Objective: In the present work attempt has been made to stabilize optimized nanosuspensions of glimepiride by solidification using a novel Oral Thin Film (OTF) formulation.Methods: Nanosuspensions were characterized for particle size, zeta potential as well as in vitro dissolution profile. As nanosuspensions are prone to destabilization by Ostwald's ripening or agglomeration/aggregation, OTF formulation as a novel approach for stabilization through solidification of optimized nanosuspension was attempted. OTF formulation method is a simple, easy and scalable method for the preparation of solid oral dosage form. Prepared formulations were evaluated for physicochemical parameters like folding endurance, disintegration time, tensile strength, in vitro drug release, in vivo bioavailability and stability. Results:The mean particle size of the nanoparticles in OTF was found to be 57.2 nm. It was observed from the results of in vivo bioavailability studies that high plasma drug concentrations(Cmax) were achieved for nanosuspension loaded OTF (NSOTF) i.e. 4900 ng/ml as compared to marketed oral formulation (Cmax-2900 ng/ml). Results of the stability studies indicated that nanosize of the particles was retained even after 3 mo of the study. Conclusion:Therefore it can be concluded that OTF formulation has a potential for stabilization of nanosuspensions.
Curcumin is used in the treatment of colon cancer, but its very poor absorption in the upper part of the GIT is a major concern. As a site for drug delivery, the colon offers a near neutral pH, reduced digestive enzymatic activity, a long transit time and an increased responsiveness to absorption enhancers. The aim of the present study was to identify a suitable polymer (guar gum) based matrix tablet for curcumin with sufficient mechanical strength and promising in vitro mouth-to-colon release profile. Three formulations of curcumin were prepared using varying concentrations of guar gum containing 50 mg curcumin by the wet granulation method. Tablets were subjected to evaluation by studying parameter like hardness, friability, drug content uniformity, and in-vitro drug release. In vitro drug release was evaluated using simulated stomach, intestinal and colonic fluids. The susceptibility of guar gum to colonic bacteria was also assessed by a drug release study with rat caecal contents. The 40% guar gum containing formulation (F-1) showed better drug release (91.1%) after 24 hours in the presence of rat caecal contents in comparison with the 50% guar gum containing formulation (F-2) (82.1%). Curcumin could, thus, be positively delivered to the colon for effective colon cancer treatment using guar gum.
. Results: The average retention time for buprenorphine was 14.319 min. The method was validated according to the ICH guidelines. The validation characteristics included accuracy, precision, linearity, range, specificity, limit of Quantitation and robustness. The calibration curves were linear (R 2 > 0.999) over the concentration range 1.0 -500.0 µgmL −1 for buprenorphine hydrochloride and recovery study for the compound was above 95 %. No spectral or chromatographic interferences from the microemulsion excipients were found. The drug was found to be labile under oxidative stress condition; whereas stable under all other stress conditions. Conclusion: This method is simple, rapid and suitable for routine quality control analysis.
Objective: A randomized, open-label, balanced, two-treatment, two-period, two-sequence, single-dose, crossover bioequivalence study comparing Rizatriptan 10 mg Orally Disintegrating Strips (ODS, test) with that of established Oral Lyophilisate Rizatriptan 10 mg, Maxalt-MLT® (reference) was conducted in 24 healthy male volunteers under fasting conditions. A single oral dose of 10 mg Rizatriptan was administrated to each volunteer. Methods: Plasma concentrations of Rizatriptan were determined by a validated LC-MS/MS bioanalytical method. The plasma concentrations of Rizatriptan were considered for statistical analysis and for establishing bioequivalence. Pharmacokinetic analysis was done by using the non-compartmental method. Pharmacokinetic parameters Cmax, AUC0→t, AUC 0→∞, t1/2, Tmax, and Ke1 were estimated for each subject and each treatment. Results: Ninety percent confidence intervals (90% CI) calculated for the ratio of AUC0→t, AUC0→∞, and Cmax values for the test and reference formulations were 96.91-110.30%, 96.24-109.07%, and 90.37-113.56%, respectively for Rizatriptan. The 90% CIs of AUC0→t, AUC0→∞, and Cmax values were totally within 80-125%. Conclusion: Based on a statistical analysis of the results, both formulations of Rizatriptan 10 mg, were found to be bioequivalent in terms of rate and extent of absorption under fasting conditions.
