scholarly journals Polymer-free electrospun nanofibers from sulfobutyl ether 7 -beta-cyclodextrin (SBE 7 -β-CD) inclusion complex with sulfisoxazole: Fast-dissolving and enhanced water-solubility of sulfisoxazole

2017 ◽  
Vol 531 (2) ◽  
pp. 550-558 ◽  
Author(s):  
Zehra Irem Yildiz ◽  
Asli Celebioglu ◽  
Tamer Uyar
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Electrospun Nanofibers ◽  
Beta Cyclodextrin ◽  
Sulfobutyl Ether

scholarly journals Efficient Encapsulation of Citral in Fast-Dissolving Polymer-Free Electrospun Nanofibers of Cyclodextrin Inclusion Complexes: High Thermal Stability, Longer Shelf-Life, and Enhanced Water Solubility of Citral

Nanomaterials ◽  
2018 ◽  
Vol 8 (10) ◽  
pp. 793 ◽  
Author(s):  
Zeynep Aytac ◽  
Asli Celebioglu ◽  
Zehra Yildiz ◽  
Tamer Uyar
Keyword(s):  
Thermal Stability ◽  
Inclusion Complex ◽  
Shelf Life ◽  
Water Solubility ◽  
Temperature Stability ◽  
Electrospun Nanofibers ◽  
High Temperature Stability ◽  
Fiber Morphology ◽  
Electrospinning Technique ◽  
Beta Cyclodextrin

Here, we report a facile production of citral/cyclodextrin (CD) inclusion complex (IC) nanofibers (NFs) from three types of CDs (hydroxypropyl-beta-cyclodextrin (HPβCD), hydroxypropyl-gamma-cyclodextrin (HPγCD), and methylated-beta-cyclodextrin (MβCD)) by an electrospinning technique without the need of any polymeric carrier matrix. Self-standing nanofibrous webs of citral/CD-IC nanofibers (citral/CD-IC-NF) with uniform fiber morphology have been successfully electrospun from aqueous solutions of citral/CD-IC. Thanks to the inclusion complex formed with CDs, the efficient preservation of citral (up to ~80%) in citral/CD-IC-NFs was observed. In addition, the citral/CD-IC-NFs have shown ~50% preservation of citral for 15 days at room temperature even though citral has a highly volatile nature. The enhanced thermal stability of citral (~100–300°C) in citral/CD-IC-NFs compared to pure citral (~50–165°C) has been observed. Moreover, citral/CD-IC-NFs tended to disintegrate in water very quickly. To summarize, citral was efficiently encapsulated in citral/CD-IC-NFs, and these citral/CD-IC-NFs have been shown to be fast dissolving. In citral/CD-IC-NFs, citral/CD-ICs have enhanced water solubility of citral along with high-temperature stability and a longer shelf-life.

An Assessment of Olmesartan Medoxomil Tablet by Inclusion Complex Technique

2021 ◽  
pp. 193-197
Author(s):  
Deepak Sarangi ◽  
Subhashree Mallick ◽  
Anjum Ara ◽  
Sanjeeb Kumar Sahoo ◽  
Rabinarayan Rana
Keyword(s):  
Inclusion Complex ◽  
Water Solubility ◽  
Olmesartan Medoxomil ◽  
Complexing Agents ◽  
Complexing Agent ◽  
Angiotensin Ii Receptor ◽  
Current Effort ◽  
Ir Studies ◽  
Beta Cyclodextrin ◽  
Ft Ir

Olmesartan Medoxomil is an AT1 subtype selected angiotensin-II receptor antagonist approved for the treatment of hypertension. It has low water solubility, so the current effort is being made to enhance the solubility of the Olmesartan by inclusion complex and to incorporate them into tablets by direct compression. Complexing agent like Beta cyclodextrin and polyvinyalpyrrolidone has been used for complexation method. FT-IR studies have shown that there is no link between drugs and complexing agents. Among all methods, the inclusion complex (OLBCD 3) containing the drug: Beta cyclodextrin in a 1: 3 ratio showed rapid drug release (87.41% within 30 minutes) and post compression parameters are within limits. All the values obtained from pre compression and post compression parameters meets the legal requirements for tablets. Stability studies of batch no OLBCD 3 shows no significant change. Therefore, it can be concluded that the structure was stable.

scholarly journals Preparation and characterization of cyanazine–hydroxypropyl-beta-cyclodextrin inclusion complex

RSC Advances ◽  
2019 ◽  
Vol 9 (45) ◽  
pp. 26109-26115 ◽  
Author(s):  
Shuang Gao ◽  
Chao Bie ◽  
Qiuyu Ji ◽  
Haiyang Ling ◽  
Chunyan Li ◽  
...  
Keyword(s):  
Thermal Stability ◽  
Inclusion Complex ◽  
Water Solubility ◽  
Herbicidal Activity ◽  
Beta Cyclodextrin ◽  
Cyclodextrin Inclusion ◽  
Cyclodextrin Inclusion Complex ◽  
Hydroxypropyl Beta Cyclodextrin

