Journal of Pharmaceutical Technology, Research and Management
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Estimation of Isolated Triterpenoid - Ursolic Acid in Verbena officinalis L. Aerial Parts Using TLC Densitometry
Get PDFVerbena officinalis L. (Vervain; family-Verbenaceae),a traditionally used and medicinally promising plant, has been reported to contain triterpenoids as major class of phytoconstituents. But no work has ever been carried out on V. officinalis to isolate major chemical constituent(s), and to standardize plant material on the basis of isolated constituent(s) using TLC densitometry.The chloroform extract of V. officinalisaerial parts was prepared by extracting properly identified plant in a Soxhlet apparatus.Preliminary phytochemical screening of chloroform extract showed presence of triterpenoids. Column chromatography of chloroform extract using solvent systems viz., hexane:chloroform, chloroform and chloroform:methanol in different concentrationsyielded five fractions (F1- F5). Preliminary phytochemical screening of various fractions of chloroform extract revealed presence of triterpenoids in F2 and F3 fractions. Therefore, these fractions were further subjected to column chromatography. White colored crystals were obtained in SF1 sub-fraction separated from F2and was designated as VOC-1. Structure of VOC-1 was elucidated by IR and NMRspectral studies and was characterized as ursolic acid. Further, ursolic acid was quantified in V. officinalisaerial parts by validated TLC densitometric method. The content of ursolic acid was found to be 0.1580% in V. officinalis aerial parts.The linearity range, correlation coefficient, intra-day precision, inter-day precision, LOD, LOQ and accuracy were found to be 300-1800 ng, 0.997, 1.2% CV, 1.6% CV, 40 ng/spot, 130 ng/spot and 98.27% respectively
Panoramic View on Quality by Design
Get PDFQuality by design (QbD) is an essential tool in pharmaceutical environment for having product/process/method impregnated with quality. Now, QbD is the greatest solution to construct quality in all pharmaceutical products, while in the same time making it as a part of system is also a key challenge for Industry. For understanding of QbD, it is very much essential to understand the desire product performance profile [Target product Profile (TPP), Target Product Quality Profile (TPQP)] and identify critical quality attributed (CQA). Basically, for meeting the product attributes, the product formulation and process can be designed on the basis of these stated parameters. Nonetheless, this helps in recognizing the effect of raw materials, critical material attributes (CMA), critical process parameters (CPP) on the CQAs and identification and control sources of variability. The in and out understanding for QbD in generic pharmaceutical industry is really vital, because now and then FDA is taking firm stand to make mandatory “deadline” for inclusion of QbD. Therefore, an attempt has been made to highlight quality by design for generic drugs and its implications to pharmaceutical industry
Formulation, Optimization and Evaluation of Sustained Release Microspheres using Taguchi Design
Get PDFThe aim of present study is to prepare microspheres of eudragit RL 100 loaded with Nefopam Hydrochloride by single emulsion solvent evaporation technique. Taguchi L9 orthogonal array design has been used to optimize the composition and operating conditions for preparation of formulations. Nine batches (F1-F9) were prepared by taking three independent variables (X1- drug: polymer ratio, X2- stirring speed and X3- stirring time) at three levels (+1, 0, -1). Response variables studied for batches (F1-F9) were mean particle size (μm) (Y1), drug entrapment efficiency (% w/w) (Y2) and drug loading (% w/w) (Y3). Drug- polymer compatibility study was carried out by DSC and FTIR spectroscopy and indicates no physicochemical interaction. Microspheres were analyzed for morphological characteristics, mean particle size, drug entrapment efficiency, drug loading and in-vitro drug release. Percentage cumulative drug release for optimized batch F5 was found to be 85.421 ± 0.054 and followed higuchi model for release of drug
Anxiolytic activity of Angiotensin-Receptor-Blocker in Experimental Models of Anxiety in Mice
Get PDFThe present study aimed to explore the role of Angiotensin- Receptor-Blocker in the management of anxiety. Male Swiss albino mice of age 6-8 weeks and weight 25-30 g were used in the present study. Candesartan (Angiotensin receptor blocker) was administered in two doses (1 and 2 mg/kg; i.p.) to mice for 14 successive days regularly. Anxiety was induced in mice by two different methods: (i) exposing the mice to immobilization stress for a period of 6 h daily for 7 consecutive days; (ii) administration of caffeine (25 mg/kg; i.p.) daily for 7 days. Elevated Zero Maze and Open Field Apparatus were used to evaluate the level of anxiety in different groups. After behavioral evaluation, the animals were sacrificed and their brains were used for estimation TBARS, GSH and Nitrite levels in the brain. Administration of Candesartan (1 and 2 mg/kg; i.p) for 14 successive days significantly (p<0.05) reduced anxiety due to immobilization stress and caffeine induced anxiety. Candesartan (1and 2 mg/kg; i.p) treated mice showed an increase (p<0.05) in GSH levels while a decrease (p<0.05) in TBARS and nitrite levels in brain. Thus, candesartan may prove to be a useful remedy for the management of anxiety owing to its neuroprotective and antioxidant activity
Antihepatotoxic Potential of Citrullus colocynthis Root Extract, Fractions and Isolated Compounds
Get PDFMedicinal plants are considered to be effective and safe alternative treatment for liver toxicity. The article reveals the hepatoprotective activity of the ethanolic extract of the roots of the Citrullus colocynthis commonly known as INDRYAN using carbon tetrachloride (CCl4) experimental model in albino rats. After receiving significant protection of Ethanolic extract on liver the extract further undergone fractionation into three fractions & the activity was localized in the toluene fraction. These on purification led to the isolation of two pure compounds which were identified as - Cucurbitacin B[1] and Colocynthin [2]. The pure compound shows reduction in enzymatic level viz. (SGOT 68.09%, SGPT 63.64%, ALP 76.81%, BL 68.22%) and (SGOT 71.28%, SGPT 65.24%, ALP 80.68%, BL 54.92%) at 50 mg/ kg dose respectively whereas drug Silymarin showed reduction as (SGOT 79.73%, SGPT 74.26%, ALP 87.88%,BL 82.75% ) at 25 mg/kg dose level. On comparing the obtained data it was observed that the roots of C. colocynthis Sch. exhibited significantly better hepatoprotective activity, thus justifying the traditional claims
