Komar University of Science and Technology

Pharmacy Orientation and Calculation II

Lecture 9: Active Drug Moiety
Dr. Kajan Ezzat
MSc Clinical Pharmacy and International Practice and Policies
 Outline

• Introduction
• Chemically Equivalent Quantities
• Active Drug Moiety Equivalence
 Active Drug Moiety
• When we give a drug we want to produce a pharmacological activity
• The term moiety is the part of the drug compound that produces a
therapeutic response

• Do we express it in the amount of the active drug moiety? Or just the salt
or both? Both
 Introduction
• A pharmacist must be able to calculate the active drug (chemical)
moiety when present in salt, ester, hydrated, or complex chemical
form.
• When quantitatively comparing products of the same drug
moiety but differing in chemical form.
 What is the role of these salts?
• Some drug forms require a salt.
• Without absorption, a drug can not have a therapeutic
effect.
• What is the role of the salts?
• Some drug have salts so to enhance their absorption
or to boost its absorption into the bloodstream or to
increase it effectiveness.
 Introduction
• Most chemical problems involve the use of atomic or equivalent
(combining) weights of the elements
• The validity of their solutions depends on the Law of Definite
Proportions
• The Law of Definite Proportions
• States that elements invariably combine in the same proportion
by weight to form a given compound.
 Atomic Weight
• It is the ratio of the weight of its atom to the weight of an atom of
another element taken as a standard.
 Equivalent (Combining) Weight Of An
Element
• It is the weight of a given element that will combine with (or
displace) 1-g atomic weight of hydrogen (or the equivalent weight of
some other element).
• For example,
• when hydrogen and chlorine react to form HCl, 1.008 g of hydrogen reacts
with 35.45 g of chlorine; therefore, the equivalent weight of chlorine is
35.45.
 Equivalent Weight of a Compound

• The weight of a given compound that is chemically equivalent to

1.008 g of hydrogen.
• 1 mol or 36.46 g of HCl:
• contains 1.008 g of hydrogen, and this amount is displaceable by one
equivalent weight of a metal; hence, its equivalent weight is 36.46
• One mol or 98.09 g of H2SO4:
• contains 2.016 g of hydrogen, which is displaceable by two equivalent
weights of a metal; consequently, its equivalent weight is 98.08/2 or 49.04.
 Example 1
• Calculate the percentage composition of anhydrous dextrose,
C6H12O6.
• C6 H12 O6
(6 X 12.01) + (12X 1.008) + (6X 16.00) =
• 72.06 + 12.096 + 96.00 = 180.16
 Example 1
!".$% ( !".$% ✕ &$$%
• Carbon (C )%: = −−→ ( = = .$%
&'$.&% &$$ &'$.&%
&".$/% 0 &".$/%✕&$$%
• Hydrogen (H)%: = −−→ Y= = 6.71%
&'$.&% &$$% &'$.&%
/% 1 /%✕&$$%
• Oxygen (O)%: = −−→ Z= = 53.29%
&'$.&% &'$.&% &'$.&%

• 40.00% + 6.71% + 53.29% = 100%

 Example 2
Calculate the percentage of lithium (Li) in lithium
carbonate, Li2CO3.
• Molecular weight of lithium carbonate = 74
• Atomic weight of lithium = 7
No of Li Atoms in the compound = 2
"✕! (
• =
!. &$$
&.✕&$$%
• X= =18.9%
!.
 Example 3
A ferrous sulfate elixir contains 220 mg of ferrous sulfate
(FeSO4⋅7H2O) per teaspoonful dose.
How many milligrams of elemental iron are represented in the
dose?
• Molecular weight of FeSO4⋅7H2O = 278
• Atomic weight of Fe = 56
2% (
• =
"!' ""$ 34
2% 5 ""$
• X= = 44.3 circa 44mg in a dose of teaspoonful (5ml)
"!'
 Example 4

