Gastroretentive Cosolvent-Based In Situ Gel as a Promising Approach for Simultaneous Extended Delivery and Enhanced Bioavailability of Mitiglinide Calcium
| Autor: | Aliaa Nabil ElMeshad, Dina B. Mahmoud, Marwa Hassan Shukr |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Drug
In situ Alginates media_common.quotation_subject Pharmaceutical Science Biological Availability 02 engineering and technology Isoindoles 030226 pharmacology & pharmacy Polyvinyl alcohol 03 medical and health sciences chemistry.chemical_compound Viscosity 0302 clinical medicine Animals Hypoglycemic Agents media_common Chromatography Chemistry Polysaccharides Bacterial 021001 nanoscience & nanotechnology Controlled release Gellan gum Bioavailability Drug Liberation Delayed-Action Preparations Drug delivery Rabbits 0210 nano-technology Gels |
| Zdroj: | Journal of pharmaceutical sciences. 108(2) |
| ISSN: | 1520-6017 |
| Popis: | Ion cross-linking in situ gels are novel liquid sustained-release drug delivery systems. These systems are unsuitable for poorly water-soluble drugs such as the novel antidiabetic drug mitiglinide calcium (MTG). Thus, our goal was to assess the possibility of using cosolvency approach in formulating gastroretentive in situ gel of the short half-life MTG to simultaneously enhance its bioavailability and sustain its release. MTG in situ gel formulations were developed using propylene glycol as a cosolvent to dissolve MTG in the polymer solution, followed by characterization of viscosity, gel strength, floating ability, and in vitro MTG release and phramacokinetics evaluation. The optimized formulation (composition: 1% gellan gum, 0.75% sodium alginate, 0.75% calcium carbonate, and 7.5% propylene glycol) exhibited reasonable viscosity but on introduction into simulated gastric fluid, it formed firm gel that floated within seconds over the surface and remained buoyant for 24 h. The formula exhibited in vivo sustained release manner of MTG over 24 h and improved the bioavailability of the drug. Thus, cosolvency presents a promising approach to deliver hydrophobic drugs in sustained-release liquid formulations. These formulations will improve diabetic patients' compliance by eliminating the necessity of frequent dosing with a better disease management. |
| Databáze: | OpenAIRE |
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