Poly(dimethylsiloxane) coatings for controlled drug release--polymer modifications.
Modifications of endhydroxylated poly(dimethylsiloxane) (PDMS) formulations were studied for their ability to be applied onto tablet cores in a spray-coating process and to control drug release in zero-order fashion. Modifications of the crosslinker from the most commonly used tetraethylorthosilicate (TEOS) to the trifunctional 3-(2,3-epoxypropoxy)propyltrimethoxysilane (SIG) and a 1:1 mixture of the two were undertaken. Addition of methylpolysiloxane-copolymers were studied. Lactose, microcrystalline cellulose (MCC) and polyethylene glycol 8000 (PEG) were the channeling agents applied. The effects on dispersion properties were characterized by particle size distribution and viscosity. Mechanical properties of resulting free films were studied to determine applicability in a pan-coating process. Release of hydrochlorothiazide (marker drug) was studied from tablets coated in a lab-size conventional coating pan. All dispersions were found suitable for a spray-coating process. Preparation of free films showed that copolymer addition was not possible due to great decline in mechanical properties. Tablets coated with formulations containing PEG were most suitable to control drug release, at only 5% coating weight. Constant release rates could be achieved for formulations with up to 25% PEG; higher amounts resulted in a non-linear release pattern. Upon adding 50% PEG, a drug release of 63% over 24 h could be achieved.
Schulze Nahrup
J
J
Industrial Pharmacy Graduate Program, University of Cincinnati Medical Center, 3223 Eden Avenue, Cincinnati, OH 45267-0004, USA.
Gao
Z M
ZM
Mark
J E
JE
Sakr
A
A
D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003432:Cross-Linking Reagents / Q000737:chemistry; D003692:Delayed-Action Preparations; D004129:Dimethylpolysiloxanes / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry*; D006852:Hydrochlorothiazide / Q000008:administration & dosage / Q000737:chemistry; D007700:Kinetics; D007785:Lactose / Q000737:chemistry; D019563:Mechanics; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry; D012828:Silicones / Q000737:chemistry*; D013499:Surface Properties; D013997:Time Factors
D003432:Cross-Linking Reagents; D003692:Delayed-Action Preparations; D004129:Dimethylpolysiloxanes; D005079:Excipients; D012828:Silicones; D006852:Hydrochlorothiazide; D011092:Polyethylene Glycols; C013830:baysilon; D002482:Cellulose; D007785:Lactose; C109691:microcrystalline cellulose