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Solvent-shift strategy to identify suitable polymers to inhibit humidity-induced solid-state crystallization of lacidipine amorphous solid dispersions.
Int J Pharm. 2016 Apr 30; 503(1-2):238-46.IJ

Abstract

The solvent-shift strategy was used to identify appropriate polymers that inhibit humidity-induced solid-state crystallization of amorphous solid dispersions (ASDs). Lacidipine with the polymers, PVP-K30, HPMC-E5 or Soluplus, were combined to form amorphous solid dispersions prepared by solvent evaporation. The formulations were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FT-IR) and were subjected to in vitro dissolution testing. The moisture had a significant impact on the amount dissolved for the solid dispersions. Molecular docking studies established that hydrogen bonding was critical for the stabilization of the solid dispersions. The rank order of the binding energy of the drug-polymer association was Soluplus (-6.21 kcal/mol)>HPMC-E5 (-3.21 kcal/mol)>PVP-K30 (-2.31 kcal/mol). PVP-K30 had the highest water uptake among the polymers, as did ASD system of lacidipine-PVP-K30 ASDs. In the Soluplus ASDs, with its strong drug-polymer interactions and low water uptake, moisture-induced solid-state crystallization was not observed.

Authors+Show Affiliations

School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang 110016, China.Department of Pharmacy, Tianjin Medical University Cancer Institute and Hospital, China.School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang 110016, China.School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang 110016, China.School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang 110016, China.School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Wenhua Road, No.103, Shenyang 110016, China.School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang 110016, China.Key Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Ministry of Education, Wenhua Road, No. 103, Shenyang 110016, China. Electronic address: jianwang@syphu.edu.School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang 110016, China; Municipal Key Laboratory of Biopharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, China. Electronic address: sunjin66@21cn.com.

Pub Type(s)

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

Language

eng

PubMed ID

26869398

Citation

Sun, Mengchi, et al. "Solvent-shift Strategy to Identify Suitable Polymers to Inhibit Humidity-induced Solid-state Crystallization of Lacidipine Amorphous Solid Dispersions." International Journal of Pharmaceutics, vol. 503, no. 1-2, 2016, pp. 238-46.
Sun M, Wu C, Fu Q, et al. Solvent-shift strategy to identify suitable polymers to inhibit humidity-induced solid-state crystallization of lacidipine amorphous solid dispersions. Int J Pharm. 2016;503(1-2):238-46.
Sun, M., Wu, C., Fu, Q., Di, D., Kuang, X., Wang, C., He, Z., Wang, J., & Sun, J. (2016). Solvent-shift strategy to identify suitable polymers to inhibit humidity-induced solid-state crystallization of lacidipine amorphous solid dispersions. International Journal of Pharmaceutics, 503(1-2), 238-46. https://doi.org/10.1016/j.ijpharm.2016.01.062
Sun M, et al. Solvent-shift Strategy to Identify Suitable Polymers to Inhibit Humidity-induced Solid-state Crystallization of Lacidipine Amorphous Solid Dispersions. Int J Pharm. 2016 Apr 30;503(1-2):238-46. PubMed PMID: 26869398.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solvent-shift strategy to identify suitable polymers to inhibit humidity-induced solid-state crystallization of lacidipine amorphous solid dispersions. AU - Sun,Mengchi, AU - Wu,Chunnuan, AU - Fu,Qiang, AU - Di,Donghua, AU - Kuang,Xiao, AU - Wang,Chao, AU - He,Zhonggui, AU - Wang,Jian, AU - Sun,Jin, Y1 - 2016/02/08/ PY - 2015/10/28/received PY - 2015/12/24/revised PY - 2016/01/24/accepted PY - 2016/2/13/entrez PY - 2016/2/13/pubmed PY - 2017/1/4/medline KW - Drug–polymer interactions KW - Humidity-induced solid-state crystallization KW - Molecular docking KW - The solvent-shift strategy KW - Water uptake SP - 238 EP - 46 JF - International journal of pharmaceutics JO - Int J Pharm VL - 503 IS - 1-2 N2 - The solvent-shift strategy was used to identify appropriate polymers that inhibit humidity-induced solid-state crystallization of amorphous solid dispersions (ASDs). Lacidipine with the polymers, PVP-K30, HPMC-E5 or Soluplus, were combined to form amorphous solid dispersions prepared by solvent evaporation. The formulations were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier-transform infrared spectroscopy (FT-IR) and were subjected to in vitro dissolution testing. The moisture had a significant impact on the amount dissolved for the solid dispersions. Molecular docking studies established that hydrogen bonding was critical for the stabilization of the solid dispersions. The rank order of the binding energy of the drug-polymer association was Soluplus (-6.21 kcal/mol)>HPMC-E5 (-3.21 kcal/mol)>PVP-K30 (-2.31 kcal/mol). PVP-K30 had the highest water uptake among the polymers, as did ASD system of lacidipine-PVP-K30 ASDs. In the Soluplus ASDs, with its strong drug-polymer interactions and low water uptake, moisture-induced solid-state crystallization was not observed. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/26869398/Solvent_shift_strategy_to_identify_suitable_polymers_to_inhibit_humidity_induced_solid_state_crystallization_of_lacidipine_amorphous_solid_dispersions_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(16)30062-X DB - PRIME DP - Unbound Medicine ER -