Hygeia journal for drugs and medicines

1-12

Authors: S. Sandhya*, E. Vidya Sravanthi, K.R Vinod

Plan: The objective of this research investigation was to formulate and evaluate herbal hydrogel incorporated with the extract of Ipomea pes-tigridis intended for anti acne activity. Methodology: The formulation was evaluated for various parameters like organoleptic characters, pH, skinirritation test by multiple compartment patch, microbial contamination, extrudeability, spread ability, drug content, diffusion studies using pig skin,accelerated stability studies, drug excipient interaction studies by FTIR, invitro anti acne and in vivo anti inflammatory activity. Outcome: The formulated hydrogel passed all the evaluation parameters. The hydrogel was olive green in colour and had an excellent fragrance. The diffusion studies revealed that the drugrelease was in controlled release form. The accelerated stability studies revealed that formulation was stable at room temperature whereas its stability reduced with increase in temperature. The FTIR studies showed that there were no drug excipient interactions. The anti acne and anti inflammatory activity showed an activity comparable to that of the standard drugs clindamycin and diclofenac,respectively. Hence it can be concluded that the formulation can be a good substitute for the existing synthetic anti acne agents.

27-33

Authors: Isaac U. Asuzu* and Chinaka O. Nwaehujor

Plan: The anti-diabetic and anti-hyperlipidemic effects of D-3-O-methylchiroinositol were investigated in male Wistar rats. Methodology: Diabetes was induced by a single intra-peritoneal injection of 150 mg/kg of alloxanmonohydrate. Five groups of rats comprising six animals in each group were used including a positive control group (glibenclamide, 2 mg/kg), treatment groups (8,4 and 2 mg/kg of D-3-O-methylchiroinositol respectively) and control(untreated) group. Blood samples were obtained from the rat tails every morning before treatment. Outcome: Alloxan-induced hyperglycaemia was significantly (p< 0.05) reduced by 59%, 48% and 41% after four days at 8, 4 and 2 mg/kg respectively compared with the untreated group(-135%) and Glibenclamide (50%). The in vitro anti-oxidant assays (DPPH andFRAP) showed that D-3-O-methylchiroinositol increased anti-oxidant activities with increasing concentration (10 – 400 μg/ml).D-3-O-methylchiroinositol therefore has anti-diabetic hypolipidemic and anti-oxidant activities.

43-50

Authors: S.Deepa*, K.Kanimozhi and A.Panneerselvam

Plan: Isolate and characterize the antimicrobial actinomycetes from sediments of salt pan region of Vedharanyam, located in the Nagapattinam District, Tamil Nadu, India. Methodology: The salt pan soil samples were collected The Physico - chemical parameters of soil sample were analyzed. Totally 16 actinomycete strains were isolated. The isolated strains were identified based on the morphological, biochemical, and physiological characteristics. All the 16 actinomycetes were selected for antimicrobial activity. Totally 16 actinomycetes strains were isolated. Antifungal activity was determined against two fungal pathogenic such as Aspergillus niger, Fusarium moniliforme. Streptomyces griseoflavus SDAP101 showed maximum level of inhibition against Aspergillus niger followed by Fusarium moniliforme. Molecular characterization of Streptomyces griseoflavus SDAP101were evaluated by PCR amplification of 16SrRNA gene. The genomic DNA and amplified products were separated in agarose gel and the16SrDNA gene of Streptomyces griseoflavusSDAP101species isolated from soil was partially sequenced using specific 16SrDNA sequence primer. The phylogenetic analysis revealed that its closest neighbor was EU827474.1. The16SrDNA secondary structure and the restriction sites of SDAP101 were predicted using Genebee online software respectively. Outcome: The isolation, characterization of the rare actinomycetes from the saltpan region will be useful for the discovery of the novel bioactive metabolites that are effective against wide range of pathogens

