Diacerein (DCN) was obtained by diacetylation of an anthraquinone derivative rhein and was approved by FDA in 2008, in the treatment of osteoarthritis due to its inhibitory effect on proinflammatory cytokines, including IL-6 and IL-1β. It was synthesized in 1980s and marketed as a tablet in some European Union and Asian countries from 1994. Along with its great potential in the treatment of osteoarthritis, its other applications are also being explored day by day, such as in the treatment of psoriasis, epidermolysis bullosa, breast cancer, type 2 diabetes and periodontitis. The main aim of this review is to explore mechanism of action, various applications and side effects associated with DCN. This has been reviewed that apart from the risk of diarrhea on long-term administration of DCN, various clinical studies has also shown its modest benefits in treatment of various pathological conditions. Hence, DCN is emerging as a new and potentially safe derivative with maximum therapeutic efficacies and minimum side effects which can results in improving the living status of patients suffering from various inflammatory diseases.
Objectives:
The present study aims on preparing Levosulpiride loaded solid lipid nanoparticles (SLNs) to reduce the dose, frequency of dosing, reduce side effects and to increase the bioavailable fraction of drug (<30% orally in general).
Methods:
Levosulpiride was characterized by preformulation studies like physical appearance, melting point, assay, calibration curve, FTIR analysis and DSC analysis. The calibration curve of the drug was prepared in pH 6.8 phosphate buffer. Two lipids (Stearic acid and Palmitic acid) were used as lipid phase to prepare SLNs. Factorial design (23) was applied to formulate 16 formulations (8 for each lipid i.e. SF1-SF8 and PF1-PF8). Levosulpiride SLNs were prepared by solvent evaporation method followed by homogenization.
Results:
The optimized formulations were characterized by particle size analysis, zeta potential analysis, in vitro drug release and drug release kinetics. Drug-excipient interaction in optimized formulation was characterized by FTIR, DSC and TEM analysis.
Conclusion:
On the basis of evaluation parameters, the formulation SF1 (containing Stearic acid) and PF1 (containing Palimitic acid) found to be better formulations amongst their groups with a controlled drug release after a period of 24 hrs.
Objective: The main objective of this review is to investigate the potential role of milk in improvement of bioavailability and patient compliance. Method: The study reviews the types of milk based on its composition, mechanism of how milk improves the solubility of poorly soluble drugs, masks the taste of bitter drugs and improves the patient compliance to dosage regimen. It also reviews various research studies done so far that recommend the use of milk in formulations. Along with this, the regulatory aspect of using milk is also considered in the present study. Conclusion: Investigation concludes that medicated milk formulations open a new hope of utilizing milk as multi-functional drug carrier for a variety of drugs.
Literature survey revealed that DCN is unstable under basic stress conditions specifically with sodium hydroxide when kept at room temperature for 48 h [14] , hence citric acid is used as a stabilizer in novel formulations [15,16]. No analytical method thus far has
A simple, accurate, precise and economical spectrophotometric method has been developed for estimation of Levosulpiride in bulk form as well as marketed formulations. The estimation of Levosulpiride was done at 291.2 nm in pH 6.8 phosphate buffer using UV-Visible double beam spectrophotometer. In the developed method, linearity over the concentration range of 10-100µg/ml of Levosulpiride was observed and was found in agreement of Beer's law. The linear regression was found to be 0.999. The results of analysis have been validated statistically and recovery studies confirmed the accuracy of the proposed method. The precision (intra-day & inter-day) of method was found within limits (RSD < 2%). The sensitivity of the method was assessed by determining limit of detection and limit of quantification. The percentage of Levosulpiride in the marketed formulation (LEFIT-50) was observed to be 99.46%. It could be concluded from the results obtained in the present investigation that the method for estimation of Levosulpiride in pure form and in pharmaceutical dosage form is simple, rapid, accurate, precise and economical and can be used, successfully, in the quality control of pharmaceutical formulations and other routine laboratory analysis.
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