Effect of poloxamer on the dissolution of felodipine and preparation of controlled release matrix tablets containing felodipine

Abstract

The effects of poloxamer and HPMC on the dissolution rate of felodipine were investigated and a felodipine controlled release tablet was developed by increasing the water solubility of felodipine and using swelling polymer to control release rate. Milling of felodipine slightly increased the dissolution rate of felodipine when compared with physical mixture. XRD results indicated that felodipine remained in the crystalline form even after co-milling with poloxamer. Improved dissolution rates after co-milling with HPMC and poloxamer were due to both solubilization effect of polymer and milling. The effect of poloxamer on dissolution rate was more significant than that of HPMC. Based on increased solubility of felodipine in the presence of poloxamer, it was concluded that the improved dissolution rate of felodipine was mainly due to a high local concentration of poloxamer around felodipine. Controlled release felodipine tablets were prepared using poloxamer as a solubilizing agent and Carbopol as a controlled release matrix.

Application of Pharmaceutical QbD for Enhancement of the Solubility and Dissolution of a Class II BCS Drug using Polymeric Surfactants and Crystallization Inhibitors: Development of Controlled-Release Tablets

“…It is obvious that CR-10 showed the highest drug release (t 75% =5.85 h). This observation confirms that the prolongation of the release time might be due to an interaction between Pluronic® F-127, Carbopol® 974, and HPMC which retards the disintegration of the tablet matrix (4). It was reported that the release of drug from HPMC/Carbopol® 974 may be hindered due to a 3D network like structure formed by interpolymer complexation following the penetration of dissolution medium into the tablet.…”

“…It is used for treatment of chronic hypertension. Increasing the solubility of the sparingly water soluble drug and controlling its release rate from the product is critical during the development of a controlled-release (CR) tablet (4). Several formulation techniques have been used to improve dissolution rate of felodipine such as micronization (5), solid dispersion (6)(7)(8), and co-grinding (9).…”

“…Several formulation techniques have been used to improve dissolution rate of felodipine such as micronization (5), solid dispersion (6)(7)(8), and co-grinding (9). However, these techniques suffer from problems that prevent its commercial use such as physical instabilities, limited improvement of dissolution, and crystallization from the supersaturated solution generated by dissolution of the amorphous drug (4,6,10,11).…”

Enhancement of solubility and dissolution of Coenzyme Q10 using solid dispersion formulation

“…1, increasing the proportion of poloxamer 407 in the physical mixtures did not increase the solubility of CoQ 10 significantly. The critical micelle concentration of poloxamer 407 was found to be 0.0076% (w/v) at 37 • C and 0.18% (w/v) at room temperature (Lee et al, 2008). Hence, the amount of poloxamer 407 in all physical mixtures, subjected for solubility test in the present study, was above critical micelle concentration.…”

Quality-by-Design Case Study: Investigation of the Role of Poloxamer in Immediate-Release Tablets by Experimental Design and Multivariate Data Analysis

“…This combinatorial approach has only been explored by a few in the area of pharmaceutical and product development (7)(8)(9)(10)(11)(12)(13)(14) Surfactants used in tablet formulations usually tend to increase dissolution by promoting hydrophilicity within the tablet matrix and increased active pharmaceutical ingredient (API) solublization (15,16). Illustrated by example in this paper is the opposite effect, i.e., presence of a surfactant poloxamer 188 retarded tablet dissolution.…”