Dissolution kinetics and physical characterization of three-layered tablet with poly(ethylene oxide) core matrix capped by Carbopol.
We have prepared poly(ethylene oxide) (PEO) tablets which have three-layered structure by direct compression. Carbopol (CP) was coated on both sides of the central PEO matrix which contains solid-dispersed nifedipine (NP) in PEG4000. For comparison, physical mixture of PEO with poly(ethylene glycol 4000) (PEG4000) solid dispersion was also prepared. The differential scanning calorimetry (DSC) thermogram and X-ray diffraction (XRD) pattern obtained after 4 weeks of storage indicated that the crystallinity of PEG4000 in solid dispersion only slightly increased upon aging during this storage period. The formation of crystalline domain of NP, PEO or sodium dodecyl sulfate (SDS) was not observed. CP layers decreased the surface area exposed to dissolution medium, and after swelling, they also covered the exposed side area of the tablet. It seems that swelling and morphological change of CP layers minimize the erosional release for rapidly erodible PEO200K (Mw 200,000) and change the NP release to a diffusion-controlled process. For PEO900K (Mw 900,000), initial release rate was slower than that of PEO200K, possibly due to the slower swelling and erosional release from the side of the tablet. Diffusional release seemed to be the dominating mechanism for the release of NP from PEO7000K (Mw 7,000,000) tablet. Physical mixture of PEO and CP delayed the release of NP remarkably. The increase in pH, ionic strength and buffer concentration of the dissolution medium decreased the release rate. The data obtained for capped and blended tablets were fitted using the power law equation to understand the release mechanism. These results provided some useful information on parameters which can be modulated in the design of a controlled release dosage form for NP.
Hong
Sung In
SI
College of Pharmacy, Sookmyung Women's University, Chungpa-dong 2-ga, Yongsan-gu, Seoul 140-742, South Korea.
Oh
Seaung Youl
SY
D000180:Acrylic Resins; D002121:Calcium Channel Blockers / Q000008:administration & dosage* / Q000737:chemistry; D003460:Crystallization; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry; D004356:Drug Storage; D006863:Hydrogen-Ion Concentration; D009543:Nifedipine / Q000008:administration & dosage* / Q000737:chemistry; D009994:Osmolar Concentration; D011092:Polyethylene Glycols / Q000737:chemistry*; D011145:Polyvinyls / Q000737:chemistry*; D012967:Sodium Dodecyl Sulfate / Q000737:chemistry; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013607:Tablets
D000180:Acrylic Resins; D002121:Calcium Channel Blockers; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D011145:Polyvinyls; D013501:Surface-Active Agents; D013607:Tablets; C006912:carboxypolymethylene; D012967:Sodium Dodecyl Sulfate; D011092:Polyethylene Glycols; D009543:Nifedipine