Pharmaceutical Compounding Lab

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University of Sulaimani

College of Pharmacy
Dept. of Pharmaceutics
2017

Practical Pharmaceutical
Compounding

Prepared by:
Dr. rer. nat. Rebaz H. Ali
Lab. No. 1 First Semester Simple Solutions

Some useful abbreviations

Abbreviation Meaning Abbreviation Meaning


aa Of each a.c. Before meals
ad Up to a.d. Right ear
a.m. Morning amp. ampul
aq. Water a.s. left ear
a.u. Each ear b.i.d. twice a day
c. With cap. capsule
cc Cubic centimeter Comp. compound
disc. Discontinue Disp. dispense
DW Distilled water Fl fluid
Ft. Make gr grain
gtt. Drop hr. hour
h.s. At bed time noct. night
non rep. Don’t repeat NOP nothing by mouth
o.d. Right eye o.l. left eye
o.s. Left eye o.u. each eye
p.c. After meals p.m. after noon, evening
p.o. Per mouth q.d. every day
q.h. Every hour q.i.d. four times daily
q.o.d Every other day q.s. sufficient quantity
sig. Write on label ss half
tbsp. Tablespoonful t.i.d. three times a aday
t.i.w. Three times a week tsp. teaspoonful

SS = ½, I = 1, V = 5, X =10, L =50, C =100, D = 500, M = 1000


Liquid measure Weight measure
1 mL = 16.2 ɱ minims (drops) 1 kg = 2.2 Ib (poud)
1 fluidounce = 29.6 mL 1 g = 15.4 gr
1 pint = 473 mL 1 gr = 64.8 mg
1 tumblerful = fl oz viii = 240 mL
1 teacupful = fl oz iv = 120 mL
1 tablespoonful = fl oz ss = 15 mL
1 teaspoonful = fl dm I = 5 mL

Practical pharmaceutical compounding 1


Lab. No. 1 First Semester Simple Solutions

Simple solution

It is a liquid pharmaceutical preparation consists of one or more chemical substance in


one phase system which is physically homogeneous.
Types of solution
 Liquid in liquid like alcohol in water.
 Gas in liquid like ammonia in water.
 Solid in liquid like NaCl in water.

Classification according to method of preparation:


 Solution prepared by simple solution method.
 Solution prepared by chemical reaction.
 Solution prepared by simple method with sterilization like ophthalmic solution,
irrigation solution, anticoagulant.
 Solution prepared by extraction.

Classification according to their use:


Gargle, mouth wash, injection, drops, spray, oral solution…..etc.

General method for preparation of simple solution:


 Weigh solid ingredients and mix them together, then dissolve it in ¾ volume of
the vehicle in a beaker or conical flask.
 Subtract any volume of liquid if exist in the prescription from ¾, and then
dissolve the solid ingredient in remainder of ¾.
 After dissolution of solid ingredients add any liquid ingredient if exist then
complete the volume by adding the vehicle.
 Keep prepared dosage form in a suitable container then label it.

Practical pharmaceutical compounding 2


Lab. No. 1 First Semester Simple Solutions

Notes:
 If the solid ingredient in form of crystal; use mortar and pestle to grind it well so
as to decrease particle size (increase solubility by increasing surface area).
 Choose the solvent that dissolves solid ingredient easily (like dissolve like).
 Pink label use for external preparation and white label for internal preparations.

Rx Sodium Chloride Solution


Sodium chloride 9g
Purified water 1000 mL
Procedure: dissolve sodium chloride in sufficient amount of purified water to produce
1000mL and filter.
Use: electrolyte replenisher.
Explanation: sodium chloride solution 0.9%w/v is also known as normal saline solution
which is used to make the preparation isotonic with blood serum, that is, the solution
has the same osmotic pressure as blood serum, and therefore readily diffuses through
the walls of small arteries, veins and capillaries, without causing dilation or collapse.
Similarly RBCs are unaffected. Sometime sodium chloride solution is also used as
irrigation fluid.

Rx Hydrogen Peroxide Solution


Hydrogen peroxide 30 mL
Water 100 mL
Uses: mild antiseptic, astringent and 1.6% is used in the deodorant, gargle and mouth
wash.

Practical pharmaceutical compounding 3


Lab. No. 1 First Semester Simple Solutions

Rx Carminative Mixture for infant


Sodium Bicarbonate 0.06 g (antacid)
Aromatic Spirit of Ammonia 0.06 mL (carminative)
Compound Tr. Of Cardamom 0.12 mL (carminative and flavor)
Glycerin 0.3 mL (sweetening agent)
Peppermint water q.s. 4 mL (vehicle)
Fit. Mist.
Mitt. 40mL

Rx Carminative Mixture for Adult


Sodium bicarbonate gr vii
Aromatic Spirit of Ammonia ɱ xv
Comp. Tr. Of Cardamom ɱx
Strong Tr. Of ginger ɱx
Peppermint water q.s. fl oz
Fit. Mist.
Mitt. fl oz iii
Sig. fl dm ss t.i.d p.c.

Rx Carminative Pediatric Mixture with Chloralhydrate


Chloralhydrate 0.03 g
Compound Tr. Cardamom 0.18 mL
Aromatic Spirit of Ammonia 0.12 mL
Glycerin 0.3 mL
Peppermint water q.s. 5 mL
Fit. Mist.
Mitt. 30 mL
Sig. fl dm t.i.d. p.c.

Practical pharmaceutical compounding 4


Lab. No. 1 First Semester Simple Solutions

Peppermint water
Peppermint oil has carminative, antiseptic and flavoring properties and has been
included to a range of official and non-official pharmaceutical preparations; which is a
saturated solution of peppermint oil (0.05% v/v) in water.
Peppermint water usually prepared by diluting one part of concentrated peppermint
water (2% v/v peppermint oil in solution, ethanol has to be included in the formulation
as a co-solvent) with 39 parts of purified water (1 in 40 dilution).

Rx
Prepare 500mL potassium permanganate solution 0.2% and label with directions for
preparing 2 liters quantities of a 1 in 8000 solution for use as an antiseptic footbath.
 Prepare concentrated solution (0.2%) as follow:
Potassium permanganate 1g
Water for preparations qs 500 mL
Strength of dilute solution is 1 in 8000 = 0.0125%

Method 1:
 Divide the request (2 L) by the dilution factor, the result is the amount of the
concentrated that required to be diluted to the request.
 2000 mL ÷ 16 = 125 mL of the concentrated solution
 Take 125 mL of the concentrated solution, then add water to 2 L.
Method 2:
C1 X V1 = C2 X V2
0.002 X ? = 0.000125 X 2000 mL (2 L)
? = 125 mL
So, take 125 ml of the concentrated solution (0.2%) and add water to 2 L.

