Sodium alginate microspheres containing multicomponent inclusion complex of domperidone
Sodium alginate microspheres of domperidone for intranasal systemic delivery were developed to eliminate first pass metabolism, improve patient compliance and obtain improved therapeutic efficacy in treatment of migraine, gastro-esophageal reflux and chemotherapy induced nausea and vomiting. Domp...
Guardado en:
| Autores principales: | , , , |
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| Formato: | Articulo |
| Lenguaje: | Inglés |
| Publicado: |
2010
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| Materias: | |
| Acceso en línea: | http://sedici.unlp.edu.ar/handle/10915/8049 http://www.latamjpharm.org/resumenes/29/7/LAJOP_29_7_1_22.pdf |
| Aporte de: |
| Sumario: | Sodium alginate microspheres of domperidone for intranasal systemic delivery were developed
to eliminate first pass metabolism, improve patient compliance and obtain improved therapeutic efficacy
in treatment of migraine, gastro-esophageal reflux and chemotherapy induced nausea and vomiting.
Domperidone was encapsulated as ternary inclusion complex with β-cyclodextrin and citric acid to improve
solubility. The phase solubility studies were performed in order to select suitable acid and ternary
inclusion complex was prepared by kneading method. The complex was characterized by differential scanning
calorimetry, X-ray diffraction and Fourier transform infrared spectroscopy. In vitro dissolution
study was carried out in simulated nasal electrolyte solution, pH 6.4. The microspheres of optimised
ternary inclusion complex were prepared by emulsification-cross-linking method and were evaluated for
particle size, encapsulation efficiency, equilibrium swelling degree, in vitro mucoadhesion and in vitro drug
release. The effect of various formulation variables such as drug loading, polymer concentration, crosslinking
agent concentration and cross-linking time on microsphere characteristics were studied. The microspheres
size range was 57.63-65.3 µm, whereas the percentage drug encapsulation was within the range
15-50 %. All microspheres showed good bioadhesive properties. The formulation variables influenced the
drug release profile. The treatment of in vitro release kinetics with kinetic equations indicated that the
domperidone release followed Higuchi's matrix model. |
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