Nitrendipine nanocrystals: its preparation, characterization, and in vitro-in vivo evaluation.
AAPS PharmSciTech
; 12(4): 1136-43, 2011 Dec.
Article
in En
| MEDLINE
| ID: mdl-21892695
ABSTRACT
The present investigation was undertaken with the objective of developing a solid formulation containing nitrendipine nanocrystals for oral delivery. Nitrendipine nanocrystals were prepared using a tandem precipitation-homogenization process. Then, spray drying, a cost-effective method very popular in industrial situations, was employed to convert the nanocrystals into a solid form. The parameters of the preparation process were investigated and optimized. The optimal process was as follows firstly, nitrendipine/acetone solution (100 mg/ml) was added to a polyvinyl alcohol solution (1 mg/ml) at 10°C, then the pre-suspension was homogenized for 20 cycles at 1,000 bar. Both differential scanning calorimetry and X-ray diffraction analysis indicated that nitrendipine was present in crystalline form. The in vitro dissolution rate of the nanocrystals was significantly increased compared with the physical mixture and commercial tablet. The in vivo testing demonstrated that the C(max) of the nanocrystals was approximately 15-fold and 10-fold greater than that of physical mixture and commercial tablet, respectively. In addition, the AUC(0â24) of the nanocrystals was approximately 41-fold and 10-fold greater than that of physical mixture and commercial tablet, respectively.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Calcium Channel Blockers
/
Nitrendipine
/
Technology, Pharmaceutical
/
Nanotechnology
/
Nanoparticles
Limits:
Animals
Language:
En
Journal:
AAPS PharmSciTech
Journal subject:
FARMACOLOGIA
Year:
2011
Document type:
Article
Affiliation country:
China