Cyanazine/HPβCD inclusion complex was prepared to improve water solubility and thermal stability and herbicidal activity of cyanazine.

scholarly journals Preparation and Characterization of Flurbiprofen/β-Cyclodextrin Inclusion Complex

2020 ◽  
Vol 36 (3) ◽  
Author(s):  
Nguyen Thi Thanh Binh ◽  
Ho Thi Quynh Xuan ◽  
Nguyen Thi Hai Yen
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Inclusion Complex ◽  
Oral Bioavailability ◽  
High Performance ◽  
Water Solubility ◽  
Cyclodextrin Complexes ◽  
Beta Cyclodextrin ◽  
Cyclodextrin Inclusion ◽  
Cyclodextrin Inclusion Complex

This study aims to ameliorate the water solubility of flurbiprofen by using β-cyclodextrin (β-CD). The drug/ligand 1:1 (M/M) stoichiometry was determined based on the effect of β-CD on the solubility of flurbiprofen. Several methods of preparing flurbiprofen/β-CD inclusion complex were investigated and a solvent method using hot water to dissolve the starting materials was selected. The selected method showed a lot of advantages such as high complexing ability, good product yield, simple and eco-friendly process. The obtained product was characterized using various analytical techniques such as high-performance liquid chromatography, differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy. The product had a predominantly amorphous form with clathrate particles of about 2-7 µm in size, irregular edges and rough surfaces. The study results show that in the complexing process, flurbiprofen replaced water molecules located in the conical cavity of β-CD. The complex contained 19.91% flurbiprofen by mass with water solubility at 37°C was 1,100 µg/ml. The results also show that the complexing with β-CD significantly improved the water solubility of flurbiprofen by both speed and level. Keywords Flurbiprofen, β-cyclodextrin, inclusion complex, water solubility, preparation, characterization. References [1] K. Maroof, F. Zafar, H. Ali, S. Naveed, Flurbiprofen: a potent pain reliever, J. Bioequiv. Availab. 7(1) (2015) 056-058. https://doi.org/10.4172/jbb.1000214.[2] J.J. Thebault, G. Lagrue, C.E. Blatrix, L. Cheynier, R. Cluzan, Clinical pharmacology of flurbiprofen: a novel inhibitor of platelet aggregation, Curr. Med. Res. Opin. 5(1) (1977) 130-134. https://doi.org/10.1185/03007997709108990.[3] H. Geerts, Drug evaluation: (R)-flurbiprofen - an enantiomer of flurbiprofen for the treatment of Alzheimer's disease, Idrugs. 10(2) (2007) 121-133.[4] P.L. McGeer, M. Schulzer, E.G. McGeer, Arthritis and anti-inflammatory agents as possible protective factors for Alzheimer's disease: a review of 17 epidemiologic studies, Neurology. 47(2) (1996) 425-432. https://doi.org/10.1212/WNL.47.2.425.[5] S. Meister, I. Zlatev, J. Stab, D. Docter, S. Baches, et al., Nanoparticulate flurbiprofen reduces amyloid-β 42 generation in an in vitro blood-brain barrier model, Alzheimers Res. Ther. 5(6) (2013) 51-63. https://doi.org/10.1186/alzrt225.[6] K.P. Townsend, D. Praticò, Novel therapeutic opportunities for Alzheimer’s disease: focus on nonsteroidal anti-inflammatory drugs, FASEB J. 19(12) (2005) 1592-1601. https://doi.org/10.1096/fj.04-3620rev.[7] C.K. Kim, Y.S. Yoon, J.Y. Kong, Preparation and evaluation of flurbiprofen dry elixir as a novel dosage form using a spray-drying technique, Int. J. Pharm. 120 (1995) 21-31. https://doi.org/10.1016/0378-5173(94)00375-F.[8] M.J. Habib, M.T. Phan, G. Owusu-Ababio, Dissolution profiles of flurbiprofen in phospholipid solid dispersions, Drug Dev. Ind. Pharm. 24 (1998) 1077-1082. https://doi.org/10.3109/03639049809089952.[9] D.H. Oh, Y.J. Park, J.H. Kang, C.S. Yong, H.G. Choi, Physicochemical characterization and in vivo evaluation of flurbiprofen-loaded solid dispersion without crystalline change, Drug. Deliv. 18 (2010) 46-53. https://doi.org/10.3109/10717544.2010.509365.[10] G.D. Gupta, S. Jain, N.K. Jain, Formulation of an aqueous injection of flurbiprofen, Pharmazie. 52 (1997) 709-712. https://doi.org/10.1080/10826079708005547.