Preparation and In Vitro Evaluation of Carboxymethyl Konjac Glucomannan Coated 5-Aminosalicylic Acid Tablets for Colonic Delivery

2010 ◽  
Vol 152-153 ◽  
pp. 1712-1715 ◽  
Author(s):  
Xiao Yan Long ◽  
Xue Gang Luo ◽  
Neng Wu Zou ◽  
Yong Hong Ma
Keyword(s):  
Konjac Glucomannan ◽  
Viscosity Measurement ◽  
Simulation Environment ◽  
Aminosalicylic Acid ◽  
Colonic Delivery ◽  
Buffer Solutions ◽  
Lower Viscosity ◽  
Potential Use ◽  
Carboxymethyl Konjac Glucomannan

Konjac Glucomannan(KGM) was denatured by Carboxylmethylation to prepare Carboxymethyl konjac glucomannan(CMKGM) as coating material of 5-aminosalicylic acid(5-ASA) tablets. The 5-ASA release properties of the tablets were measured in vitro in the gastrointestinal tract simulation environment and in buffer solutions with β-mannase of pH 6.8 at 37 ± 0.5 degrees. The properties of the CMKGM were analyzed by FTIR spectra, viscosity measurement and swelling measurement. The integrality of the 5-ASA was investigated by ultraviolet spectrometry. The viscosity and swelling showed that CMKGM has lower swelling and lower viscosity compared to KGM. 5-ASA was released least in stimulating gastric environment and in pH 6.8 phosphate buffers,while the preparation was fast released in pH 6.8 phosphate buffers with β-mannase. The preparation was released 14% after 4 hours in pH 6.8 phosphate buffers , at the same time the preparation in pH 6.8 phosphate buffers with 0.2u ml-1 β-mannase was released 97% in 12 hours.The results suggested that CMKGM may be a useful carrier of 5 –ASA for colon-specific delivery. It has a potential use for advanced controlled release.

scholarly journals Statistical optimization of alginate-based oral dosage form of 5-aminosalicylic acid aimed to colonic delivery: In vitro and in vivo evaluation

2019 ◽  
Vol 52 ◽  
pp. 177-188 ◽  
Author(s):  
Ehsan Kaffash ◽  
Farinaz Saremnejad ◽  
Mohammadreza Abbaspour ◽  
Seyed Ahmad Mohajeri ◽  
Hadi Afrasiabi Garekani ◽  
...  
Keyword(s):  
Dosage Form ◽  
Statistical Optimization ◽  
Oral Dosage ◽  
Aminosalicylic Acid ◽  
Colonic Delivery ◽  
In Vivo Evaluation ◽  
Oral Dosage Form

Rhenium-188 Labeled Hydroxyapatite and Rhenium-188 Sulfur Colloid

1997 ◽  
Vol 36 (02) ◽  
pp. 71-75 ◽  
Author(s):  
S. Glatz ◽  
S. N. Reske ◽  
K. G. Grillenberger
Keyword(s):  
Synovial Fluid ◽  
Ph Value ◽  
Surgical Removal ◽  
Radiation Synovectomy ◽  
Sulfur Colloid ◽  
Target Organs ◽  
Aseptic Conditions ◽  
In Vitro Stability ◽  
Potential Use

Summary Aim: One therapeutic approach to rheumatoid arthritis and other inflammatory arthropathies besides surgical removal of inflamed synovium is radiation synovectomy using beta-emitting radionuclides to destroy the affected synovial tissue. Up to now the major problem associated with the use of labeled particles or colloids has been considerable leakage of radionuclides from the injected joint coupled with high radiation doses to liver and other non target organs. In this study we compared 188Re labeled hydroxyapatite particles and 188Re rhenium sulfur colloid for their potential use in radiation synovectomy. Methods: To this end we varied the labeling conditions (concentrations, pH-value, heating procedure) and analyzed the labeling yield, radiochemical purity, and in vitro stability of the resulting radiopharmaceutical. Results: After optimizing labeling conditions we achieved a labeling yield of more than 80% for 188Re hydroxyapatite and more than 90% for the rhenium sulfur colloid. Both of the radiopharmaceuticals can be prepared under aseptic conditions using an autoclav for heating without loss of activity. In vitro stability studies using various challenge solutions (water, normal saline, diluted synovial fluid) showed that 188Re labeled hydroxyapatite particles lost about 80% of their activity within 5 d in synovial fluid. Rhenium sulfur colloid on the other hand proved to be very stable with a remaining activity of more than 93% after 5 d in diluted synovial fluid. Conclusion: These in vitro results suggest that 188Re labeled rhenium sulfur colloid expects to be more suitable for therapeutic use in radiation synovectomy than the labeled hydroxyapatite particles.

