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• W2922641500 abstract "Targeted drug delivery systems are designed to release the medicamentcontinuously in a predetermined pattern for a fixed period of time either systemically orto a specified organ to ensure safety and to improve its efficacy as well as patientcompliance. Drug released from these drug delivery systems should be at a desired,predictable and reproducible rate. Gastroretentive system (GRS) is a topic of currentinterest in the design of controlled release drug delivery systems to target the drug to thesite of absorption. It prolongs the residence time of the dosage form at the site ofapplication or absorption and facilitates an intimate contact of the dosage form with theunderlying absorption surface and thus contributes to improved and/or better therapeuticperformance of the drugs. In the present investigation design of floating tablets (GRS) offluorouracil for oral controlled release is aimed.Fluorouracil is used in the treatment of cancer. It is sparingly soluble in water andits absorption is dissolution rate limited. Fluorouracil has a short biological half life anderratic absorption. To avoid the dose related toxicity and to prolong its duration of actioncontrolled release products are necessary.The first chapter deals with introduction about the clear advantage of controlledrelease dosage forms and the advantages derived with gastro retentive system. In thischapter absorption window, modulation of GI transit time, basic gastrointestinal tractphysiology, factors affecting gastric retention, classification of floating drug deliverysystem, evaluation methods are discussed. Gastric cancer, its causes and the treatmentwere also discussed.Chapter II contains literature review on the gastroretentive systems, fluorouraciland β cyclodextrin. Drug profile, polymer profile and excipient profile are given inchapter III. Preformulation studies of the drug were documented in chapter IV. Thecharacterization of the drug material, 5 fluoro uracil that included physicochemicalproperties such as melting point, loss on drying, bulk and tapped density were done.A compatibility study for polymer and drug was carried out to assess any interaction, byIR spectroscopy. The spectra showed no interaction had occurred with the excipients.As fluorouracil is sparingly soluble in water, it was complexed with βcyclodextrin to enhance the solubility of the drug. The aqueous solubility and dissolutionrate of 5-fluorouracil can be increased by inclusion complexation with β-cyclodextrin.Molecular-modeling studies support the formation of stable molecular inclusioncomplexation of 5-fluorouracil with β-cyclodextrin monomer (1:1). Complexes wereprepared by physical mixture, kneading, co evaporation and freeze drying methods. Tworatios 1:1 and 1:2 were formulated. These eight complexes were subjected to Phasesolubilitystudy, molecular modeling to confirm the ratio and dissolution study. Thecomplexes formed were confirmed by DSC studies. Phase solubility profile indicated thatthe solubility of 5-fluorouracil increased in the presence of β-cyclodextrin monomer.Results obtained by different characterization techniques clearly indicate that the freezedryingmethod leads to formation of solid state complexes between 5-fluorouracil and β-cyclodextrin. The complexation of 5-fluorouracil with β-cyclodextrin lends an amplecredence for better therapeutic efficacy. Complexation and the enhancement of solubilityare discussed in chapter V.In the present work, a floating gastro retentive drug delivery system wasdeveloped and fabricated containing the drug 5 fluoro uracil. The aim of the work wasto get a modified release pharmaceutical dosage form that could be used in the treatmentof cancer. Floating drug delivery system are well proved and documented to betherapeutically superior to conventional dosage system in number of studies.In chapter VI the optimization of the tablet process parameters was performed tofind out the optimum operational conditions and to optimize the formula. The tabletswere obtained by wet granulation method for all the formulations F- I to F- XII andevaluated for the buoyancy lag time and floating time, hardness, weight variation anddrug content. Based on the performance with respect to buoyancy lag time, floating timeand the release characteristics, the formulation (F- IX) was selected as the best formula asit showed a buoyancy time of 24 seconds and a floatation time of 24 hours. Thisformulation (F- 9) showed a sustained release rate throughout its release period." @default.
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• W2922641500 date "2009-04-01" @default.
• W2922641500 modified "2023-09-22" @default.
• W2922641500 title "Targeted Drug Delivery of Anti Cancer Drug by Applying Gastro Retentive Systems and Its Pharmacological Evaluation" @default.
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