Abstract

A series of new 2-(phenylthio) phenyl substituted carbamate (3a-d) and N-(2-(phenylthio) phenyl substituted sulfonamide derivatives (5a-d) were synthesized from 2-(phenylthio) aniline (1) using various pharmacologically active carbonochloridates (2a-d) and sulfonyl chlorides (4a-d) in the presence of a mild base. The structures of all the newly synthesized compounds were characterized by the IR, NMR (1H & 13C) and mass analysis. Further, all the synthesized compounds were screened for the antimicrobial activity. Among all the tested compounds, 3c and 5b showed potent antibacterial and antifungal activities and these compounds might be used as antibiotic drugs.

Abstract

The objective of this study was to demonstrate the significant difference in the rate of amylase production when different carbon, nitrogen and oil cakes were used for the amylase production. To this end, bacterial strain (AVMB1) isolated from Chilli rhizosphere was screened for Amylase production and identified as genus Bacillus by morphological, physical, physiological, biochemical and molecular characterization by partial 16S r RNA gene sequencing. α-amylase enzyme production was quantitatively characterized from the Bacillus strain and optimized the culture conditions for bioprocessing under submerged fermentation with different organic sources. The production of amylase was increased by 35-60% under optimized conditions of 35°C, pH7.0 with maltose as carbon sources and yeast extract as nitrogen sources respectively after 48 hrs of incubation. Soya bean oil seed cake induced maximum amylase production.

Abstract

The field of Ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. The most frequently used dosage forms i.e. ophthalmic solutions and suspensions are compromised in their effectiveness by several limitations, leading poor ocular bioavailability. In situ hydrogels are instilled as drops into the eye and undergoes a sol to gel transition in the cul-de -sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop pH-triggered an ophthalmic drug delivery system using combination of gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride,a fluoroquinolone antibiotic. With the advent of new generation of flouroquinolones such as Moxifloxacin HCl, the treatment of gram positive bacterial infections has been achieved.  In situ gels were prepared by simple dispersion method using carbopol along with HPMC in factorial design  and then evaluated for pH, gelling capacity, drug content, rheological, gel strength and  in-vitro diffusion studies and comparison with marketed eye drop formulation along with statistical studies.  Among formulation batches F1- F9; optimized formulation F6 imparted sustained release property to the gel formed in situ and effective other evaluation parameters. The developed formulations were therapeutically efficacious, stable, non-irritant and provided sustained release of the drug overcoming convential drawbacks leading to better patient acceptance.

Abstract

Caesalpinia digyna rottler is used in the treatment of hypertension, inflammation, diabetes, hepatotoxicity. In the present study methanolic extract of Caesalpinia digyna Rottler root (MECD) at doses of 200 and 400 mg/kg was evaluated on N-nitro-L-arginine methyl ester (L-NAME) induced hypertensive rats by observing blood pressure and heart rate. The anti hypertensive activity of the MECD were studied using a non-invasive rat tail-cuff blood pressure system.The MECD produced significant decrease (p<0.01) in systolic blood pressure (SBP), diastolic blood pressure (DBP) and heart rate on L-NAME induced hypertensive rats at all test doses with maximum effect with 400mg/kg. The extract also exhibited significant (p<0.01) increase in cardiac markers like NO, cGMP, enzymatic and non-enzymatic antioxidants. Our study also revealed that MECD induce vasodilation in an endothelium dependant manner. Thus, Caesalpinia digyna root might be potential therapeutic agents for treating L-NAME induced hypertension.From the results of our study it can be concluded that MECD (200 & 400 mg/kg bwt) possesses strong anti hypertensive and antioxidant properties in L-NAME induced hypertensive rats.

Abstract

Aim: To evaluate the effect of ketofol on haemodynamic response and recovery parameters and to compare it with Propofol in direct laryngoscopic examination /biopsy (DLBX). Method: Three hundred fifteen patients posted for DLB were allocated in this prospective double blind study. Patients were randomly assigned to either Group KP (Ketamine 50 mg +Propofol 100mg in 10 cc) or Group P (100 mg in 10 cc).Inj. Succinylcholine 1mg/kg given in all patients. Pulse, BP and Spo2 were noted at 0, 1, 3, 5, 7 minutes and after every 15 minute’s interval up to discharge. Total volume of drug used and Ramsay sedation scale in each procedure was noted. Results: Time to eye opening was earlier in Group KP (10.56+/-4.22v/s 15.82+/-5.66 P value < 0.0001) than Group P. Time to follow the verbal command was longer in group P than group KP (30.6+/- 5.2 v/s 20 . 2 +/- 5.5, p value < 0.0001). In Group P, marked hypotension (p <0.001) was noted in 15 patients and SPO2 fall up to 94% was noted in 14/154(9.09%) patients. Analgesic requirement in recovery period was high (35 v/s 4) in Group P. Mean dosage of ketofol (23.25+/- 0.79mg ketamine, 46.5+/- 0.79 mg propofol) and Propofol (69.4+/- 1.5 mg) was required in procedures. Conclusion: Adjuvant use of ketamine with Propofol in Direct laryngoscopic examination provides significant haemodynamic stability, analgesia and rapid recovery.

Abstract

Asthma is a chronic disease of airways; that is widely characterized by an increased responsiveness to a large variety of stimuli, airway inflammation and obstruction. Responsiveness to the treatment of asthma is good but sometimes resistance develops, and variability in symptoms also occurs due to the limited therapy adherence and awareness of patients. A cross-sectional survey was conducted at Armed Forces Hospital Southern Region, Khamis Mushait, Kingdom of Saudi Arabia, May 2014, to evaluate the risk factors of asthma and the pharmacotherapy used by patients. A self-administered questionnaire was answered by 207 asthmatic people aged ≥15 years. They responded to questions regarding demographics, risk factors for asthma, its severity, drug used for asthma therapy. Most of the asthma risk factors are an allergy (71.5%), and family history (60.9%). Some patients, especially the elderly use non-steroidal anti-inflammatory (26.5%) and aspirin (5.8%). Most of the asthmatic patients had mild intermittent (69.6%). Patients used an inhaler (61.4%), most of them prefer to use Ventolin inhaler (78.3%) and the majority of them non-compliance for pharmacotherapy (76%). Subjects in past month got shortness of breath once or twice in a week (61.4%). Patients wake up once or twice during the month because of asthma symptoms (20.3%). Nearly half of them have increased symptoms of asthma in winter (56.5%), and less than half of cases had proper control of asthma (48.3%). The majority of patients were non-compliance and used Ventolin. Most of respondents had allergy and family history of asthma.

