Objective: An assortment of commercially accessible enteric coated rabeprazole tablets were evaluated comparatively in vitro disintegration and dissolution profile in association with its’ drug content. Methods:In-vitro disintegration and dissolution profiling of our selected all enteric coated rabeprazole brands in Bangladesh were carried out using a dissolution apparatus USP at a paddle speed of 100 rpm and UV-VIS spectrophotometer. BP method was used to determine the time required for tablet to disintegrate in acid stage, pH 1.2 and buffer stage, pH 6.8. Results: The in vitro disintegration and dissolution time were found to be varying for each tablet, but within the B.P. prescribed limit. Brand10 showed the fastest disintegration. All the brands showed no disintegration, cracks or swelling in 0.1 N HCl, except brand 4 and 10, which showed cracks, leakage, and blackspot after 120 min. However, the disintegration of all the products in phosphate buffer meets B.P requirements. Dissolution of tablets in 0.1 N HCl showed less than 10% drug release after 120 minutes. Moreover, the comparison of percentage drug release on the basis of dissolution study demonstrated that Brand 1, 2, 4, 5, 6, 7, 8, 9, and 10 (80% drug release) complied best whereas Brand 3 (78.16% drug release) does not fulfill with pharmacopoeial specification. Conclusion: All the brands (10) of rabeprazole tablets tested in vitro assessment of disintegration and dissolution were showed pharmacopoeial specification except brand 3, 4 & 10. So, this study helps to make pharmacopoeial specified rabeprazole tablets.
The use of medicinal products of various categories is burgeoning geometrically in the global landscape over the past few decades. Although Africa and Asia culturally remain the home for complementary and alternative medicines (CAM), the north with the most sophisticated allopathic medical system is making headway in CAM use. Whilst herbal medicine is generally considered "safe" because it is natural and neutral, copious evidence suggests that herbal medicine could be lethal if not used rationally. Education and training of practitioners, scientific validation, legislative regulation of herbal medicine use and open patient-practitioner communication remain the crux of the safety, quality and standardisation of medicinal products.
Important conceptual changes concerning human thermoregulation have revealed in the last decade. Recent investigations in central and peripheral thermosensitivity have emphasized the importance of temperature-activated transient receptor potential (TRP) cation channels and they are being ardently pursued as targets for analgesic drug discovery. They are the largest group of sensory detectors expressed in nerve terminals and pain receptors activated by temperature and provide information about thermal changes in the environment. Thermo-TRP channels are capable of initiating sensory nerve impulses following the detection of thermal, as well as mechanical and chemical irritant stimuli. At least, a family of six thermo-TRP channels has been characterized to date (TRPA1, TRPM8, TRPV1, TRPV2, TRPV3, and TRPV4) that exhibit sensitivity to increases or decreases in temperature as well as to chemical substances that elicit similar hot or cold sensations. Such irritants include menthol, cinnamaldehyde, gingerol, capsaicin, mustard oil, camphor, eugenol, and others. The thermal thresholds of many thermo-TRP channels are known to be modulated by extracellular mediators, released by tissue damage or inflammation, such as bradykinin, prostaglandins, and growth factors. Antagonists or blockers of these channels are likely as promising targets for new analgesic drugs at the periphery and central levels and thus, controlling the modulation of thermo-TRP channels by inflammatory mediators and ligands may be a useful alternative strategy in developing novel analgesics.
Aims: To screen for the presence of bioactive phytoconstituents in hexane fraction of Archidium ohioenseusing the GC-MS technique. Study Design: Phytochemical screening via GC-MS technique. Place and Duration of Study: Department of Biochemistry, Obafemi Awolowo University, Ile-Ife, between September 2013 and June 2014. Methodology: The whole plant material was collected, sundried, pulverized and extracted with 80% (v/v) methanol for 48 hours using cold extraction method. The filtrate was concentrated in vacuo on rotary evaporator to yield the crude extract. The crude extract was partitioned with saturated n-hexane to afford the hexane fraction. The hexane fraction was analyzed via GC-MS technique. Identification of the constituents was done by comparing the mass spectrum fragmentation pattern of each of the constituents (head to tail) with those stored in the database of National Institute Standard and Technology 11 (NIST11.L) library. Results: The GC-MS analysis of A. ohioense revealed the presence of thirty eight compounds (phytochemical constituents). Three components appeared to be most prominent which constitute 60.03% of the total hexane fraction. The three major compounds are: pentadecanoic acid, 14-methyl-, methyl ester (19.03%), 9, 12- octadecadienoic acid, methyl ester (21.66%), and 9, 12, 15-octadecatrienoic acid, methyl ester, (Z, Z, Z) (28.39%). Conclusion: GC-MS analysis of the hexane fraction of A. ohioense afforded three major constituents identified as: pentadecanoic acid, 14-methyl-, methyl ester, 9, 12- octadecadienoic acid, methyl ester, and 9, 12, 15-octadecatrienoic acid, methyl ester, (Z, Z, Z).These compounds have been reported to exhibit various biological activities, hence hexane fraction of A. ohioense could serve as a source for these bioactive compounds.
