Drug Delivery and Therapeutic Impact of extended-release Acetylsalicylic Acid

Figures & data

Figure 1. Recovery of platelet aggregation and thromboxane A₂ production after immediate-release acetylsalicylic acid administration.

(A) Arachidonic acid-induced platelet aggregation and (B) TxB₂ production in healthy volunteers and patients with cardiovascular disease after a single dose of IR-ASA 75 mg. Platelet aggregation was measured using the Multiplate^® Analyzer (Roche Diagnostics International LDT, Rotkreuz, Switzerland), which detects differences in electric resistance between two electrodes in aggregated whole blood. Platelet aggregation was stimulated by arachidonic acid 1.0 mM and collagen 3.2 µg/ml. Serum TxB₂ concentrations were measured using an ELISA (Cayman Chemical, Ann Arbor, MI, USA). Platelet aggregation and TxB₂ production were significantly greater 24 h after ASA dosing compared with 1 h post-treatment.

ASA: Acetylsalicylic acid; CAD: Coronary artery disease; ST: Stent thrombosis; TxB₂: Thromboxane B₂.

Reproduced with permission from [61].

Figure 2. Micropump^® (Flamel Technologies SA, Pessac, France) delivery platform for extended-release acetylsalicylic acid.

Each extended-release capsule contains a core of release rate-limiting, film-coated microcapsules containing 162.5 mg of ASA.

ASA: Acetylsalicylic acid.

Figure 3. Characteristic diffusion-based dissolution profile based on Fick’s second law.

Figure 4. Pharmacokinetics of extended-release acetylsalicylic acid.

(A) Mean concentration time profiles of single-dose ASA for ER-ASA and IR-ASA; and (B) single-dose mean concentration time profiles of SA for ER-ASA and IR-ASA.

ASA: Acetylsalicylic acid; ER: Extended release; IR: Immediate release; SA: Salicylic acid.

Data taken from [75].

Figure 5. Antiplatelet effects of a single dose of extended-release acetylsalicylic acid.

(A) Mean percent inhibition of TxB₂ production and (B) 11-dehydro-TxB₂ after single-dose exposure to ER-ASA 162 mg and IR-ASA 81 mg in healthy volunteers. ER-ASA provides 24-h reduction of TxB₂ production.

ASA: Acetylsalicylic acid; ER: Extended release; IR: Immediate release; TxB₂: Thromboxane B₂.

Data taken from [75].

Figure 6. Inhibition of prostacyclin levels^† in healthy volunteers with extended-release acetylsalicylic acid 162.5 mg/day for 10 days.

Mean vascular prostacyclin levels were not reduced after multiple extended-release acetylsalicylic acid administrations.

^†Mean urine excretion level of 6-keto prostaglandin F1α is a surrogate marker for vascular prostacyclin level

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