Gastric floating tablet improves the bioavailability and reduces the hypokalemia effect of gossypol in vivo
| Autor: | Hao Liu, Chenyun Gan, Jingjing Chen, Sijiao Wang, Houyin Shi, Yue Hu, Mengwu Zhang, Xingyu Qu, Ruirui Zhang, Kunyan Qu, Xinyu Shi, Weiling Zeng |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Bioavailability
Pharmaceutical Science 02 engineering and technology Adverse effect 030226 pharmacology & pharmacy Dosage form 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Pharmacokinetics Ethyl cellulose Gastric floating tablet Magnesium stearate Pharmacology Sodium bicarbonate Chromatography Gossypol 021001 nanoscience & nanotechnology chemistry Methyl cellulose Original Article 0210 nano-technology Sustained release |
| Zdroj: | Saudi Pharmaceutical Journal : SPJ |
| ISSN: | 2213-7475 1319-0164 |
| Popis: | 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. In vivo 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 in vivo 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. |
| Databáze: | OpenAIRE |
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