Abstract

A simple, extraction free spectrophotometric method for the quantitative estimation of levetiracetam (LEV) in bulk drugs and pharmaceutical formulations (tablets) has been developed. The method is based on the oxidation of 2, 4- dinitrophenylhydrazine (2, 4-DNP) and coupling of the oxidized product with drugs to give intensely colored chromogen. Levetiracetam at its λmax 455 nm shows linearity in the concentration range of 30-130 µg mL^-1. The relative standard deviation for this method is 0.422%. Linear relationship with good correlation coefficients (0.995-0.996) was found between absorbance and the corresponding concentrations of the drug. The reliability and performance of the proposed method was validated statistically the percentage recovery ranged from 99.88 and 100.2. The results of analysis for this method have been validated statistically and by recovery studies.

Abstract

Green leafy vegetables (GLV) consumption has been reported to contribute to lowering the risk of age-related cataract. These are known to contain antioxidants necessary in neutralizing free radicals which are known human chemical hazards.Green leafy vegetables have been identified as good sources of natural antioxidants such as tocopherols, vitamin C and polyphenols which are responsible for maintaining good health and protect against coronary heart diseases and cancer. GLV are the major sources of lutein and, in developing countries where access to animal food is restricted, contribute substantially to fighting retinol deficiencies by being rich sources of the provitamine A, β-carotene, not withstanding bioavailability issues.In the present study evaluation of synergistic antioxidant activity of extract from Ocimum gratissimum, Vernonia amygdalin and Alternanthera sessilis were carried out. Synergistic antioxidant activity of the leaf extract were carried out using DPPH, H₂O₂ and Nitric oxide scavenging assay at 100 µg/mL and 200 µg/mL and compared with the standard Ascorbic acid. In the present study, extract showed a significant effect in inhibiting DPPH, reaching up to 85.00% (Combined extract) at concentration of 200 µg/mL. The extract showed a significant effect in inhibiting H₂O₂, reaching up to 84.00 % (Combined extract) at concentration of 200 µg/mL. The extract showed maximum activity of 85.00 % (Combined extract) at 200 µg/mL, where as ascorbic acid at the same concentration exhibited 94.96% inhibition in Nitric oxide scavenging assay.

Abstract

Dry seeds of the fruits of the plant, Solanum lycopersicum (family:  Solanaceae), are highly valued in traditional medicine in the treatment of various human diseases, including diabetes mellitus and obesity. In the present study, the hypoglycaemic and weight loss effects of 50 - 200 mg/kg of the aqueous seed extract of Solanum lycopersicum (SL) were investigated in normal and drug-induced hyperglycaemic rats. In addition, the acute oral toxicity using the preliminary and the main tests of the Up-and-Down Procedure according to OECD/OCDE Test Guidelines on Acute Oral Toxicity was conducted. Phytochemical analysis of the aqueous seed extract was also carried out. Results showed that SL caused progressive and significant (p<0.05, p<0.01 and p<0.001) dose-related reduction in the blood glucose concentrations in normal and drug-induced hyperglycaemic rats. SL also caused significant (p<0.05 and p<0.01) dose-dependent reduction in the average body weight of treated rats when compared to untreated rats.  Results of the phytochemical analysis of SL revealed the presence of alkaloids, flavonoids, tannins and glycosides.

Abstract

Solid dispersions (SDs) of etravirine (ETR) were prepared with the objective of dissolution enhancement by solvent evaporation technique by using polymers like PEG 6000 and PVP (k30).  In vitro dissolution studies of SDs performed in 0.1 N HCl and pH 6.8 phosphate buffer solution showed a significant increase in dissolution rates of ETR comparing to physical mixtures and pure drug. Comparatively, SD of ETR: PEG 6000 and ETR: PVP (K30) in various weight ratios (1:2, 1:4, 1:6) were prepared by solid dispersion method exhibited a higher release rate than the conventional method. Improved dissolution of model drug may be attributed to the modification in drug crystalline in SDs as was evident from our analytical studies. The dissolution pattern of the ETR from all the SDs followed predominantly, first order kinetics. This study reflects the vital role of polymers as a novel approach to improve the solubility of ETR, which could minimize the variable dissolution rates with increase in bioavailability.

Abstract

Simple, extraction free spectrophotometric method for the quantitative estimation of Lamotrigine (LMT) in bulk drugs and pharmaceutical formulations (tablet) has been developed. It is based on the diazotization of drug with nitrous acid, to form diazotized compound, followed by its coupling with N-(1-naphthyl) ethylene- diamine dihydrochloride [Bratton-Marshall reagent] to form a violet colored compound. Lamotrigine at its λ max of 464 nm shows linearity in the concentration range of 50-350 µg/ml. The relative standard deviation for Lamotrigine is 0.308% was obtained. Linear relationship with good correlation coefficients (0.998) was found between absorbance and the corresponding concentrations of the drug. The reliability and performance of the proposed method was validated statistically the percentage recovery ranged from 100.1% and 99.7%. The result of analysis for the method has been validated statistically and by recovery studies.

Abstract

Matrix type of ocular insert was prepared using starch isolated from un-ripped bannana in different concentration by solvent casting method. The compatibility study of drug and polymer was performed by FTIR. Physicochemical evaluations like weight variation, thickness, content uniformity, moisture absorption, moisture loss test were performed. In vitro release study was carried out for all formulations and overall results revealed that as concentration of starch increases there was slow release of Timolol maleate occurred from the formulation.  It proved that drug and polymer are compatible to each other; there was no interaction between drug and excipients.  The weights of all inserts were found to be in the range of 32.29 to 7.63 mg with least standard deviation.  The thickness of the prepared insert varies from 0.063 to 0.099 mm.  The drug content of all the formulation was found to be in the range of 98.11 to 99.40 %.  The surface pH of the prepared inserts varied between 7.2 to 7.4, which is comparable with the pH of tear fluid i.e. 7.4.  The folding endurance of all the formulations was found to be good.  Moisture absorption of prepared formulations was found to be in the range of 4.41 to 7.51 %.  Moisture loss of prepared formulation was found to be in the range of 2.00 to 4.89 %. The in vitro release of drug from the different ocular insert was studied using the classical standard cylindrical tube fabricated in the laboratory (bi-chambered donor receptor compartment model).  It was observed that almost 100 % drug released from all formulations occurred at the end of 180 to 300 minutes. Fast release of drug from formulation F1 occurred may be due to low concentration of starch. The overall result revealed that as the concentration of starch increases there was slow release of drug from formulation occurred

Abstract

Artemisia species are used in traditional medicine for the treatment of various ailments such as indigestion, infection, irregular menstruation, cramp, cold, epilepsy, typhoid, tuberculosis, urinary calculi, colic, fever, asthma, bronchitis, sciatica, flatulence, anaemia, insomnia, gout, depression, nervousness, hysteria, measles, bruise, chilblain, leprosy, malaria and cancer. Similarly, most species has been used as antiseptic, antioxidant, anthelmintic, expectorant, diuretic and insect repellent.  The biological activity shown by the plants was due to the essential oil present in them. The present study describes the fractionation of essential oil and its antioxidant potentialities in two allied species - Artemisia japonica Thunb. and A.nilagirica (Clarke) Pamp. The essential oil from Artemisia japonica and A.nilagirica was isolated by hydrodistillation and analyzed by GC-MS. 30 and 19 compounds were noticed in the oil respectively. The predominant phytocomponents in the essential oil of A.nilagirica were camphor (41%), 8-Cineole (17.0%), Borneol (8.6%) Artemisia ketone (6.4%) and β-Thujone (6.0%). Meanwhile A. japonica contain Linalool (70.4%), Caryophyllene oxide (6.7%), trans-Linalool oxide (4.5%), p-cymene (3.4%) and 1, 8-Cineole (2.3%). Significant antioxidant potentialities was displayed in terms of  DPPH scavenging, beta carotene bleaching, total antioxidant activity, soybean oil rancidity and sun flower oil free fatty acids and iodine values. Interestingly, A.nilagirica showed remarkable antioxidant potentialities and was comparable with synthetic antioxidants such as ascorbate, butylated hydroxytoluene and BHA. The present study suggests that the tested Artemisia species revealed a pool of potential biomolecules in the essential oil and also exerted remarkable antioxidant values. Further studies are warranted to isolate and purify the principle component from the essential oil.

