ABSTRACT

Plants are potent biochemical factories and have been components of phytomedicine. Since time immemorial man is able to obtain from them a wondrous assortment of industrial chemicals. Plant-based natural constituents can be derived from any part of the plant like bark, leaves, flowers, roots, fruits, seeds, etc., which may contain active components. Sudan with its uniquely variable climatic conditions possesses a huge wealth of flora. Capparis decidua Family (Capparidaceae), Cyperus rotundus Family (Cyperaceae) and Tribulus terrestris Family (Zygophyllaceae) were used successfully in Sudanese folkloric medicine for treatment of inflammatory disorders.  The present review described Botanical description, biological activites and phytochemical profile of these three plants.

Keywords: Capparis decidua, Cyperus rotundus, Tribulus terrestris, inflammatory disorders

ABSTRACT

Diabetes mellitus is one of the common endocrine disorders characterized by deranged secretion of insulin and/or glucagon with extensive disturbance of carbohydrate, protein and lipid metabolism. GymnemaSylvestre is a woody, climbing plant of tropical forests of central and southern India and in parts of Africa. Gymnema has played an important role in Ayurvedic medicine for centuries. Its use has been confined primarily to the management of diabetes mellitus and similar hypo/hyperglycemic conditions. The first scientific confirmation of G. sylvestre use in human diabetics came almost a century back when it was demonstrated that the leaves of G. sylvestre reduce urine glucose in diabetics. Costusigneus Nak commonly known as fiery costus, Step ladder or Spiral flag or Insulin plant, is native to South and Central America. This is a recent introduction to India from America as an herbal cure for diabetes and hence commonly called as 'insulin plant. 

Keywords: Ayurveda, Anti-Diabetic Activity, Herbal Drug, Gymnemasylvestre, Costusigneus.

ABSTRACT

The stratum corneum of the skin or the sclera/cornea of the eye, the outermost layer of the skin and others has the principal barrier to topically-applied medications. Thus, many therapeutic agents are limited by their inability to reach the systemic circulation. Transdermal delivery of hydrophilic drugs and macromolecular agents of interest is problematic. Therefore, facilitation of drug penetration through this barrier may involve by-pass or reversible disruption of molecular architecture. Microneedles, when used to puncture skin, will by-pass the barrier and create transient aqueous transport pathways of micron dimensions and enhance the transdermal permeability. These micropores are orders of magnitude larger than molecular dimensions, and, therefore, should readily permit the transport of hydrophilic macromolecules. This microneedle based drug delivery system will useful for the eye treatments by avoiding drawbacks of topical administration of drug, multiple drug treatment and other dosage form intended in the eye. This review gives the details of history, various types of microneedles, drug delivery, fabrication methods, manufacturing, evaluation and, importantly, investigations of clinical safety of microneedles.

Keywords: Microneedle, Ocular drug delivery system, Fabrication of microneedles.

ABSTRACT

Mouth dissolving tablets (MDT) have received ever increasing demand during last decade and It is a rapidly a growing area in the pharmaceutical industry. After introduction into the mouth these tablets dissolve or disintegrate in the mouth and leaving an easy to swallow residue. Novel MDTs address the patient and pharmaceutical needs of convenient dosing particularly for busy or traveling patient, pediatric, geriatric and psychiatric patients who have difficulty in swallowing (dysphagia) conventional tablets and capsules. These tablets also have faster onset of action due to buccal absorption of the drug. The popularity and usefulness of the formulation resulted in development of several MDT Technologies. It is expected that this delivery system will get more importance in future as that of conventional delivery systems.

Keywords: Mouth dissolving tablets, disintegrate, residue, conventional delivery system.

ABSTRACT

Sandal safaid (Santalum album Linn.) is one of the most important medicinal Plants in the world.It is very well known since antiquity for its perfumery and medicinal properties worldwide. Greek physicians were aware of medicinal properties of sandal from the time of Alexander. They used it widely as qabiz (astringent), muffareh, muhallilawram (anti-inflammatory) and musaffikhoon (blood purifier). It is cultivated in many countries like Malaysia, Australia, New Zealand, India etc. but Indian variety is considered to be the best among all varieties. Seeds and wood is used to extract oil.The essential oil extracted from the wood is known as “East Indian sandal wood oil”. Chief constituent of oil is santalol (alpha and beta-santalol). It has been introduced into red list of threatened species as vulnerable.

Keywords: Sandalsafaid; Unani medicine; SantalumalbumLinn;Santalol.

ABSTRACT

Drugs belonging to BCS class II, low solubility and high permeability; undergo dissolution-rate limited gastrointestinal absorption. Glimepiride is one of the famous drugs belonging to BCS class II. Its poor aqueous solubility usually causes poor dissolution and unpredicted bioavailability. Hence, formulation techniques that accelerate drug dissolution can guarantee a parallel improvement in bioavailability. Now a days different techniques are available to enhance the solubility of drug like co-solvent, solid dispersion, chemical modification of drug, liquisolid technique etc. One of the favorable strategy to improve the solubility and hence bioavailability of poorly water soluble drugs is theformulation of solid dispersion. The solid dispersion may be prepared by solvent evaporation method, melting method, melt solvent method, kneading method, co-grinding method, co-precipitation method, modified solvent evaporation method, spray drying, gel entrapment techniqueand co-precipitation with supercritical fluid. This review article comprises of the research materialized in the field of solubility and dissolution enhancement of glimepiride.

Keywords: Biopharmaceutical classification system, Diabetes, Glimepiride, Solubility, Solid dispersion.

ABSTRACT

Co-crystals consists of API and a stoichiometric amount of a pharmaceutically acceptable co-crystal former. Pharmaceutical Co-crystals are nonionic supramolecular complexes and can be used to address physical property issues such as solubility, stability and bioavailability in pharmaceutical development without changing the chemical composition of the API. Maximum of the drugs belong to BCS class II, means these are drugs which have low solubility and high permeability. There are various methods of solubility enhancement such as salt formation, solvates, polymorphs, complexation, co-crystallization, etc. Co-crystallization mainly consists of two components the API and the coformer. Thse coformer is the one which acts as a main component for solubility enhancement. In case of ionization or salt formation there is a drawback as compared to co-crystallization. In case, of salt formation or ionization presence of an ionic center is required. This is not a requirement in case of co-crystallization.FDA has approved such combination called Juvisync¹ (Sitagliptin and Simvastatin) in 2011.Glipizide belongs to the anti-diabetic class of drug and Rosuvastatin calcium is a cholesterol reducing agent. As both these drugs are class II drug, solubility issues has to be solved. As Glipizide was available not in its salt form, its co-crystallization was decided to do. Hence, co-crystallization method was selected as the method to enhance the solubility. The co-crystals were characterized and showed the conformance of the presence of both the APIs.

Keywords: Glipizide, Rosuvastatin calcium, co-crystals, coformer.

ABSTRACT

To evaluate the preliminary phytochemical, antioxidant and anti-inflammatory activity of77 Anaphyllum wightii Schott. Bovine Serum Albumin denaturation inhibition assay was used for the evaluation of in-vitro anti-inflammatory activity and DPPH. Free radical scavenging and super oxide scavenging assays were used to assess the antioxidant activity of chloroform and aqueous extracts of the tubers of Anaphyllum wightii Schott. In anti-denaturation study, it was observed that chloroform extract showed greater percentage of inhibition of bovine serum albumin denaturation ie 49.2% whereas aqueous extract showed 38.4% at the 400µg/ml concentration respectively. In case of antioxidant screening also, chloroform extract showed better antioxidant power compared to aqueous extract dose dependently. Among the two extracts evaluated for anti-inflammatory and antioxidant activities chloroform extract of Anaphyllum wightii was found to possess significantly good anti-inflammatory and antioxidant activities and this can be attributed to the presence of alkaloids, saponins, flavonoids and phenolic compounds.

Keywords: Anaphyllum wightii, Anti-inflammatory, Antioxidant, DPPH.

ABSTRACT

A study of 84 cases of patients with Hepatitis A and E Virus has been presented with special reference to epidemiological aspects. A Prospective study was conducted in patients with acute Hepatitis in Hepatitis A and E virus. The Hepatitis A virus is found majorly in Males whereas Hepatitis E virus is found more in Females. The incidence of Hepatitis A and E Virus was progressively higher with age group 21-30 years and lowest occurring in 0-10 and 61-70 years. Patients most commonly presented with hepatomegaly, malaise, yellow discoloration of eyeballs. Enterically transmitted hepatitis A and E infections is seen in throughout the world in developed as well as developing countries.  Sanitation and standard of living conditions determine its incidence.  The present study aimed to find out the acute hepatitis A and hepatitis E infections in patients with acute viral hepatitis.

Keywords: Hepatitis A and E, hepatomegaly

ABSTRACT

Carbohydrate science has been extensively studied and many excellent reviews are available. N and S-linked derivatives of various sugars have received a great attention because of their vital role in several biological processes. Ureas, thioureas and their derivatives have strong antibacterial, antitumor activities. They also play an important role in organic synthesis as intermediates. This considerable attention has been directed towards the synthesis of various thiomaltosides. A series of S-hepta-O-acetyl maltosyl-1-aryl dithiocarbamates have been synthesized by the interaction of hepta-O-acetyl maltosyl bromide and various ammonium aryl dithiocarbamates in isopropanolic medium. The newly synthesized compounds have been characterized by analytical and IR, ¹H NMR and Mass spectral analysis. The polarimetric study of the compounds has been carried out. Antibacterial and antifungal activities of these compounds were determined on E. coli, S. aureus, Ps. aeruginosa, S. typhi, R. oligosporus and A. niger. These compounds show appreciable activity towards these microorganisms.