[11] K.W. Ambade, S.L. Jadhav, M.N. Gambhire, S.D. Kurmi, V.J. Kadam, K.R. Jadhav, Formulation and evaluation of flurbiprofen microemulsion, Curr. Drug Deliv. 5 (2008) 32–41[12] H.H. Baek, S.Y. Kwon, S.J. Rho, W.S. Lee, H.J. Yang, J.M. Hah, H.G. Choi, Y.R. Kim, C.S. Yong, Enhanced solubility and bioavailability of flurbiprofen by cycloamylose, Arch. Pharm. Res. 34 (2011) 391-397. https://doi.org/10.1007/s12272-011-0306-x.[13] A. Muraoka, T. Tokumura, Y. Machida, Evaluation of the bioavailability of flurbiprofen and its β-cyclodextrin inclusion complex in four different doses upon oral administration to rats, Eur. J. Pharm. Biopharm. 58(3) (2004) 667-671. https://doi.org/10.1016/j.ejpb.2004.03.030.[14] T. Tokumura, A. Muraoka, Y. Machida, Improvement of oral bioavailability of flurbiprofen from flurbiprofen/beta-cyclodextrin inclusion complex by action of cinnarizine, Eur. J. Pharm. Biopharm. 73 (2009) 202-204. https://doi.org/10.1016/j.ejpb.2009.04.018.[15] D. Li, M. Han, P. Balakrishnan, Y. Yan, D. Oh, et al., Enhanced oral bioavailability of flurbiprofen by combined use of micelle solution and inclusion compound, Arch. Pharm. Res. 33(1) (2010) 95-101. https://doi.org/10.1007/s12272-010-2231-9.[16] H. Arima, K. Motoyama, T. Irie, Recent findings on safety profiles of cyclodextrins, cyclodextrin conjugates, and polypseudorotaxanes, in: E. Bilensoy (Ed.), Cyclodextrins in Pharmaceutics, Cosmetics, and Biomedicine: Current and Future Industrial Applications, John Wiley & Sons Inc., Hoboken, 2011, pp. 91-122. https://doi.org/10.1002/9780470926819.ch5.[17] T.J. Grattan, Inclusion complexes of beta-cyclodextrin with flurbiprofen, ketoprofen and naproxen, International patent WO1995007104A1, March 16, 1995.[18] M. Cirri, C. Rangoni, F. Maestrelli, G. Corti, P. Mura, Development of fast-dissolving tablets of flurbiprofen-cyclodextrin complexes, Drug Dev. Ind. Pharm. 31(7) (2005) 697-707. https://doi.org/10.1080/03639040500253694.[19] M. Tirunagari, N. Mehveen, M.F. Qureshi, J.P. Sultana, V. Tirunagari (2012), Solubility Enhancement of Flurbiprofen using Different Solubilization Techniques, Int. J. Pharm. Pharm. Sci. 4(4) (2012) 97-100.[20] P. Saokham, C. Muankaew, P. Jansook, T. Loftsson, Solubility of cyclodextrins and drug/cyclodextrin complexes, Molecules. 23(5) (2018) 1161-1175. https://doi.org/10.3390/molecules23051161.[21] S. Pereva, T. Sarafska, S. Bogdanova, T. Spassov, Efficiency of “cyclodextrin-ibuprofen” inclusion complex formation, J. Drug Deliv. Sci. Tec. 35 (2016) 34-39. https://doi.org/10.1016/j.jddst.2016.04.006.[22] T.T.B. Nguyen, N.A. Dang, M.A. Tran, T.H. Nguyen, Validation of a high-performance liquid chromatographic method with diod array detection for the quantification of flurbiprofen in 100 mg film-coated tablet, VNU Journal of Science: Medical and Pharmaceutical Sciences. 33(2) (2017) 41-49. https://doi.org/10.25073/2588-1132/vnumps.4085.[23] T. Higuchi, K.A. Connors, Phase-solubility techniques, Adv. Anal. Chem. Instrum. 4 (1965) 117-122.    

NMR Studies of the Inclusion Complexes Between Ezetimibe and Cyclodextrins

2018 ◽  
Vol 69 (7) ◽  
pp. 1838-1841
Author(s):  
Hajnal Kelemen ◽  
Angella Csillag ◽  
Bela Noszal ◽  
Gabor Orgovan
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Water Solubility ◽  
Solution Nmr ◽  
Spectroscopic Techniques ◽  
Nmr Studies ◽  
The Poor ◽  
Poor Water Solubility

Ezetimibe, the antihyperlipidemic drug of poor bioavailability was complexed with native and derivatized cyclodextrins.The complexes were characterized in terms stability, stoichiometry and structure using various 1D and 2D solution NMR spectroscopic techniques. The complexes were found to be of moderate stability (logK[3). The least stable inclusion complex is formed with b-cyclodextrin, while the ezetimibe-methylated-b--cyclodextrin has a 7-fold higher stability. The results can be useful to improve the poor water-solubility and the concomitant bioavailability of ezetimibe.

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