Dissolution test of various low-dose acetylsalicylic acid preparations marketed in Indonesia
Aim To compare the dissolution profi les of various enteric-coated low-dose acetylsalicylic acid (ASA) tabletsÂ marketed in Indonesia.
Methods The dissolution study was carried out according to US Pharmacocopoeiae (USP) /European Pharmacopoeiae,Â method A, using USP apparatus 1 (basket) 100 rpm, with 2 media: 0.1 N HCl, 120 minutes for acid stage, and phosphateÂ buffer pH 6.8, 90 minutes for buffer stage. The sampling points were 120 minutes for the acid stage, and every 10 minutesÂ until 90 minutes for the buffer stage. The acetylsalicylic acid was assayed using spectrophotometry at 280 nm for the acidÂ stage, and at 265 nm for the buffer stage. The free salicylic acid was determined only at the end of the buffer stage with HPLCÂ method. There were 6 test products (Cardio AspirinÂ® 100 mg, AptorÂ® 100 mg, AscardiaÂ® 80 mg, Thrombo AspiletÂ® 80 mg,Â AstikaÂ® 100 mg and FarmasalÂ® 100 mg), 3 batches for each product, and 6 units for each batch.
Results The amount of ASA released from each ASA product tested at the end of acid stage (120 minutes) ranged fromÂ 1.79% for Cardio AspirinÂ® to 6.92% for Thrombo AspiletÂ®, all conformed to the compendial requirement for enteric-coatedÂ product (< 10%). The amount of salicylic acid observed at the end of the dissolution test ranged from 3.47% for CardioÂ AspirinÂ® to 10.90% for AstikaÂ® and 11.90 % for Thrombo AspiletÂ®. Thrombo AspiletÂ® showed sustained-release properties,Â causing high variability in ASA release, such that one of the 3 batches tested did not fulfill the compendial requirementÂ of more than 75% (the release was only 55.11%). High variability in ASA release between batches was also found withÂ FarmasalÂ® at 10, 20, and 30 minutes in buffer medium. The lowest effective dose of ASA as an antiplatelet drug for longtermÂ use is 75 mg of plain ASA, and this is equivalent to 100 mg of enteric-coated ASA.
Conclusions All of the low-dose ASA preparations marketed in Indonesia are enteric-coated products, while ThromboÂ AspiletÂ® is not only an enteric-coated but also a sustained-release product. Cardio AspirinÂ®, followed by AptorÂ®, hasÂ the right dose for low-dose enteric-coated preparation (100 mg), produces consistent ASA release between batches,
and the most stable towards deacetylation (antiplatelet inactivation). (Med J Indones 2009;18:159-64)
Key words: Dissolution profile, enteric coated, deacetylation
Copyright (c) 2009 Yeyet C. Sumirtapura, Arini Setiawati, Jessie S. Pamudji, Heni Rachmawati
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with Medical Journal of Indonesia agree to the following terms:
- Authors retain copyright and grant Medical Journal of Indonesia right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial License that allows others to remix, adapt, build upon the work non-commercially with an acknowledgment of the work’s authorship and initial publication in Medical Journal of Indonesia.
- Authors are permitted to copy and redistribute the journal's published version of the work non-commercially (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in Medical Journal of Indonesia.