Objective: The present research study was undertaken to formulate mucoadhesive sustained release buccal tablets and patches of 5-fluorouracil (5-FU).Method: For the research experiment work design expert software version 10, stat-ease, Inc. has been used. A 3 2 full factorial design was selected for the formulation of the buccal tablet as well as buccal patches. In this research work, formulated tablets and patches using different polymers such as carbopol 974p, polyvinylpyrrolidone-K 30, sodium deoxycholate, microcrystalline cellulose, and polyvinyl alcohol. An after formulation of batches formulated products studied for characterization, namely, Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC). Evaluation parameters studied such as weight uniformity, thickness, hardness, friability, and content uniformity also carried out. For drug release purpose from the formulation of buccal tablet and patches in vitro drug released performed. In vivo drug releases study also carried out using Rabbit for drug reaction point of view.Results: Design expert showed the significant results on independent and dependent variables. The R-Squared 0.9943 for drug release and 0.9985 for swelling index is in reasonable agreement with the formulations. FTIR and DSC indicating compatibility of the drug and polymers in the tablet formulation and patch formulations at the molecular level. The drug release of buccal tablet showed 75.10-99.34% and buccal patches showed 58.41-81.43%. These formulations showed good results when compared to the conventional tablet. Conclusion:Formulation of mucoadhesive sustained release buccal tablets and patches of 5-FU successfully done using different polymers, which would definitely help in increasing bioavailability of the drug.
Background: Triphala, which is a combination of fruits of Terminalia chebula, Terminalia bellerica and Embilica officinalis generally recommended as herbal drug formulation in the Indian traditional medicine system. Study Design: To study the in-silico inhibitory potential of Triphala constituents against cytochrome P450 2E1 (CYP2E1) for the prevention of Thioacetamide-induced Hepatotoxicity Place and Duration of Study: The work has been performed at MUP's College of Pharmacy (B Pharm), Degaon, Risod, Washim, Maharashtra, India in between February 2021 to May 2021. Methodology: We have studied the inhibitory potential of Triphala on CYP2E1 by applying molecular docking tools. The major chemical constituents of Triphala i.e. gallic acid, chebulic acid, ellagic acid, epicatechin, syringic acid, and ascorbic acid were docked on CYP2E1. Results: Docking results revealed the very good inhibitory potential of Triphala in terms of binding affinity towards CYP2E1. All the chemical constituents have formed at least 2 and at most 6 hydrogen bonds with the crystal structure of CYP2E1. The binding energies (kcal/mol) of gallic acid, chebulic acid, ellagic acid, epicatechin, syringic acid, and ascorbic acid are -6.1, -7.1, -9.1, -8.3, -6.3, and -5.7, respectively. Ellagic acid has formed strong hydrogen bonds with Thr-303 and Thr-304 with bond length of 1.98 A0 and 2.26 A0 which confirms the excellent inhibition of CYP2E1. Conclusion: These findings can be used to control the CYP2E1-facilitated biotransformation and drug interactions in the development of new chemical entities. In future, these phytoconstituents can be used as lead molecules to overcome the cancer associated with oxidative stress resulting from the hyperactivity of CYP2E1.
1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives are amongst the family of heterocycles which showed many promising pharmaceutical applications.Extensive literature survey of 1,3,4-oxadiazole scaffold revealed the activities such as antimicrobial, anti-inflammatory, anti-tubercular, anti-oxidant, anti-cancer, anti-convulsant, anti-diabetic and analgesic properties. 1,2,4-oxadiazole, have shown activity against a variety of diseases like Alzheimer's, parasitic worms (helminths) and other internal parasites, edema, infectious diseases, diabetes, pain and cramp, cardiovascular disease, HIV, tuberculosis, antioxidant, cancer, seizure disorders, and arthritis.As oxadiazoles exhibited many different types of pharmacological activities, we reviewed its pharmacological activities reported by different researchers in the field.In present article we reviewed different articles which has been published in English literature. The search engine used to search for the articles were Scopus, Google scholar, Bentham science, Science direct, Tayler and Francis, Springer nature, Frontiers, and Hindawi. Oxadiazole patent applications have grown by 100% in the previous 9 years, reaching a total of 646, making this a highly sought-after compound in the scientific community. From present review we concluded that Oxadiazoles are potent enough to be developed as potential antidiabetic agents more precisely as DPP-IV inhibitors. We believe that present review can provide insight to the researchers working to develop some novel Oxadiazole derivatives as potential antidiabetic agents.
Background and Aims: The outcomes of plexus and peripheral nerve blocks depend on needle-nerve contact and the spread of local anesthetic (LA) around the plexus or nerve. Needle-nerve distance and spread of LA could be visualized during US-guided lumbar plexus block (LPB). Material and Methods: After Institutional Ethics Committee approval and after obtaining informed consent, 24 American Society of Anesthesiologists’-physical status I–III patients who underwent surgical fixation of fractures of proximal femur were enrolled. Spinal anesthesia was a primary anesthetic in all patients. At the end of the surgery, all patients received US and neurostimulation-aided LPB at the third lumbar nerve root (LNr). The primary aim was to determine the spread of LA in the lumbar plexus area with the relation of the needle tip and LNr contact. The secondary aim was to understand block efficacy in terms of pain scores monitored at regular intervals and 100 mg intravenous tramadol was administered as a rescue analgesic if VAS >4. Results: In all 24 patients, we observed an oval and antegrade LA spread after lumbar plexus was identified with neurostimulation at L3. With the needle closer to intervertebral foramina (IVF), a retrograde spread was visualized. Only 2/24 patients received rescue analgesia in the first 24 h. Conclusion: The type of spread after the US-guided LPB could predict block success of block and a possible epidural spread.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.