Příprava a hodnocení alginátových mikročástic s obsahem indometacinu
:
Penjuri Subhash Chandra Bose; Ravouru Nagaraju; Damineni Saritha; Budumuru Padmasri; Poreddy Srikanth Reddy
:
Department of Pharmaceutics, MNR College of Pharmacy, Sangareddy, Telangana, India
1; Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Visvavidyalayam, India
2; Department of Pharmaceutics, Sultan-ul-Uloom College of Pharmacy, Hyderabad, Telangana, India
3
:
Čes. slov. Farm., 2016; 65, 104-110
:
Original Articles
Alginátové mikrosféry s indomethacinem byly připraveny intovou gelací za použití chloridu vápenatého. Byl hodnocen vliv koncentrace chloridu vápenatého na velikost, enkapsulační účinnost a sféricitu připravených mikročástic. Bylo zjištěno, že změnou různých formulačních proměnných lze měnit enkapsulační účinnost i disoluční profil mikrosfér. Optimální in vitro disoluční profil indometacinu (podle USP specifikace s prodlouženým uvolňováním) byl dosažen ze vzorku obsahujícího 2 % natrium-alginátu a 2 % methylcelulosy tvrzeného v 3% roztoku chloridu vápenatého. Dle kinetického modelování disolučních dat byl Highuchi difuzní model vybrán jako vhodný. Dle FTIR studie nebyly potvrzeny žádné interakce mezi složkami mikročástic. DSC a XRD studie odhalily, že krystalinita léčiva inkorporovaného do mikročástic byla nižší ve srovnání s čistým léčivem. Farmakokinetické parametry byly získány na základě in vivo testů na králících s použitím HPLC techniky. Bylo zjištěno, že indomethacinové mikrosféry prokázaly vyšší t1/2 a AUC ve srovnání s indomethacinovou suspenzí. Jednoznačně bylo tedy prokázáno řízené uvolňování léčiva z mikrosfér, poskytující delší působení léčiva v terapeutickém rozmezí, které je výhodné zejména v léčbě chronických onemocnění
Klíčová slova:
indometacin • řízené uvolňování • Fickova difuze • farmakokinetika
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Czech and Slovak Pharmacy
2016 Issue 3
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