Abstract

Transdermal drug delivery system is being extensively investigated as a viable alternative to drug delivery with improved bioavailability. The aim of the present investigation is to develop membrane type Transdermal drug delivery patches of antihypertensive agent Ramipril. Transdermal patches of Ramipril were prepared by using polymers, like HPMCK15M, Ethyl Cellulose and PVPK30. The patches were transparent, smooth and flexible. The results of weight variation, thickness, moisture content, moisture uptake, Folding Endurance, Tensile strength, drug content with the range. The patches were evaluated by DSC and SEM to ensure compatibility of drug with polymer and . The optimized formulation R5 is 96.42% drug release after 24 hours uniform distribution of the drug.

Abstract

Itraconazole, a potent antifungal drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, itraconazole, with sodium starch glycollate, croscarmellose sodium, eudragit E-100 for the enhancement of the solubility and dissolution rate of the drug. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The dissolution was enhanced greatly in the itraconazole with croscarmellose sodium (1:7 ratio). The best formulation, itraconazole with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 in 1:1 ratio by milling for almost 10min to form ternary mixture. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows first order release. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time. The increased dissolution rate was achieved by more than seven times and ten percent comparatively to the itraconazole API and marketed product respectively.

Abstract

Enoyl-ACP reductases catalyze the final step in the elongation cycle of the bacterial fatty acid biosynthesis (FAS-II) pathway, has been recognized as a promising target for the development of new drugs for TB. Here we present the discovery of a quinoline class of compounds as inhibitors of this enzyme using a combined approach of rational selection of compounds for screening, analogue search and docking studies. Various arylhydrazides were added to 3^rd position of the 2-chloro/2-methoxy-quinoline nucleus to evaluate their influence on the activity toward Mycobacterium tuberculosis H₃₇Rv (MTB) and Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Vibrio cholera. Structures of these compounds were established by FTIR, ¹H NMR, ¹³C NMR and mass spectroscopy. The synthesized compounds showed a MIC range of antitubercular activity, extending from 0.2 to 3.125 µg/ml against M. tuberculosis H₃₇Rv. Among the Schiff bases, compound 6b, 6c and 6e exhibited highest activity against the tested mycobacteria at a MIC of 0.2 µg/mL. Hydrogen bonding pattern and Cscore for compounds 4a-e, 6a-6e, 7a and 8a found satisfactory on enoyl ACP-reductase enzyme. Compounds showed promising inhibitory potency because of replacement of 2^nd position chlorine atom with electron-donating methoxy group which can cause a compound to become less acidic. Analysis of the docking study provided details on the fine relationship linking structure and activity, and offer clues for structural modifications that can improve the activity

Abstract

The two factorial design was used to develop the controlled release mucoadhesive peroral in situ gel containing voriconazole as drug candidate. Carbopol 934P and hydroxy propyl methyl cellulose (HPMC E50) were taken as formulation factors (independent variables). Gelation time (R1), Mucoadhesive Strength (R2), drug release at 1 hour (R3), drug release at 8 hrs (R4), drug release at 12 hrs (R5), and Gel strength (R6) were taken as responses (dependent variables). The polymers had significant effect on gelation time, mucoadhesive strength, drug release at 8^th hour. It was found that carbopol shows higher mucoadhesive strength than HPMC E50. Comparatively carbopol controls the drug release greater than that of HPMC E50. The n value of Peppas equation for optimized formula is 0.67 which indicates that optimized formulation follows non-Fickian release mechanism. The FT-IR and DSC studies indicate no physic-chemical interaction. Stability studies revealed that optimized formulation was stable. The predicted values of optimized formula like gelation time, mucoadhesive strength, drug release at 1 hr, drug  release at 8 hrs, drug release at 12 hrs,  and gel strength are 82 sec, 17150 dynes/cm, 23.2%, 64.1%, 91.1%, 52.0 sec respectively and the actual values found to be 82 sec, 17540 dynes/cm, 21.0%, 63.0%, 91.1%, 52 sec.

Abstract

A  Rapid, isocratic UPLC method was developed and validated for simultaneous estimation of Sulfamethoxazole (SMX) and Trimethoprim (TMP) in Tablet formulation. The separation was selected by using a column with BEH C18 (50 x 2.1mm, 1.7µm) and further elution was also optimized using buffered mobile phase (0.1% v/v Phosphoric acid) and Acetonitrile as a modifier in a ratio of 14:86v/v, with a flow rate of 0.5 ml^-1. This UV Detection of these compounds was monitored at 210nm. The retention times for Sulfamethoxazole (SMX) and Trimethoprim (TMP) were found to be 0.6, 1.5 min, respectively. The validation Results were found to be linear in the concentration range of 5-50 μg/ml for SM and 5-30 μg/ml for TP. The Intra-day and Inter-day variation, as RSD (%), was found to be <1.0%. The % Mean Recovery was found to be within 98-102%. The results showed, the method was demonstrated that this proposed UPLC method to be Specific, Linear, Precise, Accurate and Robust for simultaneous determination of SMX and TMP in combined dosage form.

 Abstract

A novel nitrogen containing analogues of podophyllotoxin 6a-d i.e., substituted 5-phenyl-4,5-dihydro-2H-benzo[g]indazoles were synthesized in high yields by the condensation of   hydroxylmethylene tetralones and hydrazine hydrate in absolute ethanol. The structures of the compounds were confirmed by IR, ¹H-NMR, ¹³C-NMR, Mass spectral and elemental analysis data. The new compounds were evaluated for their antimitotic activity by onion root tip method and also antimicrobial activity against bacterial and fungal strains. The antimitotic activity was compared with control, compound 6d showed more potent inhibitions and compound 6c exhibited moderate inhibitions. The antimicrobial activity of the synthesized compounds were compared with standards, compound 6d showed excellent activity and compound 6c showed moderate activity against bacterial and fungal strains. In the antimicrobial activity, among the synthesized analogues 6a-d, compound 6d showed high activity against all the bacterial and fungal strains. Hence, compound 6d showed very good activity in both antimitotic and antimicrobial activity.

Abstract

The aim of the study was to investigate the anti-arthritic activity in methanolic and hydro alcoholic extracts of Withania Coagulans dunal fruits i.e. WCME and WCHAE by in vitro procedures in past. Phytochemical analysis has indicated presence of alkaloids, flavonoids, glycosides, steroids, saponins, fixed oil, carbohydrates. Both the extracts have showed anti-arthritic activity by Protein denaturation method, Membrane stabilization method, and Protienase inhibitory method in all various concentrations i.e. 50,100, 150, 200, 250µg/ml. The IC₅₀ value of WCME, WCHAE and Diclofenac sodium (standard) was found to be 145.37µg/ml, 124.25µg/ml, 106.29µg/ml in case of membrane stabilization method, 127.41µg/ml, 103.24µg/ml, 87.14µg/ml in case of protein denaturation method and 166.4737µg/ml, 126.9737µg/ml, 94.5737µg/ml in case of proteinase inhibitory method respectively. Maximum inhibition of 68.80±2.262%, 72.01±3.565% and 79.5±5.35% at 250 µg/ml ml in case of membrane stabilization method, 70.59±7.02%, 75.51±6.59% and 80.99±6.379% in case of protein denaturation method and 65.72±6.94, 65.86±5.5 and 80.27±2.88%  in case of proteinase inhibitory method by WCME, WCHAE and Diclofenac sodium (standard) respectively. Both the extracts showed the good dose dependent activity in three of the in vitro models. But WCHAE showed the most significant anti-arthritic activity than WCME. The findings of the present study suggested that Withania Coagulans dunal fruits could be a potential natural source of anti-arthritic activity.

