1. School of Pharmacy, Zhejiang University of Technology, Hangzhou 310014, China; 2. Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine,Nanjing 210028, China
Abstract��OBJECTIVE To investigate the effect of geniposide phospholipid complex on the degradation of geniposide by intestinal microflora, which provides the rationale for the design of an appropriate geniposide dosage form.METHODS The intestinal flora was collected from fresh rat feces. The geniposide and geniposide physical mixtures and their complexes were incubated with the rat intestinal flora in anaerobic conditions, respectively. Samples were taken at 0,2, 4, 6, 8 and 12 h. The content of geniposide was determined by HPLC. The preparative geniposide phospholipid complexes were characterized by DSC and X-ray diffraction.RESULTS In the physical mixture of geniposide and geniposide phospholipids, geniposide continuously decreased in the first 2 h, while the degradation accelerated at 2 to 4 h and completely degraded at 4 h. In the phospholipid complex group, the content of geniposide was decreased by 67.2% within 6 h, and it was completely degraded at 8 h.CONCLUSION The geniposide can be completely degraded in the gut microbiota of male SD rats in vitro. After the preparation of the phospholipid complex, the degradation rate of geniposide was slowed down. In the physical mixture group, the presence of phospholipids does not delay the degradation of jasminoidin.
NI H, ZHANG Z H, FU H Z. Research and development of Fructus Gardeniae . China J Chin Mater Med(�й���ҩ��־), 2006,31(7):538-541.
[2]
ZHANG Q, DU S Y, LU Y, et al. Studies on O/W partition coefficient and absorption kinetics of geniposide in fructusgardeniae extract in rat intestine . China J Chin Mater Med(�й���ҩ��־), 2009, 34(14):1840-1844.
[3]
TANG L, WU L, SUN B X, et al. Preparation and evaluation of geniposide phospholipid complex. Zhejiang Univ Technol(�㽭��ҵ��ѧѧ��), 2018(1):110-113,118.
[4]
MEN W, CHEN Y, LI Y J, et al. Research progress of biotransformation on effective ingredients of Chinese medicine via intestinal . Chin J Exp Tradit Med Form(�й�ʵ�鷽��ѧ��־),2015, 21(2):229-234.
[5]
CHEN X Y, ZHONG D F, JIANG H, et al. Characterization of some glucuronide conjugates by electrospray ion trap mass spectrometry. Acta Pharm Sin(ҩѧѧ��),1998, 33(11):849-854.
[6]
DAI Y H, WANG M, ZHU Y N, et al. Effect of D-cellobiose on oral bioavailability of gentiopicroside. China J Chin Mater Med(�й���ҩ��־), 2016,41 (10):1855-1859.
[7]
HOU Y C, TSAI S Y, LAI P Y, et al. Metabolism and pharmacokinetics of genipin and geniposide in rats. Food Chem Toxicol(ʳƷ�뻯ѧ����ѧ), 2008, 46(8):2764-2769.
[8]
LIU L J, ZHAO X L, LI Q, et al. Formation mechanism of phospholipid complex . Heilongjiang Med(������ҽҩ), 2009, 22(2):146-147
[9]
CHEN X M, WU X S, KONG D G, et al. Preparation and preliminary study of quality evaluation of ginsenosides phospholipid compound. Qilu Pharm Aff(��³ҩ��), 2001, 30(9):497-498.
[10]
CAO W Y, WANG P Y, FENG B, et al. Biological transformation of ardipusilloside iby human intestinal bacteria in vitro. Res Develop Nat Prod(��Ȼ�����о��뿪��), 2015, 27(8):1357-1361.
[11]
CAO D, FANG Z, ZHU J P, et al. Effect of rat intestinal bacteria on metabolism of pedunculoside in vitro. China Pharm(�й�ҩʦ), 2016, 19(4):621-624.
[12]
YANG B, FAN Z, ZHOU L, et al. In vitro metabolic transformation of syringin by rat intestinal flora. Chin Tradit Herb Drugs(�в�ҩ), 2015, 46(9):1333-1337.
[13]
XIONG W N, HUANG M Q, LIANG J Q, et al. In vitro metabolism of naringin by human intestinal microflora . Chin J Exp Tradit Med Form(�й�ʵ��ҽѧ������־), 2015, 21(12):69-71.
[14]
SINDHUMOL P G, MARIA T, MOHANACHANDRAN P S. Phytosomes: a novel dosage form for enhancemen of bioavailability of botanicals and neutraceuticals. Int J Pharm Pharm Sci, 2010, 2(4):10-14.
[15]
VERMA P, RAM A, JHA A K, et al. Phosphatidylcholine: a revolution in drug delivery technology . Int J Pharm Sci Res, 2010, 1(2):1-2.
[16]
DAI Y H, WANG M, JU J M, et al. Solidification of magnolol phospholipid complex with polyvingypyrrolidone . China J Chin Mater Med(�й���ҩ��־), 2016,41 (12):2250-2254.
[17]
ZHENG L S, NINA, LIU X Q, et al. Study and application of geniposide and genipin. Study Drug Eval(ҩ�������о�), 2012, 35(4):289-298.
[18]
AKAO T, KOBASHI K, ABURADA M. Enzymic studies on the animal and intestinal bacterial metabolism of geniposide. Biol Pharm Bull, 1994, 17(12):1573-1576.
[19]
YANG Y S, ZHANG T, YU S C. Progress in pharmacological research of genipin and its value. Chin Pat Med(�г�ҩ), 2011, 33(1):130-133.
[20]
WANG C J, WANG S W, LIN J K. Suppressive effect of geniposide on the hepatotoxicity and hepatic DNA binding of aflatoxin B 1 in rats. Cancer Lett, 1991, 60(2):95-99.
[21]
YANG H J, FU M H, WU Z L, et al. Experimental studies on hepatotoxicity of rats induced by Fructus Gardeniae. China J Chin Mater Med(�й���ҩ��־), 2006, 31(13):1091-1093.