Study on the Adsorption of Berberine Hydrochloride

Journal of the Pharmaceutical Society of Korea 15. 1-7C 19 71)

Berberine Hydrochloride ^{의 콜에} BS ^한

솔휴 5 ^축 • mmm ^•

(Received January 13. 1971)

Yong Joo Kim, Chong Hak Woo and Shin Keun Kim:

Study on the Adsorption of Berberine Hydrochloride.

When a large quantity of insoluble drugs was added into a solution containing a small amount of soluble drugs, the latter was adsorbed to the former. Their adsorption was expected to alter the drug activity. Berberine hydrochloride (BH) was selected as a soluble drug and tested with frequ­

ently combined insoluble drugs and antacids for their adso­

rption phenomena in purified water, gastric and intestinal fluid test solutions, respectively. The adsorption isotherms of kaolin and natural aluminum silicate with BH in the three media fitted the Langmuir (LM ) equation, and that of talc in purified water and gastric fluid fitted it, but in inte­

stinal fluid it fitted the Freudlich equation. The adsorption isotherm of aluminum hydroxide fitted the LM equation only in intestinal fluid. The degree of adsorption of BH in purified water and gastric fluid is in. the following order:

magnesium trisilicate, kaolin, natural aluminum silicate and talc; in intestinal fluid: magnesium trisilicate, kaolin, talc, natural aluminum silicate and aluminum hydroxide. Magne­

sium stearate did not adsorb BH.

흔풀의 후론 S I S 에 의 파® 떻ffi이 E 슴될 경우 에 ^ 흠 가 되고 따라서 그 에 를 일으킴이 예상되어 행® K 클에 대한 가 fT하여지고 있다 .

Ridout호>는 atropine;jC®?S에서외 kaolin외 SR 를에 ¥후하여 또한 Kubo등은*5 atropine의 m Igfii과외 ® 클에 황하여 또 에 는 Nogami동은3■«> i황a 됐체루S상인 ® 에 서 여 러 몇포의 K * 에 Si한 « ? * 후 » 언 두fe으로 하여 황쯤하고 있 다.

풀놓둥온 3EE®S：0MB1 로 많이 쓰이고 있는 ' 락 촬 (S언 berberine hydrochloride와 이와•

E 슴 되고 있는 및 © 헬 울 하여 fi름sbK. A x m m ^

에서외 그 을 jRlS하여 올 얻었기에 이륨 황콤하는 바이다.

* College of Pharmacy, Seoul National University.

1

Berberine hydrochloride--- 서울약풍에서 제 공 한 Berberine hydrochloride를 축! ; 으로

WiM

후 혔 으 르 Talc, Kaolin(Yamata Co.,), 황알머놓 (Hannoto Co.,), Aluminum hydroxide (Kishida Chemical Co.,), Magnesium stearate (Iwaki C o .,),Magnesium irisilicate (Iw a k i Co.,) 를 의 크기룰 하게 하기 위하여 200 m e sh의 체를 통 과한 것흘 105°

에 서 4혹!ki 활 : 하 여 하였다. _

Berberine hydrochloride의효S Berberine hydrochloride률 확®데시케이타에 서 {1S;

으로 될 때까지 l&lii하여 fflgSTfC에 ^쪽 하 여 iS S 420m/i게서 so토하여 따로 만

■든 별mffii볼에서 J??rberine hydrochloride의 풀울 하였다•

® • 푸ffiSl평축WS1호一Berberine hydrochloride;® J쫓(50배/ m l) 50ml 및 떻to은

■OOmg을 ^하 여 lOOml의 삼각푸라수크에 부고 3 0 ° ® g ff에서 15^ 마다 g g 하고 一달 타rs그 (1,2, 3, 4,5,24^rsT) 황 (ISicbb r"pm)-§i•여 _h할jfiN f t울]•늬 Serberine hydro hloride외 S을 ®토하였다.

이때 혔율 하였다.

m S i idOmg을 JE® 히 fP한하여 lOOmI 삼각푸라스크에 넣고 따로 berberine hydrochloride톨 늙 니 A ± S ® . 론 하 여 ml 10. 20,30, 40, 50;/g롤 충 * 하 게 단든 jS 50ml씩 을 넣-어 주 Si 5!j；l ^ K I iffiS과 같흔 활주놓으로 S # ! ：

을 하였다.

35*■푸 ^ S liiS 두!"aTiPJllS Berberine hydrochloride와 뿐 철£ 의 주 SSPJaStral은 Table 1과 같다.

