Hot-Melt Extruded Amorphous Solid Dispersion for Solubility, Stability, and Bioavailability Enhancement of Telmisartan

Giri, Bhupendra Raj; Kwon, Jaewook; Vo, Anh; Bhagurkar, Ajinkya M.; Bandari, Suresh; Kim, Dong Wuk

doi:10.3390/ph14010073

Cited by 45 publications

(40 citation statements)

References 48 publications

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“…Thermal processing technologies are often used for manufacturing of ASD for solid formulations [ 47 ]. Commonly utilized thermal processing methods for bulk and powder manufacturing include hot-melt extrusion (HME) [ 48 , 49 , 50 , 51 , 52 ] and spray drying (SD) [ 53 , 54 , 55 , 56 , 57 ]. In contrast, vacuum drying does not require a heating process [ 28 ], and offers many advantages such as applicability to APIs with a high melting point or low resistance against thermal and shear stress, and the potential for processing highly viscous solutions and those of high molecular weight, which are difficult to process using HME and SD [ 58 , 59 ].…”

Section: Discussionmentioning

confidence: 99%

Formulation and In Vitro Characterization of a Vacuum-Dried Drug–Polymer Thin Film for Intranasal Application

Inoue

Yamashita

2022

Polymers

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Intranasal drug applications show significant therapeutic potential for diverse pharmaceutical modalities. Because the formulation applied to the nasal cavity is discharged to the pharyngeal side by mucociliary clearance, the formulation should be dissolved effectively in a limited amount of mucus within its retention time in the nasal cavity. In this study, to develop novel formulations with improved dissolution behavior and compatibility with the intranasal environment, a thin-film formulation including drug and polymer was prepared using a vacuum-drying method. The poorly water-soluble drugs ketoprofen, flurbiprofen, ibuprofen, and loxoprofen were dissolved in a solvent comprising water and methanol, and evaporated to obtain a thin film. Physical analyses using differential scanning calorimetry (DSC), powder X-ray diffraction analysis (PXRD), and scanning electron microscopy SEM revealed that the formulations were amorphized in the film. The dissolution behavior of the drugs was investigated using an in vitro evaluation system that mimicked the intranasal physiological environment. The amorphization of drugs formulated with polymers into thin films using the vacuum-drying method improved the dissolution rate in artificial nasal fluid. Therefore, the thin film developed in this study can be safely and effectively used for intranasal drug application.

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Section: Discussionmentioning

confidence: 99%

Formulation and In Vitro Characterization of a Vacuum-Dried Drug–Polymer Thin Film for Intranasal Application

Inoue

Yamashita

2022

Polymers

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“…Different features and applications of HME have been reviewed recently by various other researchers [ 63 , 64 ]. HME’s application has largely propagated to formulate ASD and to enhance oral bioavailability of poorly water-soluble drugs, mainly BCS class II [ 65 , 66 ]. This technique’s clinical and commercial success is indicated by the presence of several melt-extruded ASD products in the market [ 66 ].…”

Section: Methods Of Preparing Transdermal Coamorphous Systemmentioning

confidence: 99%

Amorphization of Drugs for Transdermal Delivery-a Recent Update

et al. 2022

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Amorphous solid dispersion is a popular formulation approach for orally administered poorly water-soluble drugs, especially for BCS class II. But oral delivery could not be an automatic choice for some drugs with high first-pass metabolism susceptibility. In such cases, transdermal delivery is considered an alternative if the drug is potent and the dose is less than 10 mg. Amorphization of drugs causes supersaturation and enhances the thermodynamic activity of the drugs. Hence, drug transport through the skin could be improved. The stabilization of amorphous system is a persistent challenge that restricts its application. A polymeric system, where amorphous drug is dispersed in a polymeric carrier, helps its stability. However, high excipient load often becomes problematic for the polymeric amorphous system. Coamorphous formulation is another approach, where one drug is mixed with another drug or low molecular weight compound, which stabilizes each other, restricts crystallization, and maintains a single-phase homogenous amorphous system. Prevention of recrystallization along with enhanced skin permeation has been observed by the transdermal coamorphous system. But scalable manufacturing methods, extensive stability study and in-depth in vivo evaluation are lacking. This review has critically studied the mechanistic aspects of amorphization and transdermal permeation by analyzing recent researches in this field to propose a future direction.

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“…For example, in Telmisartan antihypertensive drug, by using the hot melt extrusion technique, the properties like solubility, bioavailability, and stability were improved. This was attained by using Telmisartan (TEL) with the formulation of TELloaded pH-modulated solid dispersion [21].…”

Section: Extrusion Spheronizationmentioning

confidence: 99%

A Review on Multifunctional Excipients with Regulatory Considerations

Swami

Chavan

Chakankar

et al. 2021

JPRI

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The practice of multifunctional excipients is gaining more and more attention as it simplifies the process of drug formulation by substituting the necessity of using mixture of many excipients. The multifunctional excipients are the class of excipients which includes pre-–processed and co-processed excipients and it provides added functionalities to the formulation. Functionality of an excipient is a useful property which helps in manufacturing and improves quality as well as applicability of the material. Researchers have identified that single component excipients may not always give the required results during development and manufacturing of definite API, hence they are concentrating to develop multifunctional excipients which will have improved quality that will fulfil the requirements of the formulation experts in terms of cost. The cost of new excipient development is very high as it demands toxicity studies, hence the industry is now focusing on co-processing of approved materials. The demand for directly compressible co-processed excipients has also increased due to the availability of high-speed tableting machines, time saving in Abbreviated New Drug Application (ANDA), simplified validation and stability of active ingredients. The intention of this review article is to highlight applicability and increasing attention focusing the benefits of co-processed excipients. Their advantages over conventional blend of excipients include development methods, testing and also highlighting their regulatory consideration.

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Hot-Melt Extruded Amorphous Solid Dispersion for Solubility, Stability, and Bioavailability Enhancement of Telmisartan

Cited by 45 publications

References 48 publications

Formulation and In Vitro Characterization of a Vacuum-Dried Drug–Polymer Thin Film for Intranasal Application

Formulation and In Vitro Characterization of a Vacuum-Dried Drug–Polymer Thin Film for Intranasal Application

Amorphization of Drugs for Transdermal Delivery-a Recent Update

A Review on Multifunctional Excipients with Regulatory Considerations

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