# Evidence: drug leaching

Parent: — · class: transport and absorption · names merged here: drug leaching; leaching from amorphous suspensions

4 papers measured or used it, 0 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.

## 2015 Chen — Impact of Surfactants on the Crystallization of Aqueous Suspensions of Celecoxib Amorphous Solid Dispersion Spray Dried Particles · Dissolution / B. Supersaturation from ASD dissolution

[2015-chen-surfactants-crystallization-celecoxib-hpmcas-asd-suspensions](../../../cards/2015-chen-surfactants-crystallization-celecoxib-hpmcas-asd-suspensions/paper.html) · Dissolution / B. Supersaturation from ASD dissolution · measured · as: drug leaching

| id | kind | content | locator |
|---|---|---|---|
| R17 | record, derived (E1) | celecoxib supersaturation in the suspension medium vs time — six media of A1, 10 mg/mL ASD, 25 °C; no error bars plotted — sub-table R17 | Results pp. 17–18; Fig. 7, p. 19 |
| C12 | claim, conclusion, authors: asserted | Celecoxib leaching is greatest in SDS; in HCl, Polysorbate 80, STC and Poloxamer 188 it is lower, with maximum S of 3.4–5.4 reached in the first six hours. [rests on: R17] | Results pp. 17–18 |
| C13 | claim, mechanism, authors: asserted | Rises in solution concentration come from celecoxib leaching out of the ASD particles; the subsequent falls (SDS after ≈10 min, Polysorbate 80 between 0.5 and 3 h) come from crystallization. [rests on: R17.a, R17.b, R14.a, R14.b] | Results pp. 17–18; Fig. 7 caption p. 19 |

## 2016 Li — Leaching of Lopinavir Amorphous Solid Dispersions in Acidic Media · Dissolution / B. Supersaturation from ASD dissolution

[2016-li-lopinavir-asd-leaching-acidic-media](../../../cards/2016-li-lopinavir-asd-leaching-acidic-media/paper.html) · Dissolution / B. Supersaturation from ASD dissolution · measured · as: leaching from amorphous suspensions

| id | kind | content | locator |
|---|---|---|---|
| R2 | record, measured | polymer leached from spray-dried pure polymers (µg/mL; triplicate samples, error bars) — 100 mg/10 mL, pH 3, 25 °C, no additive (P4) — sub-table below; text: average 60–180 min 15 ± 2 (LF), 19 ± 2 (MF), 68 ± 11 (HF), <5 (HPMCP); less than 100 µg/mL in all cases and less than 1% of the polymer dissolved, from the solids loading | Fig. 2a, pdf p.5; text pdf p.5 |
| R3 | record, measured | polymer leached from LPV ASDs (µg/mL; triplicate samples, error bars) — LPV–HPMCAS LF, MF, HF ASDs, 100 mg/10 mL, pH 3, 25 °C (P4); no HPMCP series plotted — sub-table below; text: average 60–180 min below 5 µg/mL for all the polymers; HPMCP leaching too low to compare with and without LPV | Fig. 2b, pdf p.5; text pdf p.5 |
| R4 | record, measured | LPV leached from ASDs (µg/mL; triplicate samples, error bars) — LPV–HPMCAS LF, MF, HF and LPV–HPMCP ASDs, 100 mg/10 mL, pH 3, 25 °C (P4) — sub-table below; text: average 60–180 min around 7 µg/mL for the three HPMCAS grades, "not statistically different" (printed with "p < 0.05"); around 5 µg/mL for HPMCP | Fig. 2c, pdf p.5; text pdf p.5 |
| R7 | record, measured | LPV leached from LPV–HF ASD with each surfactant (µg/mL; triplicate samples, error bars) — pH 3, surfactants at P4 levels, 100 mg/10 mL, 25 °C — sub-table below; text: with STC around 25 µg/mL, "a 3.5-fold increase"; increase with poloxamer 188 "marginal" | Fig. 3a, pdf p.7; text pdf p.6 |
| R9 | record, measured | LPV leached from LPV–HPMCP ASD with each surfactant (µg/mL; triplicate samples, error bars) — pH 3, surfactants at P4 levels, 100 mg/10 mL, 25 °C — sub-table below | Fig. 3c, pdf p.7 |
| R13 | record, measured | LPV and HPMCAS HF leached from LPV–HF ASD at pH 3 and pH 5, with and without SDS (µg/mL; triplicate samples, error bars) — SDS 0.055% w/v (P4), 100 mg/10 mL, 25 °C — sub-table below; text: average LPV and polymer around 13 and around 21 µg/mL at pH 3, around 36 and around 120 µg/mL at pH 5 with SDS; without surfactant no significant pH effect on LPV, polymer similar within experimental error | Fig. 5a–b, pdf p.9; text pdf p.6 |
| R17 | record, measured | LPV leached from LPV–HF ASD with 0.5% w/v PVPVA, without and with SDS (µg/mL; triplicate samples, error bars) — pH 3, 100 mg/10 mL, 25 °C (P4); SDS level not stated (X10) — sub-table below; text: average 60–180 min around 7 (LPV–HF), around 9 (LPV–HF–PVPVA) and around 50 µg/mL (LPV–HF–PVPVA–SDS), "more than a five-fold increase" | Fig. 7a, pdf p.10; text pdf p.7 |