Practical pharmaceutical compounding 5


Lab. No. 1 First Semester Simple Solutions

Rx Calculate the quantity of potassium permanganate required to prepare 200mL of a


0.25% w/v solution and give dilution directions for 100mL quantities of a 0.0125%
solution of potassium permanganate.
Potassium permanganate 0.25 g
Water qs 100 mL
 Weigh 0.5 g potassium permanganate
 Put it in a beaker and add some water to dissolve it
 Complete the volume of the solution to 200 by using volumetric flask.

100 ÷ 20 = 5 mL
 Take 5 mL of 0.25% solution and add water to 100 mL.

Homework
Make a calculation according to C1 X V1 = C2 X V2

Practical pharmaceutical compounding 6


Lab. No. 2 First Semester Simple Solutions

Rx Aqueous Iodine Solution (Lugol’s solution)


Iodine 50 g
Potassium Iodide 100 g
Purified water q.s. 1000 mL
Fit. Mist.
Mitt. 20mL
Sig. 0.3 mL diluted with water or milk t.i.d.
Use: Treatment of hypothyroidism
Procedure:
 Dissolve iodine in concentrated solution of KI.
 Shake it well until iodine dissolve.
 Complete the volume by purified water up to 1000 mL.

Rx Weak Iodine Solution or Tr. Iodine (external use)


Iodine 20 g
NaI 24 g
DW 500 mL
Alcohol (96%) q.s. 1000 mL
Fit. Mist.
Mitt. 50 mL
Sig. b.i.d externally
Procedure: dissolve Iodine and NaI in 500 mL of DW, and then add alcohol to 1000 mL.

Practical pharmaceutical compounding 7


Lab. No. 2 First Semester Simple Solutions

Rx Strong Iodine Tincture Solution


Iodine 70 g
KI 50 g
DW 50 mL
Alcohol (96%) q.s. 1000 mL
Use: both weak and strong iodine solution use as antiseptic.
Dissolve the KI in DW, add iodine and agitated until get a solution, then add alcohol to
1000 mL.

Practical pharmaceutical compounding 8


Lab. No. 3 First Semester Simple Solutions/Ear Preparations

Ear preparations
Ear preparations are liquid, semi-solid or solid preparations intended for instillation, for
spraying, for insufflation, for application to the auditory meatus or as an ear wash.
Ear drops and ear sprays are solutions, emulsions or suspensions of one or more active
substances in liquids suitable for application to the auditory meatus without exerting
harmful pressure on the eardrum (for example, water, glycols or fatty oils). They may
also be placed in the auditory meatus by means of a tampon impregnated with the
liquid.
Ear drops are usually supplied in multidose containers of glass or suitable plastic
material that are fitted with an integral dropper or with a screw cap of suitable
materials incorporating a dropper and rubber or plastic teat. Alternatively, such a cap
assembly is supplied separately.

Rx Sodium Bicarbonate Ear Drop


Sod. Bicarb 5 g (was softener)
Glycerin 30 mL (viscosity builder, lubricant)
D.W. q.s. 100 mL

Practical pharmaceutical compounding 9


Lab. No. 4 First Semester Simple Solutions/Nasal Preparations

Nasal preparations
Nasal preparations are liquid, semi-solid or solid preparations intended for
administration to the nasal cavities to obtain a systemic or local effect. They contain one
or more active substances. Nasal preparations are as far as possible non-irritating and
do not adversely affect the functions of the nasal mucosa and its cilia. Aqueous nasal
preparations are usually isotonic and may contain excipients, for example, to adjust the
viscosity of the preparation, to adjust or stabilize the pH, to increase the solubility of the
active substance, or to stabilize the preparation.
Nasal preparations are supplied in multi-dose or single-dose containers, provided, if
necessary, with a suitable administration device which may be designed to avoid the
introduction of contaminants.
Unless otherwise justified and authorized, aqueous nasal preparations supplied in
multi-dose containers contain a suitable antimicrobial preservative in appropriate
concentration, except where the preparation itself has adequate antimicrobial
properties.
Over use of topical decongestant can lead to oedema of the nasal mucosa and they
should only be used for short periods of time about 5 days.

Rx Ephedrine Nasal Drop


Ephedrine HCl 500 mg (decongestant)
NaCl 500 mg (to makes the solution isotonic)
Chlorbutol 500 mg (preservative)
D.W. q.s. 100 mL
Procedure:
Prepare chlorbutol solution by using warm water.
Dissolve salt in the warm chlorbutol solution.
Cool and filter if necessary then complete the volume by adding vehicle.

Practical pharmaceutical compounding 10


Lab. No. 4 First Semester Simple Solutions/Nasal Preparations

Rx Nasal drop
Glycerin 20 mL (humectant, preservative)
Ethanol 70% 40 mL (preservative, antiseptic)
Normal saline solution qs 500 mL
Dispense 60mL

Practical pharmaceutical compounding 11


Lab. No. 5 First Semester Simple Solutions/Mouthwash

Mouthwash and Gargles


Mouthwashes and gargles: These are aqueous solutions for prevention and
treatment of mouth and throat infections. They usually contain antiseptics, analgesics,
and/or astringents. These solutions are used directly or diluted with warm water.
Gargles: A gargle is a liquid medicine intended to be retained in the mouth and placed
in contact with the back of the throat by throwing back the head and agitated by
air released from the larynx.; while Mouthwashes are aqueous solutions intended for
use in contact with the mucous membrane of the oral cavity.. They are not to be
swallowed. They are supplied as ready-to-use solutions or concentrated solutions to be
diluted. They may also be prepared from powders or tablets to be dissolved in water
before use.

Rx Compound Sodium Chloride Mouthwash


Sodium Bicarbonate 10 g
Sodium Chloride 15 g
Concentrated Peppermint Emulsion 25 mL
Double-strength Chloroform Water 500 mL
Water q.s 1000 mL
Concentrated Peppermint Emulsion
Peppermint Oil 20 mL
Polysorbate 20 1 mL
Double-strength Chloroform Water 500 mL
Purified Water freshly boiled and cooled q.s 1000 mL
Shake the Peppermint Oil with the Polysorbate 20 and add gradually, shaking well
after each addition, the Double-strength Chloroform Water and sufficient Purified
Water to produce 1000 mL.
Double-strength Chloroform Water
Chloroform 5 mL
Purified Water freshly boiled and cooled q.s. 1000 mL

Practical pharmaceutical compounding 12


Lab. No. 5 First Semester Simple Solutions/Mouthwash

Rx Mandle’s (throat) paint (used in case of laryngitis and tonsillitis)


KI 25 g
I2 12.5 g
Alcohol 96% 40 mL
Water 25 mL
Peppermint oil 4 mL
Glycerin q.s 1000 mL

Practical pharmaceutical compounding 13


Lab. No. 6 First Semester Simple Solutions/Ophthalmic

Ophthalmic solutions:
Ophthalmic solutions are sterile, free from foreign particles, and specially prepared for
instillation in the eye. Most ophthalmic solutions are dispensed in eye dropper bottles.
Patients should be shown how to properly instill the drops in their eyes, and every effort
should be made to emphasize the need for instilling only one drop per administration,
not two or three. When more than one drop is to be administered, wait at least five
minutes between administrations. Immediately after instilling a drop on the eye, place
pressure on the lacrimal sac for one or two minutes. This will reduce the rate of drug
loss through this pathway.
Formulations used include aqueous solutions, aqueous suspensions, ointments, and
inserts. Every ophthalmic product must be sterile in its final container to prevent
microbial contamination of the eye. Preservatives are added to the formulation to
maintain sterility once the container has been opened. Ophthalmic formulations also
require that the pH, buffer capacity, viscosity, and tonicity of the formulation is carefully
controlled.