T able I —Time required for reaching equilibrium.

Insoluble drug Time required for reaching equilibrium

Talc 1

Kaolin 2

Natural aluminum silicate 3

Aluminim hydroxide 2

Magnesium trisilicate 3

® 씀옳fe 를 의 i병;S 롤 L a n ^ u ir 자 Freundlich외 ffi를놓S S 에 하면 Table 2 ~ 5 와 같고 이것을 텔끌하면 Fig. 1-•송과 같다.

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T a b le I I — Adsorption of berberine hydrochloride on talc in purified water, simulated fluid T .S. and simulated intestinal fluid T .S .

gastric

Berberine HCl conc.

Mg/rol.

. c .

/<g/mL tX /(g/lOOmg

m = lOOmg x/m C x io * )

다( ^ ) CXlO-5)

lo g C log

X

Purified water

50 40 30 20 10

43.6 33.6 23.6 13.8

4.2

6.4 6.4 6.4 6 .2 5.8

6.4 6.4 6.4 6.2 5.8

6.8125 5. 2500 3.6871 2.2258 0- 7241

1.6395 1.5263 1.3729 1.1399 0.6232

0.8062 0.8062 0.8062 0.7924 0.7634

Simulated gastric fluid T .S .

50 40 30 20 10

44.9 35.2 25.5 16.0 6.9

5 .1 4.8 4 .5 4.0 3 .1

5 .1 4.8 4 .5 4.0 3 .1

8.8039 7.3333 5.6666 4.0000 2.2258

1.6532 1.5465 1.4065 1.2041 0.8388

0. 7076 0.6812 0.6532 0. 6021 0.4914

Simulated intestinal fluid T.S.

50 40 30 20 10

39.8 30.5 21.3 12.5

4.2

10.2 9 .5 8.7 7 .5 5.8

10.2 9 .5 8.7 7.5 5.8

3.9019 3.2105 2.4482 6666 0.7241

1. 5999 1.4843 1. 3284 1.0969 0- 6128

1.0086 0 .9777 0.9375 0.8 751 0. 7709

T a b le I I I — Adsorption of berberine hydrochlorids on kaolin in purified w a t e r , s i m u l a t e d g a s t r i c

fluid T .S . and simulated intestinal fluid T .S.

Berberine HCl conc.

pg/ml.

C /xg/ml.

X

Mg/lOOmg

m=100mg x/m

^ (X IO *) 다

CXIO'*)

lo g C iog X

Purified water

50 40 30 20 10

4 1.7 31.9 21.9 12.0 3.4

8.3 8-1 8 .1 8.0 6 .6

8.3 S. 1 8 .1 8.0 6.6

5.0240 3. 9382 2. 7037 1.5000 0. 5151

1. 6201 1. 5038 1. 3404 1- 0792 0.5315

0. 9191 0. 9085 0. 9085 0. 9031 0-8195

Simulated gastric fluid T .S .

50 40 30 20 10

42.5 32.7 23.0 14.0 5.5

7 .5 7 .3 7.0 6.0

* 4 .5

7 .5 7.3 7.0 6-0 4.5

5.6566 4. 4794 3. 2857 2. 3333 1. 2222

1.6284 1. 5145 1-3617 1-1461 0-7404

0. 3751 0. 8633 0- 8451 0. 7782 0. 6532

Simulated intestinal fluid T .S.

50 40 3D 20 10

39.3 29.7 21.0 12.6 5 .5

10 .7 i a 3

9.0 7 .3 4-5

10 .7 10.3

9.0 7 .3 4 .5

3.6728 2.8834 2-3333 1.7260 1.2222

1. 5944 1.4728 1.3222 1.1004 a 7404

1. 0294 1. 0128 0. 9542 a 8633 0. 6532

Tftble IV —Adsorption of berberine hydrochloride on natural aluminiiiit silicate in purified water»

simulated gastric fluid T.S. and simulated intestinal fluid T.S.

Berberine HCI conc.

fig/tnL C p g /n d .

