Abstract
In this study, nifedipine tablets were formulated with different types of cyclodextrins (CDs) by direct compression method. Spray dried lactose and microcrystalline cellulose (MCC) were used as tablet fillers. The prepared tablets showed good appearance with acceptable crushing strength and disintegration time. The tablets showed fast dissolution within 11 to 68 min for 80% of the drugs depending on the type of CD and tablet filler. Some of the formulated tablets presented good fast release properties similar to soft gelatin capsules (USP XXIV) and based on the calculated dissolution efficiency (DE%), tablets containing hydroxypropyl-β-CD and lactose as a filler were chosen for in vivo study by oral administration to beagle dogs when compared with the commercially available 10 mg soft gelatin capsule (Adalat®) and 10 mg film coated tablets (Corinfar ®). The formulated tablets showed significantly higher area under the curve (AUC0-∞) than the commercial soft gelatin capsule and film coated tablets as result of increased drug absorption. It was concluded that the formulated fast release tablets could replace the nifedipine soft gelatin capsules with the advantages of ease of preparation and less restricted storage and handling conditions. Key words: Nifedipine tablets, cyclodextrins, bioavailability, beagle dogs.
Highlights
Cyclodextrins (CDs) and their derivatives play an important role in the development of drug formulation due to their multifunctional characteristics and bioadaptability, that is, they are capable of alleviating the undesirable properties of drug molecules through the formation of inclusion complexes (Baboota and Agarwal, 2003; Rasheed et al, 2008)
Microcrystalline cellulose (MCC; Avicel PH101) and spray dried lactose were chosen as tablet
The dissolution properties of nifedipine from the formulated nifedipine-CD complex tablets were initially dependent on the type of CD along with the tablet filler
Summary
Cyclodextrins (CDs) and their derivatives play an important role in the development of drug formulation due to their multifunctional characteristics and bioadaptability, that is, they are capable of alleviating the undesirable properties of drug molecules through the formation of inclusion complexes (Baboota and Agarwal, 2003; Rasheed et al, 2008). These inclusion complexes have been shown to improve the stability, solubility, dissolution rate and bioavailability of drugs (Duchene and Wouessidjewe, 1990; Bekers, 1991). In our previously published report, we succeeded to protect nifedipine against the effect of light along with improving its dissolution profile by inclusion complexation with different types of CDs (Bayomi et al, 2002), namely: -CD, HP- -CD or DM- -CD
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