卡爾指數與溶解速率常數的交叉行為關係與混合率的應用:批次對乙醯氨基酚的研究

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許富賓(Fu-Bin Hus) 查詢紙本館藏

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化學工程與材料工程學系

論文名稱

卡爾指數與溶解速率常數的交叉行為關係與混合率的應用:批次對乙醯氨基酚的研究
(A Cross-Performance Relationship between Carr’s Index and Dissolution Rate Constant and the Application of Mixing Rules: The Study of Acetaminophen Batches)

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摘要(中)

在製藥工業上，藥物溶解速率是很重要的參數之ㄧ。藉由傳統方法來決定溶解速率是相當消耗材料與時間的。因此，發展一個能夠預測藥物溶解速率的方法是必要的。Carr’s Index與mixing rules被用來做為預測藥物溶解速率的指標。Carr’s Index原本是作為粉體流動性的指南，而mixing rules原本是發展來測量在異質系統的介電常數、多晶的熱傳導係數、電磁穿透率以及擴散係數。藥物溶解速率測試是用來測量藥物顆粒釋放速率。藥物顆粒是利用濕式造粒法製造。在經過溶解速率測試之後，收集的數據被用來計算溶解速率常數，k。最後，k-C關係式形成，並且預測範圍在經過mixing rules的計算之後能夠被標示出來。最終，藥物溶解速率透過這些方法能夠很快的決定。另外，這些方法也能夠應用在配方的發展上。藉由快速的決定藥物溶解速率，可以決定最好的配方。而本論文研究的模型藥則是對乙醯甲基氨酚。

摘要(英)

In the pharmaceutical industry, the drug dissolution rate was one of the most important parameters. The determination of dissolution rate by conventional method was materials and time consuming. Hence, to develop a method to predict the drug dissolution rate was indispensable. The Carr’s Index, C and the mixing rules were used as an indicator and equations for predicting the drug dissolution rate, respectively. The Carr’s Index was guidance for the powder flowability and the mixing rules were developed originally for measuring the thermal conductivity of a polycrystal, the dielectric constant, magnetic permeability and diffusion coefficient of a heterogeneous system. The drug dissolution rate test was used to measure the drug release rate of granules. The granules were made by wet granulation. After the dissolution rate test, the collected data were utilized to calculate the dissolution rate constant, k. Finally, the k-C relationship was developed and the prediction region was indicated after calculating by mixing rules. Eventually, it is necessary only to implement a few experiments and the drug dissolution rate could rapidly determine by these methods. In addition, these methods could help the formulation development. The determination of the best formulation could be performed through the rapid determination of the dissolution rate. Acetaminophen was used as a model active pharmaceutical ingredient (API) in this thesis.

關鍵字(中)

★ 卡爾指數
★ 溶解速率常數
★ 混合率
★ 對乙醯氨基酚

關鍵字(英)

