The p re pa ra tion a nd a ntiba c te ria l a c tiv ity in vitro of be rbe rine hyd rochlo ric na nom e te r m ic roem uls ion
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1 35 1 () V o l. 35 N o Journal of N o rthw est A & F U niversity (N aṫ Sci. Ed. ) Jan Ξ, (, ) [ ]4 ( IPM ) 3 (EL 40 Tw een280) ;,,,,, ( ), EL 402 2IPM ;, nm ;, ;, [ ]; ; ; ; [] R ; R [] A [] (2007) The p re pa ra tion a nd a ntiba c te ria l a c tiv ity in vitro of be rbe rine hyd rochlo ric na nom e te r m ic roem uls ion SUN Hong2w u,ou YAN G W u2qing (Colleg e of A nim al S cience and T echnology, N orthw est A & F U niversity, Y ang ling, S haanx i, , Ch ina) Abstract: T he so lub ility of berberine hydroch lo ric respectively disso lved in fou r k inds of o il ( IPM, soy2 bean o il, peanu t o il, salad o il) and th ree k inds of SF EL 40, soybean pho sphatidylcho line, Tw een280 w ere m easu red by H PL C. T he compo sition w as p relim inarily determ ined u sing the key evo lu tional no rm al of nanom eter m icroem u lsion. T he p seudo tertiary phase diagram s w ere p ro traited by titrating, acco rding to the sequen tial design theo ry. T he fo rm u lation s of the berberine nanoem u lsion w ere op tim ized. T he basic physicochem ical characteristics including the mo rpho logy, diam eter, co lo r, defecation and the self2em u lsif2 ing speed and stab ility w ere studied. T he an tibacterial pharm acodynam ics of the nanom eter m icroem u lsion w as studied in v itro. In th is test, the best compo sition (EL 402Glycero l2ipm ) w as determ ined. T he nanom e2 ter m icroem u lsion w as a k ind of clear so lu tion w ith sm all spherical drop s under election m icro scopy w ith an average diam eter of abou t nm. T he nanom eter m icroem u lsion w as stab le under h igh temperatu re and strong ligh t condition s. Compared w ith the berberine hydroch lo ric tab let, cap su le,w atery so lu tion, b lank ing nanom eter m icroem u lsion to S. au reas, E. coli, S. ag a lactae, S am onella l, berberine hydroch lo ric nanom eter m icroem u lsion had st ronger an t ibacteria l act ion than o ther do sage2fo rm s. T he resu lt s show tha t the nanom eter m icroem u lsion is the good an tibacterial p reparation w ith stab le quality and h igh efficiency. Key words: berberine hydroch lo ric; nanom eter; m icroem u lsion; stab ility; an tibacterial activity [] [] (130709) [](1977- ),,,, E2m ail: sunhongw u2001@ 163. com [](1960- ),,,,, E2m ail: oyw q506@ sina. com
2 1 : 55 ( Berberine) ( ), [1 ],,, [2 ], [3 ], ( 10% ),, [4 ],,,,, ( ), UV () ; H Z8802S ( ) ; Incubato s SK IP ( ) ; T GL 216B ( ) ; BN icomp 388gZetaPAL S ( Particle Sizing System ) ; H I2 TA CH I () ( 98. 4%,, ) ; ( ) ; (, ) ; (, ) ; ( IPM,, ) ; (, ) ; (C remopho r EL 40, BA SF ) ; ( D egu ssa ) ; 80 (Tw een280) , 1. 2 IPM (C14)(C16 C18) 4 ( > IPM > > ),,, h (H PL C) EL 40 Tw een280 3 (SF) SF 4 (CoSF), 9 1, 8 2, 7 3, 6 4, 5 5, 4 6, 3 7, (SF CoSF ) SF CoSF, 1. 2,,,,, SF CoSF [425 ] :,, ( rgm in, 30 m in),, nm ;,, ;, [5 ] 1. 4 [6 ], 2SF2CoSF,, ( rgm in, 30 m in), nm EL 40,,,,, 1. 5 (25 1) , 1,, 10 m in, 2% (ph 7. 4) 3 m in,, (2005
