ABSTRACT

Poisoning is a significant global public health problem. Every year, approximately half a million people die world-wide due to poisoning. Immediate poisoning information and management in the early diagnosis, treatment, management, prevention and hazards management of poisoning is provided by specialized unit, Poison Information Center (PIC) through well trained poison information specialist. Poison information service (PIS) also deals with the risk assessment, diagnosis, management and prevention of exposure to any poison, in patients of any age irrespective of type (intentional or accidental) and route of exposure. The effective functioning of a PIC depends on the availability of an adequate volume of evaluated data to furnish a basis for the advice given. A timely provision of poisoning information is appropriate for the poison management which is provided by Poison Information Services as per the needs of the enquirer. Poison information resources are of different types including primary, secondary, tertiary resources. Secondary sources such as Poisindex, Hypertox, Intox and Toxinz are must for the retrieval of quick and updated information. Many of the countries have their own databases for the products available in their region. Thus Poison information resources plays a crucial role in the prevention and management of poisoning cases through provision of information to general public and also to healthcare professionals.

Keywords: Poison Information Center (PIC), PIS, Poison information resources (PIR), Poison information databases (PID)

ABSTRACT

Bioassay is the determination of the relative strength of a substance by comparing its effect on a test organism with that of a standard preparation. It is typically conducted to measure the potency of a new compound, examine effects of the substance on a living organism, essential in the development of new drugs and in monitoring environmental pollutants. Bioassays are broadly of two types: qualitative and quantitative. Qualitative bioassays are used for assessing the physical effects of a substance that may not be quantified, such as abnormal development or deformity. Quantitative bioassays involve estimation of the concentration or potency of a substance by measurement of the biological response that it produces. Bioassay can again be categorized into quantal and graded response. The main aim of bioassay is to provide information that will predict the effect of the drug in the clinical situation. The purpose of bioassay is to ascertain the potency of a drug and to standardize the preparation so that each contains the uniform specified pharmacological activity. Thus, it serves as a pointer in the Commercial Production of drugs when chemical assays are not available or do not suffice and provides a predictive link towards quantitative pharmacology.

Keywords: Bioassay, potency, drug response, drug characterization, Pharmacopoea.

ABSTRACT

Liver disease is a major health problem in all countries, especially in developing countries. The drugs available to treated liver disease may cause further damages. There is an urgent need of some herbal medicines to treat liver disease without causing any further damages. Psidium guajava is one of the important plant in the Myrtaceae family. P. guajava which was reported the antibacterial, antidiarrhoeal, antihyperglycemic, antimalarial, cytotoxic, antioxidant activity etc. The aim of this review to compile the data of the hepatoprotective activity of a P. guajava extract in a recent years.

Keywords: Psidium guajava, Liver, Hepatoprotection.

ABSTRACT

Medicinal plants possess immense traditional applications encompassing antibacterial, antifungal, antiviral, antimalarial, antitumor and many. These diverse curative properties attributed to their phytochemicals which can be obtained from different morphological plant parts. In Sudan, medicinal plants are rather diverse species; pertaining with the diverse climate condition. Four plant species namely, Ambrosia maritima L., Ammi visnaga L., Aristolochia bracteolata L. and Lawsonia inermis L., are widely held in folkloric medicine for the treatment of vast myriad of diseases including solid mass tumor conditions. This review gives a bird’s eye view on the plant species distribution, traditional uses, biological activities and chemical constituents.

Keywords: Ambrosia maritima L., Ammi visnaga L., Aristolochia bracteolata L., Lawsonia inermis L., Solid mass tumor, Sudan

ABSTRACT

Chronotherapeutics is the discipline concerned with the delivery of drugs according to inherent activities of a disease over a certain period of time. Chronotherapy can particularly benefit patients suffering from allergic rhinitis, rheumatoid arthritis and related disorders, asthma, cancer, cardiovascular diseases, and peptic ulcer disease. The biological systems require different amounts of drug at expected times within the circadian cycle. Many therapeutic agents are most effective when made available at constant rates, near the absorption sites or at the correct time of administration. Hence there exists a need for the development of such delivery system that matches the circadian rhythm. With the Chronotherapeutic drug delivery system this requirement can be fulfilled. As these systems deliver the right dose at right time at a specific site, they are gaining importance in the field of pharmaceutical technology. Hence a desired effect at the required time can be achieved by selecting a pulsatile system based on the pathological behavior. And also there will be a reduction in undesirable side effects due to the therapeutic action of the drug delivery system at the time of flare up of the disease symptoms. This review gives a comprehensive emphasis on circadian behavior of certain diseases, various approaches for the chronotherapeutic drug delivery systems and the existing technologies. Pulsatile drug delivery system can be classified as time controlled pulsatile release, stimuli induced and external stimuli pulsatile release systems etc. Still, a significant progress in achieving chronopharmaceutical drug delivery systems for the treatment of diseases in a pulsatile manner.

Keywords:Chronological behaviour, circadian rhythm, Chronotherapeutic drug delivery system, pulsatile release, chronopharmaceutical technologies.

ABSTRACT

The drug delivery through the skin to achieve a systemic as well as local effect of a drug is known as Transdermal drug delivery system. Its main advantage includes controlled drug release with minimum side effects, improved bioavailability and many more. The human skin is readily accessible surface for drug delivery. For penetration of drug through the skin the stratum corneum is the main barrier. So to avoid the stratum corneum and to increase the flux through the skin membrane different techniques of penetration enhancement are used.  This review mainly represents different factors affecting Transdermal bioavailability, technologies for developing Transdermal drug delivery system, different evaluation tests for Transdermal patches, different methods of preparation of TDDS, recent techniques for enhancing Transdermal drug delivery system.

Keywords: Transdermal drug delivery system [TDDS], Controlled release, Enhancement technique.

ABSTRACT

ABSTRACT

The observational study was a retro-selective, unicenter, nonrandomized study to evaluate the clinical safety and efficacy of the stainless steel and cobalt-chromium alloy stent. Use of the cobalt-chromium alloy in place of stainless steel offers enhanced visibility and radial strength with thinner structural elements. The study enrolled 128 patients with symptomatic ischemic heart disease attributable to de novo or restenotic nonstented native lesions of a single vessel amenable to percutaneous stenting. The primary composite end point was the incidence of major adverse cardiac events (death, myocardial infarction, emergency bypass surgery, or target lesion revascularization) 365 days after PCI. The mean age of patient was 56.17 ± 10.43 years, with 50.81% and 47.36% of unstable angina patient. No difference in most clinical angiographic characteristic between two groups. At 1 month follow up there was no significant difference between two groups (p = 0.96). The individual clinical component showed no difference in occurrence of death (p = 0.29), MI (p = 0.29) and TLR (p = 0.96) at end of 6 month. At 1 year MACE occurred 8.1% in cobalt chromium group and 14.0% in stainless steel stent (p = 0.31). Rate of TLR was 0 % in cobalt chromium group and 3.5% in stainless steel stent (p = 0.14). The incidence of restenosis was 3.27 % in cobalt chromium group and 7.01% in stainless steel stent (p = 0.35).

Keywords: PCI, CABG, CAD, MACE, MI, TLR

ABSTRACT

Acacia farnesiana L. Willd (huizache, Mimosoideae, AF) is a leguminous plant possessing diuretic, anti-inflammatory and antimalaria properties. The aim of this study is to investigate the molecular pharmacological activity of aqueous and ethanol extract of AF in inflammatory response. Results showed that aqueous or ethanol extracts of AF reduced the productions of pro-inflammatory factors, including tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), nitrite oxide (NO) and prostaglandin E2 (PGE₂) with dose-dependent manner in murine marcrophage induced by 0.5 μg/ml lipopolysaccharide (LPS). Both aqueous and ethanol extracts did not exhibited cell cytotoxicity at the concentration up to 100 μg/ml. Reverse transcription polymerase chain reaction (RT-PCR) assay indicated that aqueous extract at 10 μg/ml completely inhibited the LPS-induced iNOS gene expression, and at 50 μg/ml suppressed cyclooxygenase 2 (COX-2), IL-6 and IL-1β gene expression. Ethanol extracts significantly blocked iNOS, COX-2, IL1-β and TNF-α gene expression as well, at the concentration of 5 μg/ml, 50 μg/ml and 100 μg/ml, respectively. The ethanol extracts showed more effectiveness in anti-inflammation activity compared with the same dose of aqueous extracts based on the inhibiting activity in iNOS expression. However, both types of extracts had no effect on the expression of COX-1. In conclusion, our present findings showed the anti-inflammatory activity of AF against RAW264.7 cells in vitro, and that both aqueous and ethanol AF extracts possess good anti-inflammatory activity. The molecular mechanism of the bioactivity of AF may be through down-regulating the gene expressions of inflammatory related factors.