★ Carr's Index
★ dissolution rate constant
★ Mixing Rules
★ Acetaminophen

論文目次

摘要………………………………………………………………………………………I
Abstract……..………………………………………………………………………… II
Acknowledgments………….….…….………………………………………………...III
Table of Contents……………………...………………………………………………IV
List of Tables…………………..….…………………………………………………...IX
List of Figures……………..………………………………………………………….XI
Chapter 1 Executive summary………….……………………..………………………..1
1.1 Introduction………………………………………………………………….…1
1.2 Brief Introduction of Acetaminophen………………………………………….6
1.3 Conceptual Framework………………………………………………………...8
References………………………………………………………………………...13
Chapter 2 Analytical Instruments……………………………………..………………19
2.1 Introduction…………………………………………………………………...19
2.2 Thermal Analysis……………………………………………………………...22
2.2.1 Differential Scanning Calorimetry (DSC)…………………..………22
2.3 Spectroscopic Identification…………………………………………………..25
2.3.1 Ultraviolet and Visible Spectrophotometer (UV/Vis)………………..25
2.3.2 Fourier Transform Infrared (FT-IR) Microscope……………………28
2.4 Microscopic Methods…………………………………………………………30
2.4.1 Optical Microscopy (OM)…………………………………………...30
2.4.2 Scanning Electron Microscope (SEM)………………………………32
2.5 Surface Properties…………………………………………………………….35
2.5.1 Brunauer-Emmett-Teller (BET)……………………………………..35
2.5.2 Pycnometer…………………………………………………………..37
2.5.3 Sieving……………………………………………………………….40
2.5.4 Mercury Intrusion……………………………………………………42
2.6 Conclusions…………………………………………………………...………44
References……………………………………...…………………………………45
Chapter 3 A Cross-Performance Relationship between Carr’s Index and Dissolution
Rate Constant………………………………………………………………..50
3.1 Introduction…………………………...………………………………………50
3.2 Materials and Instruments…………………………………………………….57
3.2.1 Materials……………………………………………………………..57
3.2.2 Experimental Equipments…………………………………………...58
3.2.3 Analytical Instruments………………………………………………59
3.2.3.1 Dry Sieving and Tapping………………………………………59
3.2.3.2 Optical Microscopy (OM)……………………………………..61
3.2.3.3 Brunauer-Emmett-Teller (BET)………………………………..62
3.2.3.4 Pycnometer and Mercury Intrusion…………………………….62
3.2.3.5 Scanning Electron Microscope (SEM)…………………………63
3.2.3.6 Differential Scanning Calorimetry (DSC)……………………...64
3.2.3.7 Ultraviolet and Visible Spectrophotometer (UV/Vis)……….....64
3.2.3.8 Fourier Transform Infrared (FT-IR) Microscope………………65
3.3 Experiment……………………………………………………………………66
3.3.1 Preparation of Different Particle Size of Acetaminophen…………...66
3.3.2 Wet Granulation……………………………………………………..68
3.3.3 Dissolution…………………………………………………………..70
3.4 Results and Discussion……………………………………….……………….72
3.4.1 Particle and Granule Size Distribution……………………………....72
3.4.1.1 Ingredients……………………………………………………...72
3.4.1.2 Granule Size Distribution and Granule Growth Mechanism…..76
3.4.1.3 Hausner ratio and Carr’s index…………………………………82
3.4.2 Dissolution rate……………………………………………………...87
3.4.2.1 Granule Homogeneity………………………………………….87
3.4.2.2 Kinetics of Dissolution rate…………………………………….90
3.4.2.3 The relationship between the dissolution rate constant k and Carr’ index C…………………………………………………………93
3.5 Conclusions…………………………………………………………………...96
References………………………………………………………………………...99
Chapter 4 The Application of Mixing Rules……………………..………………….108
4.1 Introduction………………………………………………………………….108
4.2 Materials and Instruments…………………………………………………...113
4.2.1 Materials……………………………………………………………113
4.2.2 Experimental Equipments………………………………………….113
4.2.2.1 Ball Miller…………………………………………………….113
4.2.2.2 Granulator……………………………………………………..114
4.2.2.3 Dissolution Test Station……………………………………….114
4.2.3 Analytical Instruments……………………………………………...114
4.2.3.1 Dry Sieving……………………………………………………114
4.2.3.2 Optical Microscopy (OM)…………………………………….115
4.2.3.3 Brunauer-Emmett-Teller (BET)………………………………115
4.2.3.4 Differential Scanning Calorimetry (DSC)…………………….116
4.2.3.5 Ultraviolet and Visible Spectrophotometer (UV/Vis)………...116
4.2.3.6 Scanning Electron Microscope (SEM)………………………..117
4.3 Experiment…………………………………………………………………..118
4.3.1 Ball Milling………………………………………………………...118
4.3.2 Granulation…………………………………………………………119
4.3.3 Granular Mixing……………………………………………………120
4.3.4 Dissolution Test…………………………………………………….120
4.4 Results and Discussion………………………………………………………122
4.4.1 Particle Size Distribution…………………………………………..122
4.4.2 Granule Growth…………………………………………………….124
4.4.3 Dissolution Rate……………………………………………………125
4.4.4 Mixing Rules……………………………………………………….129
4.5 Conclusions………………………………………………………………….132
References……………………………………………………………………….133
Chapter 5 Conclusions and Future Works……………………………………..…….137
Appendix……………………………………………………………………………..A1

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指導教授

李度(Tu Lee)

審核日期

2007-7-19

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