BIOPHARMACEUTICS AND PHARMACOKINETICS

Name: Banag, Angela Joy Date: October 3, 2021

Chiu, Cheryl
Mallari, Abegail
Manuel, Cielo
Section: BSPH 2-Y1-1 Score:

Assignment No. 2
RATES AND ORDERS OF REACTION

The rate of a chemical reaction or process is the velocity with which it occurs. The order
of a reaction refers to the rate to the way in which the concentration of drug or reaction or
process. When the drug concentration changes with respect to time at a constant rate, it follows
Zero order reaction. If the amount of drug is decreasing at a rate that is proportional to the
amount of drug remaining, then the rate of disappearance of drug is following First order
reaction.

1. Define the following terms

Half life
- A drug's half-life is the time it takes for the amount of active substance in your body to
decrease by half. This is dependent on how the drug is processed and eliminated by the
body. It can last from a few hours to several days, or even weeks.

Rate constants
- The proportionality constant in the equation that defines the link between the rate of a
chemical reaction and the concentrations of the reacting substances is the rate constant,
also known as the specific rate constant.

Area under the curve

- The area under the curve, or AUC, is a pharmacological term that refers to the area
under the plot of a drug's plasma concentration vs time after dosing. It contains
information about the drug's exposure and clearance rate from the body.

2. Differentiate linear and non-linear kinetics

LINEAR PHARMACOKINETICS NON-LINEAR PHARMACOKINETICS

Pharmacokinetic parameters for a drug would Pharmacokinetic parameters for a drug can
not change with change in dose. change with change in dose.
Dose independent Dependent in dose
First order kinetics Also called as:
• Mixed order
• Saturated kinetics
• Capacity limited
All semi-log plots of C vs t for different doses Not superimposable.
are superimposable.
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3. Differentiate zero order and first order kinetics. List down the formulas used and units for
each element
Zero order kinetics First order kinetics

Zero-order kinetics is described when a First-order elimination kinetics depends on the

constant amount of drug is eliminated per unit concentration of only one reactant (drug) and
time but the rate is independent of the a constant fraction of the drug in the body is
concentration of the drug. eliminated per unit time. The rate of
elimination is proportional to the amount of
drug in the body. The majority of drugs are
eliminated in this way.
Formulas used
log C = -Kt + log Co
C = -Kot + Co -----------------
2.3
-Ko = Y2 - Y1
----------- ln C = =Kt + ln Co
X2 - X1
-K = 2.3(log Y2 - log Y1)
Half Life: ---------------------------
t ½ = 0.5 Co/Ko X2 - X1

Half Life:
t ½ = 0.693/K

Units used for each variable Units used for each variable
a. Initial concentration a. Initial concentration
Mass/Volume (mg/ml, mg/L) Mass/Volume (mg/ml, mg/L)

b. Rate constant b. Rate constant

Mass/Volume • hr 1/time (hr-, 1/day)
(mg/ml • hr, mg/L • hr)

c. Elimination half life

c. Elimination half life Time (mins, hrs, days)
Time (mins, hrs, days)

4. The conc of formaldehyde remaining after 360 mins was 15 mL from an initial volume of
2000 mL. Compute for the first order rate constant.

-k= 2.3 (logy2 – logy1)

x2 – x1

-k= 2.3 (log200 – log15)

360 mins – 0 min

k= 0.0136/min
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5. A pharmacist weighs exactly 10 g of a drug and dissolved it in 100 mL of water. The

solution is kept at room temperature and samples are removed periodically and assayed
for the drug. The pharmacist obtains the following data:
Drug Concentration Time
(mg/mL) (mins)
100 0
70 120
50 240
35 360
15 480
10 600
5 720
a. Construct a graph by plotting the concentration of drug versus time.

b. Determine the type of its rate of decline.

- First order kinetics.

6. A pharmacist dissolved a few milligrams of a new antibiotic drug into exactly 100 ml of
distilled water and placed the solution in a refrigerator (50C). At various time intervals the
pharmacist removed a 324.62 minims aliquot from the solution and measured the amount
of drug contained in each aliquot. The following data were obtained:
Time (hr) Antibiotic(ug/dL)
0.5 0.92
1.0 0.86
2.0 0.76
3.0 0.66
6.0 0.43
8.0 0.24
12.0 0.09
a. Is the decomposition of this antibiotic a first-order or zero-order process?
- First-order Process
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b. What is the rate of decomposition of this antibiotic?

