Pharmaceutical Solutions

By
Getahun Paulos (PhD)
Assistant Professor of Pharmaceutics

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 Outline
Introduction
Methods of preparation
Solutions taken orally
Solutions used in the mouth and throat
Solutions instilled into body cavities
 Topical solutions
Injectables (sterile products)

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 1. Introduction

 Solutions are homogenous mixtures of two or more

components.
 Contain one or more solutes dissolved/dispersed in

one or more solvent

 Most pharmaceutical solutions are solid-liquid

systems.
 liquid-liquid, gas –liquid and solid-solid solutions

are also available

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 Introduction…..
Classification
 Depending on the route of administration/site
of application
1. Solutions taken orally
elixirs, linctuses, syrups, pediatric drops,
draughts, mixtures.
2. Solutions used in the mouth and throat
 mouthwashes, gargles, throat paints, throat
sprays.
3. Solutions instilled into body cavities
douches, enemas, ear drops, nasal drops, nasal
spays.
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 Introduction…..

4. Solutions applied to body surfaces (topical

solutions)
 collodions, liniments, lotions, paints.

5. Parenteral solutions
 infusions, irrigations, dialysis solutions, total
parenteral nutrition (TPN), other injectables.

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 2. Preparation/compounding of solutions
 Weigh/measure the ingredients
 Dissolve the ingredients in the vehicle
 Dissolution can be facilitated by:
Agitation/stirring/shaking
Size reduction (poorly soluble solutes)
Heating (if the solution process is endothermic)
 Direct heat is not advisable ( Water bath, Steam
jacketed vessels)
 Not suitable for heat sensitive and volatile components

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 Preparation/compounding of solutions…..
 Clarification (filtration)
 Removal of insoluble impurities or excess solute
 Filter paper, sintered glass filters, membrane filters

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 Preparation/compounding of solutions…..
Solubility enhancement
 Water is always solvent of choice for solutions
 Bioavailability of poorly water soluble directly
proportional to their solubility
 Thus a need for techniques to increase the solubility
of such drugs: The common methods are:
Cosolvency
solubilization
pH control
Complexation
particle size control (micronizaiton)

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 Solutions taken orally
elixirs
linctuses
syrups
pediatric drops
draughts

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 Solutions taken orally
Advantages of solutions as dosage forms
Absorption of drug form the GIT is rapid
fastest onset of action
Uniform distribution of the drug
no need to shake before dose measurement
Easy to swallow
Safe means of administering some GI irritant drugs (eg.
KCL), than solid dosage forms.
Attractive appearance has beneficial psychological effect.
Can be given by other routes of administration

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 Solutions taken orally…..

Disadvantages of solutions as dosage forms

 The drugs are less stable in solution than in solid dosage forms
 Unpleasant taste and smell is more pronounced
 Bulky for transportation and storage
 Vulnerable to loss upon breakage of the container
 A means of measuring the dose is required
 Dose usually measured by the patient (accuracy and
reliability problem)

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 A. syrups

 Concentrated aqueous preparations of sugar (sucrose,

dextrose) or sugar substitutes with or without flavouring
agents and medicinal substances
Types
 Medicated syrup: If medicinal substance is added the syrup
 non-medicated syrup: If it contains the sugar only (± flavour)
- Non medicated syrups are used as a vehicle (sweetened &
flavorured) for elixirs & linctuses, or as diluents.

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 Solutions taken orally…..

Syrups…

Uses
Mask bitter, saline or any objectionable taste.
Physical concealment of the substance
Sweetening effect of the sugar
Prolong contact time of drug at site of application
vehicle for elixirs and linctuses

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 Syrup…..
 Most syrups contain sucrose (60-80 %) (simple syrup
85g/100ml)
attain the desired viscosity, sweetness and stability
 Sugar substitutes (for diabetic patients)
Polyols →→ sorbitol, glycerol, propylene glycol
Cellulose derivatives →→ MC, HEC (nonglycogenetic)
Artificial sweeteners (typically saccharin sodium,
aspartame)

