Study Of Manufacturing Technique And Quality Evaluation For Acetaminophen Sustained-release Tablets

Acetaminophen, which is the aniline derivatives, is one of the preferred antipyreticanalgesics in clinic. It is widely used in medical field for lower price and the advantage of safeand effective. But it is inconvinient for its shorter half-life and limited effective time, thepatients have to take it many times daily. Slow-release technology based on the double layertablet, which the faster-released layer can release quickly to reach the effective bloodconcentration while slow-released layer release slowly to sustain continuous smooth effect, getmore and more attention and be used in sustained release pharmaceutical preparations nowadays.The combination of both above is greatly beneficial to patients with the convenience and safetyof the drug, enrich the domestic acetaminophen preparation market, and reducing the costs ofmedication.Double-layer slow-release technology of acetaminophen were conducted in this research.The process was divided into three parts, including preformulation study, prescription andprocess research, quality evaluation.Preformulation study focused on the establishment of the analytical method in vitroand thephysical and chemical properties of acetaminophen.The content and release degree weredetermied by ultraviolet analysis, through the methodology validation can guarantee the methodcould meet the requirement of testing. The results of physical and chemical propertiesmeasurements indicated that acetaminophen is a lipotropy drugs with stable property,complementary makings almost has no effect on it, and it has the good solubility at pH1.68~6.86.Layered analysis was used for prescription and process researching. The finally processwas that croscarmellose sodium2.6%for disintegrating agent，microcrystalline cellulose3.9%for filler to be instant-release layer; hydroxypropyl methylcellulose K100LV4.5%andhydroxypropyl methylcellulose K4M1.1%for sustained-release material, microcrystallinecellulose3.9%as filler, pressure of tabletting is11kg for sustained-release layer. Homemadeacetaminophen sustained-release tablets were compare to onsell Tylenol for releasing rate, theyhave the similar results, and the former released more uniformly..The character, identification,release degree, difference of piece weight and the content ofthree batches homemade samples were checked, meanwhile the stress testing and acceleratedtest, I reference national standards of Paracetamol Sustained-Release Tablets,the results confirmed meet the requirements.