methylcellulose and aceclofenac

The purpose of this study was to develop a once daily sustained release tablet of aceclofenac using chitosan and an enteric coating polymer (hydroxypropyl methylcellulose phthalate or cellulose acetate phthalate). Overall sustained release for 24 h was achieved by preparing a double-layer tablet in which the immediate release layer was formulated for a prompt release of the drug and the sustained release layer was designed to achieve a prolonged release of drug. The preformulation studies like IR spectroscopic and differential scanning calorimetry showed the absence of drug-excipient interactions. The tablets were found within the permissible limits for various physicochemical parameters. Scanning electron microscopy was used to visualize the surface morphology of the tablets and to confirm drug release mechanisms. Good equivalence in the drug release profile was observed when drug release pattern of the tablet containing chitosan and hydroxypropyl methylcellulose phthalate (M-7) was compared with that of marketed tablet. The optimized tablets were stable at accelerated storage conditions for 6 months with respect to drug content and physical appearance. The results of pharmacokinetic studies in human volunteers showed that the optimized tablet (M-7) exhibited no difference in the in vivo drug release in comparison with marketed tablet. No significant difference between the values of pharmacokinetic parameters of M-7 and marketed tablets was observed (p > 0.05; 95% confidence intervals). However the clinical studies in large scale and, long term and extensive stability studies at different conditions are required to confirm these results.

Topics: Administration, Oral; Anti-Inflammatory Agents, Non-Steroidal; Calorimetry, Differential Scanning; Cellulose; Chemistry, Pharmaceutical; Chitosan; Cross-Over Studies; Delayed-Action Preparations; Diclofenac; Double-Blind Method; Drug Administration Schedule; Drug Carriers; Drug Compounding; Drug Stability; Humans; Hydrogen-Ion Concentration; Methylcellulose; Microscopy, Electron, Scanning; Solubility; Spectrophotometry, Infrared; Surface Properties; Tablets, Enteric-Coated; Technology, Pharmaceutical; Therapeutic Equivalency

The objective of the present study was to develop bilayer tablets of aceclofenac that are characterized by initial burst drug release followed by sustained release of drug.. The fast-release layer of the bilayer tablet was formulated using microcrystaline cellulose (MCC) and HPMC K4M. The amount of HPMC E4M (X(1)) and MCC (X(2)) was used as independent variables for optimization of sustained release formulation applying 3(2) factorial design. Three dependent variables were considered: percentage of aceclofenac release at 1 h, percentage of aceclofenac release at 12 h, and time to release 50% of drug (t(50%)). The composition of optimum formulation of sustained release tablets were employed to formulate double layer tablets.. The results indicate that X(1) and X(2) significantly affected the release properties of aceclofenac from sustained release formulation. The double layer tablets containing fast-release layer showed an initial burst drug release of more than 30% of its drug content during first 1 h followed by sustained release of the drug for a period of 24 h.. The double layer tablets for aceclofenac can be successfully employed as once-a-day oral-controlled release drug delivery system characterized by initial burst release of aceclofenac for providing the loading dose of drug.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Cellulose; Chemistry, Pharmaceutical; Delayed-Action Preparations; Diclofenac; Drug Delivery Systems; Lactose; Methylcellulose; Solubility; Tablets

Aceclofenac is a new generation non-steroidal anti-inflammatory drug showing effective anti-inflammatory and analgesic properties. It is available in the form of tablets of 100 mg. Importance of aceclofenac as a NSAID has inspired development of topical dosage forms. This mode of administration may help avoid typical side effects associated with oral administration of NSAIDs, which have led to its withdrawal. Furthermore, aceclofenac topical dosage forms can be used as a supplement to oral therapy for better treatment of conditions such as arthritis. Ointments, creams, and gels containing 1% (m/m) aceclofenac have been prepared. They were tested for physical appearance, pH, spreadability, extrudability, drug content uniformity, in vitro diffusion and in vitro permeation. Gels prepared using Carbopol 940 (AF2, AF3) and macrogol bases (AF7) were selected after the analysis of the results. They were evaluated for acute skin irritancy, anti-inflammatory and analgesic effects using the carrageenan-induced thermal hyperalgesia and paw edema method. AF2 was shown to be significantly (p < 0.05) more effective in inhibiting hyperalgesia associated with inflammation, compared to AF3 and AF7. Hence, AF2 may be suggested as an alternative to oral preparations.

Topics: Acrylic Resins; Administration, Topical; Animals; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Diclofenac; Edema; Gels; Hyperalgesia; Hypromellose Derivatives; Inflammation; Male; Methylcellulose; Ointments; Polyethylene Glycols; Rabbits; Rats; Rats, Wistar; Skin Irritancy Tests; Solubility

The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.

Topics: Chemistry, Pharmaceutical; Delayed-Action Preparations; Diclofenac; Hypromellose Derivatives; Methylcellulose; Solubility; Tablets; Verapamil; Water