Dobijanje kokristala paliperidona sa poboljšanom rastvorljivošću i brzinom rastvaranja
Sažetak
U ovom istraživanju, kokristali (CCs) paliperidona (PPD) sa koformerima kao što su benzojeva kiselina (BA) i p-aminobenzojeva kiselina (PABA) sintetisani su, i okarakterisana su poboljšanja njihovih fizičko-hemijskih svojstava i brzine rastvaranja. Kokristali su pripremljeni postupkom isparavanja rastvarača (SE) i upoređeni su sa proizvodima dobijenim postupkom suvog (NG) i vlažnog mlevenja (LAG) u pogledu poboljšanja rastvorljivosti. Formiranje kokristala je potvrđeno metodama infracrvene spektroskopije, rendgenske difrakcije na prahu i termalne analize. Ispitivanja rastvorljivosti ukazuju na to da je rastvorljivost kokristala PPD-BA i PPD-PABA u vodi bila značajno veća i dostigla je vrednosti od 1,343±0,162 mg/ml i 1,964±0,452 mg/ml, u poređenju sa rastvorljivošću PPD koja iznosi 0,473 mg/ml. To znači da je rastvorljivost povećana 2,83, odnosno 3,09 puta. Za PPD je uočena niska brzina rastvaranja od 37,8% za 60 min, dok se brzina rastvaranja kokristala znatno povećala do 96,07% i 89,65% za 60 min. Kokristali PPD sa BA i PABA predstavljaju savremeni pristup u prevazilaženju izazova vezanih za rastvorljivost slabo rastvorljive lekovite supstance PPD.
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