56-62

Authors: Dhivya R*, Manimegalai K

Plan: To assess the repellent efficacy of the flower extracts of Calotropis gigantea against Culex quinquefasciatus mosquito and to screen the bioactive compounds present in theflower extract. Methodology: The flower extracts of Calotropis gigantea were extracted with petroleum ether, chloroform and ethanol and the efficacy of the extracts as repellent were assessed on three day blood starved female Culex quinquefasciatus mosquito. The repellent study was following the method of WHO(1996). Outcome: The results suggested thatflower ethanol extract of Calotropis gigantea showed a higher repellency on the adult of female Culex quinquefasciatus mosquito than the other two extracts.The repellent activity was found to be dose dependent and the percentage of protection was found to be directly proportional to the concentration ofextract. The results of phytochemical screening showed the presence of bioactive compounds such as alkaloids, tannins, phenol, flavonoids, sterols, anthraquinone, proteins and quinones in the flower extract. It may be concludedfrom the result that ethanol extract of Calotropis gigantea flower was effective in mosquito vector control and has an excellent potential in controlling the mosquito.

76-86

Authors: KhaledRashed, Lucy Ono

Plan: The aim of the present research was focused on cytotoxic, antiviral and antibacterial properties and the main phytoconstituents of Terminalia laxiflora leaf methanolic extract. Methodology: The methanolic 80%extract of Terminalia laxiflora leaves was tested for cytotoxicityevaluation in Vero cells in-vitro, anti-HSV-1 activity and antibacterialactivity determinations against some bacteria strains and alsophytoconstituents were detected. Outcome: The results showed that T. laxiflora leaves methanol 80% extract showed CC50= 1851 μg/mLand also inhibited completely the development of the HSV-1 induced cytopathic effect at concentration of 238 μg/mL while the extract had no effect on bacterial strains. Phytochemical analysis of theextract revealed the presence of carbohydrates, tannins, flavonoids, alkaloids,triterpenes and chromatographic separation of the extract of T.laxiflora leaves resulted in the isolation and identification ofβ-sitosterol, m-gallate, gallic acid, ellagic acid and five flavonoids,quercetin, vitexin, iso vitexin, quercetin 3-O-α-rhamnoside and rutin. Thisresearch may be useful in the development of new and effective antiviral agents.

97-103

Authors: Lalit Kumar Sharma *,Narendra Nyola , Shashi Kant, and G.Jeyabalan

Plan: Stability indicating RP-HPLCmethod for the ceftaroline fosamil acetate. Preface: The developed method is simple, fast and accurate and can be used for routine analysis of Market formulations. Methodology: Stability indicating reverse phase high performance liquid chromatography method was developed and validated for the analysis of ceftaroline fosamil in bulk form. Chromatographic separation was achieved on aX- Bridge shield RP (4.6×100mm, 5µ) column, maintained at 300c with a mobile phase consisting of acetonitrile and ammonium dihydrogen orthophosphate buffer in the ratio of 10: 90. The mobile phase pumped at a rate of 1ml/ min. and the detection was carried out at 242.6nm by PDA detector. The retention time was obtained 4.312.The peak area plot was linear over theconcentration range of 50µg/ml to 250µg/ml. The different experimental parameters affecting the stability were optimized. The method was validated for accuracy, precision, specificity, robustness, LOD and LOQ in accordance with International Conference on Harmonization (ICH) guidelines. Outcome: The proposed method was successfully applied for the analysis of ceftaroline fosamil in bulk form.

1-4

Authors: Meignanalakshmi S, Vinoth Kumar S, Deepika J and Farida Begum .

