Awareness of the release kinetics of active drugs is important in formulating drugs that have the desired delivery and in predicting the behaviour of the formulated drug in vivo. The study aims to determine the mechanism of drug release from griseofulvin tablets formulated with different surfactants using mathematical models and to compare the use of graphs and DD solver software in fitting dissolution profiles to kinetic models. The batches P1 -P3 were composed of the surfactant - PEG 4000 in different concentrations. A control batch without surfactant and a commercial brand (Mycoxyl 500) were used for comparison. Granule and tablet quality tests indicated quality formulations. Dissolution profiles showed that the surfactant improved drug release of griseofulvin and batches (batches P1 -P3) formulated with PEG 4000 had the best release profiles comparable with the commercial brand. The Excel Add-in DD solver and kinetic plots were used to determine the kinetic model of best fit. The Higuchi model was the best fit for batches P1 -P3. The first order and Hixon -Crowell also fit batches P2 and P3. The Korsmeyer’s model showed that batches P1 -P3 exhibited anomalous diffusion. The tablets formulated with PEG were as good as the commercial brand and they had an anomalous diffusion of the drug from the tablet; meaning that drug diffused following Fickian law and also diffused through a swollen and porous matrix. Kinetic plots and the DD solver can be used for fitting dissolution profiles to kinetic models. Keywords: Griseofulvin, Kinetics, Models, Surfactants, Polyethylene glycol (PEG) 4000, DD solver, Dissolution profile, mathematical models
Calabash chalk is a naturally geophagic mineral composed mainly of fossilized seashells or an artificial preparation of a combination of clay, mud, and sand. It is one of the widely consumed earth materials in the practice of geophagia. The present study is aimed at evaluating the effects of oral administration of calabash chalk on haematological parameters and body weight using Wistar rat models. Ten (10) healthy female mice and twenty (20) adults female Wistar rats weighing 20-30 g and 160 -200 g were used for the determination of the LD50 and the experimental study respectively. Locally sourced calabash chalk was orally administered to the Wistar rats at 400, 600 and 800 mg/kg respectively for twenty-eight (28) days. Haematological parameters were determined using a standard automated procedure. The result of the study shows that there was a significant decrease in red blood cell count, haemoglobin concentration, packed cell volume, total white blood cell count, neutrophils, lymphocytes, mid-range absolute and platelet counts among the experimental groups compared to the control (p<0.05). Also, there was a significant reduction in the percentage of weight changes among the experimental animals compared to the control (p<0.05). The present study has shown that despite the wide safety margin of calabash chalk, it can depress haematopoiesis by reducing the red blood cell, white blood cell and platelet counts.
Objective: Griseofulvin, an antifungal drug belongs to the class II of the Biopharmaceutical Classification System (BCS). It has the characteristics of poor aqueous solubility and good lipid permeability. Attempts have been made severally to improve the solubility and hence release of griseofulvin from different dosage forms. The study aimed to evaluate the effect of the different surfactants-Kolliphor® HS-15 (KHS 15), Sodium lauryl sulphate (SLS) and Polyethylene glycol (PEG) 4000 on the in-vitro dissolution and release of griseofulvin from compressed tablets. Method: Griseofulvin tablets were formulated with different concentrations of the surfactants and a control batch without surfactants using the wet granulation method. Dissolution test was carried out on the formulated tablets in 1000ml of 80% methanol. Comparisons were made amongst the dissolution profiles of the formulated tablets and a commercial brand using model dependent and independent methods. MANOVA was used in the analysis of percent drug release of the tablets. Result: All the different methods of comparing in-vitro dissolution are important. The tablets formulated with surfactants had better dissolution profiles than the control batch. Tablets containing PEG 4000 exhibited the best dissolution. The PEG 4000 containing tablet batches exhibited anomalous mechanism of drug release while the other batches of griseofulvin tablets including the commercial brand all exhibited quasi-Fickian mechanism of drug release. Conclusion: PEG 4000 containing tablets had the best dissolution profile. At the concentrations used, SLS and Kolliphor® HS 15 only had marginal improvement of griseofulvin dissolution compared with the control batch.
Obesity is a metabolic disease caused by a large buildup of fat in the body and a deficit in energy consumption compared to energy disposal. It has been related to a shorter life expectancy, has been connected to various cancer types, and has been linked to secondary metabolic illnesses such as diabetes, atherosclerosis, and hypertension. Due to an increase in white adipose tissue deposition, oxidative stress can lead to obesity, and obesity can lead to increased oxidative stress in the body. Coenzyme Q10 (Ubiquinone) is an endogenous anti-oxidant with anti-oxidant properties that aids to reduce oxidative stress. It boosts the anti-oxidant activity of superoxide dismutase and glutathione peroxidase, reduces lipid peroxidation, neutralises free radicals, and promotes vitamin E and C regeneration in the body. It can be found in the form of ubiquinol or ubiquinone. CoQ10 may be found in both diet and supplements. It can be made as a syrup, tablet, soft gel capsule, hard shell capsule, or oral powder as a supplement. It is classified as a biopharmaceutical class II compound with low solubility but good permeability. When CoQ10 supplement is taken with a fatty meal, its bioavailability is increased. CoQ10 slows the evolution of obesity-related atherosclerosis and helps to mitigate the harmful bodily environment caused by obesity.
This study investigates the anti-inflammatory, fibrinolytic and anti-oxidant activities of the n-hexane extract and fractions of Ficus sur Forssk leaves. The extract was separated on column chromatography using a gradient elution of hexane, dichloromethane and ethanol. Pooled column fractions were assayed for membrane stabilizing for anti-inflammatory, Streptokinase inhibition for fibrinolytic and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) reduction for anti-oxidant activity. Column fractions were pooled into five fractions (F1 – F5). The n-hexane crude extract and the fraction F3 consistently exhibited anti-inflammatory and fibrinolytic ability. The leaf extract of F. sur showed negligible anti-oxidant activity. Except for F1 all the fractions and the crude extract showed very high dose-dependent anti-inflammatory property even significantly higher (p <0.05) than the reference drug – diclofenac. Crude extract, F2 and F3 exhibited fibrinolytic ability. F1 showed the lowest assayed biological activity consistently. The study shows that the column fractions of n-hexane extract of F. sur leaves have fibrinolytic and anti-inflammatory activity and can be used in the management of thrombosis and inflammation.
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