A multiple-unit floating drug delivery system based on gas formation technique was developed, in order to prolong the gastric residence time and to increase the overall bioavailability of the dosage form. The floating bead formulations were prepared by dispersing nevirapine together with calcium carbonate in a mixture of sodium alginate and hydroxypropyl methylcellulose solution and then dripping the dispersion into an acidified solution of calcium chloride. Calcium alginate beads were formed, as the alginate underwent ionotropic gelation by calcium ions, and carbon dioxide developed from the reaction of carbonate salts with acid. The obtained beads were able to float due to CO ₂ -gas formation and the gas entrapment by the polymeric membrane. The prepared beads were evaluated for percent drug loading, drug entrapment efficiency, morphology, surface topography, buoyancy, in-vitro release, and release kinetics. The formulations were optimized for different weight ratios of the gas-forming agent and sodium alginate. The beads containing higher amounts of calcium carbonate demonstrated an instantaneous, complete, and excellent floating ability over a period of 24 hours. The increased amount of the gas forming agent did not affect the time to float, but increased the drug release from the floating beads, while increasing the coating level of the gas-entrapped membrane, increased the time to float, and slightly retarded the drug release. Good floating properties and sustained drug release were achieved. Finally, these floating beads seemed to be a promising gastroretentive drug delivery system.

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The objective of this study was to evaluate the effect of formulation variables on the release properties, floating lag time, and hardness, when developing floating tablets of Ranitidine hydrochloride, by the statistical optimization technique. The formulations were prepared based on 3 ² factorial design, with polymer ratio (HPMC 100 KM: Xanthan gum) and the amount of aerosil, as two independent formulation variables. The four dependent (response) variables considered were: percentage of drug release at the first hour, T _50% (time taken to release 50% of the drug), floating lag time, and hardness of the tablet. The release profile data was subjected to a curve fitting analysis, to describe the release mechanism of the drug from the floating tablet. An increase in drug release was observed with an increase in the polymer ratio, and as the amount of aerosil increased, the hardness of the tablet also increased, without causing any change in the floating lag time. The desirability function was used to optimize the response variables, each having a different target, and the observed responses were in accordance with the experimental values. The results demonstrate the feasibility of the model in the development of floating tablets containing Ranitidine hydrochloride.

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The objective of the present investigation was to design a vesicular formulation of brimonidine tartrate and evaluate its ability to reduce the dosing frequency and improve the therapeutic efficacy of the drug. Nano-vesicles of brimonidine tartrate were prepared by film hydration method. The prepared vesicles were evaluated for photomicroscopic characteristics, entrapment efficiency, in vitro, and ex-in vitro drug release and in vivo intraocular pressure (IOP) lowering activity. The methods employed for preparation of vesicles produced nano vesicles of acceptable shape and size. The in vitro, and ex-in vitro drug release studies showed that there was slow and prolonged release of the drug, which followed zero-order kinetics. The IOP-lowering activity of nano vesicles was determined and compared with that of pure drug solution and showed that the IOP-lowering action of nano-vesicles sustained for a longer period of time. Stability studies revealed that the vesicle formulations were stable at the temperature range of 2-8°C, with no change in shape and drug content. The results of the study indicate that it is possible to develop a safe and physiologically effective topical formulation that is also convenient for patients.

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Albendazole, a member of benzimidazole group of compounds, has been shown to have a broad spectrum activity against all classes of helminth parasites. Although it has also been experimentally proven to be effective against cestode infection of poultry, the actual effects of the drug are not yet described. The present in vitro study demonstrated that the commercial prescription drug Zentel^® was significantly effective against adult Raillietina echinobothrida Mégnin, the major cestode parasite of domestic chicken, Gallus domesticus Linnaeus. It clearly exhibited dose-dependent lethal activity at the different concentrations that were tested. Scanning electron microscopy (SEM) revealed that the drug caused extensive structural alterations on the body surface of the cestode. Severe contraction and shrinkage were evident throughout the entire length of the body. The suckers on the scolex became invaginated due to shrinkage. The distinct body segments, the proglottides, were completely distorted. The fine hairy microtriches on the tegument were obliterated and in its place were formed abnormal clumps of tissues. The results of this investigation are in favor of the use of albendazole as a drug of choice in the management of poultry helminthiasis.