Abstract

A series of 3N-substituted 2-methylquinazoline-4(3H)-one derivatives were synthesized by cyclization of anthralinic acid with acetic anhydride followed by amination with different amines. The structures of the compounds were characterized on the basis of IR, C13NMR and H1NMR.The compounds were assessed by Insilco methods to predict the toxicity, drug likeness and inhibition towards cytochromeP450 enzyme and its subtypes. The compounds has shown better bioactive scores against enzyme and protease inhibition. The compounds 1and 2 are the inhibitors of CYP2C19, 3 and 4 showed inhibition towards CYP1A2 and CYP2C9.

Abstract

A simple, rapid, precise, accurate and highly sensitive High Performance Liquid Chromatographic method has been developed and validated for the simultaneous quantitative estimation of Amlodipine and Telmisartan in bulk pharmaceutical dosage form. Chromatography was carried on Boston pH lex C18 ODS (150 x 4.6 mm) 5μ Column with mobile phase based comprising mixture of pH 3.0 ammonium acetate buffer: acetonitrile –70: 30 v/v. The flow rate was adjusted to 0.75 mL/min with UV detection at 236 nm. The retention times of Amlodipine and Telmisartan were found to be 2.21 and 6.72 min respectively. The different analytical parameters such as linearity, accuracy, precision, ruggedness and robustness were determined according to the International Conference on Harmonization (ICH) Q2B guidelines. The detector response is linear in the range of 1-7 μg/mL and 8-56 μg/mL respectively. In the linearity study, the regression equation and coefficient of correlation for Amlodipine and Telmisartan were found to be (y = 39.68x + 0.494, r = 0.999), (y = 649.5x+ 116.9, r = 0.998) respectively. The results of the all validation parameters were within their acceptance values. The proposed method was successfully applied for quantitative estimation of Amlodipine and Telmisartan.

Abstract

Antibiotics are the second most widely prescribed drugs in today’s scenario due to the increasing rate of infections. Irrational prescriptions of antibiotics can lead to the emergence of antimicrobial resistance and the present study was carried in our hospital surgery department with the objective to estimate the antibiotic prescribing pattern in surgery department.A prospective and observational study was carried out in 207 patients from October 2014 to March 2015. Relevant information was obtained from the interview as well the treatment chart of patients, by using case report form. Results from the study suggest that majority of the patients enrolled in study were females (72.94%).Among the study population majority were belonging 59-68 years age group (23.1%) in which majority was farmers (59.4%).Most of the subjects were diagnosed with Hernia(21.7%), Appendicitis (14.5%) in which surgery was done for 70.7%. After the treatment (96.1%) of the study population showed improvement and 26% patients had drug-drug interactions in which 20.7% the drug interaction was mild .3.8% of underwent with culture sensitivity test with blood and peritoneal fliud.Cephalosporins (63.8%) and Nitroimidazole (53.1%) were the most commonly prescribed antibiotics.It can be concluded from the study that prescribing pattern of drugs antibiotics needs to be continuously evaluated in surgery department in order to promote the more rational prescribing to decrease morbidity and cost of therapy to the patient.

Abstract

Colon cancer is the third most common cancer in men and second most in women worldwide. The current treatment practices have only limited improvement in the prognosis of colon cancer. So newer alternative therapies are needed to improve cancer management. Bauhinia variegata is a medium sized deciduous tree belonging to the family Caeselpinaceae. Various parts of this medicinal plant have been used in different systems of medicine for the treatment of many ailments. The purpose of the present study was to investigate the chemo preventive action of B.variegata leaf extract against COLO 320 (a human colon carcinoma cell lines) in vitro condition. The ethanol extract of B.variegata leaf (EBV) was fractionated using column chromatography with solvents of increasing polarity from hexane to methanol. The anticancer activity of the fractions were examined by MTT (3-(4, 5-dimethylthiazol-2-yl) -2, 5-diphenyltetrazolium bromide) assay, DNA fragmentation assay and flow cytometry after PI (Propidium iodide) staining of COLO 320 cell lines. Totally 11 fractions were obtained. Fraction I (F-I) and X (F-X) have higher cytotoxicity value (IC50 for F-I:10.3 μM/ml and IC50 of F-X:42.5μM/ml). Hence, they were considered as active fractions I and II respectively. Treatment of COLO 320 cells with the active fractions (at their IC50 concentration) for 48 hrs significantly inhibited the proliferation in a concentration dependent manner. Both the active fractions I and II significantly induced DNA damage in treated COLO 320 cells. The active fractions I and II induced cell cycle arrest at sub G1 and G2/M phase respectively and executed apoptotic cell death. The present study therefore demonstrates the anticancer activity of B.variegata leaves. Further identification of lead molecules in the active fractions might help in the development of new alternative chemopreventive agent against colon cancer after further clinical trials.

Abstract

Herpes simplex virus type -2 (HSV-2) infection has a prevalence of 70% in the human population.The available drug treatment lead to the development of resistant strains. Since natural products offer unlimited opportunities for the discovery of antiviral compounds. The present study is aimed to analyse the phytochemical constituents of the ethanol leaf extract of Hypericum hookerianum through Gas Chromatography-Mass spectrometry and to test the anti viral activity against HSV-2 using HEp-2 cell line.The cytotoxic effect of leaf extract was estimated against HEp-2 cell line by MTT assay and the toxic free concentrations were performed for anti HSV-2 assay. GC–MS analysis of H.hookerianum revealed the presence of twelve different compounds. 25 μg /0.1 ml of leaf extract was non toxic to HEp-2 cell line and also expressed significant antiviral activity against HSV-2. These results concluded that the herbal extract had potent anti-viral agents against HSV-2 that can be exploited for development of an alternative remedy for herpes viral infections.

