PREPARATION AND EVALUATION OF CONTROLLED RELEASE FLOATING MICROSPHERES OF REPAGLINIDE: OPTIMIZATION AND IN-VITRO STUDIES
DOI:
https://doi.org/10.22159/ajpcr.2017.v10i3.15310Abstract
ABSTRACT
Objective: To develop and evaluate floating microspheres of repaglinide (RG).
Materials and Methods: RG loaded noneffervescent microspheres of different ratios of ethylcellulose (EC) and hydroxypropyl methylcellulose (HPMC
K4M) were prepared using polyvinyl alcohol as emulsifier by solvent evaporation technique. Various process variables such as polymer ratio, stirring
speed, concentration of drug, and emulsifying agent were studied. Compatibility of drug and polymers was studied by Fourier-transform infrared
spectroscopy (FTIR). Characterization, in-vitro evaluation, and kinetic studies were performed.
Results: FTIR spectra have revealed no drug-excipient incompatibility. The average particle size of microspheres was in the range of 312-359 μm. The
results showed that floating microspheres were successfully prepared with good yield (56.15-64.3%), high entrapment efficiency (58.22-70.14%),
and good floating behavior (63.1-76.2%), respectively. In-vitro release data indicates appreciable amount of drug is released (62.28-73.27%) from the
microspheres in gastric fluid. The mechanism of drug release founds to follow first order kinetics (r2=0.986).
Conclusion: The developed floating microspheres of RG may be used for prolonged drug release for at least 12 hrs, thereby improving bioavailability
and patient compliance.
Keywords: Repaglinide, Compatibility, Kinetic, Ethylcellulose.
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Table 2: Results of micromeritics properties
Batch code
Mean particle size
Bulk density
Tapped density
Angle of repose
C1
±11.2
68±0.24
84±0.12
81±1.11°
C2
±24.0
67±0.48
85±0.47
57±1.82°
C3
±24.2
66±0.54
84±0.34
34±2.11º
C4
±77.2
67±0.31
83±0.25
85±2.84°
C5
±92.1
70±0.36
87±0.21
23±1.54°
C6
±110.5
68±0.41
86±0.38
97±1.27°
C7
±82.3
69±0.48
87±0.35
72±3.01°
C8
±93.5
65±0.21
84±0.65
12±0.87°
C9
±72.7
64±0.45
86±0.31
65±2.51°
Fig. 4: Effect of emulsifier concentration on various optimization parameters. All data are represented as mean±standard deviation (n=3)
Fig. 5: First order plot of optimized formulation (C2)
Asian J Pharm Clin Res, Vol 10, Issue 3, 2017, 103-107
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