Abstract
Liquisolid compacts were used to formulate water insoluble drugs in non-volatile solvents and converting into acceptably flowing and compressible powders. The main objective of present investigation was to enhance the dissolution rate of water insoluble drug ketoprofen by using liquisolid technique. Several liquisolid tablets were prepared by using different carrier materials such as microcrystalline cellulose (Avicel pH-101), starch, dicalcium phosphate and lactose, and coating material such as silica gel, respectively. Polyethylene glycol 400 was used as non volatile water miscible liquid vehicle. The liquid loading factors for such liquid vehicle was calculated to obtain the optimum amounts of carrier and coating materials necessary to produce acceptable flowing and compactable powder admixtures viable to produce compacts. The ratio of carrier to coating material was kept constant in all formulations at 20 to 1. Before compression, powdered mass were evaluated for various parameters like flow properties, content uniformity etc. All the prepared formulations were compressed using 12mm punch after addition of 5 % Sodium starch glycolate (super disintegrating agent) to each formulation. The formulated liquisolid tablets were evaluated for post compression parameters such as weight variation, hardness, drug content uniformity, percentage friability and disintegration time. The in-vitro release characteristics of the pure drug, drug from marketed tablets (as reference) and liquisolid technique (test sample), were studied. X-Ray Diffraction (XRD) and Fourier-Transform infrared spectroscopy (FT-IR) were performed. The results showed that liquisolid formulations of ketoprofen exhibited higher percentage of drug release than marketed formulation. And it was concluded that there was no interaction between drug and excipients.
Highlights
Therapeutic effectiveness of a drug depends upon the bioavailability which is dependent on the solubility and dissolution rate of drug molecules
Polyethylene glycol was used as a liquid vehicle, Avicel PH 101 (Mycro crystalline Cellulose-MCC), Dicalcium Phosphate (DCP), Starch, and Lactose were used as carrier materials and Silica gel was used as coating material, respectively
3.2 Precompression studies for liquisolid systems 3.2.1 Flow properties: Results of angle of repose, consolidation index and hausner’s ratio are given in the Table No 2. 3.2.2 X-ray Diffraction Studies: X-Ray Diffraction (XRD) curves of pure drug and all liquisolid formulations were shown in fig no 1-5 respectively. 3.2.3 Infra red spectra analysis: FTIR curves of pure drug and all liquisolid formulations were shown in fig no 6-10 respectively. 3.2.4 Content Uniformity: FTIR curves of pure drug and all liquisolid formulations were shown in fig no 6-10 respectively
Summary
Therapeutic effectiveness of a drug depends upon the bioavailability which is dependent on the solubility and dissolution rate of drug molecules. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Water soluble drugs will be inherently released at a slow rate owing to their limited solubility within the GI contents. The dissolution rate is often the rate determining step in the drug absorption. The challenge for poorly water soluble drugs is to enhance the rate of dissolution. This in turn subsequently improves absorption and bioavailability
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