Keywords: Maltosyl bromide, ammonium aryl dithiocarbamates, maltosyl aryl dithiocarbamates, Microbial assay.

ABSTRACT

The objective of this research work was to formulate and evaluate the floating drug delivery system containing Pantoprazole sodium sesquihydrate as a model drug and to optimize its drug release profile. Pantoprazole sodium tablets were prepared by direct compression technique. Formulations contained Xanthan gum, PVP K₃₀ and gas generating agent such as sodium bicarbonate and citric acid were taken as independent variables. The physical parameters of the tablets were characterized and were found within the limits. By comparing dissolution profiles of different formulations, the formulation F5 was considered as a better formulation. The drug release from all the formulations was found to follow zero order kinetics and Peppas modeling. The diffusion exponent of formulations was found (n<0.89) to have non-fickian (anomalous) diffusion mechanism. The tablets eroded upon contact with the release medium, and the relative importance of drug diffusion, polymer swelling and tablet erosion for the resulting release patterns varied significantly with the type of matrix former

Keywords : Floating tablet, Pantoprazole sodium sesquihydrate, PVP K₃₀, Xanthan gum

ABSTRACT

In the present study the seeds of Annona reticulata was extracted with ethanol, and evaluated for mosquitocidal effect against the dengue vector Aedes aegypti. The preliminary phytochemical analysis showed the presence of alkaloids, flavanoids, glycosides, steroids and phenols in the ethanol seed extract of Annona reticulata. The percentage of egg hatchability in ethanol seed extract was 73% in 0.1%, 59% in 0.2% 42% in 0.3%, and 25% in 0.4%, 11% in 0.5% respectively and 100% hatchability was seen in control. The level of the toxicity of Annona reticulata was expressed in terms of LC50/24 hour value. The LC50 values of ethanol seed extract for I, III & IV instar larvae  and pupae of Aedes aegypti were 0.717 %, 1.263 %, 1.369 %, 1.425 % respectively. The morphogenetic abnormalities are commonly caused by botanical extracts and the disturbance from the growth regulating hormones. It is therefore suggested that Annona reticulata derivatives are considered for vector control operations besides their use in other fields after exploring field trails.

Keywords : Annona reticulata, Aedes aegypti, Larvicidal effect, Insecticide.

ABSTRACT

The objective of present study was to prepare and evaluate Zaltoprofen (ZLT) enteric coated oral mucoadhesive sustained release (SR) tablet in order to improve its GI residence time and improve its bioavailability by using natural biopolymers like xanthan gum and semisynthetic polymer HPMC for its safe use in rheumatoid arthritis, osteoarthritis, ankylosing spondylitis condition. The sustained release polymers, hydroxypropyl methylcellulose (HPMC) of different viscosities and xanthan gum evaluated in different proportions as a major matrix material. Drug-polymer compatibility studies by FTIR and DSC gave confirmation about their purity and showed no interaction physically between drug and selected polymers. ZLT matrix tablets were prepared by wet granulation.  The effect of polymer concentration on the drug release profile and in-vitro bioadhesion of the matrix tablets was studied. A 3² full factorial design was utilized in the optimizing the levels of HPMC and Xanthan gum. Concentration of HPMC K4M and the concentration of xanthan gum per tablet were used as the independent variables.  The dependent variables were the bioadhesive strength, percent drug dissolved at 2, 6 and 10 hours. The data obtained were fit to a model and polynomial equations were generated. Response surface graph was generated based on these equations. Formulation composition with desired release characteristics and bioadhesive strength were found to be predictive using this model. The optimized factorial batch was further given the coating of Opadry® enteric (94 series) polymer in order to avoid GI disturbances. The Z-22 tablets were kept for stability study at 40°C ±2°C and 75% ± 5% RH for a period of 6 months according to ICH guidelines. The formulation was found to be stable after 6 months of study. The pharmacokinetic parameters C_max, T_max, Mean Residence Time (MRT) and Area under Curve (AUC) of developed SR tablet were found to be improved with significant difference (p<0.05) when compared with marketed immediate release tablets each containing 80 mg of drug. From these results, it was concluded that the enteric coated oral mucoadhesive SR tablet containing Xanthan gum and HPMC K4M can be a good alternative to immediate release single unit dosage forms to treat rheumatoid arthritis.

Keywords: Zaltoprofen, Mucoadhesion, HPMC, Xanthan gum, Bioavailability studies

ABSTRACT

This paper signifies the process of aseptic germination of seeds of Taraxacum officinale, using various sterilizing agents and their influence on the physiology of seed. The three sterilizing agents, mercuric chloride (HgCl₂)_, sodium hypochlorite (NaOCl) and ethanol (CH₂OH) were used in the experiment alone and also in combination with each other in various concentrations. The degree of contamination, seed colour and % of seed germination during the course of experiment was studied. The aim of this study is to establish best surface sterilization for in-vitro propagation of Dandelion. The seeds of Taraxacum officinale were tried to germinate aseptically under various conditions and finally it was observed that seeds showed good germination using sodium hypochlorite (NaOCl) at concentration of 0.1% for 7 minutes.

Keywords: Taraxacum officinale, seeds, sterilizing agent, NaOCl, CH₂OH, HgCl_2.

ABSTRACT

This study helps to determine the efficacy of tacrolimus (generic form) in renal transplant patients in India. To assess the efficacy of tacrolimus in renal transplant recipients by using graft survival rate (primary objective) and patient survival rate (secondary objective). This is a retrospective study involving collection of data from medical records of patients who underwent renal transplantation in between JUNE 2010-JUNE 2013 at a tertiary care hospital) in India. Study population involves 65 patients between age group of 10-60 years, Male and Female gender, patients receiving tacrolimus (generic form) in their immunosuppressive regimen. Exclusion criteria involved patients with hyperacute graft dysfunction, patients who did not receive tacrolimus as a part of immuno suppressive regimen. Tacrolimus was given in combination with mycophenolatemofetil, corticosteroids. Tacrolimus was given at a dose of 0.15 mg/kg and titrated based on the graft function, trough levels of tacrolimus and other parameters. Of 65 patients,59 were men and 6 were women.86% of patients received graft from living donor, where as 14 % of patients received from cadaveric donor. Graft survival rates for the 1st, 2nd, 3rd years of transplantation were found to be 93.84%,89.23%,87.68 %.Patient survival rate was 98.46% during the 1st year, and it remained same for the succeeding years with no loss of patient lives. The main limitations of this study are inadequate sample size and retrospective nature of study. Through this study, it was concluded that tacrolimus(generic form) demonstrated efficacy in majority of renal transplant patients in preventing graft rejection and maintained favorable function for a period of 3 years.

ABSTRACT

An accurate, simple and precise RP-HPLC method for the simultaneous estimation sulfadiazine and trimethoprim in pharmaceutical formulations was developed and validated. Chromatographic separation of two drugs was achieved on PEAK 7000 isocratic HPLC with rheodyne manual sample injector by using the mobile phase consisting of methanol, water and aceticacid in the ratio 70:25:05 (v/v/v) at a flow rate of 1mL/min and the wavelength of detection was at 237 nm. The retention time for sulfadiazine and trimethoprim were found to be 4.24 and 7.25 min respectively. The linearity of the method was tested over a concentration range of 41-287 µg/mL for sulfadiazine and 9-63 µg/mL for trimethoprim and the correlation coefficient was 0.999 for sulfadiazine and 0.998 for trimethoprim which is almost equal to 1. The limit of quantification was 3.5 μg/mL for sulfadiazine and 1 μg/mL for trimethoprim and the limit of detection was 1 μg/mL for sulfadiazine and 0.3 μg/mL for trimethoprim. The percentage recoveries were ranged from 98.64-101.64 for sulfadiazine and 98.56-100.86 for trimethoprim.

Keywords: Sulfadiazine, trimethoprim an RP-HPLC.

ABSTRACT

Kidneys are complex organs, which perform several important functions. Though the formation of urine is their most obvious role, but they also perform the vital co-ordination of water and salt metabolism, acid-base balance and secretion of hormones. The effects of occupational or therapeutically exposure to toxic metals on kidney have been known for many years. A large number of chemicals in common usage are potential nephrotoxic viz. Glycols (plastics solvents), paints, lacquers, cosmetics and flavouring extracts. The nephropreotective activity of the poly herbal formulation (composed of the extracts from Terminalia chebula, tinospora cordifolia, Phyllanthus emblica, Portulaca oleracea) was evaluated in Gentamicin induced nephrotoxicity in rats, Gentamicin like other aminoglycoside antibiotics causes nephrotoxicity by inhibiting protein synthesis in renal cells. The serum creatinine and blood urea nitrogen (BUN) were found to be significantly increased in rats treated with only gentamicin, whereas treatment with PHME the effect of gentamicin indicating nephroprotective activity. Among various doses, 200mg/kg, 400mg/kg has shown good nephroprotective activity.

