35 1 () V o l. 35 N o. 1 2007 1 Journal of N o rthw est A & F U niversity (N aṫ Sci. Ed. ) Jan. 2007 Ξ, (, 712100) [ ]4 ( IPM ) 3 (EL 40 Tw een280) ;,,,,, ( ), EL 402 2IPM ;, 56. 8 nm ;, ;, [ ]; ; ; ; [] R 944. 1 + 7; R 978. 1 + 9 [] A [] 167129387 (2007) 0120054204 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, 712100, 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 56. 8 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 [] 2006207217 [] (130709) [](1977- ),,,, E2m ail: sunhongw u2001@ 163. com [](1960- ),,,,, E2m ail: oyw q506@ sina. com
1 : 55 ( Berberine) ( ), [1 ],,, [2 ], [3 ], ( 10% ),, [4 ],,,,, ( ), 1 1. 1 1. 1. 1 UV 22102 () ; H Z8802S ( ) ; Incubato s SK IP 02. 420 ( ) ; T GL 216B ( ) ; BN icomp 388gZetaPAL S ( Particle Sizing System ) ; H I2 TA CH I () 1. 1. 2( 98. 4%,, 20050928) ; ( ) ; (, 20051024) ; (, 20050828) ; ( IPM,, 20050625) ; (, 20000829) ; (C remopho r EL 40, BA SF ) ; ( D egu ssa ) ; 80 (Tw een280) 1. 1. 3, 1. 2 IPM (C14)(C16 C18) 4 ( > IPM > > ),,, 37 24 h (H PL C) 1. 3 1. 2 EL 40 Tw een280 3 (SF) SF 4 (CoSF), 9 1, 8 2, 7 3, 6 4, 5 5, 4 6, 3 7, 2 8 1 9 (SF CoSF ) SF CoSF, 1. 2,,,,, SF CoSF [425 ] :,, (13 000 rgm in, 30 m in),, 10 100 nm ;,, ;, [5 ] 1. 4 [6 ], 2SF2CoSF,, (13 000 rgm in, 30 m in), 10 100 nm EL 40,,,,, 1. 5 (25 1) 1. 5. 1, 1,, 10 m in, 2% (ph 7. 4) 3 m in,, 1. 5. 2 (2005
56 () 35 ) g IXA IXB, 1. 5. 3, 1. 5. 4 (2005 ) 3 ( ) 100 ml, 37, 50 rgm in,,, 10, 20, 30, 45 60 m in 4 ml,, (340 1) nm 1. 5. 5( ) ( 40, 60 ) ( 4 ) (4 500 500 lx), 5 10 1. 6 1. 6. 1 6, 3 [ 7 ] 1. 6. 2 0. 2 ml 20 ml, 1. 6. 3, 12 (0. 2 ml g ),, 37 24 h, (cm ), SSPP 11. 0, 2 2. 1, (C16 C18) 0. 383, 0. 375, 0. 241 m g g, IPM, 1. 5 m g g, IPM IPM 2. 2, EL 40 (> 2. 0 m g g ), IPM 2 EL 402 4 CoSF,, 4 CoSF 1, 22,, CoSF, CoSF 2. 3 2. 3. 1, ( 1), 500,,, 10 100 nm, 56. 8 4. 3 nm 1 ( 80 000) F ig. 1 E lectron m icro scope of bererbins hydroch lo ric nanom eter m icroem ulsion (80 000 tim es) 2. 3. 2, 56. 8 nm, < 60 nm 75%, < 70 nm 90%,, 2. 3. 3, (2005 ) g 1 ;, (2005 ) 2. 3. 420 m in, 20 m in, 2. 3. 5, 2. 4 1,, > 1. 0
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 + (1. 2 0. 5 C) + (1. 2 0. 2 C) + (1. 2 0. 3 C) + (1. 2 0. 1 C) Cap sule group + (1. 2 0. 6 C) + (1. 2 0. 3 C) + (1. 2 0. 4 C) + (1. 2 0. 1 C) W atery so lution group + (1. 2 0. 7 C) + (1. 2 0. 4 C) + (1. 2 0. 1 C) + (1. 2 0. 3 C) B lank nanom eter m icroem ulsion group + + + (3. 2 0. 4 B ) + + + (3. 2 0. 3 B ) + + + (3. 2 0. 4 B ) + + + (3. 2 0. 2 B ) Berberine nanom eter m icroem ulsion group + + + (4. 8 0. 3 A ) + + + (4. 6 0. 2 A ) + + + (4. 6 0. 3 A ) + + + (4. 4 0. 1 A ) : - < 1. 0 cm, ; + 1. 0 2. 0 cm, ; + + 2. 0 3. 0 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 ],,, : 10 100 nm,,, [11 ], ( ),,,,,,,, :, 200610104418. 2 [] [ 1 ]. [ J ]., 2002, 29 (6) : 4232425. [ 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) : 3752378. [ 3 ],,. [J ]., 2003, 7 (4) : 33237. ( 62 )
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