## 2023 Moseson — Impact of Aluminum Oxide Nanocoating on Drug Release from Amorphous Solid Dispersion Particles · ASD process / ASD process

[2023-moseson-aluminum-oxide-nanocoating-drug-release-asd-particles](../../../cards/2023-moseson-aluminum-oxide-nanocoating-drug-release-asd-particles/paper.html) · ASD process / ASD process · measured · as: drug leaching

| id | kind | content | locator |
|---|---|---|---|
| R11 | record, measured | PCZ leached concentration vs time in acid (µg/mL) — PH25/L/NC and PH25/L/C39; media labelled pH 1.2 and pH 4.0 (X2); 60 min — sub-table below; at pH 1.2 the coated and uncoated means overlap from ≈40 min; at pH 4.0 the coated mean stays below the uncoated mean to 58 min; early points of the pH 4.0 series plotted below zero | Fig. 5, p.598 |
| R12 | record, measured | PCZ concentration vs time, two-stage (µg/mL) — PH25/L/NC and PH25/L/C39; pH 4.0 for 30 min, 1 h or 4 h, then pH 6.5 (P14) — sub-table below; coated mean below uncoated mean throughout each acid stage | Fig. S5 (printed "Figure S6"), SI p.6; text p.598 |
| C17 | claim, conclusion, authors: asserted | In the pH 1.6 gastric stage a low amount of amorphous drug leaches, consistent with other HPMCAS ASDs, and coated samples show a small delay in the start of leaching [rests on: R10; cited: ref 51] | p.597 |
| C20 | claim, conclusion, authors: asserted | The coating slowed leaching at both acidic pH values; at pH 1.2 coated and uncoated concentrations became comparable within 30-60 min (discussion: after approximately 30 min), while at pH 4.0 a difference remained for an extended period (discussion: greater than 60 min) [rests on: R11, R12] | p.598; p.602 |
| C27 | claim, conclusion, authors: "in line with expectations" | Leaching was greater at 50% than at 25% DL, in line with the drug/polymer ratio, as more drug is at the surface [rests on: R10, R16, R17; cited: refs 32, 33, 54] | p.599 |

## 2023 Nguyen — Enteric coating of tablets containing an amorphous solid dispersion of an enteric polymer and a weakly basic drug: A strategy to enhance in vitro release · Dissolution / B. Supersaturation from ASD dissolution

[2023-nguyen-enteric-coating-delamanid-hpmcp-asd-release](../../../cards/2023-nguyen-enteric-coating-delamanid-hpmcp-asd-release/paper.html) · Dissolution / B. Supersaturation from ASD dissolution · measured · as: drug leaching

| id | kind | content | locator |
|---|---|---|---|
| R2 | record, measured or cited per row | drug concentration in gastric medium at 60 min and after pH shift plus 30 min (µg/mL; complete = 100) — uncoated tablets of 25% DL ASDs, pH-shift test (P11) — sub-table below; text (discussion): release from DLM ASD tablets of ~40, ~1 and ~7 µg/mL at pH 1.6, 3.0 and 5.0 | Fig. 1B, p.4; text p.8 |
| R9 | record, measured | drug in medium and release after coating failure — coated tablets after loss of coating integrity at pH 4.5-5.0 — drug leaching < 5 µg/mL (Table S3) and/or crystallization; notably reduced release upon transition to a higher-pH medium (Fig. S3); no values printed in the main text | text p.4, p.9 (Table S3, Fig. S3, not supplied) |
| C35 | claim, generalisation, authors: asserted ("Thus") | Weakly basic drugs partially release from enteric-polymer ASDs at low pH because the drug is molecularly dispersed in the polymer, and the extent rises with drug loading; a continuous enteric coating on a tablet or particle prevents gastric release [rests on: cited: refs 12, 35, 44, 68; R2, R10] | p.8 |