In the present work, the possibility of manufacturing by injection molding (IM) a gastro-resistant capsular device based on hydroxypropyl methyl cellulose acetate succinate (HPMCAS) was investigated. By performing as an enteric soluble container, such a device may provide a basis for the development of advantageous alternatives to coated dosage forms. Preliminarily, the processability of the selected thermoplastic polymer was evaluated, and the need for a plasticizer (polyethylene glycol 1500) in order to counterbalance the glassy nature of the molded items was assessed. However, some critical issues related to the physical/mechanical stability (shrinkage and warpage) and opening time of the device after the pH change were highlighted. Accordingly, an in-depth formulation study was carried out taking into account differing release modifiers potentially useful for enhancing the dissolution/disintegration rate of the capsular device at intestinal pH values. Capsule prototypes with thickness of 600 and 900 μm containing Kollicoat® IR and/or Explotab® CLV could be manufactured, and a promising performance was achieved with appropriate gastric resistance in pH 1.2 medium and break-up in pH 6.8 within 1 h. These results would support the design of a dedicated mold for the development of a scalable manufacturing process.

Gastroresistant capsular device prepared by injection molding / L. Zema, G. Loreti, A. Melocchi, A. Maroni, L. Palugan, A. Gazzaniga. - In: INTERNATIONAL JOURNAL OF PHARMACEUTICS. - ISSN 0378-5173. - 440:2(2013 Jan), pp. 264-272. [10.1016/j.ijpharm.2012.05.071]

Gastroresistant capsular device prepared by injection molding

L. Zema
Primo
;
G. Loreti
Secondo
;
A. Melocchi;A. Maroni;L. Palugan
Penultimo
;
A. Gazzaniga
Ultimo
2013-01

Abstract

In the present work, the possibility of manufacturing by injection molding (IM) a gastro-resistant capsular device based on hydroxypropyl methyl cellulose acetate succinate (HPMCAS) was investigated. By performing as an enteric soluble container, such a device may provide a basis for the development of advantageous alternatives to coated dosage forms. Preliminarily, the processability of the selected thermoplastic polymer was evaluated, and the need for a plasticizer (polyethylene glycol 1500) in order to counterbalance the glassy nature of the molded items was assessed. However, some critical issues related to the physical/mechanical stability (shrinkage and warpage) and opening time of the device after the pH change were highlighted. Accordingly, an in-depth formulation study was carried out taking into account differing release modifiers potentially useful for enhancing the dissolution/disintegration rate of the capsular device at intestinal pH values. Capsule prototypes with thickness of 600 and 900 μm containing Kollicoat® IR and/or Explotab® CLV could be manufactured, and a promising performance was achieved with appropriate gastric resistance in pH 1.2 medium and break-up in pH 6.8 within 1 h. These results would support the design of a dedicated mold for the development of a scalable manufacturing process.
Injection molding (IM); Micromolding; Capsular device; Gastric resistance; Enteric polymer; Hydroxypropyl methyl cellulose acetate succinate (HPMCAS)
Settore CHIM/09 - Farmaceutico Tecnologico Applicativo
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/175414
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