Abstract

L-Asparaginase is an enzyme belongs to amidase group (L-Asparaginase amidohydrolase; EC 3.5.1.1), a potential chemotherapeutic agent in the treatment of Acute Lymphoblastic Leukemia (ALL). Commercially available chemotherapeutic L-Asparaginase obtained from bacteria is associated with some major complications which necessitates the requirement to frame better forms of this enzyme. This study aims the isolation and identification of the fungal endophytes from some medicinal plants to produce the antileukemic enzyme, L-Asparaginase. In the present study, 16 different medicinal plants were considered for the isolation of endophytes. Fungal isolates obtained were screened using qualitative plate assay and the positive isolates were further quantified using Nesslerization reaction. Among the 48 fungal endophytes isolated from medicinal plants, 28 showed L-Asparaginase activity. Among these isolates, four fungal endophytes, hosted in three different medicinal plants namely Annona muricata, Averrhoa bilimbi and Ocimum sanctum showed maximum enzyme activity in the range of 0.402-1.669 U/ml and hence were selected for further studies. These L-Asparaginase producing isolates were identified as Penicillium citrinum, Penicillium limosum, Aspergillus niger and Aspergillus tamarii. From this study we could suggest that these fungal endophytes can be used for further studies to improve the enzymatic activity of the organism.

Abstract

The present research is directed towards the extraction and evaluation of phytoconstituents from stem of Euphorbia hirta L. was evaluated by using various in- vitro and in-vivo animal models. Methods- In vitro models like isolated goat tracheal chain preparation, isolated guinea pigs tracheal chain and ileum preparation were studied to know basic mechanism by which extracts shows relaxant activity. In-vivo studies were performed on clonidine, haloperidol induced catalepsy and milk induced leukocytosis in mice. The study showed that extracts are effective against histamine-induced contraction. In isolated goat tracheal chain preparation and isolated guinea pigs tracheal and ileum preparation ethyl acetate extract exhibits maximum relaxant effects against histamine. Animal studies involved use of histamine induced broncho constriction in guinea pigs and clonidine and haloperidol induced catalepsy in mice. This studies showed significant (P<0.05) protection at lower doses while further increase in the dose level showed reduced activity. Biochemical estimation in milk-induced total leucocytes count and milk induced differential leukocyte count were also studied, there was increase in leucocytes and lymphocytes (P<0.05) and decrease eosinophil up to 0% at dose 100 mg/kg p.o. body weight was observed. The result of these studies indicated usefulness of ethyl acetate extracts of stem of Euphorbia hirta in allergy.

Abstract

First stereoselective total synthesis of epi-Trocheliophorilide E has been described by two approaches from commercially available chemical (+)-diethyl tartrate (DET). The overall yields for the total synthesis of epi-Trocheliophorilide E are 25.1% (8 steps) and 17.8% (5 steps). The key steps of the strategy include reduction, Swern oxidation, Wittig olefination reaction and lactonization.

Abstract

The aim of the present work is develop a simple, rapid, accurate, precise and reproducible RP-HPLC method was developed for the estimation of Mirabegron in tablet dosage form. The method was carried out using EnableC18G (250 x 4.6 mm, 5μm) column in an binary mode with mobile phase comprising of Methanol: 0.1% OPA (pH5) (70:30v/v).The flow rate was 1ml/min and detection was carried out at 246nm using a PDA detector. The retention time for Mirabegron was found to be 3.601min. The method showed linearity in the concentration range of 10-50μg/ml (R2=0.999). The amount of mirabegron present in the formulation was found to be 99.3. The recovery studies also carried out and % RSD for Reproducibility was found to be below 2%. LOD and LOQ for this method for found to be 0.202μg/ml and 0.612μg/ml respectively. Robustness of the method was done by the deliberate changes in flow rate, column oven temperature and wavelength and % RSD 0.11, 0.23, 0.59, 0.27 and 0.77, 0.22 and The method was simple, sensitive and specific. Hence method can be used for the estimation of Mirabegron in pharmaceutical dosage form.

Abstract

Althaea rosea is a stately ornamental plant, producing large single, semi-double, double or frilled flowers of many colours belongs to the family Malvaceae. It is commonly known as Hollyhock. The aim of this review is to reveal the comprehensive information about Althaea rosea, to highlight the areas of research have been carried out in this drug and to promote further studies in this particular plant. Data were gathered from ethnobotanical books, traditional texts books, monographs, scientific journals and databases such as PubMed, Google Scholar, etc. The herbs can best be grown during the winter in the plains, but where the monsoon is not heavy; it also grows during the rains. Under moderate climatic conditions, it has been grown throughout the year in the plains. Propagation is generally through seeds. The main parts used in medicine are roots, leaves, seeds and flowers. The fruits and leaves contain primary alcohols, cyclohexanol, limonene, phellandrene, β-sitosterol, sucrose, glucose and mannose. Linoleic acid is the major constituent of the seed oil. The plant is having mucilaginous, demulcent, emollient, analgesic, anti-inflammatory, diuretic and febrifugal property. This is beneficial for chest complains, gastrointestinal disorders, boils, abscesses, skin cuts, ulcers, burns, peptic ulceration, renal calculi, kidney disorders, cough, arthritis, inflammatory conditions, asthma, bronchitis and many more. Though, it is evident that the Althaea rosea possesses various medicinal properties, very few studies have been carried out to prove its effects scientifically, such as antimicrobial, anti-inflammatory, cytotoxic, analgesic, antibiotic, antioxidant, antiurolithiatic, immunomodulatory, etc. Hence, it is suggested that relevant studies should be carried out in this particular plant to utilize its maximum benefits.

Abstract

Psoriasis is a common, chronic, non-contagious, auto-immune disease that primarily affects the skin.It is characterized by excessive growth and abnormal differentiation of keratinocytes, which leads to hyper proliferation and other inflammatory reactions on the skin. Topical therapy is a first line treatment for psoriasis management as it has many advantages over phototherapy and oral medication like avoidance of first pass metabolism, patient compliance, ease of application, local therapeutic effect and lower incidence of side-effects. This article focuses on drugs as well as novel approaches used in topical treatment for Psoriasis.