X flg/lOOmg

m = 100mg x/m

(X 10») CX lO r*)

logC logx

50 42.2 7.8 7.8 5.4102 1.6253 0.8921

Purified w ater 40 32.2 7.8 7.8 4.1282 1-5079 0.8921

30 22.5 7.5 7.5 ^0000 1-3522 0.8751

20 12.8 7.2 7.2 1.7777 M 0 7 2 0.8573

10 3.9 6 .1 6 .1 0l6393 0-5911 0.7853

50 45.2 4.8 4.8 9.41G6 1.6551 0.6812

Simulated gastric fluid 40 35.3 4.7 4.7 7.5106 1.5478 a 6721

T.S. 30 25.5 4-5 4.5 S G 666 1.4065 0.6532

20 15.8 4.2 4.2 3.7B19 1.1987 0.623^

10 6.5 3.5 3.5 L85T1 a 8129 0.5441

50 41.9 8-1 8-1 5.1728 1-6222 0.9085

Simulated intestinal 40 32.1 7.9 7-9 4.0633 1-5065 0.8976

fluid T.S. 30 22.2 7.9 7.9 2.8461 1.3464 0.8921

20 12.6 7.4 7.4 1.7027 1 . 1664' ~0.8692

10 4.7 5.3 5.3 a 8868 a 6721 0.7243

T able V —Adsorption of berberine hydrochloride on alumimnn hydroxide in simulated intestinal fluid T.S.

Berberine HCI conc.

fig/m l.

C /«g/ml

X

/<g/100mg

m = lOOmg x/m (X10»)

다 (슴) C X 1(T»)

logC log X

50 42.6 7.4 7.4 5.7567 1.6294 0.8692

Simulated intestinal 40 32.9 7.1 7.1 4.6338 1-5172 0.8513

fluid T.S. 30 22.9 7.1 7.1 3.2253 1.3598 0.8513

20 12.9 7 .1 7.1 ^{1.8169 1-1106 0.8513}

10 4 .2 5.8 5.8 a7241 a 6232 0.7634

Langmuir equAtion

C / ^ X ^ = 1 /a b + c /b

Freundlich equation

x ~ k C *

logx=logk+ log C

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March. 1971 황

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Fig*. 1 —Freundlich plots for adsorption of be­

rberine hydrochloride on talc in purified waterC#), simulated gastric fluid T .S.(A ) and simulated intestinal fluid T .S .(0 )

Fig, 2—Freundlich plots for adsorption of berberine hydrochloride on kaolin in puri­

fied waterC#), simulated gastric fluid T.S.

(A ) and simulated intestinal fluid T .S .(O )

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Fiif. 3—Freundlich plots for adsorption of ber­

berine hydrochloride on natural aluminum silicate in purified water( 홈), simulated gastric fluid T.S. ( A ) and simulated intes­

tinal fluid T.S. CO)

Fi 4—Freundlich plots for adsorption of berberine hydrochloride on aluminum hyd­

roxide in simulated intestinal fluid T.S.CO)

Figr. 5— Langmuir plots for adsorption o f berberine on talc in purified Water( 좋), fluid T.S. ( A ) and sifllul- simuiated gasteric

ated intestirtal fluid T.S. ( O )

Fiff. 7—Langmuir plots of adsorption of ber- 그 benne hydrochloride on n atu m aluminum silicate m purified w ater(# ), simulated gastric fluid T.S. ( A ) and simulated intesti­

nal fluid T.S. ( O )

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F ig：. 6— Langmuir plots for adsorption of ber*

berine hydrochloride on kaolin in purified w aterC # ), simulated gastric fluid T .S ,(A ) and siirfulated intestinal fluid T .S .(0 >

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F iy. 8—Langmuir plots of adsorption of ber-

" bcrifle hydrochloride on aluminum hydrox­

ide in simulated intestinal fltrids T.S. ( Q )

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March, 1971 H ^{부 솔} l£

I용

Berberine HCl와 주 ® 혈 음 과 의 을 볼 때 ffliy c , A X g ? g . A ：E ® ?g 4 버I 서의 kaolin, ^ 쌓.S ® 알미자온 fangm uir외, ® 웰 즉 에 一 & 하고 A J：W ^ ^ 에서외 talc외 왔#^은 Langmuir의 ^^ 1 되었으^ A H IE ^S 에선 Freundlich외 K 를쏟

에 一& 되 었 다• 또 한 aluminum . hydroxide는 에 서 만 Langmuir의 ^ 에 一 g ： 되었다 •

K 콜의 JiB에 있어서 S IS tK 및 떼 서 는 magnesium trisilicate, kaolin,.

알미 놓, talc. A 그 쩨 서 는 magnesium trisilicate, kaolin, talc, 랐알미 농, alu­

minum hydroxide외 ® 이였다.

Magnesium stearate는 물과외 함fO：tl이 없기 에 berberine HCl 렸과의 S 든해이 주 5E요하여 전혀 ® 클하지 않았다

JK

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