Keywords: Terminalia chebula, tinospora cordifolia, Phyllanthus emblica, Portulaca oleracea,PHME

ABSTRACT

The synthesis of a number of 4-(2’-alkyl/aryl benzimidazolo N-1-yl-methyl) -7 hydroxycoumarins containing pharmacophores of the coumarin and benzimidazole in a single molecule has been achieved.  4-Chloromethyl coumarins is used as N-alkylating (N-alkylation of benzimidazole) agent which is prepared by Pechmann condensation. 2-Substituted benzimidazoles were prepared by interaction of carboxylic acids and o-phenylenediamine. The structures of synthesized compounds have been assigned on the basis of chemical tests, IR, ¹H NMR, and Mass spectral data.

Keywords: 4-Chloromethyl coumarin, 7-hydroxy coumarin, N-alkylation, benzimidazole.

ABSTRACT

An accurate, rapid, selective and specific reverse phase high performance liquid chromatographic method was developed for the simultaneous estimation of Rosuvastatin and Clopidogrel in a combined formulation. Chromatographic separation was achieved on Inertsil ODS 3 C-18 (250mm x 4.6mm,5µm) column by isocratic elution mode with three mobile phase components, 0.05M potassium phosphate buffer (pH4.2): methanol: acetonitrile (60: 30:10 v/v/v) at a flow rate of 1.0 mL/min and quantified at 238 nm. The average retention times for Rosuvastatin and Clopidogrel were 4.57 and 2.96 min, respectively. The method offers excellent separation of two drugs with resolution > 2.0 and tailing < 1.0 and with no interferences from the excipients. The method is linear over the concentration range of 3.1-18.6 µg/mL for Rosuvastatin and 22.68-136.08 µg/mL for Clopidogrel with a correlation not less than 0.999. The method is accurate with recoveries of both the drugs in between of 98.0 -101.0% and precise with %RSD value less than 2.0% for the Assay of both the drugs. This method is simple, rapid, accurate and specific for the assay of commercial capsules.

Keywords: Clopidogrel (CD), Rosuvastatin (RSV), Validation, Capsules and Reverse phase High performance liquid chromatography (RP-HPLC)

ABSTRACT

Embelin is the principal phytoconstituent of Embelia tsjeriam-cottam A. DC., commonly known as Baibidanga, belonging to the family Myrsinaceae. Embelin, obtained from E. tsjeriam-cottam (an alternative source to E. ribes),is having diverse biological activities and used as anti-inflammatory, anti-diabetic, antimicrobial, anticancer and antioxidant. Fruit-samples of E. tsjeriam-cottam were collected from five different geographical locations of Odisha. These fruits were extracted and assessed for embelin content through spectrophotometric and high performance liquid chromatographic (HPLC) methods utilizing different solvent systems. Significant variation in embelin content was observed among the samples. Embelin content in fruits of E. tsjeriam-cottam was ranged from 4.93 to 2.1% (dry wt.), when extracted with chloroform and 4.88 to 1.03% (dry wt.), when extracted with methanol. However, in case of HPLC analysis, embelin content in the selected fruits were varied from 2.72 to 1.32% (dry wt.), when extracted with chloroform and 1.75 to 0.5% (dry wt.), when extracted with methanol. In general, embelin content was found higher in the fruits collected from Chura Reserve Forest (AG₃) followed by Sulia Reserve Forest (AG₄), Bargarh (AG₁), Ghana Reserve Forest (AG₅) and Jajpur (AG₂). Among the selected solvent systems, chloroform prevailed to be the excellent solvent for extraction of embelin.

Keywords: Baibidanga, Embelia tsjeriam-cottam, Embelin, Geographical Regions, HPLC, Spectrophotometry

ABSTRACT

Herbal medicines are formulations of therapeutic herbs to prevent and treat disease and ailments or to promote health and healing. There are various aspects Indian manufactures have to focus on to establish their products in the global markets. Right from the analysis of raw materials and in-process testing to analysis of finished products, system have to be established to stringently monitor every step in the manufacture. Maintaining quality of herbal products includes a strict set of processes within the specified limits laid down by the World Health Organization (W.H.O) to maintain consistency. D-Diabetes S.M.A.R.T powder is an authentic ayurvedic preparation consisting of nineteen herbal medicines namely Acacia arabica, Asphaltum, Bombax ceiba, Butea monosperma, Emblica officinalis, Eugenia jambolana,Ficus bengalensis, Gymnema sylvestre,Holarrhena antidysentrica, Momordica charantia,Pistacia integerrima, Plumbago zeylanica, Pongamia glabra, Pterocarpus marsupium, Santalum album, Swertia chirata, Terminalia chebula, Tribulus terrestris and Woodfordia fruticosa. The herbal medicines Eugenia jambolana,Gymnema sylvestre, Momordica charantia and Tribulus terrestrisare present in maximum quantity in the formulation and can be chosen as biological standard for studies. World Health Organization has set specific guidelines for assessment of safety, efficacy and quality herbal medicines. The various steps involve are botanical parameter, physicochemical parameters, biological parameters, toxicological parameters and pharmacological parameters.

Keywords: Microscopy, Ash value, Microbial contamination, Chromatographic techniques. 

ABSTRACT

The target of the present study is to use experimental design in screening and optimizing experimental variables to develop a spectrophotometric method for determination of Cefdinir (CFN) antibiotic. The proposed method is based on the oxidative coupling reaction of CFN with 3-methylbenzothiazolinone-2- hydrazone (MBTH) in presence of FeCl₃ in acidic medium forming a green colored chromogen measured at λ _max of 660 nm. A 2^5-2 fractional factorial design was utilized to screen the effect of FeCl₃, HCl and MBTH concentrations, in addition to reaction time and nature of diluting solvent on the absorbance of the formed chromogen. One way ANOVA and Pareto ranking analyses have shown that all variables were statistically significant. Full factorial design was then utilized to evaluate the effects of the variables on the selected response. With the help of a response surface and contour plots the optimum value of each variable was determined and used for further experiments. These optimum values were 5mg/mL FeCl₃, 0.06% HCl, 4mg/mL MBTH, reaction time of 10 min and methanol as diluting solvent. Beer’s law is obeyed in the range of 0.5-6.0 μg/mL. The proposed method was successfully applied for the determination of CFN in bulk powder and commercial dosage forms without interference from the commonly encountered excipients and additives. The mean recoveries of the analyte in pharmaceutical preparations were in agreement with those obtained from a comparison method, as revealed by statistical analysis of the obtained results using the Student's t-test and the variance ratio F-test.

Keywords: Cefdinir; MBTH; experimental design; factorial design; spectrophotometry.

ABSTRACT

A simultaneous estimation of RP-HPLC method was developed and validated for the estimation of Nimesulide, Cetrizine and Pseudo ephedrine HCl in tablet dosage form using C18 column (250mm 4.6mm, 5mm) with mobile phase consisting of Methanol: Water (65:35v/v) with a  flow rate of 1.0ml/min (UVdetection 220nm). Linearity was observed over the concentration range 0.1–5 µg/ml (R²=0.996) with regression equation y = 0.501x + 0.043 for Nimesulide and for Cetrizine 0.1–5 µg/mL (R²=0.994) with regression equation y = 0.4519x + 0.1656 and PseudoephidrineHcl 0.1–5 µg/mL (R²=0.997) with regression equation y = 0.3554x + 0.0088. The method was validated as per ICH guidelines.

Keywords:HPLC,Nimesulide, Cetrizine and Pseudoephedrine HCl.

ABSTRACT

An accurate & precise liquid chromatographic method was developed for the simultaneous estimation of Itopride (ITP) and Gliclazide (GCZ) in API matrix. The chromatographic analysis was performed on GRACE C₁₈ [250 x 4.6 mm i.d, 5 µ particle size) with mobile phase consisting of 0.05M Potassium Dihydrogen phosphate and 0.5% Tri Ethyl Amine (TEA) buffer having pH 2.7 and Methanol in the ratio of 60:40 v/v at a flow rate of 0.8 mL/ min and UV detection was carried out at 238 nm. The calibration curves of peak area versus concentration, which was linear from 10 - 100 µg/mL for ITP and 5 – 50 µg/mL for GCZ respectively. The retention times of ITP and GCZ were 2.951 and 7.735 min respectively. The method had the requisite accuracy, precision and robustness for simultaneous determination of ITP & GCZ in API matrix. The percentage assays of ITP & GCZ were found out to be 100.80% and 99.76% respectively. The method was validated by determining its accuracy, precision and system suitability. The results of the study showed that the proposed RP-HPLC method is simple, rapid, precise and accurate, which is useful for the routine determination of ITP & GCZ in bulk drug and in its pharmaceutical dosage forms.

Keywords: Itopride (ITP), Gliclazide (GCZ), RP-HPLC 

ABSTRACT

Glipizide is oral hypoglycemic agent, used for treatment of type II diabetes mellitus. Glipizide is insoluble in water. To increase the solubility, dissolution rate and bioavailability of glipizide it must be made its a suitable formulation by incorporating with suitable hydrophilic carriers. Such formulation provides a means of reducing particle size to nearly a molecular level. solid dispersion technique was adapted to enhance the solubility and dissolution rate of glipizide by incorporating hydrophilic carrier such as  Polyvinylpyrrolidone  K30 (PVP-K30) in different ratios were used . The formulation of the solid dispersion were carried our by preparing the  physical mixtures of glipizide using the Polyvinylpyrrolidone  K30 (PVP-K30) in four  different ratios.(1:2, 1:4, 1:6 and 1:8).Characterization of solid dispersions and physical mixtures were confirmed by Determination of Drug content, Solubility study, Thermal study, I R Spectral Analysis, Differential Thermal Analysis (DSC) and Powder x-ray Diffraction Analysis (XRD).From the results it was concluded that the Glipizide : polyvinylpyrrolidone  K30 The dissolution study showed that a maximum increase in dissolution rate was obtained with glipizide: PVP K-30 solid dispersions with a higher ratio of (1:8).

