A donepezil/cyclodextrin complexation orodispersible film: Effect of cyclodextrin on taste-masking based on dynamic process and in vivo drug absorption

Liu, Tingting; Wan, Xiaocao; Luo, Zheng; Liu, Chao; Quan, Peng; Cun, Dongmei; Fang, Liang

doi:10.1016/j.ajps.2018.05.001

Cited by 43 publications

(26 citation statements)

References 27 publications

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“…Based on information from the literature on highly water-soluble and small molecules encapsulating using DESE [ 9 , 10 , 11 , 12 , 19 , 20 , 21 , 22 , 23 , 24 , 25 ], the factors affecting microparticle preparation (i.e., materials, environment, double emulsion preparation condition, and solvent evaporation condition) were determined, as illustrated in the fishbone (Ishikawa) diagram in Figure 2 .…”

Section: Resultsmentioning

confidence: 99%

Optimized Taste-Masked Microparticles for Orally Disintegrating Tablets as a Promising Dosage Form for Alzheimer’s Disease Patients

et al. 2021

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The objective of this research was to optimize the tasted-masked microparticles for orally disintegrating tablets containing donepezil hydrochloride using quality risk assessment and design of experiment approaches. The double emulsion solvent evaporation technique using aminoalkyl methacrylate copolymer (AMC) was used to prepare taste-masked microparticles. Factors affecting the quality of the taste-masked microparticles were analyzed using an Ishikawa diagram. A risk-ranking approach was used to rank the formulation and process risks. Furthermore, the effect of AMC quantity, stirring time, and volume of outer water phase on various responses, such as particle size, the amount of drug dissolved at 5 min (Q5) in simulated saliva fluid, and mean dissolution time (MDT) in simulated gastric fluid, was investigated using the Box-Behnken design. The optimized microparticles were then used to prepare orally disintegrating tablets (ODTs) and evaluated by in vitro and in vivo testing. The results demonstrated that particle size was influenced by the AMC amount and stirring time. Q5 was significantly affected by the amount of AMC and the volume of the outer water phase. On the other hand, these two factors had a positive effect on MDT. The optimized microparticles had a particle size of 174.45 ± 18.19 µm, Q5 of 5.04%, and MDT of 5.97 min. The ODTs with taste-masked microparticles showed acceptable in vitro dissolution with an MDT of 5 min. According to the results of a panel of six human volunteers, they greatly improved palatability.

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Section: Resultsmentioning

confidence: 99%

Optimized Taste-Masked Microparticles for Orally Disintegrating Tablets as a Promising Dosage Form for Alzheimer’s Disease Patients

et al. 2021

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“…Moreover, CD systems identified in this work may be of additional value for diastereomers separation [ 11 ], solid-state chemical stabilization under certain conditions [ 7 ] and bitter taste masking [ 12 , 13 ].…”

Section: Discussionmentioning

confidence: 99%

“…The separation of diastereomers, affecting the bioactivity of CA, may be achieved by the application of CDs [ 11 ]. CDs as multifunctional excipients may be also used for taste masking [ 12 , 13 , 14 ], which is especially important to improve the comfort of patients taking bitter drugs such as β-lactam antibiotics.…”

Section: Introductionmentioning

confidence: 99%

Computer-Aided Discovery of New Solubility-Enhancing Drug Delivery System

et al. 2020

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The poor aqueous solubility of active pharmaceutical ingredients (APIs) places a limit on their therapeutic potential. Cyclodextrins (CDs) have been shown to improve the solubility of APIs, but the magnitude of the improvement depends on the structure of both the CDs and APIs. We have developed quantitative structure–property relationship (QSPR) models that predict the stability of the complexes formed by a popular poorly soluble antibiotic, cefuroxime axetil (CA) and different CDs. We applied this model to five CA–CD systems not included in the modeling set. Two out of three systems predicted to have poor stability and poor CA solubility, and both CA–CD systems predicted to have high stability and high CA solubility were confirmed experimentally. One of the CDs that significantly improved CA solubility, methyl-βCD, is described here for the first time, and we propose this CD as a novel promising excipient. Computational approaches and models developed and validated in this study could help accelerate the development of multifunctional CDs-based formulations.

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“…23 Mucoadhesive buccal films are pharmaceutical dosage form that utilizes a water-dissolving polymer to allow the prepared films to quickly hydrate, adhere and dissolve when placed in the buccal, palatal, gingival, lingual, sublingual or cheek mucosa of the buccal cavity. 24,25 They are promising drug delivery that release their drug content directly toward the buccal mucosa with subsequent drug absorption through the venous blood system that drains from the cheek. Accordingly, development of these films has the advantage of avoiding the extensive liver metabolism that are common with orally administered medications.…”

Section: Introductionmentioning

confidence: 99%

<p>Enhancement of Simvastatin ex vivo Permeation from Mucoadhesive Buccal Films Loaded with Dual Drug Release Carriers</p>

Ahmed¹,

Bawazir²,

Alharbi³

2020

IJN

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Background: Simvastatin (SMV), a hypocholesterolemic agent, suffers from very low bioavailability due to its poor aqueous solubility and extensive first-pass metabolism. Methods: Two SMV carrier systems, namely, polymeric drug inclusion complex (IC) and mixed micelles (MM) nanoparticles, were developed and loaded into mucoadhesive buccal films to enhance SMV bioavailability. The two carrier systems were characterized and their permeation across human oral epithelial cells (OEC) was studied. The effect of IC to MM ratio (X 1 ) and the mucoadhesive polymer concentration (X 2 ) on the cumulative percent of drug released, elongation percent and the mucoadhesive strength, from the prepared mucoadhesive films, were optimized. Ex vivo permeation across bovine mucosal tissue was investigated. The permeation parameters for the in vitro and ex vivo release data were calculated. Results: Complexation of SMV with hydroxypropyl beta-cyclodextrin (HP β-CD) was superior to all other polymers as revealed by the equilibrium saturation solubility, stability constant, complexation efficiency and thermodynamic potential. SMV-HP β-CD IC was utilized to develop a saturated polymeric drug solution. Both carrier systems showed enhanced permeation across OEC when compared to pure drug. X 1 and X 2 were significantly affecting the characteristics of the prepared films. The optimized mucoadhesive buccal film formulation loaded with SMV IC and drug MM nanoparticles demonstrated superior ex vivo permeation when compared to the corresponding pure drug buccal film, and the calculated permeation parameters confirmed this finding. Conclusion: Mucoadhesive buccal films containing SMV IC and drug MM can be used to improve drug bioavailability; however, additional pharmacokinetic and pharmacodynamic studies are required.

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A donepezil/cyclodextrin complexation orodispersible film: Effect of cyclodextrin on taste-masking based on dynamic process and in vivo drug absorption

Cited by 43 publications

References 27 publications

Optimized Taste-Masked Microparticles for Orally Disintegrating Tablets as a Promising Dosage Form for Alzheimer’s Disease Patients

Optimized Taste-Masked Microparticles for Orally Disintegrating Tablets as a Promising Dosage Form for Alzheimer’s Disease Patients

Computer-Aided Discovery of New Solubility-Enhancing Drug Delivery System

<p>Enhancement of Simvastatin ex vivo Permeation from Mucoadhesive Buccal Films Loaded with Dual Drug Release Carriers</p>

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