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A rapid, simple, accurate, and economical spectrophotometric method has been developed and validated for the assay of the anti-retroviral agent lamivudine in active pharmaceutical ingredients (API) and in its tablet formulation. The analysis is based on the UV absorbance maxima at about 270nm wavelength of lamivudine, using methanol as solvent. A sample of API was dissolved in methanol to produce a solution containing 10 μg/mL of lamivudine. Similarly, a sample of ground tablets were extracted with methanol, centrifuged, and diluted with the same solvent. The absorbance of the sample preparation was measured at 270 nm against the solvent blank, and the assay was determined by comparing with the absorbance of a similarly prepared 10 μg/mL standard solution of lamivudine. The calibration graph was rectilinear from 5 μg/mL to 15 μg/mL for lamivudine with the correlation coefficient being more than 0.999. The relative standard deviation of the replicate determination was about 0.5%. The percent recovery was within the range of 98%-102%, indicating insignificant interference from the other ingredients in the formulation. The method can be applied for the routine QC quantitation of lamivudine in API and tablet formulation.

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In the medical device field, there are a number of players, having quite different responsibilities and levels of understanding of the processes, but all with one common interest, that of ensuring the availability of sound medical devices to the general public. To assist in this very important process, there is a need for a common method for describing and identifying these medical devices in an unambiguous manner. The Global Medical Device Nomenclature (GMDN) now provides, for the first time, an international tool for identifying all medical devices, at the generic level, in a meaningful manner that can be understood by all users. Prior to the GMDN, many nomenclature systems existed, all built upon different structures, and used locally or nationally for special purposes, with unusual approaches. These diverse systems, although often workable in their own right, have had no impact on improving the overall situation of providing a common platform, whereby, medical devices could be correctly identified and the related data safely exchanged between the involved parties. Work by standard organizations such as, CEN (European Committee for Standardization) and ISO (International Organization for Standardization), from 1993 to 1996, resulted in a standard that specified a structure for a new nomenclature, for medical devices. In this article we are trying to explain GMDN as the prime method to reduce medical device errors, and to understand the concept of GMDN, to regulate the medical device throughout the globe. Here we also make an attempt to explain various aspects of the GMDN system, such as, the process of development of the GMDN-CEN report, purpose, benefits, and their structural considerations. In addition, there will be an explanation of the coding system, role of the GMDN agency, and their utilization in the unique device identification (UDI) System. Finally, the current area of focus and vision for the future are also mentioned.

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In the present study, five new derivatives (GG4 to GG8) of benzothiazoles were synthesized and evaluated against Staphylococcus aureus (MTCC 737), Pseudomonas aeruginosa (MTCC 424), Escherichia coli (MTCC 1687), and yeast-like fungi Candida tropicalis. p-Toluidine on treatment with ammonium thiocynate formed 2-benzothiazolamines (II), which on reaction with hydrazine hydrate formed a hydrazino derivative (III). Compounds GG4 to GG8 were synthesized by reacting the hydrazine derivative with different acetophenones. All the synthesized compounds were identified by IR and ¹ H-NMR, and antimicrobial activity was performed on the synthesized compounds. Presence of NO ₂ , Br, OCH ₃ , and Cl groups to the substituted benzothiazole enhanced the antibacterial and antifungal activities.

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An isocratic reversed phase high-performance liquid chromatographic method with ultraviolet detection at 220 nm has been developed for the quantification of itopride hydrochloride in tablet dosage form. The quantification was carried out using C ₈ column (250 mm × 4.6 mm), 5-μm particle size SS column. The mobile phase comprised of two solvents (Solvent A: buffer 1.4 mL ortho-phosphoric acid adjusted to pH 3.0 with triethyl amine and Solvent B: acetonitrile). The ratio of Solvent A: Solvent B was 75:25 v/v. The flow rate was 1.0 mL ^-1 with UV detection at 220 nm. The method has been validated and proved to be robust. The calibration curve was linear in the concentration range of 80-120% with coefficient of correlation 0.9995. The percentage recovery for itopride HCl was 100.01%. The proposed method was validated for its selectivity, linearity, accuracy, and precision. The method was found to be suitable for the quality control of itopride HCl in tablet dosage formulation.

