The Effect of Polymeric Excipients on the Physical Properties and Performance of Amorphous Dispersions: Part I, Free Volume and Glass Transition

Li, Jinjiang; Zhao, Junshu; Tao, Li; Wang, Jennifer; Waknis, Vrushali; Pan, Duohai; Hubert, Mario; Raghavan, Krishnaswamy; Patel, Jatin

doi:10.1007/s11095-014-1478-0

Cited by 40 publications

(20 citation statements)

References 38 publications

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“… Factor (increase) Stability Cause Ref. Glass transition temperature ( T g ) Increases Antiplasticization effect by polymers 74 Molecular mobility Decreases Molecular mobility is directly responsible for drug recrystallization 75 Configurational entropy Increases Low configurational entropy will favor crystallization 76 Configurational enthalpy Decreases The greater thermodynamic driving force for crystallization causes an increased rate of nucleation 77 Drug chemical potential Decreases Systems with lower drug chemical potential are generally more stable 78 Humidity, mechanical stress, and temperature Decreases These factors can significantly increase molecular mobility and may plasticize the material 79 Polymer concentration Increases Kinetic stabilization 11 Surfactant concentration Decreases Enhance nucleation, accelerate solution-mediated crystallization 57 …”

Section: Introductionmentioning

confidence: 99%

Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies

Bhujbal

Mitra

Jain

et al. 2021

Acta Pharmaceutica Sinica B

276

131

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Amorphous solid dispersions (ASDs) are popular for enhancing the solubility and bioavailability of poorly water-soluble drugs. Various approaches have been employed to produce ASDs and novel techniques are emerging. This review provides an updated overview of manufacturing techniques for preparing ASDs. As physical stability is a critical quality attribute for ASD, the impact of formulation, equipment, and process variables, together with the downstream processing on physical stability of ASDs have been discussed. Selection strategies are proposed to identify suitable manufacturing methods, which may aid in the development of ASDs with satisfactory physical stability.

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Section: Introductionmentioning

confidence: 99%

Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies

Bhujbal

Mitra

Jain

et al. 2021

Acta Pharmaceutica Sinica B

276

131

View full text Add to dashboard Cite

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“…To produce ENZ containing drugs, hydroxypropyl methylcellulose acetate succinate (HPMC-AS), has been used as polymer matrix for preparing solid dispersion. 7,[20][21][22][23][24] Chemical structures of ENZ and HPMC-AS are shown in Fig. 1.…”

Section: Introductionmentioning

confidence: 99%

Using Acetone/Water Binary Solvent to Enhance the Stability and Bioavailability of Spray Dried Enzalutamide/HPMC-AS Solid Dispersions

Zhang

Rao

Qiu

et al. 2021

Journal of Pharmaceutical Sciences

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We demonstrated a facile approach, by adjusting the solvent ratio of water/acetone binary mixture, to alter the intermolecular interactions between Enzalutamide (ENZ) and hydroxypropyl methylcellulose acetate succinate (HPMC-AS) for spray drying process, which can be readily implemented to produce spray-dried dispersions (SDD) with enhanced stability and bioavailability.The prepared SDD of ENZ/HPMC-AS were examined systematically in terms of particle size, morphology, dissolution, solubility, stability, and bioavailability. Our results show that the introduction of water (up to 30% volume fraction) can effectively reduce the hydrodynamic diameter of HPMC-AS from approximately 220 nm to 160 nm (a reduction of c.a. 20%), which increases the miscibility of the drug and polymer, delaying or inhibiting the crystallization of ENZ during the spray drying process, resulting in a homogeneous amorphous phase. The benefits of using acetone/water binary mixture were subsequently evidenced by an increased specific surface area, improved dissolution profile and relative bioavailability, enhanced stability, and elevated drug release rate. This fundamental finding underpins the great potential of using binary mixture for spray drying process to process active pharmaceutical ingredients (APIs) that are otherwise challenging to handle.

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“…2c). The ΔΗ values of glass transition increase as the molecular weight of PVP increases [10,13,15,21]. Namely, ΔH= -141.5 J mol -1 for MW: 10,000, -171.7 J mol -1 for MW:29,000 and -237.0 J mol -1 for MW:55,000.…”

Section: Dsc Curves Of Pure Excipientsmentioning

confidence: 99%

Thermal analysis studies on the compatibility of furosemide with solid state and liquid crystalline excipients

Vlachou

Pippa

Siamidi

et al. 2020

Hem Ind

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In the context of the present study, the thermal behavior of furosemide and the solid state excipients, sodium alginate, poly(ethylene oxide), poly(vinylpyrrolidone), lactose mono-hydrate and magnesium stearate, using Differential Scanning Calorimetry (DSC), was probed. It was found that the thermal behavior of these solid-state pharmaceutical excipients and furosemide correlates nicely with the literature relevant data. Regarding the furosemide-excipients mixtures, the DSC scans appear as a compilation of the thermal curves of each excipient. This suggests that the formulations containing these mixtures, may retain their stability over time. This information, which arises from the cooperativity of materials, their thermal stability and behavioris very helpful for the research and development of safe and effective pharmaceutical formulations. DSC experiments were also carried out with chimeric bilayers (called ?liposomes?), composed of hydrogenated soy phosphatidylcholine (HSPC) and poly(n-butylacrylate)-b-poly(acrylic acid) block copolymer with 70 % content of poly(acrylic acid (PnBA-b-PAA 30/70) with the addition of furosemide at the molar ratio of 9:0.1:1.0 in the system HSPC:PnBA-b-PAA 30/70:furosemide. Chimeric liposomal systems were characterized as ?fluid-like? by their DSC curves, which may be potentially translated as an easy way for release of furosemide from the advanced delivery system.

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The Effect of Polymeric Excipients on the Physical Properties and Performance of Amorphous Dispersions: Part I, Free Volume and Glass Transition

Abstract: Both the backbone chain rigidity of polymers as well as drug-polymer interaction can impact the free volume and glass transition behaviors of the dispersions.

Cited by 40 publications

References 38 publications

Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies

Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies

Using Acetone/Water Binary Solvent to Enhance the Stability and Bioavailability of Spray Dried Enzalutamide/HPMC-AS Solid Dispersions

Thermal analysis studies on the compatibility of furosemide with solid state and liquid crystalline excipients

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