Gastroresistant capsular device prepared by injection molding.
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 1h. These results would support the design of a dedicated mold for the development of a scalable manufacturing process.
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, via G Colombo 71, 20133 Milano, Italy.
Lucia
L
Zema
Giulia
G
Loreti
Alice
A
Melocchi
Alessandra
A
Maroni
Luca
L
Palugan
Andrea
A
Gazzaniga
D002214:Capsules / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D010968:Plasticizers / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods*
D002214:Capsules; D003692:Delayed-Action Preparations; D010968:Plasticizers; D011108:Polymers; C048331:hydroxypropylmethylcellulose acetate succinate; D008747:Methylcellulose