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Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer.
Drug Deliv. 2010 Jul; 17(5):322-9.DD

Abstract

To develop a valsartan-loaded gelatin microcapsule using hydroxypropylmethylcellulose (HPMC) as a stabilizer, which could improve the physical stability and bioavailability of valsartan, the gelatin microcapsules were prepared with various ratios of gelatin and HPMC using a spray-drying technique. Their solubility, dissolution, thermal characteristics, crystallinity, and physical stability were investigated. The bioavailability of drug in valsartan-loaded microcapsule was then evaluated compared to drug powder and commercial product in rats. The microcapsule with gelatin and/or HPMC enhanced the solubility and dissolution of drug compared to valsartan powder. Among the formulations tested, the valsartan-loaded gelatin microcapsule at the weight ratio of valsartan/gelatin/HPMC of 1/2/1 gave excellent drug solubility of approximately 2 microg/ml and dissolution of 70% at 1 h. The crystal state of valsartan in this microcapsule was changed from crystalline to amorphous form during the spray-drying process and maintained as an amorphous form at 40 degrees C for at least 3 months, indicating that it was physically stable. HPMC in this microcapsule could inhibit the recrystallization, resulting in stabilizing the amorphous form of valsartan. Furthermore, it improved the oral bioavailability of valsartan compared to valsartan powder and gave the similar AUC, C(max), and T(max) values to commercial product, suggesting that it was bioequivalent to commercial product in rats. Thus, the gelatin microcapsule with HPMC would be a more effective and stable oral delivery system of poorly water-soluble valsartan.

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

20367177

Citation

Li, Dong Xun, et al. "Development of Valsartan-loaded Gelatin Microcapsule Without Crystal Change Using Hydroxypropylmethylcellulose as a Stabilizer." Drug Delivery, vol. 17, no. 5, 2010, pp. 322-9.
Li DX, Yan YD, Oh DH, et al. Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer. Drug Deliv. 2010;17(5):322-9.
Li, D. X., Yan, Y. D., Oh, D. H., Yang, K. Y., Seo, Y. G., Kim, J. O., Kim, Y. I., Yong, C. S., & Choi, H. G. (2010). Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer. Drug Delivery, 17(5), 322-9. https://doi.org/10.3109/10717541003717031
Li DX, et al. Development of Valsartan-loaded Gelatin Microcapsule Without Crystal Change Using Hydroxypropylmethylcellulose as a Stabilizer. Drug Deliv. 2010;17(5):322-9. PubMed PMID: 20367177.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of valsartan-loaded gelatin microcapsule without crystal change using hydroxypropylmethylcellulose as a stabilizer. AU - Li,Dong Xun, AU - Yan,Yi Dong, AU - Oh,Dong Hoon, AU - Yang,Kwan Yeol, AU - Seo,Yoon Gi, AU - Kim,Jong Oh, AU - Kim,Yong-Il, AU - Yong,Chul Soon, AU - Choi,Han-Gon, PY - 2010/4/7/entrez PY - 2010/4/7/pubmed PY - 2010/9/3/medline SP - 322 EP - 9 JF - Drug delivery JO - Drug Deliv VL - 17 IS - 5 N2 - To develop a valsartan-loaded gelatin microcapsule using hydroxypropylmethylcellulose (HPMC) as a stabilizer, which could improve the physical stability and bioavailability of valsartan, the gelatin microcapsules were prepared with various ratios of gelatin and HPMC using a spray-drying technique. Their solubility, dissolution, thermal characteristics, crystallinity, and physical stability were investigated. The bioavailability of drug in valsartan-loaded microcapsule was then evaluated compared to drug powder and commercial product in rats. The microcapsule with gelatin and/or HPMC enhanced the solubility and dissolution of drug compared to valsartan powder. Among the formulations tested, the valsartan-loaded gelatin microcapsule at the weight ratio of valsartan/gelatin/HPMC of 1/2/1 gave excellent drug solubility of approximately 2 microg/ml and dissolution of 70% at 1 h. The crystal state of valsartan in this microcapsule was changed from crystalline to amorphous form during the spray-drying process and maintained as an amorphous form at 40 degrees C for at least 3 months, indicating that it was physically stable. HPMC in this microcapsule could inhibit the recrystallization, resulting in stabilizing the amorphous form of valsartan. Furthermore, it improved the oral bioavailability of valsartan compared to valsartan powder and gave the similar AUC, C(max), and T(max) values to commercial product, suggesting that it was bioequivalent to commercial product in rats. Thus, the gelatin microcapsule with HPMC would be a more effective and stable oral delivery system of poorly water-soluble valsartan. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/20367177/Development_of_valsartan_loaded_gelatin_microcapsule_without_crystal_change_using_hydroxypropylmethylcellulose_as_a_stabilizer_ L2 - https://www.tandfonline.com/doi/full/10.3109/10717541003717031 DB - PRIME DP - Unbound Medicine ER -