Self-microemulsifying Drug Delivery System Improved Oral Bioavailability of 20(<i>S</i>)-Protopanaxadiol: From Preparation to Evaluation
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- Wang Bing
- Experiment Center of Teaching and Learning, Shanghai University of Traditional Chinese Medicine
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- Pu Yiqiong
- Experiment Center of Teaching and Learning, Shanghai University of Traditional Chinese Medicine
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- Xu Benliang
- Experiment Center of Teaching and Learning, Shanghai University of Traditional Chinese Medicine
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- Tao Jiansheng
- Experiment Center of Teaching and Learning, Shanghai University of Traditional Chinese Medicine
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- Wang Yuqin
- Shanghai BioAsia Life Technology Co., Ltd.
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- Zhang Tong
- Experiment Center of Teaching and Learning, Shanghai University of Traditional Chinese Medicine
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- Wu Peiying
- Experiment Center of Teaching and Learning, Shanghai University of Traditional Chinese Medicine Shanghai Xingling Science and Technology Pharmaceutical Co., Ltd.
Bibliographic Information
- Other Title
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- Self-microemulsifying Drug Delivery System Improved Oral Bioavailability of 20(S)-Protopanaxadiol : From Preparation to Evaluation
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Description
20(S)-Protopanaxadiol (20(S)-PPD) is one type of sapogenin of protopanaxadiols and has a variety of pharmacological activities. In order to improve the dissolution of 20(S)-PPD as well as its oral bioavailability, a self-microemulsifying drug delivery system (SMEDDS) was utilized for 20(S)-PPD preparation. Following the preparation of the 20(S)-PPD SMEDDS, its dissolution, stability, and intestinal absorption in rats were studied, and the pharmacokinetics and optimal dosage after oral administration were evaluated. The dissolution tendency of the SMEDDS in phosphate buffered saline (PBS), 0.1 M HCl and distilled water was consistent. SMEDDS was stable under a condition of high temperature (40°C), high humidity or with strong light irradiation, or within 6 h in artificial digestive tracts. 20(S)-PPD SMEDDS was well-absorbed in all intestinal segments in rats. When the drug concentration was higher than 200 µg/mL or the perfusion flow was faster than 0.5 mL/min, passive diffusion of drug in the duodenum reached a saturated level. In addition, P-glycoprotein inhibitor did not affect the intestinal absorption of 20(S)-PPD SMEDDS. Pharmacokinetic study showed that Tmax in male rats was shortened significantly, while Cmax and area under the curve (AUC(0–t)) were remarkably increased. The relative oral bioavailability of 20(S)-PPD SMEDDS was increased approximately three fold compared with the 20(S)-PPD carboxy methyl cellulose (CMC). 20(S)-PPD SMEDDS (100 mg/mL) was administered by gastric infusion to both mice and rats for 14 d. SMEDDS improved the oral bioavailability of 20(S)-PPD and reduced the necessary drug dosage. 20(S)-PPD SMEDDS could become a promising clinical alternative as an anti-tumor or antidepressant drug.
Journal
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- Chemical and Pharmaceutical Bulletin
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Chemical and Pharmaceutical Bulletin 63 (9), 688-693, 2015
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390282679153975808
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- NII Article ID
- 130005096034
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- NII Book ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL BIB ID
- 026699970
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- PubMed
- 26084568
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed