Formulation and evaluation of sustained release floating capsules of nicardipine hydrochloride.
Nicardipine hydrochloride, a calcium channel blocker with significant vasodilating and antihypertensive activities, was formulated in this work as sustained release floating capsules. A hydrocolloid of high viscosity grade was used for the floating systems. The inclusion of sodium bicarbonate to allow evolution of CO2 to aid buoyancy was studied. Polymers that retard drug release were included as coprecipitates with the drug and/or as additives in the formulated capsules. Both simple powder mixing of the ingredients and granule preparation via wet granulation were used. Seven capsule formulae were prepared. The prepared capsules were evaluated in vitro by testing drug dissolution, floating time and the kinetics of drug release. In vitro evaluation of a commercially available conventional 20 mg capsule of nicardipine hydrochloride, "Micard", was carried out for comparison. The hydrocolloid used succeeded in effecting capsule buoyancy. Floating time increased with increasing the proportion of the hydrocolloid. Inclusion of sodium bicarbonate increased buoyancy. All of the seven floating capsule formulae prepared proved efficient in controlling drug release. The sustained release floating capsule formulation of choice was evaluated in vivo in comparison to "Micard" capsules using rabbits. Reversed phase HPLC with UV detection was used for drug determination in rabbit plasma. Plasma concentration time curves revealed a longer drug duration for administration in the sustained release formula than the conventional "Micard" capsule being 16 h in the former versus 8 h for the latter.
Moursy
N M
NM
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Afifi
N N
NN
Ghorab
D M
DM
El-Saharty
Y
Y
D000818:Animals; D001682:Biological Availability; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000032:analysis / Q000493:pharmacokinetics; D002138:Calibration; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D005079:Excipients; D006863:Hydrogen-Ion Concentration; D008297:Male; D009529:Nicardipine / Q000008:administration & dosage* / Q000032:analysis / Q000493:pharmacokinetics; D011817:Rabbits; D012995:Solubility
D002121:Calcium Channel Blockers; D002214:Capsules; D003692:Delayed-Action Preparations; D005079:Excipients; D009529:Nicardipine