目的 考察钠基蒙脱土(Na-montmorillonite,Na-MMT)对桑叶提取物中1-脱氧野尻霉素(1-deoxynojirimycin,DNJ)是否存在缓释效果。方法 在搅拌条件下使其进入钠基蒙脱土层间,从而制备1-脱氧野尻霉素-蒙脱土复合物。通过计算钠基蒙脱土对1-脱氧野尻霉素的载药量来选择合适的吸附时间、温度、投料比,并对该条件下制备的1-脱氧野尻霉素-蒙脱土复合物进行体外实验,评价缓释效果。结果 当钠基蒙脱土用量为5.00 g,桑叶提取物用量16.00 g(1-脱氧野尻霉素含量25.1%),在100 ℃下,于1 000 mL 去离子水中搅拌1 h时,可制得1-脱氧野尻霉素载药量为111.64 mg·g-1的1-脱氧野尻霉素-蒙脱土复合物。所制备的1-脱氧野尻霉素-蒙脱土复合物在纯净水、磷酸二氢钠缓冲液(pH 7.4)、0.1 mol·L-1盐酸溶液中均能快速释放,且溶液体积越大,1-脱氧野尻霉素释放率越高。结论 钠基蒙脱土对1-脱氧野尻霉素具有缓释效果,可以用于1-脱氧野尻霉素缓释制剂的研究。
Abstract
OBJECTIVE To investigate the sustained-release ability of Na-montmorillonite (Na-MMT) on 1-deoxynojirimycin (DNJ) in mulberry leaf extract (MLE). METHODS In order to prepare DNJ-MMT composite, DNJ was intercalated into the interlayer of MMT by stirring. Time and temperature for adsorption and ratio of DNJ to MMT were determined by calculating the loading of DNJ, then in vitro release experiment was carried out to estimate the sustained-release characteristics of DNJ-MMT. RESULTS DNJ-MMT composite with a drug loading of 111.64 mg·g-1 was obtained by stirring 5.00 g Na-MMT and 16.00 g MLE containing 4 016.0 mg DNJ in 1 000 mL deionized water at 100 ℃ for 1 h. The composite released DNJ quickly in water, potassium phosphate buffer (pH 7.4), and 0.1 mol·L-1 hydrochloric acid solution. With the increasing of volume of hydrochloric acid solution, the release ratio of DNJ also increased correspondingly. CONCLUSION The sustained-release effect of Na-MMT on DNJ is proved. Na-MMT can be used for study of DNJ sustained-release preparations.
关键词
蒙脱土 /
桑叶提取物 /
1-脱氧野尻霉素 /
高效液相色谱法 /
缓释制剂
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Key words
montmorlillonite /
mulberry leaf extract /
DNJ /
HPLC /
sustained-release preparation
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中图分类号：
R944
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参考文献
[1] HUANG J, HUANG S H, ZHAO Z G. Discussion on patterns of domestic and foreign pharmaceutical care for diabetic patients[J]. Chin Pharm J(中国药学杂志), 2014, 49(11):951-954.
[2] CHEN F J, NOBORU N, IKUKO K, et al. Hypoglycemic activity and mechanism of extracts from mulberry leaves (Folium Mori) and Cortex Mori radicis in streptozotocin-induced diabetic mice[J]. Yakugaku Zasshi, 1995, 115(6):476-482.
[3] LI X, ZENG G Y, TAN J B, et al. Active constituents of hypoglycemic part from Morus alba L. [J]. Cent South Pharm(中南药学), 2012, 10(4):245-247.
[4] LI Y G, JI D F, ZHONG S, et al. 1-Deoxynojirimycin inhibits glucose absorption and accelerates glucose metabolism in streptozotocin-induces diabetic mice[J]. Sci Rep, 2013,3(7442):1377.
[5] WANG L Q, PENG J M, WANG X, et al. Carbooxymethylcellulose sodium improves the pharmacodynamics of 1-deoxynojirimycin by changing its absorption characteristic and pharmacokinetics in rats[J]. Pharmazie, 2012, 67(2):168-173.
[6] AKIRA A, KIYOTAKA N, OHKI H, et al. Effect of mulberry leaf extract with enriched 1-deoxynojirimycin content on postprandial glycemic control in subjects with impaired glucose metabolism[J]. J Diabetes Investig, 2011, 2(2):318-323.
[7] CAO X. Studies on pharmacokinetics and metabolites of the effective hypoglycemic part from mulberry leaves in rats[D]. Zhejiang:Jiangsu Univ, 2013.
