Formulation and Evaluation of Controlled-Release Tablet of Zolpidem Tartrate by Melt Granulation Technique

The present investigation describes the influence of the concentration of PEG 6000 as a melt binder and ratio of HPMC K4M : PVP on Zolpidem tartrate controlled-release tablet formulations using 32 full factorial design. The ratio of HPMC K4M and PVP K30 (X1) and the concentration of melt binder (X2) were selected as independent variables, and drug release at 1 hr (Q1), 4 hr (Q4), 8 hr (Q8), diffusion coefficient (n), and release rate constant (K) were selected as a dependent variable. Tablets were prepared by melt granulation technique and evaluated for various evaluation parameters. It was observed that concentration of melt binder had significant effect on Q1, Q4, n, and K Binder concentration 25% w/w was found optimum. Optimized formulation (F7) showed good similarity with theoretical profile of drug. The X2 variable had a significant effect on dependent variables, and the X1 variable had no significant effect on dependent variables

On Fixed Point theorems in Fuzzy Metric Spaces in Integral Type

Abstract: This paper presents some common fixed point theorems for occasionally weakly compatible mappings in fuzzy metric spaces. Keywords: Occasionally weakly compatible mappings,fuzzy metric space

Formulation and Evaluation of Transdermal Patch of Repaglinide

Repaglinide has the half life of 1 hour, and bioavailability in the body is 56% due to first-pass metabolism. The total daily dose of Repaglinide is 16 mg (e.g., 4 mg four times daily depending on meal patterns); hence, it required frequent dosing. Transdermal patch of Repaglinide was prepared to sustain the release and improve bioavailability of drug and patient compliance. Different formulations were prepared by varying the grades of HPMC and concentration of PVP K30 by solvent casting method. The prepared formulations were evaluated for various parameters like thickness, tensile strength, folding endurance, % elongation, % moisture content, % moisture uptake, % drug content, in vitro drug release, in vitro permeation, and drug excipient compatibility. A 32 full factorial design was applied to check the effect of varying the grades of HPMC (X1) and PVP concentration (X2) on the responses, that is, tensile strength, percentage drug released in 1 hr (Q1), 9 hr (Q9), and diffusion coefficient as a dependent variables. In vitro release data were fitted to various models to ascertain kinetic of drug release. Regression analysis and analysis of variance were performed for dependent variables. The results of the F2 statistics between factorial design batches and theoretical profile were used to select optimized batch. Batch F6 was considered optimum batch which contained HPMC K100 and PVP (1.5%), showed release 92.343% up to 12 hr, and was more similar to the theoretical predicted dissolution profile (f2 = 69.187)

On Fixed Point theorems in Fuzzy 2-Metric Spaces and Fuzzy 3-Metric Spaces

In this paper, we give some new definitions of compatible mappings of types (I) and  (II) in fuzzy-2 metric space and fuzzy-3 metric space prove some common  fixed point theorems  for mappings under the condition of compatible mappings of types (I) and (II) in complete fuzzy-2 metric space and fuzzy-3 metric space. Our results extend, generalize and improve the corresponding results given by many authors. Keywords: Fuzzy metric space, Fuzzy 2-metric space, fuzzy-3 metric space ,Compatible mappings, Common fixed point

FORMULATION AND EVALUATION OF MUCOADHESIVE BUCCAL TABLETS OF CARVEDILOL

Objective: The aim of the study was to formulate and evaluate mucoadhesive buccal tablets of carvedilol to avoid the first-pass metabolism. Methods: Mucoadhesive Buccal tablets of carvedilol were prepared by direct compression techniques using a combination of bioadhesive polymers such as hydroxypropyl cellulose (HPC) and polyethlyelne oxide WSR-1105 (PEO WSR-1105). In order to improve solubility of carvedilol, solid dispersion was prepared using poloxamer 188. A 32 Full factorial design was applied to investigate the combined effect of the two independent variables i.e. concentration of HPC (X1) and concentration of PEO WSR-1105(X2) on the dependent variables, % in vitro drug release at 1 h (Y1), % in vitro drug release at 4 h (Y2), mucoadhesive strength (Y3) and mucoadhesion time (Y4). Results: Optimized mucoadhesive buccal tablets shows in vitro drug release of 96.23±2.45 in 8 h, mucoadhesive strength of 18.20±1.44 g, mucoadhesion time 420±2.6 min and surface pH 6.75±0.015. Drug excipients compatibility study by FTIR showed no interaction between drug and excipients. Conclusion: From all parameters and experimental design evaluation, it was concluded that the drug release rate decreased with an increase the concentration of HPC and PEO WSR-1105 and mucoadhesion property increased with increase the concentration of PEO WSR-1105. The in vitro release kinetics revealed the Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion

On Fixed Point theorems in Fuzzy Metric Spaces

Abstract: This paper presents some common fixed point theorems for occasionally weakly compatible mappings in fuzzy metric spaces. Keywords: Occasionally weakly compatible mappings,fuzzy metric space

Development and validation of dissolution method for carvedilol compression-coated tablets

