Formulation of cinnarizine for stabilization of its physiologically generated supersaturation
Formulation of cinnarizine for stabilization of its physiologically generated supersaturation
نویسندگان: مریم مقصودی , علی نخودچی , سمن حیدری
کلمات کلیدی: supersaturation; cinnarizine; eudragit L100; hydroxypropyl methylcellulose;
crystallization inhibition; dissolution.
نشریه: 55007 , 139 , 20 , 2019
| نویسنده ثبت کننده مقاله |
مریم مقصودی |
| مرحله جاری مقاله |
تایید نهایی |
| دانشکده/مرکز مربوطه |
مرکز تحقیقات کاربردی دارویی |
| کد مقاله |
66798 |
| عنوان فارسی مقاله |
Formulation of cinnarizine for stabilization of its physiologically generated supersaturation |
| عنوان لاتین مقاله |
Formulation of cinnarizine for stabilization of its physiologically generated supersaturation |
| ناشر |
4 |
| آیا مقاله از طرح تحقیقاتی و یا منتورشیپ استخراج شده است؟ |
بلی |
| عنوان نشریه (خارج از لیست فوق) |
|
| نوع مقاله |
Original Article |
| نحوه ایندکس شدن مقاله |
ایندکس شده سطح یک – ISI - Web of Science |
| آدرس لینک مقاله/ همایش در شبکه اینترنت |
|
| Physiologically generated supersaturation and subsequent crystallization of a
weakly basic drug in the small intestine leads to compromised bioavailability. In this study,
the pH-induced crystallization of cinnarizine (CNZ) in the presence of different polymers
was investigated. Inhibitory effect of Eudragit L100 (Eu) on crystallization of CNZ at varying
supersaturation ratios was examined. The effect of Eu on the dissolution behavior of CNZ
from CNZ/Eu physical mixtures (PMs) and solid dispersions (SDs) was assessed. Results
showed that both Eu and hydroxypropyl methylcellulose (HPMC) have a considerable
maintenance effect on supersaturation of CNZ but Eu was more effective than HPMC. When
Eudragit was used the phenomenon of liquid-liquid phase separation (formation of colloidal
phase) was observed at supersaturation ratio of 20 times above the solubility of the drug.
PMs showed a higher area under the dissolution curve (AUDC) compared with plain CNZ.
In contrast, SDs showed a lower AUDC than plain CNZ. For SDs, the AUDC was limited by
the slow release of the drug from Eu in acidic pH which in turn hindered the creation of CNZ
supersaturation following the transition of acidic to neutral pH. From these findings, it can be
concluded that the ability of the formulation to generate supersaturation state and also
maintain the supersaturation is vital for improving the dissolution of CNZ. |
| نام فایل |
تاریخ درج فایل |
اندازه فایل |
دانلود |
| Maghsoodi2019_Article_FormulationOfCinnarizineForSta.pdf | 1398/02/23 | 748297 | دانلود |