Keywords: Acacia farnesiana, pro-inflammatory, nitrite oxide, marcrophage

ABSTRACT

The present research work was to design and develop an optimized oro-dispersible tablet dosage form of an anti-psychotic drug, Olanzapine by using direct compression technology.  Total number of nine formulations were prepared as per the standard experimental design protocol using Design Expert Software (Version 8.0.5, Stat-Ease, Inc.). Independent variables such as the amount of the amount of Crospovidone XL 10 (A) and the amount of Avicel PH 102 (B) were optimized by application of Response surface methodology using Central Composite Design. The dependent variables selected were in-vitro dispersion time and wetting time of the tablets. All the evaluated physical parameters of the oro-dispersible tablets were practically within control. The direct compression method used to prepare the oro-dispersible tablets in this study is relatively simple, safe and economic. A stable, effective and pleasant tasting mouth dissolving tablet, which has a good balance over all the physical parameters was formulated.

Keywords: Oro-dispersible, Superdisintegrants, Crospovidone, Response Surface Methodology.

ABSTRACT

Pulse crops, rich in flavonoids and polyphenolics possess not only free radical scavenging properties but also they are highly safe in the treatment of many diseases. Quantitative determination of phenols and flavonoids in seed coat, dehusked raw dal, dehusked cooked dal and whole seed of locally grown red lentil (Lens culinaris L.) was carried out using spectrophotometric methods. The amount of total phenols were analysed by using Folin-Ciocalteau assay and the amount of total flavonoids were analysed using aluminium chloride calorimetric assay. Gallic acid and catechin reagents were used as the standards For the calibration of phenols and flavonoids respectively. Hydrophillic and hydrophobic phenols were also estimated to confirm total phenolic composition. Orthodihydric phenols were analysed by Arnow’s method. Free radical scavenging efficiencies and antioxidant activities were analysed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and ferric thiocyanate (FTC) assay respectively. Among the four treatments, seed coat extract showed highest scavenging activity followed by whole seed, dehusked raw dal and lowest found in dehusked cooked dal extracts in terms of their EC₅₀ values. The results from analysis of variance (ANOVA) revealed that total phenolic content (TPC), total flavonoid content (TFC) and antioxidant properties varied among the different methanolic extracts significantly (p<0.05). Moreover, a highly significant correlation (p<0.05) between antioxidant activities/free radical scavenging efficiencies and phenolic contents as well as favonoids was observed. The results concluded that the lentil seed extracts may be valuable natural antioxidant sources and are potentially applicable in both medicine and healthy food industry.

Keywords: Lentil, antioxidant, flavonoids, phenolics, free radical scavenging activity.

ABSTRACT

A simple, rapid, sensitive, reversed phase-HPLC method was developed and validated to measure simultaneously the amount of Metformin and Vildagliptin at single wavelength (210 nm) in order to assess quantification in its tablet formulation and its subsequent stability studies. An isocratic elution of filtered sample was performed on Hypercil BDS C18 column with buffered mobile phase (0.1 M potassium dihydrogen ortho Phosphate buffer (Ph 4.8) and acetonitrile in the ratio of 60:40 v/v) with Hypercil BDS detection at 210 nm. The linearity for concentrations between 12.5μg/ml–75μg/ml for Metformin and 1.25μg/ml – 7.5μg/ml for Vildagliptin were established.  The limits of detection (LOD) and quantification were 1.75 and 5.29 µg/ml for metformin and 0.46 and 1.39 µg/ml for vildagliptin. The determination of the two active ingredients was not interfered by the excipients of the products. This method was satisfactorily applied to the analysis of the tablet formulations and proved to be specific and accurate for the quality control of the cited drugs in tablet dosage form.

Keywords: RP-HPLC, Metformin, Vildagliptin, 0.1 M potassium dihydrogen ortho Phosphate buffer.

ABSTRACT

Plants use multiple defense mechanisms in order to prevent entering of phytopathogenic microorganisms. In many plant species one of the most efficient responses to combat attacking microbes is the rapid synthesis of antimicrobial low molecular weight phytoalexins, for example, stilbenes produced by several plants may be a useful lead structure for the chemical synthesis of antimicrobials. In this study, a series of novel 2, 4, 5-trimethoxy stilbene derivatives have been synthesized via the Wittig reaction. The starting material 2, 4, 5- trimethoxy benzaldehyde (asaronaldehyde) was obtained from β-asarone of sweet flag oil. The key intermediate 2, 4, 5-trimethoxybenzyltriphenyl phosphonium chloride was prepared for the first time from the corresponding benzyl chloride. All the trans-stilbenes were characterized by HRMS, ¹H and ¹³C NMR spectral analysis and tested in vitro for their fungicidal activity against two plant pathogenic fungi viz., Phytophthora capsici and Sclerotium rolfsii.

Keywords: Sweet flag oil, 2, 4, 5-Trimethoxybenzyltriphenyl phosphonium chloride, Stilbenes, Wittig reaction, Antifungal

ABSTRACT

Weeds are considered troublesome and undesirable component leading to enormous reduction in crop yield, wastages of resources and human energy. An attempt has been made to evaluate the effect extracts of four obnoxious weeds, Argemone mexicana, Parthenium hysterophorus, Cyperus rotundus Lin., Verbesina encelioides on the mitotic activity of germination of mung beans. Metabolites were extracted in methanol, acetone , hexane and distilled water using soxhlet extraction and assayed for the presence of bioactive metabolites. Presence of terpenes, flavonoids and quinines were observed in the methanol extract of all the weeds and hexane extracts indicated the presence of glycosides and flavonoids. Based on percentage inhibition studies, it was found water extracts followed by acetone extracts for all the weeds were most potent as a growth inhibitor. Argemone Mexicana and Parthenium hysterophoresus were found to be most potent in inhibiting mitotic activity and growth although statistical significance (P<0.05) was prevalent only in Argemone Mexicana.

Keywords: Mitotic inhibitors, seed germination, seedling growth, secondary metabolites

ABSTRACT

The present study will focus mainly on the new series of 1,2,3- triazoles linked with 7-amino-4-methyl coumarin (4) are synthesized using Click reaction. All the newly synthesized compounds (7a-q) are characterized by analytical and spectroscopic methods (IR, HRMS, ¹H and ¹³C-NMR) and subjected to cytotoxicity screening against a panel of six different human cancer cell lines viz. Hela, PANC1, HepG2, SKNSH, MDAMB and IMR 32 cell lines. Interestingly, among the tested molecules, some of the analogs displayed better cytotoxic activity. Out of the synthesized triazoles (7a-q), compounds 7h, 7i and 7l showed potent activity, as 7h and 7l showed more potent activity against IMR32 cell line with GI₅₀ of 0.015 and 0.02 μM, respectively and 7i with GI₅₀ of 0.02 μM against SKNSH cell line. Further photophysical properties (UV & fluorescence) for these compounds (7a-q) are also discussed.

Keywords: 1,3-Dipolar cycloaddition, 1,2,3-Triazole, Cytotoxic & photophysical properties.

ABSTRACT

This study examines the sustained release behaviour of venlafaxine hydrochloride from Hydroxyl propyl methyl cellulose & sodium carboxy methyl cellulose. Venlafaxine hydrochloride is an antidepressant agent. The present research endeavor was directed towards the development of a sustained release dosage form of venlafaxine in the form of tablets to be taken once daily. All lubricated formulations were compressed by direct compression. The compressed tablets were evaluated for uniformity of weight, content of active ingredient, friability, hardness, thickness and In-vitro dissolution study. Release studies were carried out using USP type 2 apparatus in 900 ml of Distilled Water as dissolution media. Release kinetics were analyzed using zero-order, Higuchi’s square root and Peppa’s exponential equations. All formulations showed compliance with pharmacopoeial standards. Among different formulations F7 showed sustained release of drug for 12 hours with 99.73% of drug release respectively. The regression coefficient value of zero order plots was found to be 0.993. The slope of peppas model was found to be 0.981 for F7.Thus the matrix system of HPMC & SCMC was found to be effective in retarding release of venlafaxine hydrochloride.

Keywords: Venlafaxine hydrochloride, HPMC & SCMC,CDR(Cumulative drug release), SR

ABSTRACT

A simple, specific, accurate and precise reverse phase high performance liquid chromatographic method is developed and validated for the estimation of Dapsone in tablet dosage form. The expected separation and peak shapes were obtained on Luna C18, 15 cm x 4.6 mm (5 μm)  column. To have an ideal separation of the drug under isocratic conditions, mixtures of solvents like methanol and water with or without different buffers indifferent combinations were tested as mobile phases on a Luna C18, 15 cm x 4.6 mm (5 μm) column. A mixture of Methanol:Water in the ratio of 40:60 v/v was proved to be the most suitable of all the combinations since the chromatographic peak obtained was better defined and resolved and almost free from tailing.  The flow rate was 1.0ml/min and effluents were monitored at 260 nm. The retention time for Dapsone was ± 2.4 min. The method was validated for accurate, precise, simple, sensitive and rapid and can be applied successfully for the estimation of Dapsone in bulk and in pharmaceutical formulations without interference and with good sensitivity. And recovery of Dapsone from tablet formulation was found to be 93%. The proposed method was successfully applied for the quantitative determination of Dapsone in tablet formulation.