Abstract

Biodegradation and bioremediation both are same processes which are based on the metabolism of pesticide and insecticides by microorganisms. Microorganisms which are used for the process of bioremediation are known as bioremediators.In this experiment we used an organophosphorus compound i.e. Monocrotophos (MCP) pesticide. Aspergillus fumigatus is one of the Aspergillus species to cause disease in human being with an immunodeficiency. Addition of Tween 80 stimulates the utilization of hexamer. When Aspergillus niger combined with Tween 80 this mixture effectively enhanced the solubility and degradation of MCP. Bioremediation of Monocrotophos at different concentration by using Aspergillus fumigatus and the kinetics effect of Tween 80 on fungal growth were studied and found that the A. fumigatus degrade the MCP till its 1% concentration.

Abstract

A simple, precise and reversed phase liquid chromatographic (RP-LC) method was developed and validated for estimation of valsartan in bulk drug. The separation was achieved on Acquity HSS T-3 1.8µ, (2.1 X 100) mm, Make: Waters, analytical column with mobile phase consisted of buffer (10mM Potassium dihydrogen phosphate with 0.05% triethylamine in water, adjust pH  3.0 with dilute phosphoric acid) : Acetonitrile (50:50v/v) at isocratic flow of 0.35ml/min with UV detection wavelength was at 205 nm and 3μl of sample volume was injected. The retention time of valsartan was found to be 1.9 minute. The method was successfully validated in accordance to ICH guidelines for accuracy, precision, specificity, linearity. The linear regression analysis data for calibration plots showed good linear relationship in the concentration range 25-75μg/mL for valsartan. The % Recovery/Accuracy was within the range between 98% and 102%. The percentage RSD for precision method was found to be less than 2%. The method was validated as per the ICH guidelines. The method was successfully applied for routine analysis of valsartan in bulk samples.

Abstract

A simple isocratic liquid chromatographic method was developed and validated for the quantitative estimation of valgancyclovir bulk and dosage form. Chromatograph was carried on Waters C₁₈ (4.6 x 250mm, 5 mm) column with mobile phase comprising of acetonitrile and 0.01M potassium dihydrogen phosphate buffer in the ratio 45:55 v/v and pH was adjusted to 5±0.2 with orthophosphoric acid. The flow rate was adjusted to 0.6 mL /min with UV detection at 254 nm. The retention time of valgancyclovir was found to be 3.6min. The different analytical parameters such as linearity, accuracy, precision, robustness, limit of detection (LOD), limit of quantification (LOQ) were determined according to the  International Conference on Harmonization (ICH) Q2B guidelines. In the linearity study, the regression equation and coefficient of correlation for valgancyclovir were found to be Y= 42324x –20135 (R²=0.999). The proposed method is highly sensitive, precise, and accurate.

Abstract

A simple, sensitive and statistically comparable spectrophotometric method for the estimation of allopurinol in tablet dosage form was developed drawing on hydrotropic solution of 8M urea as solubilizing agent. The allopurinol is partially soluble in water and it requires number of organic solvents for its estimation. Thus its (allopurinol) aqueous solubility was raised to more than 66 folds and further estimates by using the cheapest solvent distilled water. The drug stability in hydrotropic solution was found to be more than 48hrs.The allopurinol hydrotrope shows maximum absorbance at 250.5nm obeying Beer’s – Lambert law in the range of 1 – 20 µg/ml. The correlation coefficient for allopurinol hydrotrope was found to be 0.9976 which adds the reliability in the linear response. The non-interference of hydrotropic agent and additives in the course of allopurinol estimation ensures the specificity of the proposed method. The mean recovery be a sign of accuracy was obtained in good terms as 100.12%.The precision results of proposed method were found to be less than 2% as limit expressed in %RSD. The comparison of proposed method with standard method (IP 2010) further validate the results of proposed method. The validation (as per ICH 2005) of the proposed method accesses its use in the routinely quality control of allopurinol in tablet dosage form.

Abstract

The knowledge of the accessory renal arteries has grown importance with the increasing number of renal transplants and other uroradiological procedures. Renal artery variations include their origin, number and course. The most common is the presence of additional vessels (accessory arteries) arising above the usual trunk is more frequent than one arising below. The accessory renal arteries are always end arteries. There may be several renal arteries on each side or the renal artery may divide close to its origin into several branches. Normal renal arterial information is useful for planning and performing of endovascular, laparoscopic uroradiological procedures and renal transplants. In order to facilitate the clinical approaches, we studied renal arterial pattern in 50 embalmed cadavers during the period of one year to establish the incidence of accessory (aberrant) renal arteries in human cadavers and their incidence.

 Abstract

Flavonoids are polyphenolic compounds found to have enormous pharmacological activity, Naringin, a molecule with a wide spectrum of pharmacological activity still has not been used for treatment of any diseases due to its lacking potency. The present study was focused to synthesize various derivatives of naringin and to evaluate their anthelminthic activity. Among the various synthesized compounds, N.b, N.h, N.g, & N.q, have shown very potent activity against the worms with low paralysis time as well as death time. Thus more studies have to be carried out on these derivatives for a potent and safe anthelmintic agent,

Abstract

The aim of the present work is the evaluation of anti-diabetic activity of leaves of diospyros melanoxylon (roxb.) Approximately about 200g of shade-dried powder of leaves of Diospyros melanoxylon (Roxb.) was extracted successively with 1200ml (1:6) of various solvents in an increasing order of polarity viz., Petroleum ether, Chloroform, Ethanol in a soxhlet apparatus at room temperature for about 14 hours and aqueous extract was prepared by maceration process. The glibenclamide (2.5 mg/kg) treated normal rats show a mean (±SEM) fasting serum glucose of 96.3±0.42, 75±0.57, 63.83±0.60, 44.8±0.54, 46.3±0.3, 49.66±0.33 and 52.33±0.61  mg/dl on on 0, 1, 2, 4, 8, 12 and 24 hr respectively in normoglycemic rats. The observations show that the D. melanoxylon extracts (ethanolic and aqueous) reduces the fasting serum glucose of normal rats at the dose of 200 mg/kg, b.w. of EEDM and AEDM  i.e. ehtanolic and aqueous extract of Diospyros melanoxylon was able to reduce fasting serum glucose which was comparable with the reduction caused by glibenclamide. The above observations show that the ethanolic and aqueous extracts of leaves of Diospyros melanoxylon  reduces the fasting serum glucose of diabetic rats at the dose of 200 mg/kg, b.w. of EEDM and AEDM  i.e. ehtanolic and aqueous extract of Diospyros melanoxylon was able to reduce fasting serum glucose which was comparable with the reduction caused by glibenclamide. All the alloxon induced diabetes rats showed significant elevation of serum cholesterol, triglyceride, urea and creatinine levels compared to the normal control during the 21 days of study period.

Abstract

Stability indicating simple, sensitive method has been developed for the simultaneous determination of Cefpodoxime proxetil and Diclofenac sodium using Ultra fast liquid chromatographic method (UFLC). The analyses were performed on Kromasil C18, (250 × 4.6mm, 5μm) column using 1% formic acid in methanol and acetonitrile (80: 20 v/v) as mobile phase with flow rate 1 mL/min. The eluents were monitored with PDA detector at 270 nm. In this developed method Cefpodoxime proxetil and Diclofenac sodium elutes at a retention time of 2.30 and 3.06 min respectively. The proposed optimized method is having linearity in the concentration range from 15 to 50µg/mL of Cefpodoxime proxetil and Diclofenac sodium. The present method was validated with respect to linearity, system suitability, precision, accuracy (recovery) limit of detection (LOD) and limit of quantification (LOQ), and robustness according to the ICH guidelines. Forced degradation studies have also been carried out to check out the stability of the drugs under acidic, alkaline, thermal, Oxidation and UV degradation conditions. The proposed method can be readily utilized for determination of Cefpodoxime proxetil and Diclofenac sodium.