Keywords: Glipizide, PVPK-30, DSC, XRD, Solid dispersions.

ABSTRACT

Colon targeted drug delivery system is capable of protecting the drug in route to the colon i.e. drug gets released and absorbed once it reaches the colon. A multiparticulate system combining pH sensitive property and biodegradability has been investigated to prepare and evaluate Eudragit S-100 coated Sodium alginate microspheres for colon targeting of Tramadol Hydrochloride. Uncoated Tramadol Hydrochloride microspheres were prepared by ionotropic gelation technique using different ratios of Tramadol Hydrochloride and Sodium alginate. Coated Tramadol Hydrochloride microspheres were prepared by coacervation phase separation technique using different ratios of uncoated Tramadol Hydrochloride and Eudragit S-100/ Eudragit L-100. Uncoated and coated Tramadol Hydrochloride microspheres were evaluated for percentage yield, particle size, surface morphology, flow properties, drug content and entrapment efficiency and were found to be within the acceptable range. The uncoated microspheres sustained the release upto 8 hrs whereas coated microspheres sustained the release upto 12 hrs in a pH progression medium mimicking the condition of GIT. The drug release from MC4 formulation coated with Eudragit S-100 (1:4) showed desired rate as there was no drug release observed upto 4-5 hrs, while in colonic fluid controlled drug release was observed releasing about 69.66 % after 12 hrs. The release kinetics followed Peppas showing Super Case II transport. Stability studies suggested formulations were stable. It is concluded from the present investigation that Eudragit S-100 coated Sodium alginate microspheres are promising controlled release carriers for colon targeted delivery of Tramadol Hydrochloride.

Keywords: Colon targeted drug delivery system, Tramadol Hydrochloride, Sodium alginate, Eudragit S-100, Eudragit L-100.

ABSTRACT

The present work was defined to develop area under curve method for antipsychotic drug by UV spectrophotometric analysis which was economical, precise and an accurate method for estimation of Quetiapine fumarate. This method was based on area under curve of UV spectrum between 287 to 297 nm and validated as per ICH guideline Q2 (R1). The linearity in the range was found to be 4-14 μg/ml. The result of correlation coefficient was 0.999. The results of percent relative standard deviation for the intra-day and inter-day precision indicated that method is precise. The values of the recovery studies (99.65 % to 101.04 %) showed good accuracy of the method. LOD and LOQ were calculated as 0.3806 and 1.153μg/ml, respectively. The developed method can be applied for routine estimation of Quetiapine fumarate in bulk and tablet dosage forms.

Keywords: Quetiapine fumarate, Area under Curve, UV Spectrophotometry, Validation, ICH

ABSTRACT

A simple, rapid and sensitive high throughput liquid chromatographic method coupled with tandem mass spectrometry (LC–MS/MS) has been developed and validated to quantify tamsulosin in human plasma using tamsulosin D4 as internal standard (I.S). The analyte and internal standard were extracted from 300 μL plasma via solid phase extraction and were separated on a Kromasil C18 column (100 × 4.6 mm, 5 µ) with isocratic elution using acetonitrile: 5 mM ammonium formate (70: 30, v/v) containing 0.05 % formic acid as mobile phase. Tamsulosin was quantified using a triple quadruple mass spectrometer operated in multiple-reaction-monitoring (MRM) mode using positive electrospray ionization. The mass transitions m/z 409.2→228.0 and m/z 413.2→228.0 were used to measure tamsulosin and tamsulosin D4 respectively. The calibration curves were linear (r² >0.99) over the concentration of 0.1-89.4 ng/mL, where the regression model (1/x2) was best fitted. The intra- and inter-day batches precision (%CV) and accuracy values were found to be within the assay variability limit as per the FDA guidelines. The validated method was successfully applied to a pharmacokinetic bioequivalence study in human volunteers and found selective, sensitive and robust in quantitative measurement of tamsulosin in plasma samples.

Keywords: Tamsulosin, Solid-phase extraction, LC-MS/MS, Bioanalysis, Pharmacokinetic study 

ABSTRACT

Tuberculosis is a major infective disease affecting Indian population with high socio-economic impact. For eradication of tuberculosis and successful implementation of Revised National Tuberculosis Control Program – Directly Observed Treatment Short Course RNTCP- DOTS program regular assessment of the condition is imperative.The aim was to determine  the sputum carried out in District Tubercular Centre (DTC), Mangalore. The data of all patients registered from January 2011 to December 2011 were examined.The study was conducted on sample population of 297 patients. Of these, 183 (61.6%) patients were NSP cases and 114 (38.4%) patients were retreatment cases. The mean age of patients in category 1 and category 2 was 40.86± 18.20 and 42.49 ± 13.32 respectively. Males constituted 71.2 % and females were 28.8% of population. No significant difference in distribution with respect to gender (x² = 1.327, p = 0.249) and residential area (x² = 1.290, p = 0.256) in each categories. There is significant difference in distribution in category 1 and category 2 with mean age in years in different age category(x² = 21.521, p = 0.001). Of 183 patients in NSP, 137 patients converted to negative at the end of the 2 month intensive phase with conversion rate of 86.33% and 21 patients converted to negative at the end of extended intensive phase with conversion rate of 67.54 %.The sputum conversion rate was comparable to other study but was less than national average. Conversion rate is less in category 2 compared to category 1 showing the importance of treatment completion in patients with TB. Majority of patients belong to a productive age group between 21-60 years indicating the impact of the disease on socio-economy of patient as well as on the country.

Keywords:Tuberculosis, new smear positive, retreatment, sputum conversion, MDR TB.

ABSTRACT

To elucidate the terpenoid profile of Cucumis melo (L). fruit extract using high performance thin layer chromatography (HPTLC). The ethanolic extract prepared from the fruit of Cucumis melo (L). using Soxhlet apparatus. n-hexane: ethyl acetate (7.2: 2.9) was employed as mobile phase for terpenoids. 3µl of test solution and 2µl of standard solution was loaded as 6mm band length in the 3 x 10 Silica gel 60F254 TLC plate using Hamilton syringe and CAMAG LINOMAT 5 instrument.  HPTLC analysis was done using CAMAG HPTLC system equipped with automatic TLC sampler IV, TLC scanner 3, REPROSTAR 3 with 12 bit CCD camera for photo documentation, winCATS Planer Chromatography software. The Rf value of the different compounds present in the extract was found to 0.06, 0.21 and 0.93 of peak 1, 2 and 3 respectively. Among them, peak 1 was found to be terpenoid compounds. C. melo fruit extract showed the presence of terpenoids and it was confirmed from the chromatogram after derivatization.  HPTLC profile of terpenoids has been chosen here to reveal the diversity existing at biochemical level in C. melo. Such finger printing is useful in differentiating the species from the adulterant and act as a biochemical marker for this medicinally important plant in the pharmaceutical industry and plant systematic studies.

Keywords: HPTLC, Cucumis melo (L), Secondary metabolites, Terpenoids, Ethanol extract.

ABSTRACT

Desloratadine is an antagonist at histamine H1 receptors, and an antagonist at all subtypes of the muscarinic acetylcholine receptor. It has a long-lasting effect and in moderate and low doses, does not cause drowsiness because it does not readily enter the central nervous system. The present study is an attempt to formulate and evaluate the fast dissolving tablets of  Desloratadine. Fast dissolving tablets were prepared by direct compression after masking the bitter taste of drug by solid dispersion method with the aid of superdisintegrants. Seven formulations were developed using two different superdisintegrants in varying concentrations in such a way that total weight of the tablet remains the same. The drug-polymer incompatibility was ruled out by FTIR studies. All the formulated tablets were subjected for pre and post-compression evaluation parameters. A comparison of in vitro drug release of best formulation along with F1 formulation having no superdisintegrants is carried out. All the formulated tablets were shown satisfactory results which complies with official limits. Among the seven formulations, F7 was selected as the best formulation as its wetting time was 33 seconds, disintegration time was 29 seconds and %CDR after 8 minutes was 100.1%. F7 was found to be stable at 25°C ± 2 °C,  60°C ± 5°C and 40 °C ± 2 °C and 75 ± 5 % RH . Formulated tablets containing high concentration of croscarmellose sodium are better and effective than conventional tablets to meet patient compliance, give fast relief from allergy and cost effective.

Keywords: Desloratadine; H1 antagonist; Fast dissolving tablets; ODT; Superdisintegrant, croscarmellose sodium.

ABSTRACT

Bioadhesive gels improve both effectiveness and efficiency of the product due to intimate contact between a delivery device and the absorbing cell layer.  The interaction at the functional group level often results in the formation of mixtures capable of exhibiting rheological synergy.  Rheological synergy is the demonstration of greatly excess of viscosity and gel like properties when mixed with mucin than if the mucin and gels were examined separately.  This rheological synergism between gels and mucin could be used as an in vitro parameter to determine the mucoadhesive properties. In this study a simple rheological method is used to quantitatively determine various parameters like viscosity enhancement (η_enhance), relative viscosity enhancement of the combination system (η_rel), force of mucoadhesion (F) and viscosity component of bioadhesion (η_b). This is used to quantitatively compare different bioadhesive nasal gels prepared using carbopol which contain cyclodextrin as absorption enhancer. Composition of a gel can strongly influence its rheological properties and even one different constituent can lead to significantly different rheological behavior. The influence of the presence of cyclodextrin and different methods of addition of cyclodextrin was studied. The pattern noticed in this study was that the gels without the cyclodextrin showed the highest force of bioadhesion which was followed by the gels with cyclodextrin as inclusion complex and then by the gels with cyclodextrin as a physical mixture.  These gels were also subjected to Texture Profile Analysis. 

