Dabigatran Etexilate (DE), a prodrug of dabigatran, is a strong oral, reversible, and direct thrombin inhibitor with low oral bioavailability because of active efflux via intestinal P-glycoprotein receptors. By creating a self-emulsifying drug delivery system, the current work largely focused on improving the solubility of dabigatran. Dabigatran is a BCS class II medication with high permeability and poor water solubility. UV-spectroscopy was used to determine Dabigatran's saturated solubility in different oils, surfactants, and co-surfactants. Based on their maximum solubility and compatibility with Dabigatran, the excipients were chosen. Different oils, surfactants, and co-surfactant combinations were used to create SEDDS formulations of dabigatran (4:1 and 3:1). Pseudo ternary phase diagrams were created, and the nano emulsification area was assessed using these. Formulations were created utilising different ratios of oil (Capmul MCM NF), surfactant (Labrasol ALF), and co-surfactant (Transcutol HP) based on the pseudo ternary phase diagram. The produced formulations were chosen, and the 4:1 formulation underwent optimization and was subjected to additional tests, including self-emulsification time, phase separation and stability tests, thermodynamic stability studies, droplet size and zeta potential, and in vitro drug release investigations. According to the report's results, Dabigatran SEDDS are a viable system to increase Dabigatran's solubility.
This article focuses on microspheres, types, preparation and their applications in drug delivery system. based on recent literatures. The microspheres are used for drug delivery that offers a potent therapeutic substitute for traditional or immediate-release single-unit dose forms. Microspheres are solid objects with diameters ranging from 1 to 1000µ m. The numerous types of microsphere are employed in the delivery of medications. The efficacy and administration strategies of the variously produced microspheres differ from those of standard dose forms. The microsphere is evaluated using a variety of methods that analyse the microsphere's quality. Finally brief summary of the current difficulties in processing these microspheres, which calls for additional study and development, is offered in the end.
The aim of present investigation to formulate bilayer tablets of posaconazole by using solvent evaporation technique. Posaconazole belongs to BCS class 2 which has high permeability and low solubility. In order to enhance the solubility of posaconazole solvent evaporation technique was applied where HPMC AS was used as carrier. This tablet consist of two layers of which first layer serves as loading dose which produce immediate release of drug and second layer serves as maintenance dose that provide controlled release of drug. The whole bilayer tablet is coated with Eudragit L30D55 to produce delayed release and protect drug from acid environment in stomach. The drug excipient compatibility study was performed by FTIR and no interaction was found. Croscaramellose was used in immediate release layer as superdisintegrant. Methocel K100M and Methocel E5M are used for sustain drug release in control release layer. The powder blend for evaluated for flow properties like angle of repose, bulk density, tapped density, Carr’s index and Hausner’s ratio which showed good results. Invitro dissolution studies was performed with USP dissolution apparatus 2- Paddle type. Invitro dissolution was performed for 2 hours in 0.1N HCl which showed no drug release followed by 6.8 phosphate buffer for 12 hours. The bilayer tablet showed initial release to provide loading dose of drug followed by controlled release up to 12 hours. Change in concentration of polymer and superdisintegrant showed impact on drug release profile. Increase in concentration of superdisintegrant in immediate release layer showed increased % drug release. Whereas increase in sustain release polymers in controlled release layer showed decrease % drug release. F9 batch showed satisfactory release up to 100% for 12 hours and was selected as best formulation. Reproducible batch for F9 was formulated and called F10 which also showed satisfactory results.
Non-steroidal anti-inflammatory drugs (NSAIDs) like Ketorolac Tromethamine are frequently prescribed to alleviate pain associated with osteoarthritis, ankylosing spondylitis, acute sciatica, rheumatoid arthritis, and low back pain. Hydrogels are polymeric three-dimensional networks that are able to consume significant volumes of water and remain insoluble in water due to their physical and chemical crosslinking. They respond to temperature, pH and ionic strength. They can be prepared by using natural polymers such as dextran, pectin, alginate, or synthetic polymers such as polyvinyl alcohol, polyethylene oxide, and poly–hydroxy ethyl methacrylate. Hydrogels are used to deliver several drugs. Today, hydrogels have found a wide range of applications due to their non-toxic nature and low cost. The purpose of the current research was to formulate and assess a topical gel based on hydrogel that contained Ketorolac Tromethamine to treat inflammation and pain while reducing the gastrointestinal side effects associated with oral treatment. According to the FTIR analysis, Ketorolac Tromethamine doesn't interact with other excipients in a significant way. The physical characteristics, pH level, extrudability, spreadability, swelling property, in-vitro drug release study of hydrogel formulations were assessed. Using a dialysis membrane and a phosphate buffer solution with a pH of 7.4, in vitro and ex vivo release studies were conducted on the Franz diffusion cell. Among all formulations, HF4 showed high spreadability of 25.2 ±0.3 gm./cm/sec, extrudability, swelling index, in vitro drug release, and ex vivo drug diffusion. HF4 hydrogel showed no signs of skin irritation. The final formulation HF4 hydrogel shows an equal analgesic and anti-inflammatory effect as standard Ketorolac gel. It was found from the drug release kinetics that the Topical Ketorolac hydrogel HF4 drug release mechanism follows the Higuchi model and zero order.
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