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3 56 () 35 ) g IXA IXB, , (2005 ) 3 ( ) 100 ml, 37, 50 rgm in,,, 10, 20, 30, m in 4 ml,, (340 1) nm ( ) ( 40, 60 ) ( 4 ) ( lx), , 3 [ 7 ] ml 20 ml, , 12 (0. 2 ml g ),, h, (cm ), SSPP 11. 0, , (C16 C18) , , m g g, IPM, 1. 5 m g g, IPM IPM 2. 2, EL 40 (> 2. 0 m g g ), IPM 2 EL CoSF,, 4 CoSF 1, 22,, CoSF, CoSF , ( 1), 500,,, nm, nm 1 ( ) F ig. 1 E lectron m icro scope of bererbins hydroch lo ric nanom eter m icroem ulsion ( tim es) , nm, < 60 nm 75%, < 70 nm 90%,, , (2005 ) g 1 ;, (2005 ) m in, 20 m in, , ,, > 1. 0
4 1 : 57 cm, ; 4, 1(X { SD, n= 3) ;, > 3. 0 cm T able 1 Statistic results of the antibacterial pharm acodynam ics in v itro (X { SD, n= 3) Genius S. au reas E. coli S. ag alactae Sam onellal B lank group - (0 D ) - (0 D ) - (0 D ) - (0 D ) T ablet group + ( C) + ( C) + ( C) + ( C) Cap sule group + ( C) + ( C) + ( C) + ( C) W atery so lution group + ( C) + ( C) + ( C) + ( C) B lank nanom eter m icroem ulsion group ( B ) ( B ) ( B ) ( B ) Berberine nanom eter m icroem ulsion group ( A ) ( A ) ( A ) ( A ) : - < 1. 0 cm, ; cm, ; cm, ; > 3. 0 cm, (P < 0. 01) N o te: -. rep resents antibacterial diam eter is below 1. 0 cm. T h is show s that m edicine has no action. +. rep resents its antibacterial diam eter is from 1. 0 to 2. 0 cm. T h is show s that m edicine has action rep resents antibacterial diam eter is from 2. 0 to 3. 0 cm. T h is show s that m edicine has obvious action rep re2 sents antibacterial diam eter is above 3. 0 cm. This show s that m edicine has strong action. The different upper letters of sam e line rep resents obvious difference (P < 0. 01). 3, ( 10%, 25% ),,,,,,,,, [8 ], SF CoSF, SF,,,,,, SF CoSF,,,,,,, [9210 ],,, : nm,,, [11 ], ( ),,,,,,,, :, [] [ 1 ]. [ J ]., 2002, 29 (6) : [ 2 ] Cernakova M, Ko stalova D. A ntim icrobial activity of berberine a constituent of M ahonia aquif olium [ J ]. Fo lia M icrobio l, 2002, 47 (4) : [ 3 ],,. [J ]., 2003, 7 (4) : ( 62 )
5 62 () 35,,,,, V C V E,, V C V E,,,, [] [ 1 ],,,. C E [ J ]., 2005, 11 (2) : [ 2 ],,,. C E [ J ]., 2001, 21 (3) : [ 3 ],,,. V C V E [J ]., 2003, 23 (4) : [ 4 ],,,. [J ]., 2004, 39 (1) : [ 5 ] Rhee Y S, Cho i J G, Park E S, et al. T ransderm al delivery of ketop rofen using m icroem ulsions [J ]. Int JPharm, 2001, 228: 161. [ 6 ] Kreilgaard M, Pedersen E J, Jaro szew sk i J W. NM R character2 ization and transderm al drug delivery po tential of m icroem ul2 sion system s[j ]. J Contro lled Release, 2000, 69: 421. [ 7 ],,,. [J ]., 2003, 23 (1) : [ 8 ],. C [J ]., 2005, 4 (12) : [ 9 ]. [M ] :, 2000: 799. [ 10 ],,,. [J ]., 2006, 41 (5) : [ 11 ],. [J ]., 2001, 36 (1) : [ 12 ],,,. [J ]., 2005, 06 (27) : [ 13 ],,,. [J ]., 2001, 17 (6) : ( 57 ) [ 4 ],. [ J ]., 2005, 7 (4) : [ 5 ],,,. [J ]., 2006, 41 (5) : [ 6 ],, [J ]., 2005, 36 (6) : [ 7 ],. [M ]. :, 1991: [8 ] XU F. Po lyso rbat280 and its pharm aceutical app lication [J ]. Ch in Pharm J, 1991, 26 (8) : [ 9 ],,,. A [J ]., 2004, 21 (1) : [ 10 ] L ianlil i, Int ranasal N andi, Kwon H Kim. D evelopm ent of an ethyllaurate2based m icroem ulsion fo r rap id2onset intranasal delivery of diazepam [J ]. Int J Pharm, 2002, 23 (7) : [ 11 ] A l2a dham I S, Khalil E, A l2hmoud N D, et al. M icroem ul2 sions are m em brane active antim icrobial, self p reserving sys2 tem s[j ]. J A pp lm icrobio l, 2000, 89 (1) :
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