The formation of an inclusion complex between a metabolite of ginsenoside, compound K and γ-cyclodextrin and its dissolution characteristics

Igami, Kentaro; Ozawa, Masanao; Inoue, S.; Iohara, Daisuke; Miyazaki, Toshitsugu; Shinoda, Masamitsu; Anraku, Makoto; Hirayama, Fumitoshi; Uekama, Kaneto

doi:10.1111/jphp.12468

Cited by 23 publications

(13 citation statements)

References 13 publications

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“…Mean plasma concentrations vs time profiles after oral administration of BCL and the inclusion complex were shown in Figure b, and the primary pharmacokinetic parameters were summarized in Table . The fast‐dissolving property of the inclusion complex was reflected in the absorption, that is, the inclusion complex had an significant increase at AUC 0– t , AUC 0–∞ and C max , and a faster at T max and t 1/2 , in agreement with the reported data . AUC 0– t and AUC 0–∞ of the inclusion complex group were 2.65 and 2.53 times higher than those of the free BCL suspension group, respectively, suggesting that the relative oral bioavailability of BCL in inclusion complex increased by about two times .…”

Section: Resultssupporting

confidence: 88%

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Jiang

Deng

et al. 2017

Journal of Pharmacy and Pharmacology

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Section: Resultssupporting

confidence: 88%

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Jiang

Deng

et al. 2017

Journal of Pharmacy and Pharmacology

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“…The FG and non‐FG were provided by NAGASE Beauty Care (Tokyo, Japan). FG was produced by fermenting a 15% ginseng ( Panax ginseng , C. A. Meyer, Araliadea) mixture with Lactobacillus paracasei A221 (2%, 1010 c.f.u./mL) in culture medium for 10 days at 28°C . Following fermentation, the culture medium was sterilized for 10 min at 121°C and spray‐dried.…”

Section: Methodsmentioning

confidence: 99%

Effect of Lactobacillus paracasei A221‐fermented ginseng on impaired spatial memory in a rat model with cerebral ischemia and β‐amyloid injection

Nagao

Yamano

Imagawa

et al. 2019

Traditional & Kampo Medicine

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Aim: Ginseng, a traditional herbal medicine, has been shown to prevent the progression of dementia, but its therapeutic effects vary because ginseng's components must first be activated by intestinal bacteria before being absorbed into the blood. We therefore focused on a fermented ginseng (FG), which contains activated components prepared by Lactobacillus paracasei A221, and compared its effects with those of non-FG. In this study, we investigated whether FG is effective on spatial memory impairment in rats. Methods: Rats with spatial memory impairment were prepared with transient cerebral ischemia and intraventricular injection of β-amyloid 1-42 for 7 days (CI + Aβ). Oral FG or non-FG was given for 7 days after the cerebral ischemia. Spatial memory was evaluated using the Morris water maze (MWM). We observed neuronal neuclei-positive cells to assess hippocampal neuron loss, and investigated the protein expression of caspase-3 and cleaved caspase-3 for neuronal apoptosis, ionized calciumbinding adapter molecule 1 (Iba-1) for microglia, and glial fibrillary acidic protein for astrocytes. Results: FG treatment in the CI + Aβ-operated rats shortened the extended time to reach the platform in the MWM, whereas non-FG treatment did not affect the extended time. FG ameliorated loss of hippocampal cornu amonis (CA)1 neurons and the increase in caspase-3 and Iba-1 in the CI + Aβ-operated rats. Conclusion: FG improved spatial memory impairment in CI + Aβ-operated rats. The effect of FG might be attributed to the amelioration of apoptotic neuronal cell death and the inactivation of microglia. FG is a more useful treatment for patients with cognitive dysfunction than non-FG.

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“…The compound-complex (K/γ-CyD, 1:1) displayed a faster dissolution rate compared to K/γ-CyD complex at 1:3 ratios. The study concluded that partial inclusion complexes are more advantageous for improving the solubility of CK compared to complete inclusion [ 21 ].…”

Section: Pharmacokinetics Metabolism and Safety Of Compound Kmentioning

confidence: 99%

Ginsenoside Compound K: Insights into Recent Studies on Pharmacokinetics and Health-Promoting Activities

Sharma

Lee

2020

Biomolecules

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Ginseng (Panax ginseng) is an herb popular for its medicinal and health properties. Compound K (CK) is a secondary ginsenoside biotransformed from major ginsenosides. Compound K is more bioavailable and soluble than its parent ginsenosides and hence of immense importance. The review summarizes health-promoting in vitro and in vivo studies of CK between 2015 and 2020, including hepatoprotective, anti-inflammatory, anti-atherosclerosis, anti-diabetic, anti-cancer, neuroprotective, anti-aging/skin protective, and others. Clinical trial data are minimal and are primarily based on CK-rich fermented ginseng. Besides, numerous preclinical and clinical studies indicating the pharmacokinetic behavior of CK, its parent compound (Rb1), and processed ginseng extracts are also summarized. With the limited evidence available from animal and clinical studies, it can be stated that CK is safe and well-tolerated. However, lower water solubility, membrane permeability, and efflux significantly diminish the efficacy of CK and restrict its clinical application. We found that the use of nanocarriers and cyclodextrin for CK delivery could overcome these limitations as well as improve the health benefits associated with them. However, these derivatives have not been clinically evaluated, thus requiring a safety assessment for human therapy application. Future studies should be aimed at investigating clinical evidence of CK.

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The formation of an inclusion complex between a metabolite of ginsenoside, compound K and γ-cyclodextrin and its dissolution characteristics

Abstract: The effect of γ-CyD on enhancing the solubility of compound K is much higher than that for the β-CyD complex, and the dissolution rate of the guest when it is partially included in the γ-CyD is faster the corresponding value when it is completely included in the cavity.

Cited by 23 publications

References 13 publications

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

The formation of a host-guest inclusion complex system between β-cyclodextrin and baicalin and its dissolution characteristics

Effect of Lactobacillus paracasei A221‐fermented ginseng on impaired spatial memory in a rat model with cerebral ischemia and β‐amyloid injection

Ginsenoside Compound K: Insights into Recent Studies on Pharmacokinetics and Health-Promoting Activities

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