Objective: The objective of the study was to develop and validate new, simple, and selective reverse-phase–high-performance liquid chromatography (RP-HPLC) method for the quantitative determination of Dabigatran Etexilate (DE) and its impurities in pharmaceutical dosage form as per the International Conference on Harmonization guidelines.Method: Chromatographic analysis was performed on Princeton SPHER-l00 C18 (250 × 4.6 mm, 5 μm) HPLC column, maintained at 50°C column temperatures, 6°C sample tray temperature, and detection monitored at 225 nm. The mobile phase consisted of acetonitrile:phosphate buffer (pH 2.5) (33:67 V/V). The flow rate was maintained at 1.0 ml/min.Results: The system suitability results indicate good performance of the system. Specificity study indicates that there is no interference of placebo and blank. The percentage relative standard deviation (RSD) of six preparations for known and unknown impurity in the sample solution is found below 10%; hence, the method is precise. The calibration curve for DE (unknown impurity), Impurity A was linear from 0.38 to 4.5 μg/ml (correlation coefficients [r2] for unknown Impurity [DE] and Impurity A are 0.996 and 0.999, respectively). The calibration curve for Impurity B and Impurity E was linear from 0.38 to 9.00 μg/ml (r2 for Impurity B and Impurity E are 0.999 and 0.999, respectively); hence, the method is linear. Accuracy for DE (unknown Impurity), Impurity A, Impurity B, and Impurity E are found within 80%–120%; hence, the method is accurate. The percentage RSD for a standard solution is found below 5% up to 24 h, and percentage impurity change in the sample solution is found below 0.1% up to 18 h; hence, standard solution is stable up to 24 h, and sample solution is stable up to 18 h.Conclusion: The developed method is new, simple, adequate, specific, precise, linear, and accurate for the determination of DE and its impurities in pharmaceutical dosage forms.
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Objective: The objective of the proposed work was to study the effect of various formulation and process parameters of solvent casting method on the physical and chemical stability of Ketorolac Tromethamine (KT) in the orally dissolving film dosage form. Methods: KT-excipient interaction study was carried out both in solid state and by processing samples through the solvent casting technique. The samples were evaluated using IR spectroscopy (IR) and X-ray diffractometry (XRD). Solvent casting method was used to prepare KT films using different film-forming polymers, and solvents. The drying temperature and pH of the dispersion were also varied to study the effect of these parameters on the stability of KT. All the formulations were analysed chemically initially and after one month of storage at 40 °C/75% RH. Results: During KT-excipient interaction study in solid state KT was found to be stable. No significant changes were observed in its impurity profile. Interaction between different polymers and KT was observed after the solvent casting process as revealed by IR and XRD analysis. The interaction was further confirmed in the film formulations upon chemical analysis. The polymers showing interaction with KT in XRD and IR were making it unstable chemically and were responsible for its chemical degradation as revealed by chemical analysis. It was also revealed that KT is most stable when processed using water as the solvent. KT was found to be stable when processed at a higher temperature and at acidic pH during film formation. It was found that chemical stability is more when Polyethylene oxide (PEO) and water under acidic pH are used and films are dried at a higher temperature. Conclusion: Both formulation parameters and processing conditions of the solvent casting technique affects the stability of drugs and hence should be studied as part of pre-formulation studies while developing orally dissolving films of drugs.
Objective: The present research work aims to develop an abuse deterrent rapidly dissolving buprenorphine microemulsion loaded sublingual film for the treatment of breakthrough pain. Methods: The Buprenorphine microemulsion loaded sublingual films were prepared using Capmul MCM C8 (oil), tween 20 (surfactant) and propylene glycol (co-surfactant) with different grades of film-forming polymer (HPMC) using film casting machine. The films were evaluated for in vitro disintegration and dissolution study, tensile strength, folding endurance, content uniformity, surface pH, thickness and weight variation, % loading of buprenorphine microemulsion in sublingual film, scanning electron microscope, ex vivo permeation study, droplet size and polydispersity index, Zeta potential, % moisture content, stability and abuse deterrent potential were evaluated. Results: The optimized film formulation showed desired mechanical properties with minimum disintegration time of 21s and exhibited 34.45 % loading of Buprenorphine microemulsion. Permeation studies through goat sublingual mucosa, indicated 87% Buprenorphine release, through Buprenorphine microemulsion loaded sublingual film, whereas only 30% Buprenorphine release when it was directly added to film without microemulsion strategy. Conclusion: The present study concludes that abuse deterrent and fast acting buprenorphine microemulsion-incorporated sublingual film of buprenorphine HCL and naloxone HCL is a promising alternative to mostly marketed buprenorphine injectable delivery systems and a non-invasive route of administration for breakthrough pain management.
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