# Evidence: antiplasticization

Parent: — · class: solid-state property · names merged here: antiplasticisation; antiplasticization

8 papers measured or used it, 6 only mentioned it (of 207 kept papers). Papers in year order; each section heading ends with the paper's category / subcategory. Generated by tools/build_evidence.py from registry/concepts.csv and the cards; do not edit.

## 1997 Taylor — Spectroscopic Characterization of Interactions Between PVP and Indomethacin in Amorphous Molecular Dispersions · Solid state stability / Miscibility and drug-polymer interactions

[1997-taylor-pvp-indomethacin-amorphous-molecular-dispersions](../../../cards/1997-taylor-pvp-indomethacin-amorphous-molecular-dispersions/paper.html) · Solid state stability / Miscibility and drug-polymer interactions · used · as: antiplasticisation

| id | kind | content | locator |
|---|---|---|---|
| C5 | claim, prior hypothesis, authors: asserted | Yoshioka et al. found significant inhibition of indomethacin crystallisation at relatively low PVP levels, which could not be explained solely by the antiplasticising effect of the polymer [rests on: cited: ref 7] | p.1691 |
| C45 | claim, generalisation, authors: abstract: "may influence"; summary: "offers an explanation" | PVP may influence crystallisation kinetics by preventing the self-association of indomethacin; the hydrogen bond offers an explanation of how PVP inhibits crystallisation from the amorphous phase at levels where its antiplasticising effect is minimal [rests on: C35, C5; cited: ref 7] | p.1691, p.1697 |

## 2006 Konno — Influence of Different Polymers on the Crystallization Tendency of Molecularly Dispersed Amorphous Felodipine · Solid state stability / Physical stability

[2006-konno-felodipine-polymer-crystallization-nucleation-solid-dispersions](../../../cards/2006-konno-felodipine-polymer-crystallization-nucleation-solid-dispersions/paper.html) · Solid state stability / Physical stability · measured · as: antiplasticization

| id | kind | content | locator |
|---|---|---|---|
| R6 | record, measured | onset Tg of dispersions (°C; mean, error bars SD, n = 3) — bulk dispersions (P3, P4), DSC 20 K/min — sub-table below (0% and 100% points in B1: M1-M4); text: for HPMCAS and HPMC at low concentration Tg not significantly higher than felodipine alone, increase only for polymer above 30% w/w; Tg identical to pure felodipine over 0-25% w/w for HPMC and HPMCAS, raised by 10 °C at 25% PVP | Fig. 5, p.2698; text p.2697, p.2701 |
| C25 | claim, conclusion, authors: asserted | Although the dry polymer Tgs differ (B1), the polymers were equally effective; PVP is the best antiplasticizer, raising dispersion Tg at all concentrations and by 10 °C at 25%, whereas because of nonidealities HPMC and HPMCAS do not raise Tg over the 0-25% w/w range used for nucleation [rests on: R4, R6, M2-M4] | p.2701 |
| C2 | claim, prior hypothesis, authors: "is considered"; "has been attributed" | Tg is considered a key parameter separating high and low molecular mobility, and the stabilizing effect of polymers with high Tg relative to the drug has been attributed to antiplasticization [rests on: cited: refs 14-16] | p.2692-2693 |

## 2006 Marsac — A Comparison of the Physical Stability of Amorphous Felodipine and Nifedipine Systems · Solid state stability / Physical stability

[2006-marsac-physical-stability-amorphous-felodipine-nifedipine](../../../cards/2006-marsac-physical-stability-amorphous-felodipine-nifedipine/paper.html) · Solid state stability / Physical stability · measured · as: antiplasticization

| id | kind | content | locator |
|---|---|---|---|
| R17 | record, measured | Tg versus PVP content (°C; error bars one SD), with Gordon-Taylor (solid) and Couchman-Karasz (dashed) curves — nifedipine-PVP (a) and felodipine-PVP (b) dispersions (P3, P7); fit parameters not printed — sub-table below; text: a single Tg at every composition; Tg of felodipine with 10 wt% PVP 40.5 (±0.5) °C, slightly below pure felodipine; Tgs of the two drug-PVP systems virtually identical at every concentration | Fig. 10, p.2312; text p.2311 |
| C22 | claim, conclusion, authors: asserted ("clearly shown") | PVP antiplasticizes at all concentrations except 10 wt% PVP with felodipine, where Tg is slightly below that of the pure drug; lack of antiplasticization by small polymer amounts has been seen before [rests on: R17, R8; cited: refs 17, 37] | p.2311 |

