Investigation of physical properties and stability of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems prepared by quench cooling, coprecipitation and ball milling
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Investigation of physical properties and stability of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems prepared by quench cooling, coprecipitation and ball milling. / Lim, Ai Wei; Löbmann, Korbinian; Grohganz, Holger; Rades, Thomas; Chieng, Norman.
In: Journal of Pharmacy and Pharmacology, Vol. 68, No. 1, 01.2016, p. 36-45.Research output: Contribution to journal › Journal article › Research › peer-review
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T1 - Investigation of physical properties and stability of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems prepared by quench cooling, coprecipitation and ball milling
AU - Lim, Ai Wei
AU - Löbmann, Korbinian
AU - Grohganz, Holger
AU - Rades, Thomas
AU - Chieng, Norman
N1 - © 2015 Royal Pharmaceutical Society.
PY - 2016/1
Y1 - 2016/1
N2 - OBJECTIVES: The objective was to characterize the structural behaviour of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems (1 : 1 molar ratio) prepared by quench cooling, co-evaporation and ball milling.METHODS: Powder X-ray diffraction (PXRD) and DSC were used to characterise the samples. Structural relaxation (i.e. molecular mobility) behaviour was obtained from the Kohlrausch-Williams-Watts (KWW) relationship.KEY FINDINGS: A glass transition temperature (Tg ), on average 20 °C higher than the predicted Tg (calculated from the Fox equation), was observed in all samples. The structural relaxation was dependent on the preparative methods. At a storage temperature of 40 °C, a comparatively higher molecular mobility was observed in indomethacin-cimetidine samples prepared by ball milling (ln τ(β) = 0.8), while similar molecular mobility was found for the same sample prepared by quench cooling (ln τ(β) = 2.4) and co-evaporation (ln τ(β) = 2.5). In contrast, molecular mobility of the naproxen-cimetidine samples followed the order co-evaporation (ln τ(β) = 0.8), quench cooling (ln τ(β) = 1.6) and ball milling (ln τ(β) = 1.8).CONCLUSION: The estimated relaxation times by the DSC-KWW method suggest that different preparative methods resulted in a variation of structural characteristics. Despite the differences in molecular mobility, all sample remained co-amorphous for up to 7 months.
AB - OBJECTIVES: The objective was to characterize the structural behaviour of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems (1 : 1 molar ratio) prepared by quench cooling, co-evaporation and ball milling.METHODS: Powder X-ray diffraction (PXRD) and DSC were used to characterise the samples. Structural relaxation (i.e. molecular mobility) behaviour was obtained from the Kohlrausch-Williams-Watts (KWW) relationship.KEY FINDINGS: A glass transition temperature (Tg ), on average 20 °C higher than the predicted Tg (calculated from the Fox equation), was observed in all samples. The structural relaxation was dependent on the preparative methods. At a storage temperature of 40 °C, a comparatively higher molecular mobility was observed in indomethacin-cimetidine samples prepared by ball milling (ln τ(β) = 0.8), while similar molecular mobility was found for the same sample prepared by quench cooling (ln τ(β) = 2.4) and co-evaporation (ln τ(β) = 2.5). In contrast, molecular mobility of the naproxen-cimetidine samples followed the order co-evaporation (ln τ(β) = 0.8), quench cooling (ln τ(β) = 1.6) and ball milling (ln τ(β) = 1.8).CONCLUSION: The estimated relaxation times by the DSC-KWW method suggest that different preparative methods resulted in a variation of structural characteristics. Despite the differences in molecular mobility, all sample remained co-amorphous for up to 7 months.
U2 - 10.1111/jphp.12494
DO - 10.1111/jphp.12494
M3 - Journal article
C2 - 26663364
VL - 68
SP - 36
EP - 45
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
SN - 0022-3573
IS - 1
ER -
ID: 162186787