Tags

Type your tag names separated by a space and hit enter

Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407.
AAPS PharmSciTech. 2016 Dec; 17(6):1428-1440.AP

Abstract

Aim of current research was to prepare ibuprofen-poloxamer 407 binary mixtures using fusion method and characterize them for their physicochemical and performance properties. Binary mixtures of ibuprofen and poloxamer were prepared in three different ratios (1:0.25, 1:0.5, and 1:0.75, respectively) using a water-jacketed high shear mixer. In vitro dissolution and saturation solubility studies were carried out for the drug, physical mixtures, and formulations for all ratios in de-ionized water, 0.1 N HCl (pH = 1.2), and phosphate buffer (pH = 7.2). Thermal and physical characterization of samples was done using modulated differential scanning calorimetry (mDSC), X-ray powder diffraction (XRD), and infrared spectroscopy (FTIR). Flow properties were evaluated using a powder rheometer. Maximum solubility enhancement was seen in acidic media for fused formulations where the ratio 1:0.75 had 18-fold increase. In vitro dissolution studies showed dissolution rate enhancement for physical mixtures and the formulations in all three media. The most pronounced effect was seen for formulation (1:0.75) in acidic media where the cumulative drug release was 58.27% while for drug, it was 3.67%. Model independent statistical methods and ANOVA based methods were used to check the significance of difference in the dissolution profiles. Thermograms from mDSC showed a characteristic peak for all formulations with Tpeak of around 45°C which suggested formation of a eutectic mixture. XRD data displayed that crystalline nature of ibuprofen was intact in the formulations. This work shows the effect of eutectic formation and micellar solubilization between ibuprofen and poloxamer at the given ratios on its solubility and dissolution rate enhancement.

Authors+Show Affiliations

Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Division of Pharmaceutical Sciences, Long Island University, Brooklyn, New York, 11201, USA.Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Division of Pharmaceutical Sciences, Long Island University, Brooklyn, New York, 11201, USA.Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Division of Pharmaceutical Sciences, Long Island University, Brooklyn, New York, 11201, USA. rutesh.dave@liu.edu.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

26817763

Citation

Dugar, Rohit P., et al. "Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407." AAPS PharmSciTech, vol. 17, no. 6, 2016, pp. 1428-1440.
Dugar RP, Gajera BY, Dave RH. Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407. AAPS PharmSciTech. 2016;17(6):1428-1440.
Dugar, R. P., Gajera, B. Y., & Dave, R. H. (2016). Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407. AAPS PharmSciTech, 17(6), 1428-1440.
Dugar RP, Gajera BY, Dave RH. Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407. AAPS PharmSciTech. 2016;17(6):1428-1440. PubMed PMID: 26817763.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407. AU - Dugar,Rohit P, AU - Gajera,Bhavin Y, AU - Dave,Rutesh H, Y1 - 2016/01/27/ PY - 2015/09/25/received PY - 2016/01/13/accepted PY - 2016/1/29/pubmed PY - 2017/1/18/medline PY - 2016/1/29/entrez KW - dissolution rate enhancement KW - fusion method KW - ibuprofen KW - poloxamer KW - solubility enhancement SP - 1428 EP - 1440 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 17 IS - 6 N2 - Aim of current research was to prepare ibuprofen-poloxamer 407 binary mixtures using fusion method and characterize them for their physicochemical and performance properties. Binary mixtures of ibuprofen and poloxamer were prepared in three different ratios (1:0.25, 1:0.5, and 1:0.75, respectively) using a water-jacketed high shear mixer. In vitro dissolution and saturation solubility studies were carried out for the drug, physical mixtures, and formulations for all ratios in de-ionized water, 0.1 N HCl (pH = 1.2), and phosphate buffer (pH = 7.2). Thermal and physical characterization of samples was done using modulated differential scanning calorimetry (mDSC), X-ray powder diffraction (XRD), and infrared spectroscopy (FTIR). Flow properties were evaluated using a powder rheometer. Maximum solubility enhancement was seen in acidic media for fused formulations where the ratio 1:0.75 had 18-fold increase. In vitro dissolution studies showed dissolution rate enhancement for physical mixtures and the formulations in all three media. The most pronounced effect was seen for formulation (1:0.75) in acidic media where the cumulative drug release was 58.27% while for drug, it was 3.67%. Model independent statistical methods and ANOVA based methods were used to check the significance of difference in the dissolution profiles. Thermograms from mDSC showed a characteristic peak for all formulations with Tpeak of around 45°C which suggested formation of a eutectic mixture. XRD data displayed that crystalline nature of ibuprofen was intact in the formulations. This work shows the effect of eutectic formation and micellar solubilization between ibuprofen and poloxamer at the given ratios on its solubility and dissolution rate enhancement. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/26817763/Fusion_Method_for_Solubility_and_Dissolution_Rate_Enhancement_of_Ibuprofen_Using_Block_Copolymer_Poloxamer_407_ DB - PRIME DP - Unbound Medicine ER -