Heterochelates of metals as an effective anti - Urease agents couple with their docking studies.

The current article discusses the activities of several synthesized metal heterochelates in in-vitro as anti-ulcer agents followed by their docking study. For this purpose, two important ligands like 8-hydroxyquinoline and DL-methionine were used in synthesis of heterochelates of metal including Cr (III), Mn (II), Fe (III), Co (II), Ni (II), Cu (II), Zn (II), Cd (II) and Pb (II). It was observed that these complexes showed excellent urease inhibition activities in which thiourea was the standard having IC50 value 21.6 ± 0.12µM. The Cu (II) complex showed potent inhibitory activity (22.6 ± 0.72 µM) when compared with the standard thiourea (21.6±0.12µM) among the nine synthesized complexes while Mn (II), Fe (III), Cd (II) and Pb (II) also showed better inhibitory activities. The urease inhibitory activities of hetercochelates also tested and validated by docking analysis.

Effects of superdisintegrants in oral dissolving formulation of cinitapride tablets.

The initiation of newer techniques and development of mouth dissolving (MD) products has created new avenues of higher patients' compliance. MD formulations are actually lessen the difficulties associated with solid swallowing with better bioavailability of especially poorly soluble drugs. In the current study mouth dissolving tablet (MDT) formulations of cinitapride (1 mg) were prepared by direct compression method using various proportion and combination of superdisintegrants. Nine formulations in three batches were compressed by incorporating low (2%), intermediate (6%) and higher (10%) levels of crospovidone, croscarmellose sodium, sodium starch glycolate. Micromeritic assessment of the powder blends were carried out and were found within the acceptable official limits. All newly developed trial formulations were exposed to different pharmacopoeial and non-pharmacopoeial testing. It was found that FC2 trial tablets containing polyplasdone XL® (crospovidone) at level of 6% (4.5 mg) presented the best physico-chemical attributes deemed to be desirable for the ODT products. Disintegration and wetting time of optimized FC2 was computed between 15-17 and 12-15 seconds respectively. The assay and content uniformity of FC2 were estimated to be 100.02±0.36 and 99.66±1.70 percent correspondingly. On the basis of the findings it was concluded that MDT could be successfully developed by incorporating appropriate concentration of superdisintegrant and their combinations.

Spectrophotometric method development and validation for determination of chlorpheniramine maleate in bulk and controlled release tablets.

Spectrophotometric technique is considered to be the simplest and operator friendly among other available analytical methods for pharmaceutical analysis. The objective of the study was to develop a precise, accurate and rapid UV-spectrophotometric method for the estimation of chlorpheniramine maleate (CPM) in pure and solid pharmaceutical formulation. Drug absorption was measured in various solvent systems including 0.1N HCl (pH 1.2), acetate buffer (pH 4.5), phosphate buffer (pH 6.8) and distil water (pH 7.0). Method validation was performed as per official guidelines of ICH, 2005. High drug absorption was observed in 0.1N HCl medium with λmax of 261nm. The drug showed the good linearity from 20 to 60µg/mL solution concentration with the correlation coefficient linear regression equation Y= 0.1853 X + 0.1098 presenting R2 value of 0.9998. The method accuracy was evaluated by the percent drug recovery, presents more than 99% drug recovery at three different levels assessed. The % RSD value <1 was computed for inter and intraday analysis indicating the high accuracy and precision of the developed technique. The developed method is robust because it shows no any significant variation in with minute changes. The LOD and LOQ values were assessed to be 2.2µg/mL and 6.6µg/mL respectively. The investigated method proved its sensitivity, precision and accuracy hence could be successfully used to estimate the CPM content in bulk and pharmaceutical matrix tablets.

Development and validation of stability indicating assay method for cinitapride in bulk & tablets.

A simple stability indicating UV-spectrophotometric method has been developed and validated for the determination of cinitapride hydrogen tartrate (CHT) in bulk and solid pharmaceutical dosage form. Drug absorption was measured in different analytical mediums however; maximum absorption was seen in 0.1 N HCl at wavelength (λmax) of 266 nm. The calibration curve was found to be linear over the concentration range from 6 to14µg/mL with the correlation coefficient value (r) of 0.999. The LOD and LOQ were estimated to be 0.1019µg/mL and 0.309µg/mL respectively. The accuracy was evaluated by determining the percent drug recovery, performed at three different levels of 50%, 100% and 150%. The% recovery was found to be in the range of 99.96-100.64%. The precision of the method was determined by inter-day and intra-day variations. The % RSD value <0.5 indicates the underlying method is precise and accurate as well. The developed method was applied to characterize in vitro assay content of few brands of cinitapride (1 mg) available in local market. No interference of the formulation excipients with the drug absorption was observed during assay. Drug substance and drug product were exposed to various stressed conditions (acid, base, oxidative, thermal and photolysis). Forced degradation testing of drug product showed that the oxidation (20%) was found to be the major degradation pathway of the cinitapride. However; drug estimation was not influenced in presence of degradation moieties formed during acid, base, oxidation, thermal and photolytic breakdown. Overall, the investigated technique is robust and specific that would be successfully used to quantify the cinitapride hydrogen tartarate in pharmaceutical dosage and bulk form in future.