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 Solutions taken orally…..
Preparation of syrup
1. solution by agitation, with out the aid of heat
Adding the sugar to purified water and agitating
known as simple syrup
simple syrup USP (64.74%w/w or 85%w/v)
Sucrose…..667g sucrose…….850g
Purified water…to 1000g or purified water…..to
1000ml
simple procedure
stable, no inversion
less sweet

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 Solutions taken orally…..
2. solution with the aid of heat
 the sugar is added to purified water and heated with water
bath
 Quick/fast method of preparation
 Sucrose will be hydrolyzed to (glucose and fructose) hence
known as inverted syrup
 Volatile and heat-sensitive components should be added after
cooling

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 Solutions taken orally…..
Inverted syrup
 Sweeter than simple syrup (1.23 times)
 More susceptible to microbial growth and fermentation
 Overheating causes caramelization
 brown/dark color due to decomposition of fructose
Tips
 Cold storage leads to crystallization of the syrup
 Syrups cannot be sterilized by heat
 Preservation might not be needed or depends on the amount of
free water present
 Store in cool place in air-tight containers

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 Ferrous Sulfate Syrup
Formula: Ferrous sulfate……………..40g
Citric acid, hydrous……….2.1g
Peppermint spirit…………2ml
Sucrose……………………825g
Purified water to…………. 1000ml
send 50ml
Sig. Two tsf tid

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 B. Elixirs
Clear, sweetened and pleasantly flavored hydroalcholic
solutions
More than one solvent is used (cosolvency)
Elixirs containing 10-12% alcohol are usually self preservative

Less viscous, less sweet than syrup

Relatively stable (up to 2 years of shelf life)
Medicated or non-medicated
The diluent is syrup or non-medicated elixir
Diluted elixirs should be used within a week.

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 Elixirs….

Preparation of elixirs
Simple solution with agitation is used
Dissolve water soluble ingredients separately in purified
water
 Dissolve alcohol soluble ingredients in alcohol
Add the aqueous solution to the alcoholic solution
minimal separation of alcohol soluble components

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 Elixirs….
Phenobarbitone Elixir
 Formula: Phenobarbitone……………………………………. 0.4 g
Ethanol (90%) ………………………………..……. 40 ml
Compound orange spirit ……………………….…… 2.5 ml
Glycerol …………………………………………… 40 ml
Amaranth solution …………………………………… 1 ml
Purified water to ………………………………….. 100 ml
send 25 ml
Sig. 2 tsp. his, store in dark place

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 C. linctuses
Viscous preparations used for the treatment of cough
Contain demulcents (for mucus membrane),
expectorants or sedatives as active ingredients
The vehicle is syrup
• sooths the sore mucus membrane of the throat
The diluent is usually syrup
• diluted linctuses should be used within 2 weeks

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 Linctuses…..
Stored in air-tight containers
• entrance of moisture causes surface dilution
• causes microbial growth & fermentation of the
sugar
Stored at constant temperature
• temperature fluctuation leads to crystallization

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 D. Pediatric drops

Administered in small volumes using a suitable

measuring device
Contain potent medicaments

Hence the dose must be measured precisely using

graduated or pre-calibrated dropper

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 E. Spirits
 Spirits are the alcoholic or hydro alcoholic solutions of
volatile substances.
 They may be used internally or externally. They are mainly
used as flavoring agents, sweetening agents.
 In all cases the volatile oil content of the official spirit is
much greater than that of the corresponding aromatic water.
chloroform spirit
 Formula: Chloroform………………………….50ml
Alcohol (90%) q.s…………………...1000ml
peppermint spirit B.P.
 Formula: Peppermint oil ……………….100ml
Ethanol (90%) to……………..1000ml
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 Solutions used in the mouth and
throat
Gargles
Mouthwashes
Throat paints
Throat sprays

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 A. Gargles
 Aqueous solutions used to relive mild throat infections
 Contain antiseptics, astringents or anesthetics
 Usually prepared in concentrated form and diluted by warm
water before use
 suspended in the throat by forcing air from the lungs through it
 Expectorated, unless directed to swallow it
 toxic substances shouldn’t be used in the formulaiton
 Due to high absorption from the buccal cavity
Examples:
 Potassium chlorate and phenol gargle
 Phenol gargle

