Purpose

As per the Japanese or SUPAC guidance to maintain formulation composition similarity across tablet strengths, the coating should be applied based on the core tablet surface area or weight, respectively. These two coating approaches were compared by evaluating protective effects of coating on the light stability of three model compounds.

Methods

Core tablets of three light sensitive drugs, nifedipine, rosuvastatin calcium, and montelukast sodium were coated either with PVA-based Opadry® II white or Opadry® II beige. The coated tablets were exposed to light up to three ICH cycles.

Results

For Opadry® II white, the surface area based coating provided consistent light protection across tablet strengths when the coating amount was more than 0.1 mg/mm² compared to that based on core tablet weights. For Opadry® II beige, both approaches gave comparable and better light protection due to presence of iron oxides. The light protection by Opadry® II white could be because of physical barrier of coating, which was uniform across the strengths when it was based on core tablet surface area.

Conclusion

For a routine tablet formulation development with Opadry color coating, it does not matter whether the coating is applied based on the core tablet surface area or weight.

中文翻译：

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为了保持不同强度的包衣片剂的配方组成相似性：包衣应基于片剂的重量或表面积？

目的

根据日本或SUPAC指南，要保持片剂强度在片剂强度之间的相似性，应分别根据片剂芯的表面积或重量来涂覆包衣。通过评估涂层对三种模型化合物的光稳定性的保护作用，比较了这两种涂层方法。

方法

三种光敏药物（硝苯地平，瑞舒伐他汀钙和孟鲁司特钠）的核心片剂均涂有基于PVA的Opadry®II白色或Opadry®II米色。将包衣的片剂暴露于多达三个ICH循环。

结果

对于Opadry®II白色，与基于核心片剂重量的涂层量相比，当涂层量大于0.1 mg / mm ²时，基于表面积的涂层可在整个片剂强度上提供一致的光线保护。对于Opadry®II米色，由于存在氧化铁，因此两种方法都能提供可比的更好的光保护。Opadry®II白色对光的保护可能是由于涂层的物理屏障，当基于片剂芯的表面积时，涂层在所有强度上都是均匀的。

结论

对于使用欧巴代（Opadry）彩色包衣进行的常规片剂配方开发，是否根据芯片剂的表面积或重量来施加包衣都没有关系。