Rx Atropine ophthalmic solution


Atropine Sulfate 2%
NaCl qs
Aqua. dist. q.s. ad. 30 mL
M.ft. isotonic solution
1. Determine the amount of NaCl to make 30 mL of an isotonic solution

X = 0.27 g
2. Calculate the contribution of atropine sulfate to the NaCl equivalent

Practical pharmaceutical compounding 14


Lab. No. 6 First Semester Simple Solutions/Ophthalmic

30 mL × 2 g/100 mL = 0.6 g atropine sulfate


E atropine sulfate = 0.13
0.6 g x 0.13 = 0.078 g
3. Determine the amount of NaCl to add to make the solution isotonic by subtracting (2)
from (1)
0.27 g - 0.078 g = 0.192 g or 192 mg
Other substances may be used, in addition to or in place of NaCl, to render solutions
isotonic. This is done by taking the process one step further and calculating the amount
of the substance that is equivalent to the amount of NaCl calculated in step 3.
For example, boric acid is often used to adjust isotonicity in ophthalmic solutions
because of its buffering and anti-infective properties. If E for boric acid is 0.50, then the
amount of boric acid needed to replace the NaCl in step 3 can be calculated:

or X = 0.38 g
or, more simply: 0.192 g ÷ 0.50 = 0.38 g
Thus, 0.38 g or 380 mg of boric acid would be required to render the previous
ophthalmic solution isotonic.

Practical pharmaceutical compounding 15


Lab. No. 6 First Semester Simple Solutions/Ophthalmic

General information:
Buffers: are compounds that resist changes in pH upon the addition of limited amounts
of acids or bases. Buffer systems are usually composed of a weak acid or base and its
conjugate salt.
The pH of a buffer system is given by the Henderson-Hasselbach equation:
(for a weak acid and its salt)

(for a weak base and its salt)

Buffer capacity is a measure of the efficiency of a buffer in resisting changes in pH.


Conventionally, the buffer capacity ( ) is expressed as the amount of strong acid or
base, in gram-equivalents, that must be added to 1 liter of the solution to change its pH
by one unit.
Calculate the buffer capacity as:

= gram equivalent of strong acid/base to change pH of 1 liter of buffer


solution

= the pH change caused by the addition of strong acid/base


The relationship between buffer capacity and buffer concentrations is given by the Van
Slyke equation:

Practical pharmaceutical compounding 16


Lab. No. 6 First Semester Simple Solutions/Ophthalmic

Sample calculation:
Using acetic acid and sodium acetate prepare 500 mL of a buffer solution at pH 4.5 with
a buffer capacity of 0.05.
Acetic Acid MW = 60; Ka = 1.75 x 10-5; pKa = 4.76; density (glacial acetic acid) = 1.05
g/mL; Na Acetate MW = 82
Salt to Acid Ratio:

[salt ]
4.5 = 4.76 + log
[acid ]
[salt ]
 antilog (4.5 - 4.76) = 0.55
[acid ]
[salt] = 0.55 [acid]
Total Buffer Concentration:

[H3O+] = antilog(- pH) = antilog(- 4.5)

0.05 = 0.53C
C = 0.095M
Final Calculations:
C = [salt] + [acid]
C = 0.55 [acid] + [acid] = 1.55 [acid] = 0.095 M
[acid] = 0.095 M ÷ 1.55 = 0.061 M or 0.061 moles/L × 0.5 L × 60 g/mole = 1.85 g acetic
acid
So glacial acetic acid = 1.85 g ÷ 1.05 g/mL = 1.76 mL
[Salt] = 0.55 [acid] = 0.55 × 0.061 M = 0.034 M or 0.034 moles/L × 0.5 L × 82 g/mole =
1.38 g sodium acetate

Practical pharmaceutical compounding 17


Lab. No. 7 First Semester Syrups

Syrups
Are sweet, liquid and viscous pharmaceutical preparations; Syrups do not contain active
ingredients. They are not intended to be administered as such but are used as vehicle
ingredients for their flavoring and sweetening properties.
Rx Simple syrup B.P
Sucrose 667 g
D.W. q.s. 1000 g
 Weigh an empty beaker then add sucrose and weigh it.
 Add small quantity of water.
 Heat it gently in water bath with continuous stirring.
 Weigh again and complete the volume by hot water!

Rx Simple syrup U.S.P


Sucrose 850 g
D.W. qs 1000 mL

Rx potassium citrate mixture BP


Potassium Citrate 300 g
Citric Acid Monohydrate 50 g
Lemon Spirit 5 mL
Quillaia Tincture 10 mL
Syrup 250 mL
Double-strength Chloroform Water 300 mL
Water Sufficient to produce 1000 mL

Use: alkalinization of urine to relieve discomfort in mild urinary tract infections or


cystitis.
Procedure: Weigh and dissolve solids in the double strength chloroform water and
syrup. The quillaia tincture should be added before the lemon spirit is added with

Practical pharmaceutical compounding 18


Lab. No. 7 First Semester Syrups

stirring, so that emulsification of the old will be achieved, make up the volume with
water.

Rx Ipecac syrup U.S.P


Powdered Ipecac 70 g
Glycerin 100 mL
Syrup q.s 1000 mL

Exhaust the powdered ipecac by percolation, using a mixture of 3 volumes of alcohol


and 1 volume of water as the menstruum, macerating for 72 hours, and percolating
slowly. Reduce the entire percolate to a volume of 70 mL by evaporation at a
temperature not exceeding 60o and preferably in vacuum, and add 140mL of water.
Allow the mixture to stand overnight, filter, and wash the residue on the filter with
water. Evaporate the filterate and washings to 40mL, and to this add 2.5 mL of
hydrochloric acid and 20 mL of alcohol, mix, and filter. Wash the filter with a mixture of
30 volumes of alcohol, 3.5 volumes of hydrochloric acid, and 66.5 volumes of water,
using a volume sufficient to produce 70 mL of the filtrate. Add 100 mL of glycerin and
enough syrup to make the product measure 1000mL and mix.
Ipecacuanha has been used as an expectorant in productive cough in doses of up to
about 1.4 mg of total alkaloids.
Ipecacuanha may also be used in larger doses as an emetic. Vomiting usually occurs
within 30 minutes of an emetic dose by mouth, due to an irritant effect on the
gastrointestinal tract and a central action on the chemoreceptor trigger zone. Doses are
usually followed by a copious drink of water or fruit juice. Adults have been given doses
of 21 to 42 mg of total alkaloids; children aged 6 months to 1 year have been given 7 to
14 mg of total alkaloids and older children 21 mg. Each 5 mL of Ipecac Syrup supplies
7 mg of total alkaloids. Doses may be repeated once only after 20 to 30 minutes if
emesis has not occurred.