Abstract

The present research has systematic approach to synthesized a series of 1- pyridine-4-yl-methanone-3,5-disubstituted Pyrazolines (3a-g ) derivatives by the action of isoniazide and 1,3-diaryl-prop-2-ene-1-one (1a-h) In the present study, an attempt has been made to synthesize compounds by green chemistry technique i.e. microwave synthesis which is more convenient than conventional method Structures of all the synthesized compounds were confirmed by their IR, 1H-NMR.

Abstract

Topical microemulsion systems for the antifungal activity containing Clotrimazole are available to overcome the problems associated with its low solubility (0.49 mg/L) and slow dissolution in aqueous solutions. The objective of the study is to assess the antifungal activity and stability of Clotrimazole and jambhul honey in microemulsion formulation. The solubility of Clotrimazole in various oils, surfactants and cosurfactants was assessed to finalize the components of the w/o and o/w microemulsions. The pseudoternary diagrams were plotted to obtain the area of microemulsion region. The effect of Smix (surfactant:cosurfactant weight ratio) on the microemulsion region was determined and optimum systems were developed. Eight Clotrimazole microemulsion formulations, each four of water/oil (isopropyl myristae/Tween 80/phophotidyl choline/water) and oil/water (oleic acid/Cremophor EL/Transcutol P/water) were prepared and evaluated. The formulated systems were evaluated for drug content and drug loading capacity and characterized. Creams and gels of optimized formulations were prepared and were evaluated for spreadability, drug content, appearance, pH, viscosity, in vitro release, ex vivo skin permeation and antifungal activity. The optimized microemulsion had a uniform globule size of 84.4 nm. Outcomes of drug content and stability study showed that optimized microemulsion gel remain stable even after 90 days. Zone of inhibition was established against Candida albicans which was determined by cup plate method and compared with clotrimazole microemulsion gel and marketed gel. Microemulsion gel comprising of jambhul honey, oleic acid, Cremophor EL, Transcutol P and water was deemed promising as a topical delivery system of Clotrimazole for the treatment of skin fungal infections.

Abstract

The study includes the analysis of bioactive phytochemical, antimicrobial activity and invitro anti-diabetic activity of ethyl acetate extracts from the bark of Elaeocarpus ganitrus Roxb. Dried bark of E. ganitrus was extracted by using ethyl acetate as a solvent with the help of Soxhlet apparatus. The dried extract was subjected to phytochemical Screening; determine the antioxidant activity, anti microbial and invitro antidiabetic activity. Phytochemical screening of the sample showed the presence of Flavanoids, Tannins, Glycosides, Triterpenes, proteins and carbohydrates. The screening for Alkaloids, steroids, phenol, terpenoids and Plobatannin were found to be negative. The plant extract showed high level of antioxidant activity (upto 69%) which can be used as anti-aging agents and also showed dose-dependent increase in inhibitory effect on alpha-amylase enzyme(upto 65% ) which may be used to control high blood glucose level. Wide degrees of antibacterial activity were exhibited by the bark of Elaeocarpus ganitrus against Escherichia coli, Pseudomonas aeruginosa and Klebsilla sp. The ethyl acetate extracts of the bark of Elaeocarpus ganitrus are potential sources of anti-oxidant activity. The sample also showed high level of alpha amylase inhibition and high level of anti microbial activity against the above mentioned species. These findings showed that the bark of Elaeocarpus ganitrus is a potential natural sources of antioxidant and potent inhibitor for α-amylase activity and may be used as potent ant -diabetic agent. The present study also increases the medical importance of Elaeocarpus ganitrus.

Abstract

The objective of this study was to develop matrix tablets of aceclofenac for sustained release effect. Xanthan gum, guar gum and gum acacia used as natural polymers and study the effect of various formulation factors such as polymer proportion and effect of filler type on the in vitro release of the drug. Aceclofenac matrix tablets were prepared by wet granulation techniques. The prepared tablets were evaluated for weight variation, friability, hardness, thickness and in vitro dissolution studies. All the granules of formulations showed compliance with pharmacopoeial standards. In vitro studies were done for 10 hrs. and it was concluded that F2 which contain guar gum shows highest percent drug release ie: 95.5% at the end of 10 hrs. while F6 which contain gum acacia and Xanthan gum in equal ratio shows lowest drug release of 61.32 at the end of 10 hrs. Comparative study between Xanthan gum, guar gum and gum acacia concluded that guar gum showed best percent drug release at the end of 10 hrs. The difference in percentage drug release behavior of different formulations was clearly observed during swelling index study which shows hydration nature of different polymers used in the formulation. Further stability study of F2 formulation was done for one month and results are shown in table no. 8. The prepared matrix tablet produced sustained effect so this type for formulation are beneficial for NSAIDs drugs like aceclofenac which produce side effects like gastro intestinal disturbance, peptic ulceration and gastro intestinal bleeding due to frequent dosing.

Abstract

This research work was carried out with an objective of synthesizing some novel, potent antioxidant and less side effect having quinoline derivatives. Here some novel Schiff bases of quinoline are reported. Initially 7-substituted-2-cholro-3-formylquinolines on microwave irradiation with 4M HCl yielded 7-substituted-2-hydroxy quinoline-3-carbaldehydes I(a, b), which on further treatment with different substituted hydrazides yielded the novel Schiff bases of quinline II(a-f). The structure of all newly synthesized compounds was confirmed by spectral study such as IR, 1H NMR, 13C NMR and mass spectroscopy. All the synthesized compounds were screened for in-vitro antioxidant activity by nitric oxide scavenging and DPPH method using ascorbic acid as the standard drug. Compounds II c, II d and II f showed significant antioxidant activity.