-k = 2.3 (log y2 – log y1)

x2 – x1

-k = 2.3 (log 0.86 ug/dL – log 0.92 ug/dL)

1.0 hr – 0.5 hr
-k = - 0.1347
k = 0.1347 hr-

c. How many milligrams of antibiotics were in the original solution prepared by the
pharmacist?

C0 = e InC + kt

C0 = e In 0.92 ug/dL +( 0.1347hr x 0.5)

C0 = 0.985 ug/dL

d. Give the equation for the line that best fits the experimental data.

A = -k0(t) + C0 = 0.13 + 0.98

7. A solution of a drug was freshly prepared at a concentration of 200 mg/mL. After 30 days
at 250C, the drug concentration in the solution was 25 mg/dL (0.25 mg/mL).

Time (day) Concentration (mg/ml)

0 200
30 0.25
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a. Assuming first-order kinetics, when will the drug decline to one half of the original
concentration?
Answer: 3.1132 days

t½=?

-k = 2.3 (log y2 – log y1)

x2 – x1

-k = 2.3 (log 0.25mg/ml – log 200mg/ml)

30 days - 0
-k = -0. 2226
k= 0. 2226 day

t ½ = 0.693
k

t ½ = 0.693
0. 2226 day

t ½ = 3.1132 days

b. Assuming zero-order kinetics, when will the drug decline to one half of the original
concentration?

Answer: 360.4903 hrs

t½=?

-k0 = y2 – y1
x2 – x1
-k0 = 0.25 mg/ml – 200 mg/ml
720 hrs - 0
-k0 = - 0.2774 mg/ml • hr
k0 = 0.2774 mg/ml • hr

t ½ = 0.5 (C0)
k0

t ½ = 0.5 (200 mg/ml)

0.2774 mg/ml • hr
t ½ = 360.4903 hrs
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8. How many half-lives (t ½) would it take for 99.9% of any initial concentration of a drug to
decompose? Assume first-order kinetics?

Answer: 9.9553 or 10 (t1/2)

t½=?

C0 = 100 mg x 0.999 = 99.9 mg

C= 100 mg x 0.001 = 0.1 mg

t = 2.3 (log C – log C0) (t1/2)

-k
t = 2.3 (log 0.1 mg – log 99.9 mg) (t1/2)
-0.693
t = 9.9553 or 10 (t1/2)

9. For most drugs the overall rate of drug elimination is proportional to the amount of drug
remaining in the body. What does this imply about the kinetic order of drug elimination?

As it absorbs chemicals and medicines, the human body employs a variety of metabolic and
excretion processes. While the majority of medicines are removed by first-order kinetics,
knowing both zero and first-order kinetics is essential in a therapeutic setting since the two
modes of elimination can be fluid with the same individual molecule.

When administering medicines to attain a therapeutic level and assessing a patient who has
eaten a toxic substance, determination and comprehension of how a certain material is
eliminated are important. Standard blood/plasma tests and evaluation of the decline in
concentration will help in the identification of the consumed drug in toxicology if the ingested
chemical is unknown to the patient and practitioner.

For example, if the chemical is removed using zero-order kinetics, the quantity eliminated is
decided by time rather than the amount consumed, as opposed to first-order kinetics, which
determines the amount eliminated based on the highest blood/plasma concentration rather than
time. Furthermore, once the medication and its properties are identified, a patient who has
ingested a hazardous chemical can be effectively treated.

A doctor must understand the elimination sequence of a drug and utilize the knowledge in
consecutive dose to maintain the therapeutic concentration over a specified time in order to
achieve the desired therapeutic level. Misunderstanding of kinetic elimination can lead to toxic
symptoms and other iatrogenic harm, including death.
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10. A single cell is placed into a culture tube containing nutrient agar. If the number of cells
triples every 2 minutes and the culture tube is completely filled in 12 hours, how long
does it take for the culture tube to be only half full of cells?

Time (mins) No. of Cells

0 1
2 3

-k = 2.3 (log y2 – log y1) / x2 – x1

-k = 2.3 (log 3 – log 1) / 2 – 0
-k = 0.5487
k= - 0.5487

lnC = -kt + lnC0

= - (- 0.5487) (12 hrs) + ln 1

= 7.5844 hours

References:

Half-life. (n.d.) Retrieved from https://www.mind.org.uk/information-support/drugs-and-

treatments/medication/explaining-the-half-life/

Rate Constant. (n.d.) Retrieved from https://www.britannica.com/science/rate-constant

Scheff, J. (2011). Area Under the Curve. Retrieved from

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3152796/