Abstract

Curcumin has numerous biological and pharmacological activities, with no major side effects, and is currently being used in several clinical trials for treating several disorders, including Alzheimer’s disease, hypercholesterolemia, neurological disorders, cancer and  anti ulcer activity, but its  having poor solubility and stability. The aim of this work was to investigate the effects of formulation variables on development of curcumin nano cubosomal  formulations as potential oral  delivery systems. Curcumin cubosomes  were prepared   homogenization  method. A 3² full factorial design was employed to evaluate individual and combined effects of formulation variables, namely polyoxmar 407, glycerol monooleate, and entrapment  efficiency.  Prepared  curcumin nano cubosomes were evaluated regarding entrapment efficiency (EE%), particle size analysis, zeta potential, microscopic examination and  TEM. Anti ulcer activity  model was  followed by  pyloric ligation.  Anti ulcer activity was evaluated by   ulcer index, gastric volume, gastric P^H, total acidity and free acidity. The formulation CF6 having high percentage of entrapment  efficiency  and when compared with the other formulations.   The  optimized CF6  particle size of the formulation was about 43 nm  and zeta potential -17  kv.  Formation of cubosomes confirmed by transmission electron microscopy and optical microscopy. The anti ulcer activity  of curcumin cubosomes more than pure curcumin.  The developed curcumin loaded cubosomal  gave rise to stable, nano-sized vesicles, able to improve curcumin  anti ulcer activity in oral drug  delivery.

Abstract

The objective of the study is to formulate and evaluate Rabeprazole Delayed Release Enteric tablets comparable to the innovator product. Five formulations of  enteric coated tablets of Rabeprazole were developed by preparing core tablets using mannitol as diluent and Crospovidone as super disintegrant in different proportions and varying the compositions of sub coating and enteric coating using opadry white and enteric yellow .The core tablets were prepared by direct compression method. In the preformulation studies the micromeritic flow properties of the API were assessed by determining angle of repose, compressibility index, Hausner ratio. The results indicated good free flow of Rabeprazole. As such formulation F5 developed is considered as an efficient delayed release formulations of Rabeprazole comparable to the innovator product. Thus the study fulfilled the objective of developing efficient Rabeprazole delayed release tablets. 

Abstract

The basic algid is to admix and characterize atypical thiazolidinone derivatives and covering them for anti-hyperglycemic activity. An alternation of ten 2-(substituted phenyl)-3-[{4-(1-naphthyl) - 1, 3 -thiazol-2-yl} amino] -4-oxo- 1, 3) -thiazolidin-5-yl] acetic acid (TA₁-TA₁₀) were synthesized from 1-acetyl naphthalene. The synthesized compounds are characterized on the basis of satisfactory analytic and spectral (IR, H1NMR, Mass and elemental) data. Studies were agitated out for the synthesized  compounds which were as able evaluated for anti-hyperglycemic activity in albino rats  of Wistar strain by appliance of a Sucrose Loaded Rat Model (SLM) and Alloxan-Induced diabetic rat model. The synthesized compounds showed adequate arise in Sucrose Loaded Rat model and the clinical study was involved in evaluation of blood glucose lowering ability of of [2- (substituted phenyl)-3 - [{4-(l -naphthyl) - 1, 3) -thiazol-2-yl} amino] -4-oxo- 1, 3 –thiazolidin-5-yl] acetic acid (TA₁-TA₁₀) in accustomed rats in sucrose loaded model. It was served that compound TA₁ (Ar = 4-nitrophenyl) displayed accomplished anti-hyperglycemic activity in SLM model. This was followed by TA₄ (Ar = 2, 4-dichlorophenyl), TA₅ (Ar = 2, 6- dichlorophenyl), TA₆ (Ar = 3-fluorophenyl). TA₈ (Ar = 4-chloro-2-hydroxyphenyl) and TA₁₀ (Ar = 4-methoxyphenyl). In Alloxan induced rat model, clinical study showed that a lot of compounds exhibit more anti-hyperglycemic activity than standard drug Pioglitazone on 7^th day of study. These compounds included TA₁ (Ar = 4-nitrophenyl), TA₄ (Ar = 2, 4-dichlorophenyl), TA₅ (Ar = 2, 6-dichlorophenyl), TA₆ (Ar = 3-fluorophenyl), TA₈ (Ar = 4-chloro-2-hydroxyphenyl) and TA₁₀ (Ar = 4- methoxy phenyl). The compound TA₁ exhibited highest activity followed by TA₈, TA₆, TA₅, TA₄ and TA₁₀. It was as well observed that the blood glucose lowering effects were more pronounced and stronger in alloxan model. We address the acknowledged amalgam of atypical thiazolidinones, as able-bodied as their spectral characterization, and anti hyperglycemic action which, for some, is above to currently acclimated as anti-hyperglycemic agents.

Abstract

Stroke is a major public health challenge, not only for neuropharmacology but the society in general. This study was conducted to describe and obtain the baseline data about the prescribing pattern of drugs in stroke patients. A prospective study was conducted in a multi specialty hospital over a period of seven months. The pharmacological therapy prescribed was analysed to determine the prescribing pattern of drugs in a total of 124 patients. It was observed that enoxaparin was given to 59 and heparin to 11. Aspirin was administered to 84 and clopidogrel to 19. Patients with hypertension were treated with different classes of antihypertensives. Stroke patients who suffered seizures were given phenytoin (27). Atorvastatin was administered to 83 and mannitol to 38. Antipsychotics (26) and CNS stimulants (13) were also administered. Stroke patients are at a high risk of hospital acquired infections therefore antibiotics were given in 96 patients. Lactulose was given in 75 and multivitamins to 59. Majority of the stroke patients were prescribed anticoagulants, anti platelets and dyslipidemics. The prescribing pattern of drugs should be based on specificity and severity of stroke in order to facilitate rational use of drugs providing optimal care.  Pharmacists are in a key position to provide pharmaceutical care to stroke survivors and initiate or recommend appropriate pharmacotherapy where indicated. Integration of a role of pharmacist in the management of stroke is crucial and improves outcomes of patients.

Abstract

Antimicrobial peptides (AMPs) play a vital role in innate and adaptive immunity acting as multifunctional molecules in offering in vitro antimicrobial activities, immunomodulation, mediation of inflammation, cell proliferation, migration, wound healing etc., Herein We demonstrate the antibacterial and wound healing properties of certain protein compounds partially purified from the heart tissues of certain selective slaughter house animals (goat, cow and chicken) by chemical methods.  The antibacterial proteins (ABPs) were semi purified by consecutive procedures of acid extraction, 30% ammonium sulphate precipitation and dialysis.  The yields of respective ABPs were found to be 46.1, 48.3 and 49.4 mg/g wet weight.  The proteins isolated from the heart tissues of these three animals were tested for their antibacterial activities by performing Minimum Inhibitory Concentrations (MICs).  They exhibited potential antibacterial activities against all the eight test isolates.  The MICs of the protein solutions fell in the range of 8-63 mg concentrations.  Subsequently their wound healing properties were carried out on rat wound models.  These proteins showed 96.7%, 96.9% and 100% of wound healing activities respectively on excision wound models of albino rats at 9^th post wounding day.  The result was significantly better than the wound models treated with negative and positive controls.  The proteins were also characterized for TLC patterns and absorption spectra.  The post TLC of each protein sample showed only a single band with Rf value in a narrow range (0.341 to 0.364).  The λ-max of the proteins was found to be 280 nm invariably.  The results conclude that the semi-purified ABPs from the heart tissues of goat, cow and chicken fulfills the major criteria such as natural occurrence, low molecular weight, antibacterial and wound healing potentials to render themselves as natural antibiotics for the treatment of infectious diseases.

