Amorphous solid dispersions: Rational selection of a manufacturing process

Vasconcelos, Teófilo; Marques, Sara; Neves, José das; Sarmento, Bruno

doi:10.1016/j.addr.2016.01.012

Cited by 296 publications

(186 citation statements)

References 157 publications

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“…The two first are the most common and manufacturing processes fusion-based and solvent-based are available for industrial applications [13]. Mechanical processes such as ball milling or grinding can also be used but the degree of amorphization is usually lower in comparison with fusion and solvent methods [13,14,35,36,46]. The main obtaining methods for solid dispersions are briefly described below and their advantages and limitations are presented in Table 5.…”

Section: Preparation Methodsmentioning

confidence: 99%

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

et al. 2018

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The oral solid dosage forms are extremely relevant to drug therapy and responsible for much of the pharmaceutical industry turnover worldwide. However, the development of medicines in solid form involves significant challenges, including obtaining formulations with appropriate bioavailability for low aqueous solubility drugs (classes II and IV of the Biopharmaceutics Classification System). One of the most effective strategies to overcome poor dissolution rate and low absorption of drugs is the solid dispersion technique, however, although it has been the focus of much research in recent decades, there are relatively few commercially available products based on such technology. This is mainly due to problems related to production scale-up and physicochemical instability and creates opportunities for new studies to explore the full potential of the technology. This review presents an overall approach to the factors affecting the dissolution rate and oral bioavailability of BCS-classes II and IV drugs and a brief review of the state-of-the-art of solid dispersion technology.

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Section: Preparation Methodsmentioning

confidence: 99%

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

et al. 2018

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“…Amorphous solid dispersions (ASDs) can be defined as molecular mixtures of hydrophobic drugs with a hydrophilic carrier that has a higher chemical potential energy than the corresponding crystalline forms, and can provide a solubility advantage over the crystalline form, without the involvement of any chemical changes to the compound (Li & Taylor, 2018;Wilson et al, 2018). Drug in solid dispersions could have a significantly higher solubility due to the amorphous state which could break the crystal lattice without the requirement of energy, and greater dissolution rate owing to an increase in surface area with a decrease in particle size (Vasconcelos et al, 2016;Iwashita et al, 2019). Therefore, Solid dispersions (SDs) are becoming a primary focus in the research and development, especially regarding the dosage forms used to establish water-insoluble active pharmaceutical ingredients (Zhang et al, 2018).…”

Section: Introductionmentioning

confidence: 99%

Improved solubility, dissolution rate, and oral bioavailability of main biflavonoids from Selaginella doederleinii extract by amorphous solid dispersion

et al. 2020

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2020) Improved solubility, dissolution rate, and oral bioavailability of main biflavonoids from Selaginelladoederleinii extract by amorphous solid dispersion, Drug Delivery, 27:1, 309-322, ABSTRACT Amentoflavone, robustaflavone, 2 00 ,3 00 -dihydro-3 0 ,3 000 -biapigenin, 3 0 ,3 000 -binaringenin, and delicaflavone are five major hydrophobic components in the total biflavonoids extract from Selaginella doederleinii (TBESD) that display favorable anticancer properties. The purpose of this study was to develop a new oral delivery formulation to improve the solubilities, dissolution rates, and oral bioavailabilities of the main ingredients in TBESD by the solid dispersion technique. Solid dispersions of TBESD with various hydrophilic polymers were prepared, and different technologies were applied to select the suitable carrier and method. TBESD amorphous solid dispersion (TBESD-ASD) with polyvinylpyrrolidone K-30 was successfully prepared by the solvent evaporation method. The physicochemical properties of TBESD-ASD were investigated by scanning electron microscopy, differential scanning calorimetry, and Fourier-transform infrared spectroscopy. As a result, TBESD was found to be molecularly dispersed in the amorphous carrier. The solubilities and dissolution rates of all five ingredients in the TBESD-ASD were significantly increased (nearly 100% release), compared with raw TBESD. Meanwhile, TBESD-ASD showed good preservation stability for 3 months under accelerated conditions of 40 C and 75% relative humidity. A subsequent pharmacokinetic study in rats revealed that C max and AUC 0-t of all five components were significantly increased by the solid dispersion preparation. An in vivo study clearly revealed that compared to raw TBESD, a significant reduction in tumor size and microvascular density occurred after oral administration of TBESD-ASD to xenograft-bearing tumor mice. Collectively, the developed TBESD-ASD with the improved solubility, dissolution rates and oral bio-availabilities of the main ingredients could be a promising chemotherapeutic agent for cancer treatment. ARTICLE HISTORY

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“…The methods used for improving the solubility, dissolution rate, and bioavailability of solid medicinal substances are being developed and improved. In the last two decades, in order to enhance the solubility and bioavailability of drugs, in addition to drugs in the form of salts [2], attention has been focused on the preparation of solid amorphous dispersions [3,4], dispersions containing nanocrystals [5,6], and the synthesis of co-crystals [7,8]. Additionally, when resolving the problem of improving the bioavailability, the polymorphism phenomenon, which is defined as the possibility for the original molecule to exist in two or more crystal states, plays an important role [9][10][11].…”

Section: Introductionmentioning

confidence: 99%

The Polymorphism of Drugs: New Approaches to the Synthesis of Nanostructured Polymorphs

Chistyakov

Sergeev

2020

Pharmaceutics

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Among the significant problems of modern pharmacology are the low solubility and bioavailability of drugs. One way to resolve this problem is to obtain new polymorphic forms of drugs with improved physicochemical properties. Various approaches have been developed with this aim, including the preparation of co-crystals, the use of nanoparticles, or the use of compounds in the form of a salt. A promising direction in pharmacology concerns the production of new stable polymorphic structures. In this mini-review, we consider certain aspects of drug polymorphism, methods for the synthesis of polymorphs, and the stability, size, and transformation of crystalline polymorphs. Moreover, we summarize our results from several studies demonstrating the problems associated with the synthesis of new polymorphous modifications based on inert gases and cryotemperatures. The results indicate that the problems specific to drug polymorphisms have only been partly resolved, are of current interest, and require further development.

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Amorphous solid dispersions: Rational selection of a manufacturing process

Cited by 296 publications

References 157 publications

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Challenges to improve the biopharmaceutical properties of poorly water-soluble drugs and the application of the solid dispersion technology

Improved solubility, dissolution rate, and oral bioavailability of main biflavonoids from Selaginella doederleinii extract by amorphous solid dispersion

The Polymorphism of Drugs: New Approaches to the Synthesis of Nanostructured Polymorphs

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