Keywords: Dapsone, HPLC, Linearity, Validation, 260 nm

ABSTRACT

An easy solvent-free synthesis of pyrimidine derivatives from aldehydes, aceto acetanilide and urea/thiourea by using fluorspar mineral as catalyst has been described under microwave irradiation. The salient features of this one-pot protocol are short reaction times (4-5 min), excellent yields, cleaner reaction profiles and simple work-up. Also, the catalyst can be reused without any reduction in efficiency.

Keywords:  Biginelli reaction, Pyrimidines, Fluorspar catalyst, Microwave irradiation.

ABSTRACT

Acyclovir has low bioavailability mainly due to low solubility. In this study, solid self-nanoemulsifying drug delivery systems (S-SNEDDS) of acyclovir were developed with the objective of improving its solubility. Initial screening was carried out to select the excipients. Ternary phase diagrams were constructed to detect the nanoemulsification region. The nanoemulsion systems selected from the phase diagram were characterized for their robustness to dilution and cloud point temperature. Box- Behnken design was then applied for further optimization. The formulations obtained were further characterized for their droplet size and entrapment efficiency. The best formulation was converted to S-SNEDDS by simple adsorption technique. The liquid SNEDDS (L-SNEDDS) was adsorbed onto microcrystalline cellulose in 1:1 ratio. Zeta potential, differential scanning calorimetry, scanning electron microscopy was then carried out. In vitro drug release was studied by comparing the S-SNEDDS with pure drug. The L-SNEDDS formulation which was converted to S-SNEDDS showed particle size of 147 nm. The formulation was found to be robust to dilution and showed cloud point at 86 ◦C. Negative zeta potential meant, there was no coalescence of globules. SEM studies of nanoemulsion demonstrated that the globules in L-SNEDDS were indeed adsorbed on the MCC. Results of DSC confirmed that the drug was incorporated in the S-SNEDDS that was formulated. The in vitro drug release from acyclovir S-SNEDDS was found to be considerably higher in comparison to that of the pure drug. Therefore, it can be concluded that acyclovir loaded S-SNEDDS improved the solubility and release characteristics of the drug.

Keywords: Acyclovir, Self nanoemulsifying drug delivery systems (SNEDDS), Box-Behnken design, Powder SNEDDS

ABSTRACT

Antimicrobial’s efficiency is critically compromised by the emergence and spread of antimicrobial resistance, yet they are valuable therapeutics. Investigations were carried to test and analyze the antimicrobial susceptibility of E. coli isolates from Ajmer poultry farm. 24 tissue samples containing 6 liver, 12 small intestine, and 6 large intestine samples were processed for isolation and identification and characterization of pathogenic E. coli from 12 fowls of 4 selected poultry farms of Ajmer suspected for colibacillosis and subjected to detailed bacteriological and biochemical examination. 24 E. coli isolates were isolated following standard procedures. E. coli isolates found to be highly resistant to some of the classical drugs like tetracycline, amoxy clav, carbenicillin, cotrimoxazole and cefopodoxime and found to be highly sensitive (100%) to the remaining drugs, which is disclosed by antibiogram study. The most ineffective antibiotic drug was found to be tetracycline for all the E. coli isolates, as all these microbes were found 100% resistant to it. Multiple resistance to at least 2 to 4 antibiotics were observed in all the 24 isolates. 50% of the isolates were resistant to at least 4 antibiotics and 75% to at least 3 antibiotics and 25% to at least 2 antibiotics. Results from this study revealed the high prevalence rate of multidrug resistant E. coli isolates. It may suggest that the high resistance of E. coli to antibiotics constitutes a threat not only to poultry industry of Ajmer but also possesses a serious threat to public and animal health with adverse economic implications.

Keywords: Antimicrobial, Therapeutics, Multidrug resistance, Antimicrobial susceptibility, Colibacillosis, Antibiogram.

ABSTRACT

The purpose of the present study was to evaluate the efficacy of the Photodynamic therapy in addition to the classical treatment with scaling root planing compare to subgingival chlorhexidine irrigation. A 20 patient of chronic generalized periodontitis with probing depth more than 5mm, were included in the study. According to split mouth design, for one quadrant scaling and root planning with Photodynamic therapy was performed and other side scaling and root planning with chlorhexidine irrigation was done as a control group. A statistically significant difference in median Gingival Index score over a period of 20 days from baseline was observed  in  the site of the test group as compared to control site. The present study supports the treatment approach of Photodynamic therapy an adjunct to routine scaling and root planning. Photodynamic therapy is as efficient and safe to be used in addition to root planing when compared to sub gingival irrigation with scaling and root planning.

Keywords: Photodynamic Therapy, Periodontitis, Scaling and root planing

ABSTRACT

The anti-diabetic effect of aqueous and ethanol extract of leaves of Eugenia operculata Roxb. was evaluated in streptozotocin induced diabetic mice. Streptozotocin is a synthetic nitrosoureido glucopyranose derivative isolated from fermentations of Streptomyces acromogenes. STZ induced diabetes by selectively destroying the insulin producing β cells by inducing necrosis. Extract (250mg/kg b.w) was administered orally to albino mice both normal and diabetic for 21 days. The anti-diabetic potential was assessed by determining oral glucose tolerance, fasting blood glucose, urine glucose, change in body weight, liver glycogen content and serum lipid profile. In oral glucose tolerance test, reduction of fasting blood glucose level was observed after 60 minutes of extract and standard administration. At the end of experiment maximum reduction of blood glucose level was seen significantly (p<0.001) in ethanol treated group when compared with diabetic group and (p<0.05) with aqueous treated at a dose of 250mg/kg b.w. The body weight of treated diabetic mice was also seen regained as compared to diabetic control. Serum lipid levels reversed towards near normal and gradual decrease of urine glucose level. The extract treatment also showed a significant increase in the liver glycogen content. The results show that leaves of Eugenia operculata possess significant anti-diabetic activity.

Keywords: Eugenia operculata, Anti-diabetic, Medicinal plant, Streptozotocin, Mice.

ABSTRACT

A series of novel triazole fused thienopyrimidine derivatives are synthesized by Gewald reaction, which are well characterized by IR, ¹HNMR, ¹³CNMR and Mass spectral analysis. These compounds are screened for their in vitro anti-tubercular and antibacterial activities. Most of these compounds exhibited MIC values in the range of 20 – 100 µM against Mycobacterium tuberculosis H37Rv. In the series, compound 5c was most active with MIC 20 µM. Furthermore, the title compounds were screened for antibacterial activity against Staphylococcus aureus ATCC 29213 (gram positive) and Escherichia coli ATCC 25922 (gram negative) bacteria. Some of these compounds exhibited MIC values in the range 8 - 64µM. Compound 5c was found to be the most active with an MIC of 5 and 8µM respectively.

Keywords: Gewald reaction, Thienopyrimidine, Triazolothienopyrimidine, Anti-tubercular activiy, Anti-bacterial activity.

ABSTRACT

Anti diabetic screening of Methanolic extract of Cirullus lanatus (MECL) was done by various in vitro methods. Preliminary phytochemical screening, total phenolic and flavonoid content, tannin content and estimation of Vitamins (B₁, B₂ and C) were done by standard procedure. TLC & HPTLC of MECL was done by using Quercetin, Gallic acid and Catechin as a standard. Screening of in vitro anti diabetic activity was done by Inhibition of α-amylase & α-glucosidase enzyme assay, Glucose uptake in yeast cells and Non - enzymatic glycosylation of Hemoglobin assay. Preliminary phytochemical screening showed the presence of carbohydrates, triterpenoids, proteins, alkaloids, tannins, saponins, flavonoids, sterols and absence of glycosides, volatile and fixed oil. The amount of Phenolic content (in terms mg GAE/g of extract), Flavonoids (mg Quercetin equivalent/g of extract) and Tannin content (mg Tannic acid/g of extract) present in the MECL were found to be 47.05±0.338, 89.99±0.30 and 290.9 ± 0.12mg/g respectively. The amount of Vitamin B₁, B₂ and C of MECL were found to be 56.28 ± 0.004, 245.37 ± 0.06 and 34.00 ± 0.009mg/g respectively. TLC & HPTLC qualitative estimation confirmed the presence of Quercetin, Gallic acid and Catechin in MECL. In Non-enzymatic glycosylation of hemoglobin assay, IC₅₀ value was found to be 65.648µg/ml and 59.762µg/ml for MECL and α-Tocopherol respectively. MECL exhibited significant inhibition of glycosylation as compared with the standard drug α-Tocopherol. Glucose uptake assay in yeast cells, IC₅₀ value was found to be 77.031µg/ml and 67.408µg/ml for MECL and Acarbose respectively. MECL showed greater efficiency in increasing the glucose uptake by yeast cells as compared to standard drug Acarbose. Inhibition of α-amylase enzyme assay, IC₅₀ value was found to be 58.558µg/ml and 47.880µg/ml for MECL and Acarbose respectively. MECL showed significant α-amylase activity as compared to Acarbose. In α-glucosidase inhibition assay, IC₅₀ was found to be 627.270µg/ml & 482.188µg/ml for MECL and Acarbose respectively. Overall MECL showed significant in vitro anti diabetic activity may be due to Phenolic, Flavonoid, Vitamin and Tannin content. MECL may be used as good candidate for diabetic treatment. Furthermore, in vivo studies are required for providing scientific information on the plant.

