Background: Tetrabenazine (TBZ) is the only US Food and Drug Administration-approved drug for the treatment of chorea related to Huntington's disease and other hyperkinetic disorders. TBZ was first synthesized in 1950, and was then used for the treatment of psychosis. But later its potential in treating hyperkinetic disorders was proved by its ability to block vesicular monoamine transporters 2 and deplete monoamine stores. There is still lack of awareness about the therapeutic potential of this drug. Summary: TBZ had been approved only for the treatment of chorea, but several clinical studies have been conducted by different research groups and it was concluded that TBZ is effective in various other conditions such as tardive dyskinesia, dystonia, tics, and Tourette's syndrome, thus, highlighting the need for further clinical trials in these conditions. Key Message: The intention of this review is to sum up the information regarding chemistry, mechanism of action, pharmacokinetics, interactions, contraindications, adverse effects, and clinical efficacy of TBZ in diseases other than Huntington's chorea.
Background:Theobjective of the present study was to evaluate the anti-inflammatory activity of aqueous extract of Mirabilis jalapa Linn. (MJL)(Nyctaginaceae) leaves for scientific validation of the folklore claim of the plant. The leaves are used as traditional folk medicine in the south of Brazil to treat inflammatory and painful diseases. Cosmetic or dermo-pharmaceutical compositions containing MJL are claimed to be useful against inflammation and dry skin. Methods:Aqueous extract of the leaves was prepared by cold maceration.Results:The anti-inflammatory activity was evaluated using carrageenan and formalin-induced paw edema models in Wistar albino rats. The anti-inflammatory activity was found to be dose dependent in carrageenan-induced paw edema model. The aqueous extract has shown significant (P < 0.05) inhibition of paw oedema, 37.5% and 54.0% on 4 th hour at the doses of 200 and 400 mg/kg, respectively. Similar pattern of paw edema inhibition was seen in formalin-induced paw edema model. The maximum percentage inhibition in paw edema was 32.9% and 43.0% on 4 th day at the doses of 200 and 400 mg/kg, respectively.Conclusion:The results of present study demonstrate that aqueous extract of the leaves possess significant (P < 0.05) anti-inflammatory potential.
Multifactorial metabolic diseases, for instance diabetes develop several complications like hyperlipidemia, hepatic toxicity, immunodeficiency etc., Hence, instead of mono-drug therapy the management of the disease requires the combination of herbs. Marketed herbal drugs comprise of irrational combinations, which makes their quality control more difficult. Phytoconstituents, despite having excellent bioactivity in vitro demonstrate less or no in vivo actions due to their poor lipid solubility, resulting in high therapeutic dose regimen; phospholipids encapsulation can overcome this problem. Hence, present study was designed to develop a phospholipids encapsulated polyherbal anti-diabetic formulation. In the present study, polyherbal formulation comprises of lyophilized hydro-alcoholic (50% v/v) extracts of Momordica charantia, Trigonella foenum-graecum and Withania somnifera 2:2:1, respectively, named HA, optimized based on oral glucose tolerance test model in normal Wistar rats. The optimized formulation (HA) entrapped in the phosphatidylcholine and cholesterol (8:2) vesicle system is named HA lipids (HAL). The vesicles were characterized for shape, morphology, entrapment efficiency, polar-dispersity index and release profile in the gastric pH. The antidiabetic potential of HA, marketed polyherbal formulation (D-fit) and HAL was compared in streptozotocin-induced diabetic rat model of 21 days study. The parameters evaluated were behavioral changes, body weight, serum glucose level, lipid profile and oxidative stress. The antidiabetic potential of HA (1000 mg/kg) was at par with the D-fit (1000 mg/kg). However, the potential was enhanced by phospholipids encapsulation; as HAL (500 mg/kg) has shown more significant (P < 0.05) potential in comparison to HA (1000 mg/kg) and at par with metformin (500 mg/kg).
Nowadays, the use of natural polymers as an alternative to synthetic gastro-retentive polymers is increasing. Such natural raw materials are highly biocompatible and biodegradable with no or significantly fewer side effects and are economical too. The main aim of this research work was to design a gastro-retentive tablet of Captopril by using Maize Stem Pith (MSP) powder and Jowar Stem Pith (JSP) as novel natural low-density polymers and also to sustain the drug release for up to 12 hours. Our objective behind this research is to prepare the gastro-retentive tablet, evaluate it for floating behavior, and to achieve the sustained release effect for at least 12 hours. The novelty of this research work is that MSP powder and JSP powder possesses low density. Thus, gastro-retentive tablets with a low-density (floating) approach can be prepared at a very lost cost compared to the currently marketed formulation. Gastro-retentive tablets of Captopril were designed by using MSP and JSP powder. Using design-expert® version 13, the formulations were prepared using a 32-complete factorial design. The gastro-retentive tablet showed good floating behavior and dissolution pattern, which sustains the release of the drug for up to 12 hours. The optimization study using a contour plot and response surface plot suggested that formulation R9 is an optimized batch among all batches. The current research indicated that there is an increase in floating time with a corresponding decline in the dissolution rate of the tablet as the concentration of MSP powder and JSP powder increases. The optimized formulation R9 consists of MSP powder and JSP powder at 12% and 8 %, respectively, in combination with HPMC (K-100M), and has proven excellent floating behavior and expected drug release pattern. Therefore, MSP powder and JSP powder could be used as suitable low-density novel polymers to design gastro-retentive tablets of Captopril.
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