Liu Hao, Wang Sijiao, Shi Houyin, Zhang Ruirui, Qu Kunyan, Hu Yue, Qu Xingyu, Gan Chenyun, Chen Jingjing, Shi Xinyu, Zhang Mengwu, Zeng Weiling
School of Pharmacy, Southwest Medical University, Luzhou City, Sichuan, People's Republic of China.
Department of Orthopedics, The Affiliated Traditional Chinese Medicine Hospital of Southwest Medical University, Luzhou City, Sichuan, People's Republic of China.
Saudi Pharm J. 2021 Apr;29(4):305-314. doi: 10.1016/j.jsps.2021.03.001. Epub 2021 Mar 14.
Gossypol (Gos) is a natural polyphenolic compound that has shown a number of valuable biological properties such as antifertility, antioxidation, and antitumor activities. However, the clinical application of Gos has been hindered by its notable adverse effects such as hypokalemia, hemolytic anemia, and so on. Using sustained-release dosage form provides a hopeful solution to this problem. In this study, a gastric floating tablet for sustained-release of Gos (Gos-GFT) was developed using polyvinylpyrrolidone, hydroxypropyl methyl cellulose, ethyl cellulose, lactose, sodium bicarbonate, and magnesium stearate. Gos-GFT had an average weight of around 200 mg with a drug content percentage of around 13.66%. The physicochemical properties of Gos-GFT satisfied the pharmacopoeial requirements for tablets. Gos-GFT was able to float in an acidic medium and had a sustained drug release for over 12 h. studies showed that the relative bioavailability of Gos-GFT, as compared with Gos powders, was larger than that of a non-gastric floating tablet which was a dosage form used for comparison with Gos-GFT. Furthermore, compared with the Gos powders and the non-gastric floating Gos tablets, Gos-GFT could prolong the action time of Gos, and significantly relieve hypokalemia which is a major adverse effect of Gos. These properties made Gos-GFT a promising Gos preparation that warrants further investigation for more extensive clinical applications of this natural compound.
棉酚是一种天然多酚化合物，已显示出多种有价值的生物学特性，如抗生育、抗氧化和抗肿瘤活性。然而，棉酚的临床应用受到其显著不良反应的阻碍，如低钾血症、溶血性贫血等。使用缓释剂型为解决这一问题提供了一个有希望的解决方案。在本研究中，使用聚乙烯吡咯烷酮、羟丙基甲基纤维素、乙基纤维素、乳糖、碳酸氢钠和硬脂酸镁研制了一种用于棉酚缓释的胃漂浮片（Gos-GFT）。Gos-GFT的平均重量约为200毫克，药物含量百分比约为13.66%。Gos-GFT的理化性质符合片剂的药典要求。Gos-GFT能够在酸性介质中漂浮，并具有超过12小时的药物缓释效果。研究表明，与棉酚粉末相比，Gos-GFT的相对生物利用度高于作为与Gos-GFT对比剂型的非胃漂浮片。此外，与棉酚粉末和非胃漂浮棉酚片相比，Gos-GFT可以延长棉酚的作用时间，并显著缓解棉酚的主要不良反应低钾血症。这些特性使Gos-GFT成为一种有前景的棉酚制剂，值得进一步研究以实现这种天然化合物更广泛的临床应用。