Desirability Based Optimization of New Mesalazine Modified Release Formulations: Compression Coated Tablets and Mini Tablets in Capsules

2020 ◽  
Vol 17 (2) ◽  
pp. 114-123
Author(s):  
Marilena Vlachou ◽  
Angeliki Siamidi ◽  
Yannis Dotsikas
Keyword(s):  
Gastrointestinal Tract ◽  
Experimental Design ◽  
Desirability Function ◽  
Symptomatic Treatment ◽  
Mixture Design ◽  
Upper Gastrointestinal Tract ◽  
Modified Release ◽  
Aminosalicylic Acid ◽  
Colonic Delivery ◽  
Upper Gastrointestinal

Background: Mesalazine (5-aminosalicylic acid, 5-ASA) is a drug substance with an antiinflammatory activity, which is mainly used in the symptomatic treatment of diseases, such as Ulcerative Colitis, the Crohn's disease and the idiopathic inflammatory bowel disease. Mesalazine exerts its effect locally in the inflamed area of the intestine and not through systematic absorption, therefore the investigation of its release characteristics from solid pharmaceutical formulations is of great importance. Objective: The development of novel mesalazine modified release formulations with improved properties, regarding drug release in the gastrointestinal tract, by utilisation of the Design of Experiments (DoE) approach. Methods: D-optimal experimental design was applied. A Simplex Lattice mixture design was used for the development of suitable capsules containing 4 mini tablets and a D-optimal mixture design was used for compression-coated tablets, with the following characteristics: ≤10% release in 2 h, to minimize its degradation in the upper gastrointestinal tract, 20-40% release in 5 h for mesalazine administration in the small intestine, and quantitative release in 12 h for colonic delivery. The dissolution experiments were conducted in gastrointestinal-like fluids and pectinases to simulate the pectinolytic enzymes present in the colon. Results: The optimal compositions were reached via the desirability function, as a compromise to the different responses. The optimal solutions for both formulations led to colon-specific delivery of the active substance with minimal 5-ASA release in the upper gastrointestinal tract and appeared to conform with the pre-determined characteristics. Hard gelatin capsules, when filled with mini-tablets led to the aimed modified release profile, having sigmoidal characteristics and compression coated tablets led to colonic delivery. Conclusion: Two novel mesalazine formulations were developed with the desirable colonic release, by conducting a minimal number of experiments, as suggested by DoE experimental design.

scholarly journals In VitroActivities of Hexaazatrinaphthylenes against Leishmania spp.

2015 ◽  
Vol 59 (5) ◽  
pp. 2867-2874 ◽  
Author(s):  
Atteneri López-Arencibia ◽  
Daniel García-Velázquez ◽  
Carmen M. Martín-Navarro ◽  
Ines Sifaoui ◽  
María Reyes-Batlle ◽  
...  
Keyword(s):  
Therapeutic Agents ◽  
Content Type ◽  
Inhibition Effect ◽  
Intracellular Amastigotes ◽  
Dependent Inhibition ◽  
Leishmania Spp ◽  
Dose Dependent Inhibition ◽  
Dose Dependent ◽  
Potential Use

ABSTRACTThein vitroactivity of a novel group of compounds, hexaazatrinaphthylene derivatives, against two species ofLeishmaniais described in this study. These compounds showed a significant dose-dependent inhibition effect on the proliferation of the parasites, with 50% inhibitory concentrations (IC50s) ranging from 1.23 to 25.05 μM against the promastigote stage and 0.5 to 0.7 μM against intracellular amastigotes. Also, a cytotoxicity assay was carried out to in order to evaluate the possible toxic effects of these compounds. Moreover, different assays were performed to determine the type of cell death induced after incubation with these compounds. The obtained results highlight the potential use of hexaazatrinaphthylene derivatives againstLeishmaniaspecies, and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.

scholarly journals Native Chilean Berries Preservation and In Vitro Studies of a Polyphenol Highly Antioxidant Extract from Maqui as a Potential Agent against Inflammatory Diseases

Antioxidants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 843
Author(s):  
Tamara Ortiz ◽  
Federico Argüelles-Arias ◽  
Belén Begines ◽  
Josefa-María García-Montes ◽  
Alejandra Pereira ◽  
...  
Keyword(s):  
High Performance ◽  
Large Scale ◽  
Inflammatory Diseases ◽  
In Vitro Studies ◽  
Aminosalicylic Acid ◽  
Colon Cells ◽  
Antioxidant Power ◽  
Maqui Berry ◽  
Physiological Benefits

