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Design and in vitro and in vivo evaluation of mucoadhesive microcapsules of glipizide for oral controlled release: A technical note 总被引:2,自引:0,他引:2
Conclussion Thus, large spherical microcapsules with a coat consisting of alginate and a mucoadhesive polymer (sodium CMC, methylcellulose,
Carbopol, or HPMC) could be prepared by an orifice-ionic gelation process. The microcapsules exhibited good mucoadhesive properties
in an in vitro test. Glipizide release from these mucoadhesive microcapsules was slow and extended over longer periods of
time and depended on composition of the coat. Drug release was diffusion controlled and followed zero-order kinetics after
a lag, period of 1 hour. In the in vivo evaluation, alginate-Carbopol microcapsules could sustain the hypoglycemic effect
of glipizide over a 14-hour period. These mucoadhesive microcapsules are, thus, suitable for oral controlled release of glipizide. 相似文献
2.
The purpose of this research was to formulate and system-atically evaluate in vitro and in vivo performances of mucoadhesive
microspheres of glipizide. Glipizide microspheres containing chitosan were prepared by simple emulsification phase separation
technique using glutaraldehyde as a cross-linking agent. Results of preliminary trials indicate that volume of cross-linking
agent, time for cross-linking, polymer-to-drug ratio, and speed of rotation affected characteristics of microspheres. Microspheres
were discrete, spherical, and free flowing. The microspheres exhibited good mucoadhesive property in the in vitro wash-off
test and also showed a high percentage drug entrapment efficiency. A 32 full factorial design was employed to study the effect of independent variables, polymer-to-drug ratio (X
1), and stirring speed (X
2) on dependent variables percentage mucoadhesion, t80, drug entrapment efficiency, and swelling index. The best batch exhibited a high drug entrapment efficiency of 75% and a
swelling index of 1.42; percentage mucoadhesion after 1 hour was 78%. The drug release was also sustained for more than 12
hours. The polymer-to-drug ratio had a more significant effect on the dependent variables. In vivo testing of the mucoadhesive
microspheres to albino Wistar rats demonstrated significant hypoglycemic effect of glipizide. 相似文献
3.
Depending on the dose size and solubility characteristics of low solubility drugs, a meaningful and discriminatory power of
dissolution rate testing can be demonstrated. Saturation solubility of fenofibrate and glipizide in different media were determined.
Solubility of fenofibrate increased directly with SLS concentration. For a 54-mg fenofibrate tablet, SLS at 0.025 M level
is required for a discriminative dissolution test, while for 160-mg tablet, dissolution condition and levels of SLS should
be optimized; higher concentrations may be effective (ie, 0.052 M, ∼1.5%). A pH 6.8 phosphate buffer medium is appropriate
for glipizide 10-mg tablet dissolution study, when formulation ingredients include excipients with surface activity (eg, HPMC). 相似文献
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