Translated Abstract
Acetaminophen is the first therapeutic drug in treatment of fever and analgesic. However, due to the short biological half-life, the general oral solid preparations are inconvenience to the patient because of taking repeatedly. Acetaminophen bilayer extended release tablets are composed of the rapid release layer （RRL） and sustained release layer（SRL）. After taking the medicine, acetaminophen of the RRL dissolve fast, immediately relief the symptoms of fever and analgesic, and the SRL slowly release the acetaminophen, which have long-term effect to the fever and body-aches. So the Acetaminophen bilayer extended release tablets have a advantage of reducing the frequency of the patient‘s medication. In this research, using paracetamol sustained-release tablet of Shanghai Johnson Pharmaceutical Co., Ltd. as the reference preparations, developed a large-scale production processes and quality standards for acetaminophen sustained-release tablets. This research can ease market demand of the this medicine, reduce the cost of treatment, improve patient compliance with therapy and patient‘s life quality. More important it can get good clinical efficacy and safety.During the prescription screening and parameter optimizing. The study determines formulation of the RRL by studying different kinds and amount of the disintegrant, using disintegration time as evaluation. Meanwhile, finding the slow release material type and amount of the SRL by analyzing the release curve trend in dissolving medium. In the next step the ratio between the RRL and SRL is confirmed through experiment by the release curve of the double sustained-release tablets. In the production process research part, the particle size of API, granulation time, the sequence of tablet compressed, tablet hardness and moisture range of particles are all optimized. The results shown that the F2 release factor of the sample and the reference formulation is more than 50 in five release mediums, the equations are the same. This indicates that the sample have good similarity release behavior compared to the reference preparations .In the quality research, the standard of acetaminophen sustained-release tablet is developed. An analytical method for the determination of Acetaminophen and its related substances p-Aminophenol，p-Chloroacetanilide in acetaminophen sustained-release tablet was validated.. The results showed that the anlytical method is accurate, sensitive and stable. Under the condtions of aluminum - plastic pack，long term and accelerate stability test were conducted. The results indicated all measures in the examinations accord with the standard.By comprising with the reference preparations The results shown that the processes had been proved reasonable and stable. The quality of sample and the reference preparations are uniform.
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