Development of Enteric Polymer Based Tofacitinib Citrate Pellets via Continuous Manufacturing using Hot-Melt Extrusion Technology : 고온용융압출법 기반 연속공정을 활용한 장용폴리머 기반 토파시티닙 시트르산 장용펠렛 개발|RISS 상세보기

다국어 초록 (Multilingual Abstract)

This study aimed to develop enteric-coated pellets of tofacitinib citrate, a therapeutic agent for ulcerative colitis, using a hot-melt extrusion (HME)-based continuous manufacturing approach. The formulation was designed to shift the drug’s site of action from systemic to local delivery, achieving targeted release at specific intestinal regions (pH ≥ 6.8). Pellets produced via HME exhibited consistent quality throughout the continuous manufacturing process. The prepared pellets were evaluated through drug content uniformity, dissolution testing, and physicochemical characterization using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), and Fourier-transform infrared spectroscopy (FT-IR). TGA results confirmed the thermal stability of the active pharmaceutical ingredient (API) and excipients during processing, while XRD and FT-IR analyses demonstrated the physical and chemical stability between the drug and polymer matrix following HME. Drug content analysis indicated uniform drug distribution at target concentrations, and dissolution testing verified the enteric performance with drug release initiated at pH ≥ 6.8. Additionally, in vivo studies showed a delayed time to reach maximum plasma concentration (Tmax), further supporting the enteric characteristics of the developed pellets. Overall, this study successfully developed enteric-coated tofacitinib citrate pellets via HME-based continuous manufacturing, demonstrating their potential as a locally acting formulation for the treatment of ulcerative colitis.

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목차 (Table of Contents)

1. Introduction 1
2. Materials and methods 5
2.1 Chemicals and materials 5
2.2 Animal models 5
2.3 Preparation of the physical mixture 6

1. Introduction 1
2. Materials and methods 5
2.1 Chemicals and materials 5
2.2 Animal models 5
2.3 Preparation of the physical mixture 6
2.4 Mixture design for the development of TFC enteric pellets 8
2.5 Thermogravimetric analysis (TGA) 8
2.6 Hot melt extrusion (HME) 9
2.7 Evaluation of TFC enteric pellets 11
2.7.1 Stability to lyophilization 11
2.7.2 Drug assay study 11
2.7.3 In vitro drug release study 12
2.8 Scanning electron microscopy (SEM) 13
2.9 Physicochemical characterization 13
2.9.1 Differential scanning calorimetry (DSC) 13
2.9.2 Fourier transform infrared spectroscopy (FT-IR) 14
2.9.3 X-ray diffraction (XRD) 14
2.10 Pharmacokinetics studies 14
3. Results 16
3.1 Analytical result 16
3.2 Formulation composition and hot melt extrusion process results 16
3.3 Thermogravimetric analysis (TGA) results 18
3.4 TFC enteric pellet physicochemical characterization 20
3.4.1 TFC enteric pellet physicochemical characterization 20
3.4.2 In vitro dissolution result 22
3.5 Scanning electron microscopy analysis 24
3.6 Physicochemical characterization 26
3.6.1 DSC analysis 26
3.6.2 X-ray diffraction analysis 28
3.6.3 Fourier transform infrared spectroscopy analysis 30
3.7 In vivo pharmacokinetic study and bioequivalence assessment 32
4. Conclusion 35
5. References 37

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Development of Enteric Polymer Based Tofacitinib Citrate Pellets via Continuous Manufacturing using Hot-Melt Extrusion Technology : 고온용융압출법 기반 연속공정을 활용한 장용폴리머 기반 토파시티닙 시트르산 장용펠렛 개발

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