CNS DEPRESSION POTENTIAL EVALUATION, FORMULATION AND CHARACTERIZATION OF LYOPHILIZED HERBAL ORAL CAKE OF TERMINALIA CHEBULA FRUITS
DOI:
https://doi.org/10.22159/ijpps.2020v12i11.39029Keywords:
Terminalia chebula, Lyophilized herbal formulation, Fourier-transform infrared spectroscopy (FTIR), Locomotors movementAbstract
Objective: Terminalia chebula fruits are used as traditional herbal medicine from the ancient era but still now, the extract has not revealed any research data on CNS depression activity as well as its lyophilized herbal formulation. The present study was designed to evaluate CNS depression activity and develop lyophilized oral cake of Terminalia chebula fruit extract.
Methods: CNS depression potential of Terminalia chebula fruit was examined using the hole board, hole cross, and thiopental sodium induced sleeping time test. The human equivalent dose was calculated based on US FDA guidelines of dose conversion between animals and humans. A novel lyophilized herbal oral cake of aqueous extract of Terminalia chebula fruits with additives was then formulated. The formulated cake was subjected to characterize its physicochemical properties such as appearance, residual humidity, drug content, dissolution, and drug release profile, extract-polymer compatibility by Fourier-transform infrared spectroscopy (FTIR) and stability. The prepared cake was further evaluated with the hole board and hole cross model in mice and compared with control to ensure its CNS depression activity.
Results: Crude extract at the doses of 100, 150, 200, and 400 mg/kg body weight showed significant (p<0.01) dose-dependent inhibition of locomotor behavior. Crude extract dose of 200 mg/kg body weight in mice compared with standard diazepam dose (1 mg/kg) was used to calculate the human equivalent dose of 1000 mg/60 kg. The formulation presented a rapid drug release profile while drug content was approximately 99.5%. FTIR spectroscopy of formulation showed no drug-excipient interaction. The oral cake at the dose of 200 mg/kg body weight showed significant (p<0.01) CNS depression activity.
Conclusion: CNS depression activity, FTIR, and stability analysis ensure the preservation of active ingredients in the lyophilized oral cake as in the crude extract.
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Karunamoorthi K, Jegajeevanram K, Vijayalakshmi J, Mengistie E. Traditional medicinal plants: a source of phytotherapeutic modality in resource-constrained health care settings. Evid Based Complement Alternat Med 2013;18:67-74.
Agra MF, Freitas PF, Barbosa Filho JM. Synopsis of the plants known as medicinal and poisonous in northeast of Brazil. Rev Bras Farmacogn 2007;17:114-40.
Sofowora A. Medicinal plants and traditional medicine in Africa. New York NY, USA: John Wiley and Sons; 1982.
Park HL, Lee HS, Shin BC, Liu J, Shang Q, Yamashita H, Lim B. Traditional medicine in China, Korea, and Japan: a brief introduction and comparison. Evid Based Complement Alternat Med 2012. https://doi.org/10.1155/2012/429103.
Sharma G, Sharma V, Mishra T. Enhancement of in vitro antioxidant potential of Terminalia chebula by various fruit extracts and optimization of concentration by response surface methodology. Asian J Pharm Clin Res 2018;11:228-33.
Bag A, Bhattacharyya SK, Chattopadhyay RR. The development of Terminalia chebula retz. (Combretaceae) in clinical research. Asian Pac J Trop Biomed 2013;3:244-52.
Moussavi S, Chatterji S, Verdes E, Tandon A, Patel V, Ustun B. Depression, chronic diseases, and decrements in health: results from the World Health Surveys. Lancet 2007;370:851–8.
Qureshi NA, Al-Bedah AM. Mood disorders and complementary and alternative medicine: a literature review. Neuropsychiatr Dis Treat 2013;9:639-58.
Swarbrick J. Encyclopedia of pharmaceutical technology. 3rd ed. Florida, USA: CRC Press; 2007.
Anisuzzman M, Hasan MM, Acharzo AK, Das AK, Rahman S. In vivo and in vitro evaluation of pharmacological potentials of secondary bioactive metabolites of Dalbergia candenatensis leaves. Evid Based Complement Alternat Med 2017. https://doi.org/10.1155/2017/5034827.
Uddin SJ, Shilpi JA, Rahman MT, Ferdous M, Rouf R, Sarker S. Assessment of neuropharmacological activities of Pandanus foetidus (Pandanaceae) in mice. Die Pharmazie 2006;61:362-4.
Dehar N, Walia R, Ratol S. Potentiation of thiopentone sodium-induced hypnosis by Berberis aristata in rodents. Asian J Pharm Clin Res 2012;5:131-3.