Abstract

The aim of this investigation was to develop the potential application of a microemulsion as an oral drug delivery system for ranitidine. The bioavailability of ranitidine after oral administration is about 50% and absorbed via the small intestine. Therefore an attempt was made to develop an oral microemulsion formulation for enhancing the bioavailability of ranitidine is a BCS class III drugs which are known to have high solubility but low permeability. The here developed  microemulsion system was optimized by using pseudo ternary phase diagrams, composed of ground nut oil, Tween-80, PEG-400 and distilled water. The optimized microemulsion formulation contained ground nut oil (6.67%), Tween-80 & PEG-400 [60%(2:1 ratio)], and distilled water (33.33%), was evaluated for its transparency, droplet size, polydispersity index, zeta potential, viscosity, conductivity, DSC studies, SANS studies and Transmission electron microscopy (TEM). The droplet size (10 times diluted) and zeta potential (10 times diluted) was found to be 16.2 nm and -3.02 mV respectively. DSC thermograms suggested the presence of bulk water and free water in the formulation. Small angle neutron scattering (SANS) studies explained structural parameters of the formed micelles were obtained by fitting the micellar volume fraction, core radius, hard sphere radius. Also, spherical nature and size homogeneity of the microemulsion droplet was seen in the TEM photograph of the microemulsion. Thus the present study indicates that microemulsion can be a promising vehicle for the oral delivery of ranitidine.

Abstract

A rapid, specific and accurate HPLC method was developed for the determination of Febuxostat in human plasma using Ornidazole as internal standard. The extraction process involved a liquid – liquid extraction using 70:30 % v/v 0f t-butyl methylether and dichloromethane.  Both Febuxostat and the internal standard were eluted under isocratic mode using an YMC, C4 (4.6 X 150 mm, 3 µm) column. The mobile phase composed a mixture of 60:40 % v/v Methanol and 0.1% v/v ortho phosphoric acid at a flow rate of 1.0 mL/minute. The wavelength of detection is 310 nm. The injection volume is 20 µL. The runtime of the method is 6.0 minutes. The retention time of Febuxostat and the internal standard were 4.63 and 2.75 minutes respectively. The method showed good linearity in the range of 45.42 – 2559.64 ng/mL. The recovery of Febuxostat is 74.36 % with a standard deviation of 5.661 and recovery of internal standard was 73.77 % with a standard deviation of 5.649. The LOD of Febuxostat is 45.42 ng/mL. Matrix effects were not observed. This method is simple, specific and precise for determination of febuxostat in human plasma.

Abstract

Medicinal plants have played key role in world health. In spite of great advances observed in modern medicines; herbal formulations have reached extensive acceptability as therapeutic agents for treatment of several diseases. Herbal drug technology is used for converting botanicals materials into medicines, where standardization and quality control with proper integration of modern scientific techniques and traditional knowledge is important. ‘Standardization’ is a process of evaluating the quality & purity of crude drug by means of various parameters like morphological, microscopical, physical, chemical & biological observation. However herbal medicines differ from that of the conventional drugs and so some innovative methods are necessary for quality assessment of herbal drugs. Fingerprint analysis approach   is the most potent tool for quality control of herbal medicines because of its accuracy and reliability. Fingerprinting is a process that determines the concentrations of a set of characteristic chemical substances in an herb. Based on the conception of phytoequivalence, the chromatographic and DNA fingerprints of herbal medicines could be utilized for addressing the problem of quality control of herbal medicines. This article will review advanced techniques of chromatographic and DNA fingerprinting  in standardization of herbals.

Abstract

Quinoxaline is six membered heterocyclic nitrogen containing two nitrogen atoms are based on pyrazine so also called as benzopyrazine. α dicarbonyl compounds reacts with aromatic ortho-diamine by consecutive addition-elimination mechanism to give quinoxalines. Quinoxaline have become attractive target of extensive research due to its inherent properties and therapeutic uses. Quinoxaline finds many pharmacological activities like antibacterial, antifungal, antituberculer, anti-inflammatory, antihyperglycemic, antitumor etc.

Abstract

Herbal toxicity is a field that has rapidly grown over the last few years along with increased use of herbal products worldwide. The indication of herbal products is quite variable because these products are not subjected to regulation by the Food and Drug Administration and are often used without supervision by a healthcare provider. Moreover, their use is generally regarded as safe and natural by the lay-public.  The objective of study is to aware the researchers about most commonly used medicinal herbs, which are known to induce various types of toxicities. A Medline search was undertaken to identify relevant literature using search terms including 'herbal', 'herbs', ‘toxicities’, ‘cardiotoxicity’, ‘hepatotoxicity’, ‘nephrotoxicity’, ‘hematologic toxicity’ etc. The numbers of adverse events are reported with the use of herbal products. A number of herbs, herbal drugs and herbal supplements are associated with a spectrum of toxicity events. Advances in the understanding of the pathogenesis and precautions are needed to improve herbal medicine safety.

Abstract

Thiadiazoles having a wide range of activity so based on this concept  we have focused on 1,3,4 Thiadiazoles  which are having a free amino group so that  Schiff bases can be  prepared by using corresponding substituted benzaldehydes. The progress of reaction was monitored by TLC, then the synthesized compounds were crystallized by using  suitable solvents. Then all of them were characterized by I.R and 3 of them by N.M.R spectra. Finally the compounds were tested for in-vitro anti cancer activity on colorectal cell lines (HT-29).

Abstract

Abstract

A sufficient and steady release of drug is important for the prepared oral solid dosage forms of pharmaceutical products. Delivering the drug at appropriate site is also essential. Hence pharmaceutical products must be designed to fulfill these requirements. In the present investigation both effervescent and non-effervescent floating drug delivery systems are prepared.  Effervescent type oral floating alginate gel beads of Famotidine are prepared using gas generating agent sodium bicarbonate. Corn oil is utilized as a dispersed phase to generate a uniform emulsion to create multiple tiny chambers in the alginate matrix for better buoyancy. The effect of different concentrations of sodium alginate, calcium chloride and Famotidine is studied and their Morphological analysis, Buoyancy, Encapsulation efficiency and In-vitro drug release behavior are carried out. For the non-effervescent type, Famotidine is initially dispersed in alginate solution containing corn oil. A controlled release polymer along with solubility enhancers like PEG 4000 or PEG 6000 is added. Morphological evaluation, Buoyancy study and spectral interpretation studies are performed. It is concluded that Famotidine release from effervescent beads occurred in a “burst” within the first 5-15 min, due to rapid water ingress and creation of aqueous channels. For the non-effervescent type, the presence of solubility enhancers like PEGs resulted in fickian diffusion with erosion type of release while the presence of controlled release polymer resulted in a Higuchi type of drug release.

Abstract

The leaves of Prosopis spicigera were successive  extracted with versatile solvents to get crude extracts, and were subjected to phytochemical analysis. The preliminary phytochemical screening revealed the presence of proteins, carbohydrates and tannins in the petroleum ether extract. Ethyl acetate extract contains proteins, carbohydrates, tannins, saponins, alkaloids, phenolics and steroids. Methanolic extract contains proteins, carbohydrates, tannins, saponins, alkaloids and flavonoiuds. Ethanolic extract contains proteins, carbohydrates and alkaloids  which could make the plant useful for treating different ailments as having a potential of providing useful drugs for human use. With this view may helpful to search any new compounds from this part of the plant could be isolated hereafter, and the presence of phytochemical constituents from P. spicigera leaves may helpful to future investigations of this plant.

Abstract*

Arthritis is described in Unani system of medicine under a broad term Waja-ul-Mafasil which encompasses entire joint disorders like inflammatory, non-inflammatory, infectious, metabolic and other musculoskeletal disorders. With the advent of science and technology, modern classification has separated these individually according to their etiopathology. On deep insight of Unani literature, arthritis can be correlated with various types of Waja-ul-Mafasil in resemblance to the predisposing factors, aggravating factors and pattern of joint involvement. Unani system of Medicine is based upon Hippocrates’s theory of four humours (Akhlat). According to Unani concept, the pathological changes in the joints are caused mainly by derangement of humoural temperament and accumulation of Mawad-e-Fasida (Morbid material) in the joint spaces. The derangement may be simple, causing only functional disturbance of articular surfaces, or it may be compound in which organic disturbance and quantitative changes take place in the joints. The aim of treatment for patient with Waja-ul-Mafasil is to reduce morbidity and disability. The principle of treatment aims at restoring the normal temperament, and correcting the imbalance in the Khilt (humour) through Imala (Diversion of morbid material) and Istifraagh (Evacuation of morbid material). Hijamah (Cupping therapy) is a regimenal mode of treatment recommended by eminent Unani physicians for the management of Waja-ul-Mafasil, serve the both purposes. Based on modern parameters, Hijamah (Cupping therapy) has been proven beneficial in the improvement of various signs and symptoms of the arthritis. As an adjuvant therapy Hijamah provides significant improvement in pain and has a marked effect in improving the quality of life. It has immunomodulatory effect that could be used as monitoring tool for disease activity and prognosis.