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 Potassium chlorate gargle
KC1O3 ----------------------------30gm
Liquefied blue v (colorant ) ---15ml
Purified water qs ----------------1000ml

Phenol gargle
Phenol glycerin ----------------------5ml
Amaranth solution ------------------1ml
Water qs ----------------------------- 100ml

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 B. Mouthwashes

 are aqueous solutions, often in form containing

one or more active ingredients and excipients
 Used for cleansing/treatment of oral cavity
 therapeutic or cosmetic purpose
 used by swishing the liquid in the oral cavity
 Usually prepared in concentrated form
• diluted by warm water before use by the patient
 can be used as gargles, either as it is or diluted with water

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 Mouthwashes…..
They can be used for two purpose: therapeutic and
cosmetic.
The therapeutic washes or rinses are used to
reduced plaque, dental caries, gingivitis and
stomata’s oral candidiasis, prevention of
bleeding after oral surgery, dry mouth
(xerostomia),
Cosmetic mouthwashes are often formulated to
reduce bad breath (odour) through the use of
antimicrobial/ or flavouring agents.

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 Mouthwashes…..
Shouldn’t be swallowed unless directed
swished or gargled for about half a minute and
then spit out
Buccal absorption is high (avoid toxic substances)
Examples:
Hydrogen Peroxide Mouthwash
Povidone- Iodine Mouthwash
Compound Sodium Chloride Mouthwash

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 Compound Sodium Chloride Mouthwash BP
Sodium Bicarbonate 10g
Sodium Chloride 15g
Concentrated Prepermint Emulsion 25ml
Double-strength Chloroform Water 500ml
Water sufficient to produce 1000 ml

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 C. Throat paints
 Applied to the mucus surface for treatment of mouth/ throat
infections
 Medicated with antiseptics, astringent or analgesic substances
 Prepared in small volumes, as they are directly applied to the
place by brush
 Contain the highest amount of viscous materials
 The container must be wide-mouthed
 Dispensed with a throat brush.
 Examples
 Compound Iodine Paint (Mandl`s paint)
 Crystal violent paint

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 Examples; compound Iodine Paint (Mandl`s paint)
KI………………………25gm
I2……………………….12.5gm
Alcohol (90%) ………. 40ml
Water…………………..23ml
Papperment oil …………4ml
Glycerol ..qs ………….ad..1000ml

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 Throat spray
They are solutions sprayed in to the throat to medicate the
larynx, pharynx and lung using a nebulizer.
Throat sprays are categorized under aerosols.
Contain antibiotics and used for conditions such as laryngitis,
Pharyngitis, and tonsillitis,
But most solutions sprayed in to the throat are intended to
medicate the lungs.
Example: adrenaline and atropine throat spray

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 Solution instilled into body cavities

 A. Nasal solutions
 B. Ear/ aural/autic solution
 C. Enemas
 D. Douches

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 A. Nasal solutions
 Administered to the nasal passages in drops or sprays
Also emulsions or suspensions

 To reduce nasal congestion and irritation

 Local sympathetic effect
 Potential for systematic effect (intensive research)
 Similar to nasal secretions in regard to, pH, tonicity and viscosity
 so that normal ciliary action is maintained
 isotonic and buffered to maintain a pH of 5.5 to 6.5
 Drops spread more extensively than the spray
 Patient in supine position, head tilted back and turned left and right

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 B. Ear/ aural/autic solution
 Solutions of drugs in water, glycerol, propylene glycol or
water/alcohol mixtures
 Administrated into auditory canal as sprays, drops or washes for
local effect

Generally used for the following purposes:

1. Treating mild infections
 Antimicrobials (CAF, gentamycin, neomycin, nystain,
polymixin B) and anti-inflammatory agents
2. Removal of excess earwax (cerumen)
 H2O2, NaHCO3 solutions ( may contain glycerin or
solubilizing agents to solublize the earwax and facilitate
removal).

