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Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate.
Int J Biol Macromol. 2016 Feb; 83:282-7.IJ

Abstract

A novel surfactant-incorporated hydroxypropyl methylcellulose (HPMC) solid dispersion (SD) system was constructed in order to facilitate the release rate and oral absorption of tacrolimus (FK506), a poorly water-soluble immunosuppressant. Several emulsifiers including sodium lauryl sulfate (SLS), as drug release promotors, were employed with HPMC to fabricate SD using the solvent wetting method. The solid state characteristics using differential scanning calorimetry and X-ray powder diffraction, revealed that FK506 was molecularly distributed within all dispersions in amorphous form. The dissolution rates of FK506 in SLS-incorporated SDs were much higher than those in SDs prepared with HPMC alone, and even with stearoyl polyoxyl-32 glycerides or tocopheryl polyethylene glycol 1000 succinate. In particular, the greatest dissolution enhancement was obtained from the SD consisting of the drug, HPMC, and SLS in a weight ratio of 1:1:3, providing a 50-fold higher drug concentration within 15 min, compared with HPMC SD. In vivo absorption study in rats demonstrates that the optimized formula remarkably increased the oral absorption of FK506, providing about 4.0-fold greater bioavailability (p<0.05) compared with the marketed product (Prograf®, Astellas Pharma). These data suggest that a novel SLS/HPMC SD may be an advantageous dosage form of FK506, boosting the dissolution and absorption in gastrointestinal tract.

Authors+Show Affiliations

College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea.College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, South Korea. Electronic address: kangmj@dankook.ac.kr.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26642839

Citation

Jung, Hyuck Jun, et al. "Improved Oral Absorption of Tacrolimus By a Solid Dispersion With Hypromellose and Sodium Lauryl Sulfate." International Journal of Biological Macromolecules, vol. 83, 2016, pp. 282-7.
Jung HJ, Ahn HI, Park JY, et al. Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate. Int J Biol Macromol. 2016;83:282-7.
Jung, H. J., Ahn, H. I., Park, J. Y., Ho, M. J., Lee, D. R., Cho, H. R., Park, J. S., Choi, Y. S., & Kang, M. J. (2016). Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate. International Journal of Biological Macromolecules, 83, 282-7. https://doi.org/10.1016/j.ijbiomac.2015.11.063
Jung HJ, et al. Improved Oral Absorption of Tacrolimus By a Solid Dispersion With Hypromellose and Sodium Lauryl Sulfate. Int J Biol Macromol. 2016;83:282-7. PubMed PMID: 26642839.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate. AU - Jung,Hyuck Jun, AU - Ahn,Hye In, AU - Park,Ji Yeon, AU - Ho,Myoung Jin, AU - Lee,Dae Ro, AU - Cho,Ha Ra, AU - Park,Jun Seo, AU - Choi,Yong Seok, AU - Kang,Myung Joo, Y1 - 2015/11/28/ PY - 2015/10/10/received PY - 2015/11/06/revised PY - 2015/11/24/accepted PY - 2015/12/9/entrez PY - 2015/12/9/pubmed PY - 2016/10/8/medline KW - Bioavailability KW - Dissolution KW - Hydroxypropyl methylcellulose KW - Sodium lauryl sulfate KW - Solid dispersion KW - Tacrolimus SP - 282 EP - 7 JF - International journal of biological macromolecules JO - Int J Biol Macromol VL - 83 N2 - A novel surfactant-incorporated hydroxypropyl methylcellulose (HPMC) solid dispersion (SD) system was constructed in order to facilitate the release rate and oral absorption of tacrolimus (FK506), a poorly water-soluble immunosuppressant. Several emulsifiers including sodium lauryl sulfate (SLS), as drug release promotors, were employed with HPMC to fabricate SD using the solvent wetting method. The solid state characteristics using differential scanning calorimetry and X-ray powder diffraction, revealed that FK506 was molecularly distributed within all dispersions in amorphous form. The dissolution rates of FK506 in SLS-incorporated SDs were much higher than those in SDs prepared with HPMC alone, and even with stearoyl polyoxyl-32 glycerides or tocopheryl polyethylene glycol 1000 succinate. In particular, the greatest dissolution enhancement was obtained from the SD consisting of the drug, HPMC, and SLS in a weight ratio of 1:1:3, providing a 50-fold higher drug concentration within 15 min, compared with HPMC SD. In vivo absorption study in rats demonstrates that the optimized formula remarkably increased the oral absorption of FK506, providing about 4.0-fold greater bioavailability (p<0.05) compared with the marketed product (Prograf®, Astellas Pharma). These data suggest that a novel SLS/HPMC SD may be an advantageous dosage form of FK506, boosting the dissolution and absorption in gastrointestinal tract. SN - 1879-0003 UR - https://www.unboundmedicine.com/medline/citation/26642839/Improved_oral_absorption_of_tacrolimus_by_a_solid_dispersion_with_hypromellose_and_sodium_lauryl_sulfate_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0141-8130(15)30161-6 DB - PRIME DP - Unbound Medicine ER -