Abstract

Harsh synthetic chemicals and pollution tremendously affecting our life today, hence, nature has endowed us with its everlasting treasure of herbal ingredients. The review basically emphasis on various herbal ingredients which have potential for photo protection. Ultraviolet rays are the major cause of sunburn which further leads to dangerous skin cancer. Prohibition of U.V rays penetration can be achieved by use of herbal ingredients showing sun screening action. As compare to synthetic moites herbal shows reduced side effects, effective in chronic conditions, widespread availability at lower cost. Basically herb with Vitamin (A, C, E) flavonoids, polyphenols, carotinoids (Lycopene, β carotene), and phenolic acids enhance photo protection as they posses antioxidant action. These herbal ingredients inhibit free radical formation and neutralize reactive oxygen species (ROS) and enhance skin protection from harmful U.V rays.  This review focuses on various herbs with active constituent responsible for photo protection. This review concludes damaging and harmful effects of UV rays, types of UV radiations and at last review concludes study of chemical constituents present in various herbals responsible for UV shielding effect.

Abstract

To perform the qualitative phytochemical screening and acute toxicity of Datura metel L. Root.Method: The root is subjected to various extractions using ethanol and distilled water. Extraction process used was percolation method. With the extract phytochemical screening was done. R_f value was also calculated there after acute toxicity test was performed. After phytochemical screening different types of compounds namely alkaloids, triterpinoids, fats and fixed oils, flavonoids, carbohydrates are found in aqueous extract and flavonoids are found in ethanolic extract. After performing the acute toxicity with 2000mg/kg, 2640mg/kg, 3280mg/kg, 3920mg/kg, 5000 mg/kg. The animal dies at 3920mg/kg & 5000 mg/kg dose. This study helps us to get the information about the phytochemical present and their TLC value in the root of the plant and gives the LD₅₀ of the extract.

Abstract

The herbal medicines are the major remedy in traditional medicinal systems which have been used in medicinal practice for 100 years. These has made a great contribution in maintaining human health. A majority of the world’s population still relies on health needs. The practice continues today because of its biomedical benefits and its place in cultural beliefs in many parts of the world. Presently there is an increasing interest in herbal medicine related to isolation, characterization and pharmacological screening of extracts obtained from medicinal plants.In the present study, ethanolic extract of Leucasindicavar.nagalopuramiana was studied for preliminary phytochemical screening and anthelmintic activity at various concentrations (i.e., 10mg/ml, 25mg/ml, 50mg/ml, 100mg/ml) by using adult Indian earth worm, pheretimaposthuma from in nalgonda region. Screening revealed the presence of Alkaloids, carbohydrates, and saponins. The mean paralysis time and mean death time for each sample was calculated and compared with the Albendazole which is taken as standard. The result was found that Leucasindicavar.nagalopuramiana had an anthelmintic activity which was greater than standard Albendazole.

Abstract

The present study was taken up to understand the influence of selected antiarrhythmic drug (disopyramide) on the pharmacodynamics and pharmacokinetics of gliclazide in rabbits. This study is planned to establish the safety of the drug combinations. Studies in normal rabbit conducted with oral doses of disopyramide, gliclazide and their combination with appropriate washout periods in between treatments. Blood samples were analyzed for blood glucose by GOD/POD method, serum gliclazide levels by HPLC method. In combination antiarrhythmic drug (disopyramide) improved the activity of gliclazide. The findings suggest that the interaction observed was pharmacokinetic and pharmacodynamic in rabbits.

Abstract

Leptospirosis is a bacterial zoonotic disease caused by different pathogenic serovars of the spirochaete bacterium Leptospira. It mainly survives in both temperate and tropical regions; the occurrence in the tropics is approximately 10 fold higher than in temperate regions. The present day medicines for the treatment of leptospirosis are only effective during the early phase of the disease and no medicines available after the disease become complicated. In this connection, the present study was carried out for the identification of potential anti-leptospiral compounds from marine actinomycetes. From 18 marine sediment samples nearly 141 isolates of actinobacteria were enumerated.  The sediments were collected during the months of March to August 2013, along the coast Bay of Bengal, Palk Strait, Gulf of Mannar and Lakshadweep. Crude compounds were produced from the isolates, and all were screened against the Leptospira interrogans serovar Autumnalis strain N2 (Human isolate) to determine the anti leptospiral activity. In the primary screening, 5 samples were recorded by showing promising activity (strain no MSU5, P1, T10, PGM 15 and TCA6) and determined of having anti-leptospiral activity. In the secondary screening strains MSU5, T10 and P1 were showed significant activity. In both the screening MSU5 isolated from Manakudy mangroves, showed an effective inhibition activity against the serovars Autumnalis with a minimum inhibition concentration (MIC) at 125µg.mL^-l.  The standard antibiotic doxycycline exhibited the MIC with 200µg.mL^-l. This is first report for analyzing marine actinomycetes compounds for antileptospiral activity. The study reveals that strain MSU5 shows promising antileptospiral activity against Leptospira serovar Autumnalis and may be a potential candidate for anti-leptospiral components.

Abstract

A rapid, highly sensitive, accurate, precise and validated RP- HPLC method was developed for the simultaneous determination of Acetaminophen (ACT) and Guiafenesin (GFN) in pharmaceutical dosage form as per ICH guidelines. The mobile phase consisted of water, methanol and glacial acetic acid (60:40;1.5 % v/v) operated on isocratic mode. The flow rate of the mobile phase was 1.0 mL/minute. Chromatographic separation of acetaminophen and Guiafenesin was performed on Inertsil C₁₈  column ( 250 x 4.6 mm, 5µm). The injection volume was 10 µL. The retention time of ACT and GFN were 4.04 and 9.6 minutes respectively and the total run time of the analysis was 15 minutes. The developed method was validated for parameters such as accuracy, precision, linearity and solution stability. The proposed method had been successfully used for the estimation of the drugs in tablet dosage form. The intraday and inter day precision was found to be within the limits. Conclusion: In this research project we have reported a stability indicating RP HPLC method for the development as well as validation for the simultaneous estimation of ACT and GFN in combined dosage form using simple mobile phase. The sample recoveries in formulation were in good agreement with their respective label claims and they suggested non- interference of formulation excipients in the determination.

Abstract

Hypertension is a major health problem across the globe because of its high prevalence. It is suggested that hypertension has its roots in adolescent age but goes undetected unless it is properly diagnosed. Hence this study was conducted in a rural setup in Nayadupetta,Andhra Pradesh among children about their sleep time, diet , obesity etc.A study was conducted at Nayadupetta ,Andhra Pradesh during January 2014. The study was conducted among school children between the age group of 13 to 17. Blood pressure readings were analysed as per guidelines of JNC-7.Obesity has been increasing among adolescent kids .This is primarily due to eating of junk foods, lack of physical activity. Obesity is one of the major contributors of hypertension. 152 participants have a normal BP, while 11.48% participants have hypotension. 9.70% population had stage 2 secondary hypertension while 14.80 persons fall with stage1 hypertension.The incidence of hypertension is higher among the adolescents. Proper care should be shown to children with hypertension as this may virtually be a tougher aspect to deal with.