Abstract

With an objective of synthesizing potent analgesic and antiinflammatory agents, here we have synthesized some novel series of pyrrole derivatives. In this ethyl-4-pyrrole-1yl-benzoate (II) was synthesized by the reaction of benzocaine (I) with 2, 5-dimethoxy tetrahydrofuran in presence of glacial acetic acid. Compound (II) on treatment with hydrazine hydrate in presence of ethanol yielded 4-pyrrole-1-yl benzoic acid hydrazide (III). Compound (III) on treatment with chloroacetyl chloride yielded N1-(2-chloroacetyl)-4-(1H-pyrrole-1-yl) benzohydrazide (IV), compound (IV) on reaction with different aromatic amines and triethylamine yielded N1-[2-(substituted phenylamino) acetyl]-4-(1H-pyrrole-1-yl)-benzohydrazide derivatives (V a-t).Structure of the synthesized compounds were confirmed on the basis of physico-chemical and spectral data (IR, 1H-NMR, 13C-NMR and Mass). All the synthesized compounds were screened for their analgesic and anti-inflammatory activity using glacial acetic acid induced writhing and carageenan induced rat paw oedema method respectively. For analgesic and antiinflammatory activities screening aspirin and diclofenac are used as standard drugs respectively. Among the synthesized compounds V a, V d, V f, V i, V k, V m, V n, V o and V p have showed good anti-inflammatory activity and compound V a, V d, V h, V k and V s showed good analgesic activity. These results are encouraging and further enhancement in the pharmacological activity can be brought about by slight modification in the ring substituent.

Abstract

The present work was to formulate and evaluate an oral pulsatile drug delivery system to achieve time release of Nicotinic Acid, based on chronopharmaceutical approach for the treatment of hyperlipidemia. As fat production takes place in night time is more than day time. Pulsatile delivery system is capable of delivering drug when and where it required most. Time-delayed tablets, designed to release drug after a predictable lag time, are intended for oral chronotherapy. The basic design consists of a core tablets prepared by wet granulation method. The tablets were press coated with polymer layer containing Eudragit S-100, Eudragit L-100 and Xanthum Gum (4:4:2) so that the variability in gastric emptying time can be overcome. The prepared pulsatile tablets were evaluated for the drug content, thickness and in-vitro release profile. In-vitro release profiles of pulsatile device during six hours studies were found to have very good sustaining efficacy. During the first six hours it shows no drug release and at the seventh hour immediate release was observed. Increasing the level of the rupturable layer increased mechanical strength and retarded the water uptake and thus prolonged the lag time. The lag time of the pulsatile tablets decreased with increasing amounts of Xanthum Gum in the Press coating layer. Stability studies proved that Press coating of tablets seems to decrease the effect of temperature and moisture on the degradation of Nicotinic Acid. The programmable pulsatile release has been achieved from a press coated tablet over a 6 hour period, consistent with the demands of chronotherapeutic drug delivery. The developed pulsatile drug delivery system released NA in a time dependent manner for the treatment of hyperlipidemia.

Abstract

Alcohol abuse is defined as pattern of drinking that result in harm to a person’s health, well-being, relationships, and productivity. A person who abuses drugs and alcohol is not necessarily an addict. However, abuse of these substances is a risk factor for developing an addiction because continuous abuse can lead to physical and psychological dependence. The American Society of Health-System Pharmacists (ASHP) believes that pharmacists have the unique knowledge, skills, and responsibilities for assuming an important role in alcohol abuse prevention, education, and assistance. Pharmacists, as health care providers, should be actively involved in reducing the negative effects that alcohol abuse has on society, health systems, and the pharmacy profession. Pharmacists have unique, comprehensive knowledge about the safe and effective use of medications and about the adverse effects of their inappropriate use. The provision of pharmaceutical care to individual patients involves pharmacists assessing the appropriateness of pharmacotherapy, counselling, and monitoring medication-use outcomes. Furthermore, pharmacists have legal and organizational responsibilities for medication distribution and control across the continuum of practice settings within health care organizations. With this combination of knowledge and organizational responsibilities, pharmacists are prepared to serve in leadership and service roles in alcohol abuse prevention and education and assist in a variety of patient care, employee health, and community activities.

Abstract

The main objective of the present study was to prepare a polyherbal scrub incorporated into gel. Nowadays cosmetics have become an important part in the day to day life for both man and women to lead a happy and confident life. Cosmetics are the product applied topically to beautify and cleanse the human body. At present scenario consumers are very particular about the product benefits without any side effects, hence herbal cosmetics are in peak of demand. Herbal cosmeceuticals are product used against skin problems. The use of natural ingredients to fight against acne, wrinkle and also to control secretion of oil is known as natural or herbal cosmetics. Herbal cosmeceuticals usually contain the plant parts which possess antimicrobial, antioxidant and anti aging properties. Herbal cosmetics are the safest product to use routine with no side effects and cosmeceuticals are the product which influences the biological function of skin. In this preparation Malus domestica (green), millet, cinnamon and honey is used as active ingredients and incorporated into the gel which is prepared with carbopol of different grades. Other ingredients like propylene glycol, Triethanolamine; methyl parahydroxy benzoate was added along with sodium lauryl sulfate into the gel. The prepared gel was evaluated for various parameters such as appearance, pH, viscosity, Spreadability, washability, irritability and found to be satisfied with all required characterizations. Thus, the developed formulation can be used as an effective scrub for using it to bear a healthy and glowing skin.

Abstract

Chronic renal failure is a slow progressive loss of kidney function over a period of several years. The main role of the kidneys is to remove wastes and excess water from the body. Chronic kidney disease (CKD) slowly gets worse over months or years. The loss of function may be so slow that may not have symptoms until kidneys have almost stopped working. Chronic kidney disease is much more common than people realize, and often goes undetected and undiagnosed until the disease is well advanced and kidney failure is fairly imminent. As kidney failure advances and the organ's function is seriously impaired, dangerous levels of waste and fluid can rapidly build up in the body. Treatment is aimed at stopping or slowing down the progression of the disease - this is usually done by controlling its underlying cause.The final stage of CKD is called end stage renal disease (ESRD) and renal transplant. Eventually the patient has permanent kidney failure patients with chronic kidney disease have multiple co - morbidities and require complicated therapeutic regimen. Clinical pharmacist’s specifically manage lab tests, follow up, adapt drug dosage according to guidelines and evaluate cardiovascular risk factors and decline in renal function. The purpose of the study was to summarize the available evidence regarding the role and impact of clinical pharmacy services for these patient populations. The ultimate goal of intervention in patients with chronic kidney failure is to improve the quality of life of patients.

