GastroPlus在口服吸收與製劑開發等領域的應用文章列表
(更新至2019年7月)
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凡默谷技術部選取了如何採用GastroPlus軟體(高級房室吸收與轉運ACAT模型和生理藥代動力學PBPK模型)在口服吸收與製劑開發等領域的文獻列表。
希望對您的業務或專業學習有所幫助。內容如下:
01. 使用生理藥代動力學PBPK模型評估卡馬西平過飽和的製劑處方在大鼠體內的生物藥劑學性能
Assessment of Biopharmaceutical Performance of Supersaturating Formulations of Carbamazepine in Rats Using Physiologically Based Pharmacokinetic Modeling. Thakore SD, Thakur PS, Shete G, Gangwal RP, Narang AS, Sangamwar AT, Bansal AK. AAPS PharmSciTech. Apr 30, 2019. IF=2.608
02. 強心甙Cerberin通過PI3K / AKT / mTOR信號轉導抑制的作用發揮抗癌活性
Cardiac glycoside Cerberin exerts anticancer activity through PI3K/AKT/mTOR signal transduction inhibition. Hossan MS, Chan ZY, Collins HM, Shipton FN, Butler MS, Rahmatullah M, Lee JB, Gershkovich P, Kagan L, Khoo TJ, Wiart C, Bradshaw TD. Cancer Lett. Mar 28, 2019. IF=6.508
03. 綜合分析固體形態變化對溶解度和滲透性的影響:案例-RORc抑制劑口服給藥後在大鼠體內的暴露
An Integrated Analysis of Solid Form Change Impact on Solubility and Permeability: Case Study of Oral Exposure in Rats of a RORc Inhibitor. Chiang PC, Nagapudi K, Liu J, Zbieg JR, Plise EG, Deng Y. J Pharm Sci. Feb 7, 2019. IF=3.197
04. 採用基於生理學的吸收模型預測口服緩控制劑和速釋製劑的生物等效性
Physiologically based absorption modeling to predict bioequivalence of controlled release and immediate release oral products. Mitra A, Petek B, Velagapudi R. European Journal of Pharmaceutics and Biopharmaceutics. Volume 134, January 2019, Pages 117-125. IF=4.708
05. 通過體外,多房室轉移系統和機制性口服吸收模型獲得整體的沉澱動力學,從而預測弱鹼性藥物的體內PK
Integration of Precipitation Kinetics From an In vitro, Multicompartment Transfer System and Mechanistic Oral Absorption Modeling for Pharmacokinetic Prediction of Weakly Basic Drugs. Patel S, Zhu W, Xia B, Sharma N, Hermans A, Ehrick JD, Kesisoglou F, Pennington J. J Pharm Sci. January 2019 Volume 108, Issue 1, Pages 574–583. IF=3.197
06. 在GastroPlus™中採用動態流體學和pH模型模擬弱鹼藥物在血管內和體循環的濃度
Application of a Dynamic Fluid & pH Model to Simulate Intraluminal and Systemic Concentrations of a Weak Base in GastroPlus™. Hens B, Bolger MB. J Pharm Sci. January 2019 Volume 108, Issue 1, Pages 305–315. IF=3.197
07. 具有體內預測性的溶出方法和模擬研討會匯總:促進口服藥物製劑處方的開發和口服療效的預測
In Vivo Predictive Dissolution and Simulation Workshop Report: Facilitating the Development of Oral Drug Formulation and the Prediction of Oral Bioperformance. Tsume Y, Patel S, Fotaki N, Bergstrom CAS, Amidon GL, Brasseur JG, Mudie DM, Sun D, Bermejo M, Gao P, Zhu W, Sperry DC, Vertzoni M, Parrott N, Lionberger RA, Kambayashi A, Hermans A, Lu X, Amidon GE. AAPS J. 2018 Sep 6;20(6):100. IF=3.545
08. 採用體外-計算機建模方法評估固體分散劑能否提高纈沙坦溶出度和生物利用度
Assessing the potential of solid dispersions to improve dissolution rate and bioavailability of valsartan: In vitro-in silico approach. Medarević D, Cvijić S, Dobričić V, Mitrić M, Djuriš J, Ibric S. Eur J Pharm Sci. 2018 Nov 1;124:188-198. IF=3.532
09. 基於hPEPT1絕對表達量建立伐昔洛韋的生理藥代動力學PBPK模型及其應用