Plan: The present study was undertaken to evaluate the antimicrobial activity of aqueous and methanol extracts of Adhatoda vasica against mastitis pathogens. Methodology: Milk samples were collected from mastitis cows and five bacteria were isolated. Based on Grams staining and various biochemical tests, they were identified as Staphylococcus aureus, Streptococcus agalactiae, Klebsiella pneumoniae, Streptococcus dysgalactiae and Escherichia coli. Leaves of Adhatoda vasica was subjected to aqueous and methanol extraction. Antibacterial activity of the extracts was evaluated by disc diffusion method and zone of inhibition was measured. Outcome: The methanol extract was found to be having significant antibacterial activity against Staphylococcus aureus, Streptococcus agalactiae, Klebsiella pneumonia,Streptococcus dysgalactiae and Escherichia coli with zone of inhibition 21.7±0.58 mm, 18.3±0.58 mm, 21.3±0.58, 18.3±0.58 and 28.3±0.58 mm respectively at 200 mg/ml concentration.

10-18

Authors: Bafna PA and Balaraman R*

Plan: DHC-1, a standardized poly herbal formulation, was investigated for its hepatoprotective and antioxidant effects against CCl4-induced liver damage in rats. Methodology: DHC-1at various doses (125, 250, 500 and 1000 mg/kg, p.o.) was studied for its effect on the levels of SGPT, SGOT, alkaline phosphatase and total bilirubin.The drug was also evaluated for its effect on markers of tissue oxidative stress, namely extent of lipid peroxidation (MDA), levels of enzymatic antioxidants (SOD and catalase), non-enzymatic antioxidant (GSH) and membrane bound enzymes (Ca2+ATPase, Mg2+ATPase and Na+K+ATPase). Outcome: Reduction in the levels of serum markers of liver damage; and decrease in tissue MDA levels and increase in SOD, catalase, GSH and membrane bound enzymes indicated the hepatoprotective and antioxidant property of DHC-1. Thus it is evident that DHC-1, at least partly by virtue of its antioxidant activity, elicited protective effects on the liver against the oxidative damage induced by CCl4.

23-31

Authors: C.Bijumol*, Helen William, Jose Kurien and Thomas Kurian

Plan: Formulation of oral gastro retentive floating tablets of Theophylline. Prologue: The primary aim of the present study is to design a sustained release gastro retentive oral dosage form using intra gastric floating as formulation strategy. Theophylline, an antiasthmatic is used as the model drug. Methodology: Oral gastro retentive floating tablets of Theophylline was formulated using gel-forming hydrophilic polymers, HPMCK4M, HPMCK100M and HPMC 15cps. The work also focused on in vivo evaluation of buoyancy by x-ray imaging. Suitable In vitro methods for estimating the drug release from the tablet as a function of time were developed and compared with marketed product (Theo SR 200 mg) Outcome: The prepared Tablets exhibited satisfactory physico chemical characteristics. All the prepared batches showed good in vitro buoyancy. The tablets with HPMCK4M and HPMCK100M floated for longer duration and had more matrix integrity as compared to formulations containing HPMC 15cps. Formulations with HPMCK 100 M & HPMCK 4 M showed better control of drug release and the drug release was similar to that of marketed product.

41-58

Authors: Vinod KR*, Gangadhar M, Sandhya S, David Banji

Plan: This review discusses overall approaches of gastro retentive drug delivery systems and limelight on floating drug delivery ,its formulation development and discusses various evaluation parameters. Preface: Oral drug delivery of nearly half of the drugs gets thwarted owing to the high lipophilic nature .Bioavailability of these drugs being function of their aqueous solubility and dissolution tends to exhibit low magnitude and high intra and inter subject variability. Many drugs have a short biological half life and thus have invents potential in ameliorating GI absorption. To overcome the poor bioavailability and patient complaints much attention has been given to Gastro retentive drug delivery system,although there are various approaches in retaining the drug within the gastric region. Outcome: Floating dosage form can be broadly divided into effervescences and non effervescences both have its own merits and demerits.To state that a given floating drug delivery system successfully float ,its lagtime should be within 5 min. Factors affecting floatation are size, shape,density, single or multiple unit, fed or unfed state, nature and frequent offood, gender, age, patient related etc. Evaluation include buoyancy study,floating and swelling behavior, drug release in additional to conventional evaluation, in vivo evaluation is important since the results may not adequately correlate with in vitro results. The usual reported in vivo floatation studies include x-ray, gamma scintigraphy, gastroscophy, magnetic marker, ultrasonography and octanoic acid breath test.