Aim: To assess the antidiabetic potential of a polyherbal tea, Diabetea, and its individual ingredients; Achillea millefolium L., Agathosma betulina Bartl. & Weidl., Salvia officinalis L., Taraxacum officinalis L., Thymus vulgaris L., Trigonella foenum-graecum L. and Urtica urens L. Study Design: An in vitro laboratory-based study with appropriate positive and negative controls. Place and Duration of Study: Department of Pharmacology, February 2011 to August 2013. Methodology: The α-amylase and α-glycosidase enzyme inhibitory activity of hot water- and dichloromethane extracts (HWE and DCME) of Diabetea and its constituents were assessed spectrophotometrically and data interpreted using the Michaelis-Menten model. Glucose uptake into C2C12 myotubes was determined using a fluorometric method. Results:A. betulina (DCME) and U. urens (DCME) significantly (p<0.05) inhibited the activity of α-glucosidase (non-competitively) and α-amylase (un-competitively). The inhibitory activity of these extracts significantly (p<0.05) compared with the positive control, acarbose. The DCME of Diabetea, T. officinalis, U. urens, A. millefolium and the HWE of A. betulina, T. officinalis, T. foenum-graecum, S. officinalis, U. urens and T. vulgaris caused a significant (p<0.05) uptake of glucose into C2C12 myotubes compared to the control. S. officinalis (HWE) and T. vulgaris (DCME) were found to be more active in reducing the blood sugar level than insulin (p<0.05) at 3 and 20 μg/ml, respectively. Conclusion: Diabetea, T. officinalis, U. urens, A. millefolium, A. betulina, T. foenum-graecum, S. officinalisand T. vulgaris contain bioactive compounds that act as insulin mimetics. It can be concluded that U. urens(DCME), A. betulina (HWE) and T. vulgaris (HWE and DCME) were the most promising in vitro antidiabetic preparations due to their potent hypoglycaemic activities.
Aim: The aim of the present investigation was to develop and validate a rapid, sensitive, cost effective and reproducible stability indicating derivative spectrophotometric method for the estimation of duloxetine HCl in bulk and in formulations. Methodology: First order derivative spectrophotometric methods were developed for duloxetine HCl employing peak-zero (P-0) and peak-peak (P-P) techniques and their stability indicating potential was assessed in force degraded solutions. The methods were validated with respect to linearity, accuracy, precision and robustness. Results: Linearity was observed in the concentration range 5 μg/mL-90 μg/mL with an excellent correlation coefficient (r2) of 0.999. The limits of assay detection values were found to range from 0.33-0.41 μg/mL and quantitation limits ranged from 1.01-1.24 μg/mL for the proposed methods. The proposed method was applicable to the determination of the drug in capsules and the percentage recovery was found to be 99.68±0.95%. Conclusion: The developed methods were successfully validated and applied to the determination of duloxetine HCl in bulk and pharmaceutical formulations without any interference from common excipients. Satisfactory recovery in force degraded solutions suggests the stability indicating nature of the assay.
The purpose of this research was to evaluate the effects of supercritical precipitation on the physicochemical characteristics of Pioglitazone hydrochloride (PG). Therefore, PG powder was dissolved in methanol, ethanol, acetone, dichloromethane and binary mixtures of these solvents and the solutions were sprayed into the supercritical carbon dioxide. The processed powders were harvested then analyzed by using scanning electron microscopy (SEM), differential scanning calorimetery (DSC) and Infrared Spectroscopy (IR) methods. Different morphologies of PG particles were observed in the SEM micrographs and the particle sizes varied between 37.1 µm and 95.1 µm. The IR spectroscopy showed no changes in molecular structure of drug during the process. Also, the DSC thermograms confirmed the similar thermal behavior of PG before and after processing. The dissolution rate of unprocessed and processed powders was compared and showed enhancement in the dissolution rate of processed powders up to 2 times.