Pharmaceutical Solution intended for Oral administration. Types, Preparation and Applications of Oral solutions, Syrups, Elixirs and Spirits.

2. ORAL SOLUTIONS,
SYRUPS, ELIXIRS &
SPIRITS

3. ORAL SOLUTIONS
Preparation of Solutions, Dry mixtures for solution, Oral
rehydrate solutions, Oral colonic lavage solution

4. INTRODUCTION
Solutions are liquid preparations that contain one or more chemical
substances dissolved in a suitable solvent or a mixture of solvents.
• Examples are syrups, spirits, elixirs, etc.

5. SOLUBILITY
Solubility is the relative ability of a solute to dissolve into a solvent.
• “Like dissolves like” principle governs the solubility.
• Temperature is an important factor in determining the solubility of a drug
and in preparing its solution. Other factors include the properties of the
components, pressure, pH of the solution, etc.
• Many drugs are either weak acids or weak bases, and their solubility
depends on the pH of the solvent. These drugs react either with strong
acids or strong bases to form water-soluble salts.
Drug Water (ml) to dissolve 1g drug
Atropine 455
Atropine Sulphate 0.5
Sulfadiazine 13000
Sodium Sulfadiazine 2

6. ADVANTAGES
• Easier to swallow
• Drug is rapidly absorbed
• A solution has uniform distribution of the drug. In suspension or emulsion
formulations, uneven dosage can occur.
• Immediately diluted by the gastric contents which reduce irritation to the
gastric mucosa.

7. DISADVANTAGES
• Liquids are bulky and are inconvenient to transport and store. Moreover,
immediate loss of the whole product occurs in case of breakage of the
container.
• Poor stability of drug
• Microbial growth
• Inaccurate dosing
• The unpleasant taste of drugs is more pronounced in solutions

8. PREPARATION
Simple solutions
• Solutions are prepared by dissolving the solute in the solvent by agitation
and then filtering the solution if necessary.
• Gentian violet solution is prepared by dissolving gentian violet in water
and alcohol.

9. PREPARATION
By Chemical Reaction
• Solution is prepared by reacting two or more solutes with each other in a
suitable solvent.
• Examples: Magnesium Citrate oral solution is prepared by reacting
magnesium carbonate with citric acid.

10. PREPARATION
By Extraction
• Drugs of vegetable or animal origin often are extracted with water. So,
they are also called extracts.
• Ipecac solution is obtained from powdered ipecac.

11. DRY MIXTURES FOR SOLUTION
• Many drugs are unstable in aqueous solution. They are provided in dry
powder or granule form for reconstitution with a prescribed amount of
purified water immediately before dispensing to the patient.
• The dry powder mixture contains all of the components, including drug,
flavoring agents, colorant, buffers.
• Once reconstituted, the solution remains stable for the labeled period,
usually 7 to 14 days. This is a sufficient period for the patient to complete
the regimen usually prescribed.

12. DRY MIXTURES FOR SOLUTION
• After the patient completes the course of therapy, the patient should be
instructed to discard the remaining portion.
• Examples are Augmentin, Velosef, etc.

13. ORAL REHYDRATION SOLUTION
• Rapid fluid loss associated with diarrhea can lead to dehydration,
electrolyte imbalance and ultimately death.
• Thus, the treatment approach is promptly replace the lost fluid and
electrolytes to prevent dehydration. ORSs are usually effective in this
case.
• A liter of typical ORS contains
45 mEq Na+
20 mEq K +
35 mEq Cl−
30 mEq citrate
25 g dextrose.

14. ORAL REHYDRATION SOLUTION
• These formulations are available in liquid or powder packet form for
reconstitution.
• It is important that the user add the specific amount of water needed to
prepare the powder forms.

15. ORAL COLONIC LAVAGE SOLUTION
This method entails oral administration of a balanced solution of
electrolytes with polyethylene glycol.
• It is a method to prepare the GIT for procedures e.g. colonoscopy.
• The formulation of oral colonic lavage solution is:
PEG-3350 ------ 236.00g
Sodium sulfate ------ 22.74g
Sodium bicarbonate ------ 6.74g
Sodium chloride ------ 5.86g
Potassium chloride ------ 2.97g

16. ORAL COLONIC LAVAGE SOLUTION
• The PEG acts as an osmotic agent in the GIT, and the balanced
electrolyte concentration results in no net absorption or secretion of ions.
Thus, a large volume of this solution can be administered without a
significant change in water or electrolyte balance.
• The recommended adult dose is 4 L of solution before the procedure.
• The patient is advised to drink each portion quickly rather than sipping it
continuously.

