The present study utilized a nitroglycerin-induced rat model of migraine to detect the effects of rizatriptan benzoate on proenkephalin and substance P gene expression in the midbrain using real-time quantitative poly...The present study utilized a nitroglycerin-induced rat model of migraine to detect the effects of rizatriptan benzoate on proenkephalin and substance P gene expression in the midbrain using real-time quantitative polymerase chain reaction and investigate whether rizatriptan benzoate can regulate the endogenous pain modulatory system. The results showed that rizatriptan benzoate significantly reduced expression of the mRNAs for proenkephalin and substance P. Rizatriptan benzoate may inhibit the analgesic effect of the endogenous pain modulatory system.展开更多
Rizatriptan benzoate is a 5HT 1B/1Dreceptor agonist which is prescribed for the treatment of migraine.In the present study new,simple,specific ultraviolet spectrophotometric method for rizatriptan benzoate was develop...Rizatriptan benzoate is a 5HT 1B/1Dreceptor agonist which is prescribed for the treatment of migraine.In the present study new,simple,specific ultraviolet spectrophotometric method for rizatriptan benzoate was developed and validated.Forced degradation studies were carried out in acidic,alkaline and neutral pH conditions.The absorbance maxima peak was found to be 224 nm and linearity was observed in the concentration range of 0.5~2.5μg·mL-1 with regression coefficient value of 0.998 8.The method was validated and found to be precise.The percent recovery for rizatriptan benzoate was found to be 98.576±0.202.The bulk drug was found to be stable in neutral and acidic pH conditions but got degraded in 1N NaOH solution.展开更多
The aim of this study was to produce fine particles with different corrugated degree of surface by spray-drying and to investigate the effect of surface morphology on in vitro aerosol performance of the particles with...The aim of this study was to produce fine particles with different corrugated degree of surface by spray-drying and to investigate the effect of surface morphology on in vitro aerosol performance of the particles within HFA 134a based metered dose formulations.Compositions of rizatriptan and scutellarin were spray-dried using different spray-drying parameters,and particles were suspended within HFA 134a.The surface morphology were determined using scanning electron microscopy(SEM),while the aerodynamic performance of MDIs was evaluated using a next generation pharmaceutical impactor.The surface morphology of spraydried particles could vary from smooth to moderately corrugated,and to raisin-like depending upon spray-drying parameters and preparation compositions.In general,increasing inlet temperature,decreasing feed concentration and/or adding leucine to the feed solution tended to increase the corrugated degree of particle surface.Deposition results indicated that raisinlike particle based MDIs for all compositions of the two drugs produced significantly better aerodynamic performance in terms of fine particle fractions and mass median aerodynamic diameters relative to the formulations of the corresponding smooth or slightly corrugated particles when the particle compositions were the same.The present results demonstrated that wrinkled particles increased fine particle fractions within surfactant-free MDI formulations.展开更多
文摘The present study utilized a nitroglycerin-induced rat model of migraine to detect the effects of rizatriptan benzoate on proenkephalin and substance P gene expression in the midbrain using real-time quantitative polymerase chain reaction and investigate whether rizatriptan benzoate can regulate the endogenous pain modulatory system. The results showed that rizatriptan benzoate significantly reduced expression of the mRNAs for proenkephalin and substance P. Rizatriptan benzoate may inhibit the analgesic effect of the endogenous pain modulatory system.
文摘Rizatriptan benzoate is a 5HT 1B/1Dreceptor agonist which is prescribed for the treatment of migraine.In the present study new,simple,specific ultraviolet spectrophotometric method for rizatriptan benzoate was developed and validated.Forced degradation studies were carried out in acidic,alkaline and neutral pH conditions.The absorbance maxima peak was found to be 224 nm and linearity was observed in the concentration range of 0.5~2.5μg·mL-1 with regression coefficient value of 0.998 8.The method was validated and found to be precise.The percent recovery for rizatriptan benzoate was found to be 98.576±0.202.The bulk drug was found to be stable in neutral and acidic pH conditions but got degraded in 1N NaOH solution.
基金the National Natural Science Foundation of China(grant no.81172997)the Ministry of Science and Technology of the People’s Republic of China(grant no.2012ZX09301-002-030)for the financial supports.
文摘The aim of this study was to produce fine particles with different corrugated degree of surface by spray-drying and to investigate the effect of surface morphology on in vitro aerosol performance of the particles within HFA 134a based metered dose formulations.Compositions of rizatriptan and scutellarin were spray-dried using different spray-drying parameters,and particles were suspended within HFA 134a.The surface morphology were determined using scanning electron microscopy(SEM),while the aerodynamic performance of MDIs was evaluated using a next generation pharmaceutical impactor.The surface morphology of spraydried particles could vary from smooth to moderately corrugated,and to raisin-like depending upon spray-drying parameters and preparation compositions.In general,increasing inlet temperature,decreasing feed concentration and/or adding leucine to the feed solution tended to increase the corrugated degree of particle surface.Deposition results indicated that raisinlike particle based MDIs for all compositions of the two drugs produced significantly better aerodynamic performance in terms of fine particle fractions and mass median aerodynamic diameters relative to the formulations of the corresponding smooth or slightly corrugated particles when the particle compositions were the same.The present results demonstrated that wrinkled particles increased fine particle fractions within surfactant-free MDI formulations.