Keywords: Citrullus lanatus, Cucurbitaceae, Water melon, in vitro anti diabetic activity.

ABSTRACT

The Present study was undertaken with an aim to formulate delayed release enteric coated tablets of Tenatoprazole to avoid the degradation in stomach, as it is an acid labile drug and to improve bioavailability. The method adopted for development was direct compression. Different core tablets were prepared by using approved excipients and evaluated for parameters like hardness, friability, thickness and disintegration time. Sub coating was done for the optimized formulation (F5) by using Hydroxy propyl methyl cellulose 5cps with buildup of 3%w/w and finally enteric coating was done by using polymers like Hydroxy propyl methyl cellulose phthalate (HPMCP), Eudragit L30 D55 and Hydroxy propyl methyl cellulose acetate succinate (HPMCAS) with an average weight build up of 5%, 8% & 10% w/w. All the formulations were evaluated for their physicochemical parameters and compared with marketed sample. Results indicated that all the tablets prepared possess good integrity, desirable for enteric coated tablets. At the end it was found that prepared formulation gave satisfactory results compared with market sample dissolution profile. Among the polymers studied, the methacrylic acid polymers exhibited better dissolution rate than the cellulose polymers. The selected formulation (F5h with 8% w/w) was subjected for stability studies as per ICH guidelines and were found to be stable, as no significant change was observed in the evaluated parameters. Hence prepared formulation by-pass the degradation of Tenatoprazole by enteric coating and thus a pharmaceutically equivalent, robust formulation of Tenatoprazole enteric coated tablet was developed.

Keywords: Tenatoprazole, sub-coating, enteric coating, HPMCP, Eudragit L30 D55, stability studies.

ABSTRACT:

Hydroethanolic extract of Ricinus communis flowers was studied for treating diabetes induced oxidative stress in adult male swiss albino mice. The experimental animals were divided into four groups of seven mice each viz., Normal Control (NC), Diabetic Control (DC), Diabetic + R. communis Flower extract treated (FT) and Diabetic + Glibenclamide treated (GT). The groups DC, FT and GT were given a single intraperitoneal injection of Alloxan monohydrate (150 mg/kg body weight). Alloxan administration induced destruction of beta cells, hampering production of insulin and aggravating blood glucose levels. It also resulted in over-production of Reactive Oxygen Species (ROS) and thus oxidative stress. Groups NC and DC received normal saline while FT was given Ricinus Communis Flower Extract (RCFE) at 300 mg/kg body weight and GT was treated with Glibenclamide, for a period of 45 days. Fasting Blood Glucose (FBG) levels were observed at regular intervals. After the treatment period, the liver, kidneys and pancreas of the experimental animals were estimated for their antioxidative status. The antioxidant markers such as Catalase (CAT), Glutathione peroxidase (GPx), reduced Glutathione (GSH) and Superoxide dismutase (SOD) saw a variation from their normal values. Treatment of Alloxan induced diabetic mice with RCFE for 45 days lead to a significant (P<0.05) normalization of FBG levels and antioxidant parameters. Hence, indicating its protective effects against diabetes induced oxidative stress.

Keywords: Ricinus communis, RCFE, Diabetes, Oxidative stress, Reactive Oxygen Species, Antioxidant.

ABSTRACT

A HPLC method for simultaneous estimation of Ramipril and Hydrochlorothiazide in tablets was developed and validated. The developed method involves Purosphere^® Star Rp18e, 5μm, 150×4.6mm column with mobile phase composition of acetonitrile and sodium perchlorate (pH 2.5) buffer in the ratio of 3:2, at a flow rate of 1.0 ml/min and UV detection at 316nm for first five minutes for Hydrochlorothiazide and 210nm for Ramipril. The method was validated as per ICH guidelines, Linearity was observed over concentration range of 17.5 to 32.5 µg/ml for Ramipril and 87.5 to 162.5 µg/ml for Hydrochlorothiazide. The Accuracy of the proposed method was determined by recovery studies and found to be 97.95-102.3% and 97.98-102.66% for Ramipril and Hydrochlorothiazide respectively. The proposed method was extended for estimation of Ramipril and Hydrochlorothiazide in marketed tablet formulation (Ramace-H^TM) and it was found to be well within the acceptance limit. The developed and validated HPLC method for simultaneous estimation of Ramipril and Hydrochlorothiazide was found to be linear, accurate, precise, robust and rugged. Hence it can be used for routine analysis of Ramipril and Hydrochlorothiazide in tablets.

Keywords: HPLC, Ramipril, Hydrochlorothiazide, Ramace-H^TM.

ABSTRACT

To Evaluate the Prescribing Pattern of different types of Chronic Headache in a tertiary Care Hospital. 63 patients were the subjects in Medicine Department of a Multispecialty Hospital, in Greater Noida. It was a duly approved, prospective study, in patients on chronic Headache therapy, conducted by competent professionals. The data was obtained from physicians’ prescribing records and patients by individual interviews using the structured proformas as per World Health Organization guidelines. In 63 patients, suffering from different types of headache were evaluated. Among the 63 patients suffering from headache 17(26.98%) were males and 46(73.01%) were females, indicating 3:1 (Female: male) prevalence ratio of headache. Out of 63 patients of chronic headache, age range of 31-40 years had the maximum number 22(34.92%) of patients, followed by 21(33.33%) in age range of 21-30 year. Among the 63 patients suffering from headache Out of 31 patients diagnosed of migraine headache 23(74.19%) were females and 8(25.86%) were males, indicating prevalence of migraine 3 times more in females than in male. NSAIDs (100%) were the most prescribed abortive treatment followed by ergotamine 22(34.92%) and prochlorperazine 22 (34.92%). Among the opoid analgesics caffeine 22(34.92%) was mostly prescribed followed by tramadol 13(20.63%). Sumatriptan 9(14.28%) was less prescribed. The prospective study demonstrated that the incidence migraine headache was found to be higher in female patients. NSAIDs were the most prescribed abortive treatment followed by ergotamine 22(34.92%) and prochlorperazine22 (34.92%) Among the opoid analgesics caffeine was mostly prescribed followed by tramadol.

Keywords: Prospective, Headache, NSAID, Migraine

ABSTRACT

This study investigate uropathogenic species isolation and characterization in the population of Mansehra. The different physical chemical and microscopic properties of urine samples were examined. Isolated uropathogen organism were selected for antibiotic suceptibility and resistance pattren. Thirty seven clinics were visited to collect the data regarding the UTI patients among these nine Bacterial species were isolated from 32 urine samples which included bacterial species Escherichia coli, Enterrobacter spp. and Staphylococcus aureus. Different biochemicals tests were used for identification. The confirmed isolated bacteria were also tested against selected antibiotics for sensitivity and resistant strains. The result of present investigation revealed that UTI is most common infection among local population of Mansehra. The efficacy of antibiotics calculated and found that Ciprofloxacine, Chloramphenicol, Norfloxacine were sensitive against all isolated bacteria while Cefixime, Cefipime, Linkomycine, Sulfamethaxazole trimethoprim and Nitrofurantion  were resistant while Tobramycine and  Pipperacilline Tazobactum were intermediate. The efficacy of some antibiotics is also questionable because the efficacy of these antibiotics were found resistant and it was also found that common strains  of UTI causing Bacteria were resistant against prescribed antibiotics in District Mansehra.

