Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.
ABSTRACT:The aim of the the present study was to investigate the analgesic activity of methanolic extract of Arisaema tortuosum (MEAT) using acetic acid-induced writhing and hot plate methods. The hot plate method is useful in elucidating centrally mediated antinociceptive responses, while acetic acid-induced writhing is the chemically induced pain of peripheral origin. The MEAT was used at doses of 50, 100, 200 and 400 mg/kg body weight on swiss albino mice. The percentage inhibition of the abdominal constriction reflex increased dose dependently in case of acetic acid-induced pain and in the hot plate method model the extract at the dose of 400 mg/kg significantly increased the pain reaction time (PRT). These studies conclude that A. tortuosum (Wall.) Schott. tuber possesses analgesic activity in a dose dependent manner. In case of acetic acid-induced pain, the extract at the dose of 400 mg/kg body wt. showed 41.19% inhibition of writhing reflex. In case of hot plate method, after 60 minutes the PRT increased to 7.47 ± 0.05 seconds for the extract at the dose of 400 mg/kg body wt.
Aims: The present investigation is aimed at the identification and quantification of flavonoids in the methanol extract of leaves of Bauhinia acuminata Linn. (Caesalpiniaceae) by a validated HPTLC method and confirmation of the same by RP-HPLC. Methodology: CAMAG HPTLC system with VisionCATS software and HPLC Agilent Infinity 1260 were employed for the study. Pre-coated silica gel 60 F254 plates were used as stationary phase and Toluene : Ethyl acetate : Formic acid (5:4:0.2, v/v/v) was used as mobile phase in HPTLC while in HPLC Thermo hypersil BDS C18 column and Methanol and 0.4% Phosphoric acid (65 : 35) were used as stationary and mobile phase respectively. Results: Among different standards used in HPTLC, only quercetin was found to be present and further quantitatively analyzed. The method shows good correlation coefficient (R2 ≥ 0.99) and linearity in the range of 0.5 to 5.0 µg/band. The concentration of quercetin in the test extract was found to be 0.514 µg/mg of the extract. The LOD and LOQ values were 0.84 µg/band and 2.59 µg/band respectively. The RP-HPLC study also represented good % RSD of Retention time (0.025) and Area (0.09) which signifies the high precision and repeatability. The assay result (4.99 %) also indicated good presence of the quercetin in the extract. Conclusion: The methods were rapid, cost effective and may be employed for quality-control and standardization of quercetin in different plant extracts.
In this study free radical scavenging activity of chloroform, methanolic and aqueous leaf extracts of Ixora coccinea L. (Rubiaceae) were determined and compared by in vitro assay models such as DPPH free radical, nitric oxide radical, hydroxyl radical scavenging assay, reductive ability and total antioxidant capacity. Ascorbic acid was used as reference standard. IC 50 of all the exracts in all the method were determined. Among all the three extracts, methanolic extract have shown better scavenging and antioxidant property compared to other extracts in all the assay methods evaluated thereby leading it into the modern system of medicine in future.
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