Preparing of aspirin sustained-release granules by hot-melt granulation and micro-crystal coating |
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Authors: | Ran Li Tian Yin Yu Zhang Jingxin Gou Xing Tang |
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Affiliation: | 1. School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China;2. School of Functional food and Wine, Shenyang Pharmaceutical University Shenyang, Shenyang, China |
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Abstract: | In this work, aspirin (ASP) sustained granules were prepared using micro-crystal coating and hot-melt granulation, respectively. In the process of micro-crystal coating, PVP was used to form the isolation layer and then coated with either Eudragit RS/RL30D or ethyl cellulose (EC) as sustained-release layers to prepare sustained granules (the granules from this method were denoted m-cG). And in the process of hot-melt granulation, the granules were obtained with stearyl alcohol as a binder and EC as matrix material to prepare sustained granules (the granules were denoted h-mG). The in vitro release of ASP sustained-release granules was investigated by dissolution apparatus and the stability of the granules was studied. Since both methods effectively prevented the hydrolysis of ASP, the sustained granules by micro-crystal coating and hot-melt granulation were stable. However, there was a clear difference in the in vitro release of h-mG and m-cG. The h-mG was completely released in 4?h, while the m-cG with EC as sustained-release layer released 80% in 24?h and the m-cG with the Eudragit RS/RL 30?D as sustained-release layer released completely in 5?h. The results showed that micro-crystal coating was more suitable for the preparation of ASP sustained granules, and the granules with EC as sustained layer could achieve a better sustained-release effect. |
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Keywords: | Aspirin sustained-release stability in vitro release hot-melt granulation micro-crystal coating |
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