full issue - Association of Biotechnology and Pharmacy
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Current Trends in <strong>Biotechnology</strong> <strong>and</strong> <strong>Pharmacy</strong>Vol. 5 (2) 1110-1122 April 2011. ISSN 0973-8916 (Print), 2230-7303 (Online)1117emulsions. The formulations C4, C14 <strong>and</strong> C17did not show any kind <strong>of</strong> crystallinity whichsuggests that the drug molecules were inamorphous state. But in case <strong>of</strong> formulation C7two peaks appeared in right angles. This may bedue to the re-crystallization <strong>of</strong> the drug. Theresults were shown in Fig.3.Transmission electron microscopy:Transmission electron microscopic studies werecarried out for the formulation C14 to observethe physical properties <strong>of</strong> NE droplets.Transmission electron micrographs revealed thatthe droplets were spherical, homogeneous <strong>and</strong>no signs <strong>of</strong> precipitation. The droplet size wascorrelated with the results from particle sizeanalysis using zeta sizer. All these results werepresented in Fig.4.Pharmacokinetic studies: The plasmaconcentration vs time pr<strong>of</strong>iles <strong>of</strong> the carvedilolNE <strong>and</strong> carvedilol tablet suspension afteradministration <strong>of</strong> a single dose <strong>of</strong> 2.5mg/kg bodyweight were shown in Fig.5. The pharmacokinetic parameters were computed by noncompartmental analysis using winN onlines<strong>of</strong>tware <strong>and</strong> the results were summarized in theTable 3. The NE was more effective in enhancingoral absorption <strong>and</strong> availability <strong>of</strong> carvedilol in theplasma. The average plasma concentrations <strong>of</strong>carvedilol were 70.07±8.90 <strong>and</strong> 39.59±5.78 after1 hour following oral administration <strong>of</strong> NE <strong>and</strong>tablet suspension respectively. Plasmaconcentration <strong>of</strong> carvedilol when administeredwith the NE remained higher than with the tabletsuspension for up to 6hrs. Significantly higherC max, AUC <strong>and</strong> AUMC values were observed incase <strong>of</strong> NE compared to tablet suspension. MRT,T max<strong>and</strong> t 1/2values <strong>of</strong> carvedilol with NE werecomparable with that <strong>of</strong> oral tablet suspension.Mean T maxvalues were 0.5 hours in case <strong>of</strong> NE<strong>and</strong> 0.67±0.29 hours in case <strong>of</strong> tablet. There wasno significant difference in t 1/2.All these resultsFig.3. X-ray diffraction reports <strong>of</strong> st<strong>and</strong>ard drugCarvedilol <strong>and</strong> the nano emulsions (C4, C7, C14<strong>and</strong> C17) loaded with carvedilol.Fig.4. Transmission electron micrographs <strong>of</strong> the formulationC14 blank (A) <strong>and</strong> carvedilol loaded (B) nanoemulsions. The scale bar represents a distance <strong>of</strong> 500nmin Picture (A), 1000 nm in picture (B).revealed that the extent <strong>of</strong> oral absorption <strong>and</strong>bioavailability <strong>of</strong> carvedilol was significantlyincreased from oral nano emulsion compared withthe tablets.DiscussionSeveral drugs <strong>and</strong> dosage forms availablefor the treatment <strong>of</strong> hypertension, the mortalityKoteswari Poluri et al