Practical pharmaceutical compounding 19


Lab. No. 7 First Semester Syrups

Rx Ferrous Sulfate Syrup U.S.P


Ferrous Sulfate 40 g
Citric Acid, hydrous 2.1 g
Peppermint Spirit 2 mL
Sucrose 825 g
Purified water q.s 1000 mL

Dissolve the Ferrous sulfate, the citric acid, and peppermint spirit, and 200 g of sucrose
in 450 mL of purified water. And filter the solution until clear. Dissolve the remainder of
the sucrose in the clear filterate, and add purified water to make 1000 mL. mix, and
filter if necessary.

Rx Peppermint spirit B.P


Peppermint oil 100 mL
Ethanol 90% qs 1000 mL
Dissolve the Peppermint Oil in Ethanol (90%) and add sufficient Ethanol (90%) to
produce 1000 mL. If the solution is not clear, shake with previously sterilized Purified
Talc and filter. Peppermint oil is an aromatic carminative that relaxes gastrointestinal
smooth muscle and relieves flatulence and colic. Usual doses in adults and adolescents
from the age of 15 years are 0.2 mL three times daily by mouth, (increased to 0.4 mL
three times daily if necessary)

Rx Chloral-hydrate Syrup (non- official)


Chloral hydrate 0.5 g
Sorbitol 70 g
D.W. qs 100 mL

Practical pharmaceutical compounding 20


Lab. No. 7 First Semester Spirits

Spirits

Spirits are alcoholic solutions of volatile substances (usually volatile oils) with alcohol
contents ranging from 62-85%. They are most frequently used as flavoring agents, e.g.
Peppermint Spirit USP. Some spirits are used for their medicinal effect, but most spirits
are a convenient means of obtaining a proper amount of flavoring oil.

Rx Camphor spirit
Camphor 100 g
Alcohol qs 1000 mL

Rx Compound orange spirit


Terpeneless Orange Oil 2.5 mL
Terpeneless Lemon Oil 1.3 mL
Anise Oil 4.25 mL
Coriander Oil 6.25 mL
Ethanol q.s. 1000 mL

Practical pharmaceutical compounding 21


Lab. No. 8 First Semester Elixir

Aromatic Elixir, USP


Compound Orange Spirit 12 mL
Syrup 375 mL
Talc 30 g
Alcohol, Purified Water, each q.s. 1000 mL

Preparation:
Add to the Compound Orange Spirit sufficient quantity of alcohol to make 250 mL, add
to this the syrup in several portions, agitating vigorously after each addition and then
add in the same manner the required quantity of purified water. Mix the talc with the
liquid and filter through a filter wetted with diluted alcohol, returning the filtrate until a
clear liquid is obtained.

Uses: Pleasantly flavored vehicle used in the preparation of many elixirs.

Compound Benzaldehyde Elixir, NF


Benzaldehyde 0.5 mL
Vanillin 1g
Orange Flower Water 150 mL
Alcohol 50 mL
Syrup 400 mL
Purified Water, q.s 1000 mL

Preparation:
Dissolve the benzaldehyde and the vanillin in alcohol; add the syrup, orange flower
water and sufficient quantity of purified water in several portions, shaking the mixture
thoroughly after each addition, to make 1000ml. Filter, if necessary, until clear.
Uses: Vehicle for administering bromides and other salts, especially when a low
alcoholic content is desired.

Practical pharmaceutical compounding 22


Lab. No. 8 First Semester Elixir

Three Bromides Elixir, NF


Ammonium Bromide 80 g
Potassium Bromide 80 g
Sodium Bromide 80 g
Amaranth Solution 3 mL
Compound Benzaldehyde Elixir q.s. 1000 mL

Preparation:
Dissolve the bromides in 800 ml of Compound Benzaldehyde Elixir; add the amaranth
solution and sufficient compound benzaldehyde elixir to make the product
measure 1000 ml. Filter, if necessary, until clear.
Use: Sedative action from bromine ion.

Practical pharmaceutical compounding 23


Lab. No. 9 First Semester Gels

Gels
Cellulosic Solutions—Various cellulosics have been used as binders in solution form.
Hydroxypropyl methylcellulose (HPMC) has been used widely in this regard. Typical of a
number of cellulosics, HPMC is more soluble in cold water than hot.
It is also more dispersible in hot water than cold. Hence, to obtain a good, smooth gel
that is free from lumps or “fisheyes,” it is necessary to add the HPMC in hot, almost
boiling, water and, under agitation, cool the mixture down as quickly as possible, as low
as possible. Other water-soluble cellulosics, such as hydroxyethylcellulose (HEC) and
hydroxypropylcellulose (HPC), have been used successfully in solution as binders.

Carbomer 941 gel


Carbomer 941 0.5 (% w/w)
Glycerine 10.0 (% w/w)
Triethanolamine 0.5 (% w/w)
Water 89.0 (% w/w)
Preservative q.s.
Procedure: Water, glycerine, and preservative are mixed and the carbomer added by
sprinkling on the surface while constantly mixing at high speed. Triethanolamine is
added with slow agitation until a clear viscous gel forms.

Carbomer 934 alcoholic gel


Carbomer 934 resin 3.0 (% w/w)
Glycerine 10.0 (% w/w)
Ethanol 40.0 (% w/w)
2-Ethylhexylamine 2.5 (% w/w)
Water 44.5 (% w/w)
Procedure: The carbomer is dispersed in the glycerine and water, and a solution of the
2-ethylhexylamine in ethanol is added to the water solution with mixing until a clear
transparent gel is formed.

Practical pharmaceutical compounding 24


Lab. No. 9 First Semester Gels

Preparation of hydroxypropylmethylcellulose (HPMC) gel (2%)


HPMC (Methocel K100M) 2g
Distilled Water q.s. 100 ml
 Heat the distill water in a beaker to 80 – 90 ˚C
 Disperse the polymer with contentious stirring
 After complete dispersion of the polymer in the hot water, put the beaker in an ice bath
with continuous stirring.
the lab supervisor could divide the student into 3 group, each group prepare a different
concentration, 2%, 3% and 4%, than compare the results.