## 2008 Konno — Ability of Different Polymers to Inhibit the Crystallization of Amorphous Felodipine in the Presence of Moisture · Solid state stability / Physical stability

[2008-konno-polymers-inhibit-amorphous-felodipine-moisture-crystallization](../../../cards/2008-konno-polymers-inhibit-amorphous-felodipine-moisture-crystallization/paper.html) · Solid state stability / Physical stability · used · as: antiplasticization

| id | kind | content | locator |
|---|---|---|---|
| C2 | claim, prior hypothesis, authors: "suggesting"; "It has also been suggested" | Polymer stabilization of the amorphous state has been attributed to antiplasticization (dispersions have higher Tg than the amorphous drug, so lower mobility may be achieved) and to specific drug-polymer interactions such as hydrogen bonds [rests on: cited: refs 6, 9, 10] | p.969 |
| C16 | claim, conclusion, authors: asserted | Dry Tg rises with polymer content (ref 11), but absorbed moisture counteracts this antiplasticization: at 75% RH and low polymer content Tg falls below that of dry amorphous felodipine (about 43 °C), and all 75% RH samples with up to 25% polymer are below it; at 75% RH Tg rises with content for the cellulose polymers, while for PVP it peaks around 70% polymer and then falls sharply [rests on: R7] | p.973-974, p.976 |
| R7 | record, cited (ref 11) for dry columns; measured for 75% RH columns | Tg onset (°C, n = 3) versus polymer content — bulk dispersions (P2, P6); dry (0% RH) and after 75% RH — sub-table below | Fig. 4, p.973; text p.973-974, p.976 |

## 2008 Marsac — Spontaneous Crystallinity Loss of Drugs in the Disordered Regions of Poly(Ethylene Oxide) in the Presence of Water · Solid state stability / PEG dispersions

[2008-marsac-peo-water-spontaneous-drug-crystallinity-loss](../../../cards/2008-marsac-peo-water-spontaneous-drug-crystallinity-loss/paper.html) · Solid state stability / PEG dispersions · used · as: antiplasticization

| id | kind | content | locator |
|---|---|---|---|
| C27 | claim, mechanism, authors: "most likely" | Drug dissolving in the amorphous PEO will most likely anti-plasticize it, given the drug Tg values of Table 1 [rests on: M1, M2, M3, M4, M5, M6] | p.3191 |

## 2010 Kestur — Effects of the Molecular Weight and Concentration of Polymer Additives, and Temperature on the Melt Crystallization Kinetics of a Small Drug Molecule · Solid state stability / Physical stability

[2010-kestur-pvp-mw-concentration-temperature-felodipine-melt-crystallization](../../../cards/2010-kestur-pvp-mw-concentration-temperature-felodipine-melt-crystallization/paper.html) · Solid state stability / Physical stability · used · as: antiplasticization

| id | kind | content | locator |
|---|---|---|---|
| C33 | claim, prior hypothesis, authors: asserted | Antiplasticization (higher Tg, lower mobility, mobility ∼1/η) has been proposed for some polymers, while other studies found stabilization without a Tg change or with a Tg decrease [rests on: cited: refs 9, 11, 14, 18, 36] | p.3593 |
| C34 | claim, conclusion, authors: "which suggests" | The glass transition is largely unaffected by the presence and concentration of PVP, so antiplasticization is not the cause of the inhibition [rests on: R1] | p.3593 |

## 2011 Kestur — Influence of polymer chemistry on crystal growth inhibition of two chemically diverse organic molecules · Solid state stability / Miscibility and drug-polymer interactions

