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Development and in-vivo evaluation of dry powders for reconstitution of solubility enhanced derivative of azithromycin dihydrate
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| Author:
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SRAVYA MADDUKURI, RADHA GV
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| Abstract:
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The objective of this work was to formulate an antibiotic dry syrup, which would show improved physical and
chemical stability during its intended shelf life. Antibiotic azithromycin dihydrate, used to treat bacterial infections,
is not soluble and stable in water. Hence, pediatric oral powders for suspensions are available which are merely
stable only for 5 days after reconstitution. Solubility of azithromycin dihydrate was first improved by solid
dispersions, inclusion complexation and nanosuspensions and then used the same in dry syrups. By this, solubility,
stability could be improved, and taste masking could be achieved. Solubility enhancement was carried out through
use of poloxamer 188, poloxamer 407 and polyethylene glycol 20,000 as carriers in two different concentrations
and two methods- solvent evaporation and freeze drying. Similarly, Inclusion complexation using ß-cyclodextrin,
epichlorohydrin- ß-cyclodextrin and sulfobutyl ether cyclodextrin was attempted using solvent evaporation and
freeze drying. Nanosuspensions were also prepared using poloxamers and PVP, by nanoprecipitation technique and
nanoprecipitation with cryoprotectants. All the solid dispersions, inclusion complexes and nanosuspensions were
characterised using In-Vitro dissolution profiles, kinetic modelling, X ray diffractometry and SEM images. In vitro
dissolution profile data suggested a significant improvement in drug release with inclusion complexes using
sulfobutyl ether cyclodextrin, prepared by freeze drying and nanosuspensions using poloxamer 188, prepared by
nanoprecipitation with cryoprotectants. X ray diffractograms showed a reduction in crystallinity. Kinetic modelling
suggested a zero-order release mechanism. Hence, 2 inclusion complexes and 2 nanosuspensions were used to
formulate dry syrups using Viscarin ph 209 and Gelcarin ph 812 as suspending agents. Powdered dry syrups were
evaluated before reconstitution for their flow properties, and results showed excellent flow properties. Post
reconstitution evaluation results also suggested a stable, flocculated oral suspension with sedimentation volume
closer to 1 over tested period.
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| Keyword:
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Dry syrups, Reconstituted Suspensions, Inclusion complexation, Nanoparticles, Poloxamer.
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2019.11.03.069
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| Download:
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