Abstract

Anemia is a severe public health problem and nutritional deficiency during pregnancy. Iron deficiency anemia accounts about 50% in all cases of anemia and is common during pregnancy and can lead to serious maternal and fetal complications. Our aim was to assess the knowledge, attitude and practices of anemia among pregnant women in a rural set up. A total of 216 pregnant women are participated in our study. From the total of 216, about 169 do not attend any awareness programme of maternal health and pregnancy during their lifetime. Half of the sample size (50%) is illiterate and they don’t have the knowledge regarding anemia and antenatal visit. From our study we assessed that proper awareness and education programme regarding diet and lifestyle pattern during pregnancy can reduce the prevalence rate of anemia to some extent. The study also showed that education and awareness of anemia in pregnant women is considerably low and can be a major cause to pregnancy related problems.

Abstract

The polyherbal bitters are herbal galenicals commonly used by diabetic patients, because they are claimed to have antidiabetic potentials. Promoters of the bitters claim that, the bitters being of natural origin could be concurrently administered with conventional therapeutic drugs with no adverse effects. This research was aimed at assessing the effect(s) or otherwise of the co-administration of two popular bitters in Nigeria market Swedish bitter (SB) and Yoyo bitters (YB) and two therapeutic antidiabetic drugs metformin (MET) and glibenclamide (GLI) on the hypoglycemic and lipid profile in alloxan induced diabetic rats. Fifty four diabetic rats of both sexes weighing between 160g to 230g were divided into nine groups with six animals per group. Therapeutic doses of the bitters alone and in combination with GLI and MET corresponding to the body weight of the animals were administered orally to the different groups daily for 14 days. After an overnight fast, fasting blood glucose levels were obtained by tail tipping method on days 0, 1, 3, 5, 8, 11 and 14. On the 14th day the rats were sacrificed and blood collected by cardiac puncture. The blood was centrifuged and the plasma collected was analyzed for lipid profile. The results obtained indicated that GLI, MET, SB and YB all caused a significant decrease (p<0.05) in blood glucose during the period of studies in all treated groups compared to the control group. There was a synergistic effect on the hypoglycemic efficacy of GLI when GLI was co-administered with YB, but there was a decrease in hypoglycemic efficacy of MET when it was co-administered with YB. There was no effect when MET and GLI were respectively co-administered with SB. GLI, MET and the bitters caused an increase in the lipid profile when administered as a mono-therapy and in combination with each other. From the results of these studies, we conclude that, some bitters have hypoglycemic potency comparable to most conventional therapeutic drugs, however it is not safe to administer any of the bitters concurrently with therapeutic drugs since the effect on their hypoglycemic parameter is not predictable.

Abstract

Superficial skin infections are very common in general practice and are caused by bacteria and fungi one of the most common skin infection is dandruff. The increasing antimicrobial resistance exhibited by microorganisms causing superficial skin infections has led to extensive research on the therapeutic potential of anti dandruff herbal shampoos. These herbal shampoos contain many active constituents which are effective against many microbial infections. We tested the antimicrobial activity of twenty-six drugs against some dermatophytes. The water extracts of these selected 26 drugs were tested against Candida albicans, Staphylococcus aureus, E.Coli, S.aureus,) and Kiebsiella. We also observed that out of 26 drugs the nine extracts were effective against methicillin Staphylococcus aureus (MRSA) resistant .we suggest that infection caused by S. aureus MRSA may be cured by decoction of these active herbs.

Abstract

In the course of recent decade, extensive research has been carried out to develop a gastroretentive dosage form (GDF). This sort of dosage form can enhance the delivery and execution of drugs that are locally active in the stomach, in light of the fact that the GDF allows the drug to stay in the stomach for an adequate time interim. Distinctive methodologies have been used to develop the efficient GDFs such as low density systems, high density systems, super-porous hydrogels, hydrodynamically balanced systems, gas generating systems, super-porous hydrogels raft forming systems, swelling and expanding systems, floating systems, and ion exchange resins. However, these kinds of systems possess both advantages and disadvantages. Intra-individual and inter-individual differences in gastric physiology are impediments in the development of efficient GDFs. Examples of these individual differences include gastric pH and gastric motility, which have a significant impact on gastric retention time and drug delivery. Some of these hindrances can be overcome by building up a novel mucoadhesive floating drug delivery system (MFDDS). The MFDDS is characterized by intimate contact of the mucoadhesive dosage form with the mucosal layer, thereby increasing the localized absorption of the drug.

Abstract

Several high value added therapeutic biomolecules and their precursors exist in nature but yet to be discovered to fight against severe deadly diseases. Rapid emergence of drug resistance phenomena creates additional alarming situation and driving force to alleviate novel drug discoveries as earliest. Microscopic bugs, animals, and medicinal plants are the major source of novel therapeutic biomolecules generations following extraction, characterization, screening, and large scale production. However, conventional methodologies have not yet been shown great efficacy to generate novel drugs as far economical and industrial standpoints. To this end, the current review has shown a promising route that is combinatorial approach of synthetic biology and metabolic engineering for novel drug discovery. Though synthetic microbial metabolism is in its infancy but holds an enormous potential to battle against antibiotic resistance via providing high value added therapeutic biomolecules in near future. In conclusion, synthetic biology and metabolic engineering could be a potential avenue for novel drugs generations.

Abstract

Human Immuno deficiency Virus Infection /Acquired Immunodeficiency Syndrome (HIV/AIDS) is a disease of the human immune system caused by infection with human immunodeficiency virus (HIV).The Highly Active Anti Retro-Viral Therapy (HAART) is a complex therapy due to which the patient will be non adherent. Non adherence to the medications and lack of knowledge about disease is a major challenge to the effective management of HIV/AIDS. The reasons for non-compliance include factors such as complexity of treatment regimen, forgetfulness, patient beliefs about therapy and other socio- psychological factors. This may further lead to morbidity, mortality and many opportunistic infections. The study aims to assess, knowledge and medication adherence by means of structured knowledge assessment questionnaires and modified morisky’s medication adherence questionnaires and improve the HIV patients disease knowledge and medication adherence which will improve the therapeutic outcomes. A prospective, interventional study was conducted for a period of 6 months at the ART Center District hospital gulbarga . A total of 113 patients were enrolled into the study, among them only109 patients subjects, among them male patients were (53.21%) compared to females (46.78%) age group of 18-28years (27.52%). The assessment of patients disease knowledge and medication adherence showed that there was a statistical significant improvement (P<0.001) in their knowledge and medication adherence score from baseline to subsequent follow ups.Clinical Pharmacist can play a vital role in improving the knowledge and medication adherence which in turn improves the therapeutic outcomes thereby reduces the mortality and morbidity rate.

