orabase and betadex

A study was carried out by ultraviolet-visible (UV-vis) and Fourier transform infrared (FTIR) spectroscopies to establish the efficiency of adsorption of fluoxetine hydrochloride (FLU), onto a crosslinked β-cyclodextrin-carboxymethylcellulose (β-CD-CMC) polymer. The adsorption was performed in mixtures containing aqueous FLU solution at 20 mg/L and 0.01-0.30 g of the β-CD-CMC polymer, at 25 °C, and atmospheric pressure under stirring. The results have revealed that the adsorption is a rapid process and the polymer possesses a high affinity for FLU with an adsorption capacity of 5.076 mg of FLU/g of polymer. This adsorption may involve the formation of a stable inclusion compound β-CD-CMC/FLU through the penetration of the FLU aromatic ring (A and/or B) into the β-CD cavity, and a physical adsorption with the polymer network. The inclusion compound can be stabilized by the formation of H-bonds between the -CF(3) group of FLU and the 6'-OH group of β-CD, and van der Waals interactions between the FLU aromatic ring and β-CD cavity. The data from a kinetic study have also indicated that the adsorption process was well described by the pseudo-second-order kinetic model, in which the initial adsorption rate and constant were estimated at 1.938 mg/g min and 0.075 g/mg min, respectively. Moreover, the results of adsorption equilibrium fitted the Freundlich isotherm, indicating a multilayer coverage and heterogeneous surface. Together, these results suggest that the adsorption of FLU onto the crosslinked β-CD-CMC polymer could constitute an advantageous technology for removing this commonly used antidepressant drug from wastewater due to the high adsorption capacity of the polymer and non-toxic character of β-CD to humans and environment.

Topics: Adsorption; Antidepressive Agents; beta-Cyclodextrins; Carboxymethylcellulose Sodium; Fluoxetine; Kinetics; Polymers; Water Pollutants, Chemical; Water Purification

The aim of this study was to prepare fast-dissolving tablets of meloxicam after its complexation with β-cyclodextrin (β-CD) and to investigate the effect of using different superdisintegrants on the disintegration and release of meloxicam from the tablets. A complex of meloxicam with β-CD was prepared by spray drying and then compressed in the form of tablets utilizing the direct compression technique. Three superdisintegrants were employed at various levels - sodium starch glycolate, croscarmellose sodium, and crospovidone. Co-spray dried micro-crystalline cellulose and mannitol (Avicel HFE-102) were used as diluents in the tablets. Prior to compression, the pre-compression parameters showed satisfactory flow properties. Post-compression parameters showed that all tablet formulations had acceptable mechanical properties. Wetting and disintegration times were prolonged by increasing the level of sodium starch glycolate in the tablets. This was attributed to the formation of a viscous gel layer around the tablets by sodium starch glycolate whereas this effect was not observed with croscarmellose sodium and crospovidone. Dissolution studies showed fast release of meloxicam except in tablets containing a high level of sodium starch glycolate. Complexation of meloxicam with β-CD significantly improved the solubility of the drug and improved the mechanical properties of tablets produced by direct compression.

Topics: Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Carboxymethylcellulose Sodium; Cellulose; Excipients; Mannitol; Meloxicam; Povidone; Solubility; Starch; Tablets; Thiazines; Thiazoles; Time Factors

Carboxymethylcellulose (CMC) and beta-cyclodextrin (beta-CD)-based polymers functionalized with two types of quaternary ammonium compounds (QACs), the alkaquat DMB-451 (N-alkyl (50% C14, 40% C12, 10% C10) dimethylbenzylammonium chloride) (DMD-451) named polymer DMB-451, and FMB 1210-8 (a blend of 32 w% N-alkyl (50% C14, 40% C12, 10% C10) dimethylbenzylammonium chloride and 48 w% of didecyldimethylammonium chloride) named polymer FMB 1210-8, were synthethized and characterized by Fourier transform infrared spectroscopy. The antimicrobial activities of these polymers against Eschericia coli were also evaluated at 25 degrees C in wastewater. The results have indicated that the polymer FMB 1210-8 possesses a high-affinity binding with bacterial cells that induces a rapid disinfection process. Moreover, in the same experimental conditions of disinfection (mixture of 1.0 g of polymer and 100 mL of wastewater), the polymer FMB 1210-8 has a higher antimicrobial efficiency (99.90%) than polymer DMB-451 (92.8%). This phenomenon might be associated to a stronger interaction with bacterial cells due to stronger binding affinity for E. coli cells and greater killing efficiency of the C10 alkyl chains QAC of polymer FMB 1210-8 to disrupt the bacterial cell membrane as compared to N-alkyl (50% C14, 40% C12, 10% C10) dimethylbenzylammonium chloride. Together, these results suggest that the polymer FMB 1210-8 could constitute a good disinfectant against Escherichia coli, which could be advantageously used in wastewater treatments due to the low toxicity of beta-CD and CMC, and moderated toxicity of FMB 1210-8 to human and environment.