Keywords: UTI, E.coli, antibiotics, Resistance, uropathogen

ABSTRACT

Lebanese scabiosaprolifera(Carmel Daisy) was used to remove Pb (II) free ions from aqueous solutions. The adsorption process was found to be dependent on pH, Temperature, contact time, adsorbent dose and concentration. The maximum adsorption capacity was obtained at pH 5 after 1 hour at 25 ͦC. Langmuir and Freundlich isotherms were employed to interpret the adsorption behavior, with a better fit to Langmuir. This adsorption is a spontaneous process with applicability to pseudo second order kinetic model. It was concluded that scabiosaprolifera is an effective, low cost and environmentally friendly adsorbent.

Keywords: scabiosaprolifera, Adsorption, Isotherms, Kinetics

ABSTRACT

The authors proposed a simple, rapid and sensitive liquid chromatography / tandem mass spectrometry assay method for the determination of nateglinide in human plasma using carbamazepine as internal standard (IS). Analyte and the IS were extracted from the human plasma via liquid-liquid extraction using ethyl acetate. The chromatographic separation was achieved on a C₁₈ column by using a mixture of 0.1% formic acid buffer –acetonitrile buffer (20:80, v/v) as the mobile phase at a flow rate of 0.8 mL/min. The calibration curve obtained was linear (r² ³ 0.99) over the concentration range of 10.0–10005 ng/mL. Method validation was performed as per FDA guidelines and the results met the acceptance criteria. The proposed method was found to be applicable to pharmacokinetic studies.

Keywords: Nateglinide; Liquid-liquid extraction (LLE); LC-MS/MS; Method validation; Pharmacokinetics

ABSTRACT

Lactic acid bacteria are a group of gram positive, non-sporing, cocci or bacilli, which produce lactic acid as the major end product in carbohydrate fermentations. Lactic acid bacteria were isolated from different diary sources . Disease causing pathogenic bacteria from clinical specimen were collected. Antimicrobial activity of the above pathogens were tested with a set of conventional antibiotics by the disk diffusion method. Antibacterial effects of the lactic acid bacteria against the above bacterial pathogens were done by agar well diffusion method. 10 pathogenic bacteria, resistant to minimum of three antibiotics  were selected for the study. Results of antibacterial activity of the lactic acid bacteria in the study revealed, a varying type of  inhibition, which was later used for comparison. The study was performed to check whether Lactic acid bacteria could be used in patients with antibiotic resistance.

Keywords: Lactic acid bacteria, Bacteriocins, Antibiotics, Antibacterial activity, Antibiotic resistance

ABSTRACT

Orally disintegrating tablet are gaining popularity over conventional tablets due to their convience in administration and suitability for patients. The purpose of the research was to mask the intensely bitter taste of tramadol hydrochloride and to prepare orally disintegrating tablets for achievement of quick onset of action of the drug. Tramadol hydrochloride is an analgesic which has been prove to be efficient in managing relief from pain and including pain after surgery. In the present study an attempt has been made to prepare bitter less orally disintegrating tablet of tramadol hydrochloride using Eudragit EPO as a taste masking agent. Direct compression method was used for preparing tablet & super disintegrating agent like Crosspovidone, Crosscarmellose sodium and sodium starch glycolate were used to prepare blend and evaluated for pre-compression parameter such as bulk density, compressibility, and angle of repose etc. the prepared batches of tablets were evaluated for hardness, weight variation, friability, drug content, disintegration time and in-vitro dissolution profile was found to be satisfactory. It was found that Eudragit EPO being hydrophilic facilitated the increase in the uptake of the saliva thus showing the complimentary action of that superdisintegrant.

Keywords: Tramadol hydrochloride, superdisintegrant, orally disintegrating tablet, Eudragit EPO.

ABSTRACT

The aim of present work was to develop pulsatile release dosage form for chronotherapy of hypertension. Considering the biopharmaceutical, pharmacodynamics reasons of Valsartan and circadian rhythm of hypertension a time controlled rupturable tablet, which allowed the release of Valsartan in time controlled release manner was developed for treating early in the morning surge of blood pressure. Core tablet for formulation were prepared using direct compression technique and evaluated for various parameters like % drug content, hardness, thickness, friability and In-vitro disintegration time. To get desired lag time and release profile to achieve pulsatile delivery tablets were coated with ethyl cellulose: Eudragit L100 (3:1), containing dibutyl phthalate and magnesium stearate. Coated tablet was evaluated for in vitro dissolution study, Drug content and rupture time. Optimization was done by using 3² full factorial design by using conc. of croscarmellose in core and coating level as independent variables and rupture time or lag time as dependent variable. Formulation F-5 was found to optimized formulation containing 5% of superdisintegrant in core tablet and 5 % coating level. From the study it is also concluded that Increase in coating level increases lag time & increase in concentration of superdisintegrant decreases lag time.

Keywords: Pulsatile, Chronotherapy,Superdisintegrant, Optimization.

ABSTRACT

Achyranthus aspera Linn, Moringa oleifera Lam and Scopharia dulcis Linn are used in the traditional system of medicine for the treatment of many diseases. Achyranthus aspera (AA) the whole plant and especially the roots, characterized by their uterine stimulant activity, are prescribed in the therapy of rheumatism, lumbago, osteodynia, dysuria, post-partum haematomata and dysmenorrhoea. There is no doubt that the pure Moringa oleifera (MO) Tree leaf is the source of incredible health benefits. It's the ultimate, natural, organic, energy and endurance health supplement. Scopharia dulcis (SD) plant has long held a place in herbal medicine in almost every tropical country where it grows, and it is much used by indigenous people. In this present work the flavonoid and phenolic content of the three plants were estimated. Then the  anti inflammatory activity of the plants were evaluated by Carrageenan induced   paw oedema method with alcoholic and aqueous extracts of the plants and the Analgesic activity was evaluated by Acetic Acid Induced Writhing Test Method. The plants are having very good significant effect in the Anti-inflammatory and Analgesic activity and it  may be due to the presence of flavonoids .

Keywords: anti-inflammatory, paw oedema, Carregeenan, Writhing.

ABSTRACT

The real (ε’) and imaginary (ε’’) parts of the complex dielectric constant (ε*) of different unsaturated edible oils were measured at different temperatures ranging from 30 ⁰C to 70 ⁰C at 9.435 GHz microwave frequency. The X-band setup in the TE₁₀ mode with slotted section and crystal detector were used for this measurement. The values of dielectric constant and dielectric loss show remarkable variation with temperature. It observed that the dielectric constant and dielectric loss are different for different oils, due to their different physical and chemical properties.

Keywords: Microwave X-band, Dielectric constant, Dielectric loss.

ABSTRACT

Bacopa is the genus in which the Indian medical herb Brahmi (Bacopa monnieri) is included, which have been reported to have memory enhancing effect. Bacopa monnieri and Bacopa caroliniana are orthologous in nature. In the present study the effects of ethanolic extract of Bacopa caroliniana on behavioural changes of Albino rats in normal and stress induced rats was investigated. The animals were divided into 3 group’s control, low dose (75mg/kg) and high dose (150mg/kg).Rats in each of these groups were sub divided into 2 groups i.e., with stress and without stress. The animals in stress induced group were forced to swim in a cylindrical vessel containing water at room temperature (28˚c) i.e., chronic mild stress. After the treatment period, the rats of each group were trained on Cooks pole climbing apparatus, Elevated plus maze and on Stair case to assess cognitive improving activities. The results showed improvement in learning performance and enhanced memory retention in rats treated with Bacopa caroliniana extract when compared with control group. The in vitro antioxidant activity was carried out to correlate its protective effect against stress, significant inhibition against DPPH & Nitric oxide radicals were observed with extract in dose dependent manner and the results were compared with that of standard Gallic acid.

Keywords: Bacopa caroliniana, Oxidative stress, Cognition.

ABSTRACT

Aavaraivithaadhi Chooranam is the classical Siddha medicine used in the treatment of Diabetes mellitus. The aim of the present study was to standardize the Siddha herbal drug formulation Aavaraivithaadhi chooranam by subjecting the drug to various studies like analyzing its organoleptic character, Physicochemical and Instrumental analytical studies like Scanning Electron Microscope (SEM), Energy Dispersing X-Ray Analyser (EDAX) and Fourier Transform Infrared Spectroscopy (FTIR) and the results were noted. The Total Ash value was10.2 %±0.25, Acid Insoluble Ash value was 07.9 %±0.74, Water soluble ash value was 3.4 %±0.08, Alcohol soluble Extractive was 5.78% ±0.39, water soluble ash value was8.18% ±0.58; Loss on drying at 105^ºc was 0.0566 %±0.007. The SEM analysis shows the presence of micro particles and its morphology and topography is revealed, EDAX results shows the presence of compounds such as Carbon, Oxygen, Zinc, Magnesium, Calcium, Iron, Potassium, Silica which is responsible for its activity. FTIR analysis revealed the functional groups present through the bonds and stretches which may be the reason for its therapeutic effect. Standardization is an important analytical tool for the identification of the drug. This study brings the effective standardization of the Siddha Herbal formulation through the standard modern analytical studies thus bringing the siddha drug to the next level.