Practical pharmaceutical compounding 25


Lab. No. 1 Second Semester Suspensions

Suspensions
Oral suspensions are oral liquids containing one or more active ingredients suspended in
a suitable vehicle; suspended solids may slowly separate on standing but are easily re-
dispersed.
Common pharmaceutical products that are suspensions include: otic, ophthalmic, oral,
topical and inhalation suspensions.
Advantages and disadvantages of suspensions as dosage forms:
Advantages
 Insoluble drugs may be more palatable.
 Insoluble drugs may be more stable.
 Suspended insoluble powders are easy to swallow.
 Absorption will be quicker than solid dosage forms.
 It is theoretically possible to formulate sustained-release preparations.
Disadvantages
 Preparation requires shaking before use.
 Accuracy of dose is likely to be less than with equivalent solution.
 Storage conditions can affect disperse system.
 Suspensions are bulky, difficult to transport and prone to container breakages.

Classification of suspension:
1. Suspensions containing diffusible solid.
They are suspensions that can be prepared by using insoluble powder, that can be wet
by water readily and disperse easily throughout the vehicle (water) for long enough to
ensure even distribution for each dose.
General method for preparation:
 Grind and mix all insoluble powder by using mortar and pestle, starting from smallest
portion then to larger (ascending order- geometrical dilution).
 Add enough amount (¼ for preparing paste, ¼ for diluting of the paste and ¼ for
washing of the mortar) of vehicle gradually you get a smooth past.

Practical pharmaceutical compounding 26


Lab. No. 1 Second Semester Suspensions

 Dilute the paste and wash the mortar and pestle by using proper amount of the vehicle.
 Added enough amount of vehicle until you get desire volume.

Note:
 Add non-volatile soluble substance like sodium bicarbonate into the paste during
dilution.
 Syrup and glycerin should be added into dry powder before formation of the paste.
 Dye should be added into the paste before dilution.

Rx Magnesium Trisilicate Oral Suspension; Compound Magnesium Trisilicate Mixture


Magnesium trisilicate 50 g
Light magnesium carbonate 50 g (diffusible)
Sodium bicarbonate 50 g (soluble)
Concentrated peppermint emulsion 25 mL
Double strength Chloroform water 500 mL
Water q.s. 1000 mL
Use: Its use as antacid and cathartic
Dose: 10 mL three times daily

2. Suspension produced by dispersion of oil in inhalations


One class of inhalation consists of one or more volatile oil in water and to ensure
uniform dispersion of the oil on shaking light magnesium carbonate, a diffusible solid, is
added to adsorb some of the oil and finely subdivided the remainder. Unlike
emulsification which might seem a better method of dispersing the oil, the powder does
not interfere with free vaporization of the oil when the inhalation is added to water at
about 65o C for use. If the quantity is not included in the formula, 1g of light magnesium
carbonate for each 2 mL of volatile oil or 2g of solid should be used.

Practical pharmaceutical compounding 27


Lab. No. 1 Second Semester Suspensions

Rx Menthol and Eucalyptus inhalation


Menthol 20 g
Eucalyptus Oil 100 mL
Light Magnesium Carbonate 70 g
Purified water to 1000 mL
Use: Used to relieve symptoms of bronchitis and nasal obstruction in acute rhinitis or
sinusitis.
Direction: Add 1 teaspoonful to a pint of hot, not boiling, water and inhale the vapor
when required.

Practical pharmaceutical compounding 28


Lab. No. 2 Second Semester Suspensions

3. Suspension containing in-diffusible solid


Solid can be regarded as in-diffusible when it cannot be wet by liquid vehicle readily and
it cannot remain evenly distributed throughout the vehicle long enough to ensure the
uniformity of the measured dose; e.g. acetyl salicylic acid, salicylic acid, benzoic acid,
phenobarbition, and calcium carbonate.
This problem can be overcome by adding thickening agent; and amount of suspending
agent is depending on the volume of the mixture.
Suspending agent: acacia is a protective colloid and has a good value as suspending
agent. Its useful in mixture contain resinous tincture but less satisfactory for suspending
heavy powder unless be combined with other thickening as in compound powder of
tragacanth which contains acacia (20%), tragacanth (15%), starch (20%) and sucrose
(45%). It is useful when the vehicle is liquid other than water and chloroform-water and
in proportion of 2% w/v.
Compound powder of tragacanth is used for internal use and not external use, because
both acacia and tragacanth oxidize readily on exposure to atmosphere that produce bad
odor and cause skin shrinkage.
The second suspending agent is tragacanth mucilage (12.5g tragacanth, 25mL alcohol
and qs 1000mL chloroform-water) which can be use as 25% v/v. it can be used when we
have water or chloroform-water.
Method of preparation:
 Using compound powder tragacanth
1. Add in-diffusible solid in a mortar and start grinding, then add all other diffusible
solid by geometrical dilution, finally add compound powder tragacanth with continuous
trituration.
2. Add ¾ of the vehicle then start trituration, until you get smooth cream.
3. Then transfer it into a graduate cylinder then rinse the mortar and pestle and
complete the volume.

 Using tragacanth mucilage.

Practical pharmaceutical compounding 29


Lab. No. 2 Second Semester Suspensions

1. Add in-diffusible solid into a mortar and start grinding, then add diffusible
substance with continuous mixing.
2. Triturate the mixture with tragacanth mucilage.
3. Add half of the vehicle for dilution.
4. Complete the volume.

Rx Aspirin Suspension
Aspirin 500 mg
Orange syrup 1 mL
Conc. CHCl3 water 0.25 mL
Water q.s. 10 mL
Because the vehicle is water so tragacanth mucilage should be used.

Rx Calamine lotion
Calamine 150 g (astringent, antipruritic)
Zinc oxide 50 g (astringent, antipruritic)
Bentonite 30 g (suspending agent)
Sod. Citrate 5g
Liquefied phenol 50 mL (preservative, antipruritic)
Glycerol 50 mL
D.W qs 1000 mL
Procedure: Triturate the Calamine, the Zinc Oxide and the Bentonite with a solution of
the Sodium Citrate in about 700 mL of the Purified Water and add the Liquefied Phenol,
the Glycerol and sufficient Purified Water to produce 1000 mL.
Sodium citrate: caused partial deflocculation of the calamine and transfer the bentonite
from a gel into solution, in its absence the suspension is thicker and very difficult to pour
from the bottle.

Practical pharmaceutical compounding 30


Lab. No. 3 Second Semester Suspensions

3. Suspension containing poorly wettable solids


Some solids like sulphur insoluble in water and cannot wet by water readily, so adding
wetting agent is required for initial dispersion.

Rx Sulphur lotion
Precipitated Sulphur 4g
Quillaia tr. 5 mL
Glycerol 20 mL
Industrial methylated spirit 6 mL
Calcium hydroxide solution qs 100 mL

Rx Calcium hydroxide solution


Calcium hydroxide 10 g
Purified Water, freshly boiled and cooled qs. 1000 mL
Use: it’s used as a treatment for acne, scabies and as a mild antiseptic.
Procedure: Mix the quillaia tr. IMS and glycerol and triturate the mixture with the
Sulphur in a mortar.
Gradually dilute with lime water.
Note: if quillaia tr. is not available, try alcohol.

