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Development of Fast Disintegrating Tablets Containing Loxoprofen Sodium by HYDROFLASH Manufacturing Method
Chemical & Pharmaceutical Bulletin ( IF 1.7 ) Pub Date : 2024-01-01 , DOI: 10.1248/cpb.c23-00520
Aya Kuwata 1 , Tetsuo Ono 2 , Yuri Tsuchiya 2 , Etsuo Yonemochi 1
Affiliation  

In order to create and offer superior pharmaceuticals for consumers who wish to be relieved of headache and fever as soon as possible, we established HYDROFLASH manufacturing method that enables us to offer fast disintegration tablets containing loxoprofen sodium (LX), which are difficult to disintegrate. As a result of screening excipients, tablets using mannitol showed the fastest disintegration time, about 2 min. From the result of viscosity measurement, we found that LX produced higher viscosity when dissolved in water. This suggests that tablets containing LX disintegrate slower by inhibiting the penetration of water into the tablet due to the viscosity caused of LX. Therefore, we created a manufacturing method to make it easy for water to penetrate the tablet. It is possible to achieve fastest disintegration in about 30 s for tablets containing LX by granulating in a fluidized-bed with spraying of the dispersion of light anhydrous silicic acid (LASA). LX-containing tablets manufactured by the HYDROFLASH method disintegrated immediately after contact with water. Furthermore, it was observed that LASA was uniformly dotted on the surface of tablets by HYDROFLASH method, compared with other manufacturing methods. We considered that by fluidized-bed granulation with LASA dispersion (HYDROFLASH manufacturing method), water permeates through LASA on the tablet surface regardless of viscosity of LX. Futhermore, LX-containing tablets by the HYDROFLASH method showed that the dissolution rate of LX was nearly 100% at 5 min after starting the test. We considered that the initial dissolution became faster because of the fast disintegration.

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中文翻译:

HYDROFLASH制备法开发洛索洛芬钠快速崩解片

为了为希望尽快缓解头痛和发烧的消费者创造和提供优质药品,我们建立了 HYDROFLASH 制造方法,使我们能够提供含有难以崩解的洛索洛芬钠 (LX) 的快速崩解片。筛选辅料的结果显示,使用甘露醇的片剂崩解时间最快,约为 2 分钟。从粘度测量结果来看,我们发现LX溶解在水中时产生更高的粘度。这表明,由于LX引起的粘度,通过抑制水渗透到片剂中,含有LX的片剂崩解得更慢。因此,我们创造了一种使水易于渗透片剂的制造方法。通过在流化床中喷洒轻质无水硅酸(LASA)分散体进行造粒,可以在约 30 秒内实现含 LX 片剂的最快崩解。通过 HYDROFLASH 方法制造的含 LX 的片剂在与水接触后立即崩解。此外,与其他制造方法相比,观察到通过 HYDROFLASH 方法,LASA 均匀地点在片剂表面。我们认为,通过使用 LASA 分散体的流化床造粒(HYDROFLASH 制造方法),无论 LX 的粘度如何,水都会透过片剂表面的 LASA 渗透。此外,通过HYDROFLASH法测定含LX的片剂表明,在开始测试后5分钟,LX的溶出率接近100%。我们认为,由于崩解速度快,初始溶解变得更快。

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更新日期:2024-01-03
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