Brain Targeting Studies on Ropinirole Hydrochloride after Intranasal Administration of Thermosensiti

来源 :中国上海第七届国际新药发明科技年会 | 被引量 : 0次 | 上传用户:weishuren33
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  Mucoadhesive temperature-mediated in situ gel formulations using chitosan and HPMC were used to enhance intranasal delivery of the dopamine D2 agonist ropinirole to the brain.In vivo bioavailability and brain uptake of ropinirole were assessed in albino rats using HPLC method following intranasal administration of in situ gel,intranasal ropinirole solution and intravenous ropinirole solution.The absolute bioavailabilty of ropinirole from the temperature-mediated in situ gelling nasal formulation was 82 %.The AUC 0-480 in brain after nasal administration of ropinirole in situ gel was 8.5 times (869-250 ng/g versus 102-20 ng/g) that obtained following i.v administration,this value was also considerably higher (869-250 ng/g versus 281-52 ng/g) than that achieved with intranasal ropinirole solution.High brain direct drug transport percentage (DTP ;90.36) and drug targeting index (DTI) >1 confirms direct nose to brain transport of the intranasal in situ gel formulation of ropinirole.These results conclusively demonstrate increased access of ropinirole to the blood and brain from intranasal thermosensitive in situ gel containing chitosan and HPMC.
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