Enhancement of API solubility and bioavailability
The Science Behind

Enhancement of API solubility and bioavailability

Peer-reviewed journal articles and scientific presentations describing the use of KLEPTOSE® beta-cyclodextrins range for enhancement of API solubility and bioavailability 

Study Reference 

Related Roquette excipient(s) 

Summary of results regarding Roquette excipient(s) performances 

Solubility studies of rifampicin and hydroxypropyl-β-cyclodextrin for pediatric formulations

Echezarreta M, Ruiz-Noda Z, Suárez-González J, Soriano M, Santoveña-Estévez A, Fariña JB.

6th European Conference on Cyclodextrins, October 2-4, 2019
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© Universidad de La Laguna. Reproduced with permission

KLEPTOSE® HPB (hydroxypropyl-beta-cyclodextrin) 

Complexation with KLEPTOSE® HPB Oral Grade increased the solubility of rifampicin by 2-7 times. 

Influence of darunavir: β-cyclodextrin complex on the solubility of darunavir

Kogawa A.C.; Corrêa J.C.; Salgado H.R. Research and Reviews: Journal of Pharmacology and Toxicological Studies. 2014:50-5

http://www.rroij.com/peer-reviewed/influence-of-darunavir-946cyclodextrin-complex-on-the-solubilityof-darunavir-34859.html

KLEPTOSE® (beta-cyclodextrin) 

Complexation with beta-cyclodextrin increased the solubility of darunavir by at least 5 times in various dissolution media tested. 

Improvement of Aripiprazole Solubility by Complexation with (2-Hydroxy) propyl-B-cyclodextrin Using Spray Drying Technique

Mihajlovic, T.; Kachrimanis, K.; Graovac, A.; Djuric, Z.; Ibric, Z. AAPS PharmSciTech volume 13, 26 April 2012, Pages 623-631

https://doi.org/10.1208/s12249-012-9786-3

KLEPTOSE® HP (hydroxypropyl-beta-cyclodextrin) 

The spray-dried product containing KLEPTOSE® HP-aripiprazole complex demonstrated improved solubility, dissolution rate and stability during storage. 

Characterization and in vitro evaluation of the formoterol/cyclodextrin complex for pulmonary administration by nebulization

Hoang Thi, T.H.; Azaroual, N.; Flament, M.-P. European journal of pharmaceutics and biopharmaceutics. 2009 May 1;72(1):214-8.

https://doi.org/10.1016/j.ejpb.2008.10.012 

 

KLEPTOSE® HP (hydroxypropyl-beta-cyclodextrin) 
KLEPTOSE® CRYSMEB (methyl-beta-cyclodextrin) 

Both β-cyclodextrin derivatives were used successfully to formulate nebulizable solutions of formoterol. The cyclodextrin/formoterol aqueous solutions were able to form aerosols with particle size suitable for pulmonary deposition. 

Pharmacodynamic and pharmacokinetic investigation of cyclodextrin-mediated asenapine maleate in situ nasal gel for improved bioavailabilty.

Kulkarni, J.A.; Avachat, A.M. Drug development and industrial pharmacy. 2017 Feb 1;43(2):234-45.

https://doi.org/10.1080/03639045.2016.1236808 

 

KLEPTOSE® HP (hydroxypropyl-beta-cyclodextrin) 

An in situ nasal gel of asenapine maleate (AM)-HPβCD inclusion complex for the treatment of schizophrenia and bipolar disorder I was successfully developed. 1:1 molar ratio complexation with hydroxypropyl beta-cyclodextrin was used to improve solubility of AM through a kneading process. 

Cyclodextrins as a potential carrier in drug nebulization

Evrard, B.; Bertholet, P.; Gueders, M.; Flament, M.-P.; Piel, G.; Delattre, L.; Gayot, A.; Leterme, P.; Foidart, J.-M.; Cataldo, D. Journal of Controlled Release. 2004 May 18;96(3):403-10.

https://doi.org/10.1016/j.jconrel.2004.02.010

 

KLEPTOSE® HPB (hydroxypropyl-beta-cyclodextrin) 

Hydroxypropyl-beta-cyclodextrin was shown to undergo aerosolization and that the resulting droplet-size is compatible with pulmonary deposition. In vivo, it was demonstrated that inhaled hydroxypropyl beta-cyclodextrin solutions were non-toxic as assessed by the study of BAL, lung and kidney histology, bronchial responsiveness to methacholine and blood urea. 