Abstract

Solid dispersions have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of a range of hydrophobic drugs. By reducing drug particle size to the absolute minimum, and hence improving drug wettability, bioavailability may be significantly improved. Solid dispersion have attracted considerable interest as an efficient means of improving the dissolution rate and hence the bioavailability of a range of hydrophobic drugs. Most of the newly invented chemical entities are poorly water soluble. As a result formulating them as oral solid dosage forms is a hurdle to the specialists. Many techniques have been exercised to improve oral bioavailability of drugs. Among several methods, solid dispersion has attracted attention of the researchers for previous 50 years. Different formulation strategies have been taken to prepare solid dispersions. It is evident that solid dispersions improve solubility of drug particles thus enhancing dissolution characteristics of drugs they increase the oral bioavailability. This article reviews the various preparation techniques for solid dispersions, carriers used in the formulation of solid dispersions and pharmaceutical applications of solid dispersions which can give an overall knowledge of enhancing the solubility of poorly soluble drugs.

Abstract

Glimepiride, an oral hypoglycemic second generation drug, has problems in bioavailability and bioequivalence due to its poor water solubility. An attempt was made to improve the bioavailability with an improvement in dissolution of glimepiride through the formulation of tablet containing solid dispersion of glimepiride- polymers i.e. Sodium Starch Glycolate (SSG) / Hydroxy Propyl Cellulose (HPC)/ Crosscarmellose Sodium (CCS)/Eudragit E-100. The binary systems of glimepiride i.e. both physical mixture as well as solid dispersions were prepared with drug and polymers. The solid dispersions were prepared by solvent evaporation method using methanol as solvent. Infrared (IR) spectroscopy was performed to identify any physicochemical interaction between the drug and the carrier(s). The dissolution profile of active pharmaceutical ingredient (API), marketed product and solid dispersion were compared. Differential Scanning Calorimetry (DSC) of solid dispersion elucidate that the crystal structure of glimepiride was converted into amorphous form. The optimized formulation was compressed with different excipients into tablet dosage form. The tablets formulation under investigation was then characterized for their various physicochemical properties such as weight variation, % friability, disintegration and in vitro dissolution profiles. It was observed that solid dispersions were better than physical mixture in dissolution. The result showed no interaction between the drug and polymer, percentage yield of 69.80% to 96.50%, amorphous state of solid dispersion and significant improvement in dissolution upto 98.81% with drug: SSG in 1:3 ratio. Thus, the solid dispersion technique can be successfully used for the improvement of dissolution of glimepiride.

Abstract

Two sensitive and accurate spectrophotometric methods has been developed for estimation of ezetimibe (EZT) in pure and dosage forms. The proposed methods is based on oxidation reaction of EZT with a known excess of N-bromosuccinimide (NBS) or cerium(IV) ammonium sulphate (CAS) as an analytical reagents in acid medium followed by determination of unreacted oxidant by adding a fixed amount of amaranth (AM), methylene blue (MB), indigocarmine (IC) or orange G (OG) dyes followed by measuring the absorbance at 520, 664, 610 or 478 nm, respectively. The experimental conditions affecting the reaction were studied and optimized. The beer’s law was obeyed in the concentration ranges of 2.0-20, 2.0-12, and 2.0-12 μg mL-1 in case of NBS using AM, IC and MB dye, respectively and and 2.0-18, 2.0-12 and 2.0-15 μg mL-1 in case of CAS using AM, OG and MB dye, respectively with a correlation coefficient ≥ 0.9992. The calculated molar absorptivity values are 0.7855× 104, 0.7255 × 104, and 2.7204 × 104 L mol-1 cm-1 for method A using AM, MB and IC dyes, respectively and 0.9246 × 104, 1.3612× 104 and 0.8658 × 104 L mol-1 cm-1 for method B using AM, MB and OG dyes, respectively. The limits of detection and quantification were reported. Intra-day and inter-day accuracy and precision of the methods have been evaluated. No interference was observed from the additives and the applicability of the method was tested by analyzing the pharmaceutical preparations containing the investigated drug. The proposed methods were successfully applied to the assay of EZT in tablet preparations and the results were statistically compared with those of the reported method by applying Student’s t-test and F-test. The reliability of the methods was further ascertained by performing recovery studies using the standard addition method.

Abstract

Poor asthma control is common and remains a frequent cause of hospital admission. The aim of this study was to identify risk factors associated with uncontrolled asthma among adult patients on follow up at Jimma University Specialized Hospital (JUSH). A facility based cross-sectional study involving patient interview and chart review was conducted among asthmatic patients aged 18 years and older who were attending chest clinic of JUSH for at least 3 months. Multivariate logistic regression was employed to examine the association between variables. One hundred ninety seven asthmatic patients were included in the study. More than 57% were females. The mean age of the patients was 41.75 (±15.54). Twenty four percent of the patients had one or more comorbid conditions. According to the classification by Global Initiative for Asthma Management and Prevention (GINA), 33.6% and 18.7% of study participants had moderate persistent and severe persistent asthma, respectively. Among the patients who received asthma medications, only 21% was according to GINA guideline recommendation. Accordingly, 127 respondents (64.5 %) were found to have uncontrolled asthma. Low monthly income (p=0.023), presence of comorbidity (p=0.007), moderate persistent asthma (p=0.027), severe persistent asthma (p=0.03) and use of SABA (short acting beta2 agonist) alone as anti-asthmatic medication (p=0.000) were significantly associated with uncontrolled asthma. In conclusion, majority of the patients had uncontrolled asthma and this was significantly associated with low income, presence of comorbid condition, asthma severity and use of SABA alone as anti-asthmatic medication. Clinicians’ adherence to the available asthma management guidelines is paramount important.

