没食子栓剂成型工艺研究(1)
[摘要]以没食子水提浸膏为主药，研究其栓剂成型工艺，并对其直肠黏膜刺激性进行评价。用煎煮法制得没食子浸膏，以半合成脂肪酸甘油酯和玫瑰花油为基质，热熔法制备没食子栓剂。测定栓剂重量差异和体外融变时限，UVVis考察药效成分。用新西兰大白兔为受试对象，连续14 d使用没食子直肠栓剂，取结肠组织，病理学评分。最终确定制剂的处方组成为：以半合成脂肪酸酯和玫瑰花油(2∶1)为基质，载药量54%，制得的制剂外形光滑圆锥形，呈褐色；质量差异(143±003) g，平均融变时限(17±2) min；每枚栓剂平均含多酚3324 mg·g-1、鞣质2450 mg·g-1、多糖33 mg·g-1，连续给药对直肠黏膜无刺激。该制剂，处方设计合理、制备工艺简便、剂型适宜、给药方式符合临床使用目的；制剂对给药部位黏膜无刺激性。
[关键词]成型工艺； 没食子； 栓剂； 黏膜刺激性
Process of gallnut suppository preparation
, http://www.100md.com
IMINJAN Mubarak1，2， CHENG Xuemei3， ABUDU Nazuk2， NURULLA Abdurahman2， JI Zhihong1*， UPUR Halmurat4*
(1Xinjiang Qikang Habo Uyghur Medicine Company Limited by Shares， Urumqi 830026， China；
2College of Pharmacy， Xinjiang Medical University， Urumqi 830011， China；
3Laboratory for Standardization of Chinese Medicines， School of Pharmacy， Shanghai University of
Traditional Chinese Medicine， Shanghai 201203， China；
, 百拇医药
4Xinjiang Uygur Autonomous Region Food and Drug Administration， Urumqi 830001， China)
[Abstract]The main objective was to research the process of gallnut suppository preparation with its water extract as the main drug， and evaluate its irritation to rectal mucosa gallnut extract was obtained by decocting method， and its suppository preparation was obtained by fusion method with semisynthetic aliphatic esters and rose flower oil as the matrix Weight difference and in vitro melting time limit of the suppository were assayed and UVVis was used to determine the contents of polyphenols， tannin and saccharide The irritation to colon mucosa was evaluated after successive administration of 14 days to New Zealand white rabbits Finally， the prescription compositions were determined： semisynthetic aliphatic esters and rose flower oil with the ratio of 2：1 as the proper matrix， with the drug loading of 54% The prepared suppository was brown， conical and smooth The weight difference was (143±003) g， with an average melting time limit of (17±2) min The Contents of Polyphenols， tannic and polysaccharide were 3324， 2450， 33 mg·g-1 respectively in each suppository The results also showed that the continuous administration had no irritation to rectal mucosa It can be concluded that the suppository was an acceptable administrate form， whose preparation process was easily controlled， and with no irritation to rectum mucosa.
, http://www.100md.com
[Key words]preparation process； gallnut； suppository； mucosal irritation
潰疡性结肠炎(ulcerative colitis，UC)是炎症性肠道疾病之一，主要发病部位是直肠及乙状结肠。目前，西药以非特异性抗炎药5氨基水杨酸为活性成分的各种制剂为主，中药以辨证施治个体化用药，生物药以靶向抗肿瘤坏死因子α单抗(antiTNFα)等为临床实践中药物治疗一线药应用。从发病率角度UC已成为常见病，但发病机制尚不清楚[1]，使其成为难治性、复杂性疾病。没食子(quercus infectoria)是没食子蜂科昆虫没食子蜂的幼虫寄生于壳斗科植物没食子树幼枝上所产生的虫瘿，又称春虫秋果，具有抗炎作用[2]。维吾尔医学临床实践中，常用于治疗牙龈糜烂、口腔溃疡、疮疡息肉、肠道溃疡、肛门炎等[3]。其中的多酚类成分防止脂质过氧化效果优于抗环血酸[4]。目前没食子治疗UC的使用形式有：水煎液直接咽下、灌肠或将生药粉碎成粉栓剂形式局部应用。, 百拇医药(木巴拉克?伊明江程雪梅娜祖克?阿不都阿卜杜热合曼?努如拉)
[关键词]成型工艺； 没食子； 栓剂； 黏膜刺激性
Process of gallnut suppository preparation
, http://www.100md.com
IMINJAN Mubarak1，2， CHENG Xuemei3， ABUDU Nazuk2， NURULLA Abdurahman2， JI Zhihong1*， UPUR Halmurat4*
(1Xinjiang Qikang Habo Uyghur Medicine Company Limited by Shares， Urumqi 830026， China；
2College of Pharmacy， Xinjiang Medical University， Urumqi 830011， China；
3Laboratory for Standardization of Chinese Medicines， School of Pharmacy， Shanghai University of
Traditional Chinese Medicine， Shanghai 201203， China；
, 百拇医药
4Xinjiang Uygur Autonomous Region Food and Drug Administration， Urumqi 830001， China)
[Abstract]The main objective was to research the process of gallnut suppository preparation with its water extract as the main drug， and evaluate its irritation to rectal mucosa gallnut extract was obtained by decocting method， and its suppository preparation was obtained by fusion method with semisynthetic aliphatic esters and rose flower oil as the matrix Weight difference and in vitro melting time limit of the suppository were assayed and UVVis was used to determine the contents of polyphenols， tannin and saccharide The irritation to colon mucosa was evaluated after successive administration of 14 days to New Zealand white rabbits Finally， the prescription compositions were determined： semisynthetic aliphatic esters and rose flower oil with the ratio of 2：1 as the proper matrix， with the drug loading of 54% The prepared suppository was brown， conical and smooth The weight difference was (143±003) g， with an average melting time limit of (17±2) min The Contents of Polyphenols， tannic and polysaccharide were 3324， 2450， 33 mg·g-1 respectively in each suppository The results also showed that the continuous administration had no irritation to rectal mucosa It can be concluded that the suppository was an acceptable administrate form， whose preparation process was easily controlled， and with no irritation to rectum mucosa.
, http://www.100md.com
[Key words]preparation process； gallnut； suppository； mucosal irritation
潰疡性结肠炎(ulcerative colitis，UC)是炎症性肠道疾病之一，主要发病部位是直肠及乙状结肠。目前，西药以非特异性抗炎药5氨基水杨酸为活性成分的各种制剂为主，中药以辨证施治个体化用药，生物药以靶向抗肿瘤坏死因子α单抗(antiTNFα)等为临床实践中药物治疗一线药应用。从发病率角度UC已成为常见病，但发病机制尚不清楚[1]，使其成为难治性、复杂性疾病。没食子(quercus infectoria)是没食子蜂科昆虫没食子蜂的幼虫寄生于壳斗科植物没食子树幼枝上所产生的虫瘿，又称春虫秋果，具有抗炎作用[2]。维吾尔医学临床实践中，常用于治疗牙龈糜烂、口腔溃疡、疮疡息肉、肠道溃疡、肛门炎等[3]。其中的多酚类成分防止脂质过氧化效果优于抗环血酸[4]。目前没食子治疗UC的使用形式有：水煎液直接咽下、灌肠或将生药粉碎成粉栓剂形式局部应用。, 百拇医药(木巴拉克?伊明江程雪梅娜祖克?阿不都阿卜杜热合曼?努如拉)