Stability-indicating method for the estimation of riluzole in tablets

A stability-indicating reverse-phase high-pressure liquid chromatography method with photodiode array detector was developed and validated for estimation of riluzole in the bulk and tablet dosage forms. Riluzole was subjected to stress conditions (light, heat, humidity, acid/base hydrolysis and oxidation) and the stressed samples were analyzed by developed method. Degradation was observed in acidic, basic, oxidative and thermal conditions. The degradation products were well resolved from riluzole peak. An inertsil-ods column (250×4.6 mm, 5 μ) with a mobile phase comprising 0.02% v/v formic acid:acetonitrile(35:65 v/v) at a flow rate of 1.0 ml/min was used and eluents were monitored at 260 nm. The retention time of riluzole was 5.7 min. Complete validation for the method was carried out according to Internation Conference on Harmonization guidelines. Linearity was achieved in the range 10-50 μg/ml with a correlation coefficient (r) 0.9998. The percent assay was 100.92 and mean percentage recovery was found to be 101.10

Physicochemical characterization, in vitro dissolution behavior, and pharmacodynamic studies of rofecoxib-cyclodextrin inclusion compounds. Preparation and properties of rofecoxib hydroxypropyl β-cyclodextrin inclusion complex: A technical note

An inclusion complex of rofecoxib and HPβ-CD was prepared successfully by the spray-drying method in a molar ratio of 1∶1. The inclusion complex was found to have improved in vitro drug release compared with the pure drug. The solubility profile of complexes of rofecoxib prepared using HPβ-CD as the complexing agent in a molar ratio of 1∶1 by the spray-drying method in pH 1.2 and pH 7.4 indicated that the acid solubility of rofecoxib was enhanced considerably by formation of an inclusion complex with HPβ-CD. The above results also clearly demonstrated a significant decrease in the gastric ulcerogenic activity of rofecoxib through complexation with cyclodextrins. Even though the physical mixture of rofecoxib with cyclodextrins reduced ulcer formation, it was the spray-dried complex formation approach that minimized gastric ulceration. These findings are extremely important from a commercial point of view as the prepared complex removes a major drawback for rofecoxib in therapy

Effect of Microneedle Type on Transdermal Permeation of Rizatriptan

This is a post-peer-review, pre-copyedit version of an article published in AAPS PharmSciTech. The final authenticated version is available online at: http://dx.doi.org/10.1208/s12249-016-0702-0.The present study was aimed to investigate the effect of salient microneedle (MN) geometry parameters like length, density, shape and type on transdermal permeation of rizatriptan (RIZ). Studies were carried out using two types of MN devices viz. AdminPatch® arrays (ADM) (0.6, 0.9, 1.2 and 1.5 mm lengths) and laboratory-fabricated polymeric MNs (PMs) of 0.6 mm length. In the case of the PMs, arrays were applied three times at different places within a 1.77-cm2 skin area (PM-3) to maintain the MN density closer to 0.6 mm ADM. Histological studies revealed that PM, owing to their geometry/design, formed wider and deeper microconduits when compared to ADM of similar length. Approximately 4.9- and 4.2-fold increases in the RIZ steady-state flux values were observed with 1.5 mm ADM and PM-3 applications when compared to the passive studies. A good correlation between different dimensionless parameters like the amount of RIZ permeated (Ct/Cs), thickness (h/L) and surface area (Sa/L2) of the skin was observed with scaling analyses. Numerical simulations provided further information regarding the distribution of RIZ in MN-treated skin after application of different MNs. Overall, the study suggests that MN application enhances the RIZ transdermal permeation and the geometrical parameters of MNs play an important role in the degree enhancement