Practical pharmaceutical compounding 31


Lab. No. 4 Second Semester Emulsions

Emulsions
Rx Castor oil emulsion
Castor oil 8 mL
Water qs 30 mL
Castor oil is a fixed oil and is not miscible with water. To make it miscible gum acacia can
be used of ratio 4:2:1 so:
Oil: water: gum will be 8 mL : 4 mL : 2 g respectively.
Procedure: weight out 2g gum acacia and transfer it to the mortar. Measure 4mL water
and triturate it with gum so as to form mucilage. To this add 8mL castor oil in small
quantities at a time with thorough trituration after each addition. At this stage the
emulsion is known as primary emulsion. Add about 10mL more of vehicle in small
quantities at a time with constant trituration so as to get a homogeneous product. Then
complete the volume.
Use: castor oil is used as purgative.

Rx Olive oil emulsion


Olive oil 30 mL
Water qs 120 mL
Procedure like castor oil
Use: can be given as a nitrogen free diet during the treatment of renal failure, also acts
as mild laxative.

Rx Liquid paraffin emulsion


Liquid paraffin 30 mL
Water qs 100 mL
Procedure: like castor oil
Use: it’s used as a laxative in chronic constipation especially during pregnancy and old
age.

Practical pharmaceutical compounding 32


Lab. No. 4 Second Semester Emulsions

Rx Cod liver oil emulsion


Cod liver oil 08 30 mL
Syrup 12 mL
Ferric ammonium citrate 4 g
Chloroform 0.4 mL
Cinnamon qs 90 mL
Because cod liver oil is fixed oil so we should use this ratio 4:2:1 and follow dry gum
method for preparing primary emulsion.
Dilute the syrup with about 20mL of cinnamon water to this dissolve ferric ammonium
citrate. Add this solution to primary emulsion with continuous trituration then complete
the volume by adding cinnamon water.
Use:
1. Cod liver oil is source of vitamin A and D; it’s used as dietary supplement for
infants and children to prevent the occurrence of rickets and to improve calcification of
bones.
2. Ferric ammonium citrate is added as an antianaemic drug and help in patient
who are suffering from iron deficiency anaemia.

Rx
Liquid paraffin 50 mL
Vanillin 50 mg
Chloroform 0.25 mL
Benzoic acid solution 2 mL
MC 20 2g
Saccharin sodium 5 mg
Water to 100 mL
Methylcellulose 20 at a concentration of 2% acts as an emulsifying agent for the mineral
oil, liquid paraffin. Benzoic acid and chloroform act as preservative and vanillin and

Practical pharmaceutical compounding 33


Lab. No. 4 Second Semester Emulsions

saccharin sodium act as flavoring and sweetening agents. The amount of saccharin
sodium is not weighable and will be obtained by trituration using water as the diluent.

Procedure: Prepare mucilage by mixing the MC 20 with about six times its weight of
boiling water and allow standing for 30 minutes to hydrate. Add an equal weight of ice
and stir mechanically until the mucilage is homogenous. Dissolve the vanillin in the
benzoic acid solution and chloroform, as it is more soluble in organic solvents. Add this
solution to the mucilage and stir for 5 minutes. Make up the saccharin sodium
trituration and stir in the appropriate volume of solution to the mucilage. Make the
emulsion by adding together 50mL of liquid paraffin and 50mL of prepared mucilage
with constant stirring.
Use: as lubricant laxative for chronic constipation.

Rx
Mineral oil 50 mL
Span 60 qs
Tween 40 qs
Cherry syrup 40 mL
Distilled water qs 120 mL
Note: required HLB for mineral oil is 12, total amount of required emulsifying agent is
5% and (HLB of span 60 is 4.7 and HLB of tween 40 is 15.6).

Rx
Castor oil 45 mL
Tween 80 qs
Span 20 qs
Orange syrup qs 100 mL
Note: required HLB for castor oil o/w emulsion is 14, total emulsifier concentration is 5%
and (HLB for span 20 is 8.6 and for tween 80 is 15).

Practical pharmaceutical compounding 34


Lab. No. 4 Second Semester Emulsions

( )
( )
( )
( )

Weigh tween 80 and span 20, pour castor oil into the bottle upto 45mL, then transfer
the tween and span into the bottle and agitate well to mix. Add orang syrup to the 90
mL mark, and shake well to form the emulsion.

Peppermint Oil 20 mL
Polysorbate 20 1 mL
Double-strength Chloroform Water 500 mL
Purified Water, freshly boiled and cooled
Sufficient to produce 1000 mL

Shake the Peppermint Oil with the Polysorbate 20 and add gradually, shaking well after
each addition, the Double-strength chloroform water and sufficient purified water to
produce 1000 mL.

What is the HLB value of a surfactant system composed of 20 g Span 20 (HLB = 8.6) and
5 g Tween 20 (HLB = 13.3)?

Practical pharmaceutical compounding 35


Lab. No. 5 Second Semester Powdered Dosage Forms

Oral Powders

Oral powders may be formulated as divided powders, with each dose packaged
individually or undivided, as a bulk powder. Undivided oral powders are usually non-
potent medicaments, such as antacids, where the accuracy by which the patient
measures the dose is not critical.
Oral undivided powders are usually formulated by a simple mixture of the prescribed
medicaments without the addition of other ingredients.
Oral divided powders may contain one or more active ingredients together mixed with
inert diluents.
Class II dispensing balance or electronic equivalent usually is used at laboratory scale, it
would be better to weigh 200 mg as minimum amount.
As the amount of the active ingredient may be less than 200 mg, diluent could be added
to increase the bulk. The usual diluent used to provide ‘bulk’ is lactose monohydrate
because it is inert, water-soluble, colourless, odourless and generally harmless.

Mixing of solids
Since powders do not mix spontaneously, it may be very difficult to ensure a final
homogenous mixture of powders and energy must be introduced for the successful
mixing of powders. This problem is increased when the proportion of one ingredient is
very small.
At small scale a porcelain mortar is generally used and it should be sufficiently large to
ensure enough space for adequate mixing. It should be perfectly dry before mixing dry
powders.

Practical pharmaceutical compounding 36


Lab. No. 5 Second Semester Powdered Dosage Forms

Mixing process
1. Add the smallest (minimum amount) in to the mortar
2. Add the second ingredient in approximately the same amount that is present in the
mortar, therefore doubling-up the bulk already in the mortar.
3. Continue until you add of you ingredients (this process is known as geometrical
dilution).

