Effect of Gap Junction Blocker β-Glycyrrhetinic Acid on Taste Disk Cells in Frog

Sato, Toshihide; Nishishita, Kazuhisa; Okada, Yukio; Toda, Kazuo

doi:10.1007/s10571-008-9342-6

Cited by 6 publications

(5 citation statements)

References 31 publications

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“…More lately, the innovation in taste reduction techniques has presented taste suppressant compounds acting directly on different types of taste receptors, as e.g. by blocking gap junctions of channels and hemichannels 25,26 . However, recent trends are getting towards more cost effective and easy to scale-up techniques 27 among which, much older pharmaceutical processes, like wet granulation and fluidized bed coating, have regained great interest 28 .…”

Section: Discussionmentioning

confidence: 99%

Design, development andin-vitroevaluation of diclofenac taste-masked orodispersible tablet formulations

Guhmann

Preis

Gerber³

et al. 2014

Drug Development and Industrial Pharmacy

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Section: Discussionmentioning

confidence: 99%

Design, development andin-vitroevaluation of diclofenac taste-masked orodispersible tablet formulations

Guhmann

Preis

Gerber³

et al. 2014

Drug Development and Industrial Pharmacy

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“…We perfuse isolated adult and embryonic hearts with BGA, a nonspecific gap junction blocker known to inhibit intercellular ion transport between embryonic chick epithelial cells at 10 μM (30) and in rat, frog, mouse, and human systems (31)(32)(33)(34). Adult hearts stopped beating within 10 min posttreatment at 25 μM BGA (Fig.…”

Section: Conduction Interference Experiments Are Consistent With Mechmentioning

confidence: 99%

Mechanical signaling coordinates the embryonic heartbeat

Chiou

Rocks

Chen

et al. 2016

Proc. Natl. Acad. Sci. U.S.A.

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In the beating heart, cardiac myocytes (CMs) contract in a coordinated fashion, generating contractile wave fronts that propagate through the heart with each beat. Coordinating this wave front requires fast and robust signaling mechanisms between CMs. The primary signaling mechanism has long been identified as electrical: gap junctions conduct ions between CMs, triggering membrane depolarization, intracellular calcium release, and actomyosin contraction. In contrast, we propose here that, in the early embryonic heart tube, the signaling mechanism coordinating beats is mechanical rather than electrical. We present a simple biophysical model in which CMs are mechanically excitable inclusions embedded within the extracellular matrix (ECM), modeled as an elastic-fluid biphasic material. Our model predicts strong stiffness dependence in both the heartbeat velocity and strain in isolated hearts, as well as the strain for a hydrogel-cultured CM, in quantitative agreement with recent experiments. We challenge our model with experiments disrupting electrical conduction by perfusing intact adult and embryonic hearts with a gap junction blocker, β-glycyrrhetinic acid (BGA). We find this treatment causes rapid failure in adult hearts but not embryonic hearts-consistent with our hypothesis. Last, our model predicts a minimum matrix stiffness necessary to propagate a mechanically coordinated wave front. The predicted value is in accord with our stiffness measurements at the onset of beating, suggesting that mechanical signaling may initiate the very first heartbeats. mechanotransduction | excitable media | cardiac development | heartbeat | reaction-diffusion

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“…Bitter tastes can be masked by applying a polymeric coating layer to create a physical barrier around the drug [3, 4] or by the use of complexing agents to form inclusion complexes or resonates [5]. Recently, taste suppressant molecules have been used to block the gap junction channels and hemichannels in taste bud cells to suppress taste [6, 7]. However, there is a need for an approach to taste masking that offers robustness and cost-effectiveness while being simple to scale up.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Hot-Melt Extruded Patient-Centric Ketoprofen Mini-Tablets

Alshetaili¹,

Almutairy²,

Tiwari³

et al. 2016

CDD

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Background Bitter tasting drugs represent a large portion of active pharmaceutical ingredients. Mini-tablets are specifically designed for patients with difficulty in swallowing particular in young children up to 10 years of age, geriatric patients and patients with esophagitis. Objective The present study was aimed to prepare, taste-masked mini-tablets, which are easily swallowed dosage forms, primarily to be used by pediatric and geriatric patients. Methods Ketoprofen (10%–50% w/w) and Eudragit® EPO were blended and extruded with a 5-mm strand die and cut into consistent mini-tablets by using an adapted downstream pelletizer. Results Differential scanning calorimetry and polarized light microscopy-hot stage microscopy studies confirmed that the binary mixtures were miscible under the employed extrusion temperatures. In-vitro release studies showed that drug release was less than 0.5% within the first 2 min in simulated salivary fluid (pH 6.8) and more than 90% in the first 20 min in gastric media (pH 1.0). The results of the electronic tongue analysis were well correlated with the drug release profile of the mini-tablets in the artificial saliva. Scanning electron microscopy revealed no cracks on the surface of the mini-tablets, confirming that the mini-tablets were compact solids. Chemical imaging confirmed the uniform distribution of ketoprofen inside the polymer matrices. Conclusion Eudragit® EPO containing ketoprofen at various drug loads were successfully melt extruded into tasted-masked mini-tablets. The reduced drug release at salivary pH correlated well with Astree e-Tongue studies for taste masking efficiency.

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Effect of Gap Junction Blocker β-Glycyrrhetinic Acid on Taste Disk Cells in Frog

Cited by 6 publications

References 31 publications

Design, development andin-vitroevaluation of diclofenac taste-masked orodispersible tablet formulations

Design, development andin-vitroevaluation of diclofenac taste-masked orodispersible tablet formulations

Mechanical signaling coordinates the embryonic heartbeat

Preparation and Evaluation of Hot-Melt Extruded Patient-Centric Ketoprofen Mini-Tablets

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