A physiologically based pharmacokinetic model for valacyclovir established based on absolute expression quantity of hPEPT1 and its application. Sun L, Wang C, Zhang Y. Eur J Pharm Sci. 2018 Oct 15;123:560-568. IF=3.532
10. 採用體外方法評估空腹狀態下,藥物在小腸中的沉澱-PEARRL綜述
In vitro methods to assess drug precipitation in the fasted small intestine – a PEARRL review. O』Dwyer PJ, Litou C, Box KJ, Dressman JB, Kostewicz ES, Kuentz M, Reppas C. J Pharm Pharmacol. 2018 Jun 28. IF=2.39
11. 探討小型豬的胃排空速率:食物類型和預先給藥(甲氧氯普胺)對胃排空的影響
Exploring gastric emptying rate in minipigs: Effect of food type and pre-dosing of metoclopramide. Henze LJ, Griffin BT, Christiansen M, Bundgaard C, Langguth P, Holm R. Eur J Pharm Sci. 2018 Jun 15;118:183-190. IF=3.532
12. 根據鹼性鹽形藥物在胃酸過少或胃酸缺乏的生物相關介質中數據,建立其基於生理學的吸收模型
Physiologically Based Absorption Modeling of Salts of Weak Bases Based on Data in Hypochlorhydric and Achlorhydric Biorelevant Media. Kesisoglou F, Vertzoni M, Reppas C. AAPS PharmSciTech. 2018 Jun 5. IF=2.608
13. 聯合應用體外試驗和計算機模擬的方法指導雷尼替丁胃滯留給藥系統的製備與表徵
An in vitro – in silico approach for the formulation and characterization of ranitidine gastroretentive delivery systems. Cvijić S, Ibric S, Parojcić J, Djuriš J. J Drug Deliv Sci Technol. 2018 June. IF=2.606
14. 通過體外試驗和吸收模型聯用的方法,預測替米沙坦β-環糊精包合複合物調釋製劑
In silico prediction coupled with in vitro experiments and absorption modeling to study the inclusion complex of telmisartan with modified beta-cyclodextrin. Abhishek Chandra, M. Vivek Ghate,K. S. AithalShaila ,A. Lewis. Journal of Inclusion Phenomena and Macrocyclic Chemistry. June 2018, Volume 91, Issue 1–2, pp 47–60. IF=1.429
15. 聯用胃腸道模擬器GIS和雙相溶出,更好地預測BCS IIb類藥物的體內釋放:酮康唑和雷洛昔芬
The Combination of GIS and Biphasic to Better Predict In Vivo Dissolution of BCS Class IIb Drugs, Ketoconazole and Raloxifene. Tsume Y, Igawa N, Drelich AJ, Amidon GE, Amidon GL. J Pharm Sci. 2018 Jan;107(1):307-316. IF=3.197
16. 聯用體外動力學模型和生理藥代動力學PBPK模型,評估聚乙烯吡咯烷酮-乙酸乙烯酯共聚物的體內行為
Combining an In Vitro Kinetic Model with a Physiologically-Based Pharmacokinetic Model to Assess the Potential In Vivo Fate of Polyvinyl Pyrrolidone-Vinyl Acetate Copolymers. Hsieh DS, Luo L, Xu Y, Engstrom JD, Gao Q. Pharm Res. 2018 Feb 28;35(4):79. IF=3.896
17. 採用基於生理學的口服吸收模型研究藥物在腸道中的藥物相互作用
Physiologically Based Oral Absorption Modelling to Study Gut-Level Drug Interactions. Chung J, Kesisoglou F. J Pharm Sci. 2018 Jan;107(1):18-23. IF=3.197
18. 黃體酮納米晶的製備與評價,以減少藥物的肌肉刺激和提高生物利用度
Preparation and Evaluation of Progesterone Nanocrystals to Decrease Muscle Irritation and Improve Bioavailability. Li L, Li W, Sun J, Zhang H, Gao J, Guo F, Yang X, Zhang X, Li Y, Zheng A. AAPS Pharm SciTech. 2018 Apr;19(3):1254-1263. IF=2.608
19. 在辛伐他汀載藥的自微乳化藥物遞送系統開發中的體外/計算機模擬方法
In vitro/in silico approach in the development of simvastatin-loaded self-microemulsifying drug delivery systems. Ćetković Z, Cvijić S, Vasiljević D. Drug Dev Ind Pharm. 2018 May;44(5):849-860. IF=2.367
20.脂質體製劑生物相關性質的表徵,並預測體內暴露
Bio–relevant characterisation of lipidic formulations and prediction of in vivo exposure. Benito-Gallo P. University of Nottingham, 2017.
