“FORMULATION DEVELOPMENT AND SOLUBILITY ENHANCEMENT OF ROSUVASTATIN CALCIUM BY USING HYDROPHILIC POLYMERS AND SOLID DISPERSION METHOD”

Objective: Preparation of Rosuvastatin Calcium by Using Hydrophilic Polymers and Solid Dispersion Method, Rosuvastatin calcium is a Dyslipidaemic agent, which act as a selective competitive inhibitor of HMG CoA educates enzyme and is used in the treatment of hyperlipidemia. Methods: In the present work, Solid Dispersion was prepared by kneading method to increase the solubility of Rosuvastatin Calcium. Results: Solid dispersions were evaluated by determining percentage yield, drug content, solubility, Scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), DSC and in vitro dissolution profile. The prepared solid dispersion are formulated into capsule dosage form and characterized by various parameters i.e. weight variation, content uniformity, disintegration and dissolution. The evaluated parameters of capsule dosage form increase in solubility and dissolution rate of the pure drug. Conclusion: These are various techniques to enhance the solubility of the drug, such as particle size reduction, use of surfactants, solid dispersion etc. Carriers are the major players in these formulations, e. g. Hydroxypropylmethylcellulose, ethylcellulose, Carbopol, Acacia Gum etc. Carbopol and Acacia Gum is one of the most efficient polymers work as a carrier for these drugs to enhance solubility.

Acacia pycnantha and gum arabic an alternative to antacids and proton pump inhibitors in the management of gastroesophageal and laryngopharyngeal reflux

ABSTRACT A case report is presented where a patient with long-term gastroesophageal reflux and recently diagnosed laryngopharyngeal reflux (LPR) underwent an 8-week treatment with proton pump inhibitors (PPIs). On discontinuation of the PPIs, symptoms of LPR remained and the patient’s reflux symptoms returned with increased severity. Consumption of acacia gum exudates from Acacia pycnantha resolved the LPR. Acacia pycnantha or gum arabic were both found to reduced reflux symptoms to a manageable level. An evaluation of the therapeutic effect of acacia gums using questionnaires to evaluate reflux symptoms, quality of life and global refluxogenic scores was undertaken. It was found acacia gums can be taken after the evening meal in the same way as antacids to manage reflux symptoms but with more sustained overnight relief.

Formulation, Physical Characterization and Antioxidant Potential of Silymarin Suspensions and Emulsions

Silymarin, is a therapeutically important flavonoid act as a hepatoprotective agent. However, has a positive effect on metabolism act as a hydrophobic drug but has a very low bioavailability. The aim of the present study was to prepare appropriate formulations of Silymarin in order to enhance its bioavailability. The natural suspending agents like (Xanthan gum, Tragacanth gum, Acacia gum and Iranian gum) were used for the formulation of suspensions, while emulsions were prepared with the combination of surfactant, co-surfactant and oil. The formulations were evaluated for their physical stability, pH, refractive index and conductivity. Among different formulations and suspensions prepared with xanthan gum as a green stabilizing agents were most stable. Emulsions formulated with tween 80 as a surfactant, polyethylene glycol as co-surfactant and olive oil were clear and stable for more than six months. The refractive index, pH and conductivity of the most stable suspension and emulsions were 1.347, 6.9 and 0.18 s/m and 1.43, 6.9, 0.01 s/m respectively. It was concluded that xanthan gum and tween 80 with polyethylene glycol has a good potential to enhance the therapeutic efficiency and stability of silymarin suspension and emulsion.

Eugenol-acacia gum-based bifunctional nanofibers as a potent antifungal transdermal substitute

Aim: Fungal biofilms interfere with the wound healing processes. Henceforth, the study aims to fabricate a biomaterial-based nano-scaffold with the dual functionalities of wound healing and antibiofilm activity. Methods: Nanofibers comprising acacia gum, polyvinyl alcohol and inclusion complex of eugenol in β-cyclodextrin (EG-NF) were synthesized using electrospinning. Antibiofilm studies were performed on Candida species, and the wound-healing activity was evaluated through an in vivo excision wound rat model. Results: The EG-NF potentially eradicated the mature biofilm of Candida species and their clinical isolates. Further, EG-NF also enhanced the re-epithelization and speed of wound healing in in vivo rat experiments. Conclusion: The study established the bifunctional applications of eugenol nanofibers as a transdermal substitute with antifungal potency.

