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Lab 4

This lab document describes procedures for calculating pharmacokinetic parameters from intravenous drug administration. Specifically, it discusses: 1. Calculating drug elimination rate constants from urinary excretion data using the rate method by plotting excretion rate vs. time and the sigma minus method by plotting the log of the amount remaining vs. time. 2. Calculating total, renal, and non-renal drug clearance and the fraction of drug excreted unchanged based on urinary excretion data. 3. Three practice problems are provided to calculate elimination rate constants and clearances for different drugs using the described methods and sample urinary excretion data provided in tables.

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60 views10 pages

Lab 4

This lab document describes procedures for calculating pharmacokinetic parameters from intravenous drug administration. Specifically, it discusses: 1. Calculating drug elimination rate constants from urinary excretion data using the rate method by plotting excretion rate vs. time and the sigma minus method by plotting the log of the amount remaining vs. time. 2. Calculating total, renal, and non-renal drug clearance and the fraction of drug excreted unchanged based on urinary excretion data. 3. Three practice problems are provided to calculate elimination rate constants and clearances for different drugs using the described methods and sample urinary excretion data provided in tables.

Uploaded by

Nora
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Lab 4

Course Name

Biopharmaceutics and Pharmacokinetics


CPT3206

Lab 4

I- Pharmacokinetics of drugs administered by


intravenous route

Calculation of drug elimination rate constant from urinary excretion data


Lab 4

Variables calculated From urine data


1-Cumulative amount excreted in urine in a time interval (Du )

2-Total amount excreted in urine (Du∞)

3-Amount remaining to be excreted in urine (Du∞ - Du )

4-Excretion rate in urine (dDu / dt ) or (∆ Du / ∆t )


Lab 4
2- Calculation of drug elimination rate constant from urinary excretion data

I. Rate Method
By plotting rate of urinary excretion dDu/dt versus time (t*)
Lab 4

Time interval (t) Amount in urine Du/dt Midpoint (T*)


0-2 500 500/2-0 2+0/2
2-4 300 300/4-2 2+4/2

Log dDu/dt

T*
Lab 4

II. Sigma Minus Method


By plotting Log ARE ( Amount remained to be excreted) , (Du∞ - Du )
versus time

Kt
Equation: Log Du∞ - Du = log Du ∞ -
2.303
Log Du∞ - Du
Du∞

Slope = - K /2.303

T
Lab 4

*Total clearance (𝑪𝒍𝒕 ):

𝑪𝒍𝒕 = 𝑲𝑽𝑫
𝑪𝒍𝒕 = 𝑪𝒍𝒓 + 𝑪𝒍𝒏𝒓

*Renal clearance (CLr):

𝑪𝒍𝒓 = 𝒌𝒆 𝑽𝑫

*Non-renal clearance (𝑪𝒍𝒏𝒓 ):

𝑪𝒍𝒏𝒓 = 𝒌𝒎 𝑽𝑫

*Fraction of drug excreted unchanged (Fu):


Du∞ Ke
Fu = 𝑭𝑫𝟎 =
K
Lab 4

Problems
Lab 4

I) A single I.V dose of a new antibiotic was given to a 50 Kg woman


at a dose level of 20 mg/Kg. urine and blood samples were removed
periodically and examined for parent drug. The data is tabulated in
following table:
Time (hr) Cp (mcg/ml) Du (mg)
0.25 4.2 160
0.50 3.5 140
1.00 2.5 200
2.00 1.25 250
4.00 0.31 188
6.00 0.08 46

Estimate (K) by three methods “Plasma – rate method – Sigma minus


method
Lab 4

II) A bolus IV dose of 700 mg of tetracycline HCl was given to an adult male and
over 2 hours-time intervals, urine was collected and assayed for drug. Assuming
first order kinetics and given the data shown in the Table below, plot dDu/dt
versus midpoint time given that average volume distribution is 10 L

Plot the data on semi log paper Amount of drug excreted


Time (hr)
in urine
Evaluate:
i. Total body clearance 0-2 400
ii. Renal clearance 2-4 126
iii. Non renal clearance 4-6 40
6-8 12.6
III) Sulfaethyl thiadiqzole was injected i.v. in a dose of 2 g to a male
weighing 80 kg . The amount of drug excreted unchanged in the
urine is shown in the following table .
Time interval 0-6 3-6 6-9 9-12 12-15 15-24 24-48

Amount 534 436 181 139 110 202 195


excreted (mg)

A. Determine the t1/2 from the urine data using excretion Rate method
& estimate the fraction excreted unchanged .
B. Determine the t 1/2 from the urine data using the cumulative
excretion method .

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