Topics: beta-Cyclodextrins; Carboxymethylcellulose Sodium; Disinfectants; Escherichia coli; Filtration; Polymers; Quaternary Ammonium Compounds; Spectroscopy, Fourier Transform Infrared; Structure-Activity Relationship; Water Purification

pH-sensitive microgels were prepared by crosslinking carboxymethylcellulose (CMC) and polymeric beta-cyclodextrin (PbetaCD) using (2-hydroxyethyl)trimethylammonium chloride benzoate (TMACB) as a crosslinker. PbetaCD was prepared by reacting epichlorohydrin and beta-CD in an aqueous phase (NaOH solution, 30% (w/w)). TMACB will interact with CMC by an electrostatic interaction and it will also interact with PbetaCD by a hydrophobic interaction. The size of microgel was tens of nanometers to several micrometers. The degree of calcein release in 24h from the microgels was as low as 23% at pH 8.0. The degree of release at pH 3.0 was almost 100%. The carboxyl groups of CMC will lose their charge in an acidic condition and they would lose their ability to form salt bridges with TMACB, leading to the disintegration of microgels. The degree of release at pH 11, about 47%, was less than the value at pH 3.0 but it was greater than the value at pH 8.0. The CMC will be strongly electrostatically charged in the alkali condition, so the microgels would swell due to the electrostatic repulsion among CMC molecules, which could promote the release of their contents.

Topics: beta-Cyclodextrins; Carboxymethylcellulose Sodium; Chemistry, Pharmaceutical; Cross-Linking Reagents; Drug Carriers; Fluoresceins; Gels; Hydrogen-Ion Concentration; Hydrophobic and Hydrophilic Interactions; Particle Size; Quaternary Ammonium Compounds; Salts; Static Electricity

A study of adsorption/recovery of nonylphenol 9 mole ethoxylate (NP9EO) on a crosslinked beta-cyclodextrin-carboxymethylcellulose (beta-CD-CMC) polymer was carried out by ultraviolet-visible (UV-vis) and Fourier transform infrared (FTIR) spectroscopies. The adsorption was performed in mixtures containing 500 mg of the beta-CD-CMC polymer and aqueous NP9EO solutions at concentrations 12-82 mg/L, whereas the recovery of NP9EO was effectuated by shaking the beta-CD-CMC polymer loaded with methanol. The assays were made at 25 degrees C and atmospheric pressure under agitation. The results have shown that the adsorption is a rapid process and the beta-CD-CMC polymer exhibits a high NP9EO adsorption capacity of 83-92 w% (1.1-6.8 mg NP9EO/g beta-CD-CMC polymer) dependent of the initial NP9EO concentration in liquid phase. This adsorption may involve the formation of an inclusion complex beta-CD-NP9EO and a physical adsorption in the polymer network. The adsorption equilibrium measurements, which were analyzed using the Langmuir isotherm, have indicated a monolayer coverage and the homogeneous distribution of active sites at the surface of the beta-CD-CMC polymer. Moreover, the negative value obtained for the free energy change (-13.2 kJ/mol) has indicated that the adsorption process is spontaneous. In parallel, the beta-CD-CMC polymer exhibited a high NP9EO recovery efficiency of 97 w% that may occur through a decrease of binding strength between beta-CD-CMC polymer and NP9EO. Together, these results suggest that the beta-CD-CMC polymer could constitute a good adsorbent for removing nonylphenol ethoxylates from wastewater due to its high adsorption capacity and non-toxic character of beta-CD and CMC to environment.

