Co-stabilization of amorphous pharmaceuticals - The case of nifedipine and nimodipine
PBN-AR
Instytucja
Wydział Matematyki, Fizyki i Chemii (Uniwersytet Śląski w Katowicach)
Informacje podstawowe
Główny język publikacji
angielski
Czasopismo
MOLECULAR PHARMACEUTICS (45pkt w roku publikacji)
ISSN
1543-8384
EISSN
Wydawca
AMER CHEMICAL SOC
DOI
URL
Rok publikacji
2018
Numer zeszytu
6
Strony od-do
2455-2465
Numer tomu
15
Liczba arkuszy
0,50
Autorzy
Pozostali autorzy
+ 1
Słowa kluczowe
angielski
amorphous pharmaceuticals;
coamorphous system;
compression of amorphous APIs;
crystallization kinetics;
dielectric spectroscopy;
impact of elevated pressure on physical stability;
molecular dynamics;
nifedipine;
nimodipine;
physical stability
Streszczenia
Język
angielski
Treść
Currently, a research hotspot in amorphous active pharmaceutical ingredients (APIs) is to understand the key factors that dominate recrystallization and to develop effective methods for stabilizing amorphous forms. Consequently, we investigated the influence of the global molecular mobility and structural properties on the crystallization tendency of three 1,4-dihydropyridine derivatives (nifedipine, nisoldipine, and nimodipine) in their supercooled states using differential scanning calorimetry (DSC) and broadband dielectric spectroscopy (BDS) techniques. The BDS is also employed to monitor the isothermal crystallization kinetics of supercooled nifedipine and nimodipine at T = 333 K under ambient pressure. As a result, we found that nimodipine exhibits much slower crystallization in comparison to nifedipine. However, nimodipine crystallizes much faster when as little as 10 MPa of pressure is exerted on sample. Such compression-induced crystallization of nimodipine as well as the inherent instability of nifedipine can be solved effectively by preparing coamorphous nifedipine/nimodipine combinations. Interestingly, the high physical stability of nifedipine/nimodipine mixtures is achieved despite the fact that the nimodipine acts as a plasticizer.
Cechy publikacji
original-article
Inne
System-identifier
3342900145642
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