[2011-kestur-polymer-chemistry-crystal-growth-bifonazole-nimesulide](../../../cards/2011-kestur-polymer-chemistry-crystal-growth-bifonazole-nimesulide/paper.html) · Solid state stability / Miscibility and drug-polymer interactions · measured · as: antiplasticization

| id | kind | content | locator |
|---|---|---|---|
| R6 | record, measured | onset Tg of 5% polymer dispersions (°C) — DSC (P5); drug Tg in M1, M2 — sub-table below; text: Tg of the dispersions similar to the pure drugs | Tables 1-2, p.6715-6716; text p.6714 |
| C12 | claim, conclusion, authors: asserted | 5 wt% polymer did not change the Tg of either drug significantly, and neither this antiplasticization nor the Tg of the pure polymer correlates with growth-rate inhibition (PAA, Tg 103 °C, beats PVP, Tg 164 °C), as observed in other studies [rests on: R6, M2, M3, M7; cited: refs 5, 14] | p.6715 |

## 2017 Xie — Effect of Temperature and Moisture on the Physical Stability of Binary and Ternary Amorphous Solid Dispersions of Celecoxib · Solid state stability / Physical stability

[2017-xie-temperature-moisture-celecoxib-binary-ternary-asd-stability](../../../cards/2017-xie-temperature-moisture-celecoxib-binary-ternary-asd-stability/paper.html) · Solid state stability / Physical stability · measured · as: antiplasticization

| id | kind | content | locator |
|---|---|---|---|
| R14 | record, measured | dry Tg (onset, °C) of binary ASDs versus polymer content — P6; neat-component Tg in B1; error bars on some points, n not stated — sub-table below; text: a single Tg for each composition, intermediate between the neat components | Fig. 6, p.6; text p.5-6 |
| C6 | claim, prior hypothesis, authors: "are thought to"; "appears to have some correlation" | Polymers are thought to stabilize amorphous drugs by raising Tg (antiplasticization), but inhibition cannot always be rationalized by Tg; specific interactions such as hydrogen bonding or ionic interactions also act, and their strength appears to correlate with inhibitor effectiveness [rests on: cited: refs 3-11] | p.1 |
| C27 | claim, conclusion, authors: "apparently" | PVP-K12 and PVP/VA apparently raise the Tg of CEX ASDs more effectively than HPMCAS and HPMC despite their own lower Tg [rests on: R14] | p.6 |

## Mentioned only

- 2008 Konno — [2008-konno-polymer-type-felodipine-asd-dissolution](../../../cards/2008-konno-polymer-type-felodipine-asd-dissolution/paper.html) · Dissolution / B. Supersaturation from ASD dissolution (ref 8)
- 2010 Marsac — [2010-marsac-temperature-moisture-miscibility-felodipine-pvp-asd](../../../cards/2010-marsac-temperature-moisture-miscibility-felodipine-pvp-asd/paper.html) · Solid state stability / Physical stability (ref 2)
- 2014 Mosqueragiraldo — [2014-mosquera-giraldo-surfactants-crystal-growth-amorphous-celecoxib](../../../cards/2014-mosquera-giraldo-surfactants-crystal-growth-amorphous-celecoxib/paper.html) · Solid state stability / Physical stability (ref 17)
- 2017 Trasi — [2017-trasi-commercial-amorphous-tacrolimus-crystallization-stress](../../../cards/2017-trasi-commercial-amorphous-tacrolimus-crystallization-stress/paper.html) · Solid state stability / Physical stability (ref C3)
- 2021 Bhujbal — [2021-bhujbal-lumefantrine-asd-spray-antisolvent-precipitation](../../../cards/2021-bhujbal-lumefantrine-asd-spray-antisolvent-precipitation/paper.html) · Solid state stability / Physical stability (ref 6)
- 2022 Hiew — [2022-hiew-lumefantrine-asd-stability-dissolution-polymer-choice](../../../cards/2022-hiew-lumefantrine-asd-stability-dissolution-polymer-choice/paper.html) · Solid state stability / Miscibility and drug-polymer interactions (ref 15)