Topics: Adsorption; beta-Cyclodextrins; Carboxymethylcellulose Sodium; Ethylene Glycols; Molecular Structure; Polymers; Waste Disposal, Fluid; Water; Water Pollutants, Chemical; Water Purification

The objective of this work was to apply response surface approach to investigate main and interaction effects of formulation parameters in optimizing novel fast disintegrating tablet formulation using β cyclodextrin as a diluent. The variables studied were diluent (β cyclodextrin, X (1)), superdisintegrant (Croscarmellose sodium, X (2)), and direct compression aid (Spray dried lactose, X (3)). Tablets were prepared by direct compression method on B2 rotary tablet press using flat plain-face punches and characterized for weight variation, thickness, disintegration time (Y (1)), and hardness (Y (2)). Disintegration time was strongly affected by quadratic terms of β cyclodextrin, croscarmellose sodium, and spray-dried lactose. The positive value of regression coefficient for β cyclodextrin suggested that hardness increased with increased amount of β cyclodextrin. In general, disintegration of tablets has been reported to slow down with increase in hardness. However in the present study, higher concentration of β cyclodextrin was found to improve tablet hardness without increasing the disintegration time. Thus, β cyclodextrin is proposed as a suitable diluent to achieve fast disintegrating tablets with sufficient hardness. Good correlation between the predicted values and experimental data of the optimized formulation validated prognostic ability of response surface methodology in optimizing fast disintegrating tablets using β cyclodextrin as a diluent.

Topics: Antiemetics; beta-Cyclodextrins; Carboxymethylcellulose Sodium; Dosage Forms; Drug Compounding; Drug Delivery Systems; Excipients; Granisetron; Hardness; Lactose; Reproducibility of Results; Solubility; Tablets

Dextran, mannan and carboxymethylcellulose, previously activated by periodate oxidation, were grafted with beta-cyclodextrin moieties by reductive alkylation in the presence of sodium borohydride. These polymers were used as supramolecular carriers for naproxen, improving the "in vivo" anti-inflammatory properties of this drug.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Carboxymethylcellulose Sodium; Carcinogens; Carrageenan; Dextrans; Drug Carriers; Edema; Male; Mannans; Naproxen; Oxidation-Reduction; Periodic Acid; Rats; Rats, Wistar

Superoxide dismutase was glycosidated with cyclodextrin-branched carboxymethylcellulose. The modified enzyme contained 1.4 mol polymer per mol protein and retained 87% of the initial activity. The anti-inflammatory activity of superoxide dismutase was 2.2-times increased after conjugation and its plasma half-life time was prolonged from 4.8 min to 7.2 h.

Topics: Animals; Anti-Inflammatory Agents; beta-Cyclodextrins; Carboxymethylcellulose Sodium; Carrageenan; Cyclodextrins; Edema; Foot; Male; Rats; Rats, Wistar; Superoxide Dismutase

Bovine pancreatic trypsin was chemically modified by a beta-cyclodextrin-carboxymethylcellulose polymer using 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide as coupling agent. The conjugate retained 110% and 95% of the initial esterolytic and proteolytic activity, respectively, and contained about 2 mol of polymer per mol of trypsin. The optimum temperature for trypsin was increased to 8 degrees C after conjugation. The thermostability of the enzyme was increased to about 16 degrees C after modification. The conjugate prepared was also more stable against thermal incubation at different temperatures ranging from 45 degrees C to 60 degrees C. In comparison with native trypsin, the polymer-enzyme complex was more resistant to autolytic degradation at pH 9.0, retaining about 65% of the initial activity after 3h incubation. In addition, modification protected trypsin against denaturation in the presence of sodium dodecylsulfate.

Topics: beta-Cyclodextrins; Carboxymethylcellulose Sodium; Cyclodextrins; Enzyme Activation; Enzyme Stability; Isoenzymes; Kinetics; Macromolecular Substances; Protein Binding; Protein Denaturation; Temperature; Trypsin

The inclusion complexes of metoprolol (MT) and carboxymethyl-beta-cyclodextrin (CMCD) were prepared and the stability constants of the complexes were determined. Binding studies performed using high performance liquid chromatography (HPLC), UV spectrometry and capillary electrophoresis (CE) indicated that a complex with 1:1 stoichiometry is predominant in the solution. The enantiomers of MT possess relatively high affinity towards CMCD with stability constants of 288 and 262 per M for (R)- and (S)-MT, respectively. Through nuclear magnetic resonance (NMR) analysis, MT was predicted to be a bent structure with phenyl ring of MT inserted in the shielding cavity of CMCD during complex formation. The NMR data suggested that the chiral side chain and the methoxyethyl moiety of MT are aligned in the deshielding zone, above and below the CMCD torus ring.

Topics: Adrenergic beta-Antagonists; beta-Cyclodextrins; Carboxymethylcellulose Sodium; Carcinogens; Cyclodextrins; Metoprolol; Spectrophotometry, Ultraviolet; Stereoisomerism