Enhancement of the bioavailability of cinnarizine from its beta-cyclodextrin complex on oral administration with L-isoleucine as a competing agent.

  title={Enhancement of the bioavailability of cinnarizine from its beta-cyclodextrin complex on oral administration with L-isoleucine as a competing agent.},
  author={Tadakazu Tokumura and Yuki Tsushima and Kimio Tatsuishi and Masanori Kayano and Yoshiharu Machida and Tsuneji Nagai},
  journal={Chemical \& pharmaceutical bulletin},
  volume={34 3},
This investigation was aimed at the improvement of the bioavailability of cinnarizine (CN) by administering its β-cyclodextrin (β-CD) complex together with a competing agent. The ability of L-leucine (L-Leu) and L-isoleucine (L-Ileu) to act as competing agents was evaluated by determining the penetration rate of CN, employing a Sartorius absorption simulator. L-Ileu showed a stronger competing action than L-Leu. The bioavailability of CN, upon oral administration of the CN-β-CD inclusion… 
Developments in Cyclodextrin Applications in Drug Formulations
With regard to recent developments in cyclodextrin (CD) applications in drug formulations, here will be described on the basis mainly of (a) novel preparative methods of CD inclusion complexes, (b)
Effect of loratadine on the dissolution and bioavailability of gliclazide from its hydroxypropyl-β-cyclodextrin complex
Gliclazide (GZD) is a hypoglycemic agent that has slow dissolution rate and variable bioavailability. Inclusion complex of GZD with hydroxypropyl-β-cyclodextrin (HPβCD) was prepared with the molar
Influence of hydrophilic polymers addition into cinnarizine–β-cyclodextrin complexes on drug solubility, drug liberation behaviour and drug permeability
The aims of this study were (1) to prepare cinnarizine (CNZ)–β-cyclodextrin (β-CD) complexes by the kneading, co-precipitation and co-evaporation methods with (ternary system) or without (binary
The utility of cyclodextrins for enhancing oral bioavailability.
  • R. Carrier, L. Miller, I. Ahmed
  • Chemistry, Medicine
    Journal of controlled release : official journal of the Controlled Release Society
  • 2007
The mechanisms by which cyclodextrins influence key drug delivery processes, again emphasizing solubilization capabilities, are discussed to provide further insight into why cyclodeXTrins will increase bioavailability in certain cases but not influence or possibly decrease bio availability in others.
The Effect of Cyclodextrins on the Stability of Peptides in Nasal Enzymic Systems
The activity of the nasal mucosal homogenate against YGGFL and GGFL was significantly greater than that observed with a nasal wash fluid and the stability of GGF (with CPA) was enhanced.
Recent Advances in Delivery Systems and Therapeutics of Cinnarizine: A Poorly Water Soluble Drug with Absorption Window in Stomach
The paper provides insight to the approaches to overcome low and erratic bioavailability of cinnarizine by cyclodextrin complexes and novel dosage forms: self-nanoemulsifying systems and buoyant microparticulates.
β-シクロデキストリン包接化合物に対する競合包接阻害物質としてのシンナリジンの In vitro評価:プロゲステロン膜透過速度に対する効果
The use of competing agents is considered a powerful tool for the development of a drug-delivery system with drug/cyclodextrin inclusion complexes. However, there are very few studies examining this
Cyclodextrins: application in different routes of drug administration.
Dilution, competitive displacement, protein binding, change in ionic strength and temperature and drug uptake by tissues are the different release mechanisms of the drug from the drug-cyclodextrin complex discussed here.
Minimization of shaking-induced formation of insoluble aggregates of insulin by cyclodextrins.
The use of cyclodextrins (0.5 mg/ml) to stabilize insulin was investigated and alpha-, beta-, gamma- and hydroxypropyl-beta-cyclodextrin, each at 1.5% level, were used to prevent aggregation.
Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract.
Considering the Noyes-Whitney dissolution model shows that drug diffusivity, solubility in the gastrointestinal contents, the surface area of the solid wetted by the lumenal fluids and the GI hydrodynamics all play a role in determining the in vivo dissolution rate.