17. ORAL COLONIC LAVAGE SOLUTION
• To date, this approach has been associated with a low incidence of side
effects. The patient should not have taken any food 3 to 4 hours before
beginning to take the solution.
• PEG-ES solutions are employed for unlabeled use in the management of
acute iron overdose in children.

18. SYRUPS
Components and preparation of syrups

19. INTRODUCTION
• Syrups are concentrated aqueous preparations of a sugar or sugar
substitute with or without flavoring agents and medicinal substances.
• Syrups provide a pleasant means of administering a liquid form,
particularly for youngsters.
• Any water-soluble drug that is stable in aqueous solution may be added
to a flavored syrup. However, care must be exercised to ensure
compatibility between the drug substance and the other formulative
components of the syrup.

20. TYPES
Non-Medicated Syrup
• Syrups containing flavoring agents but not medicinal substances are
called non-medicated or flavored syrups. These syrups are intended to
serve as pleasant tasting vehicles. Examples are cocoa syrup, orange
syrup, etc.
Medicated Syrup
• Medicated syrups are prepared by combining sucrose, purified water,
flavoring agents, coloring agents, the therapeutic agent, and other
necessary ingredients.

21. COMPONENTS
Sugars
• Sucrose is the sugar mostly used in syrups, although it may be replaced
other substances such as sorbitol, glycerin, methylcellulose or
hydroxyethylcellulose.
• Sucrose and alternative agents are used for attaining the proper
viscosity.
• They also mask the taste of drug.
• In the case of anti-tussive syrups, the thick, sweet syrup has a soothing
effect on the irritated tissues of the throat as it passes over them.

22. COMPONENETS
Antimicrobial Preservative
• Concentrated sugar solutions are quite resistant to microbial growth. So,
syrups require no additional preservatives if used soon. But for a longer
time period, we need preservatives.
• The amount of a preservative required depends upon the water available
for growth, the nature of some formulative materials and the capability of
the preservative itself.
• Commonly used preservatives are benzoic acid, sodium benzoate
among others.

23. COMPONENETS
Flavorant
Most syrups are flavored with synthetic flavorants or with naturally
occurring materials, such as volatile oils (e.g., orange oil), vanillin, to
render the syrup pleasant tasting.
Colorant
To enhance the appeal of the syrup, a coloring agent that correlates with
the flavorant employed (i.e., green with mint, brown with chocolate, etc.) is
used.
• Generally, the colorant is water soluble, nonreactive with the other syrup
components, and color stable.

24. PREPARATION
Syrups are most frequently prepared by one of four general methods,
depending on the physical and chemical characteristics of the ingredients.
these methods are:
• solution by heating
• solution by agitation without heat
• addition of sucrose to a medicated or a flavored liquid
• percolation

25. PREPARATION
By Heating
• Sugar is dissolved in purified water by heating. Then, other heat-stable
components are added to the hot syrup, the mixture is allowed to cool.
Then, heat-labile or volatile substances are to be added.
• The use of heat facilitates rapid solution of the sugar and certain other
components of syrups.
• However, if overheated, Sucrose is hydrolyzed into monosaccharides.
The sweetness and colour of the syrup changes and syrup becomes
susceptible to microbial growth. So, syrups cannot be sterilized by
autoclaving. We use boiled purified water and preservative agents.

26. PREPARATION
By Agitation
• Sucrose and other agents are dissolved in purified water by agitation.
This process is more time consuming than the use of heat, but the
product has maximum stability.
• To add solid agents to a syrup, it is best to dissolve them in minimal
amount of purified water and incorporate the resulting solution into the
syrup. When solid substances are added directly to a syrup, they dissolve
slowly because of the viscous nature of the syrup.

27. PREPARATION
Addition of sucrose to medicated liquid
• We add sugar to a medicated liquid, like tincture or extract, to prepare a
syrup.
• Many such tinctures and extracts contain alcohol-soluble constituents. If
drug is alcohol-soluble, we make it water soluble. However, if the alcohol-
soluble components are unnecessary, they are removed by filtration.
Then, sucrose is added to the filtrate.
• If the tincture or fluid extract is miscible with aqueous preparations, it may
be added directly to simple syrup or to a flavored syrup.