Pharmacogenomics: Applications in Drug Discovery and Pharmacotherapy
Get PDFPharmacogenomics is the scientific study which explains individual variability of drug targets and to explore the genetic basis for such changes. With the completion of human genomic study, clear relation could now be established between the drug response in relation to a person’s genome. Pharmacogenomics, also known as personalized medicine, uses the person’s genome to determine the dose and dosage regimen, so that therapy could be optimized. As with the techniques like DNA microarray technologies person’s response to a therapy can be predicted and new therapies could be assigned. In the present review, the current technologies, and past significance has been discussed
Resveratrol: Biological Activities and Therapeutic Potential
Get PDFResveratrol is a polyphenolic flavonoid initially identified as a phytoalexin and as a major constituent of red wine. However interest in this molecule initially developed as a cardioprotective agent and in due course of time therapeutic actions came into limelight. This article explores the different therapeutic activities of Resveratrol and highlights their possible mode of action responsible for its therapeutic action. It becomes evident from this article that Resveratrol has a pharmacological agent that has widespread targets and therefore due emphasis on specific biological action need to be addressed using medicinal chemistry and quantitative structure activity relationships in developing new congeners of Resveratrol to be exploited as drugs
Dementia: An Overview
Get PDFDementia is a neurodegenerative disorder characterized by progressive and continuous loss of cognitive functions. The neuropsychiatric symptoms include apathy; agitation and depression. As the disorder progresses, the patient gradually becomes dependent on others to perform routine daily activities. Various underlying diseases or disorders are the root cause of the syndrome of dementia. Each of these disorder or disease is characterized by a specific signs and symptoms in combination with a presumed underlying neuropathology. Alzheimer’s disease is the most prevalent cause of dementia. The second most prevalent cause is vascular dementia. In this review, the clinical types, pathophysiology and pharmacotherapy is summarized
Receptor Identification: Advances in Ligands and Transmitters Discovery
Get PDFReceptor identification is an integral part of drug discovery and development. By the beginning of the next millennium, the search for the natural ligands of the orphan G-protein-coupled receptors will lead to the discovery of so many new peptides that it may well double their present number. It has recently become evident that all types of chemical messengers, hormones and transmitters act through membrane receptors which constitute our largest superfamily of proteins, i.e. the G protein-coupled receptors. The development of targeted therapies has revolutionized the treatment of various chronic diseases. Receptors have well-conserved regions that are recognized and activated by hormones and neurotransmitters. These ligands are peptides, lipids or biogenic amines, and act as transmitter molecules. Identification of orphan receptors include screening, binding and reverse engineering that help to find out cysteinyl leukotriene CysLT1 and Cys T2, hepatointestinal leukotriene B4, motilin, Ghrelin, Growth hormone-releasing peptide and growth hormone secretagogue receptor and many more. Techniques involved in screening of receptors include low stringency hybridization followed by PCR-derived approaches helps to discover various orphan g protein couple recptors (oGPCR). The discovery of the oGPCR represents a hallmark in neuroscience research, and the exploitation of its numerous physiological and pathophysiological functions is a promising avenue for therapeutic applications
Estimation of Total Phenols and Flavonoids in Selected Indian Traditional Plants
Get PDFTraditionally, aerial parts of Abies pindrow Royle (Himalayan Fir; Pinaceae); Abies webbiana Lindl. (Talispatra; Pinaceae); Cephalandra indica Naud. (Ivy Gourd; Cucurbitaceae) and roots of Calotropis gigantea (L.) Dryand (Giant Milkweed; Asclepiadaceae) have been used in the Indian systems of medicine for the treatment of various ailments. But no systematic phytochemical work has ever been carried out on these potential plants. Thus, it was planned to estimate total phenols and flavonoids content in methanol extract, ethyl acetate fraction (EAF) and remaining methanol extract (RME) of selected plants. Properly identified plants were defatted with petroleum ether, and then separately extracted in a Soxhlet apparatus with methanol. The methanol extract of each plant was partitioned by ethyl acetate solvent to obtain EAF of respective plant. The total phenols and flavonoids contents were estimated using standardized procedures. Quantitative determination of total phenols and total flavonoids was done using standard curve of gallic acid (linearity: 20 to 120 mg/ml; r2 = 0.995) and quercetin (linearity: 30 to 180 mg/ml; r2 = 0.997), respectively. EAF of selected plants contained higher content of phenols and flavonoids, where as lowest content was observed in RME of plants. The content of total phenols and flavonoids in selected plants were found to be in order of C. indica > A. webbiana > A. pindrow > C. gigantea. The available literature reveals that polyphenols have been reported to possess varied pharmacological activities. As selected Indian plants contain polyphenols as major class of phytoconstituents, it is suggested that these constituents may be responsible for their medicinal uses