Example
1. Prepare 4 sachets each containing 8 mg of propranolol
2. Prepare mix for 5 sachets to account for manipulative losses. Therefore 5 x 8 = 40 mg of
active ingredient are required
3. The minimum weighable amount of active ingredient on the balance is of 200 mg
(assuming a class B balance) therefore a minimum of 200 mg propranolol can be
Weighed
4. If each sachet of 8 mg active ingredient requires the addition of 192 mg lactose (200 mg
minus 8 mg), how much lactose must be added to 200 mg active ingredient?
5. 192 mg x 200 mg/8 mg = 4800 mg of lactose have to be added to 200 mg of the active
ingredient
6. Geometrical dilution
a. Add 200 mg propranolol in a mortar then add 200 mg lactose and start mixing
(total 400 mg)
b. For the mixed 400 mg, then added 400 mg lactose
c. For the 800 mg powder mixture, add another 800 mg lactose and continue

Practical pharmaceutical compounding 37


Lab. No. 5 Second Semester Powdered Dosage Forms

Method for wrapping the divided powder


Here the lab supervisor teaches you how to fold the paper!

1
2

Add the powder


here

Practical pharmaceutical compounding 38


Lab. No. 6 Second Semester Capsules Dosage Forms

Capsules
Many dosage forms including capsules and tablets are available in more than one
strength. If a capsule or a tablet of higher strength is prescribed but unavailable, two
capsules or tablets of one-half the strength may be dispensed. Thus, a pharmacist or a
health care professional may need to administer one-half or some other portion of the
tablet. A few helpful tips for such calculations are provided below:
(1) Do not break the tablets that are not scored.
(2) Enteric coated tablets are designed to resist the acidic environment in the stomach
and release the medication in the small intestine. If such tablets are broken, their
enteric properties may be lost. Therefore, do not break them.
(3) As a general rule, do not divide sustained/controlled release medications as they
may lose their controlled release properties.

Capsule Size Volume (ml) Mg of Lactose Mg of Aspirin


000 1.37 1340 1000
00 0.95 929 600
0 0.68 665 500
1 0.50 489 300
2 0.37 362 250
3 0.30 293 200
4 0.20 195 125
5 0.13 127 60

"Punch" Method of Compounding Capsules


To hand fill capsules at the prescription counter, the pharmacist generally uses the
"punch" method. The ingredients are triturated to the same particle size and then mixed
by geometric dilution.
The powder is placed on a powder paper or ointment slab and smoothed with a spatula
to a height approximately half the length of the capsule body. The base of the capsule is
held vertically and the open end is repeatedly pushed or "punched" into the powder
until the capsule is filled; the cap is then replaced to close the capsule. Each filled
capsule is weighed using an empty capsule as a counterweight. Powder is added or

Practical pharmaceutical compounding 39


Lab. No. 6 Second Semester Capsules Dosage Forms

removed until the correct weight has been placed in the capsule. The filled capsule is
tapped so that no air spaces are visible within the contents.
The simplest method by which a capsule may be kept free of moisture during
compounding is to wash the hands well, dry them, and keep the fingers dry by stripping
a towel through the cleansed fingers until warmth is felt.
An alternative method is to use the base of one capsule as a holder for other bases
during the filling operation. The capsules do not come in contact with the fingers.
The surest method of protecting the capsule is to wear finger cots or rubber gloves.

Practical pharmaceutical compounding 40


Lab. No. 7 Second Semester Semisolid Dosage Forms

Semisolid dosage forms


Ointments are the soft semisolid preparations meant for external application to the skin
or mucous membrane, they usually contain a medicament or medicament dissolved,
suspended or emulsified in the base. Ointments are used for their emollient and
protective action to the skin. They may also be used as vehicle or bases for the topical
application of medicinal substances.
Ointments bases are oleaginous bases, absorption bases emulsion bases and water
soluble basis.
And it can be prepared by:
1. Trituration method. Powder the medicament if already not in fine powder.
Triturate it with a small amount of base on an ointment slab with a stainless steel
spatula with long blade. Incorporate this to the rest of the base thorough trituration
until uniform. If liquids are also to be incorporated, pestle and mortar should be used
for the purpose.
2. Fusion method: when an ointment bas contains a number of solid substances.
Melt them in decreasing order of their melting points to avoid over-heating of low
melting point substance. Add the medicament to the melted bases and stir thoroughly
until the mass cools down and a homogenous product is formed. If any liquid or
aqueous substance is also to be incorporated, that must be heated to about the same
temperature as the melted bases. After mixing the tow portions they should be stirred
uniformly and thoroughly until a homogenous mass is obtained. Rapid cooling should be
avoided.
If dilution or mixing of different concentration of ointment is required we should follow
allegation method that has been clarified in the following example.

Practical pharmaceutical compounding 41


Lab. No. 7 Second Semester Semisolid Dosage Forms

Ointment Bases
There are five (5) classes or types of ointment bases which are differentiated on the
basis of their physical composition. These are:
 oleaginous bases
 absorption bases
 water in oil emulsion bases
 oil in water emulsion bases
 water soluble or water miscible bases

Oleaginous Base (White Ointment)


White Wax 5%
White Petrolatum 95%

Procedure for Preparation:


a) Melt the white wax on a hot plate. No need to heat beyond 70 - 75°C
b) When the wax has completely melted, add the petrolatum and allow the entire
mixture to remain on the hot plate until liquefied.
c) Following liquefication, remove from heat and allow the mixture to congeal. Stir
the mixture until it begins to congeal.

Absorption Base
Cholesterol 3%
Stearyl Alcohol 3%
White Wax 8%
White Petrolatum 86%
Procedure for Preparation:
a) Melt the stearyl alcohol, white wax, and petrolatum together on a hot plate.
b) Add the cholesterol to the mixture; stir until completely dissolved.
c) Remove the mixture from the hot plate and stir until congealed.

Practical pharmaceutical compounding 42


Lab. No. 7 Second Semester Semisolid Dosage Forms

W/O Emulsion Base (Cold Cream type base)


White wax 12%
Cetyl Esters Wax (or Spermaceti) 12.5%
Mineral Oil (Sp Gr = 0.9) 56%
Sodium Borate 0.5%
Water 19%

Procedure for Preparation:


a) Melt the white wax and spermaceti on a hot plate.
b) Add the mineral oil to this mixture and bring the temperature to 70°C.
c) Dissolve the sodium borate in water.
d) Heat the sodium borate solution to 70°C.
e) When both phases have reached the desired temperature, remove both phases
from the hot plate and add the aqueous phase slowly and with constant stirring
to the oil phase
f) Stir briskly and continuously until congealed.

O/W Emulsion Base (Hydrophilic Ointment)


Sodium Lauryl Sulfate 1%
Propylene Glycol (SP Gr = 1.035) 12%
Stearyl Alcohol 25%
White Petrolatum 25%
Purified Water 37%

Procedure for Preparation:


a) Melt the stearyl alcohol and white petrolatum on a hot plate.
b) Heat this mixture to 70°C.
c) Dissolve remaining ingredients in water and heat the solution to 70° C.
d) Add the oleaginous phase slowly to the aqueous phase, stirring constantly.
e) Remove from heat and stir the mixture until it congeals.