Keywords:Bioadhesive gels, mucin, bioadhesive force, texture profile analysis.

ABSTRACT

An organism is called “susceptible” to a drug when the infection caused by it is likely to act in response to treatment with this drug, at the suggested dosage. There are many bacterial species, including E.coli are showing an increasing resistance to antibiotics and E.coli is an important pathogen of urinary tract. The growing Prevelance of antimicrobial resistance is a most important health problem and is linked with high morbidity and mortality. Antimicrobial susceptibility pattern of gram negative was observed towards Nitrofurantoin (55.38%) followed by Cotrimaxazole (22.96%), amikacin (25.93) and Ceftriaxone (12.85%) in case of E.coli and Klebsiella. Enterococcus shown maximum sensitivity to linezolid (89.11%) followed by Nitrofurantoin (51.69%), but ofloxicin (9.7%), Imipenem (9.41%) and Amikacin shown very low sensivity. So, the decision on selection of antibiotic therapy should be made in discussion with microbiologist and pharmacist.

Keywords:Antibiotic sensitivity, prevalence rate, E.coli, Staphylococcus, monitoring of antibiotics.

ABSTRACT

A simple, precise and accurate UV Spectrophotometric method has been developed and validated for estimation of Sildenafil in bulk and tablet dosage form. In this method Sildenafil shows λmax at 290nm using 0.1N HCl as a solvent and calibration graphs were plotted over the concentrations ranging from 5 to 30μg/ml of Sildenafil with correlation coefficient 0.999. The proposed method was validated as per ICH Q2 (R1) guidelines for precision, linearity, accuracy and recovery. The limit of detection (LOD) and limit of quantification (LOQ) were found to be 0.113μg/ml and 0.343μg/ml respectively by simple UV spectroscopy. The proposed method was validated.

Keywords: Sildenafil, UV-Spectroscopy, Validation, 0.1N HCl.

ABSTRACT

This study reports the antioxidant potential and chemical composition of muscle from 30 fish species of different feeding habits namely carnivore, herbivore and omnivore.Different in vitro assays used for determining antioxidant potential of extracts of fish species were: thin layer chromatography (TLC) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity. No significant difference of antioxidant activity or nutrient content was observed among carnivorous, herbivorous and omnivorous fishes. The IC₅₀ measured by DPPH method varied from 154 to 2139 µg/ml of wet weight. The lowest IC₅₀ value was observed in C. idellafollowed by P.ticto, C. striatus, C. punctatus, L. rohita, A. testudineus, M. cordyla, O. mossambicus and G. giuris. Themoisture content of samples ranged from 62 - 85%. The protein content washigh in C. idella (24.3%) and low in L. calbasu (10.57 %). The lipid and ash content analyzed in the selected fish species ranged from 1.17-7.94% and 1.31-4.80%, respectively. Overall, the results suggestthat fish of different feeding habit can be exploited for their antioxidant and nutrients components and used for consumption as well as value addition in food formulations.

Keywords: Antioxidant activity, DPPH free radical scavenging, proximate composition, herbivore, carnivore, omnivore 

ABSTRACT

Trees and shrubs products have been used as principal ingredients that aid human health and well-being. Based on the literature review and traditional uses of plant Annonasquamosa (Family; Annonaceae), the present study was aimed to evaluate the CNS depressant activity of ethanol, petroleum ether and aqueous extracts of the leaves of AnnonaSquamosa in albino mice. The rotarod test and diazepam induced sleep test was used to evaluate the activity of extracts interfering with motor co-ordination and sleeping time at a dose of 200 mg/kg. 30 minutes after i.p. administration of extracts. The difference in the fall off time from the rotating rod and onset and duration of sleeping time between the control and the treated mice was recorded. It can be inferred from the results that the A. squamosaleaves extracts were exhibiting interesting aimed activity against the control group, however not on par with that of standard employed. Based on the results we can conclude that the ethanol crude extract of A. squamosaleaves exhibit significant CNS depressant activity.

Keywords: A. squamosaleaves extracts, CNS depressant activity, rotarod and diazepam induced sleep test in mice.

ABSTRACT

The environmental quality is greatly focused on water because of its importance in maintaining the human health and health of the ecosystem. Temperature, pH, electrical conductance, total dissolved solids, fluoride, sodium, potassium, chloride and Hardness calcium hardness, magnesium hardness etc. concentration in ground water was determined in Amdapur  in Warud taluka of Amravati District in Vidarbha region of  India. After examination and testing of different Physico-Chemical parameters the suitability of ground water for drinking and domestic purposes, could be found except some parameters of the sample from the ground water found above permissible limit of Indian Standards may be used for drinking purpose only after suitable treatment.

Keywords: Groundwater, physico-chemical characteristics, Amdapur.

ABSTRACT

Urinary tract infections have a high incidence in general population, with potential complications and constantly shifting trends in drug resistance that emphasizes the importance of selecting appropriate antimicrobial therapy. The present study shall focus on nitrofurantoin susceptibility in urinary E.coli isolates which heralds shifting trends in drug resistance among uropathogens and emphasizes on the need to revert back to older urinary antimicrobial agents. The study shall serve as an update on the susceptibility of E.coli to various commonly used antibiotics. A retrospective study was conducted by analyzing culture results and antimicrobial susceptibility pattern of E.coli isolated from 4533 urine samples collected from both inpatients and outpatients in Microbiology Department of tertiary care institute from January 2013 to December 2013. E.coli isolates depicted maximum sensitivity to Nitrofurantoin (87.12%) followed by Amikacin (86.53%) and Gentamicin (68.19%) whereas resistance remained high to Cefazolin (86.82%), Norfloxacin (84.53%), Cotrimoxazole (82.23%), Amoxyclav (82.23%) and Ciprofloxacin (76.22%). Nitrofurantoin susceptibility of E.coli isolates remained high in females (90.61%) as compared to males (83.09%). Among inpatients maximum sensitivity to nitrofurantoin was exhibited by isolates recovered from Gynae/obstetrics ward (94.59%) followed by pediatrics ward (82.35%). The study depicts promising use of Nitrofurantoin as narrow spectrum antibiotic to de-escalate the selection pressure and as fluoroquinolones sparing drug in areas where Cotrimoxazole resistance remains high in the uncomplicated cystitis. Clinicians should use local surveillance data to formulate empiric selection of antibiotic therapy in urinary tract infections.

Keywords: Nitrofurantoin, UTI, antimicrobialsusceptibility

ABSTRACT

A new rapid, precise and sensitive reverse phase high performance liquid chromatographic (RP-HPLC) method has been developed and validated for the estimation of Atazanavir and Ritonavir simultaneously in combined dosage form. The two components Atazanavir and Ritonavir were well resolved on an isocratic method, C18 column, utilizing a mobile phase composition of acetonitrile: 0.02M ammonium acetate buffer (40:60), v/v, pH 4.0) at a flow rate of 1.0 mL/min with UV detection at 205 nm. The retention time of Atazanavir and Ritonavir were 2.8 min and 5.7 min respectively. The developed method was validated for specificity, linearity, precision, accuracy, limit of detection (LOD), limit of quantification (LOQ) and robustness as per ICH guidelines. Linearity for Atazanavir and Ritonavir were found in the range of 18.0-42.0 µg/ml and 5.0-14.0 µg/ml, respectively. The percentage recoveries for Atazanavir and Ritonavir ranged from 98.9-101.0 % and 98.2-100.1 %, respectively. The proposed method could be used for routine analysis of Atazanavir and Ritonavir in their combined dosage forms.

Keywords:Liquid Chromatography; Atazanavir, Ritonavir, Combined dosage forms; Simultaneous estimation, Validation

ABSTRACT

The present work describes three simple, precise and economical UVmethods have been developed for the estimation of Maraviroc in bulk and pharmaceutical dosage form. Method A shown the absorbance maxima at 217 nm, method B area under curve method which involves the calculation of integrated value of absorbance with respect to the wavelength between two selected wavelength 212 -222 nm respectively. and in the first order derivative spectra showed sharp peak at 248 nm for method C. The developed methods were founded to be linear in the concentration range of 10-100 µg/ml. The developed methods were validated by following the analytical performance parameters suggested by ICH. All the validation parameters were within the acceptable range. As economical solvent is used, these methods were used for routine analysis of Maraviroc in bulk and pharmaceutical formulation.

Key words: Absorption Maxima, Area under curve, Derivative Spectroscopy, Maraviroc, Maraviroc Tablet Dosageform.