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Drug-drug interaction between esomeprazole at therapeutic and higher doses and sulfonylureas was studied. Sulfonylureas (tolbutamide 40 mg/kg and glibenclamide 40 μg/kg) were administered and the time to onset of hypoglycemia, the duration of the hypoglycemia, and the peak hypoglycemia were determined. Esomeprazole (1.8 mg/kg, 3.6 mg/kg, and 30 mg/kg) was administered for 8 days and its influence on sulfonylurea-induced hypoglycemia was studied. Therapeutic doses of esomeprazole, i.e., 1.8 mg/kg and 3.6 mg/kg dose did not influence the hypoglycemia induced by sulfonylureas. However, a higher dose, i.e., 30 mg/kg, did significantly enhance the duration of hypoglycemia and the peak hypolgycemia. Esomeprazole (30 mg/kg) by itself did not reduce the blood glucose levels; therefore, a pharmacodynamic type of drug interaction can be ruled out. Similarly, a pharmacokinetic type of drug interaction may be ruled out at therapeutic doses. The CYP isoenzyme system involved in the metabolism of sulfonylureas are not very sensitive to esomeprazole and the dose and frequency of administration of sulfonylurea need not be readjusted when they are used concomitantly with esomeprazole (at therapeutic doses).

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The aqueous fruit extract of Cucumis sativus L. was screened for free radical scavenging and analgesic activities. The extract was subjected to in vitro antioxidant studies at 250 and 500 μg/ml and analgesic study at the doses 250 and 500 mg/kg, respectively. The free radical scavenging was compared with ascorbic acid, BHA (Butylated hydroxyl anisole), whereas, the analgesic effect was compared with Diclofenac sodium (50 mg/kg). The C. sativus fruit extract showed maximum antioxidant and analgesic effect at 500 μg/ml and 500 mg/kg, respectively. The presence of flavonoids and tannins in the extract as evidenced by preliminary phytochemical screening suggests that these compounds might be responsible for free radical scavenging and analgesic effects.

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The antiulcer and in vitro anti-inflammatory activities of the aerial parts of Enicostemma littorale against aspirin, ethanol, and pyloric ligation-induced ulcers in rats and bovine serum albumin denaturation were studied. The extract (200 mg/kg and 400 mg/kg po) was administered to the overnight fasted rats, one hour prior to aspirin / alcohol / pyloric ligation challenge. The ulcer index, tissue GSH levels, and lipid peroxidation levels were estimated in all the models of ulcers and the volume of gastric secretion, acidity, and pH, were estimated in the pyloric ligation model of ulcers. Pretreatment with the extract showed a dose-dependent decrease in the ulcer index (Against Aspirin, ethanol challenge, and pyloric ligation. The prior administration of the extract also reduced the total acidity, free acidity, and volume of gastric secretion, and elevated the gastric pH. In addition, it was also observed that the extract inhibited the serum albumin denaturation in a dose-dependent manner. It may be concluded that the methanolic extract possesses antiulcer activity, and the anti-inflammatory activity of the extract may be attributed to the antioxidant potential, as reported earlier.

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Two simple, sensitive, accurate, rapid, and economical spectrophotometric methods have been developed for the estimation of diacerein in Pharmaceutical dosage forms. Method A is based on the reaction of diacerein with Folin-Ciocalteu reagent, in the presence of 0.5 N sodium hydroxide solution, giving a pink-colored chromogen, which shows maximum absorbance at 512 nm against reagent blank, while method B is based on the oxidation of diacerein with potassium permanganate in an alkaline medium giving a pink-colored chromogen, which shows maximum absorption at 497.5 nm. Beer's law was obeyed in the concentration range of 4 - 20 μg/ml for both methods A and B. Results of the analysis were validated statistically, and by recovery studies.

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The hypoglycemic effects of the fruit extract of C. metuliferus was investigated in normoglycemic and alloxan-induced hyperglycemic rats. The results showed that there was an insignificant (P > 0.05) decrease in the blood glucose concentration of normoglycemic rats treated with oral doses of 1000 and 1500 mg/kg of the extract. On the other hand, 500 mg/kg of the fruit extract produced an insignificant (P > 0.05) decrease in blood glucose levels of alloxan-treated rats, while 1000 and 1500 mg/kg oral dose points produced a significant (P < 0.05) decrease in the blood glucose concentration of hyperglycemic rats comparable to that produced by tolbutamide. From this study, the data suggested that the fruit extract did not alter the BGC level in normoglycemic rats, but had a potential hypoglycemic property in alloxan-induced hyperglycemic rats.

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A new, simple, fast and reliable zero order spectrophotometric method has been developed for determination of Escitalopram Oxalate in bulk and tablet dosage forms. The quantitative determination of drug was carried out using the zero order values (absorbance) measured at 238 nm. Calibration graph constructed at 238 nm was linear in concentration range of 2-20 μg/ml with correlation coefficient 0.9999. The method was found to be precise, accurate, specific, and validated as per ICH guidelines and can be used for determination of Escitalopram Oxalate in tablet formulations.

