Aceclofenac (AC) is a phenyl acetic acid derivative [2-(2',6'-dichlorophenyl)amino] phenylacetoxyacetic acid], a novel NSAID indicated for the symptomatic treatment of pain and inflammation (1). The short biological half-life (about 4 h) and high frequency of dosing make aceclofenac an ideal candidate for sustained release. The bioadhesive microspheres of aceclofenac would prolong the residence time at the absorption site to facilitate intimate contact with the absorption surface and thereby improve and enhance bioavailability and increase patient compliance. Natural hydrophilic polymers like alginate and pectin are widely used in numerous biomedical applications for their bioadhesion properties. Alginic acid and pectin are natural polysaccharides that are widely Ionotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigated in vitro for possible sustained drug release and their use in vivo as a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.
The present review article aims at determining the various possible techniques available to enhance the quality, safety and efficacy of pharmaceutical formulations by exploring most suitable and practically applicable experimental designs and optimization techniques. As we know that pharmaceutical industries are constantly in search of novel ideas to improve quality by various optimization techniques, hence in present review article we shall discuss latest optimization techniques and experimental designs to achieve the best combination of product and process characteristics under the given set of conditions. Experimental designs and optimization techniques are the tools that are simultaneously and systematically used to identify various types of problems that may influence research, development and production of pharmaceutical formulations. These are organized an approach to determine the relationship between the factors affecting a process and the output of that process. The screening methods discussed here include factorial design, fractional factorial designs, full factorial design, mixture designs etc. Recently, different software has been used in implementing optimization techniques in pharmaceutical products to enhance product quality by using most suitable available facilities.
Objective: To develop an innovative, rapid, simple, cost effective, stability indicating reverse phase-high performance liquid chromatography (RP-HPLC) method for simultaneous estimation of ledipasvir (LP) and sofosbuvir (SB) in combination pill dosage form. Methods: The method was developed using C8 column, 250 mm x 4.6 mm, 5mm using mobile section comprising of 0.1% (v/v) orthophosphoric acid buffer at pH 2.2 and acetonitrile in the ratio of 45:55 that was pumped through the column at a flow rate of 0.8 ml/min. Temperature was maintained at 30 °C, the effluents were monitored at 260 nm with the help of usage of PDA detector. Results: The retention time of LP and SB were found to be 2.246 min and 3.502 min. The approach was found to be linear with the variety of 9-36 µg/ml and 40-240 μg/ml for LP and SB respectively, the assay of estimated compounds were found to be 99.65% and 99.73% w/v for LP and SB respectively. Conclusion: The pressured samples changed into analyzed and this proposed a technique turned into determined to be particular and stability indicating as no interfering peaks of decay compound and excipients were observed. Hence, the approach was easy and economical that may be efficiently applied for simultaneous estimation of both LP and SB in bulk and combination tablet system.
An innovative high‐performance liquid chromatography assay method was developed and validated for quantification of dextromethorphan hydrobromide and desloratadine simultaneously in monophasic liquid formulation by preparing syrup containing 30 mg/5 mL of dextromethorphan hydrobromide and 1.2 mg/mL of desloratadine. The chromatographic severance was executed by gradient solution A and B. The composition of buffer solution A contained 0.05 M monobasic potassium, then 1 mL triethylamine was added to it and the pH was adjusted to 2.3 with orthophosphoric acid. Methanol was used as solution B. The gradient elution was executed with Kromasil C8 (250 mm × 4.6 mm) column having 1.5 mL/min flow rate and 20 µL injection volume with UV‐estimation at 254 nm for dextromethorphan hydrobromide and DES. The present research was planned according to Box‐Behnken design by utilizing design expert software, using four factors such as column temperature (A), flow rate (B), mobile phase–organic phase (C), and pH (D); correspondingly the selected response variables were resolution between A and B, that is, desloratadine and methyl paraben (Y1), tailing of dextromethorphan hydrobromide (Y2), and tailing of desloratadine (Y3). The parameters such as system suitability, linearity, accuracy, precision, robustness, limit of detection, limit of quantitation, and ruggedness were analyzed to validate the developed method in accordance with current regulatory guidelines.
Quazi et al.: Fabrication and Characterization of Optimized Aceclofenac Loaded MicrospheresThe optimized microspheres were fabricated as a controlled release system for aceclofenac incorporating polymeric cross-linking with sodium alginate as natural, hydrophilic polymer and Eudragit RS100 synthetic, hydrophobic polymer by ion-gelation technique. The method was optimized by Box Behnken design incorporating concentration of pure drug, natural and synthetic polymer along with the obtained responses that were mean particle size (Y1) and entrapment efficiency of drug (Y2). Microspheres were characterized for percentage yield, micromeritic evaluation, particle size, entrapment efficiency of drug, in vitro study, fourier transform infrared spectroscopy, scanning electron microscopy, nuclear magnetic resonance and high performance liquid chromatography quantification of optimized formulation. It was observed that application of response surface method software for Box Behnken design yielded stable and spherical microspheres with mean particle size 69.37 µm and entrapment efficiency of drug 79.86 % for the most optimized formulation F5. We can conclude that bridging of aceclofenac with natural and synthetic polymers yielded stable, cost effective microspheres bearing enhanced micromeritic properties with controlled release effect.
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