Once Daily, High-Dose Mesalazine Controlled-Release Tablet for Colonic Delivery: Optimization of Formulation Variables Using Box–Behnken Design

El-Bary, A. Abd; Aboelwafa, Ahmed A.; Sharabi, Ibrahim Al

doi:10.1208/s12249-011-9708-9

Cited by 17 publications

(10 citation statements)

References 61 publications

(50 reference statements)

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“…indicating the model ability to navigate the design space with the minimal pure error (Elbary et al, 2011). ANOVA analysis on GS (nm) of ME (Y 1 ) shows that linear mixture components have a significant effect on GS (p value < .05).…”

Section: Evaluation Of the Prepared Mesmentioning

confidence: 99%

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

et al. 2017

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Agomelatine is a new antidepressant having very low oral drug bioavailability less than 5% due to being liable to extensive hepatic 1st pass effect. This study aimed to deliver agomelatine by transdermal route through formulation and optimization of microemulsion gel. Pyramidal screening was performed to select the most suitable ingredients combinations and then, the design expert software was utilized to optimize the microemulsion formulations. The independent variables of the employed mixture design were the percentages of capryol 90 as an oily phase (X 1 ), Cremophor RH40 and Transcutol HP in a ratio of (1:2) as surfactant/cosurfactant mixture 'S mix ' (X 2 ) and water (X 3 ). The dependent variables were globule size, optical clarity, cumulative amount permeated after 1 and 24 h, respectively (Q1 and Q 24 ) and enhancement ratio (ER). The optimized formula was composed of 5% oil, 45% S mix and 50% water. The optimized microemulsion formula was converted into carbopol-based gel to improve its retention on the skin. It enhanced the drug permeation through rat skin with an enhancement ratio of 37.30 when compared to the drug hydrogel. The optimum ME gel formula was found to have significantly higher C max , AUC 0-24 h and AUC 0-1 than that of the reference agomelatine hydrogel and oral solution. This could reveal the prosperity of the optimized microemulsion gel formula to augment the transdermal bioavailability of agomelatine. ARTICLE HISTORY

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Section: Evaluation Of the Prepared Mesmentioning

confidence: 99%

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

et al. 2017

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“…In polynomial equation, Y means the response value (contents of mark ingredients), while the X 1 , X 2 and X 3 represent, respectively, three factors which could influence on the decocting process (soaking time, decocting pressure, and water volume). Terms composed of two factors represent the interaction terms, and terms with second-order factors indicate the nonlinear nature of the relationship between the responses and the factors [11] , [12] . A positive sign indicates a synergistic effect, while a negative sign represents an antagonistic effect.…”

Section: Resultsmentioning

confidence: 99%

Optimization of high pressure machine decocting process for Dachengqi Tang using HPLC fingerprints combined with the Box–Behnken experimental design

Xie

Shi

et al. 2015

Journal of Pharmaceutical Analysis

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Using Dachengqi Tang (DCQT) as a model, high performance liquid chromatography (HPLC) fingerprints were applied to optimize machine extracting process with the Box–Behnken experimental design. HPLC fingerprints were carried out to investigate the chemical ingredients of DCQT; synthetic weighing method based on analytic hierarchy process (AHP) and criteria importance through intercriteria correlation (CRITIC) was performed to calculate synthetic scores of fingerprints; using the mark ingredients contents and synthetic scores as indicators, the Box–Behnken design was carried out to optimize the process parameters of machine decocting process under high pressure for DCQT. Results of optimal process showed that the herb materials were soaked for 45 min and extracted with 9 folds volume of water in the decocting machine under the temperature of 140 °C till the pressure arrived at 0.25 MPa; then hot decoction was excreted to soak Dahuang and Mangxiao for 5 min. Finally, obtained solutions were mixed, filtrated and packed. It concluded that HPLC fingerprints combined with the Box–Behnken experimental design could be used to optimize extracting process of traditional Chinese medicine (TCM).

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“…24 Talc was added in the coating solution in half the amount of plasticizer. 25 The initial three formulations were subjected to dissolution tests and values of P1 and P2 were recorded. The responses of the parameters were then normalized and overall responses were calculated.…”

Section: Discussionmentioning

confidence: 99%

Formulation and Optimization of Controlled Release 5-Fluorouracil Tablets for Colonic Delivery

Das¹,

Ghosh²,

Sen³

et al. 2017

JYP

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Objective: Formulations were developed for targeted controlled delivery of 5-fluorouracil at the colonic site. Methods: Probable dose for drug loading in the tablets and duration of drug release at the colon was determined. Core tablets were formulated with an aim to deliver the drug at a constant rate following zero order kinetics throughout the duration of release. Hydroxypropyl methylcellulose E15 and potassium chloride were incorporated as hydrophilic agents in the core matrix for drug release at the desired level and the formulation with the best release profile was chosen for coating with a coating solution containing Eudragit S100, polyethylene glycol 400 and talc. The amounts of Eudragit S100 and weight gain of the tablet were optimized using sequential simplex optimization method. Results: The optimized coated formulation (0.6875 g of Eudragit S100; 7.5% weight gain) was able to provide minimum drug release in the 5 hr lag time (5.9% of cumulative release) and an average release rate of 19.8% per hr thereafter. Conclusion: The optimized formulation for 5-Fluorouracil delivery at the colonic site was able to achieve a sufficient lag time and controlled drug release and can be highly beneficial for optimum therapeutic activity and negligible side effects when administered orally.

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Once Daily, High-Dose Mesalazine Controlled-Release Tablet for Colonic Delivery: Optimization of Formulation Variables Using Box–Behnken Design

Cited by 17 publications

References 61 publications

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

Transdermal agomelatine microemulsion gel: pyramidal screening, statistical optimization and in vivo bioavailability

Optimization of high pressure machine decocting process for Dachengqi Tang using HPLC fingerprints combined with the Box–Behnken experimental design

Formulation and Optimization of Controlled Release 5-Fluorouracil Tablets for Colonic Delivery

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