Effect of surfactant on the in vitro dissolution and the oral bioavailability of a weakly basic drug from an amorphous solid dispersion

Tung, Nguyen-Thach; Tran, Cao-Son; Nguyen, Tran-Linh; Pham, Thi-Minh-Hue; Chi, Sang-Cheol; Nguyen, Hoang-Anh; Bui, Quang-Dong; Bui, Duc-Nhat; Tran, Thi-Quyen

doi:10.1016/j.ejps.2021.105836

Cited by 20 publications

(18 citation statements)

References 34 publications

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“…The SMEDDS improved the oral bioavailability of THP in a rabbit model by 198.63% ( Tung et al, 2018 ) and in a rat model by 225% ( Li et al, 2021 ) compared with THP suspension. The figures for self-emulsifying drug-delivery systems were 33.2% in a rat model ( Ma et al, 2012 ) and 234.77% for binary amorphous solid dispersion application in rabbit plasma ( Tung et al, 2021 ). Another method for increasing THP bioavailability is the use of hydrochloride freeze-dried powder, in which C-max, AUC, and bioavailability are significantly elevated ( Wu C. et al, 2013 ).…”

Section: Pharmacokinetic Characteristicsmentioning

confidence: 99%

A Comprehensive Review on the Chemical Properties, Plant Sources, Pharmacological Activities, Pharmacokinetic and Toxicological Characteristics of Tetrahydropalmatine

Meng

Wang

2022

Front. Pharmacol.

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Tetrahydropalmatine (THP), a tetrahydroproberine isoquinoline alkaloid, is widely present in some botanical drugs, such as Stephania epigaea H.S. Lo (Menispermaceae; Radix stephaniae epigaeae), Corydalis yanhusuo (Y.H.Chou & Chun C.Hsu) W.T. Wang ex Z.Y. Su and C.Y. Wu (Papaveraceae; Corydalis rhizoma), and Phellodendron chinense C.K.Schneid (Berberidaceae; Phellodendri chinensis cortex). THP has attracted considerable attention because of its diverse pharmacological activities. In this review, the chemical properties, plant sources, pharmacological activities, pharmacokinetic and toxicological characteristics of THP were systematically summarized for the first time. The results indicated that THP mainly existed in Papaveraceae and Menispermaceae families. Its pharmacological activities include anti-addiction, anti-inflammatory, analgesic, neuroprotective, and antitumor effects. Pharmacokinetic studies showed that THP was inadequately absorbed in the intestine and had rapid clearance and low bioavailability in vivo, as well as self-microemulsifying drug delivery systems, which could increase the absorption level and absorption rate of THP and improve its bioavailability. In addition, THP may have potential cardiac and neurological toxicity, but toxicity studies of THP are limited, especially its long-duration and acute toxicity tests. In summary, THP, as a natural alkaloid, has application prospects and potential development value, which is promising to be a novel drug for the treatment of pain, inflammation, and other related diseases. Further research on its potential target, molecular mechanism, toxicity, and oral utilization should need to be strengthened in the future.

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Section: Pharmacokinetic Characteristicsmentioning

confidence: 99%

A Comprehensive Review on the Chemical Properties, Plant Sources, Pharmacological Activities, Pharmacokinetic and Toxicological Characteristics of Tetrahydropalmatine

Meng

Wang

2022

Front. Pharmacol.

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“…rug dissolution refers to the rate and extent of drug release from solid preparations (such as tablets, capsules, or granules) in a specific medium (1). Because the dissolution rate directly affects the absorption and utilization of drugs in vivo, the dissolution test has become one of the indicators to evaluate the quality of drug production (2)(3)(4). Dissolution is widely used in the development of solid dosage forms, raw materials, and new drugs (5,6).…”

mentioning

confidence: 99%

Predicting Dissolution of Entecavir Using the Noyes Whitney Equation

Kang¹,

Chen²,

Duan³

et al. 2023

Dissolution Technol.

