scholarly journals Influence of Acetylated Annealed Starch on the Release of β-Escin from the Anionic and Non-Ionic Hydrophilic Gels

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 84
Author(s):  
Justyna Kobryń ◽  
Tomasz Zięba ◽  
Sandra Karolina Sowa ◽  
Witold Musiał

Naturally sourced products introduced to human nutrition and rediscovered for therapy include polysaccharides from potatoes. The starch may obtain unique properties via acetylation with acetic anhydride at 13 cm3/100 g of starch as the basic dose of reagent used in industrial conditions. The hydrogel formulation was applied as a carrier for escin included in the dry extract of Aesculus hippocastanum. Six hydrogels were evaluated (methylcellulose, polyacrylic acid-Carbopol 980 NF and polyacrylate crosspolymer 11—Aristoflex Velvet) with various concentrations of the modified starch. The kinetic studies of in vitro β-escin release were carried out in purified water at 37 ± 0.5 °C using a paddle apparatus at 50 rpm and a time period of 7 h. The criterion for the most suitable model was based on a high correlation coefficient of evaluated release profiles. The addition of modified annealed acetylated potato starch resulted in prolongation of β-escin release.

1973 ◽  
Vol 30 (01) ◽  
pp. 138-147 ◽  
Author(s):  
Christopher R. Muirhead

SummaryThe filter loop technique which measures platelet aggregation in vivo in the flowing-blood of the rat was compared to the optical density technique of Born which is carried out in vitro with platelet rich plasma. Using these two experimental models the effect on platelet aggregation of three known inhibitors sulfinpyrazone, dipyridamole and prostaglandin E1, and a novel compound 5-oxo-l-cyclopentene-l-heptanoic acid (AY-16, 804) was determined.The effects on platelet aggregation of the known inhibitors were consistent with information in the literature. Prostaglandin E1 was the most potent inhibitor in both techniques; sulfinpyrazone inhibited aggregation in both models but was less potent than prostaglandin E1. AY-16, 804 exhibited activity in vitro and in vivo similar to that of sulfinpyrazone. Dipyridamole did not inhibit platelet aggregation in vivo and did not inhibit aggregation in vitro in concentrations at which it remained soluble.The filter loop technique is a suitable model for measuring platelet aggregation in the flowing blood of the rat. It is a relatively simple method of determining aggregation and easily adapted to other species.


Diabetes ◽  
1975 ◽  
Vol 24 (12) ◽  
pp. 1094-1100 ◽  
Author(s):  
A. Rabinovitch ◽  
A. Gutzeit ◽  
A. E. Renold ◽  
E. Cerasi

Author(s):  
Umamaheswara G. ◽  
Anudeep D.

Fluvastatin sodium is a novel compound used as cholesterol lowering agent which acts through the inhibition of 3- hydroxyl-3- methyl glutaryl- coenzyme A (HMG-Co A) reductase. It has short biological half life (1-3h) in humans required a dosing frequency of 20 to 40mg twice a day. Due to its short variable biological half life it has been developed to a sustained gastroretentive system with a natural and synthetic polymer and to study how far the natural mucilage improves the sustained activity. Floating tablets were prepared by direct compression method using in combination of natural mucilage and synthetic polymer. Prior to the preparation of tablets the physical mixtures were subjected to FT IR studies and pre compression parameters. After preparation of tablets they were subjected to various tests like swollen index, drug content, In vitro dissolution and release kinetics with pcp disso software etc. The tablets prepared by direct compression shown good in thickness, hardness and uniformity in drug content, the prepared tablets floated more than 12h except FS1 and FS2 shows 9 and 11h. Swollen index studies shows with increase in concentration of polymer the swelling increases the diffusion path length by which the drug molecule may have to travel and cause lag time. In vitro results shows that on increasing the amount of hibiscus polymer the sustain activity is increased because of its integrity and forms a thick swollen mass and reduces the erosion property of the HypromelloseK100M, kinetic studies shows that FS 1, FS2, FS3 followed the Korsmeyer peppas model and the rest FS 4, FS 5, FS6 follows the zero order respectively. Based on n value indicating that the drug release followed super case II transport mechanism due to the erosion of the polymer.


Author(s):  
Sarika Pundir ◽  
Ashutosh Badola

In the present study we have formulated (F1 to F6) matrix tablets of atenolol and indapamide for the management of hypertension. As in simultaneous estimation of these drugs it was found that a confined release can be formulated. In the formulation of SR matrix tablet by using different concentration of delayed release agent DCP and pregelatinized starch as disintegrant we prepared tablets by wet granulation method. For sustained release action HPMC polymers were used for film coating. Preformulation studies were performed prior to compression. The compressed SR matrix tablets were evaluated for weight variation, hardness, friability, drug content, disintegration time and in vitro drug release using USP dissolution apparatus type 2 (paddle). It was found that the optimized formulation showed 49.33%, 48.90%, 48.52%, 47.65%, 46.84% and 46.51% release for atenolol in 12 hours respectively. However, indapamide released 49.62%, 49.39%, 48.72%, 48.27%, 47.59% and 47.36% at the end of 12 hr. The IR spectrum study revealed that there is no disturbance in the principal peaks of pure drugs atenolol and indapamide. This confirms the integrity of pure drugs and no incompatibility of them with excipients. The stability studies were carried out for the optimized batch for one months and it showed satisfactory results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanism of drug and release follows Zero-order, Super case II transport.


