A physically stabilized amorphous solid dispersion of nisoldipine obtained by hot melt extrusion

Fu, Qiang; Fang, Mingming; Hou, Yanxian; Yang, Wenqian; Guo, Meng; Li, Mo; Li, Jingru; Wang, Yongjun; Zhang, He; Sun, Jin

doi:10.1016/j.powtec.2016.06.032

Cited by 21 publications

(5 citation statements)

References 15 publications

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“…The in-vitro release characteristics and in-vivo performance of the final formulation were compared with Nierxin, a commercial tablet formulation. The results indicate that the developed ASD performed on par with the commercially available formulation 23 .…”

Section: Hot Melt Extrusionmentioning

confidence: 84%

Approaches to Improve Oral Bioavailability of Antihypertensive Drugs: A Mini-Review

Dole,

Kothapally,

Chukkala

et al. 2023

J. Drug Delivery Ther.

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Hypertension elevates the risk of heart disease and stroke which are one of the most frequent causes of death. Fortunately, hypertension is manageable with the use of anti-hypertensives and a healthy lifestyle. However, patient non-adherence to the prescribed dosing regimen is the primary reason for uncontrolled blood pressure levels. Daily multiple doses of medication are one of the major reasons for patient non-compliance to the dosing regimen. Multiple doses of medication are a result of low solubility and high first-pass metabolism of anti-hypertensives. There are several approaches to improve the bioavailability of anti-hypertensives like polymeric and non-polymeric approaches to enhance solubility, avoiding first-pass metabolism through alternate routes of drug delivery and others. The objective of this review is to discuss different approaches to enhance the oral bioavailability of anti-hypertensive drugs. Keywords: Solubility enhancements, solid lipid nanoparticles, hot melt extrusion, drug delivery, pharmacokinetics, poorly soluble, oral bioavailability.

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Section: Hot Melt Extrusionmentioning

confidence: 84%

Approaches to Improve Oral Bioavailability of Antihypertensive Drugs: A Mini-Review

Dole,

Kothapally,

Chukkala

et al. 2023

J. Drug Delivery Ther.

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“…Similarly, Fu et al (2016) prepared an amorphous solid dispersion of nisoldipine (M.P = 151 °C) in Kollidon® VA64 at an extrusion temperature of 153 °C and ratio of 1:10 to improve the solubility and stability of the amorphous dispersion. Among the various formulations, the maximum dissolution (100% after 1 h) was achieved at a ratio between the drug and polymer equal to 1:10.…”

Section: Role Of Polymers In Solubilizationmentioning

confidence: 99%

“…Approximately 56% of all the HME-related patents were issued in the United States or Germany (Wilson et al, 2012). Various HME products available in the market were developed for oral delivery, the enhancement of solubility and bioavailability of poorly soluble drugs, immediate release (Dierickx et al, 2012; Fu et al, 2016), sustained and controlled release (Almeida et al, 2011; Ma et al, 2013), taste masking (Gryczke et al, 2011), enteric release (Schilling et al, 2010), targeted release products, implants (Johnson et al, 2010), and ocular inserts (Balguri et al, 2017).…”

Section: Marketed Productsmentioning

confidence: 99%

Melt extrusion with poorly soluble drugs – An integrated review

Repka

Bandari

Kallakunta

et al. 2018

International Journal of Pharmaceutics

177

108

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Over the last few decades, hot melt extrusion (HME) has emerged as a successful technology for a broad spectrum of applications in the pharmaceutical industry. As indicated by multiple publications and patents, HME is mainly used for the enhancement of solubility and bioavailability of poorly soluble drugs. This review is focused on the recent reports on the solubility enhancement via HME and provides an update for the manufacturing/scaling up aspects of melt extrusion. In addition, drug characterization methods and dissolution studies are discussed. The application of process analytical technology (PAT) tools and use of HME as a continuous manufacturing process may shorten the drug development process; as a result, the latter is becoming the most widely utilized technique in the pharmaceutical industry. The advantages, disadvantages, and practical applications of various PAT tools such as near and mid-infrared, ultraviolet/visible, fluorescence, and Raman spectroscopies are summarized, and the characteristics of other techniques are briefly discussed. Overall, this review also provides an outline for the currently marketed products and analyzes the strengths, weaknesses, opportunities and threats of HME application in the pharmaceutical industry.

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“…These two observations suggest that the FFF printing process is unlikely to alter the drug release properties or cause degradation of the drug, while the surface-to-volume ratio plays an important role in influencing the release behaviors. In addition, due to the significant advantages of the HME technology in enhancing drug solubility and bioavailability, HME-based products can also be used directly as oral drug release carriers, , such as controlled release, − immediate release, , intragastric or enteric release, etc. In this context, understanding the underlying drug release mechanisms of both HME filaments and FFF-printed products is essential for better designing of new controlled drug delivery systems.…”

Section: Introductionmentioning

confidence: 99%

Phase-Field Model for Drug Release of Water-Swellable Filaments for Fused Filament Fabrication

Zhu

Yang

et al. 2022

Mol. Pharmaceutics

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This paper treats the drug release process as a phase-field problem and a phase-field model capable of simulating the dynamics of multiple moving fronts, transient drug fluxes, and fractional drug release from swellable polymeric systems is proposed and validated experimentally. The model can not only capture accurately the positions and movements of the distinct fronts without tracking the locations of fronts explicitly but also predict well the release profile to the completion of the release process. The parametric study has shown that parameters including water diffusion coefficient, drug saturation solubility, drug diffusion coefficient, initial drug loading ratio, and initial porosity are critical in regulating the drug release kinetics. It has been also demonstrated that the model can be applied to the study of swellable filaments and has wide applicability for different materials. Due to explicit boundary position tracking being eliminated, the model paves the way for practical use and can be extended for dealing with geometrically complex drug delivery systems. It is a useful tool to guide the design of new controlled delivery systems fabricated by fused filament fabrication.

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A physically stabilized amorphous solid dispersion of nisoldipine obtained by hot melt extrusion

Cited by 21 publications

References 15 publications

Approaches to Improve Oral Bioavailability of Antihypertensive Drugs: A Mini-Review

Approaches to Improve Oral Bioavailability of Antihypertensive Drugs: A Mini-Review

Melt extrusion with poorly soluble drugs – An integrated review

Phase-Field Model for Drug Release of Water-Swellable Filaments for Fused Filament Fabrication

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