Jirawat Ruamsuk Pharm.

D
Eastern Asia University
Dr.pooh@live.com

November 10, 2010

Effected of pH to Drug
Absorption

Pre-QUIZ

1. pKa Lidocain HCl

2. Unionized fraction/ ionized fraction
(UI/I) Henderson-Hasselbalch equation Lidocain
HCl

3. Lidocain HCl 2% w/v 6

mL 1800 mL
w/v

Pre-QUIZ

1. pKa Lidocain HCl

7.9

2. Unionized fraction/ ionized

fraction (UI/I) Henderson-Hasselbalch equation
Lidocain HCl
pH = pKa + log [ UI ]
[I]

Pre-QUIZ

3. Lidocain HCl 2% w/v

6 mL 1800 mL

1
C1V1 = C2V2
(2)(6) = (C2)(1806)
(2)(6) /1806 = C2

C2 = 0.0066 % w/v

Pre-QUIZ

3. Lidocain HCl 2% w/v

6 mL 1800 mL

2
2% w/v 2 g / 100 mL
= 20 mg / mL
6 mL 20 * 6
= 120 mg
120 mg 1806 mL
6.64 mg/100mL 0.0066 % w/v



0.007% w/v mL
1800 mL
Lidocain HCl 2% w/v


0.007% w/v 1800 mL

CV = CV
CV
(2)(V )
2 V
1.993 V
V

= C(V +V)
= (0.007)(V +1800)
= 0.007 V + 12.6
=12.6
= 6.32 mL


0.0066% w/v 400 mL

CV = CV
CV
(2)(V )
2 V
1.993 V
V

= C(V +V)
= (0.0066)(V +400)
= 0.0066 V + 2.64
=2.64
= 1.324 mL


Lidocain Hcl
(pKa 7.9 )
pH 7.9 50%
(Ionized form; I)
(Unionized fraction; UI)


pH
(Unionized fraction; UI)


pH
(Unionized fraction; UI)


Lidocain Hcl
(pores)

(Unionized fraction)
pH

pH


1.
2. (degree of
ionization)
3.


Lidocaine, the first amino amide-type local anesthetic
Lidocaine alters signal conduction in neurons by
blocking the fast voltage gated sodium (Na+) channels
in the neuronal cell membrane that are responsible for
signal propagation

C14H22N2OHCl

HEMODYNAMICS: Excessive blood levels may cause changes in

cardiac output, total peripheral resistance, and mean arterial
pressure. With central neural blockade these changes may be
attributed to block of autonomic fibers, a direct depressant effect
of the local anesthetic agent on various components of the
cardiovascular system, and/or the beta-adrenergic receptor
stimulating action of epinephrine when present. The net effect is
normally a modest hypotension when the recommended dosages
are not exceeded.

C14H22N2OHCl

3.
C14H22N2OHCl


pH
beaker 400 mL

Endpoint
(Endpoint 2

)

 Video


Endpoint

30 Endpoint
Endpoint >30

1 1-4 pH 6.0
2 5-8 pH 7.0
3 9-12 pH 8.0
4 13-16 pH 9.0
5 17-20 pH 10.0
2 1,22

pH 8.06
2
2


1,6,11,16,21
2,7,12,17,22
3,8,13,18
4,9,14,19
5,10,15,20

16.30 .

 (1)
pH
1
2
3
4
5
6
7
8
9
10
11
12
13

6.0
>30.00
26.33
>30.00
>30.00

7.0

8.0

9.0

7.40
17.50
19.10
3.30
2.59
2.57
4.15
5.03
1.16

10.0

8.06

 (2)
pH
14
15
16
17
18
19
20
21
22
()

UI/I

6.0

7.0

8.0

9.0

10.0

8.06

2.22
3.13
1.0
2.23
1.47
1.3
1.3
4.10
5.22


Time (minute)

30
25
20
15
10
5

0
5

pH

10

11

Post-QUIZ

1. Lidocain HCl

2. Lidocain HCl

3. Lidocain HCl pKa 7.9

Lidocain HCl buffer pH 9

Post-QUIZ

1. Lidocaine HCl

2. Lidocaine HCl

(degree of ionization)

Post-QUIZ

3. Lidocain HCl pKa 7.9

Lidocain HCl buffer pH 9

pH = pKa + log [ UI ] / [I]
pH pKa = log [ UI ] / [I]
9-7.9 = log [ UI ] / [I]
1.1 = log [ UI ] / [I]
[ UI ] / [I] = 12.589/1