[8] KIYOTAKA N, HIROYUKI K, TSUYOSHI T. Validation of an ion trap tandem mass spectrometric analysis of mulberry 1-deoxynojirimycin in human plasma:Appliaction to pharmacokinetic studies[J]. Biosci Biotechnol Biochem, 2008, 72(8):2210-2213.
[9] VISERAS C, CEREZO P, SANCHEZ R, et al. Current challenges in clay minerals for drug delivery [J]. Appl Clay Sci, 2010, 48(3):291-295.
[10] FAHIMEH F A, ALI O. A study on sustained release formulations for oral delivery of 5-fluorouracil based on alginate-chitosan/montmorillonite nanocomposite systems[J]. Appl Clay Sci, 2014, 101:288-296.
[11] KASTURI S, BUTOLA B S, MANGALA J. Synthesis and characterization of chlorhexidine acetate drug-montmorillonite intercalates for antibacterial applications[J]. Appl Clay Sci, 2014, 101:477-483.
[12] SUN H L, ZHU L Z. Simultaneous adsorption of organic pollutant and heavy metal onto surfactant-modified organobentonites with chelating ligands[J]. Chem J Chin Univ(高等学校化学学报), 2007, 28(8):1475-1479.
[13] XI L F. Study on preparation and in vitro release experiments of drugs/montomorillonite sustained-release systems[D]. Tianjin:Tianjin Univ, 2004.
[14] MADKOUR A A, MADINA E M, AZZOUNI O E, et al. Smectite in acute diarrhea in children: Adouble-blind placebo-controlled clinical trial[J]. J Pediatr Gastr Nutr, 1993, 17(2):176-181.
[15] DUPONT C, MORENO J L, BARAU E, et al. Effect of diosmectite on intestinal permeability changes in acute diarrhea[J]. J Pediatr Gastr Nutr, 1992, 14(4):413-419.
[16] DROY L M, DROUET Y, SCHATA B, et al. Sodium glycodcoxycholate and sprinability of gastrointestinal mucous: Protective effect of smectite[J]. Gastroenterology, 1985, 88(2):1369-1370.
[17] YANG J H, LU X W, WEI L P, et al. Preparation of metronidazole/MMT antibacterial composite and in vitro release characteristics[J]. Word Chin J Digestol(世界华人消化杂志), 2009, 17 (9):914-917.
[18] ZHANG C Y, WANG J, YIN H H, et al. Preparation and in vitro properties of montomorillontie/matrine nanocomposite[J]. Chin Pharm J(中国药学杂志), 2014,49(2):134-137.
[19] JIN W K, SOO U K, HEUI S L, et al. Determination of 1-deoxynojirimycin in Morus alba. leaves by derivatization with 9-fluorenylmethyl chloroformate followed by reversed-phase high-performance liquid chromatography[J]. J Chromatogr A, 2003, 1002(1-2):93-99.
[20] OZCAN A S, ERDEM B, OZCAN A. Adsorption of acid blue 193 from aqueous solution onto Na-bentonite DTMA-bentonite[J]. J Colloid Interface Sci, 2004, 280(1): 44-54.
[21] ALMEIDA C A P, DEBACHER N A, DOWNS A J, et al. Removal of methylene blue from colored effluents by adsorption on montmorillonite clay[J]. J Colloid Interface Sci, 2009, 332(1):46-53.
[22] LIU F F, DA Y T, ZHANG H, et al. Study of sodium-modification of Ca-bentonite[J]. Non-mentallic Mines(非金属矿), 2010, 33(6):37-39.
[23] Ch. P(2010)Vol Ⅱ(中国药典2010年版. 二部)[S]. 2010:Appendix 85-87.
[24] MENG Y L. Protective effects of attapulgite, montmorillonite and montmorillonite-attapulgite composites on the intestinal tract of weanling piglets [D]. Beijing:Chin Acad Agri Sci, 2011.
[25] GHANSHYAM V J, HASMUKH A P, BHAVESH D K, et al. Montmorillonite intercalated with vitamin B1 as drug carrier[J]. Appl Clay Sci, 2009, 45:248-253.
[26] KIMURA T, NAKAGAWA K, KUBOTA H, et al. Food-grade mulberry powder enriched with 1-deoxynojirimycin suppresses the elevation of post prandial blood glucose in humans[J]. J Agric Food Chem, 2007, 25(14):5869-5874.
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脚注
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基金
国家科技“十一五”重大专项-新药创制项目(2009ZX09102-110)
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