The effect of drug and EUDRAGIT® S 100 miscibility in solid dispersions on the drug and polymer dissolution rate

Higashi, Kenjirou; Hayashi, Hideharu; Yamamoto, Keiji; Moribe, Kunikazu

doi:10.1016/j.ijpharm.2015.08.007

Cited by 55 publications

(29 citation statements)

References 40 publications

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“…In addition, the extent of miscibility of an amorphous drug thei n polymer is also important as highly miscible systems are found to be more resistant to drug recrystallization. 131 The formation of a stable single phase or separate coexisting phases depends on the thermodynamic miscibility of the drug and polymer at the required condition. A change of conditions may cause phase separation of the homogenous single-phase system (Table 3).…”

Section: Rational Selection Of Polymers For Pasdsmentioning

confidence: 99%

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Baghel

Cathcart

O’Reilly

2016

Journal of Pharmaceutical Sciences

763

452

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Poor water solubility of many drugs has emerged as one of the major challenges in the pharmaceutical world. Polymer-based amorphous solid dispersions have been considered as the major advancement in overcoming limited aqueous solubility and oral absorption issues. The principle drawback of this approach is that they can lack necessary stability and revert to the crystalline form on storage. Significant upfront development is, therefore, required to generate stable amorphous formulations. A thorough understanding of the processes occurring at a molecular level is imperative for the rational design of amorphous solid dispersion products. This review attempts to address the critical molecular and thermodynamic aspects governing the physicochemical properties of such systems. A brief introduction to Biopharmaceutical Classification System, solid dispersions, glass transition, and solubility advantage of amorphous drugs is provided. The objective of this review is to weigh the current understanding of solid dispersion chemistry and to critically review the theoretical, technical, and molecular aspects of solid dispersions (amorphization and crystallization) and potential advantage of polymers (stabilization and solubilization) as inert, hydrophilic, pharmaceutical carrier matrices. In addition, different preformulation tools for the rational selection of polymers, state-of-the-art techniques for preparation and characterization of polymeric amorphous solid dispersions, and drug supersaturation in gastric media are also discussed.

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Section: Rational Selection Of Polymers For Pasdsmentioning

confidence: 99%

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Baghel

Cathcart

O’Reilly

2016

Journal of Pharmaceutical Sciences

763

452

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“…It is non-soluble in acids and water, while it is soluble in a pH 7 solvent or higher alkaline circumstance (Higashi et al 2015; Sharma et al 2016). Eu polymers are nontoxic and food-grade polymers (Gibson et al 2006; José 2006; Thakral et al 2013).…”

Section: Introductionmentioning

confidence: 99%

Effect of Eudragit S100 nanoparticles and alginate chitosan encapsulation on the viability of Lactobacillus acidophilus and Lactobacillus rhamnosus

et al. 2017

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In this study, we examined a novel method of microencapsulation with calcium alginate-chitosan and Eudragit S100 nanoparticles for the improving viability of probiotic bacteria, Lactobacillus acidophilus and Lactobacillus rhamnosus. Extrusion technique was carried out in microencapsulation process. The viability of two probiotics in single coated beads (with only chitosan), double coated beads (with chitosan and Eudragit nanoparticles), and as free cells (unencapsulated) were conducted in simulated gastric juice (pH 1.55, without pepsin) followed by incubation in simulated intestinal juice (pH 7.5, with 1% bile salt). In case of single coated beads, presumably, lack of sufficient strength of chitosan under simulated gastric condition was the main reason of 4-log and 5-log reduction of the counts of the L. acidophilus and L. rhamnosus respectively. The results showed that with the second coat forming (Eudragit nanoparticles) over the first coat (chitosan), the strength of the beads and then viability rate of the bacteria were increased in comparison with the single coated beads.Electronic supplementary materialThe online version of this article (doi:10.1186/s13568-017-0442-x) contains supplementary material, which is available to authorized users.

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“…Surfactants have been recommended to be incorporated in SDs to reduce the high temperatures during the hot-melt extrusion processes, which may cause the degradation of both drug and polymers [76]. The effectiveness of SDs developed from enteric coating polymers depends on the miscibility between drug and polymer [77]. It has been noted that excessive drug loading in SDs results in drug domains that do not interact with polymer matrixes [77].…”

Section: Effects Of Enteric Coating Polymers and Preparation Methods mentioning

confidence: 99%

“…It has been noted that excessive drug loading in SDs results in drug domains that do not interact with polymer matrixes [77]. Amorphous drugs are easily transformed into drug crystals once these domains are exposed to the dissolution medium [77]. Therefore, miscibility and drug recrystallization must be considered in SD formulations with enteric coating agents [77].…”

Section: Effects Of Enteric Coating Polymers and Preparation Methods mentioning

confidence: 99%

“…Amorphous drugs are easily transformed into drug crystals once these domains are exposed to the dissolution medium [77]. Therefore, miscibility and drug recrystallization must be considered in SD formulations with enteric coating agents [77]. The preparation method certainly affects the miscibility in SDs [78].…”

Section: Effects Of Enteric Coating Polymers and Preparation Methods mentioning

confidence: 99%

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Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Tran

2020

Polymers

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In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

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The effect of drug and EUDRAGIT® S 100 miscibility in solid dispersions on the drug and polymer dissolution rate

Cited by 55 publications

References 40 publications

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Polymeric Amorphous Solid Dispersions: A Review of Amorphization, Crystallization, Stabilization, Solid-State Characterization, and Aqueous Solubilization of Biopharmaceutical Classification System Class II Drugs

Effect of Eudragit S100 nanoparticles and alginate chitosan encapsulation on the viability of Lactobacillus acidophilus and Lactobacillus rhamnosus

Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

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