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.

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.

Insulin-Containing oral time-dependent colon delivery system (Chronotopic) : evaluation of feasibility, in vitro release performances and stability

M. Serratoni
Primo
;
A. Maroni
Secondo
;
A. Gazzaniga
Penultimo
;
M.E. Sangalli
Ultimo
2006

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.
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
2006
http://www.aapspharmaceutica.com/search/abstract_view.asp?id=936&ct=06Abstracts
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/26452
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