauv cov ntsiav tshuaj {}}
Qhov Zoo:
Kev Pom Kev Tso Tawm Yooj Yim, me ntsis cuam tshuam los ntawm kev ua kom muaj qhov tsis muaj zog los ntawm kev ua kom muaj zog .
Cov tshuaj piv nrog cov nqi sib txawv tuaj yeem ua ke rau cov kev xa khoom tus kheej (cov khoom siv tus kheej (}
Cov ntawv thov: e {{{. g. metformin expected-tso cov ntsiav tshuaj.
Cov tswv yim tsim qauv rau mk -2866}}}}} ext ext-tso cov ntsiav tshuaj
Raws li cov khoom siv dag ntawm mk -2866 (logp ≈ 3.5, solubility ≈ 3.5, solubility ≈ 1,4 mg / ml / ml
Khoom Siv Tau Devermersion:
Cov khoom thauj: polyethylene glycol (peg), polyvinylpropanone (PVP), thiab lwm yam .
Mechanism: Txhim kho cov tshuaj dispersion, nce cov lus xaus .
Rooj plaub: mk {{-2866 Thiab peg 6000 tau melted thiab sib xyaw ua ke rau 5 mg / ml .
Nanocrystal Tshuab:
Kev npaj: kev kub siab homogenization kom txo cov tshuaj kom tsawg rau<1 μm.
Cov nyhuv: solubility tau nce los ntawm 3-5 lub sij hawm, thiab bioavailability tau nce los ntawm 40%.
Cov Khoom Xaiv:
Cov khoom siv Ethylose: Hydrophobic khoom, haum rau ncua tso .
Eudragit® RS / RL: Acrylic Resin los tswj kev xaiv permeability los ntawm kev kho cov ntsiab lus ntawm Quamary Ammonium pab pawg {}}}}
Txheej Txheem Txhim Kho:
Fluidized Txaj Txheej: Tswj cov txheej hnyav nce ntawm 10%-15% rau {}}}
Laser perforation: {{{0} mm inch txoj kab uas hla ntawm cov ntsiav tshuaj kom tswj cov kev tso tawm .
Dual-txheej Micropellet Tsim:
Kev tso tawm tam sim: muaj 20% mk-2866}}}}}} dua li 80% nyob rau hauv 5 feeb.
Kev txhawb nqa txheej txheej txheem: 80% mk -2866, txhawb nqa kev tso tawm ntau dua 12 teev.
Hauv vitro tso tawm profile:
Lub Hom Phiaj: T₁ /=24 h, cmax {1} {{2} {} .
Cov ntaub ntawv tiag tiag: T₁ / ₂ tau txuas ntxiv mus 28 teev rau kev ua kom raug txo rau 12 NG / ML, thiab cov ntawv sau ua haujlwm raug txo los ntawm 180% rau 60%.
Cov nyhuv ntawm cov txheej txheem tso tawm qeeb tawm ntawm lub neej ib nrab-lub neej ntawm mk -2866
Theoretical qauv tsom xam
Thawj qhov kev tso tawm Kinetics:
REPUTIONS RISION: DM / DT=- k₀m
Ib nrab-lub neej: t₁ / ₂=ln (2) / K₀
Cov nyhuv qeeb tawm: K₀ yog txo los ntawm 50%, thiab t₁ / ₂ yog lub caij nyoog ntev los txog 1 . 4 zaug.
Higuchi Qauv:
Tso Tawm: Q=K√ K ..t
Retarded tso tawm nyhuv: caij nyoog ntawm kev tso tawm sijhawm los ntawm kev nce tus nqi ntawm k (e {}}}}}} {.
Cov ntaub ntawv cov ntaub ntawv siv tau
Cov ntsiav tshuaj niaj zaus:
Tmax {{0 {}} teev, t₁ / ₂=24}.
Kev tso cov ntsiav tshuaj txuas ntxiv:
Tmax txuas mus rau 6 teev, t₁ / ₂ ncua rau 30-36}.
Cov Ntaub Ntawv: Kawm Ntawv Kho Mob, Kev Tso Tawm Kev Ceev-Tshaj Tawm Kev Kho Mob, thiab Kev Siv Hluav Taws Xob Tsis Sib Haum tau txuas ntxiv ntawm 24 rau 36 teev.
Koom Haum Hauv PharpacyniMia
Cov leeg ua kom zoo li cas:
Cov ntsiav tshuaj ib txwm muaj: Ntshav testosterone ntau cov qib tau zoo hloov kho ntawm {}} nmol / l tshaj 24 teev {2}.
Kev tso tshuaj ntxiv-tso cov ntsiav tshuaj: Qib Serum Testosterone tau tswj hwm ntawm cov kev mob tshwm sim (e} g}}
Metabolic stability:
Kev Xa Khoom Ntxiv Tawm Kev Them Nyiaj HDL
Cov zeem muag thiab cov nyom ntawm daim ntawv thov kho mob
Ntsiab ntawm cov txiaj ntsig
Tus neeg mob ua raws: Thaum noj cov kev pheej hmoo tsawg ntawm cov koob tshuaj thiab kev kho dua kev kho ncua txuas ntxiv}
Kev Nyab Xeeb Ua Kom Nyab Xeeb: Kev ruaj khov ntawm cov ntshav nce thiab cov kev mob tshwm sim (e {} g}, pob txuv}, plaub hau) {3}
Kev lag luam: Kev kho cov qauv ntev, kev tso tawm txuas ntxiv tuaj yeem txo tus nqi ntawm cov tswv cuab los ntawm kev txo tus lej ntawm .
