Purpose: We compared efficacy and side effects of ropinirole implants with oral ropinirole in parkinsonian monkeys. Methods: Twenty monkeys received injections of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-hydrochlo...Purpose: We compared efficacy and side effects of ropinirole implants with oral ropinirole in parkinsonian monkeys. Methods: Twenty monkeys received injections of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-hydrochloride (MPTP) to render them parkinsonian. Monkeys were then placed into 3 groups based upon clinical rating scores (CRS). Group 1 received oral ropinirole and placebo implants. Group 2 receivedropinirole implants that released 1/9th of the animals’ optimal daily oral dose and oral placebo. Group 3 received placebo implants and oral placebo. Monkeys were assessed for pharmacokinetic data, CRS, Global Dyskinesia Rating Scale, and skin irritation. Results: For the ropinirole implant group, the activity pattern was similar to that seen pre-MPTP;which extended through the weekends and was greater than control treated parkinsonian monkeys. Oral ropinirole yielded a high degree of variability for activity, with values following oral dosing being higher than the pre-MPTP periodbut levels similar to placebo treated parkinsonian animals during weekends, which were excluded from oral dosing. Implants and oral treatment achieved significant improvement in CRS between 11 - 60 days and 4 - 60 days respectively. Conclusion: Low dose ropinirole implants have the potential to provide continuous clinical improvement in bradykinesia with fewer “off periods” and lower risk for medication-induced psychosis than oral medication.展开更多
Two simple and rapid spectrofluorimetric and spectrophotometric methods were described for the determination of ropinirole hydrochloride content in pharmaceutical dosage forms. Both methods are based on the reaction o...Two simple and rapid spectrofluorimetric and spectrophotometric methods were described for the determination of ropinirole hydrochloride content in pharmaceutical dosage forms. Both methods are based on the reaction of ropinirole hydrochloride and eosin Y in aqueous medium at p H 4.0. Quenching of the fluorescence intensity of eosin Y at 540 nm upon excitation at 350 nm was used for the determination of ropinirole hydrochloride levels after ion-pair complex formation. Also, the absorbance increase of eosin Y at 546 nm after ion-pair complex formation was used for spectrophotometric measurements. Both methods showed linear relationships between the fluorescence quenching or absorbance increase and ropinirole concentration in the range of 6–150 μg/m L and 50–500 μg/m L for spectrofluorimetric and spectrophotometric methods, respectively. As no organic solvents were used in these two methods, they could be categorized as green analytical methods. Both methods were accurate(Error<1.2%) and precise(CV<1.9%), as shown by statistical analysis results. Both methods were used for determination of ropinirole hydrochloride content in pharmaceutical dosage forms without any significant interference from associated impurities.展开更多
Non-ergot dopamine agonists have become popular for treating motor complications associated with long-term use of levodopa-containing drugs. We conducted a retrospective study in which we identified clinical problems ...Non-ergot dopamine agonists have become popular for treating motor complications associated with long-term use of levodopa-containing drugs. We conducted a retrospective study in which we identified clinical problems related to use of non-ergot dopamine agonists. The study included 38 patients with Parkinson’s disease (PD) who suffered the wearing-off phenomenon and had thus been under non-ergot dopamine receptor agonist therapy for 1 - 2 years. Some presented with problems such as major symptoms of PD (30.3%), psychiatric symptoms (24.2%), and postural dysfunction (21.2%). Comparison between two different non-ergot drugs showed the levodopa dosage to be greater among patients taking ropinirole than among those taking pramipexole. In patients with advanced PD, various problematic symptoms can develop early after administration of a non-ergot dopamine agonist to treat the wearing-off phenomenon, necessitating identification and treatment of such symptoms on a patient-to-patient basis.展开更多
文摘Purpose: We compared efficacy and side effects of ropinirole implants with oral ropinirole in parkinsonian monkeys. Methods: Twenty monkeys received injections of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-hydrochloride (MPTP) to render them parkinsonian. Monkeys were then placed into 3 groups based upon clinical rating scores (CRS). Group 1 received oral ropinirole and placebo implants. Group 2 receivedropinirole implants that released 1/9th of the animals’ optimal daily oral dose and oral placebo. Group 3 received placebo implants and oral placebo. Monkeys were assessed for pharmacokinetic data, CRS, Global Dyskinesia Rating Scale, and skin irritation. Results: For the ropinirole implant group, the activity pattern was similar to that seen pre-MPTP;which extended through the weekends and was greater than control treated parkinsonian monkeys. Oral ropinirole yielded a high degree of variability for activity, with values following oral dosing being higher than the pre-MPTP periodbut levels similar to placebo treated parkinsonian animals during weekends, which were excluded from oral dosing. Implants and oral treatment achieved significant improvement in CRS between 11 - 60 days and 4 - 60 days respectively. Conclusion: Low dose ropinirole implants have the potential to provide continuous clinical improvement in bradykinesia with fewer “off periods” and lower risk for medication-induced psychosis than oral medication.
文摘Two simple and rapid spectrofluorimetric and spectrophotometric methods were described for the determination of ropinirole hydrochloride content in pharmaceutical dosage forms. Both methods are based on the reaction of ropinirole hydrochloride and eosin Y in aqueous medium at p H 4.0. Quenching of the fluorescence intensity of eosin Y at 540 nm upon excitation at 350 nm was used for the determination of ropinirole hydrochloride levels after ion-pair complex formation. Also, the absorbance increase of eosin Y at 546 nm after ion-pair complex formation was used for spectrophotometric measurements. Both methods showed linear relationships between the fluorescence quenching or absorbance increase and ropinirole concentration in the range of 6–150 μg/m L and 50–500 μg/m L for spectrofluorimetric and spectrophotometric methods, respectively. As no organic solvents were used in these two methods, they could be categorized as green analytical methods. Both methods were accurate(Error<1.2%) and precise(CV<1.9%), as shown by statistical analysis results. Both methods were used for determination of ropinirole hydrochloride content in pharmaceutical dosage forms without any significant interference from associated impurities.
文摘Non-ergot dopamine agonists have become popular for treating motor complications associated with long-term use of levodopa-containing drugs. We conducted a retrospective study in which we identified clinical problems related to use of non-ergot dopamine agonists. The study included 38 patients with Parkinson’s disease (PD) who suffered the wearing-off phenomenon and had thus been under non-ergot dopamine receptor agonist therapy for 1 - 2 years. Some presented with problems such as major symptoms of PD (30.3%), psychiatric symptoms (24.2%), and postural dysfunction (21.2%). Comparison between two different non-ergot drugs showed the levodopa dosage to be greater among patients taking ropinirole than among those taking pramipexole. In patients with advanced PD, various problematic symptoms can develop early after administration of a non-ergot dopamine agonist to treat the wearing-off phenomenon, necessitating identification and treatment of such symptoms on a patient-to-patient basis.