63-68

Authors: Dhanalakshmi D, Dhivya R, Manimegalai K.

Plan: Antibacterial activity of leaves and seed of Pongamia pinnata and Lawsonia innermis have been studied for their antimicrobial activities using agar well diffusion method. Methodology: The selected bacterial strains, namely Bacillus subtilis, Escherichia coli,Enterobacter aerogenes, Micrococcus luteus and Pseudomonas aeroginosa isolated from PSG Hospital, Coimbatore, Tamilnadu were selected for the study. Maximum zone of inhibition of the active compounds was evaluated by using NCCLS Method.The plant extracts were tested with the standard positive control chloramphenicol. Outcome: Among the three solvents analysed ethanolic leaf extract of Pongamia pinnata and Lowsonia innermis exhibited a maximum resistance against Bacillus subtilus and possessed a highest inhibitory zone against Pseudomonas aeroginosa and Micrococcus luteus respectively when compared to other bacterial strains.

79-83

Authors: Ancy P, Padmaja V*, Radha K, Jomy Jose, and Hisham A

Plan: The present study was carried out to investigate the diuretic activity of the ethanolic extract of roots of Flacourtia indica (Flacourtiaceae). Prologue: It is a popular drug used to treat many diseases in Indian traditional medicine. In order to substantiate the traditional uses of the drug the scientific study of diuretic activity was undertaken by us. Methodology: Air dried; powdered roots of Flacourtia indica were defatted with petroleum ether first and subsequently extracted with 90% alcohol.The preliminary phytochemical screening of the ethanolic extract revealed the presence of carbohydrates, tannins, phenolic compounds and terpenoids. The diuretic activity of ethanolic extract was evaluated by determining the urine volume and electrolyte concentration in albino rats. Frusemide (10 mg/kg) was used as standard while normal saline (0.9%) was used as control. Ethanolicextract of the drug (250 mg/kg and 500 mg/kg) were used as tests. Outcome: The ethanolic extract (500 mg/kg) showed significant increase in urine volume as well as Na+, K+and Cl- ion concentration in albino rats.

90-104

Authors: Ammar Ebrahimi*, Neda Lalvand

Plan: The review covers the uniquerole of Mesenchymal stem cells to improve, the poor solubility, prematuremetabolic inactivation, excretion and bioavailability of different classes ofdrugs which are insoluble or sparingly soluble in water. Preface: Mesenchymal stem cells (MSCs)exhibit unique characteristics including their ability to differentiate andmigrate to sites of tissue injury/inflammation, genetic modifiability, andexpression of protein. Many of the most promising drug targets areintracellular and can only be accessed by drugs capable of traversing the cellmembrane. Gene and drug delivery using genetically modified cells offersseveral unique advantages including ease of modifying, inducible or continuousdrug production inside the body, more control on drug target and safety. Outcome: In this review article, weexamine the promising of using MSCs as a drug delivery vehicle for genetherapy, and summarize various challenges and concerns regarding thesetherapies.

113-120

Authors: Shanmugam. R1,Gowthamarajan. K *, Priyanka D.L, Madhuri.K,Hemnath.E, Dhanabal. SP

