Thermodynamics of paracetamol solubility in sugar-water cosolvent systems

Etman, M.; Naggar, Viviane F.

doi:10.1016/0378-5173(90)90193-8

Cited by 30 publications

(20 citation statements)

References 14 publications

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“…Mannitol containing formulations had lower EE values than Aerosil containing ones. This might be due to the possible RC salting out by the high mannitol concentrations incorporated into the IFN formulations [54]. Similar results were observed by Huang et al while investigating the effect of mannitol on the encapsulation efficiency of Calcein in liposomes [46].…”

Section: Resultssupporting

confidence: 61%

Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System

et al. 2019

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In situ forming nanovesicular systems (IFNs) were prepared and optimized to improve Rosuvastatin calcium (RC) oral bioavailability through increasing its solubility and dissolution rate. The IFN was composed of Tween® 80 (T80), cetyl alcohol (CA), in addition to mannitol or Aerosil 200. A single simple step was adopted for preparation, then the prepared formulations were investigated by analyzing their particle size (PS), polydispersity index (PDI), Zeta potential (ZP), entrapment efficiency (EE), and flowability properties. D-optimal design was applied to choose the optimized formulations. The maximum desirability values were 0.754 and 0.478 for the optimized formulations containing 0.05 g CA, 0.18 g T80, and 0.5 g mannitol (OFM) or Aerosil (OFA), respectively. In vitro drug release from the optimized formulations showed a significantly faster dissolution rate when compared to the market product. In vivo performance of the optimized formulations in rabbits was investigated after filling them into enteric-coated capsules. Ultimately, OFA formulation achieved a 3 times increase in RC oral bioavailability in comparison with the market product, supporting the hypothesis of considering IFNs as promising nanocarriers able to boost the bioavailability of BCS class II drugs.

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Section: Resultssupporting

confidence: 61%

Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System

et al. 2019

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“…[14] Solubility One part of acetaminophen is soluble in 70 parts of water at room temperature [15], [16] and soluble 1 in 20 parts in boiling water. [4], [15] Other sources report an aqueous solubility of 14.7 mg/mL at 20°C, [17] 14.3 mg/mL at 25°C, [18] and 23.7 mg/mL at 37°C. [17] Partition Coefficient A logP (n-octanol/water) value of 0.2 has been measured.…”

Section: Introductionmentioning

confidence: 99%

“…[4], [15] Other sources report an aqueous solubility of 14.7 mg/mL at 20°C, [17] 14.3 mg/mL at 25°C, [18] and 23.7 mg/mL at 37°C. [17] Partition Coefficient A logP (n-octanol/water) value of 0.2 has been measured. [19] Calculations using fragmentation methods based on atomic contributions to lipophilicity and by using the ClogP program (version 3.0, Biobyte Corp., Claremont, CA) gave values of 0.31(log P), [20] 0.49(ClogP), [21] and 0.89(log P).…”

Section: Introductionmentioning

confidence: 99%

Biowaiver monographs for immediate release solid oral dosage forms: Acetaminophen (paracetamol)

Kalantzi

Reppas

Dressman

et al. 2006

Journal of Pharmaceutical Sciences

151

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Literature data are reviewed on the properties of acetaminophen (paracetamol) related to the biopharmaceutics classification system (BCS). According to the current BCS criteria, acetaminophen is BCS Class III compound. Differences in composition seldom, if ever, have an effect on the extent of absorption. However, some studies show differences in rate of absorption between brands and formulations. In particular, sodium bicarbonate, present in some drug products, was reported to give an increase in the rate of absorption, probably caused by an effect on gastric emptying. In view of Marketing Authorizations (MAs) given in a number of countries to acetaminophen drug products with rapid onset of action, it is concluded that differences in rate of absorption were considered therapeutically not relevant by the Health Authorities. Moreover, in view of its therapeutic use, its wide therapeutic index and its uncomplicated pharmacokinetic properties, in vitro dissolution data collected according to the relevant Guidances can be safely used for declaring bioequivalence (BE) of two acetaminophen formulations. Therefore, accepting a biowaiver for immediate release (IR) acetaminophen solid oral drug products is considered scientifically justified, if the test product contains only those excipients reported in this paper in their usual amounts and the test product is rapidly dissolving, as well as the test product fulfils the criterion of similarity of dissolution profiles to the reference product.

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“…Sugars are understood to create order within an aqueous solution, and that there can be a “sugaring out” effect on aromatic organic molecules [32]–[34]. If an excipient, such as sucrose, were to decrease the aqueous solubility of t RES, its inclusion in an OTM dosage would slow absorption across the oral mucosa.…”

Section: Discussionmentioning

confidence: 99%

Development of a Lozenge for Oral Transmucosal Delivery of Trans-Resveratrol in Humans: Proof of Concept

Blanchard¹,

Friesenhahn

Javors

et al. 2014

PLoS ONE

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Resveratrol provides multiple physiologic benefits which promote healthspan in various model species and clinical trials support continued exploration of resveratrol treatment in humans. However, there remains concern regarding low bioavailability and wide inter-individual differences in absorption and metabolism in humans, which suggests a great need to develop novel methods for resveratrol delivery. We hypothesized that oral transmucosal delivery, using a lozenge composed of a resveratrol-excipient matrix, would allow resveratrol to be absorbed rapidly into the bloodstream. We pursued proof of concept through two experiments. In the first experiment, the solubility of trans-resveratrol (tRES) in water and 2.0 M solutions of dextrose, fructose, ribose, sucrose, and xylitol was determined using HPLC. Independent t-tests with a Bonferroni correction were used to compare the solubility of tRES in each of the solutions to that in water. tRES was significantly more soluble in the ribose solution (p = 0.0013) than in the other four solutions. Given the enhanced solubility of tRES in a ribose solution, a resveratrol-ribose matrix was developed into a lozenge suitable for human consumption. Lozenges were prepared, each containing 146±5.5 mg tRES per 2000 mg of lozenge mass. Two healthy human participants consumed one of the prepared lozenges following an overnight fast. Venipuncture was performed immediately before and 15, 30, 45, and 60 minutes following lozenge administration. Maximal plasma concentrations (C max) for tRES alone (i.e., resveratrol metabolites not included) were 325 and 332 ng⋅mL−1 for the two participants at 15 minute post-administration for both individuals. These results suggest a resveratrol-ribose matrix lozenge can achieve greater C max and enter the bloodstream faster than previously reported dosage forms for gastrointestinal absorption. While this study is limited by small sample size and only one method of resveratrol delivery, it does provide proof of concept to support further exploration of novel delivery methods for resveratrol administration.

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Thermodynamics of paracetamol solubility in sugar-water cosolvent systems

Cited by 30 publications

References 14 publications

Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System

Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System

Biowaiver monographs for immediate release solid oral dosage forms: Acetaminophen (paracetamol)

Development of a Lozenge for Oral Transmucosal Delivery of Trans-Resveratrol in Humans: Proof of Concept

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