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 Ear/ aural/autic solution….
3. Astringents to dry weeping surfaces
aluminum acetate
4. Antiseptics and anesthetics
Phenol
 patients should remain on their side for a few minutes
 so that the solution doesn’t run out of the ear

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 Ear drops (to relief itching)
Formula: - Sodium Bicarbonate………. 5 gm
Glycerine……………………30 ml
Purified water ………..q.s. 100 ml

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 C. Enemas
aqueous or oily solutions or suspensions introduced into
rectum
Uses:
1. cleansing : evacuation enemas
Constipation, before surgery, childbirth
Contain laxatives
Large volume (macroenemas)
warmed to body temperature before use
They include osmotic agents, such as sodium chloride, sodium
mono/dihydrogen phosphate, sodium bicarbonate; irritants or
simulating laxatives, such as soft soaps or lubricating oils, such
as fixed oils (casteroil, oil olive oil, arachis oil, etc.)

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 Enemas….

2. Therapeutic : retention enemas or microenemas

Retained in the large intestine
local effect in the large bowel or for systemic effects
Small volume (not more than 150ml in adults)
usually administered by rectal applicators

3. diagnostic
 X-ray contrast media (eg Barium sulphate)
 aid diagnostic investigation of the large bowel

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 D. Douches
 medicated solutions for rinsing a body cavity
 The word ‘douche’ is often used for a vaginal solutions
 for rinsing the vaginal cavity (antiseptic)
 must be sterile is used after childbirth or surgery
 solutions for the bladder (irrigations)
 Irrigating the bladder
 Bladder irrigations must be isotonic and sterile
 NS could be used
 Solutions for the rectum (enemas)

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 They are prescribed as:
Cleansing agents, e.g isotonic sodium chloride solution
Astringents, e.g., ZnSO4, potassium alum (AlK(SO 4)2.
12H2O(1%)
Antipruritis, e.g., phenol, menthol.
Douches are often supplied as liquid concentrates or as
solids (powders, tablets) which may be prepared in
bulk or as single- use packages, and
should be diluted or prepared in the appropriate amount
of warm water (usually 1 to 2 liters) before use

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 Solution used externally
Collodions
Liniments
Lotions
paints

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 A. collodions
Solution of pyroxylin ( a nitrocellulose) in a mixture of
organic solvents, usually ethyl ether and ethanol
Intended for local effect
Applied by soft brush or other suitable applicator
 the ether and alcohol evaporates, a film of pyroxylin is left on the
surface
 used to seal minor cuts and wounds or

hold the drug (salicylic acid) in contract with the skin for
longer period

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 Collodions…..
Flexibility is conferred by inclusion of caster oil
Colophony (an adherent) and camphor (water repellent)
could also be incorporated
Collodion BP
Pyroxylin……………4% w/w
Ether/alcohol (90%)….in 3:1 ratio
Flexible collodion BP
Colophony …………………….25g
Castor Oil ……………………..25g
Collodion, qs ………………… 1000ml
Store in air-tight container, in cool place remote from fire

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 B. liniments
Liniments are Alcoholic solutions or oleaginous
emulsions (usually semisolid)
The vehicle may be alcohol, oil or soap
applied to unbroken skin
Applied with friction or rubbing to the skin

Oily liniments are less irritant, easily spreadable

and preferred when massage is necessary

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 C. lotions

 Solutions, suspensions or emulsions

 liquids or semi- solids

 applied to unbroken skin without friction

 used as protective or for therapeutic purpose

(astringents, antiseptics, antipruritis)

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 D. Paints
 Solutions, suspensions or emulsions
 applied to skin or mucus membrane with brush
 contain antiseptics, astringents, analgesics, etc
 The solvent for skin paints is alcohol, acetone or
ether
 evaporate quickly leaving a film on the skin
 If rapid evaporation is not required water could be
used as a vehicle
 A viscosity modifier, eg. glycerol, is often added
 to ensure prolonged contact with the skin

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 Parentral solutions
Infusions,
Irrigations,
Dialysis solutions,
Total parenteral nutrition (TPN),
Other injectables

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