Preparation and Evaluation of Novel Directly-Compressed Fast-Disintegrating Furosemide Tablets with Sucrose Stearic Acid Ester

Koseki, Takuma; Onishi, Hiraku; Uchida, Minoru; Machida, Yoshiharu

doi:10.1248/bpb.32.1126

Cited by 6 publications

(2 citation statements)

References 29 publications

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“…Previous research showed that the addition of SEs with high HLB values shortened tablet disintegration time, 17) and SEs with high HLB values slowed the disintegration process. 31,32) In addition, the method for manufacturing the diluent used in the tablets has been reported to affect disintegration time, 18) and there are reports that SEs absorb water and form a gel. 33,34) Based on these reports, in the present study we assumed that the addition of SEs with high HLB values slowed disintegration because the compression pressure was approximately double that utilized to manufacture tablets in the reports by Yamamoto et al and Hayashi et al 17,18) Further, along with tablet hardness, the pores on the surface of the tablets were made smaller, which prevented water permeation.…”

Section: Effects Of Se As An Additive On Tablet Propertiesmentioning

confidence: 99%

Evaluation of Sucrose Fatty Acid Esters as Lubricants in Tablet Manufacturing

Nakamura

Ishii

Nakashima

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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Lubricants are essential additives in tablet formulations. Magnesium stearate (Mg-St) is the most commonly used lubricant in tableting. Here, we used sucrose fatty acid ester (SE) as an additive to manufacture tablets by direct compression. We evaluated the effects of hydrophile-lipophile balance (HLB) and the amount of SE on the flowability of a pharmaceutical powder using angle of repose and practical angle of internal friction measurements. In addition, we investigated the effects of SE on tablet properties. When SEs with an HLB ≥3 were added, the angle of repose was approximately the same as that of a pharmaceutical powder containing Mg-St, with no major differences in flowability. However, the practical angle of internal friction became closer to pharmaceutical powder containing Mg-St as HLB decreased. As HLB increased, the practical angle of internal friction approached the value of additive-free pharmaceutical powder. Tablets containing 2.0% Mg-St had a mean hardness of 40 N and disintegrated in approximately 6 min, whereas tablets containing 2.0% SE (low HLB) had a mean hardness of approximately ≥80 N and disintegrated within 3 min. The results indicate that SEs can be used as lubricants in tablet production by direct compression and to reduce problems associated with the use of Mg-St. In particular, we suggest that SEs with low HLB values can be used as excipients to achieve high tablet hardness and short disintegration time.

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Section: Effects Of Se As An Additive On Tablet Propertiesmentioning

confidence: 99%

Evaluation of Sucrose Fatty Acid Esters as Lubricants in Tablet Manufacturing

Nakamura

Ishii

Nakashima

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Esters are valuable and provide useful applications as flavor and fragrance compounds in cosmetics, beverages, food, coating, and adhesive industries . Esters also have diversified application as solvents and intermediates, plasticizers used in polymer industries, medicinal agents, and in drug delivery . The catalysts used for the synthesis of esters are either homogeneous or heterogeneous.…”

Section: Introductionmentioning

confidence: 99%

Kinetics, mass transfer, and thermodynamic and statistical modeling study for esterification of valeric acid with n‐butanol: Homogeneous and heterogeneous catalysis

Khudsange

Wasewar

2018

Int J of Chemical Kinetics

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The esterification of valeric acid with n-butanol was studied with homogeneous and heterogeneous catalysts. The activity and performance of homogeneous ptoluenesulfonic acid and heterogeneous cation exchange resin catalysts Amberlyst 36, Indion 190, and Amberlite IRC-50 were evaluated. The pseudo-homogeneous kinetic model was used to investigate the kinetic parameters of homogeneous-and heterogeneous-catalyzed esterification. The UNIFAC (universal functional activity coefficient) approach was used to study the nonideality of the esterification reaction.The reaction was statistically modeled and optimized by the application of response surface methodology. The effects of independent variables such as reaction temperature, initial molar ratio, and catalyst loading on the conversion of valeric acid were investigated. The optimized conditions for the esterification reaction catalyzed by Amberlyst-36 were found as temperature 360.4 K, initial molar ratio 3.8, and catalyst loading 6.7 wt%. The predicted conversion (89%) at these optimized conditions is in good agreement with the experimental conversion (87.3 ± 1.6%). K E Y W O R D Sesterification, ion exchange resins, kinetics, p-toluenesulfonic acid, response surface methodology, UNI-FAC Int J Chem Kinet. 2018;50:710-725.wileyonlinelibrary.com/journal/kin

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Sugar Fatty Acid Esters

Zheng

et al. 2015

Polar Lipids

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Preparation and Evaluation of Novel Directly-Compressed Fast-Disintegrating Furosemide Tablets with Sucrose Stearic Acid Ester

Cited by 6 publications

References 29 publications

Evaluation of Sucrose Fatty Acid Esters as Lubricants in Tablet Manufacturing

Evaluation of Sucrose Fatty Acid Esters as Lubricants in Tablet Manufacturing

Kinetics, mass transfer, and thermodynamic and statistical modeling study for esterification of valeric acid with n‐butanol: Homogeneous and heterogeneous catalysis

Sugar Fatty Acid Esters

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