21. 通過種屬間的PK/PD轉化,評價TRPM8阻斷劑PF-05105679對核心體溫降低的作用
A cross-species translational pharmacokinetic-pharmacodynamic evaluation of core body temperature reduction by the TRPM8 blocker PF-05105679. Gosset J R, Beaumont K, Matsuura T, et al. European Journal of Pharmaceutical Sciences, 2017. IF=3.532
22. 在藥物發現階段,將高親脂性的難溶性化合物鹽形開發成高劑量給藥的脂質SEDDS製劑
Lipophilic salts of poorly soluble compounds to enable high-dose lipidic SEDDS formulations in drug discovery. Morgen M, Saxena A, Chen X Q, et al. European Journal of Pharmaceutics and Biopharmaceutics, 2017, 117: 212-223. IF=4.708
23. 採用具有體內預測力的溶出系統:胃腸模擬器(GIS),探索過飽和程度對BCS IIb類藥物口服吸收的影響,以雙嘧達莫和酮康唑為例
The impact of supersaturation level for oral absorption of BCS class IIb drugs, dipyridamole and ketoconazole, using in vivo predictive dissolution system: Gastrointestinal Simulator (GIS) . Tsume Y, Matsui K, Searls A L, et al. European Journal of Pharmaceutical Sciences, 2017, 102: 126-139. IF=3.532
24. 通過吸收模型和溶出試驗,探索難溶性化合物Basmisanil速釋製劑的釋放特徵
Characterising Drug Release from Immediate-Release Formulations of a Poorly Soluble Compound, Basmisanil, Through Absorption Modelling and Dissolution Testing. Stillhart C, Parrott N J, Lindenberg M, et al. The AAPS journal, 2017, 19(3): 827-836. IF=3.545
25. 探索藥品研發中狗和人的差異性II:採用建模與模擬的方法探索製劑因素對環丙沙星狗體內吸收與溶出的影響
Exploring Canine-Human Differences in Product Performance. Part II: Use of Modeling and Simulation to Explore the Impact of Formulation on Ciprofloxacin In Vivo Absorption and Dissolution in Dogs. Martinez M N, Mistry B, Lukacova V, et al. The AAPS journal, 2017, 19(3): 712-726. IF=3.545
26. 通過體外和計算機建模的方法,表徵他克莫司在具有生物相關溶出條件下的釋放
In vitro and in silico characterisation of Tacrolimus released under biorelevant conditions. Mercuri A, Wu S, Stranzinger S, et al. International journal of pharmaceutics, 2016, 515(1): 271-280. IF=4.213
27. 摻有自納米乳化藥物遞送系統的抗結核藥物的體外-體內-計算機模擬研究
In vitro–in vivo–in silico simulation studies of anti-tubercular drugs doped with a self nanoemulsifying drug delivery system. Hussain A, Singh S K, Singh N, et al. RSC Advances, 2016, 6(95): 93147-93161. IF=3.049
28. 比較狗和人體的腸液對溶解度和生物藥劑學風險評估的影響
Comparing Dog and Human Intestinal Fluids: Implications on Solubility and Biopharmaceutical Risk Assessment [J]. Walsh P L, Stellabott J, Nofsinger R, et al. AAPS PharmSciTech, 2017, 18(4): 1408-1416. IF=2.608
29. 採用體外溶出-滲透池室定量預測pH依賴性藥物與胃酸減少劑的藥物相互作用DDI:採用生理藥代動力學PBPK模型進行比較
Utilizing In Vitro Dissolution-Permeation Chamber for the Quantitative Prediction of pH-Dependent Drug-Drug Interactions with Acid-Reducing Agents: a Comparison with Physiologically Based Pharmacokinetic Modeling [J]. Zhu A Z X, Ho M C D, Gemski C K, et al. The AAPS journal, 2016, 18(6): 1512-1523. IF=3.545
30. 採用生理藥代動力學PBPK模型評估藥物輔料對藥物口服吸收的影響:敏感性分析
Using physiologically based pharmacokinetic (PBPK) modeling to evaluate the impact of pharmaceutical excipients on oral drug absorption: sensitivity analyses [J]. Chow E C Y, Talattof A, Tsakalozou E, et al. The AAPS journal, 2016, 18(6): 1500-1511. IF=3.545
