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Excipients and Their Attributes in Granulation
Published in Dilip M. Parikh, Handbook of Pharmaceutical Granulation Technology, 2021
Sugar alcohols or polyols are polyhydric alcohols that occur naturally and can be synthetically produced from sugars and resemble sugars in that some exhibit significant sweetness but since they are polyols, they do not have the same incompatibilities as reducing sugars. They are also non-cariogenic and have a much lower glycemic index than sugar. These compounds are used in food products, confections, and pharmaceuticals. Most are available in different particle size grades in crystalline as well as granular form. As most manufacturers prefer to manufacture tablets by direct compression whenever possible, these products are positioned for direct compression applications through wet granulation of the sugar alcohols is not uncommon. In studying the granulation performance of three sugar alcohols – mannitol, sorbitol, and xylitol – in different amounts as compared to sucrose, researchers found that the increased viscosity of the liquid bridges formed, as a result of the partial dissolution of the sugars, strongly contributed to the agglomeration process. The viscosity influenced the liquid mobility and distribution of the solution. As with any soluble filler-diluent-binder, its solubility in the granulating fluid (typically water) is expected to have some influence in the process (visible in torque rheometry measurements) and the outcome of granule and tablet properties.
Introduction to Bioresponsive Polymers
Published in Deepa H. Patel, Bioresponsive Polymers, 2020
Deepa H. Patel, Drashti Pathak, Neelang Trivedi
Other approach includes polymers with phenylboronic groups and polyol polymers that form a gel through complex formation between the pendant phenyl borate and hydroxyl groups [136]. Instead of polyol polymers, short molecules such as diglucosylhexadiamine have been used. As the glucose concentration increases, the cross-linking density of the gel decreases and as a result insulin is released from the eroded gel. The glucose exchange reaction is reversible and reformation of the gel occurs as a result of borate-polyol cross-linking. The major limitation of this system is the low specificity of PBA-containing polymers [137].
Peripheral Mechanisms of Mammalian Sweet Taste
Published in Robert H. Cagan, Neural Mechanisms in Taste, 2020
William Jakinovich, Dorothy Sugarman
Based on whole nerve electrophysiological experiments with the rat, hamster,10 and gerbil,4 there appears to be a correspondence between polyol chain length and the stimulating effectiveness of linear polyols. In the gerbil, the effectiveness of the linear polyol increases with the chain length up to five carbons and then levels off.
Diabetic eye: associated diseases, drugs in clinic, and role of self-assembled carriers in topical treatment
Published in Expert Opinion on Drug Delivery, 2021
Axel Kattar, Angel Concheiro, Carmen Alvarez-Lorenzo
Hyperglycemia is also responsible for triggering the polyol pathway. Under normoglycemic conditions, the Embden–Meyerhof–Parnas catabolism route that transforms glucose into pyruvate, NADH, and ATP becomes saturated. Consequently, the polyol pathway, which commonly transforms 3% glucose, enters into action with the participation of two enzymes: (i) aldose reductase that transforms glucose into sorbitol with the consumption of NADPH and (ii) sorbitol dehydrogenase that slowly converts sorbitol into fructose while consuming NAD+. The polyol pathway, which is very active in retina and lens, metabolizes more than 30% glucose under diabetic conditions [73]. Accumulation of sorbitol causes osmotic stress, triggers leukocyte accumulation, disrupts blood-retinal barrier, favors cells apoptosis, and starts a cascade of oxidative stress-mediated reactions [74]. The excess of fructose acts as precursor of advanced glycation-end products (AGEs). In this context, aldose reductase inhibitors are gaining increased attention, and epalrestat is approved in some countries for oral administration. As an alternative, drugs that accelerate the metabolic rate of sorbitol dehydrogenase and, thus, decrease the levels of sorbitol are being tested [73].
Multivariate analysis in the development of bioequivalent tablets containing bicalutamide
Published in Pharmaceutical Development and Technology, 2021
Roman Goněc, Aleš Franc, Petr Doležel, Pavel Farkaš, Petr Sova
Various excipients can be used to increase the solubility, for instance, cyclodextrines form a soluble complex with bicalutamide (Patil et al. 2009). Furthermore, hydrophillic carriers of polyol character can be used; the most common is lactose (Ortega and Esco 2004), rarely polyethylenglycols (Szafraniec et al. 2018), poloxamers (Bohr et al. 2019) or mesoporous silica (Saroj and Rajput 2019). However, lactose does not create independent capillary structure in tablets and natural porosity decreases with the increasing radial hardness of tablets. Moreover, if the tablet contains also micronized particles of substance that is insoluble in water, the micropores are obstructed and dissolution is decreased. This may be improved by compressing the tablets with very low hardness (Juppo 1996). This can be the reason why generic bicalutamide tablets containing micronised bicalutamide and lactose exhibit satisfactory dissolution profile in low radial hardness only (Ortega and Esco 2004). However, such value of hardness may cause problems, e.g. during tablet coating or packaging. When using microcrystalline cellulose instead of lactose in combination with supersdisintegrants in the formulation, these disadvantages do not occur (Franc et al. 2008).
Effects of xylitol and erythritol consumption on mutans streptococci and the oral microbiota: a systematic review
Published in Acta Odontologica Scandinavica, 2020
Eva Söderling, Kaisu Pienihäkkinen
Prospective randomized controlled clinical trials (RCTs) conducted in healthy subjects were included in the review. The literature review includes literature from 20 years and started from the year 2000 since studies published before that are unlikely to meet the present standards of RCTs. The aims of the included trials were to study effects of xylitol or erythritol consumption on oral counts of MS and/or the composition of the oral microbiota. MS/the microbiota were either the primary or secondary outcome measures in the included studies. Ten oral microbial species was considered the minimum number of microbes to represent oral microbiota. Only studies in which chewing gums or candies (including pastilles/tablets/gummy bears) were the xylitol/erythritol vehicles were included in the review. The comparison was a polyol gum or candy or no product. Xylitol/erythritol should be the polyol with the highest concentration in the tested product to meet with the inclusion criteria.