R & D cov nyom
Txheej txheem nyuaj:
Cov khoom siv micro ntsiav tshuaj yuav tsum muaj cov khoom siv ntsuas ua ke, nce ntau lawm nqi.
Txheej txheej txheem kev tswj hwm yuav tsum tau sim nruj ua tau zoo .
Tus neeg sib txawv:
Cov plab zom mov PH sib txawv tej zaum yuav cuam tshuam kev sib txuam ntawm cov txheej txheem sib txawv, xav tau kev hloov kho cov kheej {}}
Cov Cai Tswj:
Kev ncua tawm-tso tawm yuav tsum xa cov ntaub ntawv ntau ntxiv, uas tau ncua kev pom zoo.
Yav Tom Ntej Cov Lus Qhia
Kev Txawj Ntse qeeb-tso tawm:
pH / enzyme-teb cov cab kuj rau cov kev nkag siab zoo tso .
3D luam tawm rau tus kheej koob tshuaj rau .
Co-tswj hwm:
Ua ke nrog vitamin d3 thiab calcium los txhim kho cov osteoporosis kev kho {}}
Ua ke nrog cov tshuaj anti-estrogen (e {{1} g {} Tamoxifen) los txo cov kev mob estrogen-ntsig txog {}}
Tag
Mk -2866 tov tshuaj tau tsim los kom muaj kev ua haujlwm ib zaug, tab sis kuj tau ua kom muaj kev ua raws li ib zaug ntawm kev xa hluav taws xob txuas ntxiv-tso tawm thiab cov tshuaj kho mob, mk {{{}}}}}}}}}}}}}} Txoj kev sib tw thiab tus kheej sib txawv {}}
Yam uas pab
Mk -2866 ntsiav tshuaj(Ostarine), raws li ib qho kev xaiv Androgen Revenor Modle (sarm), ua kom pom qhov tseem ceeb ntawm cov leeg nqaij rov ua haujlwm {}} Cov ntsiab lus tseem ceeb tuaj yeem ua raws li hauv qab no:
Cov leeg muaj zog tseem ceeb nrog cov kev mob tshwm sim
Precision leeg lub tsev:Mk -2866 Xaiv tau cov leeg thiab cov pob txha ua kom muaj zog ua ntej ntawm 3 lub zog
Cov kev mob me:Piv rau cov khoom siv steroids, mk {-2866 Tsis yuav siv tshuaj tiv thaiv kab mob, lossis ua kom muaj zog}} kev siv tshuaj haormones) qib .
Dav muaj feem xyuam:Vim nws muaj kev nyab xeeb, mk -2866 yog dav siv los kho cov leeg leeg, thiab tau dhau los ua cov leeg nqaij hlav cancerers) thiab muaj zog rau cov leeg nqaij {}}
Tiv thaiv cov leeg hauv lub sijhawm ua kom lub sijhawm rog thiab kev txhim kho meabolic
Los tiv thaiv cov leeg nqaij tawg:Thaum lub sij hawm calorie-tsis muaj roj tsis zoo, mk-2866}}}} poob thaum tsim cov leeg ".
Txhim kho cov ntsuas metabolic:Mk -2866 Yuav ua rau cov neeg siv lub plab zom mov thiab tsis muaj kev sib cav sib ceg
Txhim Kho Kev Ncaws Pob Ua Haujlwm:Los ntawm kev ua kom muaj zog thiab lignament lub zog, mk -2866 tuaj yeem txhim kho kev cob qhia kev ua haujlwm muaj zog thiab kev pheej hmoo ntawm kev kis las kis las {}}
Lub mis scientula thiab yooj yim
Ntev ib nrab-lub neej:Ib nrab-lub neej ntawm mk -2866 yog 24 teev, thiab kev tswj hwm ntshav ib zaug tuaj yeem ua kom tiav cov tshuaj ua ntej.
Saj zawg zog ntau:Qhov kev pom zoo tau muab tshuaj pleev tau yog 10-40 mg ib hnub, uas tuaj yeem hloov kho raws li lub sijhawm rog, nws pom zoo kom siv {4-8 lub lis piam; Thaum lub sij hawm lub leeg lub sij hawm lub sij hawm lub sij hawm lub sij hawm lub sij hawm lub sij hawm lub sij hawm lub sij hawm lub sij hawm lub sij hawm, nws raug nquahu kom siv 20-30} 8-12 part.
Cov yam ntxwv tsis yog methylation:Mk -2866 Tsis muaj lub siab xav tau los ntawm sterid metabolism hauv lub siab.
Cov chaw kuaj mob pov thawj thiab kev nyab xeeb
Txhawb nqa los ntawm ntau-theem kev sim:Mk -2866} Tau ua tiav ntau yam I, II, thiab III theem kev sim siab, thiab nws tau muaj kev nyab xeeb rau cov neeg mob tsis sib xws
Cov kev mob tshwm sim muaj pob tshab:Kev paub cov tshwm sim muaj qib Testosterone me me), thiab kev txaus siab ntev dua), tab sis cov kev phom sij ntev (HDL
Cim npe nrov: mk -2866} ntsiav tshuaj, chaw muag khoom, chaw tsim khoom, Hoobkas, lag luam, yuav, nqe, loj, rau muag