ABSTRACT

Barleria gibsoni belonging to the family Acanthaceae is commonly known as Neel Koranti.  Several species of Barleria are reported for treatment of inflammation associated diseases like Gout, Rheumatism and swelling etc. So, the present work has been taken for phytochemical screening and to investigate anti-inflammatory activity. Anti-inflammatory activity was done by Carrageenan induced hind paw edema method using a plethysmometer. Ibuprofen was used as a standard drug and control receives saline. The test groups received 200 mg/kg and 400 mg/kg of Ethanolic extract of Barleria gibsoni. Phytochemical screening of EEBG revealed the presence of phytocontituents like carbohydrates, tannins and flavonoids. In acute oral toxicity study it was observed that there was no mortality at any doses up to 2 mg/kg. The EEBG shows significant anti-inflammatory activity in carrageenan induced rats.

Keywords: Barleria gibsoni, Anti-inflammatory activity, Carrageenan.

ABSTRACT

The present work deals with the synthesis of azetidinone derivatives of quinazolinones and  the structures of the compounds obtained have been established based on spectral (IR, ¹H NMR,¹³C NMR and Mass) data. The present study also involves in vitro anthelmintic and antibacterial activity of the synthesized derivatives a few strains (gram positive and gram negative) of bacteria. All the compounds showed against moderate to satisfactory activities.

Keywords: Azetidinones, Quinazolinones, Anthelmintic, Antibacterial.

ABSTRACT

Asthma is one of the most common chronic diseases affecting an estimated 300 million people worldwide and ranks third responsible for hospitalization. In developing regions (Africa, Central and South America, Asia), asthma prevalence is rising sharply with increasing urbanization and westernization.  Plant-based medicines are the 3^rd most popular choice of both adults (11 %) and children (6 %) suffering from asthma. WHO encourages, recommends and promotes traditional herbal medicines and their formulations in National Health Care Programme which need to ensure quality control using modern techniques applying suitable standards. Asavas are polyherbal Ayurvedic formulations mentioned in Bhaishajya Ratnawali and its modern English translated version known by the name Ayurvedic Pharmacopoeia of India. Kanakasava, a polyherbal Ayurvedic asava formulation, consists of Datura metel Linn. Adhatoda vasica Nees.,  Glycyrrhiza glabra Linn., Piper longum Linn., Solanum xanthocarpum Scrad & Wendl, Zingiber officinalis Rosc., Clerodendrum serratum (Linn.) Moon, Mesua ferrea Linn, Abies webbiana Lindl., Woodfordia fruticosa Kurz., has been used traditionally since ages for the treatment of asthma. Standardization of the formulation was done as per API. The results of standardization parameters of pH (3.85 ± 0.029), specific gravity (1.046 ± 0.009), viscosity (1.52 CS ± 0.006), phenolic content (0.079 % w/v ± 0.012%), alcohol content (7.18% v/v ± 0.577), total solid content (14.64 % w/v ± 0.348) and estimation of heavy metals, aflatoxin, pesticide residues, microbial load complies with the official limits.

Keywords: Asthma, traditional, Kanakasava, polyherbal, Ayurvedic, Standardization.

ABSTRACT

A simple, sensitive and specific HPLC method with UV detection was developed for the estimation of irbesartan in tablet dosage form. Separation was achieved by Lithosphere 100 RP-18e, 5µ column having 250x4.0 mm internal diameter with mobile phase containing phosphate buffer and acetonitrile in 50:50 (v/v) with an ambient temperature. The flow rate was 0.8mL min^-1 and eluent was monitored at 220 nm. The proposed method was found to be rectilinear over theconcentration range of 20µg/ml to 60µg/ml. This method was validated for system suitability, Specificity, Linearity, Precision, Accuracy, Range, Stability studies, Ruggedness, Robustness and Filter validation.  The results of all the validation parameters were well within their acceptance values. Therefore the proposed method can be used for routine analysis of estimation of Irbesartan in its tablet formulation

Keywords: Irbesartan, Tablet formulation, Antihypertensive, HPLC, Validation

ABSTRACT

In present study long-acting biodegradable Nateglinide loaded Poly (lactic-co-glycolic) acid nanoparticleformulation is reported for treatment of Type 2 Diabetes Mellitus (T2DM).Different formulations were prepared by varying drug: polymer ratio (1:1, 1:2, and 1:3) and polyvinyl alcohol as stabilizer in 0.5-1.5% concentration range by emulsificationsolventevaporation technique. Optimization was carried out by evaluating entrapment efficiency and particle size. Optimized formulation was characterized for in vitro drug release, surface charge property, SEM, chemical incompatibility and invivo evaluated for blood glucose lowering property in rat model. The obtained resultsindicatethat formulation composition containing drug:polymer ratio 1:3 and stabilizer concentration 1.5%  gives high encapsulation efficiency (82.15%) with mean particle diameter of 216 nm and drug release for 72h. Drug release data was best fitted to Higuchi model indicating drug release was mainly took place by diffusion mechanism. Oraladministrationof optimized nanoparticle formulation showed two fold better activity as compared to standardNateglinide formulation(P<0.05). Study suggested that Nateglinide loaded controlled PLGA nanoparticle can be used for better control of blood glucose level by sustaining its release. 

Keywords:Nateglinide, PLGA, Poly vinyl alcohol, nanoparticle, Diabetes mellitus

ABSTRACT

In the present research work attempt was to formulate tasteless complexes of Ambroxol hydrochloride using cation exchange resins and to evaluate molecular properties of drug complexes. Tulsion 343 that contained crosslinkedpolyacrylic backbone was used. The drug loading onto ion-exchange resin was optimized for mixing time, activation, effect of pH, mode of mixing, ratio of drug to resin, and temperature. Drug resin complexes (DRC) were evaluated for taste masking and characterized by x-ray diffraction study and infrared spectroscopy.Ambroxol hydrochloride is a potent mucolytic agent capable of inducing bronchial secretion. It is used in the treatment of asthma, bronchitis and cough.It is a highly bitter drug and not suitable for pediatric patients hence taste masking of drug was required. Ambroxol hydrochloride-Tulsion 343 complex of ratio 1:0.7% w/w  was  developed into  suspension formulation  using different  suspending agents  with  varying concentration  and was evaluated for  sedimentation volume, pH, drug content  and viscosity. The prepared suspensions were evaluated for taste, drug content, particle size, viscosity, sedimentation volume, drug release. The results showed that Ambroxol Hydrochloride was successfully taste masked,showed easy redispersibility and more than 80% drug release within 45 minutes and when compared with  marketed preparation.

Key words:Tulsion 343, Drug-resinate complex, Taste masking, Suspension

ABSTRACT

Several 1-Tetra-O-acetyl-β-D-glucopyranosyl-5-aryl-isothiobiurets were synthesized by the interaction of tetra-O-acetyl-β-D-glucopyranosylthiocarbamides with various aryl isocyanatesand were evaluated for their antibacterial and antifungal activities. The identities of these new N-glucosides have been established on the basis of elemental analysis, IR, ¹HNMR, ¹³CNMR and MS spectral studies.

Keywords: Glucopyranosylthiocarbamides, GlucosylIsothiobiurets, Synthesis, Antimicrobial Activity.

ABSTRACT

A specific, rapid, reliable and precise reversed phase ultra-performance liquid chromatographic method has been developed and validated for the simultaneous estimation of aspirin, clopidogrel and atorvastatin in tablet dosage form. Chromatography was carried out on a 100 × 2.1 mm i.d., 1.7 µm C18 column with gradient flow programming mobile phase The mobile phase is a mixture of two solutions mobile phase A and mobile phase B in the ratio of 30:70. The mobile phase – A, contains buffer and methanol in the ratio of 93:7, the buffer used is 2.76 gms of Sodium phosphate in 100 ml. The mobile phase – B, contains 0.1% orthophosphoric acid and acetonitrile (60:40, v/v), at a flowrate of 0.5 mL/min. The detection was carried out by PDA detector. The retention times were about 0.55, 0.98 and 2.75 min for Aspirin, Clopidogrel and Atorvastatin, respectively. The runtime was 5 mins. The method was validated according to ICH guidelines and the acceptance criteria for accuracy, precision, linearity, specificity and system suitability were found to be under ICH limits. The method was linear in the range of 5-25 µg/mL of Aspirin, 5-25 µg/mL of Clopidogrel and 1-5 µg/mL of Atorvastatin. Limit of detection obtained were 0.02 µg/mL of Aspirin, 0.05 µg/mL of Clopidogrel and 0.07 µg/mL of Atorvastatin.

Keywords: Ultra performance liquid chromatography, Assay method, Gradient flow programming, tablet dosage forms, Aspirin, Clopidogrel bisulphate and Atorvastatin calcium.

ABSTRACT

Studies carried out in the past have shown that in infectious diseases there is increase in the levels of Erythrocyte Sedimentation Rate (ESR), White Blood Corpuscles (WBC) and liver enzymes Alanine Aminotransferase (ALT), Gamma GlutamylTransferase (GGT) and Lactate Dehydrogenase (LDH).  There are other inflammatory markers like C reactive protein (CRP) and Procalcitonin, both of which are altered in several infectious diseases.  This study is an attempt to find out the correlation of ESR  to WBC and  several analytes of liver function tests such as  Aspartate aminotransferase (AST), ALT,  ALP,  GGT and  Albumin.  Results available for 100 patients attending the master health check up were used to find out the above associations. Very good correlations were observed between ESR and WBC for all patients (p<0.0001) and males  & females (p<0.01).  When the results for ESR was grouped as normal and abnormal, ESR showed association to ALT,AST and ALP (p<0.05) for normal patients and to only WBC for abnormal patients (p<0.05).  The results obtained in this study confirms that ESR results always correlates with WBC and to some extend to liver function tests like ALT,AST and ALP and GGT. Further studies are required using a large number of patients and to extend such studies to find out association of ESR to various inflammatory markers.