Keywords: Standardization, ash values, SEM, EDAX, FTIR spectroscopy

ABSTRACT

The present study was aimed to evaluate the antiovulatory activity of the Siddha polyherbal formulation Maavilingathy Mathirai in female Wistar albino rats. Female adult mature non pregnant Wistar albino rats weighing 120 to 200 g with at least three regular estrous cycles were administered two doses of 100 and 200 mg/kg orally for 15 days and the control group received 2 ml/kg of CMC solution. On the 16^th day all the animals were sacrificed. The effect of the drug on estrous cycle was studied. The proestrous phase of the rats at dose levels of 100, 200mg/kg were found to be highly significant (P < 0.01) when compared with the control. The decrease in median duration of the estrous phase of the rats at dose levels of 100, 200mg/kg were found to be highly significant (P < 0.01) when compared with the control. Metestrous phase was also significantly reduced at dose levels of 100, 200mg/kg as compared to the control and the p value was found to be extremely significant.The results also showed that the p value of ovarian weight at dose levels of 200 mg/kg was found to be highly significant. The cholesterol value of the ovarian tissue at the doses of 100, 200 mg/kg were found to be significant (p<0.05) when compared with the control.Hence the drug proved to have a better antifertility effect on the administration of 100, 200 mg/kg dose levels.

Keywords: antiovulatory, Maavilingathy Mathirai, estrous phase, Wistar albino rats

ABSTRACT

Investment is the process of ‘Sacrificing something now for the prospect of gaining something later. It is an economic activity which involves creation of assets or exchange of assets with profit motive. Eventhough utmost care should be taken by the Individual investors while making investment decisions. Because sometimes emotions such as fear and greed may play a vital role while making their investment decisions. Keeping this in mind the authors in this paper make an attempt to analyse the attitude of the individual investors on select investments in Chidambaram taluk of cuddalore district. The study has been conducted among 100 individual investors living in different parts of Chidambaram taluk through a structured questionnaire. There is a general view that the research work should even be understood by the young budding research scholars. Keeping this in view no statistical tools have been used in this research paper.

Keywords: Investments, Individual Investors, investment decisions, Attitudes.

ABSTRACT

Medication error is an essential variable to determine patient safety. So it is crucial to realize the bottle necks of care giving. Studies proved that the role of clinical pharmacist can attribute to positive outcomes in patient care. The main objective is to assess the impact of the interventions provided by clinical pharmacist in the medical wards. Secondary objectives comprise of evaluating the impact of intervention in the patients with renal failure, assessing the acceptance by physician and estimating the effect of intervention in cost saving. The set of interventions collected are regrouped into various categories like indications, safety, dosing and miscellaneous. Under each category, sub-categories are listed and their respective percentages are explained using pictorial representation. Also, the acceptance rate of the interventions by the physician is calculated. The cost saving accrued because of the interventions is estimated to look into to know how the role of clinical pharmacist can help the patients economically. The interventions are regrouped into: indication – 36.3 %; safety – 40.8 %; dosing – 16.03 % and miscellaneous – 6.8 %. Majority of the interventions are given for safety and the acceptance rate of the interventions by the physicians is high – 87.2 %. It is also found that 40 % of these interventions accrued to cost saving to the patients. There is a possibility of multiple benefits, by allotting a clinical pharmacist for every medical team in the ward. This strategy helps the patients to gain better health care and cost saving.

Keywords: Intervention, Adverse Drug Reaction (ADR), International Normalized Ratio (INR), Acceptance Rate, Clinical Pharmacist.

ABSTRACT

Context: Inhalation of drugs like salbutamol sulphate (SBS) suffers from low pulmonary deposition due to its micronized size. Objective: (a) to develop submicronic-SBS respiratory fluid, (b) pre-clinical toxicity study, (c) in-vitro and in-vivo evaluation in terms of respiratory fraction, and (d) clinical study to assess safety and efficacy. Methods: Formulation was optimized on basis of particle size and in-vitro nebulization rate. Anderson cascade impaction (ACI) was done to validate its advantage in terms of respirable fraction. Effect on cardiopulmonary parameters (spirometry, pulse-oxymetry, echocardiography and 6-minute walk test) was evaluated and compared with control (n=12). In-vivo pulmonary deposition pattern was compared using gamma scintigraphy. Results: Formulation was optimized with average particle size of 410nm. SBS was radiolabeled with Tc-99m and ^99mTc-SBS was found suitable for estimating in-vivo SBS deposition. Preclinical toxicity studies in two-animal species showed no biochemical or behavioural toxicity. In-vitro ACI data showed high respirable fraction (81.7±7.1%) in comparison to control (42.5±3.8%). In-vivo scintigraphy suggested significantly higher pulmonary deposition for test formulation in comparison to control. Better improvement in cardiopulmonary parameters was seen in test treated group. Conclusions: As demonstrated for SBS, nano-sizing may enhance regional pulmonary deposition and provide an attractive therapeutic option for bronchopulmonary disorders like COPD.

Keywords: Chronic obstructive pulmonary disease; submicronic salbutamol sulphate; nebulization; gamma scintigraphy

ABSTRACT

Nootropic drugs used as a memory enhancer can improve thinking, memory, and alertness in people with Alzheimer’s disease and other disease that affect the mind. Memory is perhaps the most vital of all aspects that differentiates human beings from other animals. However, memory can become faulty due to several reasons, and in that case the person is not able to make full use of his or her potentials. Since ages, drugs and natural remedies have been prescribed to enhance memories in people. 4 million people are thought to be suffering from age related memory and increased risk of developing Alzheimer’s disease. The present study investigate the nootropic activity of poly herbal methanolic extraction (Rhodiola Rodantha Root, Blepharis Maedeterpensis Root, Celastrus Paniculatus Plant seed, Brassica Caulorapa  Bud) by using Active avoidance paradigm, Passive avoidance paradigm, Scopolamine-induced amnesia,  Sodium nitrite intoxication method to assess the nootropic activity.

Keywords: Nootropic activity, Alzheimer’s disease, RhodiolaRodantha, Blepharis Maedeterpensis, Celastrus Paniculatus, Brassica Caulorapa

Abstract

The objective of this study is to select between native and treated guar gum as tablet disintegrant and to explore the possible influences of disintegrant content and production method on different tablet attributes using promethazine-HCl as a model drug. Tablet batches were formulated according to 2³ full factorial design in which each of the selected factors was investigated at two possible levels for their individual and combined influences on tablets properties. Native and treated gum were considered for guar gum type, guar content was examined at 2 and 8%w/w whereas dry and wet granulation were selected as levels for tablets production method. Guar gum content was demonstrated to affect weight variation, thickness variation and friability properties of different tablet batches (p ranged 0.012-0.038). Guar gum type was also established to influence weight and thickness variation as well as disintegration and drug dissolution properties (p ranged 0.025-0.039). Influences of production method on weight variation, thickness variation, friability, disintegration and drug dissolution properties were found to be considerable (p< 0.05, for all effects). None of the investigated factors has measured a significant effect on tablet hardness property (p ranged 0.4511- 0.9214 for the effects of all factors). Compared to native guar gum, treated guar gum was found to be more efficient as a tablet disintegrant (p= 0.039). Formulations including 2 or 8% w/w treated guar gum and processed by dry granulation were found to yield tablets with average short disintegration time (5.0 ± 0.9 min) and enhanced dissolution efficiency (0.805 ± 0.005).

Keywords: Guar gum; Treated guar gum; Tablets' properties; Dry granulation; Wet granulation.

ABSTRACT

A new, simple, accurate, precise and reproducible RP-HPLC method for the simultaneous estimation of Sitagliptin Phosphate Monohydrate and Simvastatin has been developed and validated. Chromatographic separation was achieved using Neosphere C-18 column (4.6 mm 250mm,5mm) in gradient mode with a mobile phase consisting a mixture of acetonitrile:methanol:0.1% orthophosphoric acid in water (70:15:15v/v) at a flow rate of 1ml/min. The eluents were detected at 254 nm using UV detector. The retention time of Sitagliptin Phosphate Monohydrate and Simvastatin were found to be 2.09min and 7.79min respectively. The method was linear over the concentration range of 25-150μg/mL for Sitagliptin Phosphate Monohydrate and 10-60μg/mL for Simvastatin. The % recoveries for Sitagliptin Phosphate Monohydrate and Simvastatin were found to be 98.98-101.06% and 99.89-102.43% respectively. The developed method was validated for parameters like system suitability, specificity, linearity, accuracy, precision, ruggedness and robustness as per International Conference on Harmonization guidelines and the results were found to be within the limits. This validated method can be used for the routine quality control analysis of Sitagliptin Phosphate Monohydrate and Simvastatin in combined dosage form.