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The dissolution rate of a drug directly affects its absorption and utilization in vivo. The dissolution test is used to evaluate the quality of formulation and production process. Entecavir is approved by the United States FDA for the treatment of chronic hepatitis B. Entecavir monohydrate (ETV-H) is used in commercial ETV tablets. The anhydrous form of entecavir (ETV-A) often appears as an impurity polymorph during the preparation process. This study aims to investigate the dissolution behavior of ETV-H in four dissolution media (water, pH 1.2, pH 4.0, and pH 6.8) and compare with those of ETV-A. The dissolution rates of ETV-H at pH 6.8, pH 4.0, and ultrapure water were faster than those of ETV-A, resulting in faster complete dissolution of ETV-H. To save time in the dissolution testing, an analytical method based on the Noyes Whitney equation is proposed to obtain the fitted (predicted) dissolution curve. Differences (loss values) between the predicted and experimental dissolution curves for ETV-H at pH 6.8 and pH 1.2 were 0.0013 and 0.016, respectively. The proposed analytical method can save up to 75% of experimental time and can be used for dissolution testing of active pharmaceutical ingredients in the production of pharmaceutical crystals.

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“…Thus, the addition of Span 20 in the twin screw extruder was the critical factor for the precipitation behavior. Surfactants with lower hydrophilic–lipophilic balance (HLB) values (e.g., Span 20) have been reported to interfere more with the interaction between the polymeric carrier and the drug, and therefore, could not maintain the supersaturation of the ternary system more effectively than surfactants with higher HLB values (e.g., SDS and Tween 80) [ 46 ]. Nevertheless, Span 20 can generate and stabilize the nanodroplets in the ternary system relative to SDS and Tween 80 [ 32 ].…”

Section: Resultsmentioning

confidence: 99%

Effect of Span 20 Feeding Zone in the Twin Screw Extruder on the Properties of Amorphous Solid Dispersion of Ritonavir

Wang

Zhao

et al. 2023

Pharmaceutics

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A ternary amorphous solid dispersion (ASD) system consisting of drug/polymer/surfactant is receiving increased attention to improve the oral bioavailability of poorly water-soluble drugs. The effect of polymers has been extensively studied, while the impact of surfactants has not yet to be studied to the same extent. Challenging questions to be answered are whether the surfactants should be added with the drug or separately and the resulting differences between the two operating processes. By adjusting the liquid feeding zone for Span 20 in the hot-melt twin screw extruder equipment, we investigated the effect of Span 20 on the properties of the polyvinylpyrrolidone/vinyl acetate (PVPVA)-based ASD formulations of ritonavir. We found that with the delayed feeding positions of Span 20 in the twin screw extruder, the ability of the ternary ASDs to maintain the supersaturation of the milled extrudates was observed to be significantly enhanced. Furthermore, adding surfactant after a thorough mixing of polymer and drug could decrease the molecular mobility of ternary ASD formulations. In addition, the effects of Span 20 on the complex viscosity and structure of PVPVA were also investigated. The delayed addition of Span 20 could improve the complex viscosity of PVPVA, thus leading to the drug precipitation inhibition. In conclusion, the delayed addition of Span 20 in the twin screw extruder and prolonging the mixing time of the drug and polymer may be critical to the maintenance of supersaturation.

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Effect of surfactant on the in vitro dissolution and the oral bioavailability of a weakly basic drug from an amorphous solid dispersion

Cited by 20 publications

References 34 publications

A Comprehensive Review on the Chemical Properties, Plant Sources, Pharmacological Activities, Pharmacokinetic and Toxicological Characteristics of Tetrahydropalmatine

A Comprehensive Review on the Chemical Properties, Plant Sources, Pharmacological Activities, Pharmacokinetic and Toxicological Characteristics of Tetrahydropalmatine

Predicting Dissolution of Entecavir Using the Noyes Whitney Equation

Effect of Span 20 Feeding Zone in the Twin Screw Extruder on the Properties of Amorphous Solid Dispersion of Ritonavir

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