31. 開發用於描述在空腹和餐後條件下氯吡格雷片劑給藥的體外體內相關IVIVC模型
Development of in vitro in vivo correlation models for clopidogrel tablets to describe administration under fasting and fed conditions. Savu S N, Silvestro L, Mircioiu C, et al. Farmacia, 2016, 11(16): 18. IF=1.527
32. 通過胃腸模擬技術探索BCS III類藥物的豁免可行性:拓展到特定部位吸收的試驗
Exploring the Feasibility of Biowaiver Extension of BCS Class III Drugs with Site-Specific Absorption Using Gastrointestinal Simulation Technology [J]. Sun L, Sun J, He Z. European Journal of drug metabolism and pharmacokinetics, 2017, 42(3): 471-487. IF=1.497
33. 採用基於生理學的吸收模型,探討食物和胃液pH值變化對艾樂替尼PK的影響
Physiologically Based Absorption Modeling to Explore the Impact of Food and Gastric pH Changes on the Pharmacokinetics of Alectinib [J]. Parrott N J, Li J Y, Takano R, et al. The AAPS journal, 2016, 18(6): 1464-1474. IF=3.545
34. 用於無定形固體分散體製劑處方的基於生理學的吸收模型
Physiologically Based Absorption Modeling for Amorphous Solid Dispersion Formulations. Mitra A, Zhu W, Kesisoglou F. Molecular pharmaceutics, 2016, 13(9): 3206-3215. IF=4.396
35. 基於Lesinurad速釋片劑的PBPK吸收模型,探索藥品溶出速率和原料藥粒徑規格的豁免
Justification of drug product dissolution rate and drug substance particle size specifications based on absorption PBPK modeling for Lesinurad immediate release tablets. Pepin XJ, Flanagan TR, Holt DJ, Eidelman A, Treacy D, Rowlings CE. (2016) Mol Pharm. Jul 20. 13(9): 3256-3269. IF=4.396
36. 用於酯類前藥臨床試驗藥品緩釋製劑設計的基於生理學的吸收模型
Physiologically Based Absorption Modeling to Design Extended-Release Clinical Products for an Ester Prodrug. Ding X, Day J S, Sperry D C. The AAPS journal, 2016, 18(6): 1424-1438. IF=3.545
37. 採用PBPK吸收模型指導加波沙朵的調釋製劑處方開發,這是一種高溶解度且吸收具有胃腸道區域依賴性的化合物
Utility of PBPK Absorption Modeling to Guide Modified Release Formulation Development of Gaboxadol, a Highly Soluble Compound with Region-Dependent Absorption. Kesisoglou F, Balakrishnan A, Manser K. (2015) J Pharm Sci. Oct 12. IF=3.197
38. 採用建模與模擬探究處方對低溶解度藥物吸收的影響-環丙沙星
Implementing Toxicity Testing in the 21st Century (TT21C): Use of Modeling and Simulation Tools for Understanding the Impact of Formulation on the Absorption of Low Solubility Compound: Ciprofloxacin. Martinez M, Mistry B, Lukacova V, Polli J, Hoag S, Dowling T, Kona R, Fahmy R. AAPS J. Apr 26. IF=3.545
39. 針對腸溶包衣製劑具有生物預測力的溶出方法
Toward Biopredictive Dissolution for Enteric Coated Dosage Forms. Al-Gousous J, Amidon GL, Langguth P. (2016) Mol Pharm. May 10. IF=4.396
40. 溶解度-滲透性的相互影響和口服製劑處方的設計:考慮雙因素比單因素效果更好
The solubility-permeability interplay and oral drug formulation design: Two heads are better than.one. Dahan A, Beig A, Lindley D, Miller JM. (2016) Adv Drug Deliv Rev. Apr 26. IF=15.519
41. 通過模擬大鼠的腸液提高難溶性化合物口服暴露量的預測性能,且該預測是寬劑量範圍的
Simulated rat intestinal fluid improves oral exposure prediction for poorly soluble compounds over a wide dose range. Berghausen J, Seiler FH, Gobeau N, Faller B. ADMET & DMPK 4(1) (2016) 35-53.
