Objective: The primary objective of the project was to formulate and evaluate hard capsule containing the solution of ibuprofen. It also included enhancement of solubility of ibuprofen in hydrophilic solvents to obtain a unit dose capsule acceptable for human consumption.
Methods: Solution of ibuprofen was developed by the salt formation of partial drug using potassium hydroxide in PEG 600 and water. The solution was encapsulated in hard capsules with band sealing. The final formulation was evaluated for uniformity of weight, disintegration, drug content and stability. The dissolution profile was compared with that of available marketed tablets and softgels.
Results: The capsules were evaluated and found compliant as per specifications mentioned in general monograph of capsules in IP 2014. The uniformity of weight of the batch of capsules was found to be 734.8 mg (±0.58). The disintegration time of these capsules was observed to be 4.45 min. The drug content was found to be 100.03% and the product is stable over three months of test period under room temperature as well as accelerated conditions. The dissolution profile showed that softgels take longer time to release the drug whereas marketed tablets showed a dissolution profile comparable with that of formulated capsules.
Conclusion: The developed capsule is a unit dose of liquid containing solubilized ibuprofen delivering the drug directly into the gastrointestinal tract (GIT). These are newer solid oral dosage forms with higher patient compliance and ease in manufacturing. They require lesser steps and manufacturing area when compared to the manufacturing of compressed tablets.
The formulation of liquid fill dispersion is an effective method of increasing the dissolution rate of poorly soluble drugs, and hence, of improving the bioavailability. The dispersion was used to prepare different dispersion of Piroxicam using triethyl citrate(TEC), acconon and polysorbate-80. The physical characteristics of the binary systems were determined Particle size analysis, Zeta potential and by HPLC. The release rate from the resulting dispersion was determined from dissolution studies by use of USP dissolution apparatus I (basket method). The dissolution rate of Piroxicam is increased in all the dispersion systems compared to that of pure drug. A liquid dispersion system of Piroxicam and triethyl citrate(TEC): acconon : polysorbate-80 blend in different ratios, was also prepared. The capsule formulation was subjected to stability studies at different temperature and humidity conditions as per ICH guidelines. Physical and chemical properties of the dispersion didn’t change during a period of storage at room temperature and at 40°C, 75% RH. It was found that Piroxicam was chemically stable against the effects of temperature and humidity. However, the relative humidity and storage time exerted an effect on the dissolution behaviour of Piroxicam. The changes in dissolution behaviour after storage under conditions of high humidity and temperature might be related to the formation of Piroxicam microcrystal and to water absorption by the carrier during storage. It is predicted that acceptable shelf-lives should result when moisture resistant packaging is used for pharmaceutical formulations of this type.
The different assay methods for the determination of Piroxicam in the pharmaceutical preparation have been reviewed. The determination of recoveries of Piroxicam has been described by HPLC method. The aim of the present study was to develop and validate analytical method for determination of non micronized Piroxicam in SEEDS formulation in hard gelatin capsules by High Performance liquid chromatography (HPLC) method. It is therefore necessary to study the behavior of non micronized Piroxicam when it is incorporated in SEDDS formulation. The HPLC method was developed using chromatopack, peerless basic C18, 250x4.6mm, 5µm analytical column. The mobile phase comprising of acetonitrile : potassium dihydrogen ortho phosphate buffer [pH-3.0] in the ratio (40:60) v/v. The flow rate was maintained at 1.0ml/min and elute was monitored by using U.V detector at 230nm.The retention time of Piroxicam was about 12 minutes. The method was validated for its specificity, accuracy, precision, and linearity, limit of detection(LOD), limit of quantification(LOQ), robustness and stability parameters. The linear regression analysis data for the calibration plots shows a good linear relationship over the concentration range of 5-150 mg/mL. The method showed good recoveries (98.0 – 99.8%) and has been applied to formulation without interference of excipients in the formulation. The result of method was reproducible and within official limits. The HPLC method has been proved more authentic as it can be used for the quantitative and entrapment efficient to determine non micronized Piroxicam in SEDDS formulation in hard gelatin capsules.
Piroxicam is a poorly soluble, highly permeable drug and is characterized by a slow and gradual absorption via the oral route and this causes a delayed onset of therapeutic effect. Thus, plain piroxicam preparations are not indicated for analgesia. The results of the in vivo study revealed that the GL dosage form would be advantageous with regards to rapid onset of action, especially in various painful conditions where an acute analgesic effect is desired. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. There are several techniques to enhance the dissolution of poorly soluble drugs. Among them, the technique of liquisolid compacts is a promising technique towards such a novel aim. Hence in the present study, it was attempted to formulate Piroxicam in the form of self emulsifying drug delivery system (SEDDS) technique. Preformulation studies were performed to check the compatibility of drug and excepient for the preparation of formulation. Compatibility study, brittleness and softness study, solubility study, phase solubility were performed. Hence it was concluded that SEDDS of Non Micronized piroxicam could be formulated. The aim of this research article is to understand and overcome the challenges of physicochemical and physical properties of liquid excipients with different type of hard capsules and to shorten expensive development phase and to reduce time to market. To facilitate the development of novel drug delivery systems, the demand for new liquid excipients have been increased. The quality of finished formulation depends not only on the active principles and production processes, but also on the performance of the liquid excipients.
Piroxicam is a nonsteroidal anti-inflammatory drug that is characterized by low solubility-high permeability and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry there are several techniques to enhance the dissolution of poorly soluble drugs. Among them, the technique of liquisolid compacts is a promising technique towards such a novel aim. The present study was designed to improve the dissolution rate of non micronized piroxicam at the physiological pH's through its increased solubility by preparing liquid-solid dispersions of drug using triethyl citrate(TEC): acconon : polysorbate-80. The dissolution tests of the preparations were performed 1.2 pH simulating gastric using USP dissolution apparatus II. The concentration of the dissolved drug in the medium was determined by direct or first-derivative UV spectroscopy. The dissolution rates of the formulations were dependent on the nature and ratio of drug to carriers in SEDDS and the corresponding physical mixtures as well as the pH of the medium. Hence in the present study, it was attempted to evaluate non micronized Piroxicam formulation in the form of self emulsifying drug delivery system(SEDDS) technique. Formulation studies were performed to check the In Vitro study, Particle size analysis, Zeta potential, were performed. Hence it was concluded that SEDDS of Non Micronized piroxicam could be formulated.
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