28. PREPARATION
Percolation
• In one method, sucrose may be percolated to prepare the syrup.
• In the other method, the source of the medicinal component is percolated
to form an extract to which sucrose or syrup may be added. This latter
method really is two separate procedures: first the preparation of the
extractive of the drug and then the preparation of the syrup.
• An example of a syrup prepared by percolation is ipecac syrup, which is
prepared by adding glycerin and syrup to an extractive of powdered
ipecac obtained by percolation.

29. ELIXIRS
Preparation of elixirs, Medicated and non-Medicated
elixirs

30. INTRODUCTION
• Elixirs are clear, sweetened flavored hydro-alcoholic solutions to be taken
orally. An elixir contains at least one active ingredient.
• Elixirs are less sweet and less viscous than syrups.

31. COMPONENTS
• Elixirs’ alcohol content ranges from 5-40%. The proportion of alcohol
varies because the components have different water and alcohol
solubilities.
• Although many elixirs are sweetened with sucrose, some use sorbitol,
glycerin or artificial sweeteners.
• Elixirs having a high alcoholic content usually use an artificial sweetener,
such as saccharin, which is required only in small amounts than sucrose.
• All elixirs contain flavoring agent and coloring agents.
• Elixirs containing more than 10% to 12% of alcohol usually do not require
an antimicrobial agent.

32. PREPARATION
• Elixirs are usually prepared by simple solution. Alcohol-soluble and
water-soluble components are generally dissolved separately. Then the
aqueous solution is added to the alcoholic solution.
• Frequently, the final mixture will be cloudy, principally because of
separation of some of the flavoring oils by the reduced alcoholic
concentration. If this occurs, the elixir is permitted to stand for some time
for oil globules to coalesce and then removed by filtration.
• The presence of glycerin, syrup, sorbitol, and propylene glycol in elixirs
enhances the stability of the preparation. However, the presence of these
materials adds to the viscosity of the elixir and slows the rate of filtration.

33. TYPES
Non medicated Elixir
• Non-medicated elixirs are used as a vehicle, and dilution of an existing
medicated elixir.
• In selecting as vehicle, solubility and stability of the drug in water and
alcohol is concerned. The proportion of alcohol should be only slightly
above the amount needed to maintain the drug’s solution.
• When we have to dilute an existing medicated elixir, the diluent should
have the same alcoholic concentration, flavor and color.
• Examples are aromatic elixir, benzaldehyde elixir, and isoalcoholic elixir.

34. TYPES
Medicated elixirs
• Medicated elixirs contain at least one active ingredient.
• Most official and commercial elixirs contain a single therapeutic agent.
So, the dose of that drug can be increased or decreased by simply taking
more or less of the elixir.
• When two or more therapeutic agents are present in the same
preparation, we may do adjustment in the dose which may not be
desired. Thus, for patients required to take more than a single
medication, many physicians prefer them to take separate preparations
of each drug.

35. ADVANTAGES
• Elixirs are better than syrups to maintain both water soluble and alcohol-
soluble components.
• Easy preparation
• More stable
• Flexibility and ease of administration

36. DISADVANTAGES
• Less effective than syrups in masking the drug taste
• Alcoholic content
• Addiction
• Sedation & Dizziness
• Ignitable

37. SPIRITS
Introduction, Uses and Preparation of Spirits

38. INTRODUCTION
• Spirits are alcoholic or hydro-alcoholic solutions of volatile substances.
• The alcoholic concentration of spirits usually over 60%. Because of the
greater solubility of aromatic or volatile substances in alcohol than in
water, spirits can contain a greater concentration of these materials.
• When mixed with water or with an aqueous preparation, the volatile
substances present in spirits generally separate from the solution and
form a milky preparation.

39. USES
• As flavoring agents, they are used to impart the flavor of their solute to
other pharmaceutical preparations.
• For medicinal purposes, spirits may be taken orally, applied externally, or
used by inhalation. When taken orally, they are generally mixed with a
portion of water to reduce the pungency of the spirit.

40. PREPARATION
Simple Solution
• Majority of spirits are prepared by dissolving the solute in alcohol by
agitation. Filtration is done to obtain a clear product. Example: Aromatic
Spirit
Maceration
• Macerate the vegetable materials in a suitable solvent to extract desired
constituent. Example, Peppermint Spirit
Chemical Reaction
• It involves a chemical reaction. Example is Ethyl Nitrate spirit.
Distillation
• No spirits currently official are prepared by distillation. However, two
important products Brandy and whisky are prepared by distillation.