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Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach.
Eur J Pharm Sci. 2016 Jun 10; 88:37-49.EJ

Abstract

Efavirenz is a non-nucleoside reverse transcriptase inhibitor and categorized in to BCS class II drug. The aim of the present investigation was to apply quality by design approach to enhance the solubility, dissolution and stability of amorphous solid dispersions (ASDs) of efavirenz using a combination of Soluplus® and HPMCAS-HF polymers. In design of experiments, the user defined quadratic model was used to study the effect of variable concentrations of Soluplus® and HPMCAS-HF for the formation of ASDs of efavirenz. Similarly, a prototype ASD was made using Soluplus® as a carrier with efavirenz loading of 30%. The efavirenz ASDs granular extrudates were evaluated for saturation solubility as well as dissolution rate studies. X-ray powder diffraction, Differential scanning calorimetry, Fourier transform infrared, Atomic force microscopy and FTIR imaging to determine the solid state of efavirenz in the ASDs. DSC and XRD data confirmed that bulk crystalline efavirenz transformed to the amorphous form during the hot melt extrusion processing. Prototype ASD batch showed instability upon storage as per ICH guidelines over a period of 6months, observations inferred from DSC, XRD and in vitro dissolution studies. The maximum dissolution rate was observed when Soluplus® and HPMCAS-HF was in ratio of (60:20) as optimized by design of experiments study. Moreover, the optimized ASDs batch were stable at 40°C, 75% RH for a period of 6months without any dissolution rate changes, and remained into amorphous state.

Authors+Show Affiliations

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, University under Section-3 of UGC Act-1956, Elite Status & Centre of Excellence - Govt. of Maharashtra, N. P. Marg, Matunga, Mumbai 400019, India. Electronic address: jaywantpawar.ict@gmail.com.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, University under Section-3 of UGC Act-1956, Elite Status & Centre of Excellence - Govt. of Maharashtra, N. P. Marg, Matunga, Mumbai 400019, India.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, University under Section-3 of UGC Act-1956, Elite Status & Centre of Excellence - Govt. of Maharashtra, N. P. Marg, Matunga, Mumbai 400019, India.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, University under Section-3 of UGC Act-1956, Elite Status & Centre of Excellence - Govt. of Maharashtra, N. P. Marg, Matunga, Mumbai 400019, India.Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, University under Section-3 of UGC Act-1956, Elite Status & Centre of Excellence - Govt. of Maharashtra, N. P. Marg, Matunga, Mumbai 400019, India.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27049050

Citation

Pawar, Jaywant, et al. "Solubility and Dissolution Enhancement of Efavirenz Hot Melt Extruded Amorphous Solid Dispersions Using Combination of Polymeric Blends: a QbD Approach." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 88, 2016, pp. 37-49.
Pawar J, Tayade A, Gangurde A, et al. Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach. Eur J Pharm Sci. 2016;88:37-49.
Pawar, J., Tayade, A., Gangurde, A., Moravkar, K., & Amin, P. (2016). Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 88, 37-49. https://doi.org/10.1016/j.ejps.2016.04.001
Pawar J, et al. Solubility and Dissolution Enhancement of Efavirenz Hot Melt Extruded Amorphous Solid Dispersions Using Combination of Polymeric Blends: a QbD Approach. Eur J Pharm Sci. 2016 Jun 10;88:37-49. PubMed PMID: 27049050.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Solubility and dissolution enhancement of efavirenz hot melt extruded amorphous solid dispersions using combination of polymeric blends: A QbD approach. AU - Pawar,Jaywant, AU - Tayade,Apurva, AU - Gangurde,Avinash, AU - Moravkar,Kailas, AU - Amin,Purnima, Y1 - 2016/04/02/ PY - 2015/12/22/received PY - 2016/02/12/revised PY - 2016/04/01/accepted PY - 2016/4/7/entrez PY - 2016/4/7/pubmed PY - 2017/3/28/medline KW - Efavirenz KW - FTIR imaging KW - HPMCAS-HF KW - Hot melt extrusion KW - Solubility KW - Soluplus® SP - 37 EP - 49 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 88 N2 - Efavirenz is a non-nucleoside reverse transcriptase inhibitor and categorized in to BCS class II drug. The aim of the present investigation was to apply quality by design approach to enhance the solubility, dissolution and stability of amorphous solid dispersions (ASDs) of efavirenz using a combination of Soluplus® and HPMCAS-HF polymers. In design of experiments, the user defined quadratic model was used to study the effect of variable concentrations of Soluplus® and HPMCAS-HF for the formation of ASDs of efavirenz. Similarly, a prototype ASD was made using Soluplus® as a carrier with efavirenz loading of 30%. The efavirenz ASDs granular extrudates were evaluated for saturation solubility as well as dissolution rate studies. X-ray powder diffraction, Differential scanning calorimetry, Fourier transform infrared, Atomic force microscopy and FTIR imaging to determine the solid state of efavirenz in the ASDs. DSC and XRD data confirmed that bulk crystalline efavirenz transformed to the amorphous form during the hot melt extrusion processing. Prototype ASD batch showed instability upon storage as per ICH guidelines over a period of 6months, observations inferred from DSC, XRD and in vitro dissolution studies. The maximum dissolution rate was observed when Soluplus® and HPMCAS-HF was in ratio of (60:20) as optimized by design of experiments study. Moreover, the optimized ASDs batch were stable at 40°C, 75% RH for a period of 6months without any dissolution rate changes, and remained into amorphous state. SN - 1879-0720 UR - https://www.unboundmedicine.com/medline/citation/27049050/Solubility_and_dissolution_enhancement_of_efavirenz_hot_melt_extruded_amorphous_solid_dispersions_using_combination_of_polymeric_blends:_A_QbD_approach_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0928-0987(16)30102-6 DB - PRIME DP - Unbound Medicine ER -