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Effect of the solid-dispersion method on the solubility and crystalline property of tacrolimus.
Int J Pharm. 2010 Aug 16; 395(1-2):161-6.IJ

Abstract

Three solid dispersions containing poorly water-soluble tacrolimus were prepared with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and dioctyl sulfosuccinate (DOSS) using a spray-drying technique via the solvent-evaporation method with a methylene chloride/ethanol mixture, the solvent-wetting method with ethanol and the surface-attached method with water, respectively. The solubility and dissolution of the drug in the three solid dispersions were evaluated compared to drug powder. Furthermore, their physicochemical properties were investigated using SEM, DSC and powder X-ray diffraction. The solubility and dissolution of the drug were significantly improved in the order of the tacrolimus-loaded solid dispersion prepared by: solvent-evaporation method>solvent-wetting method>surface-attached method. The solid dispersions prepared by solvent evaporation appeared as an aggregated form with the amorphous form. In particular, the solid dispersion prepared by the solvent-evaporation method improved solubility about 900-fold and dissolution of tacrolimus 15-fold because of its reduced particle size, increased surface area and close contact between the hydrophilic carrier and the drug. In the solvent-wetting method, the drug, which was changed to an amorphous form, was attached onto the surface of undissolved carriers. However, the solid dispersion prepared by the surface-attached method gave an unchanged crystalline form. In this solid dispersion, the carriers were attached to the surface of the undissolved drug, resulting in changing the drug from being hydrophobic to hydrophilic. As the crystal form of drug in this solid dispersion was not converted to the amorphous form unlike other solid dispersions, it gave relatively less solubility and dissolution of the drug than did the others. Thus, in the development of a solid-dispersion system containing poorly water-soluble drugs, the method of preparation plays an important role in the solubility and crystallinity of the drugs.

Authors+Show Affiliations

College of Pharmacy, Yeungnam University, 214-1 Dae-Dong, Gyongsan 712-749, South Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20580799

Citation

Joe, Jung Hyun, et al. "Effect of the Solid-dispersion Method On the Solubility and Crystalline Property of Tacrolimus." International Journal of Pharmaceutics, vol. 395, no. 1-2, 2010, pp. 161-6.
Joe JH, Lee WM, Park YJ, et al. Effect of the solid-dispersion method on the solubility and crystalline property of tacrolimus. Int J Pharm. 2010;395(1-2):161-6.
Joe, J. H., Lee, W. M., Park, Y. J., Joe, K. H., Oh, D. H., Seo, Y. G., Woo, J. S., Yong, C. S., & Choi, H. G. (2010). Effect of the solid-dispersion method on the solubility and crystalline property of tacrolimus. International Journal of Pharmaceutics, 395(1-2), 161-6. https://doi.org/10.1016/j.ijpharm.2010.05.023
Joe JH, et al. Effect of the Solid-dispersion Method On the Solubility and Crystalline Property of Tacrolimus. Int J Pharm. 2010 Aug 16;395(1-2):161-6. PubMed PMID: 20580799.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of the solid-dispersion method on the solubility and crystalline property of tacrolimus. AU - Joe,Jung Hyun, AU - Lee,Won Mo, AU - Park,Young-Joon, AU - Joe,Kwan Hyung, AU - Oh,Dong Hoon, AU - Seo,Youn Gee, AU - Woo,Jong Soo, AU - Yong,Chul Soon, AU - Choi,Han-Gon, Y1 - 2010/05/24/ PY - 2010/01/19/received PY - 2010/05/13/revised PY - 2010/05/18/accepted PY - 2010/6/29/entrez PY - 2010/6/29/pubmed PY - 2010/10/16/medline SP - 161 EP - 6 JF - International journal of pharmaceutics JO - Int J Pharm VL - 395 IS - 1-2 N2 - Three solid dispersions containing poorly water-soluble tacrolimus were prepared with hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and dioctyl sulfosuccinate (DOSS) using a spray-drying technique via the solvent-evaporation method with a methylene chloride/ethanol mixture, the solvent-wetting method with ethanol and the surface-attached method with water, respectively. The solubility and dissolution of the drug in the three solid dispersions were evaluated compared to drug powder. Furthermore, their physicochemical properties were investigated using SEM, DSC and powder X-ray diffraction. The solubility and dissolution of the drug were significantly improved in the order of the tacrolimus-loaded solid dispersion prepared by: solvent-evaporation method>solvent-wetting method>surface-attached method. The solid dispersions prepared by solvent evaporation appeared as an aggregated form with the amorphous form. In particular, the solid dispersion prepared by the solvent-evaporation method improved solubility about 900-fold and dissolution of tacrolimus 15-fold because of its reduced particle size, increased surface area and close contact between the hydrophilic carrier and the drug. In the solvent-wetting method, the drug, which was changed to an amorphous form, was attached onto the surface of undissolved carriers. However, the solid dispersion prepared by the surface-attached method gave an unchanged crystalline form. In this solid dispersion, the carriers were attached to the surface of the undissolved drug, resulting in changing the drug from being hydrophobic to hydrophilic. As the crystal form of drug in this solid dispersion was not converted to the amorphous form unlike other solid dispersions, it gave relatively less solubility and dissolution of the drug than did the others. Thus, in the development of a solid-dispersion system containing poorly water-soluble drugs, the method of preparation plays an important role in the solubility and crystallinity of the drugs. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/20580799/Effect_of_the_solid_dispersion_method_on_the_solubility_and_crystalline_property_of_tacrolimus_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(10)00384-4 DB - PRIME DP - Unbound Medicine ER -