Keywords:ESR, WBC, ALT, AST, ALP and GGT

ABSTRACT

The present paper deals with the phytochemical screening and Inorganic elemental analysis of the plant materials. Curcuma leucorhiza belongs to the family zinziberacea and has been used in folklore medicine to treat various ailments. . The rhizomes of curcuma leucorhiza are used for the treatment of enlarged liver spleen and stomach ulcer. The decoction of its rhizomes is used in the treatment of diabetes and cancer in local traditional medicines .The biological activities of curcuma leucorhiza include antioxidant activity, antibacterial activity and antifungal activity. The  rhizome parts of curcuma leucorhiza was slice,dried,grind into powder and then extracted with acetone, chloroform, methanol and ethanol solvents giving 9.06,12.90,7.30 and 13.20% yield respectively.  Phytochemical studies of the extracts showed the presence of terpenoids, alkaloids, saponins, flavonoids, glycosides, carbohydrates, phenolic, tannins, phytosterols, anthocyanin, proteins and amino acids etc. Quantitative determination of alkaloid was done by Harborne (1973) method. Inorganic elements are determined by a Graphite Furnace Atomic Absorption Spectrometer. Rhizome of curcuma leucorhiza contains minerals such as Fe, Zn, Cu, Mo, Cr, Mn and were found to be 0.971, 0.414, 1.70, 0.013, 5.091 and 0.015 ppb respectively  The results obtained shows that the extracts contain bioactive compounds and also trace element present in the plant extracts were within the permissible limits. The study will provide referential information for the treatment of various diseases.

Keywords: Curcuma leucorhiza, Phytochemicals, extract, element Analysis.

ABSTRACT

Wound is a physical injury that causes breakdown in the protective function of the skin and the loss of continuity of epithelium with or without loss of underlying connective tissues. Proper healing of wound is essential for the restoration of normalcy in disrupted anatomical continuity and altered functional status of the skin. Wound healing is a complex and dynamic process of restoring cellular structures and tissue layers. It can be divided into 3 distinct phases: an immediate haemostatic phase, an early phase of re-epithelialization, a later phase of dermal repair and remodelling. The present investigation was undertaken to determine the efficacy of Butea monosperma leaves aqueous extract, isolated acidic ingredient and its newly synthesized amide analogue along with silver sulphadiazine as control on burn wound in Wistar albino rats. The histopathological examinations confirmed that the treated animals showed improved rate of epithelialization and wound contraction. On comparison among the impact of test compounds; it was further revealed that, the Butea monosperma leaves aqueous extract and synthesized amide analogue showed significant wound healing activity than isolated acidic ingredient.     

Keywords: Butea monosperma, isolated ingredient, amide analogue, burn wound.

ABSTRACT

The contamination of processed or unprocessed drinking water by pathogenic bacteria has been reported worldwide. Even though a high incidence of waterborne diseases have been well documented, enterobacteriaceae is an under acknowledged pathogen of concern to public health in India. The study was aimed to isolate and biochemically characterize Enterobacteriaceae as well as to determine  antibiotic sensitivity pattern and primer designing specific to their signature gene sequences for rapid detection by PCR methods. Total plate count was determined in potable water sample collected from three different sites of Jaipur city and was found to be nearly equal or more than 10⁵ cfu/ ml. Enterobacteriaceae were enumerated using the most probable number method (MPN index). Enterobacteriaceae (n = 36), randomly isolated from three sites, were identified, biochemically characterized and were screened for sensitivity to 9 antimicrobials by the disk diffusion method. The isolated bacteria had shown variable susceptibility and resistance patterns in response to different antibiotics used in the study. Polymerase chain reaction based methods can be a powerful molecular technique for rapid, sensitive and specific detection. Hence, in the present study primers were also designed specific to virulence signature sequences and their specificity was assessed by BLAST.

Keywords: Antimicrobial Susceptibility, Resistance, Enterobacteriaceae, Potable water, Detection

ABSTRACT

Four Pd(II) and Pd(IV) complexes with 3-thiolanespiro-5’-hydantoin and 4-thio-1H-tetrahydropyranespiro-5’-hydantoin were synthesized. Thechemical structures of newcomplexes were studied by elemental analysis, IR, ¹H, ¹³C NMR spectra. The spectroscopic investigation of new palladium complexes in comparison with the metal free ligands show that the bonding of the ligands with metal ions is realized through the sulfur atom from the S-containing saturated rings. This coordination mode is in accordance with the data obtained for the platinum complexes with the same ligands. The new complexes were investigated for cytotoxicity on panel of human tumor cell lines. The tested compounds exerted concentration-dependent cytotoxic effects against some of the tumor cell lines.

Keywords: Pd complexes, cytotoxicity, S-containing saturated rings

ABSTRACT

Achievement of patient medication adherence remains challenging in Type 2 Diabetes management particularly population belongs to villages in South India.The aim is to assess adherence to anti diabetic drug therapy and self-management practice among type-2 diabetic patient by using Morisky-8-Item Medication adherence questionnaire at a community pharmacy located in South Indian village.: The results of morisky based questionnaire shows almost 84.8% of the respondents belongs to low adherence (>2). 15.2% having medium adherence and none having high medication adherence. The reasons including duration of disease, economy, co-morbidities, short consultation of time, multiple drug therapy and poor patient-health care professional relationship. However, short consultation of time and poor patient healthcare relationship are potentially modifiable to improve medication adherence in patients with diabetes.

Keywords: Morisky, Type 2 Diabetes

ABSTRACT

The study was aimed to determine antioxidant activity of methanolic extracts of both leaf and root of 12 nos. of therapeutically used mangrove species of Odisha coast using different antioxidant assays i.e., DPPH, FRAP and ‘Reducing Power’. Significantly higher DPPH radical scavenging effect was observed in leaf extracts of Heritierafomes (IC₅₀=13µg/ml). However, in root extract, the activity was higher in Rhizophoraapiculata (IC₅₀=17µg/ml). As far as total antioxidant content is concerned, Avicennia marina showed highest content i.e94.16±5.36 mg AEAC/g dry wt.in leaf sample and87.33±0 mg AEAC/g dry wt. in root sample. The highest FRAP value (4.75±0.08 mM AAE/g dry wt.)  in leaf samples was found in Cerberamanghas. Whereas, highest FRAP value (5.19±0.40 mM AAE/g dry wt.) in root extract was noted in Cynometrairipa. As regard to reducing power, Kandeliacandel showed highest activity e.g.,3.49±0.08 mg AAE/g dry wt. in leaf extracts among the studied species. In root extract, Aglaiacucullata exhibited highest reducing activity (3.35±0.01 mg AAE/g dry wt.). This study revealed that H. fomes, R. apiculata, A. marina, C. manghas, C. iripaand K. candelwere found to be good sources of natural antioxidants for pharmaceutical utilization.

Keywords: Antioxidant, DPPH, FRAP, Mangrove, Medicinal

ABSTRACT

Securinega leucopyrus (Willd.) Muell has long been used by the tribes of Sri Lanka traditionally known as ‘Katupila’and also in India as ‘Humri’. Common in scrub jungls, limited to India, Sri Lanka and Burma. DNA fingerprinting for cultivar or varietal identification has become an important tool for genetic identification in plant breeding and germplasm management.Several different PCR based techniques have been developed during the last decade, each with specific advantages and disadvantages. The Random Amplified Polymorphic DNA (RAPD) marker technique is quick, easy and requires no prior sequence information.Pharmacognostical evaluation of leaf and stem of Securinega leucopyrus (Willd.) already established but no research work have been established on its roots and DNA fingerprints; for the first time leaf samples were subjected to fingerprints and studied the pharmacognostical aspects of roots. Pharmacognostical study showed that presence of oil globules, rosette crystals and uni to multiserriate medullary rays. DNA finger prints showed that OPC 6, OPD 8 and OPB 10 showed that merging 2 bright bands and one light band.

Keywords:  Finger prints, Katupila, RAPD, Root, Securinega leucopyrus.

ABSTRACT

The present study was carried out to find out the antimicrobial activity and phytochemical analysis of Mint (Mentha arvensis) leaves solvent extracts against selected enteric pathogens. Plants have been an important source of medicine with qualities for thousands of years. In the present study, the antimicrobial efficacy of Mint leaves solvent extracts was examined using Ethanol, Methanol, Diethyl ether and Acetone as solvents and tested against nine enteric pathogens namely E.coli, Salmonella typhi, Sal.Para.A, Sal. Para. B, Shigella sonnei, Shigella dysentarie, Enterobactor spp.,Citrobactor spp.and Klebsiella spp. Antimicrobial analysis was done by using agar well diffusion method against selected enteric pathogens. The MIC values were determined by both agar and broth dilution method. The functional chemical group was determined by Fourier Transform Infrared Spectroscopy (FTIR).The Ethanol extract of Mint showed highest antimicrobial activity against Shigella sonnei., while lowest antimicrobial activity was observed by Ethanol extract of Mint against Citrobactor spp and by Acetone extract of Mint against Shigella dysentarie .The phytochemical analysis of Mint leaves solvent extracts showed presence of alkaloid, flavonoid, phenol, tannin, glycosides etc.

Keywords: Antibacterial activity, Mentha arvensis, Enteric pathogens, MIC, Phytochemical analysis, FTIR etc.