42. 孔隙阻塞:防止酒精傾瀉的多顆粒製劑處方的新策略
Pore blocking: An innovative formulation strategy for the design of alcohol resistant multi-particulate dosage forms. Schrank S, Jedinger N, Wu S, Piller M, Roblegg E. (2016) Int J Pharm. 509(1-2):219-28. IF=4.213
43. 採用生理藥代動力學PBPK模型預測雙環醇控釋製劑在人體的PK
Application of physiologically based pharmacokinetic modeling in the prediction of pharmacokinetics of bicyclol controlled-release formulation in human. Wang B, Liu Z, Li D, Yang S, Hu J, Chen H, Sheng L, Li Y. (2015). Eur J Pharm Sci. Jun 24. IF=3.532
44. 生理學吸收模型在安非他命鹽型藥品的仿製藥評價中的應用
Application of Physiologically Based Absorption Modeling for Amphetamine Salts Drug Products in Generic Drug Evaluation. Babiskin AH, Zhang X. (2015). J Pharm Sci. May 13. IF=3.197
45. 自我聚合和過飽和在難溶性弱鹼藥物口服吸收中的作用
Role of Self-Association and Supersaturation in Oral Absorption of a Poorly Soluble Weakly Basic Drug. Narang AS, Badawy S, Ye Q, Patel D, Vincent M, Raghavan K, Huang Y, Yamniuk A, Vig B, Crison J, Derbin G, Xu Y, Ramirez A, Galella M, Rinaldi FA. (2015) Pharm Res. Feb 28. IF=3.896
46. 對比腸道環境的具有生物相關性的模擬溶出介質,評估難溶性藥物的溶解度曲線
Comparison of biorelevant simulated media mimicking the intestinal environment to assess the solubility profiles of poorly soluble drugs. Prasad D, Gu CH, Kuldipkumar A. (2015) Pharm Dev Technol. Feb 23:1-7. IF=2.347
47. 藥學-難溶性是藥學中的難題:探索C型肝炎蛋白酶抑制劑的機制和解決方案
The potency–insolubility conundrum in pharmaceuticals: Mechanism and solution for hepatitis C protease inhibitors. Connelly PR, Snyder PW, Zhang Y, McClain B, Quinn BP, Johnston S, Medek A, Tanoury J, Griffith J, Walters WP, Dokou E, Knezic D, Bransford P. (2015) Biophysical Chem. 196:100-108. IF=1.745
48. 開發溶出和沉澱的合併模型,並用於預測藥物的口服吸收
Development of a Unified Dissolution and Precipitation Model and Its Use for the Prediction of Oral Drug Absorption. Jakubiak P, Wagner B, Grimm HP, Petrig-Schaffland J, Schuler F, Alvarez-Sánchez R. (2016) Mol Pharm. Jan 5. IF=4.396
49. 通過數學模型加速鹽酸二甲雙胍緩釋片劑的開發
Mathematical Model-Based Accelerated Development of Extended-release Metformin Hydrochloride Tablet Formulation. Chen W, Desai D, Good D, Crison J, Timmins P, Paruchuri S, Wang J, Ha K. (2015) AAPS PharmSciTech Oct. 19. IF=2.608
50. 通過調釋製劑的設計降低窄治療指數窄藥物引起的臨床不良反應事件:體外,體內,計算機預測和臨床PK分析
Mitigation of Adverse Clinical Events of a Narrow Target Therapeutic Index Compound through Modified Release Formulation Design: An In Vitro, In Vivo, In Silico, and Clinical Pharmacokinetic Analysis. Good DJ, Hartley R, Mathias N, Crison J, Tirucherai G, Timmins P, Hussain M, Haddadin R, Koo O, Nikfar F, Fung NK. (2015) Mol Pharm. Nov 4. IF=4.396
51. 使用體外、計算機模擬和大鼠體內模型預測具有pH依賴性的藥物吸收:在先導化合物優化階段儘早評估
Prediction of pH dependent absorption using in vitro, in silico, and in vivo rat models: Early liability assessment during lead optimization. Saxena A, Shah D, Padmanabhan S, Gautam SS, Chowan GS, Mandlekar S, Desikan S. (2015) Eur J Pharm Sci. May 8;76:173-180. IF=3.532
