SYNTHESIS AND FORMULATION OF IBUPROFEN PRO-DRUGS FOR ENHANCED TRANSDERMAL ABSORPTION
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 2
Abstract
Objectives: The aim is to synthesize ibuprofen prodrugs that have more suitable physicochemical properties and formulate them into a liquid formulation for topical administration. The transdermal delivery (TDD) is one of the most attractive routes for drug administration as it eliminates the GIT absorption variable, improves patient compliance and also reduces drug plasma fluctuations. However, TDD only drugs with suitable physico-chemical properties can be absorbed. The oral administration of NSAIDs for a long time can cause gastric mucosal damage, which may result in ulceration and bleeding. Thus, the development of a TDD of NSAIDs is of great interest as it decreases GIT side effectsMethods: The synthesis of ibuprofen alkyl esters was carried out by esterification reactions with methanol, ethanol, propanol, butanol, pentanol and hexanol. The formulated samples were then subjected to stability studies according to ICH guidelines.Results: We have successfully synthesized and characterized various esters of ibuprofen. Moreover, ibuprofen butyl ester has been prepared as topical solutions. The formulated TDD was tested for stability according to ICH guidelines and the results showed no changes in the initial appearance during three months of study at room temperature & at 40 °C.Conclusion: The assay and pH were within the pharmacopeial limits during the period of the study. In conclusion, stable topical formulation of Ibuprofen esters was obtained.Â
Authors and Affiliations
Murad Abualhasan, Mohyeddin Assali, Nidal Jaradat, Rana Tarayra, Aseel Hamdan, Rula Ardah, Abdel Naser Zaid
Keywords
Related Articles
- EP ID EP579094
- DOI -
- Views 70
- Downloads 0
ESTABLISHMENT OF CALLUS AND SUSPENSION CULTURE IN SESAMUM INDICUM L
Objective: Sesame (Sesamum indicum L.) is one of the most important oilseed crops in the world. We intended to evaluate the effects of different explants, carbon sources and growth regulators on callus induction and cell...
IN SILICO PHARMACOKINETICS AND MOLECULAR DOCKING OF THREE LEADS ISOLATED FROM TARCONANTHUS CAMPHORATUS L.
Objective: To investigate the pharmacokinetic and toxicity profiles and spectrum of biological activities of three phytochemicals isolated from Tarconanthus camphoratus L. Methods: Several integrated web based in silico...
INFLUENCE OF LOCALLY APPLIED HEAT ON THE PERFORMANCE OF TRANSDERMAL DICLOFENAC SODIUM PLASTERS
Objective: Applied heat to dermatologic preparations influences the medicine’s performance, such as drug release rate and drug absorption. However, there is little information concerning the performance of non-steroid...
BIOLOGICAL ACTIVITIES OF EXTRACTS FROM PADINA BOERGESENII AND SARGASSUM STENOPHYLLUM, SEAWEEDS NATURALLY FOUND IN BAIA DE TODOS OS SANTOS, BRAZIL
Objective: Here we present the results of the biological potential as antioxidant, anti-cancer and leishmaniscidal from extracts of Padina boergesenii Allender & Kraft and of Sargassum stenophyllum Martius, seaweed s...
MYRICETIN ISOLATED FROM TURBINARIA ORNATA AMELIORATES ROTENONE INDUCED PARKINSONISM IN DROSOPHILA MELANOGASTER
Objective: Parkinson’s disease (PD) is a neurodegenerative disorder which affects the elderly population. Free radicals overproduction, oxidative stress, apoptosis, inflammation and abnormalities in mitochondria are cr...