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布地奈德直肠原位温敏凝胶的处方设计与优化

沈婷, 陈林, 谢兴亮, 张正爽, 许小红, 张全

沈婷, 陈林, 谢兴亮, 张正爽, 许小红, 张全. 布地奈德直肠原位温敏凝胶的处方设计与优化[J]. 中国药科大学学报, 2018, 49(6): 689-694. DOI: 10.11665/j.issn.1000-5048.20180608
引用本文: 沈婷, 陈林, 谢兴亮, 张正爽, 许小红, 张全. 布地奈德直肠原位温敏凝胶的处方设计与优化[J]. 中国药科大学学报, 2018, 49(6): 689-694. DOI: 10.11665/j.issn.1000-5048.20180608
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SHEN Ting, CHEN Lin, XIE Xingliang, ZHANG Zhengshuang, XU Xiaohong, ZHANG Quan. Preparation and evaluation of the formulation of budesonide rectal in situ thermogel[J]. Journal of China Pharmaceutical University, 2018, 49(6): 689-694. DOI: 10.11665/j.issn.1000-5048.20180608
Citation: SHEN Ting, CHEN Lin, XIE Xingliang, ZHANG Zhengshuang, XU Xiaohong, ZHANG Quan. Preparation and evaluation of the formulation of budesonide rectal in situ thermogel[J]. Journal of China Pharmaceutical University, 2018, 49(6): 689-694. DOI: 10.11665/j.issn.1000-5048.20180608
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布地奈德直肠原位温敏凝胶的处方设计与优化

  • 成都医学院药学院

基金项目: 四川省教育厅成果转化重大培育资助项目(No.18CZ0026)；四川省大学生创新性实验资助项目(No.201713705060)

Preparation and evaluation of the formulation of budesonide rectal in situ thermogel