The best conservation method for native Chilean berries has been investigated in combination with an implemented large-scale extract of maqui berry, rich in total polyphenols and anthocyanin to be tested in intestinal epithelial and immune cells. The methanolic extract was obtained from lyophilized and analyzed maqui berries using Folin–Ciocalteu to quantify the total polyphenol content, as well as 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP), and oxygen radical absorbance capacity (ORAC) to measure the antioxidant capacity. Determination of maqui’s anthocyanins profile was performed by ultra-high-performance liquid chromatography (UHPLC-MS/MS). Viability, cytotoxicity, and percent oxidation in epithelial colon cells (HT-29) and macrophages cells (RAW 264.7) were evaluated. In conclusion, preservation studies confirmed that the maqui properties and composition in fresh or frozen conditions are preserved and a more efficient and convenient extraction methodology was achieved. In vitro studies of epithelial cells have shown that this extract has a powerful antioxidant strength exhibiting a dose-dependent behavior. When lipopolysaccharide (LPS)-macrophages were activated, noncytotoxic effects were observed, and a relationship between oxidative stress and inflammation response was demonstrated. The maqui extract along with 5-aminosalicylic acid (5-ASA) have a synergistic effect. All of the compiled data pointed out to the use of this extract as a potential nutraceutical agent with physiological benefits for the treatment of inflammatory bowel disease (IBD).

scholarly journals Antimicrobial Activity of Chitosan Oligosaccharides with Special Attention to Antiparasitic Potential

Marine Drugs ◽  
2021 ◽  
Vol 19 (2) ◽  
pp. 110
Author(s):  
Nayara Sousa da Silva ◽  
Nathália Kelly Araújo ◽  
Alessandra Daniele-Silva ◽  
Johny Wysllas de Freitas Oliveira ◽  
Júlia Maria de Medeiros ◽  
...  
Keyword(s):  
Disease Outbreaks ◽  
Biological Properties ◽  
Enzymatic Production ◽  
Infectious Disease Outbreaks ◽  
Chitosan Oligosaccharides ◽  
Lower Viscosity ◽  
Biomedical Industry ◽  
Parasite Aggregation ◽  
Hydrolysis Of

The global rise of infectious disease outbreaks and the progression of microbial resistance reinforce the importance of researching new biomolecules. Obtained from the hydrolysis of chitosan, chitooligosaccharides (COSs) have demonstrated several biological properties, including antimicrobial, and greater advantage over chitosan due to their higher solubility and lower viscosity. Despite the evidence of the biotechnological potential of COSs, their effects on trypanosomatids are still scarce. The objectives of this study were the enzymatic production, characterization, and in vitro evaluation of the cytotoxic, antibacterial, antifungal, and antiparasitic effects of COSs. NMR and mass spectrometry analyses indicated the presence of a mixture with 81% deacetylated COS and acetylated hexamers. COSs demonstrated no evidence of cytotoxicity upon 2 mg/mL. In addition, COSs showed interesting activity against bacteria and yeasts and a time-dependent parasitic inhibition. Scanning electron microscopy images indicated a parasite aggregation ability of COSs. Thus, the broad biological effect of COSs makes them a promising molecule for the biomedical industry.

scholarly journals Ultramicronized Palmitoylethanolamide (um-PEA): A New Possible Adjuvant Treatment in COVID-19 patients

2021 ◽  
Vol 14 (4) ◽  
pp. 336
Author(s):  
Annalisa Noce ◽  
Maria Albanese ◽  
Giulia Marrone ◽  
Manuela Di Lauro ◽  
Anna Pietroboni Zaitseva ◽  
...  
Keyword(s):  
Adjuvant Treatment ◽  
Pulmonary Involvement ◽  
In Vivo Studies ◽  
Pharmacological Treatments ◽  
Beneficial Effects ◽  
Coronavirus Infection ◽  
Ultramicronized Palmitoylethanolamide ◽  
Potential Use

The Coronavirus Disease-19 (COVID-19) pandemic has caused more than 100,000,000 cases of coronavirus infection in the world in just a year, of which there were 2 million deaths. Its clinical picture is characterized by pulmonary involvement that culminates, in the most severe cases, in acute respiratory distress syndrome (ARDS). However, COVID-19 affects other organs and systems, including cardiovascular, urinary, gastrointestinal, and nervous systems. Currently, unique-drug therapy is not supported by international guidelines. In this context, it is important to resort to adjuvant therapies in combination with traditional pharmacological treatments. Among natural bioactive compounds, palmitoylethanolamide (PEA) seems to have potentially beneficial effects. In fact, the Food and Drug Administration (FDA) authorized an ongoing clinical trial with ultramicronized (um)-PEA as an add-on therapy in the treatment of Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) infection. In support of this hypothesis, in vitro and in vivo studies have highlighted the immunomodulatory, anti-inflammatory, neuroprotective and pain-relieving effects of PEA, especially in its um form. The purpose of this review is to highlight the potential use of um-PEA as an adjuvant treatment in SARS-CoV-2 infection.

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