Optimization of a metformin effervescent floating tablet containing hydroxypropylmethylcellulose and stearic acid.
This study optimizes the composition of an effervescent floating tablet (EFT) containing metformin hydrochloride (M) regarding tablet hardness (H), time to dissolve 60% of the embedded drug (t60%), and buoyancy, the floating lag time (FLT). A simplex lattice experimental design has been used comprising different levels of hydroxypropylmethylcellulose (HPMC), stearic acid (SA), sodium bicarbonate (SB) as tablet matrix components, and hardness (H), t60%, FLT as response variables. Two models have been applied to decide which composition will result in Fickian diffusion or in overlapping of two dissolution mechanisms, diffusion and matrix erosion. Three of EFT showed the two dissolution mechanisms but most of EFT showed Fickian diffusion only. Checking the experimental response by a linear, quadratic, special cubic and cubic model using multivariate regression analysis resulted in best fit for the cubic model. Overlaying the results for the cubic model under constraints defined shows the domain of accepted values of response variables. The optimized EFT shall have been included HPMC between 15.6% and 24.2%, SA between 12.8 and 15.6% and SB between 16.1% and 17.5%. The result of this study has been critically evaluated considering analogous EFT described in literature.
Rajab
M
M
Faculty of Pharmacy, Arab International University, Ghabaghib, Daraa, Syrian Arab Republic.
Jouma
M
M
Neubert
R H
RH
Dittgen
M
M
D002152:Calorimetry, Differential Scanning; D004339:Drug Compounding; D005079:Excipients; D006245:Hardness Tests; D007004:Hypoglycemic Agents / Q000008:administration & dosage* / Q000737:chemistry; D065347:Hypromellose Derivatives; D007700:Kinetics; D007785:Lactose / Q000737:chemistry; D008687:Metformin / Q000008:administration & dosage* / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D011208:Powders; D012044:Regression Analysis; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013229:Stearic Acids / Q000737:chemistry*; D013607:Tablets
D005079:Excipients; D007004:Hypoglycemic Agents; D011208:Powders; D013229:Stearic Acids; D013607:Tablets; D065347:Hypromellose Derivatives; C031183:stearic acid; D008747:Methylcellulose; D008687:Metformin; D007785:Lactose