Development of a Taste-Masked Orodispersible Film Containing Dimenhydrinate
Preis, M.; Pein, M.; Breitkreutz. J. Pharmaceutics. 2012 Dec;4(4):551-62.

KLEPTOSE® HPB (hydroxypropyl-beta-cyclodextrin) 
KLEPTOSE® Linecaps 17 (pea maltodextrin) 

Hydroxypropyl-beta-cyclodextrin and pea maltodextrin were able to improve the solubility of dimenhydrinate and could prevent the recrystallization of the drug substance in solid state of the film. Both excipients also demonstrated taste-masking effects through electronic tongue evaluation. 

Contribution of cyclodextrins in the development of different pharmaceutical formulations of a new matrix metalloproteinase inhibitor

Evrard, B.; Bertholet, P.; Gueders, M.; Piette, M.; Piel, G.; Cataldo, D.; Delattre, L. Journal of Inclusion Phenomena and Macrocyclic Chemistry. 2007 Apr 1;57(1-4):303-8.
https://doi.org/10.1007/s10847-006-9177-z

 

KLEPTOSE® HPB (hydroxypropyl-beta-cyclodextrin) 

Hydroxypropyl beta-cyclodextrin was able to improve the aqueous solubility of Ro 28-2653 (5-biphenyl-4-yl-5-[4-(4-nitro-phenyl)-piperazin-1-yl]-pyrimidine-2,4,6-trione) (RO) when mixed with randomly methylated-b-CD (RAMEB). There was also a synergistic effect between L-lysine with hydroxypropyl-beta-cyclodextrin that resulted in a significant increase in RO aqueous solubility (70,000 times). 

Optimization of Drug Permeation from 8% Ciclopirox Cyclodextrin/Poloxamer-Soluble Polypseudorotaxane-Based Nail Lacquers

Cutrín-Gómez, E.; Conde-Penedo, A.; Anguiano-Igea, S.; Gómez-Amoza, J.L.; Otero-Espinar, F.J. Pharmaceutics. 2020 Mar;12(3):231.
https://doi.org/10.3390/pharmaceutics12030231 
Licensed under a Creative Commons Attribution License

KLEPTOSE® HPB (hydroxypropyl-beta-cyclodextrin) 

These results demonstrate the potential of the hydroxypropyl-beta-cyclodextrin/poloxamer-soluble polypseudorotaxane base for ungual administration of antifungal medicines. 

Curcumin complexation with cyclodextrins by the autoclave process: Method development and characterization of complex formation

Al Hagbani, T.; Nazzal, S. International journal of pharmaceutics. 2017 Mar 30;520(1-2):173-80.
https://doi.org/10.1016/j.ijpharm.2017.01.063

 

KLEPTOSE® HPB (hydroxypropyl-beta-cyclodextrin) 

Hydroxypropyl-beta-cyclodextrin was comparable with sulfobutylether beta-cyclodextrin in enhancing the poor aqueous solubility of curcumin (CUR) through complexation in a 1:1 molar ratio.  

Solid-state characterization and dissolution profiles of the inclusion complexes of omeprazole with native and chemically modified b-cyclodextrin

Figueiras, A.; Carvalho, R.A.; Ribeiro, L.; Torres-Labandeira, J.J.; Veiga, F.J.B. European Journal of Pharmaceutics and Biopharmaceutics. 2007 Sep 1;67(2):531-9.
https://doi.org/10.1016/j.ejpb.2007.03.005 

 

KLEPTOSE® (beta-cyclodextrin) and KLEPTOSE® CRYSMEB (methyl-beta-cyclodextrin) 

Inclusion complex of 1:1 molar ratio was formed between omeprazole and both beta-cyclodextrin and methyl-beta-cyclodextrin via a freeze-drying method. In addition, inclusion complex was also formed with methyl-beta-cyclodextrin via spray-drying. Significant improvement of dissolution (p < 0.001) was observed by the complexed forms versus a physical mixture control. 

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