1997 ◽  
Vol 62 (11) ◽  
pp. 1804-1814 ◽  
Author(s):  
Marie Stiborová ◽  
Hana Hansíková

Tulip bulbs (Tulipa fosteriana, L.) contain peroxidases catalyzing the oxidation of the xenobiotics N-nitrosodimethylamine (NDMA) and N-nitroso-N-methylaniline (NMA). Three anionic (A1, A2, A3) and four cationic (B, C, D, E) peroxidases were purified from this tissue, partially characterized and used for kinetic studies. Demethylation of NDMA and NMA producing formaldehyde is catalyzed by one anionic (A1) and three cationic (C, D, E) peroxidases. The oxidation of NDMA by tulip peroxidases exhibits the Michaelis-Menten kinetics. The apparent Michaelis constant and the maximal velocity values for this substrate were determined. On the other hand, non-Michaelian kinetics for the NMA oxidation were observed with tulip peroxidases. The most abundant cationic peroxidase (peroxidase C) was used for detailed enzymatic studies. In addition to formation of formaldehyde, methylaniline, aniline, 4-aminophenol and phenol were found to be metabolites formed from NMA. Phenol was formed presumably by N-demethylation via a benzenediazonium ion, while methylaniline, aniline and 4-aminophenol were products of denitrosation of the substrate. The efficiencies of plant peroxidases to oxidize NDMA and NMA in vitro are compared with those of cytochromes P450 and discussed.


2021 ◽  
pp. 2100102
Author(s):  
Shuyu Jia ◽  
Bin Yu ◽  
Haibo Zhao ◽  
Haiteng Tao ◽  
Pengfei Liu ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 998
Author(s):  
Virgínia Barreto Lordello ◽  
Andréia Bagliotti Meneguin ◽  
Sarah Raquel de Annunzio ◽  
Maria Pía Taranto ◽  
Marlus Chorilli ◽  
...  

Background: Probiotic bacteria have been emerging as a trustworthy choice for the prevention and treatment of Candida spp. infections. This study aimed to develop and characterize an orodispersible film (ODF) for delivering the potentially probiotic Enterococcus faecium CRL 183 into the oral cavity, evaluating its in vitro antifungal activity against Candida albicans. Methods and Results: The ODF was composed by carboxymethylcellulose, gelatin, and potato starch, and its physical, chemical, and mechanical properties were studied. The probiotic resistance and viability during processing and storage were evaluated as well as its in vitro antifungal activity against C. albicans. The ODFs were thin, resistant, and flexible, with neutral pH and microbiologically safe. The probiotic resisted the ODF obtaining process, demonstrating high viability (>9 log10 CFU·g−1), up to 90 days of storage at room temperature. The Probiotic Film promoted 68.9% of reduction in fungal early biofilm and 91.2% in its mature biofilm compared to the group stimulated with the control film. Those results were confirmed through SEM images. Conclusion: The probiotic ODF developed is a promising strategy to prevent oral candidiasis, since it permits the local probiotic delivery, which in turn was able to reduce C. albicans biofilm formation.


2021 ◽  
Vol 99 (Supplement_1) ◽  
pp. 177-177
Author(s):  
Gabriela E Martinez Padilla ◽  
Rajesh Jha ◽  
Vivek Fellner ◽  
Eric van Heugten

Abstract This study evaluated short-chain fatty acid (SCFA) production from purified fiber sources when fermented in vitro using pig cecal contents as an inoculum. Fiber sources of interest were inulin from chicory root (native and long-chain inulin with 90 and 98% fiber, respectively), pectin from citrus peel (high methoxyl pectin), resistant starch (native starch), potato starch (commercial grade), and β-glucan (β-1,3;β-1,6 yeast-derived). Cellulose and cornstarch were used as indigestible and highly digestible carbohydrates, respectively. Triplicate samples of substrates (2 g) were subjected to enzymatic hydrolysis with pepsin and pancreatin for 6 h. Subsequently, hydrolyzed residues (200 mg) were incubated under anaerobic conditions at 39°C with 30 mL solution of cecal inoculum collected from 3 sows fed a standard commercial diet and buffered mineral solution. After 48 h of incubation, solutions from fermented samples were analyzed for pH, SCFA, and branched-chain fatty acids (BCFA) using gas-liquid chromatography. Enzymatic hydrolysis had no effect on digestion of β-glucan, but total SCFA concentration after fermentation was highest (26.13 mmol/g) followed by resistant starch (22.61 mmol/g) and potato starch (22.20 mmol/g) and was lowest for cellulose (13.91 mmol/g). In contrast, native inulin was highly digested during enzymatic hydrolysis, resulting in the lowest substrate available for fermentation (11.84% DM) and the highest pH (5.98). Enzymatic hydrolysis and fermentation of resistant starch increased (P< 0.001) concentrations of acetate (0.60 mg/g), whereas potato starch and β-glucan yielded more butyrate (0.60 and 0.54 mg/g respectively), and β-glucan resulted in greater (P< 0.001) propionate concentrations (0.69 mg/g). Pectin resulted in the highest fermentation (82.38% DM disappearance) and the lowest pH (4.03) compared to the other fiber sources (P< 0.001) and yielded the lowest BCFA concentration (1.89 mM, P< 0.001). Results suggest that fermentation of resistant starch, potato starch, and β-glucan produced higher SCFA concentrations, while pectin resulted in a decreased pH of fermentation solution.


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