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Rapidly absorbed orodispersible tablet containing molecularly dispersed felodipine for management of hypertensive crisis: development, optimization and in vitro/in vivo studies.
- Source :
-
Pharmaceutical development and technology [Pharm Dev Technol] 2013 Mar-Apr; Vol. 18 (2), pp. 407-16. Date of Electronic Publication: 2012 Feb 18. - Publication Year :
- 2013
-
Abstract
- A liquisolid orodispersible tablet of felodipine, a BCS Class II drug, was developed to improve drug dissolution and absorption through the buccal mucosa for management of hypertensive crisis. A 24 full-factorial design was applied to optimize felodipine liquisolid systems (FLSs) having acceptable flow properties and possessing enhanced drug dissolution rates. Four formulation variables; The liquid type, X1 (PG or PEG), drug concentration, X2 (10% and 20%), type of coat, X3 (Aerosil® and Aeroperl®) and excipients ratio, X4 (10 and 20) were included in the design. The systems were assessed for dissolution and flow properties. Following optimization, the formulation components (X1, X2, X3 and X4) were PEG, 10%, Aerosil® and 20, respectively. The optimized FLS was compressed into felodipine liquisolid orodispersible tablet using Prosolv® as carrier material (FLODT-2). The in vitro and in vivo disintegration times of FLODT-2 were 9 and 7 s, respectively. The in vivo pharmacokinetic study using human volunteers showed a significant increase in dissolution and absorption rates of the formulation of FLODT-2 compared to soft gelatin capsules filled with felodipine solution in PEG under the same conditions. Our results proposed that the optimized FLODT formulation could be promising to manage hypertensive crisis.
- Subjects :
- Absorption
Adult
Chemistry, Pharmaceutical methods
Cross-Over Studies
Excipients chemistry
Felodipine administration & dosage
Humans
Hypertension, Pulmonary metabolism
Liquid Crystals chemistry
Male
Mouth Mucosa metabolism
Solubility
Tablets administration & dosage
Tablets chemistry
Tablets pharmacokinetics
Felodipine chemistry
Felodipine pharmacokinetics
Hypertension, Pulmonary drug therapy
Subjects
Details
- Language :
- English
- ISSN :
- 1097-9867
- Volume :
- 18
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Pharmaceutical development and technology
- Publication Type :
- Academic Journal
- Accession number :
- 22339303
- Full Text :
- https://doi.org/10.3109/10837450.2012.659258