Keywords: Sitagliptin phosphate monohydrate, Simvastatin, Reverse-phase high performance liquid chromatography, Simultaneous estimation, Validation.

ABSTRACT

Clitora ternatea is a disease resistant plant used in ethno-pharmacological preparations for its high therapeutic value of primary and secondary metabolites. The aim of this study was to investigate the amount of quercetin in plant parts of Clitoria ternatea and its antifungal activity on dermatophytes. To obtain chemical pattern of flavonoids and quercetin in different plant parts, the extraction solvent was standardized and a finger printing profile of flavonoid was established by means of high performance liquid chromatography (HPLC). The greatest amount of flavonoid was observed in methanolic extracts of C.ternatea flowers while the lowest level was found in the C.ternatea stem extracts, whereas HPLC fingerprinting of flavonoids in flowers was significantly different from stem and leaf extracts. These extracts also differ in their fungicidal capacity against dermatophytes tested, although they all showed significant antifungal activity against Candida sp.. and Aspergillus sp.. flower extracts showed concentration dependent strong inhibition on growth of Microsporum gypseum and Epidermophyton floccosum, and weak inhibition on Trichophyton metagraphytes. The results of this study will be used to promote application of C.ternatea for improving human health by providing antidermatophytic effect on skin infections.

Keywords: Quercetin, Clitoria ternatea, HPLC, Antidermatophytic, Flavonoids.

ABSTRACT

This study investigated the spherical agglomeration of itraconazole for enhanced drug dissolution rate and bioavailability at various polymers percentage like 0.2%, 0.4%and 0.6% with Soluplus®, HPMC and PEG-4000 by simple stirring at 900 r.p.m. (The spherical agglomerates(SA) were dried powdered and with method followed by characterized by differential scanning calorimetry and X-ray powder diffraction. The SAs of itraconazole were also evaluated by drug content study, solubility study and in-vitro dissolution study. The pharmacokinetic studies of the formulations and pure itraconazole were evaluated i.e. Cmax, Tmax and AUC   in vivo study by pharmacokinetic model on wistar rats.

Keywords: Itraconazole, Spherical Agglomeration, Dissolution, Bioavailability.

ABSTRACT

The present research work was aimed to enhance the solubility and dissolution rate of Olanzapine using Poloxamer as carrier by preparing solid dispersion. The solid dispersions and physical mixtures prepared was also evaluated  for the drug content and percentage drug yield and characterization of prepared systems is done with the help of in-vitro drug release, FTIR, XRD and DSC analysis. The results obtained showed that the percentage yield and percentage drug content was 98.32% and 99% respectively. It was clear that there was no loss of drug and polymer. The rate of dissolution of the drug in the case of solid dispersions was much enhanced as compared to the pure drug and their physical mixtures. FTIR spectra showed that there was not any interaction or hydrogen bonding between the drug and polymers in solid dispersions as well as physical mixtures. The polymorphic changes were studied with the XRD gave the idea that the solid dispersions were quite amorphous in nature as compared to the pure drug. In the diffraction pattern for solid dispersions, the number of crystalline peaks due to drug had disappeared. DSC showed that there was shifting in melting endotherm of drug in case of solid dispersion. From the XRD and DSC it was confirmed that the increase in the solubility and dissolution rate was due to polymorphic transition of drug from crystalline to amorphous form.

Keywords: Solid Dispersion, Olanzapine, Poloxamer-407, Dissolution

ABSTRACT

In the present study structure based virtual screening of compound data base, prediction of activity of high extra precision glide docking scored (XPGS) molecules by atom based 3D QSAR model, XP glide docking analysis of known inhibitors to know the key residue interactions and ADME study of identified Histone Deacetylase 2 (HDAC2) inhibitors were performed. A 3D QSAR model was build for both training set (R² = 0.9867, SD= 0.104, F= 322.1 and N= 17) and test set (Q² = 0.9137, Pearson r= 0.9671, RMSE = 0.160, N = 7) molecules and showed a statistically significant and good predictive model. The visualization of 3D QSAR model suggested that introduction of hydrogen bond donor group in 5-position of pyridine ring, 6-position of 1,2-diaminobenzene ring; hydrophobic groups in the 2,4-position of pyridine ring, 5,6 -position of 1,2-diamino benzene ring, 2,3,5,6-position of amonomethylbenzamide ring of highest active compound 1 were suitable to increase the HDAC2 inhibitory activity. The XP glide docking analysis of the known inhibitors showed that residues PHE-155, Gly-154, His-145, His-146, Asp-104 and Zn-ligand interaction in the active site region play a crucial role for inhibitory activity. The activity of high glide scored molecules resulted from virtual screening were predicted by atom based 3D QSAR model. After prediction of activity the molecules were subjected to ADME study to know the drug likeness properties and reported 10 molecules having XPGS > 12.0 and predicted activity > 6.7 as potent HDAC2 inhibitors. The docking interaction of known inhibitors was also similar to the docking interaction of identified ten potent inhibitors.

Keywords: HDAC2 inhibitors, Virtual Screening, 3D QSAR, Docking, ADME study

ABSTRACT

Target drug delivery is beneficial for the delivery of pharmaceutical product to its appropriate site and with the resurgence in the use of herbal therapies as health care medication and this new field of drug delivery holds intensive research. The purpose of the current study was to design, gastroretentive  mucoadhesive tablets using powdered leaves of Murraya koenigii and to optimize  a product using natural gums and their combinations. The gastroretentive, boiadhesive drug delivery prolongs the residence time of the dosage form at the site of absorption and facilitates an intimate contact of the dosage form with the underline absorption surface and thus contribute to improve and/or better therapeutic performance of the drug and shows promising future in enhancing the bioavailability and specific needs by utilizing the physiochemical characters of both the dosage form and the mucosal lining Gastroretentive, mucoadhesive tablets using powdered leaves of Murraya koenigii were prepared using direct compression method and evaluated for parameters such as Weight variation, Hardness, Friability, Drug content, Swelling index, In –vitro drug release study, In – vitro and In – vivo mucoadhesive strength. Different types of natural gums such as Carbopol, Hydroxypropyl methylcellulose (HPMC) and a gas – generating agent (Sodium bicarbonate) were used. The investigation shows that the tablet composition and mechanical strength have the greatest influence on the floating properties and the drug release. With the incorporation of a gas – generating agent, along with the polymers, increased optimum floating (floating lag time to 30 minutes, and the duration of floating > 8 hours ). The drug release was also increased and was sufficiently sustained (more than 8 hours) and non –Fickian transport of the drug was confirmed.

Keywords: Gastroretentive, mucoadhesive, Murraya koenigii, natural gums.

ABSTRACT

1,4-Benzothiazine derivatives having variable antifungal activity against four species of fungus such as Candida albicans, Trichophyton rubrum, Epidermophyton floccosum and Malassazia furfur  were selected to develop 2D and 3DQSAR models. The best 2DQSAR model was selected, having correlation coefficient r² (0.8747) and cross validated squared correlation coefficient q² (0.7145) with external predictive ability of pred_r² (0.9658). 2DQSAR parameters are Quadrople1, SssCH2count, XA Average hydrophobicity, X Amost hydrophilic area and Polar surface area excluding P and S contributed in the model. The best 3DQSAR model having the correlation coefficient r²= 0.8635 was selected for further study. The model was further validated by means of crossed squared correlation coefficient q² =0.7614 and pred_r² =0.6654, which show that the model has good predictive ability and was developed by Forward SW-MLR. From QSAR model it concluded that the bulky substitution is require at para and meta position of Phenyl ring and less bulky substitution at ortho position of phenyl ring for antifungal activity.

Keyword: 2DQSAR, 3DQSAR, Antifungal, 1,4-Benzothiazine, Vlife MDS and MLR

ABSTRACT

A novel, convenient, accurate, precise and reproducible reverse phase high performance liquid chromatography was developed and validated for the estimation of Vilazodone in bulk and pharmaceutical tablet dosage form. Objective was achieved under optimized chromatographic conditions on Shimadzu LC-20AT Prominence Liquid Chromatograph with Welchrom C₁₈ isocratic column, (250 mm × 4.6 mm i.d., particle size 5 μm, maintained at ambient temperature), is used as stationary phase. An isocratic mode with mobile phase consisting of Acetonitrile: Water (50:50 v/v), with apparent pH of 3.3, at a flow rate of 1.0 mL/minutes. The effluent was monitored at 240 nm using Shimadzu SPD-20A prominence UV-Vis detector. The retention time of Vilazodone was found to be 4.103 minutes. The linearity range was found to be 1-5 μg/mL with correlation coefficient (R²) is 0.999. Validation parameters such as specificity, linearity, precision, accuracy, and robustness, limit of detection (LOD) and limit of quantitation (LOQ) were evaluated for the method according to the International Conference on Harmonization ICH Q2 (R1) guidelines. The LOD and the LOQ were found to be 0.044 μg/mL and 0.135 μg/mL respectively. Recovery of Vilazodone was found to be in the range of 99.80 % - 99.92 %. The method was validated statistically using the % RSD and the values are found to be within the limits. Therefore this method was conveniently and easily applied for the quantitative determination of Vilazodone in pharmaceutical dosage forms.