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The everted gut sac method was used to assess the role of the P-glycoprotein (P-gp) on the intestinal secretion of glibenclamide, a prototype of drug used to treat diabetic mellitus. The study included the evaluation of a P-gp modulator carbamazepine used at equimolar doses in the rat. Furthermore, the influence of carbamazepine on the disposition kinetics of glibenclamide in plasma was characterized. For the in vitro experiments, ileal sacs were incubated with glibenclamide in the presence or absence of carbamazepine. In the in vivo experiments, albino rats of either sex were randomly allocated to two groups (n = 6) and oral treatment with glibenclamide (3.6 mg/kg), alone and coadministration with carbamazepine (90 mg/kg). Blood samples were collected at an interval of 1, 2, 4, 6, and 8 h, respectively. Glibenclamide concentrations in both in vitro and in vivo samples were estimated by a sensitive RP-HPLC method. The rate of glibenclamide accumulation in the intestine wall of everted sacs was significantly lower after its incubation with carbamazepine when compared to glibenclamide alone treated. In the agreement with the in vivo and in vitro experiments, the presence of carbamazepine induced an enhancement in the concentrations of glibenclamide in plasma and gastrointestinal tract. The results obtained in this study, both under in vivo and in vitro conditions confirm the relevance of P-gp-mediated transport to the intestinal secretion of glibenclamide.

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Monitoring of adverse drug reactions of a drug is a continuous process and runs through-out the life of a drug. Many rare adverse effects of a drug are documented after years of use; when a single case (signal generation) is reported leading subsequently to reporting of more cases. Deficiency of Vitamin B12 (vit B ₁₂ ) is a known sequel of prolonged metformin therapy. It was recommended to have annual measurement of serum vit B ₁₂ levels in patients on long term metformin therapy way back in 1970 itself. After more than 50 years of use of metformin, we have come to know that metformin induced vit B ₁₂ deficiency can cause neuropathy; forcing to change the recommendation from annual screening of vit B ₁₂ levels to annual supplementation of vit B ₁₂ .

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Using the water eliminated mechanism, reactions of 4-pyridinecarboxylic acid hydrazide and salicylaldehyde, benzaldehyde, cinnamaldehyde, and formaldehyde afforded the corresponding N ⁴ [(E)-1-(2-hydroxyphenyl) methylidene] (NHPM), N ⁴ -[(E)-2-phenylethylidene] (NPI), N ⁴ [(E,2E)-3-phenyl-2-propenylidene] (NPPI), and N ⁴ [(E) ethylidene] (NEI) isonicotinohydrazide, in high yields, after several minutes, as reported. These new compounds have shown antitumor activity against two kinds of cancer cells, which are K562 (human chronic myeloid leukemia) and Jurkat (human T lymphocyte carcinoma).

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This is the first on the modulation of norfloxacin antibiotic activity by the volatile compounds of an essential oil. We report the chemical composition and antibiotic modifying activity of the essential oil extracted from the leaves of Croton zehntneri Pax et Hoffm (variety estragole), using the minimal inhibitory dose method and gaseous contact. The leaves of Croton zehntneri Pax et Hoffm (Euphorbiaceae) were subjected to hydrodistillation, and the essential oil extracted was examined with respect to the chemical composition, by gas chromatography-mass spectrometry (GC/MS), and to inhibitory activity of efflux pump by gaseous contact. The main component of the essential oil of C. zehntneri was estragole (76,8%). The gaseous components of the oil enhanced the inhibition zone of norfloxacin in 39,5%. This result shows that this oil influences the antibiotic activity of norfloxacin, possibly affecting the bacterial NorA efflux system, and may be used as an adjuvant in the antibiotic therapy of multidrug resistant pathogens.

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A three-dimensional quantitative structure-activity relationship (3D QSAR) of 44 structurally and functionally diverse series of 1- (Naphthylalkylimidazoles) as antiepileptic agents was studied using the Comparative molecular similarity indices analysis (CoMSIA) method. A training set containing 34 molecules served to establish the models. The optimum CoMSIA model obtained for the training set were all statistically significant, with cross-validated coefficients (q ² ) of 0.725 and conventional coefficients (r ²_ncv ) of 0.998. The predictive capacities of the model were successfully validated by using a test set of 10 molecules that were not included in the training set. CoMSIA model (Model 1) obtained from the hydrophobic and Hbond acceptor field was found to have the best predictivity, with a predictive correlation coefficient (r ²_pred ) of 0.67. The information obtained from this 3D-QSAR model can be used to guide the development of imidazoles as novel antiepileptic agents.

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