The present study describes the development and validation of a dissolution method for carvedilol compression-coated tablets. Dissolution test was performed using a TDT-06T dissolution apparatus. Based on the physiological conditions of the body, 0.1N hydrochloric acid was used as dissolution medium and release was monitored for 2 hours to verify the immediate release pattern of the drug in acidic pH, followed by pH 6.8 in citric-phosphate buffer for 22 hours, to simulate a sustained release pattern in the intestine. Influences of rotation speed and surfactant concentration in medium were evaluated. Samples were analysed by validated UV visible spectrophotometric method at 286 nm. 1% sodium lauryl sulphate (SLS) was found to be optimum for improving carvedilol solubility in pH 6.8 citric-phosphate buffer. Analysis of variance showed no significant difference between the results obtained at 50 and 100 rpm. The discriminating dissolution method was successfully developed for carvedilol compression-coated tablets. The conditions that allowed dissolution determination were USP type I apparatus at 100 rpm, containing 1000 ml of 0.1N HCl for 2 hours, followed by pH 6.8 citric-phosphate buffer with 1% SLS for 22 hours at 37.0 ± 0.5 ºC. Samples were analysed by UV spectrophotometric method and validated as per ICH guidelines.O presente estudo descreve o desenvolvimento e a validação de método de dissolução para comprimidos revestidos de carvedilol. O teste de dissolução foi efetuado utilizando-se o aparelho para dissolução TDT-06T. Com base nas condições fisiológicas do organismo, utilizou-se ácido clorídrico 0,1 N como meio de dissolução e a liberação foi monitorada por 2 horas para se verificar o padrão de liberação imediata do fármaco em condições de pH baixo, seguidas por pH 6,8 em tampão cítrico-fosfato por 22 horas, para simular o padrão de liberação controlada no intestino. Avaliou-se a influência da velocidade de rotação e a concentração de tensoativo no meio. As amostras foram analisadas por método espectrofotométrico UV-visível validado, em 286 nm. O laurilsulfato sódico a 1% (SLS) mostrou-se ótimo para aumentar a solubilidade do carvedilol em pH 6,8 em tampão cítrico-fosfato. A análise da variância não mostrou diferença significativa entre os resultados obtidos a 50 e a 100 rpm. O método da dissolução discriminante foi desenvolvido com sucesso para os comprimidos revestidos de carvedilol. As condições que permitiram a determinação da dissolução foram: aparelho USP tipo I a 100 rpm, contendo 1000 mL de HCL 0,1 N por 2 horas, seguido de pH 6,8 com tampão cítrico-fosfato, com 1% de SLS por 22 horas a 37,0 ± 0,5 ºC. Amostras foram analisadas por método espectrofotométrico e validadas pelas normas ICH

Weaving indigenous agricultural knowledge with formal education to enhance community food security : school competition as a pedagogical space in rural Anchetty, India

In communities from the remote rural regions of Anchetty, young learners’ informal learning experiences often come through interactions with local agriculture and the environment in which they and their families work and learn. These informal learning experiences are essential to what are otherwise called ‘indigenous knowledge systems’. For primary school students in Anchetty, the ways in which they engage in learning community-based agricultural knowledge are challenged by school-based formal education processes. Using a school competition as a pedagogical strategy for integrative space, this paper supports and explores the meaning and characteristics of indigenous agricultural knowledge (IAK)

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors

The growing practice of exploiting noninvasive fluorescence-based techniques to study G protein-coupled receptor pharmacology at the single cell and single molecule level demands the availability of high-quality fluorescent ligands. To this end, this study evaluated a new series of red-emitting ligands for the human β-adrenoceptor family. Upon the basis of the orthosteric ligands propranolol, alprenolol, and pindolol, the synthesized linker-modified congeners were coupled to the commercially available fluorophore BODIPY 630/650-X. This yielded high-affinity β-adrenoceptor fluorescent ligands for both the propranolol and alprenolol derivatives; however, the pindolol-based products displayed lower affinity. A fluorescent diethylene glycol linked propranolol derivative (18a) had the highest affinity (log KD of -9.53 and -8.46 as an antagonist of functional β2- and β1-mediated responses, respectively). Imaging studies with this compound further confirmed that it can be employed to selectively label the human β2-adrenoceptor in single living cells, with receptor-associated binding prevented by preincubation with the nonfluorescent β2-selective antagonist 3-(isopropylamino)-1-[(7-methyl-4-indanyl)oxy]-butan-2-ol (ICI 118551) (J. Cardiovasc. Pharmacol. 1983, 5, 430-437.

Synthesis and in vitro and in vivo characterization of highly β1-Selective β-Adrenoceptor partial agonists

β-Adrenoceptor antagonists boast a 50-year use for symptomatic control in numerous cardiovascular diseases. One might expect highly selective antagonists are available for the human β-adrenoceptor subtype involved in these diseases, yet few truly β1-selective molecules exist. To address this clinical need, we re-evaluated LK 204-545 (1),1 a selective β1-adrenoceptor antagonist, and discovered it possessed significant partial agonism. Removal of 1’s aromatic nitrile afforded 19, a ligand with similar β1-adrenoceptor selectivity and partial agonism (log KD of −7.75 and −5.15 as an antagonist of functional β1- and β2-mediated responses, respectively, and 34% of the maximal response of isoprenaline (β1)). In vitro β-adrenoceptor selectivity and partial agonism of 19 were mirrored in vivo. We designed analogues of 19 to improve affinity, selectivity, and partial agonism. Although partial agonism could not be fully attenuated, SAR suggests that an extended alkoxyalkoxy side chain, alongside substituents at the meta- or para-positions of the phenylurea, increases ligand affinity and β1- selectivity