Practical pharmaceutical compounding 43


Lab. No. 7 Second Semester Semisolid Dosage Forms

Water Soluble Base


Polyethylene Glycol 400 (SP Gr = 1.12) 60%
Polyethylene Glycol 3350 40%

Procedure for Preparation:


a) Melt the PEG 400 and Carbowax 3350 on a hot plate.
b) Warm the mixture to about 65°C.
c) Remove from the hot plate and stir until congealed.

Example 1: In what proportion should a 20% coal tar ointment be mixed with white
petrolatum (diluent) to produce a 2% coal tar ointment?

Example 2: In what proportion should a 10% and 4% zinc oxide ointments be mixed to
prepare a 6% ointment?

Example 3: A physician ordered 20% monobenzone (Benoquin®) ointment to be used for


the temporary bleaching of hyperpigmented skin. In what proportion may 25%, 10%,

Practical pharmaceutical compounding 44


Lab. No. 7 Second Semester Semisolid Dosage Forms

and 5% monobenzone ointments be mixed in order to prepare an ointment of the


desired concentration?

Rx Calamine ointment
Calamine powder 15 g
White soft paraffin 85 g
Procedure: trituration method
Use: calamine has a mild astringent action of the skin and is used in ointments to relieve
discomfort of dermatitis.

Rx Sulphur ointment
Sulphur 10 g
Simple ointment prepared with white soft paraffin 90 g
Procedure: trituration method
Use: sulphur ointment is used as fungicidal ointment and is also used in scabies and
right worm infestation.
Rx Zinc oxide ointment
Zinc oxide 15 g
Simple oint. 85 g
Procedure: trituration method
Use: zinc oxide is used in ointments as a mild astringent for the skin, as a soothing and
protective application in eczema.

Practical pharmaceutical compounding 45


Lab. No. 7 Second Semester Semisolid Dosage Forms

Rx whitfield’s ointment
Salicylic acid 3g
Benzoic acid 6g
Emulsifying oint. 91 g
Procedure: trituration method
Use: as a fungicidal.

Rx Emulsifying ointment
Emulsifying Wax 300 g
White Soft Paraffin 500 g
Liquid Paraffin 200 g
Procedure: melt together and stir until cool

Rx Emulsifying wax
Cetostearyl Alcohol 800 g
Macrogol Cetostearyl Ether (22) 200 g
Procedure: melt together and stir until cool

Rx Cold Cream
White Beeswax 10 g
Liquid paraffin 30 g
Borax 0.5 g
Water 9.5mL
Grate the beeswax, melt it with liquid paraffin and raise the temperature to 70oC.
dissolve the borax in the water and heat the solution to 70 oC then gradually add the
solution to the melted mixture and stir.
Borax soaps are generally made by the interaction of borax and free acid in beeswax.

Practical pharmaceutical compounding 46


Lab. No. 7 Second Semester Semisolid Dosage Forms

Cream prepared with Sorbian ester.


Sorbitan mono-oleart 6g
White beeswax 3g
White soft paraffin 36 g
Liquid paraffin 15 g
Purified water freshly
Boiled and cooled 40 g

Rx Compound Zinc paste


Zinc oxide 250 g
Starch 250 g
White soft paraffin 500 g

Practical pharmaceutical compounding 47


Lab. No. 8 Second Semester Suppositories

Suppositories
Suppositories are special shaped solid dosage form of medicament for insertion into
body cavities other than mouth. They may be inserted into rectum, vagina or urethra.
These products are so formulated that after insertion, they will either melt or dissolve in
the cavity fluids to release the medicament. Suppositories vary in shapes, size and
weight. Generally suppositories weighing 1-2 g are prepared. The bases used for the
preparation of suppositories include cocoa butter, glycerol gelatin and soap glycerin.
Displacement value: since the volume of suppositories from a particular mould remains
same but its weigh varies due to the variation in densities of medicaments and the base
with which the mould was calibrated. To get a product of uniform and accurate weight,
allowance must be made for the change in densities of the mass due to added drugs. For
this purpose the displacement value of the medicament is taken into consideration.
Displacement value may be defined as the quantity of the drug which displaces one part
of medicament.

Rx
Boric acid 200 mg
Theobroma oil q.s.
Prepare 8 suppositories.
DV of boric acid = 1.5
Use 1 g mould

Instead of 8 we make calculation for preparing 10 suppositories.


 Each mould will occupy by 1 g of theobroma oil, so we need 10 g of TO for preparing
10 suppositories.
 Total amount of BA require: if 200 mg for each supp. So we need (200 x 10) 2000 mg
 DV of boric acid is 1.5 which occupy just 1 part of TO; so:2g x 1/1.5= 1.3 g
 10 g of TO – 1.3 g = 8.7 g total amount of TO.
Use: it used as antibacterial and antifungal

Practical pharmaceutical compounding 48


Lab. No. 8 Second Semester Suppositories

Rx
Prepare 4 suppositories; each contains 300mg bismuth subgallate and glycerol as a base.
DV of bismuth subgallate = 3 and use 1 g mould

 Total amount of bismuth subgallate = 300 x 5 = 1500 mg


 Total amount of glycerol = 5 x 1 = 5 g, but glycerol is 1.2 times denser than
theobroma oil; so: 1.2 x 5 = 6 g of base.
 DV = 1.5 x 1 / 3 = 0.5 g
 6 g – 0.5 g = 5.5 g of base

If 12 cocoa butter suppositories containing 40% zinc oxide weigh 17.6 grams, what is the
displacement value of zinc oxide? Assume that the suppositories are made in a 1 g mold.
Given weight of 12 suppositories with zinc oxide = 17.6 g
Weight of zinc oxide in the suppositories = (40/100) × 17.6 = 7.04 g
Weight of cocoa butter in the suppositories = (60/100) × 17.6 = 10.56g
Theoretical weight of 12 suppositories without zinc oxide = 12 g
Cocoa butter displaced by 7.04 g of zinc oxide = 12 − 10.56 = 1.44
Displacement value of zinc oxide = (7.04/1.44) = (X/1); X = 4.89

General method for preparing suppository: Using 12 cavity molds, a quantity of vehicle
known to be insufficient is added to the correct amount of drug for 12 suppositories.
The mixture is poured into the mold, leaving one or two cavities unfilled; the excess is
scraped off after congealing and returned to the pouring dish; a little more pure vehicle
is added, melted together with the excess of drug-vehicle mixture, and poured into the
unfilled cavities. More pure vehicle is added in the same way until all 12 holes are
correctly filled. After removing the hardened suppositories from the molds, they are
again melted, mixed and poured. Since actually a slight excess is poured into each cavity
and some mass adheres to the pouring vessel, less than 12 suppositories are obtained
on the final pouring.

Practical pharmaceutical compounding 49


Lab. No. 8 Second Semester Suppositories

The second method is called double casting

Practical pharmaceutical compounding 50

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