ABSTRACT

Physiological and biochemical analysis responses of 6-day-old seedlings of two pigeon pea (Cajanuscajan(L.) millspaugh) cultivars namely ICPL-85063 (short duration, lakshmi) and ICPL -87119 (medium duration, Asha) were studied. Stress was applied with polyethylene glycol (PEG-6000) and water potentials were: zero (control), -0.3Mpa (50mM),-1.1Mpa (100mM) and -2.3Mpa (150mM). In this study, the water stress effects on different parameters like chlorophyll content, protein and total amino acid content was measured following the standard methods. Total free amino acid content registered higher values in ICPL-85063. The protein and total chlorophyll content was observed as lower values when compared to their controls in lakshmi cultivar. It was observed that amino acid content was highest in stress level was -2.3Mpa and the least exist in blank. The results of chlorophyll content demonstrate a concentration dependant decline with increasing concentration of polyethylene glycol (PEG-6000). ICPL-85063 cultivar showed better performance in total amino acid content than Asha cultivar. It was established that the applied doses of PEG-6000 caused stress on young pigeon pea plants, which found suppression of photosynthesis.    

Keywords:CajanusCajan, water potential, water stress, amino acid, protein, chlorophyll content, polyethylene glycol, drought.     

ABSTRACT

The objective of this work was to develop and validate simple, rapid and accurate chromatographic method for determination of Desvenlafaxine succinate in solid dosage form. This RP-HPLC method was based on Reversed Phase High Performance Liquid Chromatography, on ODS C18 RP column (250 mm × 4.6 mm i.d., 5 μ), using Acetonitrile: Ammonium Phosphate buffer (pH 3.0) (70:30 v/v) as the mobile phase, at a flow rate of 1 mL/min at ambient temperature. Quantification was achieved by UV detection at 220 nm over a concentration range of 20-160 μg/mL for Desvenlafaxine succinate. The mean retention time for Desvenlafaxine succinate was found to be 2.44 min. The amount of Desvenlafaxine succinate estimated as percentage label claim was found to be 99.67.

Key words: RP-HPLC, Desvenlafaxine succinate, marketed formulation.

ABSTRACT

Meloxicam has been analyzed in a number of ways but the methods proved to be slow and tedious due to the involvement of buffers, maintaining of pH and lengthy process of HPLC or potentiometric titration. Our aim was development and validation of a new, fast, simple and inexpensive method for the analysis of Meloxicam by UV visible spectrophotometry. A new solvent system consisting of Acetonitrile and Methanol (70:30) was formulated by trial and error method. Different concentrations of meloxicam were made in this solvent system and were analyzed by UV visible spectroscopy. The absorbance was studied over the range of 240 to 400nm. The obtained results were used to study and calculate various validation parameters of this technique.  The calibration curve was found to be linear over the range of 0.1 to 0.6ug/ml with linear coefficient of 0.999. The precision was calculated to be equivalent to 0.251%. The LOD and LOQ of this method were found to be around 0.006ug/ml and 0.02ug/ml respectively. The system showed accuracy over the range of 90-100%. This method proved to be a good alternative to existing reported methods as it showed sensitivity, accuracy as well as reproducibility with low cost and time.

Keywords: Meloxicam; UV spectrophotometry; Acetonitrile

ABSTRACT

During June 2013 to October 2013, a total of 100 water samples were collected from various coastal regions of Trivandrum district, Kerala state, India. These samples were examined for the presence of pathogenic bacteria especially the pathogenic salmonella species. Water samples were collected in sterilized screw caped glass bottles, transported to the microbiology laboratory of Noorul Islam Institute of Medical Sciences, Neyyattinkara, Trivandrum, Kerala and processed according to the standard protocols for the identification of pathogenic Salmonella species, within 6 hours. The type of water included in the present study were pond water, river water, household water, well water, municipality supplied tap water and packaged bottled water. The present study revealed that the pond water, river water and household water were contaminated with pathogenic Salmonella species. The packaged bottled water and municipality supplied tap water devoid of Salmonella contamination. So based on the present study it is strongly suggested that water should be boiled before use or use packaged bottled water of good quality for drinking purposes.

Keywords: Salmonella, Selenite F broth,Wilson and Blair Medium, Gram staining. 

ABSTRACT

Acute promyelocytic leukemia is classified with a classic translocation  t(15;17) (q22;q12), and the other subtypes such as: t(11;17 ( (q23;q21) , t(11;17)) q13;q21)  t(5;17) (q35;q21).   Unfortunately, about 5% of APL subtypes, do not have a good prognosis due to resistance to ATRA.   Therefore, there is a major concern for hematologists and oncologists to diagnosis subtype of APL and start the treatments as soon as possible. 28 patients with suspected acute promyelocytic leukemia who hospitalized in two Iranian general hospitals were under study . In this study, we applied molecular and western blotting methods to detect major oncoproteins in APL subtypes. Cytogenetic results have been shown that the PML / RARa oncogene is positive in 26 of patients, and two of them did not have appreciated result. The results of western blotting showed that in 26 patients, the proteins with molecular weights 115 and 85 KD was detected by specific anti-RARa antibodies. The western blotting assay for one patient showed the protein with molecular weight of 85 KD was detected by specific anti- PLZF antibodies. The results indicate that the molecular and western blotting techniques were able to differentiate the APL with t (15; 17) from the other subtypes, like t (11; 17). We indicated by western blotting, two oncoproteins:  PML / RARa and PLZF / RARa, respectively to the relative two translocation t (15; 17) and t (11; 17). Western blotting techniques can be a substantial contribution of to the final diagnosis of leukemia.
Keywords: Acute promyelocytic leukemia, oncoprotein, western blotting

ABSTRACT

Herein, a series of azetidinone derivatives incorporating dihydropyrimidinone moiety 4(a-h) were prepared. The structures of newly synthesized compounds were confirmed on the basis of elemental analysis, FTIR and ¹H NMR spectroscopy. The synthesized compounds were evaluated for their anthelmintic and anti-bacterial activity and it was found that the compounds were pharmacological active and gave appreciable results.

Keywords: Azetidinone derivative; anthelmintic; anti-bacterial.

ABSTRACT

For Indigenous people, food is also a medicine; they have rich traditional practices of using food in the management of various health problems. Arunachal Pradesh is a mountainous state with full of floral resources; aborigines of this state use numbers of food plants in their health practices. The folk food system in Arunachal Pradesh is composed mostly of semi-domesticated and wild collected vegetables. The present study was carried out to document the folk medicinal food plants used among the indigenous people of East Siang District of Arunachal Pradesh. The folk food plants are studied under nutraceutical point of view. Our work revealed a total of 36 plant species of folk medicinal food plants. The findings are given with scientific name, local name and uses as food and medicine in the paper.

Keywords: Folk food, Nutraceutical, Indigenous people, Medicinal plant.

ABSTRACT

3-(2-bromacetyl) phenyl benzoate is key starting material used in synthesis of phenylephrine, (R)-3-[-1-hydroxy-2-(methylamino)ethyl]phenol which is selective α1-adrenergic receptor agonist used primarily as decongestant, as an agent to dilate the pupil, and to increase blood pressure. Hence the current research work was aim to synthesize a series of 3-(2-bromacetyl) phenyl benzoate  derivatives by treatment of secondary amines with carbon disulphide and 3-(2-bromacetyl) phenyl benzoate  in presence of strong base in ethanol afforded the corresponding Dithiocarbamates. Their chemical structures are characterized by ¹H &¹³C NMR, MS, Elemental analysis, and chromatography methods (TLC). The antimicrobial activity was evaluated by their MIC and zone of inhibition by taking Penicillin, Streptomycin and Amphotericin as standard reference drugs. The microbial assay revealed that compounds D4 and D5 showed the most potent antimicrobial activity against variety of bacteria as well as fungal isolates, which may be a promising antimicrobial leading compound for the further research.

Keywords: 3-(2-bromacetyl) phenyl benzoate, Dithiocarbamates, Carbon disulphide, Antimicrobial activity.

ABSTRACT

The present study highlights the living condition and the ethnomedicinal knowledge of the Irulasin the Gingee hills, Villupuram District, Tamilnadu. Extensive field surveys were conducted in seven villages in Gingeetaluk. Living conditions and ethnobotanical knowledge were taken through personal interview. A total of 16 species of 11 families were documented. The present study observed that the Irulasin Gingee hills have very sound knowledge of medicinal values of plants. This type of studies may help in the pharmacological research in various dimensions.

Keywords:Ethnobotany, ethnomedicinal, irulas, pharmacognosy

ABSTRACT

Amlodipine Besylate is a molecule used in Hypertension and currently available in tablet dosage form. The objective of present study was to develop and evaluate Amlodipine Besylate intraoral sublingual formulation for faster release and absorption. Four formulations containing varying concentrations of Croscarmellose sodium and b-Cyclodextrin were formulated. Various evaluations like weight variation, % friability, Hardness, diameter, water absorption ratio, wetting time, disintegration time, drug content and calibration curve were performed. From the results, it was concluded that all batches pass the evaluation tests with F4 showing the fastest wetting and Disintegration. From the data of Dissolution studies it was concluded that formulation F4 showed highest drug release in 10 minutes. It can be concluded that sublingual tablets of Amlodipine Besylate will prove to be patient friendly.

Keywords: Amlodipine Besylate, Croscarmellose sodium, b-Cyclodextrin, sublingual