In Situ Intestinal Absorption Behaviors of Tanshinone IIA from Its Inclusion Complex with Hydroxypropyl-.BETA.-cyclodextrin

Wang, Ling; Rui, Li Chen; Hua, Jiang

doi:10.1248/bpb.30.1918

Cited by 16 publications

(5 citation statements)

References 23 publications

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“…ÀKat , where Q represents the remaining berberine detected in the perfusate at each sampling time, t is the time of circulation of the perfusate, Q 0 is the calculated amount at zero time, and K a is the absorption rate constant of the drug (15).…”

Section: Discussionmentioning

confidence: 99%

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Enhancement of Sodium Caprate on Intestine Absorption and Antidiabetic Action of Berberine

Zhang

et al. 2010

AAPS PharmSciTech

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Abstract. Berberine, a plant alkaloid used in traditional Chinese medicine, has a wide spectrum of pharmacological actions, but the poor bioavailability limits its clinical use. The present aim was to observe the effects of sodium caprate on the intestinal absorption and antidiabetic action of berberine. The in situ, in vitro, and in vivo models were used to observe the effect of sodium caprate on the intestinal absorption of berberine. Intestinal mucosa morphology was measured to evaluate the toxic effect of sodium caprate. Diabetic model was used to evaluate antidiabetic effect of berberine coadministrated with sodium caprate. The results showed that the absorption of berberine in the small intestine was poor and that sodium caprate could significantly improve the poor absorption of berberine in the small intestine. Sodium caprate stimulated mucosal-to-serosal transport of berberine; the enhancement ratios were 2.08, 1.49, and 3.49 in the duodenum, jejunum, and ileum, respectively. After coadministration, the area under the plasma concentration-time curve of berberine was increased 28% than that in the absence of sodium caprate. Furthermore, both berberine and coadministration with sodium caprate orally could significantly decrease fasting blood glucose and improve glucose tolerance in diabetic rats (P<0.05). The hypoglycemic effect of coadministration group was remarkably stronger, and the areas under the glucose curves was decreased 22.5%, compared with berberine treatment group (P< 0.05). Morphologic analysis indicated that sodium caprate was not significantly injurious to the intestinal mucosa. The study demonstrates that sodium caprate could significantly promote the absorption of berberine in intestine and enhance its antidiabetic effect without any serious mucosal damage.

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Section: Discussionmentioning

confidence: 99%

“…Experiments were carried out as described previously (15), with minor modification. Rats were fasted for 16 h, anesthetized with 20% urethane (5 mL kg −1 ), and affixed supine on a surface under a surgical lamp to maintain body temperature.…”

Section: Recirculating Intestinal Perfusion In Ratsmentioning

confidence: 99%

Enhancement of Sodium Caprate on Intestine Absorption and Antidiabetic Action of Berberine

Zhang

et al. 2010

AAPS PharmSciTech

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“…Zhang et al observed that CT was transported primarily via an active mechanism across the intestinal epithelium, a saturable process that could pump CT into the luminal side (47). Meanwhile, other studies reported that TSIIA might not exclude a passive transport process (48,49) due to its low molecular weight (294 D) and high lipophilicity (logP = 6.1) (50). The plasma level of tanshinones is low, generally in the nM to the sub-µM range in animals after oral or injection.…”

Section: Tanshinonesmentioning

confidence: 99%

Salvia miltiorrhiza Bge. (Danshen) in the Treating Non-alcoholic Fatty Liver Disease Based on the Regulator of Metabolic Targets

Liu

Shi

Peng

et al. 2022

Front. Cardiovasc. Med.

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Non-alcoholic fatty liver disease (NAFLD) is rapidly prevalent due to its strong association with increased metabolic syndrome such as cardio- and cerebrovascular disorders and diabetes. Few drugs can meet the growing disease burden of NAFLD. Salvia miltiorrhiza Bge. (Danshen) have been used for over 2,000 years in clinical trials to treat NAFLD and metabolic syndrome disease without clarified defined mechanisms. Metabolic targets restored metabolic homeostasis in patients with NAFLD and improved steatosis by reducing the delivery of metabolic substrates to liver as a promising way. Here we systematic review evidence showing that Danshen against NAFLD through diverse and crossing mechanisms based on metabolic targets. A synopsis of the phytochemistry and pharmacokinetic of Danshen and the mechanisms of metabolic targets regulating the progression of NAFLD is initially provided, followed by the pharmacological activity of Danshen in the management NAFLD. And then, the possible mechanisms of Danshen in the management of NAFLD based on metabolic targets are elucidated. Specifically, the metabolic targets c-Jun N-terminal kinases (JNK), sterol regulatory element-binding protein-1c (SREBP-1c), nuclear translocation carbohydrate response element–binding protein (ChREBP) related with lipid metabolism pathway, and peroxisome proliferator-activated receptors (PPARs), cytochrome P450 (CYP) and the others associated with pleiotropic metabolism will be discussed. Finally, providing a critical assessment of the preclinic and clinic model and the molecular mechanism in NAFLD.

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“…[30][31][32] This method was used to determine absorption characteristics at four different segments: 33 duodenum, jejunum, ileum, and colon. Three different concentrations were studied: 140 µg/mL, 160 µg/mL, and 180 µg/mL.…”

Section: In Vivo Transport Studiesmentioning

confidence: 99%

Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption

Bei

Chen²,

Liu³

et al. 2012

IJN

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Abstract:In this paper, two novel liver-targeting nanoparticles, norcantharidin-loaded chitosan nanoparticles (NCTD-CS-NPs) and norcantharidin-associated galactosylated chitosan nanoparticles (NCTD-GC-NPs), were prepared using ionic cross-linkage. The physical properties, particle size, encapsulation efficiency, and drug release characteristics of the nanoparticles were investigated in vitro. To investigate the intestinal absorption mechanisms of the two preparations, a series of experiments was carried out, including in situ circulation method, in vitro everted gut sacs, and Ussing chamber perfusion technique. The absorption rate constants (Ka) of NCTD at different segments were found to be duodenum . jejunum . ileum . colon. The concentration had no distinctive effect on absorption kinetics, suggesting that drug absorption is not dosedependent. The transport of NCTD was found to be inhibited by P-glycoprotein (P-gp) inhibitor, indicating that NCTD might be the substrate of P-gp. The order of the absorption enhancer effects were as follows: low molecular weight chitosan (CS-8kDa) . high molecular weight chitosan (CS-30kDa) . Poloxamer . sodium dodecyl sulfate (SDS) . sodium deoxycholate (SDCh). The results indicate that the chitosan nanoparticles can improve intestinal absorption of NCTD.

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In Situ Intestinal Absorption Behaviors of Tanshinone IIA from Its Inclusion Complex with Hydroxypropyl-.BETA.-cyclodextrin

Cited by 16 publications

References 23 publications

Enhancement of Sodium Caprate on Intestine Absorption and Antidiabetic Action of Berberine

Enhancement of Sodium Caprate on Intestine Absorption and Antidiabetic Action of Berberine

Salvia miltiorrhiza Bge. (Danshen) in the Treating Non-alcoholic Fatty Liver Disease Based on the Regulator of Metabolic Targets

Novel norcantharidin-loaded liver targeting chitosan nanoparticles to enhance intestinal absorption

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