52. 使用親水和疏水等級的二氧化矽Aerosil®製備氯雷他定的自微乳釋藥系統SNEDDS固體製劑,並進行PK評估,使用計算機模擬的GastroPlus™的進行體內預測
Solidified SNEDDS of loratadine: formulation using hydrophilic and hydrophobic grades of Aerosil®, pharmacokinetic evaluations and in vivo–in silico predictions using GastroPlus™. Verma S, Singh SK, Verma PRP. (2016) RSC Adv. 6:3099-3116. IF=3.049
53. 以地爾硫卓作為模型藥物,通過新型口服可吞咽IntelliCap(®)裝置對人胃腸道區域的藥物吸收進行定量研究
Novel Orally Swallowable IntelliCap(®) Device to Quantify Regional Drug Absorption in Human GI Tract Using Diltiazem as Model Drug. Becker D, Zhang J, Heimbach T, Penland RC, Wanke C, Shimizu J, Kulmatycki K. (2014) AAPS PharmSciTech. Dec;15(6):1490-7. IF=2.608
54. 新的抗腫瘤吡唑衍生化合物的生物藥劑學概況
Biopharmaceutical profiling of new antitumor pyrazole derivatives. Anuta V, Nitulescu GM, Dinu-Pîrvu CE, Olaru OT. (2014) Molecules. Oct 13;19(10):16381-401. IF=3.06
55. 生物藥劑學分類BCS系統的亞型:用於預測體內溶出(IPD)的方法和IVIVC
The Biopharmaceutics Classification System: Subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC. Tsume Y, Mudie DM, Langguth P, Amidon GE, Amidon GL. (2014) Eur J Pharm Sci. Jan 28. IF=3.532
56. 在藥物早期開發階段,通過臨時調配緩控釋製劑加速候選藥物的開發
Extemporaneously prepared controlled release formulations for accelerating the early phase development of drug candidates. Thombre AG, Berchielli A, Rogers JF. (2014) Drug Discov Today. Feb 19. IF=6.88
57. 新的組織蛋白酶K抑制劑ONO-5334對骨吸收標誌物的影響:對具有不同PK模式的4種緩釋製劑進行研究
Effects of novel cathepsin K inhibitor ONO-5334 on bone resorption markers: a study of four sustained release formulations with different pharmacokinetic patterns. Tanaka M, Hashimoto Y, Sekiya N, Honda N, Deacon S, Yamamoto M. (2013) J Bone Miner Metab. Oct 11. IF=2.31
58. 基於機制性胃腸模擬和人工神經網絡開發的藥物吸收體外-計算機模擬-體內模型:以硝苯地平滲透泵緩釋片為例
In vitro – in silico – in vivo drug absorption model development based on mechanistic gastrointestinal simulation and artificial neural networks: Nifedipine osmotic release tablets case study. Ilic M, Duriš J, Kovacevic I, Ibric S, Parojcic J. (2014) Eur J Pharm Sci. Jun 6. IF=3.532
59. 用於難溶性藥物遞送系統的無定形固體分散體和納米晶技術
Amorphous solid dispersions and nano-crystal technologies for poorly water-soluble drug delivery. Brough C, Williams RO 3rd. (2013) Int J Pharm. Jun 7. IF=4.213
60. 用生理藥代動力學PBPK模型評價藥物鹽形的溶解度,並納入篩選程序:以苯妥英為例
Incorporation of Physiologically Based Pharmacokinetic Modeling in the Evaluation of Solubility Requirements for the Salt Selection Process: A Case Study Using Phenytoin. Chiang PC, Wong H. (2013) AAPS J. Aug. 14. IF=3.545
61. 通過臨床前狗的研究試驗和吸收模型,促進BCS II候選藥物後期的製劑處方橋接
Use of Preclinical Dog Studies and Absorption Modeling to Facilitate Late Stage Formulation Bridging for a BCS II Drug Candidate. Kesisoglou F. (2013) AAPS Pharm SciTech. Sep 11. IF=2.608
62. 評估新化合物的吸收具有pH依賴性的風險:通過新的體外溶出試驗,物理化學性質分析和風險評估策略