Plan: Quercetin and rutin are the flavonoides possess good therapeutic properties.The main objective of our work wasto develop a simple, rapid and sensitive UFLC method for simultaneous estimation of quercetin and rutin. Methodology: A simple chromatographic separation was done by using a reverse phase C8 column (250 x 4.6mm) by using isocratic flow with the constituted a mixture of 25 mM potassium dihydrogen ortho phosphate (pH4) and acetonitrile mobile phase at the ratio of70:30 with the flow rate of l ml/min. Detection was carried out at 230 nm.Different validation parameters such as specificity,sensitivity, linearity, accuracy, precision, ruggedness and robustness were performed. Outcome: Optimized Chromatographic conditions were achieved and results showed good peakresolution between quercetin and rutin. The retention time was found at 7.4 min and 2.8 min. The LOD for quercetin and rutin was found to be 10 ng and 15 ng& LOQ was found to be 90 ng and 100 ng. The calibration curve was fixed at 0-100000 ng/ml. With change in analytical method parameters, analyst,laboratory conditions did not affect the results. % CV was calculated for all the parameters and found to be within specification limits. The developed method can be used for the quantitative and qualitative estimation of quercetin and rutin for the herbal medicinal products.

129-134

Authors: Sindhu T, Mamatha A, Sahith Reddy K, Venkateshwarlu K*

Plan: Depression is a common chronic recurrent syndrome, characterised by apathy, loss of energy, retardation of thinking and activity, as well as profound feelings of gloominess, despair and suicidal ideation. The present study refers to the anti-depressant activity of pyrimidine derivatives. Methodology: Anti-depressant activity was evaluated by using forced swim test and tail suspension test in mice. The behavioural parameter observed in this test was immobility period, which is indicative of anti-depressant effect of the compounds. Outcome: Test compounds 1b and 1c (15mg & 30mg) were effective and significant reduction in immobility period was observed when compared to standard drug Fluoxetine (20mg/kg) without any accompanying changes in the ambulation in open field test. These results indicate that the pyrimidine derivatives 1b and 1c are potential compounds for use in the designing of new candidates for the treatment of depression.

141-147

Authors: Rajasree RS*, K. Radha, Shyni.Bernard, K.N.Girija, A.K.C Nair .

Plan: An analytical method for the estimation of Lomefloxacin in bulk drug and pharmaceutical dosage forms by HPTLC is described. Prologue: The method is simple, fast and accurate and can be used for routine analysis of commercial Lomefloxacin tablets. Methodology: The developed method used precoated silica gel 60F 254 as stationary phase. The mobile phase used was a mixture of 2-Propanol: water: ammonia (86:8:6 %v/v/v).The RF value was 0.14.The detection of spots was carried out at 288nm. The calibration curve was found to be linear between 10 and 70 ng/spot with a correlation coefficient of 0.9969. The limit of detection (LOD) and limit of quantification (LOQ) were found to be 5 ng/spot and 10 ng/spot respectively. Outcome: The proposed method has been applied successfully for the determination of Lomefloxacin in pharmaceutical dosage forms. No significant interference was observed from excipients, coloring and flavoring agents commonly used in the formulation. The mean recovery of drug from tablets was in the range of 100.8% to 102.7 %.

152-163

Authors: Rajina PV and Shini Dominic *

Plan: To verify the toxic effects of the ethanolic extract of Asteracantha Longifolia seeds after single and repeated administration Prologue: Usually traditional medicines are not subjected to routine toxicological studies. As a result many adverse effects caused by the chronic use of herbal medicines may be wrongly attributed to certain acute or chronic diseases Though Asteracantha longifolia seeds are traditionally y used for the treatment of sexual debility, premature ejaculationand oligospermia, there is no evidence about its toxicity. Methodology: Acute Toxicity of the plant extract was carried out as per the OECD guideline 425. Sub acute toxicity study of 28 day duration was carried out in three different doses of 100 mg/kg, 250 mg/kg and 500 mg/kg orally. Outcome: No significant variation in hematologic and biochemical parameters and in relative organ weight with doses of 100, 250 and500mg/kg body weight. Histopathology showed the presence of slight necrosis in seminiferous tubules at dose of 500mg/kg. It may be concluded that the alcoholic extract of Asteracantha longifolia seeds is safe for oral administration at low and moderate doses while high dose(500 mg/kg) is not absolutely free from toxic effects.