Abstract

The present work was aimed with the objective of formulating fast dissolving films of paracetamol to enhance the convenience and compliance by the elderly and pediatric patients. The films were prepared by incorporating the prepared paracetamol physical mixtures so as to achieve the aimed percent drug release (using cyclodextrins, sucrose and polaxomer 188) in different film forming agents (hydroxyl propyl methyl cellulose E5 &E15). Particular attention was given to the selection of the suitable taste masking agents. The large dose of the drug offered the greatest challenge in optimization of film formula leading to the thickness of the film and further altering the drug release from the film. The films were characterized in term of paracetamol content, mechanical properties, and disintegration time and dissolution test. The promising film F2 having the optimal formula showing the greatest dissolution and satisfactory in in-vitro disintegration time and physico-mechanical properties compared with a reference marketed product (Paracip tablets). FT-IR studies revealed that there is no interaction between the drug and the polymers used in the study. Statistical analysis revealed significant difference between the test films and the reference product, indicated that the test formulations F1, F3, F4, and F5 exhibited enhanced percentage T90 profiles, F2 and F6 showed comparable profiles with reference.

Abstract

The enzymes from microbial sources are more stable and obtained cheaply. Amylases are among the most important enzymes and are of great significance in present day industry. Starch degrading bacteria are most important for industries such as food, fermentation, textile and paper. Thus isolating and manipulating pure culture from various soils has manifold importance for various biotechnology industries. Amylase production from bacteria is economical as the enzyme production rate is higher in bacteria as compared to other microorganism. The aim of the current study was to isolate amylase producing bacteria from the soil samples collected. The isolation was done by serial dilution and plating method. Characteristic feature of the strains indicates them as Bacillus sps. Bacterial isolates were screened for amylolytic activity by starch agar plate method. The optimum ph for production was 7, whereas maximum growth was observed at 1gm Orange Peel and pomegranate Powder. The concentration of enzyme increases with increase in substrate concentration. The pH range was found to be 7 and incubation time 48hrs with 1ml as inoculum for optimum growth.

Abstract

Research has demonstrated the importance of dietary plants in daily life. Moringa oleifera a multipurpose green leafy vegetable plays an important role in sustainable communities due to its high nutritional quality and adaptability to diverse environment. Moringa oleifera plays a crucial role in the prevention of chronic diseases, as most of them find use in a number of pharmaceutical compounds. The present study was designed to study the therapeutic potential of the flower extracts by screening its biological activity under oxidative stress conditions in vitro and to understand the molecular insights taking place. To understand the assault and its protection, three different membrane systems like RBC ghosts, liver homogenate and liver slices were used and the oxidant induced cell injury was quantified as the extent of thiobarbituric acid reactive substances (TBARS) formed. In order to investigate its role in immune response the activity of the flower extracts were studied against the cyclophosphamide stress in mice and the level of hematological parameters like RBC, WBC count and differential count were recorded. Neutrophil adhesion test, haemagglutinating antibody (HA) titre, delayed-type hypersensitivity (DTH) response were also determined. The extract showed significant dose dependent increase in WBC, percent neutrophils and substantially enhanced cellular immune response, humoral immune response, neutrophil index in doses of 200 and 400mg/kg body weight. Phytochemical and TLC analysis revealed the presence of flavonoids and further showed a significant DPPH free radical scavenging activity.Quercetin and kaempferol were identified as the major components by HPTLC in the extract. Additionally high levels of minerals like iron, magnesium, zinc and trace amounts of selenium were quantified in the flower extracts by atomic absorption spectroscopy. The results obtained in this study indicate that flower extracts contain active components and minerals that stimulate the immunomodulatory activity by enhancing both cellular and humoral response and have the potential for the maintenance of general immune health and this plant can be exploited for the production of new drugs, industrial products and phytopharmaceuticals.

Abstract

The present study delineates synthesis and characterization of Glipizide microspheres using tragacanth gum, inulin and HPMC as polymers for colon-specific delivery for better treatment of Type 2 Diabetes, avoiding the side effects. The Glipizide microspheres were prepared by ionotropic gelation technique by the use of various cross linking agents. The polysaccharides reacted with sodium alginate in the presence of various cross linking agents to form microspheres with a polyelectrolyte complex membrane by electrostatic interaction between the two oppositely charged polymers. The microspheres were then studied for entrapment efficiency, drug-polymer compatibility and surface morphology. In vitro drug release pattern was studied in buffer medium using USP dissolution apparatus. Further, kinetics modelling was employed to find out release mechanisms. Glipizide microspheres showed high entrapment efficiency (87.75%) and the microspheres were free flowing, non aggregated and spherical, between 500-700 μm in diameter. The FT-IR spectrum showed that there is no interaction between the polymer and drug. The in vitro release study found to be affected by using various cross linking agent. The microspheres with Barium chloride as cross linking agent showing no drug release at acidic pH but show maximum release at the end of 12th hour in simulated intestinal fluid. The rate of drug release follows koresmeyer-peppas model and zero order kinetics. It was seen from the observation data that the cumulative percentage release from all the drug loaded batches of microspheres fell within the range of 47.73% to 64.14% in 12 hours study and it was found that the % cumulative release in microspheres encapsulated with tragacanth gum was maximum for Batch GA2 (64.14%) and minimum for Batch GC3 (47.73%).The study reveals that Glipizide loaded inulin microspheres can be used effectively for colon targeting.

Abstract

The universalisation of the web and online networking in the course of recent years has prompted a progressive movement in how individuals are communicating with each other today. Online networking stages and applications are quickly becoming the most preferred communication method. The increased uses of tablets, mobile phones and other hand held smart devices have led to the rapid increase of users of social media. Advanced media is utilized by biopharmaceutical organizations for correspondence with patients to gather information about infections and medicines, clinical trial enlistments, patient support programs etc. This paper analyses the scope importance and challenges of data mining with social media as a source for the process of Pharmacovigilance (PV) and the potential impact of the same in the larger arena of population and public health.