Large ring cyclodextrins for solubilization of Domperidone

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Large ring cyclodextrins were prepared and studied as alternatives for drug solubilization [1]. A mixture of CD22-48 was compared with single CD26, CD27, CD28, CD29, CD30, CD33 and CD34 as well as with the natural CDs (CD6, CD7 and CD8) concerning the solubilization of Domperidone having low aqueous solubility (0.025 mM). The largest solubility enhancement (2.7 fold) was obtained for CD33 (0.2 mM), which was a bit higher than the 1.8-fold enhancement with CD6 (alpha-CD) and CD7 (beta-CD) of the same concentration.

The results are interesting but have to be compared with HPBCD: about 10-fold enhancement was obtained using 0.1 M HPBCD solution [2]. Even higher results (76 fold and 160 fold enhancement) were achieved by applying BCD and citric acid as a third component [3] and mannitol and citric acid as components of multicomponent inclusion complex with synergistic effect on the solubilizing efficiency [4], respectively. The highest effect was observed by CycloLab as illustrated below:

Szente, L.: Cyclodextrins in 2010: Unusual Harmony between Science, Technology and Industry. 15th International Cyclodextrin Symposium, Vienna, 2010

[1] Ismail, A., Kerdpol, K., Rungrotmongkol, T., Tananuwong, K., Ueno, T., Ekasit, S., Muangsin, N., Krusong, K. (2021) Solubility enhancement of poorly water soluble domperidone by complexation with the large ring cyclodextrin. International Journal of Pharmaceutics, 606, 120909,

[2] Ghodke DS, Chaulang GM, Patil KS, et al. (2010) Solid State Characterization of Domperidone: Hydroxypropyl-β-Cyclodextrin Inclusion Complex. Indian J Pharm Sci. 72(2):245-249. doi:10.4103/0250-474X.65032

[3] Mali KK, Dias RJ, Ghorpade VS, Havaldar VD. (2010) Sodium alginate microspheres containing multicomponent inclusion complex of domperidone. Latin American Journal of Pharmacy 29:1199-207.

[4] Ghorpade, V., Dias, R.J., Mali, K.K., Havaldar, V. (2016) Preparation and Evaluation of Domperidone/β-Cyclodextrin/Citric Acid/Mannitol Quaternary Inclusion Complex: An In Vitro Study. Asian Journal of Pharmaceutics 10(3):S375-S385. DOI:10.22377/AJP.V10I03.777

Featured image:

Ivanov et al. (2015) Org. Biomol. Chem.,13:1680-1689.

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