Administration-Route Dependency of Absorption of Glycyrrhizin in Rats: Intraperitoneal Administration Dramatically Enhanced Bioavailability.

Yamamura, Yoshikazu; Santa, Tomofumi; Kotaki, Hajime; Uchino, Katsuyoshi; Sawada, Yasufumi; Iga, Tatsuji

doi:10.1248/bpb.18.337

Cited by 63 publications

(40 citation statements)

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“…In the experiment by Hase et al (1999), GL was orally administered twice at 18 and 2 h before intoxication. It has been reported that an oral administration of GL did not inhibit serum ALT elevation because of the poor absorption of GL from the intestinal tract (Yamamura et al, 1995). The discrepancy between the present results and theirs may be due to variances in the manner of administration.…”

Section: Discussioncontrasting

confidence: 94%

The inhibition of apoptosis by glycyrrhizin in hepatic injury induced by injection of lipopolysaccharide / D-galactosamine in mice

Ikeda

Abe²,

Kuroda

et al. 2008

Archives of Histology and Cytology

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Section: Discussioncontrasting

confidence: 94%

The inhibition of apoptosis by glycyrrhizin in hepatic injury induced by injection of lipopolysaccharide / D-galactosamine in mice

Ikeda

Abe²,

Kuroda

et al. 2008

Archives of Histology and Cytology

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“…During this period, the average particle size was approximately 300 nm, and the size distribution was 135-421 nm (10 to 90% interval of particle size), guaranteeing pharmaceutical stability of the GZ emulsion. The next step was to investigate the release profile of GZ from the w/o emulsion, because the sustained release of GZ from the w/o emulsion is important for reducing the frequency of hospital visits, and thus elevating patient QOL.Pharmacokinetic studies of GZ were investigated in detail in human, 12,13) rodent (rat), [14][15][16] and other species. The elimination half-life of GZ in chronic hepatitis patients after infusion of GZ (80 mg) is 4.4-4.7 h in serum.…”

mentioning

confidence: 99%

“…Pharmacokinetic studies of GZ were investigated in detail in human, 12,13) rodent (rat), [14][15][16] and other species. The elimination half-life of GZ in chronic hepatitis patients after infusion of GZ (80 mg) is 4.4-4.7 h in serum.…”

mentioning

confidence: 99%

Utility of Nano-Sized, Water-in-Oil Emulsion as a Sustained Release Formulation of Glycyrrhizin

Koga

Nishimon

Ueta

et al. 2011

Biological & Pharmaceutical Bulletin

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Glycyrrhizin (GZ) is the main constituent of Glycyrrhiza glabra L. and chemically is the glycoside of glycyrrhetic acid. In addition to having anti-allergic, anti-inflammatory, and anti-hepatitis properties, GZ has interferon-inducing properties.1-3) Although oral (25 mg/tablet) and intravenous (2 mg/ml GZ solution containing glycine and L-cysteine) formulations are commercially used in Japan, the intravenous formulation is more effective for chronic hepatitis therapy. [4][5][6] This is because GZ is poorly absorbed from the intestinal tract, 7) as GZ is hydrolyzed by b-glucuronidase in the large intestine.8) The intravenous formulation is administered 2 or 3 times per week over a prolonged period. Frequent hospital visits and pain from repeated intravenous injections are inconvenient, which directly results in reduced quality of life (QOL) for chronic hepatitis patients. Therefore, the development of a more patient-oriented formulation would be tremendously beneficial. Moreover, a patientoriented formulation would likely increase compliance.To address these issues and to reduce the unpleasant side effects of GZ, various type formulations were developed for oral, 9) rectal, 10) and nasal 10) administrations. However, each the bioavailability of GZ after the administration of non-vascular type formulations in dogs or rats was in the range of 2.4 to 20.2%.9,10) Namely, non-vascular route is inconvenient to improve the bioavailability of GZ. Therefore, we focused the subcutaneous administration to enhance the GZ bioavailability and to sustain the therapeutic effect of GZ. Previously, the preparation methods and phase behavior stability of a nanosized water-in-oil (w/o) emulsion encapsulating GZ have been reported. 11) Briefly, a 400-mg/ml GZ solution was dispersed into an oil phase (soybean oil and condensed ricinoleic acid tetraglycerin ester) using a Polytron. The solution was then evaporated until the water content in the emulsion reached approximately 9% (w/w).11) The dispersion properties of the nano-sized w/o emulsion were maintained at a constant level for 2 months. During this period, the average particle size was approximately 300 nm, and the size distribution was 135-421 nm (10 to 90% interval of particle size), guaranteeing pharmaceutical stability of the GZ emulsion. The next step was to investigate the release profile of GZ from the w/o emulsion, because the sustained release of GZ from the w/o emulsion is important for reducing the frequency of hospital visits, and thus elevating patient QOL.Pharmacokinetic studies of GZ were investigated in detail in human, 12,13) rodent (rat), [14][15][16] and other species. The elimination half-life of GZ in chronic hepatitis patients after infusion of GZ (80 mg) is 4.4-4.7 h in serum.17) The elimination half-life of GZ in rats after the intravenous administration (20-50 mg/kg) is approximately 2-4 h in plasma.18,19) GZ is rapidly excreted into bile via multidrug resistance-associated protein 2 (MRP2) ATP-binding cassette transporter C2 (ABCC2) transporter. 20) C...

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“…Bioavailability (BA) of GZ was determined by the ratio of AUC after rectal administration to that after i.v. administration cited from the reference; 12) plasma GZ concentration vs. time data after i.v. administration of GZ 50 mg/kg dose to rats.…”

mentioning

confidence: 99%

“…12) and rectal administrations. Morphologic Observation At the end of in vivo absorption study, the bottom, ca.…”

mentioning

confidence: 99%

Preparation and Rectal Absorption of Highly Concentrated Glycyrrhizin Solution

Koga

Kawashima

Shibata

et al. 2003

Biological & Pharmaceutical Bulletin

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Administration-Route Dependency of Absorption of Glycyrrhizin in Rats: Intraperitoneal Administration Dramatically Enhanced Bioavailability.

Cited by 63 publications

References 0 publications

The inhibition of apoptosis by glycyrrhizin in hepatic injury induced by injection of lipopolysaccharide / D-galactosamine in mice

The inhibition of apoptosis by glycyrrhizin in hepatic injury induced by injection of lipopolysaccharide / D-galactosamine in mice

Utility of Nano-Sized, Water-in-Oil Emulsion as a Sustained Release Formulation of Glycyrrhizin

Preparation and Rectal Absorption of Highly Concentrated Glycyrrhizin Solution

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