Keywords: Vilazodone, LOD, LOQ, Recovery studies, ICH guidelines.

ABSTRACT

The Present study was carried out to study the larvicidal efficacy of Aedes aegypti on ethanol, ethyl acetate, petroleum ether and aqueous extracts of Hemidesmus indicus root. The root extract of Hemidesmus indicus with different solvents were tested for their phytochemical constituents. The analysis revealed the presence of Steroids, terpenoids, flavonoids, and carbohydrates in most prominent amount. Larval mortality was observed and recorded after 24, 48, 72 hours exposure periods. All the tested extracts showed moderate to good larvicidal activities. However, the maximum larval mortality was in aqueous extract of Hemidesmus indicus root observed at 72 hours. The LC₅₀ and LC₉₀ values of  Hemidesmus indicus root against the 1^st and 2^nd , 3^rd and 4^th instar larvae of Aedes aegypti LC₅₀136.74,LC₉₀ 259.16 ppm and LC₅₀ 101.09, LC₉₀ 198.92 ppm respectively. These results revealed that larvicidal properties of Hemidesmus indicus root and encourages further effort to investigate the bioactive compounds in those extracts that might possess good larvicidal properties when it will be isolated in pure form.

Keywords: Hemidesmus indicus®, Aedes Aegypti, Phytochemical, Larvicidal Activity.

ABSTRACT

A simple, accurate, precise and stability-indicating RP-HPLC method has been developed and validated for the simultaneous estimation of Telmisartan and Chlorthalidone in fixed-dosage formulation. The separation was achieved on a octadecyl C-18 reversed phase column (Symmetry C-18, 250mm x 4.6mm , 5µ) using acetonitrile:phosphate buffer at pH 6.5 (70:30 v/v) as mobile phase at a flow rate of 1.0mL/min and temperature of 25°C. The UV detection was carried out at 270nm. The retention time of Chlorthalidone and Telmisartan was found to be 5.48 and 13.38 min. respectively. The method has been validated for Specificity, Linearity, Accuracy, Precision and Robustness. The calibration curve for Chlorthalidone and Telmisartan were linear from the range of 1.25-20.01 µg/mL and 8.0 to 128.4 µg/mL respectively. The mean recoveries obtained for Telmisartan and Chlorthalidone were 100.9% and 99.7% respectively. The developed method was found to be Specific, accurate, Precise, Robust and rapid for the simultaneous estimation of Telmisartan and Chlorthalidone in Telmisartan and Chlorthalidone Tablets 80mg/12.5mg.

Keywords: Telmisartan, Chlorthalidone, RP-HPLC, Simultaneous estimation, Method development and Validation.

ABSTRACT

A simple, precise, rapid and specific reversed phase high performance liquid chromatographic method for determination of S (-) Metoprolol Succinate was developed and validated. The chromatographic separation was achieved on Inertsil ODS column (125×4.6mm, 5µ), using a mixture of 20mM potassium dihydrogen phosphate (pH adjusted to 3.5 with ortho-phosphoric acid) and acetonitrile as mobile phase in the ratio of 80:20 at flow rate of 1.5 mL/min. The detection was performed at 220 nm. The calibration curve was linear in the range of 30 - 90 µg/mL (r² = 0.99999). Major impurities and degradation products were well separated from S(-) Metoprolol Succinate. Thus this assay method can be considered as stability-indicating.

Keywords: S (-) Metoprolol Succinate, Stability-indicating assay, RP-HPLC.

ABSTRACT

In order to achieve rapid action and sustained release, we have fabricated dual type of mini-tablets of Diclofenac Sodium enclosed in a single capsule. 10 formulations of rapid release (IF1-10) mini tablets were prepared using sodium starch glycolate, Cross povidone and Micro crystalline cellulose. 12 formulations of sustained release (SF1-12) mini tablets were prepared by using HPMC, carbopol, Ethyl cellulose, xanthan gum and guar gum. All formulations were evaluated for pre-compression and post-compression parameters. Drug Excipient interaction was determined by FTIR, Short term stability studies were carried out at 40 ⁰C /75 % RH for 3 months. Pre-formulation and studies conformed that all formulations showed better flow property. In vitro studies showed that all mini tablets in combination released more than 55 % within 30 min whereas marketed tablet Voveran SR 100 showed only 11 % release indicating the rapid drug release and the release was extended up to 80 % in 20^th hour indicating the sustainability of the release. Natural polymers, Xanthan gum and guar gum containing formulations showed above 90 % in 12^th hour indicating little rapid drug release when compared to synthetic polymers. FTIR report indicated no interaction of drug with excipients. Stability studies showed no significant loss in drug content, release profile and physical appearance. Hence it can be concluded that, the release profiles duel type mini tablets were quite promising for once a day formulation.

Keywords: Diclofenac Sodium, capsules, rapid release mini-tablets, sustained release mini-tablets.

ABSTRACT

The present study reports the physiochemical and biological parameters of water and identification of organisms present in Kolavai Lake, Tamil Nadu, India. The lake is heavily polluted due to the dumping of municipal and agriculture wastes from surrounding localities.  Water samples were collected from different places across the lake and examined. Eleven microorganisms were identified by primary and secondary biochemical assays and two bacterial samples were sequenced with 16S rRNA regimen to identify the species. Obtained results were compared with standard values. The new bacterial species identified belonged to taxa Brevundimonas nasdae and Microbacterium trichothecenolyticum which are uncommon in this area.

Keywords: Kolavai Lake, Pollution, 16S rRNA, Brevundimonas nasdae, Microbacterium trichothecenolyticum.

ABSTRACT

Fishes adopt themselves to some extent when natural waters have high BOD, heavy metals and ozone contamination. The present work studied the effects of hypoxia, anoxia, ozone, copper sulphate and a combination of copper sulphate + ozone on the lipid and hematological profiles of  Clarias batrachus. In case of lipid profile, total cholesterol level (195.5 ± 1.5) was highest in normal condition, triglyceride (204 ± 3.162), HDL (38 ± 1.224) and VLDL (40.75 ± 1.478) in 2 hour hypoxia, and LDL (129 ± 2.236) in copper sulphate + ozone treated condition. Analysis of blood samples showed elevation Hemoglobin level (9.7 ± 0.070) was highest in 4 hour hypoxia condition, RBC count ( 3 ± .070) and glucose level (186.75 ± 1.478)  in 2 hour hypoxia , PCV percentage (28 ± 0.707) in anoxia , and total protein in normal (6 ± 0.070) and 2 hour hypoxia (6 ± 0.141) conditions.

Keywords: Hypoxia, Anoxia, Ozone, Copper Sulphate, Lipid profile, RBC, Heamoglobin,  Clarias batrachus.

ABSTRACT

A new series of novel derivatives of pyrazole were synthesized. These derivatives were identified on the basis of melting point range, R_f values, IR and ¹H NMR spectral analysis. The derivatives were screened for antibacterial activity. All derivatives exhibited significant to moderate antibacterial activity.

Keywords: Antibacterial Activity, R_f values

ABSTRACT

In most parts of Nigeria, traditional medicine practitioners and most rural dwellers use plant parts for treatment of ailments without scientific proof. This study was designed to investigate the antimicrobial activities of the aqueous and ethanol root extracts of Anogeissus leiocarpus against Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 10145, Bacillus subtilis NCTC 8236, Staphylococcus aureus ATCC 25923, Candida albicans 24433 and clinical isolates of Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus, Klebsiella spp and Candida albicans. The antimicrobial assays were carried out using the agar ditch diffusion and agar well diffusion methods. Statistical analysis was done using two way anova without replication. The ethanol extract inhibited all organisms and had lower minimum inhibitory concentrations (MIC) compared to the aqueous extract (P < 0.05). Staphylococcus aureus recorded the lowest MIC in ethanol and aqueous extract while Klebsiella spp had the highest MIC in ethanol extract. The aqueous extract had no activity against Candida albicans ATCC 24433. The use of this plant root alone and in combination with other plants by herb medicine practitioners for the treatment of infectious diseases can therefore be justified. However further work should carried out to isolate the active component that furnishes the understudied plant with its antimicrobial potential and as well determine the toxicity of the plant.

Keywords: Antimicrobial activity, Minimum Inhibitory Concentration, Anogeissusleiocarpusand Criprofloxacin.