Assessing the Risk of pH-Dependent Absorption for New Molecular Entities: A Novel in Vitro Dissolution Test, Physicochemical Analysis, and Risk Assessment Strategy. Mathias NR, Xu Y, Patel D, Grass M, Caldwell B, Jager C, Mullin J, Hansen L, Crison J, Saari A, Gesenberg C, Morrison J, Vig BS, Raghavan K. (2013) Mol Pharm. Sep 13. IF=4.396
63. 通過對阿西替尼Axitinib與人外排和肝臟攝取轉運體的體外相互作用進行表徵,了解這些因素對處置和藥物相互作用的影響
In Vitro Characterization of Axitinib Interactions with Human Efflux and Hepatic Uptake Transporters. Implications for Disposition and Drug Interactions. Reyner E, Sevidal S, West MA, Clouser-Roche A, Freiwald S, Fenner K, Ullah M, Lee C, Smith BJ. (2013) Drug Metab Dispos. May 31. IF=3.354
64. 通過基於生理學的吸收模型,研究阿片類拮抗劑在臨床上PK的變異度
Investigation of clinical pharmacokinetic variability of an opioid antagonist through physiologically based absorption modeling. Ding X, He M, Kulkarni R, Patel N, Zhang X. (2013) J Pharm Sci. 102(8):2859-74. IF=3.197
65. 採用計算機預測腸道pH的變化對BCS II類弱酸性藥物溶出和吸收的影響:布洛芬和酮洛芬
In silico prediction of drug dissolution and absorption with variation in intestinal pH for BCS class II weak acid drugs: ibuprofen and ketoprofen. Tsume Y, Langguth P, Garcia-Arieta A, Amidon GL. (2012) Biopharm. Drug Dispos. doi: 10.1002/bdd.1800. IF=1.611
66. 通過最大可吸收劑量評估臨床藥品的可開發性
Developability assessment of clinical drug products with maximum absorbable doses. Ding X, Rose JP, Van Gelder J. (2012) Int. J. Pharm. 427(2):260-9. IF=4.213
67. 尼羅替尼臨床前PK和針對臨床項目的口服吸收和體循環生理利用度的實際應用
Nilotinib preclinical pharmacokinetics and practical application toward clinical projections of oral absorption and systemic availability. Xia B, Heimbach T, He H, Lin TH. (2012) Biopharm Drug Dispos. Oct. 24. IF=1.611
68. 在藥物發現階段,通過對口服生物利用度的篩選來增強後期製劑的開發
Selection of oral bioavailability enhancing formulations during drug discovery. Zheng W, Jain A, Papoutsakis D, Dannenfelser RM, Panicucci R, Garad S. (2012) Drug Devel. Indus. Pharm. 38(2):235-47. IF=2.367
69. 狗體內胃pH對BCS II類化合物PK的影響:利用人工胃和十二指腸溶出模型和GastroPlus™模擬預測藥物的吸收
Effect of gastric pH on the pharmacokinetics of a BCS Class II compound in dogs: Utilization of an artificial stomach and duodenum dissolution model and GastroPlus™ simulations to predict absorption. Bhattachar SN, Perkins EJ, Tan JS, Burns LJ. (2011) J Pharm Sci. Jun 16. IF=3.197
70. 通過pH稀釋法估算胃腸道不同區域的具有生物相關性的溶解度:採用生理藥代動力學PBPK模型
A pH-Dilution Method for Estimation of Biorelevant Drug Solubility along the Gastrointestinal Tract: Application to Physiologically Based Pharmacokinetic Modeling. Gao Y, Carr RA, Spence JK, Wang WW, Turner TM, Lipari JM, Miller JM. (2010) Mol Pharm. 7(5):1516-26. IF=4.396
71. 對含有十二烷基硫酸鈉的模擬空腹狀態的胃液(FaSSGF)進行評估,並提出改良配方的建議
A critical evaluation of fasted state simulating gastric fluid (FaSSGF) that contains sodium lauryl sulfate and proposal of a modified recipe. Aburub A, Risley DS, Mishra D. (2008). Int J Pharm. 347(1-2):16-22. IF=4.213