Abstract

The aim of the present work was to evaluate the phytochemical composition of Camellia sinensis and to assess the antibacterial activities of Camellia sinensis using in vitro antibacterial screening techniques. Extracts of leaves from the tea plant Camellia sinensis contain polyphenolic components with activity against a wide spectrum of microbes. Studies conducted over the last 20 years have shown that the green tea polyphenoliccatechins, in particular (−)-epigallocatechingallate (EGCg) and (−)-epicatechingallate (ECg), can inhibit the growth of a wide range of Gram-positive and Gram-negative bacterial species with moderate potency. The leaves were collected from the market and identified by the Pharmacognosy department of our own college. Phytochemical analysis revealed the presence flavonoids.The study was carried out on various species of bacteria including E-coli (MTCC No.40), Staphylococcus aureus (MTCC No.87), Proteus vulgaris (MTCC No.742), Pseudomona saeruginosa (MTCC No.424), Bacillus subtilis (MTCC No.441), Staphylococcus epidermidis (MTCC No.9041), and Micrococcus luteus (MTCC No.106), using cup plate method. The results obtained were compared against standard antibiotic streptomycin. The aqueous extract is effective against proteus vulgaris and alcoholic extract is found effective against Staphylococcus aureus, Staphylococcus epidermidis,  Micrococcus luteus. The ability of tea plant extract to inhibit the growth of bacterial strains is an indication of its antibacterial property that might be used in the management of bacterial infections in future.

Abstract

Present study was carried out on commercially important fresh water fish (Clarias batrachus).A total number of 36 fishes infected  with ulcerative mycoses were collected from Larpur reservoir, Bhopal. Isolation of fungi from different parts of  body of fish showed the presence of  Saprolegneous  fungi  ( Saprolegnia diclina) in all the specimens collected. Pathogenicity of isolated fungi was tested on host fish  with  concentration of 2x10⁴  zoospores /ml  and  all the fishes got infection  leading to 100% mortality within  ten days. Histopathological studies of infected fishes showed varying degree of destruction in the tissue. Skin showed loss of epidermis, necrotized hypodermis and penetration of hyphae in underlying musculature with fibrillar granuloma. Degenerative liver and kidney cells with fungal spores were found, gills showed degeneration of lamellae. The aim of present  work is to find out the parasitic ability S.diclina with its histtopathological studies.

Abstract

Niflumic Acid in human plasma using Diclofenac as an internal standard (IS) was determined quantitatively by a well developed and validated RP - HPLC method by UV detection. The extraction process involved a protein precipitation technique. Both Niflumic Acid and the internal standard were eluted under isocratic mode. The mobile phase composed of a mixture of 60:40 % v/v methanol and 10mM mixed phosphate buffer (pH 3.0±0.05) at a flow rate of 1.0 mL/Minute. The wave length of detection is 295 nm. The injection volume is 20 µL and the runtime of the method is 7.5 minutes. The method showed good linearity in the range of 55.44 – 5082.41 ng/mL. The recovery of Niflumic Acid is 7.79 % with a standard deviation of 0.587 and recovery of internal standard was 9.39 %. The LOD of Niflumic Acid is 59.14 ng/mL. Matrix effects were not observed.

Abstract

Clotrimazole is an Anti-fungal drug and used to  treat Antifungal diseases. Clotrimazole is characterised by its poor water solubility and low bioavailability. The main objective of present study was to prepare Clotrimazole gels by hydrotropic phenomenon using Sodium salicylate, Sodium Benzoate as hydrotropic salt and by using corn and potato starch. Clotrimazole formulation was prepared by Hydrotropic technique and Hydrotropic starch gel was formed and characterize systematically for various physico-chemical parameters like drug content estimation, pH, tube extrudability, spreadability, IR spectral analysis for any drug excipients interactions etc. All the prepared formulations were subjected to in-vitro drug release studies by diffusion method for six hours In 100 ml phosphate buffer (pH 7.4) and compared with marketed formulation and stability study of the best formulation was carried out for a period of 90 days at 28 ±2 ^oC and 5± ^oC. The hydrotropic starch gel was found to be in an acceptable range. The pH of all the formulation were found between 6-7.5 pH. Drug content was found within  range 98.5%-100.5%.The percent drug release of hydrotropically starch gel among all the formulation the percent drug release of W8s-c-d was found to be best 85 %.where as the marketed was found to be 46%.The  viscosity (cp) value of W8s-c-d was found to be 6960. Spreadability plays an important role in patient compliance and help in uniform application of gel to the skin as gels should spread easily , the formulation was found to have better spreadability. Drug and polymer interaction study done by FTIR and revealed that there is no interaction.and concluded that W8s-c-d formulation was the best formulation

Abstract

An attempt has been made to formulate solid lipid nanoparticles (SLNs) for the drug Thiocolchicoside, which is a muscle relaxant with anti-inflammatory and analgesic effects. Controlled release of SLNs of the drug thiocolchicoside were prepared by the solvent evaporation method. Optimisation was done using a Box-Behnken design which was constructed using the parameters solid lipid (X1), surfactant (X2), and drug/lipid ratio (X3) level as independent factors based on the preliminary experimental data. The formulations were evaluated on various parameters such as size of the nanoparticles, entrapment efficiency of thiocolchicoside and its release behavious from the formulation. Optimized solid lipid nanoparticles were found to have a particle size of 542 nm and EE% of 85 %.FTIR spectra and of thiocolchicoside, lipids, indicate that there is no chemical interaction between them and confirmed the stability of the drug. SEM study confirmed the non-spherical shape of Solid lipid nanoparticles. The solid state of the drug in the Solid lipid nanoparticles and lipid modification was characterized. The in vivo characterisation studied by rat paw edema technique suggested effective anti-inflammatory response. Due to enhanced bioavailability, these thiocolchicoside- Solid lipid nanoparticles can be considered to be promising vehicles for drug delivery.

Abstract

The aim of present investigation is the design and evaluation of controlled release matrix tablets for Selective β₁ receptor blocker of Metoprolol succinate. Optimization of formulations of matrix tablet was done by 2³ factorial design. Formulation of controlled release matrix tablets of Metoprolol succinate was carried out by wet granulation method by using different polymers like HPMC K4M, Guar gum and Sodium Carboxy Methyl Cellulose. The micromeritic properties of prepared granules such as Bulk density, Tapped density, Angle of repose, Compressibility index, Hausner’s ratio indicated the good flow property of prepared granules. The physicochemical characterization of prepared matrix tablets such as Thickness, Weight variation, Hardness, Friability and Drug content were evaluated. Almost satisfactory results were obtained in all the formulations. The compressed tablets were subjected for in-vitro drug release, kinetic studies and stability studies. The formulations MT4 (95 mg) and MT14 (95 mg) sustained the action upto 24 hrs. Drug diffusion from matrix tablets showed apparently zero order kinetics and release mechanism was diffusion controlled. The best formulations subjected to stability studies indicated that the tablets did not show any characteristic changes. It was concluded that the developed controlled release matrix tablet using HPMC K4M and Guar Gum shows satisfactory release retarding of Metoprolol succinate and its improved efficacy can perform therapeutically better than a conventional tablet.

Abstract

The aim of this study is to evaluate the production and antimicrobial potential of bacteriocins released by Lactococcus garvieae. Bacteriocins are extracellular in nature having inhibitory activity against other bacteria. The Lactococcus garvieae was isolated from cow’s milk which produces bacteriocins was evaluated by using different media such as MRS (Mann Rogasa Sharpe), M17, Soybean casein digest broth and Brain Heart Infusion (BHI) broth. Further, the effect of various supplements on antimicrobial activity of bacteriocins against gram-positive bacteria viz., Staphylococcus aureus, Bacillus subtilis and Bacillus cereus and gram-negative bacteria viz., Pseudomonas aeruginosa and Escherichia coli was also evaluated. The results indicate that Lactococcus garvieae yielded high level of bacteriocins 14363.6 AU/ml in M17 medium, where as 11064.5 AU/ml in Soyabean casein digest, 12119.3 AU/ml in BHI, and 13219.0 AU/ml in MRS media at 48 h of incubation. Addition of supplements viz., tween 20, tween 80, amylase, proteinase K and asparginase reduced the antimicrobial activity of bacteriocins.  Whereas Urea, EDTA and NaCl have increased antimicrobial activity of bacteriocins. It is noticed that incubation period of 40, 50 and 60 h, at temperature of 30°C, 40 °C and pH of 6 was found to be an ideal for higher bacteriocins activity. In conclusion, the M17 medium was found to be best for bacteriocins production and the supplements such as Urea, EDTA, and NaCl were found to enhance the antimicrobial activity of bacteriocins. Whereas, pH of 6 was found to be best for bacteriocins production. Therefore, these results are encouraging since the inclination nowadays is to produce large quantities of bacteriocins/probiotics/Antimicrobial peptides (AMPs) which have immense clinical usage in manufacture of alternative types of antibiotics and in various drug preparations.

