TY - JOUR
T1 - Experimental Study on the Influence of Excipients on the Heterogeneous Crystallization and Dissolution Properties of an Active Pharmaceutical Ingredient
AU - Verma, Vivek
AU - Peddapatla, Raghu V.G.
AU - Crowley, Clare M.
AU - Crean, Abina M.
AU - Davern, Peter
AU - Hudson, Sarah
AU - Hodnett, Benjamin K.
N1 - Publisher Copyright:
© 2017 American Chemical Society.
PY - 2018/1/3
Y1 - 2018/1/3
N2 - This study is based on the heterogeneous nucleation of active pharmaceutical ingredients (APIs) in the presence of various excipients widely used in the pharmaceutical industry. Carbamazepine (CBMZ) was successfully crystallized in the presence of the following heterosurfaces: α/β-lactose, β-d-mannitol, microcrystalline cellulose, and carboxymethyl cellulose. The successful crystallization of CBMZ FIII in the presence of all the excipients was confirmed by powder X-ray diffraction and scanning electron microscopy, while CBMZ crystals' apposition was confirmed using in situ scanning electronic microscopy-Raman. A pronounced improvement in the dissolution of CBMZ FIII was observed when crystallized in the presence of excipients when compared with CBMZ FIII recrystallized using the same conditions in the absence of the excipients. The isolated solids could be simply tabletted by direct compression upon mixing with the desired amount of disintegrant and lubricant. Hence employing this process could potentially streamline the downstream process in pharmaceutical industries and also increase the throughput with reduced cost.
AB - This study is based on the heterogeneous nucleation of active pharmaceutical ingredients (APIs) in the presence of various excipients widely used in the pharmaceutical industry. Carbamazepine (CBMZ) was successfully crystallized in the presence of the following heterosurfaces: α/β-lactose, β-d-mannitol, microcrystalline cellulose, and carboxymethyl cellulose. The successful crystallization of CBMZ FIII in the presence of all the excipients was confirmed by powder X-ray diffraction and scanning electron microscopy, while CBMZ crystals' apposition was confirmed using in situ scanning electronic microscopy-Raman. A pronounced improvement in the dissolution of CBMZ FIII was observed when crystallized in the presence of excipients when compared with CBMZ FIII recrystallized using the same conditions in the absence of the excipients. The isolated solids could be simply tabletted by direct compression upon mixing with the desired amount of disintegrant and lubricant. Hence employing this process could potentially streamline the downstream process in pharmaceutical industries and also increase the throughput with reduced cost.
UR - http://www.scopus.com/inward/record.url?scp=85038857296&partnerID=8YFLogxK
U2 - 10.1021/acs.cgd.7b01336
DO - 10.1021/acs.cgd.7b01336
M3 - Article
AN - SCOPUS:85038857296
SN - 1528-7483
VL - 18
SP - 338
EP - 350
JO - Crystal Growth and Design
JF - Crystal Growth and Design
IS - 1
ER -