Insulin-Containing oral time-dependent colon delivery system (Chronotopic) : evaluation of feasibility, in vitro release performances and stability
Articolo
Data di Pubblicazione:
2006
Citazione:
Insulin-Containing oral time-dependent colon delivery system (Chronotopic) : evaluation of feasibility, in vitro release performances and stability / M. Serratoni, A. Maroni, S. De Luigi Bruschi, F. Giordano, A. Gazzaniga, M.E. Sangalli. - In: THE AAPS JOURNAL. - ISSN 1550-7416. - 8:S2(2006), pp. T3187-T3187.
Abstract:
Purpose.
To investigate the preparation, in vitro performances and stability of a previously proposed oral time-dependent device for
colon delivery containing insulin. The system under investigation consists of a drug-containing core and a release-delaying
hydroxypropyl methylcellulose (HPMC) layer. An outer enteric film would also be required to target the colon according to
the time-based approach.
Methods.
Immediate release tablets (diameter: 5mm, 80mg) containing 2 mg of bovine insulin (57.6 IU) were coated up to 800 μm in a
top-spray fluid bed (temperature of fluidized cores: 36-38°C) with HPMC 2910 in 8.0% w/v aqueous solution. For stability
studies, insulin specimens, powder mixture samples, tablet cores and HPMC-coated systems were stored at 4°C or 25°C and
60% RH. Assays were performed monthly by HPLC according to Ph. Eur. 5th Ed methods. Release tests (n=3) were carried
out in phosphate buffer pH 6.8 at 37±0.5°C.
Results.
There was no evidence of chemical degradation for insulin either in physical mixture or after tableting during one-year
storage at 4°C. Notably, the aqueous coating process seemed not to impact on the peptide stability. Differently from samples
stored at 4°C, those kept at 25°C and 60% RH showed an approximately 50% decrease in the drug content, which was even
more marked for uncoated cores. Moreover, in vitro release performances, which were characterized by the pursued lag phase
followed by a prompt release of insulin, appeared unchanged throughout the whole 4°C storage period.
Conclusion.
A time-dependent oral insulin delivery system was prepared and evaluated. Neither the manufacturing process nor storage at
4°C for one year showed to impair the drug stability. Delayed release of the model peptide was achieved through the abovedescribed
drug delivery platform, thus potentially meeting the requirements of time-based colon targeting.
Tipologia IRIS:
01 - Articolo su periodico
Elenco autori:
M. Serratoni, A. Maroni, S. De Luigi Bruschi, F. Giordano, A. Gazzaniga, M.E. Sangalli
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