Abstract

The present study mainly focused on ethno-medico-botanical survey which was carried out by first hand questioning among the traditional (folk) health practitioners for treating different diseases or disorders. Here, 30 different herbal compositions are mainly focused; those are being used to treat different diseases by the folk practitioners using different plant species. Along with this the herbal compositions containing 54 different medicinal plants of 36 different families are also listed out. These plants are economically important because of their medicinal values and distributed throughout the forests of Tripura. In this paper, we have explored the herbal composition along with their method of preparation, mode of administration and dose. We also unfold the local name, botanical name, habit, parts used and medicinal values of the plants investigated in this survey which are being used by the folk practitioners to treat several different medical complications of rural peoples.  All these formulations are quite effective according to traditional claim but still suitable experimental evaluation including preclinical and clinical trials are required, that may lead to suitable new drug discovery and development.

Abstract

Cyanobacteria are can colonize everywhere there is possibility of life. As usual we can easily observe them near water bodies. Their diversity is rich but lacks the evaluation. Most of the species of these are even today are unrecognized. Although, in recent years many research work prove them as a suitable source of secondary metabolite which act as drug. This review summarized the research update on secondary metabolites of Cyanobacteria from various habitat and also cover some extant of non-ribosomal and polyketide gene which involve in synthesis.

An oral controlled release system has been developed to improve the delivery of drugs to the systemic circulation. The aim of this investigation was to synthesize and formulate controlled release matrix tablet using pH sensitive poly (methacrylic acid)-graft-karaya gum (p(MAA)-g-KG) as a graft copolymer. The pH-sensitive p(MAA)-g-KG copolymer was synthesized by free radical polymerization using cerric ammonium nitrate (CAN) as initiator and methylene bisacrylamide (MBA) as a crosslinker under nitrogen atmosphere. Grafting parameter such as grafting ratio, efficiency, add on and conversion were identified with respect to change in concentration of CAN (0.01-0.15 mol dm^-3) and methacrylic acid concentration (0.05–0.15 mol dm^-3). The grafting was confirmed by Fourier transform infrared spectroscopy. Differential scanning calorimetry and X-ray diffraction studies were carried out to know the internal characteristics of polymeric material. Scanning electron microscopic analyses shows the change in surface morphology of the graft copolymer. The swelling studies illustrate that there is less swelling property of graft copolymer as compared to karaya gum (KG). Tablets were formulated with different concentration of graft copolymer and other excipients by incorporating diclofenac sodium (DS) as a model drug. In vitro drug release studies were performed in pH 1.2 for 2 hours followed by pH 6.8 without enzyme at 37°C. The release time increased with increasing grafting ratio in matrix tablet which indicates the swelling behavior of graft copolymer to release drug in dissolution medium. The release rates were fitted to an empirical equation to calculate the diffusional exponent (n), which indicate Super Case II transport mechanism for controlled release of diclofenac sodium.

Abstract

Liquisolid is a novel technique to enhance solubility and dissolution rate of BCS class II drugs through oral route. This technique of delivering drugs is suitable mostly for liphophilic drugs and poorly water soluble drugs. However, an apparent limitation of this technique is the formulation of a high dose because a large amount of liquid vehicle is needed, which finally results in a low-dose liquid solid formulation. This approach is suitable for both immediate and sustained release formulations. The purpose of the present work is to improve the solubility and dissolution rate of poorly soluble drug, Piroxicam, by liquisolid technique. Solubility is increased by using non-volatile solvents such as PEG 400, Labrosol, Span 20 and Tween 80 in single or combination which are suitable for drug and dissolving the drug in those non volatile solvents, which is termed as ‘liquid medicament’. The liquid medicament is blended with carriers such as microcrystalline cellulose and Aerosil to convert the liquid medicament into a non-adhering, dry looking powder which has acceptable flow properties and compression behavior. These Liquisolid systems are evaluated by micromeritic studies like flow behavior, bulk density, tapped density, compressibility index, drug content, in vitro release, Fourier transform infra red spectroscopy and powder X-ray diffraction. Increase in dissolution rate and in turn improvement in bioavailability is observed in the case of poorly water soluble drug i.e. Piroxicam by this Liquisolid technique.

Abstract

A simple, economic, accurate stability indicating RP-HPLC method was developed and validated for the estimation of tenofovir disoproxil fumarate in tablet dosage form. The method was carried out using HYPERSIL BDS C18 (150 x 4.6 mm, 5µm column). The detection was carried out at the wavelength of 254nm. The elution was achieved isocratically with a mobile phase comprising a mixture of potassium dihydrogen phosphate buffer pH 6.5 and Acetonitrile in the ration of 60:40 (%v/v). The flow rate was 1.0 ml/min. The procedure was validated as per ICH rules for specificity, accuracy, linearity, precision, ruggedness, LOD, LOQ and robustness. Under different prescribed stress conditions (acid, base, peroxide, thermal, photolytic and humidity) following the ICH guidelines indicating the method is selective and specific. The linearity range was 25% to 150%, with the correlation coefficient of 0.9990. The percentage recovery for tenofovir disoproxil fumarate was found to be 99.49-100.05%. Limit of detection and limit of quantification was found to be 0.1382µg/ml and 0.4188µg/ml respectively. The assay of tablet dosage form was found to be 99.48%. The developed method was successfully applied to estimate the amount of Tenofovir disoproxil fumarate in tablet formulations.

Abstract

The paper presents the ring opening reaction of itaconic anhydride with 4-aminoantipyrine resulted in the formation of title compound, 4-[(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)amino]-2-methylidene-4-oxobutanoic acid (1). The structure of the newly synthesized compound was characterized by IR, ¹H NMR, ¹³C NMR, mass, elemental and thermal analysis data. The present study examines the possible antioxidant, antimicrobial and thermal properties of the titled compound 1. In order to evaluate the antioxidant activity, different in vitro methodologies such as DPPH radical scavenging, nitric oxide radical scavenging and reducing power assays were used. In addition, in vitro antimicrobial activity of the compound 1 was tested against four microorganisms. Antioxidant and antimicrobial activities of the compounds 1 were found to be significant in comparison with standard in all the in vitro methodologies adopted. Thermal stability of the compound 1 was determined by using TGA, DTA, DSC analysis  and the results showed that endothermic peak is correlate with the value (189–190 ^oC) measured by a capillary method.

Abstract

The marketed α- glucosidase inhibitor like Acarbose, Miglitol and Voglibose are wide used for treatment of DM, apart from these drugs Salacia Oblonga and Salacia Reticulata are plants native to India and Sri Lanka these are widely used for thousands of years in Ayurvedic medicine for the oral treatment of diabetes a chronic disorder in metabolism of carbohydrates, proteins and fat due to absolute or relative deficiency of insulin secretion with/without varying degree of insulin resistance. Attenuation of postprandial glycemia is hypothesized to reduce the risk of progression from impaired glucose tolerance to diabetes. It is also thought to reduce the number of complications associated with diabetes. A clinical trial conducted to assess the comparison of outcome of marketed drugs and its combination with Salacia species, found significant effect on weight and HbA1C value of patients of Type II DM