• How many milligrams of sodium fluoride (NaF) will provide 500

µg of fluoride ion?
• Na F
23 + 19 = 42
&/ 2$$µ6
• =
." (
." ( 2$$
• X= = 1105µ6÷1000
&/
• X= 1.1 mg
 Chemically Equivalent Quantities; Example 1
• The formula for magnesium citrate oral solution calls for 27.4 g of
anhydrous citric acid (C6H8O7) in 350 mL of the product. How many grams
of citric acid monohydrate (C6H8O7 ⋅ H2O) may be used in place of the
anhydrous salt?
• C6H8O7 ⋅ H2O= 210
• C6H8O7 =192
&/" "!..
• =
"&$ (
"&$ 5 "!..
• X= = 29.976 o7 30 6 of citric acid monohydrate is used to replace
&/"
27.4 g
 Active Drug Moiety Equivalent

• In the drug therapy of diseases the active moiety of drug products is

responsible for the effects.
• The drugs are not only available as active moiety but instead as
salts, esters, complexes.
• In pharmacy practice:
• The pharmacist may need to calculate the active drug moiety in a given
preparation and/or compare the content between products.
 Calculations of Active Drug Moiety in
Compounding Procedures

• Pharmacists are required to perform calculations to determine the

exact quantities of ingredients needed to compound a medication
order.
• This may include the calculation of the precise quantity of the active
moiety required, taking into account the molecular composition of
the substance;
• The anhydrous equivalent if it is a chemical hydrate, and the possible
effect of ambient humidity on the ingredient’s gain or loss of water
 USP Formula
89:;<= >?=:@9 ABC; DE:9=F (>) 89:;<= <FAB>=9/L>M=(J)
=
IJ >?=:@9 ABC; DE:9=F (9) IJ <FAB>=9./L>M= (9)
or
> N
W=
A 9

• W =amount of substance to be weighed

• a = prescribed or calculated weight of active moiety
• b = chemical or formula weight of the ingredient (a) including any water
of hydration
• d = decimal fraction of dry weight (from known moisture content)(d=1; for
no moisture)
• e = formula weight of active drug moiety
 Example 1
• How many mg of aminophylline dihydrate (MW 456) needs to be weighed
to obtain 250 mg anhydrous theophylline (MW 180)?Moisture content of
aminophylline dihydrate= 0.4%; aminophylline contains 2 molecules of
theophylline.
>N
• W=
A9
• D= 1- 0.004=0.996
OPQ D; (RPS D;)
• W= = 318 mg
Q.TTS (USQ)
 Example 2
• How many milligrams of aminophylline (theophylline
ethylenediamine) USP should be weighed to obtain 250 mg of
anhydrous theophylline? The molecular weight of aminophylline
dihydrate is 456, and the container indicates the presence of 0.4%
w/w adsorbed moisture. The molecular weight of theophylline is
180, with 2 molecules present in aminophylline.
• Moisture content = 0.4%
• Exact weight = 1000-0.004=996
TTS
• Fraction= = 0.996
[QQQ
> N OPQ ] RPS
• \= = =317.9 mg
A 9 Q.TTS ] USQ
 Example 3

• What is the percentage strength of methadone (m.w. 313) in a

solution containing 10 mg of methadone hydrochloride (m.w. 349) in
each milliliter?
• Methadone HCl = 10mg/ 1ml (convert to %)
• Methdone HCl % = 10 mg /1ml *100 = 1%
^&^ (
• =
^./ &%
^&^ 5 &%
• X= = 0.89 % circa 0.9%
"./
• or
 Solution
> N
• \=
A 9
•
> ] URT U[UQ
10_6 = −−−→ `= =8.9 mg of Methadone in 1ml
[ ] U[U URT
• Methdone = 8.9 mg /ml ÷ 1000 = 0.0089 g
• Methdone % = 0.0089 g X 100= 0.89 %
 Example 4

• If a prescription calls for the preparation of 30 mL of a 1% solution of

lidocaine (m.w. 234), but for the purposes of solubility the pharmacist
used lidocaine hydrochloride (m.w. 288), how many milligrams of the
latter should be used?
• The amount of lidocaine required: 30 mL x 1% w/v = 0.3 g or 300 mg
> N UQQ a Obb
• \= = =369 mg of Lidocaine Hydrochloride must be used
A 9 [ aOUR