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    Lab 4

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    Nora
    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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    Lab 4

    Uploaded by

    Nora
    14 views10 pages
    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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    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.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    14 views10 pages

    Lab 4

    Uploaded by

    Nora
    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.

    Copyright:

    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
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    of 10

    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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