Yuandani, Suwarso E. Acute toxicity evaluation of ethanol extract of Curcuma manga rhizome. Asian J Pharm Clin Res 2017;10:383-5.
OECD test guideline 423. Acute Oral Toxicity–Acute Toxic Class Method; 2001. p. 1-14.
Nair AB, Jacob S. A simple practice guide for dose conversion between animals and human. J Basic Clin Pharm 2016;7:27-31.
Ahmed IS, Nafadi MM, Fatahalla FA. Formulation of a fast ketoprofen tablet using freeze-drying in blisters technique. Drug Dev Ind Pharm 2006;32:437-42.
Safar R, Abdelwahed W, Chehna MF, Degobert G, Fessi H. Preparation and characterization of new oral lyophilizates containing a non-steroidal anti-inflammatory drug. Int J Pharm Pharm Sci 2011;3:108-14.
Siddiqui MR, Alothman ZA, Rahman N. Analytical techniques in pharmaceutical analysis: a review. Arab J Chem 2013;10:S1409-21.
Corveleyn S, Remon JP. Formulation and production of rapidly disintegrating tablets by lyophilization using hydrochlorothiazide as a model drug. Int J Pharm 1997;152:215-25.
Hua S. Comparison of in vitro dialysis release methods of loperamide-encapsulated liposomal gel for topical drug delivery. Int J Nanomed 2014;9:735-44.
Vigneshwaran N, Ashtaputre NM, Varadarajan PV, Nachane RP, Paralikar KM, Balasubramanya RH. Biological synthesis of silver nanoparticles using the fungus Aspergillus flavus. Mater Lett 2007;61:1413-8.
Takeda H, Tsuji M, Matsumiya T. Changes in head-dipping behavior in the hole-board test reflect the anxiogenic and/or anxiolytic state in mice. Eur J Pharmacol 1998;350:21–9.
Dey P, Chandra S, Chatterjee P, Bhattacharya S. Neuropharmacological properties of Mikania scandens (L.) Willd. (Asteraceae). J Adv Pharm Technol Res 2011;2:255–9.
Moniruzzaman M, Rahman MA, Ferdous A. Evaluation of sedative and hypnotic activity of ethanolic extract of Scorpia dulcis linn. Evid Based Complement Alternat Med 2015. https://doi.org/10.1155/2015/873954
Bernhard L, Qiuying S, Nadia S. The GABAergic deficit hypothesis of major depressive disorder. Mol Psychiatry 2011;16:383-406.
Kavita G, Vijay KL, Shivesh J. Anticonvulsant potential of ethanol extracts and their solvent partitioned fractions from Flemingia strobilifera root. Pharm Res 2013;5:265–70.
Shans-Ud-Doha KM, Mahmud ZA, Bachar SC, Qais N. Antinociceptive, anti-inflammatory, antimicrobial and central nervous system depressant activities of ethanolic extract of leaves and roots of Gomphostemma parviflorum var. parviflorum wall. Pharm Res 2013;5:233–40.
Fernandez S, Wasowski C, Paladini AC, Marder M. Sedative and sleep-enhancing properties of linarin, a flavonoid-isolated from Valeriana officinalis. Pharmacol Biochem Behav 2004;77:399–404.
Kahnberg P, Lager E, Rosenberg C, Schougaard J, Camet L, Sterner O, et al. Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABAA receptor. J Med Chem 2002;45:4188-201.
Datta BK, Datta SK, Chowdhury MM, Khan TH, Kundu JK, Rashid MA, et al. Analgesic, antiinflammatory and CNS depressant activities of sesquiterpenes and a flavonoid glycoside from polygonum viscosum. Pharmazie 2004;59:222–5.
Fernandez SP, Wasowski C, Loscalzo LM, Granger RE, Johnston GAR, Paladini AC, et al. Central nervous system depressant action of flavonoid glycosides. Eur J Pharmacol 2006;539:168-76.
Kumar A, Lakshman K, Jayaveera KN, Tripathi SNM, Satish KV. Estimation of gallic acid, rutin and quercetin in Terminalia chebula. Jordan J Pharm Sci 2010;3:63-8.
Takahashi RN, de Lima TCM, Morato GS. Pharmacological actions of tannic acid; II. Evaluation of CNS activity in animals. Planta Med 1986;52:272-5.
Reddy LH, Ghosh BR. Fast dissolving drug delivery systems: a review of the literature. Indian J Pharm Sci 2002;64:331‐6.
Seager H. Drug-delivery products and the Zydis fast-dissolving dosage form. J Pharm Pharmacol 1998;50:375-82.
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