摘要

    摘要
  • 摘要: 优化布地奈德直肠原位温敏凝胶的制剂处方。采用冷法配制凝胶溶液，反转试管法测定胶凝温度，以胶凝温度为指标，采用星点设计-效应面法，对泊洛沙姆407(P407)、泊洛沙姆188(P188)以及羟丙甲基纤维素(HPMC)的用量进行优化，并考察在大鼠体内的胶凝情况，以Franz扩散池法考察释放性能。确定的最优处方为布地奈德0.002%，HPMC 0.93%，P188 2.00%，P407 18.31%。优化确定了布地奈德直肠用原位温敏凝胶的制剂处方，其能够在直肠广泛与黏附，并长时间释放药物。
    Abstract: To prepare a budesonide rectal thermogel. The gel solution was prepared by cold method, and the gelation temperature of the gel solution was determined by reverse tube method. The amount of poloxamer 407(P407), poloxamer 188(P188)and hydroxy propyl methyl cellulose(HPMC)was optimized by central composite design/response surface method. The in vivo gelation character was investigated after rectal administration of the budesonide thermogel into the rat, and the in vitro drug release from the gel was examined by the Franz diffusion cell method. Finally, the optimal formulation includes 0. 002% budesonide, 0. 93% HPMC, 2. 00% P188, and 18. 31% P407. It is preferable to obtain the appropriate formulation for budesonide rectal in situ thermogel, which can achieve wide distribution and adhesion to the rectum, as well as long-term drug release.
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  • [1] Bai WY,Liu N.Mechanism and efficacy of budesonide in the treatment of inflammatory bowel disease[J].Clin Med J(临床药物治疗杂志),2011,9(2):37-40.
    [2] Santos AA,Ramos CE,Keppler AF,et al.Budesonide-hydroxypropyl-beta-cyclodextrin inclusion complex in binary poloxamer 407/403 system for ulcerative colitis treatment:a physico-chemical study from micelles to hydrogels[J].Colloids Surf B Biointerfaces,2016,138:138-147.
    [3] Li W,Li HJ,Nai XJ,et al.Formulation and preparation optimization of budesonide suspensions for inhalation[J].West China J Pharm Sci(华西药学杂志),2016,31(5):453-455.
    [4] Wang MH,Li YH,Cao XH,et al.Progress in research on ulcerative colitis[J].Chin Med Modern Distance Edu China(中国中医药现代远程教育),2011,9(24):170-175.
    [5] Abdalla MI,Herfarth H.Budesonide for the treatment of ulcerative colitis[J].Expert Opin Pharmacother,2016,17(11):1549-1559.
    [6] Corman.Colorectal Surgery(结直肠外科学)[M].6th Ed.Shanghai:Shanghai Scientific & Technical Publishers,2015:963-985.
    [7] Li MS,Zhu WM,Chen BL.Ulcerative Colitis(溃疡性结肠炎)[M].Beijing:Higher Education Press,2015:33-98.
    [8] Qu DD,Jin SL.Progress in the pathogenesis of ulcerative colitis[J].J Clin Med Pract(实用临床医药杂志),2016(3):184-187.
    [9] Chen YC. Internal Medicine(内科学)[M]. Chongqing:Chongqing University Press,2016:315-323.
    [10] Sullivan JF,Katz JA.Treatment of acute pouchitis[J].Seminars Colon Rectal Surgery,2017,28(3):1-25.
    [11] Gross V,Barmeir S,Lavy A,et al.Budesonide foam versus budesonide enema in active ulcerative proctitis and proctosigmoiditis[J].Aliment Pharmacol Ther,2006,23(2):303-312.
    [12] Chen MW,Chen X,Pan X,et al.Overview of studies on medicinal aerosol foam and its application[J].Prog Pharm Sci(药学进展),2009(12):549-552.
    [13] Sandboran WJ, Bosworth B, Zakko S, et al. Budesonide foam induces remission in patients with mild to moderate ulcerative proctitis and ulcerative proctosigmoiditis[J].Gastroenterology,2015,148(4):740.
    [14] Xue LF,Yin YZ,Xie XL,et al.Preparation and performance evaluation of matrine-loaded thermosensitive in situ gel for rectum[J].Chin Tradit Herbal Drugs(中草药),2018(6):1311-1316.
    [15] Wang LJ,Che KK,Zhu ZJ.Influence of hydroxypropyl-β-cyclodextrin on the formation of poloxamer thermosensitive in situ gel[J].J China Pharm Univ(中国药科大学学报),2014,45(1):54-58.
    [16] Sun J,Jue CY,Zhang C.Preparation and anti-tumor activity of paclitaxel thermo-sensitive hydrogel[J].J China Pharm Univ(中国药科大学学报),2012,43(5):424-429.
    [17] Chen GT,Wu YT,Shi J,et al.Research progress on thermosensitive gels[J].J Guangdong Pharm Univ(广东药学院学报),2017,33(4):556-560.
    [18] Shu Y,Li XF,Wu S,et al.Progress of in situ gel drug delivery system in the application of traditional chinese medicine preparation[J].J Chengdu Univ Tradit Chin Med(成都中医药大学学报),2014,37(3):120-123.
    [19] Wang YX,Zhang R,Li MJ,et al.Study on the process of compound danshen nasal thermosensitive gel forming[J].Lishizhen Med Materia Medica Res(时珍国医国药),2018,29(2):344-346.
    [20] Zhang DS,Zhang ZB,Song XM,et al.Preparation of injectable temperature-sensitive hydrogel and in vitro evaluation[J].Appl Chem Ind(应用化工),2017,46(10):1946-1948.
    [21] Yang L,Wang AB,Liu S.General research situation and clinical application of gel[J].J Liaoning Univ Tradit Chin Med(辽宁中医药大学学报),2014,16(7):147-150.
    [22] Zhao JT,Liu H,Li GK,et al.Research and application progress of thermo-sensitive gels[J].Guangzhou Chem Ind(广州化工),2013,41(24):9-11.
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  • 刊出日期:  2018-12-24

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