BIOAVAILABILTY STUDY OF NICARDIPINE LIQUISOLID COMPACT TABLETS IN RABBITS AFTER ORAL ADMINISTRATION

* J. Ramesh 1 , B. Vijaya kumar 2 and Y. Narasimha Reddy 3 . 1. Research Scholar Jawaharlal Nehru Technological University Kakinada, Kakinada, A.P. India. 2. Jangaon Institute Of Pharmaceutical Sciences, Jangaon, Warangal Dist, Telangana, India. 3. University College Of Pharmaceutical Sciences, Warangal Dist, Telangana, India. ...................................................................................................................... Manuscript Info Abstract ......................... ........................................................................ Manuscript History

Aim of the present research work is to conduct bio availability study of nicardipine liquisolid compact tablet in rabbit and compare with plain nicardipine drug. Study is conducted by using Randomized Balanced Incomplete Block Design (BIBD) method. Total 8 healthy rabbits were selected with weight of 2.5 kg to 3 kg. Rabbits were labeled by numbers. Each rabbits receiving both formulations after proper wash out period (7 days). Blood samples were collected from marginal ear vein at pre determined time intervals up to 24 Hrs. then blood samples were analyzed by validated high performance liquid chromatography method. Liquisolid compact exhibit c max at 212 ng/ml, t max at 1.63 Hr, AUC (0-t) at 1349 ng.min/ml, AUC (0-∞) at 1403 ng.min/ml and t 1/2 at 1.25 hr. AUC and maximum plasma concentration of the liquisolid compact is higher than pure nicardipine drug it indicates liquisolid compacts produce more bioavailability than nicardipine powder.

Material and Methods:-
Materials: Nicardipine was gifted by Natco laboratories Hyderabad, tween80, avicel pH 102 and aerosil were purchased from E.Mecrk (India), Crospovidone, Methanol for HPLC grade were purchased from SD fine chemicals (India). Administration of the dose and blood sample collection: 8 healthy rabbits were selected with the average weight of 2.5 kg to 3 kg. Two study periods are conducted on each rabbit. Between two study periods one wash out period is maintained i.e., 7 days. Equivalent to 2.5 mg of the nicardipine is taken from liquisolid compact powder and it is dispersed in 0.25% carboxy methyl cellulose. Then drug solution administered through oral feeding tube (Nanda gopal anitha et al., 2014). Then at predetermined time intervals blood samples were collected up to 24 hrs from marginal ear vein at 0.0, 0.25, 0.50, 1.00, 1.50, 2.00, 2.50, 3.00, 6.00, 12.00 and 24.00 Hrs. blood samples were collected in heparin contain test tubes. Then separation of plasma done by centrifugation process at 5000 rpm for 5min and stored under frozen condition till the analysis was performed.
Sample preparation: 0.5 ml plasma sample is transferred to 2 ml of test tube then 10 mcg/ml of di ethyl stelbesterol was added and centrifuged then supernatant was removed. 200 L of methanol was added and mix well then centrifuge for 5 min for separation of phases then evaporate at room temperature. Then again 200 L of mobile phase was added then 10L solution is injected to HPLC.

Pharmacokinetic of nicardipine:-
The individual plasma concentrations of test and reference products in each subject were given in Table 4 and 5.
Individual pharmacokinetics parameters of test and reference product in each subject was given in table 6 and 7 .The plots of comparative mean plasma concentrations of test and reference products in Rabbit were shown in figure 2.
The mean peak plasma concentration of test (T) formulation C max 212.25 ng/ml was gradually reached in 1.63 hr. In case of conventional reference formulation (R) the C max was 125.25ng/ml. It takes time 1.8 hr. The C max of the Test formulation (T) was higher when compared with Reference (R) formulation. The lower in T max of test formulation (1.63) was clearly indicating the drug shown quicker on set action when compared to reference product. The AUC 0-t of the reference (R) was found to be 1017.65ng.min/ml. The increase in AUC 0-t was observed in the test (T) formulation, which was around 1348.95ng.min/ml. This clearly indicates the drug shown higher bio-availability than reference formulation.

Conclusion:-
From the above study it was concluded that, the test product Nicardipine Liquid compacts was increases bioavailability with reference product of Nicardipine marketed formulation.