Formulation and Evaluation of Conventional Metronidazole Tablets using Natural Gum Extracted from Grewia species

Aims: The pharmaceutical world has been paying increasing attention to the extraction, development and use of natural gums as binders in the formulation of solid dosage forms. The use of natural gums as binders is more advantageous than the use of synthetic ones due to availability, low cost, biodegradability and biocompatibility. In this study, gum extracted from Grewia species was compared with that fromAcacia in metronidazole tablets. Study Design: Ten batches of metronidazole tablets were formulated with varied concentration of Grewiaspp gum and Acacia gum. Place and Duration of Study: The study was carried out in Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Delta State University, Abraka, Nigeria; between January and December 2019. Methodology: Five batches of metronidazole tablets containing 0.5, 0.75, 1.0, 1.25 and 1.5% w/w of Grewia gum were preparedby wet granulation. Resulting granules were characterised by measuring flow and packing properties. In other experiments, five batches of tablets were formulated using same concentration of gum, with Acacia gum substituted for Grewia gum. Both sets of granules were compressed into tablets using tableting machine at a load of 27 arbitrary units. Tablets so formed were evaluated for hardness, friability, disintegration time, drug content and drug release profiles. Drug – excipient interaction was investigated with FTIR. Results: The resulting metronidazole tablets showed hardness of 5.46 kgF to 7.87 kgF (Grewiagum) and 6.06 kgF-8.20 kgF (Acacia gum). Friability percentages of all the batches were above 1% except for A3-A5 and B5 which are less than 1%. All formulations released more than 75 % of the drug content within 60 min. The FTIR analysis revealed no interaction between the metronidazole and Grewia species gum. Conclusion: Metronidazole granules and tablets were successfully prepared using Grewiagum and showed comparable pre-compression and post-compression properties with those formulated with Acacia.

The Neuroprotective Effects of Policosanol on Learning and Memory Impairment in a Male Rat Model of Alzheimer's Disease

Alzheimer's disease (AD) as a neurodegenerative disease is recognized with progressive cognitive function failure, which is determined by beta-amyloid (Aβ) accumulation in extracellular space and hyperphosphorylation of intracellular Tau protein. Aβ stimulates some kinds of active oxygen and causes oxidative stresses and apoptosis. Policosanol (PCO) is a reducing lipid complement, which has antioxidant and anti-inflammatory activities. In the current research, the PCO effects on learning and memory impairment were investigated in a rat model of AD. Healthy adult male Wistar rats (230–250g) were divided randomly into 7 groups (n=6-7): Control, Sham (5 µL of phosphate-buffered saline, intracerebroventricular (ICV) microinjection), AD model (5 µL, ICV injection of Aβ), acacia gum (50 mg/kg, 8 weeks, gavage), PCO (50 mg/kg, 8 weeks, gavage), AD + acacia gum (50 mg/kg, 8 weeks, gavage), and AD + PCO (50 mg/kg, 8 weeks, gavage). Passive avoidance learning (PAL) and memory were assessed by shuttle box, cognitive memory by novel object recognition (NOR), and spatial memory by the Morris water maze (MWM) test. The oxidant and antioxidant parameters were examined at the end of the experiments. According to our results, ICV injection of Aβ caused reduced cognitive memory in NOR, spatial memory in MWM, and passive avoidance in PAL tests. PCO caused a recovery in cognitive memory, spatial memory, and PAL memory. Aβ plaques increased in the AD group, while PCO decreased it. Aβ increased total oxidant status and decreased total antioxidant capacity, whereas PCO reversed these parameters. Our results demonstrated that PCO has neuroprotective effects and can protect learning and memory impairments via its hypolipidemic and antioxidant effects.

Aplikasi Pre-Heating dan Edible Coating untuk Peningkatan Kualitas Keripik Kentang

This study aimed to improve the crispness and to reduce oil absorption in potato chips. Potato chips crispness was improved by applying pre-heating, namely boiling and steaming before frying, while oil absorption was reduced by adding acacia gum as an edible coating. Boiling and steaming was conducted at 100°C for 0, 2, 3, 4, 5, and 6 minutes. Acacia gum (0, 3, 4, 5, and 6%) and calcium chloride (0, 0.5, and 1%) were added in the formulation. Boiling for 4 minutes yielded hardness of 384.902±25.10 g, moisture content of 3.02±0.07%, crispness score of 5.04±0.60 (crispy), and overall hedonic score of 5.10±1.43 (somewhat like). Further process by adding acacia gum 5% and calcium chloride 1% yielded potato chips with fat content of 28.01±1.56%, oil absorption ratio of 0.32±0.03, moisture content of 1.07±0.78%, and hardness level of 411.111±25.32 g. The products recuded oil absorption during frying up to 41.81±5.86%.