Ball-milled solid dispersions of BCS Class IV drugs: Impact on the dissolution rate and intestinal permeability of acyclovir

Nart, Viviane; França, Maria Terezinha; Anzilaggo, Daiane; Riekes, Manoela Klüppel; Kratz, Jadel M.; Campos, Carlos Eduardo Maduro de; Simões, Cláudia Maria Oliveira; Stulzer, Hellen Karine

doi:10.1016/j.msec.2015.04.028

Cited by 21 publications

(4 citation statements)

References 38 publications

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“…They point to the fact that the appropriate dosing volumes of solutions or suspensions in neonates are difficult to reproduce 35 . Recently, APIs of BCS class IV like Aciclovir, Furosemide and Nystatin have been formulated as solid dispersions since their dose and improved solubility, permeability and effectiveness, respectively, are assured [36][37][38][39] .…”

Section: Resultsmentioning

confidence: 99%

Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study

Santoveña

Suárez-González

Martín-Rodríguez

et al. 2016

Pharmaceutical Development and Technology

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Section: Resultsmentioning

confidence: 99%

Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study

Santoveña

Suárez-González

Martín-Rodríguez

et al. 2016

Pharmaceutical Development and Technology

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“…In this method, drug and the carrier are physically mixed using a blender at an adequate speed, and then this mixture is transferred in a vibration ball mill chamber. After that, the combination is ground for a specific time by adding steel balls in it [68].…”

Section: Co-grinding Methodsmentioning

confidence: 99%

Recent Patents on Solid Dispersions of Antihyperlipidemic Drugs

Singh

Nanda²

2023

Int J App Pharm

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Hyperlipidemia is a worsening health condition in developed and developing countries, especially among the younger generation due to their lifestyle. The World Health Organization reported 2.6 million deaths globally due to hyperlipidemia. Therefore, there is a huge demand of antihyperlipidemic drugs in the pharmaceutical market. Approximately 60% of the total active drug content used in hyperlipidemia suffer from poor water solubility, particularly BCS class II drugs. Poor water solubility may result in insufficient absorption and finally affects the bioavailability of the drug causes ineffectiveness in lowering lipid profile of patients. In recent years, solid dispersion technology has proved to be a simple, effective and economical approach for industrial application to increase the solubility of these drugs. This review paper is an attempt to compile up various research as well as patents reports related to solid dispersions of poor water soluble antihyperlipidemic drugs.

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“…Solid dispersions of acyclovir (20%) in neutral carriers (chitosan, hydroxypropylmethyl cellulose K100M ® or Pluronic F68 ® ) were prepared in a mixer ball mill over three hours [ 88 ]. All dispersions displayed antiviral activity and enhanced aqueous dissolution rates.…”

Section: Reviewmentioning

confidence: 99%

Mechanochemistry of nucleosides, nucleotides and related materials

Eguaogie¹,

Vyle²,

Conlon³

et al. 2018

Beilstein J. Org. Chem.

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The application of mechanical force to induce the formation and cleavage of covalent bonds is a rapidly developing field within organic chemistry which has particular value in reducing or eliminating solvent usage, enhancing reaction rates and also in enabling the preparation of products which are otherwise inaccessible under solution-phase conditions. Mechanochemistry has also found recent attention in materials chemistry and API formulation during which rearrangement of non-covalent interactions give rise to functional products. However, this has been known to nucleic acids science almost since its inception in the late nineteenth century when Miescher exploited grinding to facilitate disaggregation of DNA from tightly bound proteins through selective denaturation of the latter. Despite the wide application of ball milling to amino acid chemistry, there have been limited reports of mechanochemical transformations involving nucleoside or nucleotide substrates on preparative scales. A survey of these reactions is provided, the majority of which have used a mixer ball mill and display an almost universal requirement for liquid to be present within the grinding vessel. Mechanochemistry of charged nucleotide substrates, in particular, provides considerable benefits both in terms of efficiency (reducing total processing times from weeks to hours) and by minimising exposure to aqueous conditions, access to previously elusive materials. In the absence of large quantities of solvent and heating, side-reactions can be reduced or eliminated. The central contribution of mechanochemistry (and specifically, ball milling) to the isolation of biologically active materials derived from nuclei by grinding will also be outlined. Finally non-covalent associative processes involving nucleic acids and related materials using mechanochemistry will be described: specifically, solid solutions, cocrystals, polymorph transitions, carbon nanotube dissolution and inclusion complex formation.

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Ball-milled solid dispersions of BCS Class IV drugs: Impact on the dissolution rate and intestinal permeability of acyclovir

Cited by 21 publications

References 38 publications

Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study

Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study

Recent Patents on Solid Dispersions of Antihyperlipidemic Drugs

Mechanochemistry of nucleosides, nucleotides and related materials

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