Biopharmaceutics and Pharmacokinetics

Prepared by: JPMDS

Activity 1
Activity for Elimination & Reaction Kinetics

Demalata, Stephanie Nicole T.

Mamangun, Marianne Francesca D.
3A

1. A drug suspension (125 mg/mL) decays by zero order kinetics with a reaction rate constant
of 0.5 mg/mL/hr. What is the concentration of intact drug remaining after 3 days? How
long will it take the drug to reach 90% of its original concentration?
a. What is the concentration of intact drug remaining after 3 days?
i. Given: C = ?
Co = 125 mg/mL
K = 0.5 mg/mL/hr
t = 3 days = 72 hours
ii. Solution: zero-order kinetics
𝐶 = −𝑘𝑡 + 𝐶𝑜
0.5 𝑚𝑔 125 𝑚𝑔
𝐶 = −( ) (72 ℎ𝑟) + ( )
𝑚𝐿 𝑚𝐿
ℎ𝑟

36 𝑚𝑔 125 𝑚𝑔
𝐶 = (− )+ ( )
𝑚𝐿 𝑚𝐿
𝑚𝑔
𝐶 = 89
𝑚𝐿

b. How long will it take the drug to reach 90% of its original concentration?
i. Given: C = ?
Co = 125 mg/mL
K = 0.5 mg/mL/hr
t = 3 days = 72 hours
ii. Solution: zero-order kinetics
𝑚𝑔 𝑚𝑔
90% 𝑥 125 𝑚𝐿 = 112.5 𝑚𝐿 90% of the initial concentration

𝐶 = −𝑘𝑡 + 𝐶𝑜
(𝐶 − 𝐶𝑜)
𝑡=
−𝑘
 𝑚𝑔 𝑚𝑔
(112.5 𝑚𝐿 − 125 𝑚𝐿 )
𝑡= 𝑚𝑔
−0.5 𝑚𝐿
ℎ𝑟
𝑚𝑔
− 13 𝑚𝐿
𝑡= 𝑚𝑔
−0.5 𝑚𝐿
ℎ𝑟

𝑡 = 25 ℎ𝑟𝑠

2. Initially a drug has concentration of 50mg/mL and after 20 days, the drug concentration
became 24mg/mL. Compute for 1st order rate constant.
i. Given: C = 24mg.mL
Co = 50 mg/mL
K=?
t = 20 days = 480 hours
ii. Solution: first- order kinetics
ln 𝐶 = −𝑘𝑡 + ln 𝐶𝑜
ln 𝐶𝑜 − ln 𝐶
𝑘=
𝑡
𝑚𝑔 𝑚𝑔
ln (50 𝑚𝐿 ) − ln (24 𝑚𝐿 )
𝑘 =
20 𝑑𝑎𝑦𝑠

0.03669845875 0.0367
𝑘= 𝑜𝑟
𝑑𝑎𝑦 𝑑𝑎𝑦
3. A drug has a biological half-life of 2 hours. At the end of eight hours, what percentage of
the drug’s original activity will remain?
i. Given: C = ? (Percentage of initial quantity)
Half-life = 2 hrs
t = 8 hrs
ii. Solution:
Assuming: half-life and time will start at 0, the drug will be 100% available,
as we progress, we will reach 2 as its half-life. As time progresses by 2, we
will reach 8 hrs as the final time. The percentage of the drug will be divided
by 2 each time until we reach 6.25 % at 8 hrs.

Half-life 0 1 2 3 4
Time (hrs) 0 2 4 6 8
Concentration (%) 100 50 25 12.5 6.25
As per numerical solution:
𝑡
1 𝑡1/2
𝑁𝑡 = 𝑁𝑜 ( )
2

1 8 ℎ𝑟𝑠
𝑁𝑡 = 100 ( )2 ℎ𝑟𝑠
2

𝑁𝑡 = 6.25 %