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Purpose: The aim of this study was to formulate methscopolamine floating drug delivery system to increase its gastro retention for further enhancement of absorption and overall bioavailability.
Method: Direct compression method was used to formulate floating drug delivery system of methscopolamine bromide.: Different amount of HPMC, PVP K25, and MCC were used for preparation of tablets.
Result: The prepared tablets were evaluated for thickness, hardness, weight variation, floating lag time, swelling index and in-vitro drug release. All the formulations showed less than 10% of weight variation. The hardness and thickness of all the formulations were within the range of 3.7-4.2 kg/cm and 3.63-3.83 mm respectively. Floating lag time for all the formulations was reported in seconds. The degree of swelling was reported in range of 82.10-85.83%. In vitro release was carried out for 24 h. The maximum release was shown by F1 (93.947%) while the minimum release was observed for F4 (90.420%). The best formulation was optimized on the basis of percentage cumulative drug release, floating lag time and swelling index. F1 found to be the best formulation. Further on analyzing the drug release mechanism, F1 found to exhibit korsmeyer peppas model of drug release.
Conclusion: Floating gastroretentive tablet of methscopolamine bromide was successfully developed using direct compression method with potential to enhance the drug absorption and effective treatment of peptic ulcer.
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http://dx.doi.org/10.1055/a-1249-8186 | DOI Listing |
J Pharmacol Sci
December 2024
Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi-City, Chiba, 274-8510, Japan.
We investigated the inhibitory effects of 32 antidepressants on [H]N-methylscopolamine ([H]NMS)-specific binding in the mouse cerebral neocortex to determine which antidepressants should be recommended for patients with Alzheimer's disease (AD). Of those tested, nine antidepressants (10 M) exhibited less inhibitory effect on [H]NMS-specific binding (<35%): tianeptine (a tricyclic); trazodone (a serotonin 5-HT blocker); sulpiride (a dopamine D blocker); fluvoxamine (a selective serotonin reuptake inhibitor (RI)); milnacipran, levomilnacipran, venlafaxine, and desvenlafaxine (serotonin and noradrenaline RIs); and bupropion (a noradrenaline and dopamine RI). Therefore, these antidepressants show little anticholinergic effect in the brain and are recommended for use in patients with AD.
View Article and Find Full Text PDFDrug Res (Stuttg)
December 2020
SHEAT College of Pharmacy, Varanasi.
Purpose: The aim of this study was to formulate methscopolamine floating drug delivery system to increase its gastro retention for further enhancement of absorption and overall bioavailability.
Method: Direct compression method was used to formulate floating drug delivery system of methscopolamine bromide.: Different amount of HPMC, PVP K25, and MCC were used for preparation of tablets.
Int J Neuropsychopharmacol
October 2019
The Florey Institute of Neuroscience and Mental Health, Parkville, Victoria, Australia.
Background: Preclinical and some human data suggest allosteric modulation of the muscarinic M1 receptor (CHRM1) is a promising approach for the treatment of schizophrenia. However, it is suggested there is a subgroup of participants with schizophrenia who have profound loss of cortical CHRM1 (MRDS). This raises the possibility that some participants with schizophrenia may not respond optimally to CHRM1 allosteric modulation.
View Article and Find Full Text PDFLearn Mem
July 2019
School of Behavior and Brain Sciences, The University of Texas at Dallas, Richardson, Texas 75080-3021, USA.
Vagus nerve stimulation (VNS) enhances extinction of conditioned fear in rats. Previous findings support the hypothesis that VNS effects on extinction are due to enhanced consolidation of extinction memories through promotion of plasticity in extinction-related brain pathways however, alternative explanations are plausible. According to one hypothesis, VNS may produce a hedonic effect and enhance extinction through counter-conditioning.
View Article and Find Full Text PDF