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Solution

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Solution

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SOLUTION

UZMA MUMTAZ
Solution
Solutions are homogeneous mixtures of one or more solutes molecularly dispersed in a suitable
solvent or a mixture of mutually miscible solvents.
A homogenous mixture that is prepared by dissolving a solid, liquid or gas in another liquid and
represents a group of preparations in which the molecules of the solute or dissolved substance
are dispersed.
Pharmaceutical solutions are used for many routes of administration, including Oral, Rectal,
Vaginal, Ophthalmic, and Parenteral.
Solution
A solution is a thermodynamically stable, one-phase system composed of 2
or more components, one of which is completely dissolved in the other.
The solution is homogeneous because the solute, or dispersed phase, is
dispersed throughout the solvent in molecular or ionic sized particles
Broadly defined, a solution may be any combination of solids, liquids, and/or
gases. We will restrict our definition of pharmaceutical solutions to those
composed of a solid, liquid, or gas dissolved in a liquid solvent
Pharmaceutical solutes may include
• active drug components,
• flavouring agents
• colouring agents
• preservatives
• stabilizers
• buffering salts
solvent for pharmaceutical solutions,
• water
• ethanol
• glycerine
• propylene glycol
• isopropyl alcohol or other liquids may be used, depending
on the product requirements.
Solvent properties
To be an appropriate solvent,
the liquid must completely dissolve the drug and other solid ingredients at
the desired concentration,
be nontoxic and safe for ingestion or topical application,
aesthetically acceptable to the patient in terms of appearance, aroma,
texture, and/or taste
Solubility
The solubility of a drug is the expression of the quantity of a drug
that can be maintained in solution in a given solvent at a given
temperature and pressure.
It is usually expressed as the number of milliliters of solvent required
to dissolve 1 gram of the drug. Understanding drug solubility is
critical in formulating solutions.
On the basis of water as solvent
Aqueous solution
An aqueous solution is a solution in which the solvent is water.
Non aqueous solution
The solution obtained by dissolving solute in any liquid other than water.
Based on the amount of
solute in solution
1. Unsaturated
An unsaturated solution is a solution that contains less than the maximum amount
of solute that is capable of being dissolved
2. Saturated
A saturated solution is one that contains the maximum amount of solute that
the solvent will accommodate at room temperature and pressure.
3. Supersaturated
. A supersaturated solution is one that contains a larger amount of solute than
the solvent can normally accommodate at that temperature and pressure. It is
usually obtained by preparing a saturated solution at a higher temperature,
filtering out excess solute and reducing the temperature.
Basis on amount of solvent
present
Concentrated solution
A concentrated solution is one that has a relatively large amount of dissolved solute.
Dilute solution
A concentrated solution is one that has a relatively large amount of dissolved solute.
Basis of concentration of solute
in two solution
Isotonic solution
An isosmotic solution is one that has the same osmolarity as another solution irrespective of
the membrane permeabilites of the dissolved solutes.
An isotonic solution does not cause cell swelling or shrinkage (i.e. net movement of water across cell
membranes is zero).
E.g 0.9% NaCl or 5% glucose
Hypotonic solution
A hypotonic solution is a solution that has a lower concentration of solute compared to the cell.
Hypertonic solution
A solution will be hypertonic to a cell if its solute concentration is higher than that inside the cell,
and the solutes cannot cross the membrane.
Solution type base on solute
molecular size
Micromolecular solutions consist of dispersed molecules or ions in the 1-
10 A size (MW < 10,000).
In macromolecular solutions (MW > 10,0000), the solutes are in true
solutions, but the solute size of macromolecular solutions lends special
properties to them.
Because the particles are so large, most cannot be sterilized by filtration.
The solutions are also quite viscou, and may be used as thickening agent for
other dispersed dosage forms.
Macromolecular solutions include those containing acacia, methylcellulose
and other cellulose derivatives, and proteins such as albumin.
Pharmaceutical application

Solutions have a wide variety of uses in the pharmaceutical


industry. They are used therapeutically as vehicles for oral,
parenteral, topical, otic, ophthalmic, and nasal products.
They are also used as flavourings, buffers, preservatives, and
suspending agents for various liquid dosage forms.
Concentrated stock solutions often serve as components of
extemporaneously prepared products.
Test solutions also play an important role in, the analysis of
pharmaceutical products of all types.
Advantages of Pharmaceutical
Solutions
1. The drug immediately available for absorption. By providing drug in a solution,
the dissolution phase absorption can have bypassed → quicker absorption .
2. Flexible dosing is possible. The active ingredient within solution present in a
certain Conc. per unit volume.
3. Solutions are designed for any route of absorption: the oral route of
administration, via Parenteral preparations (injections), enemas for rectal use,
Topical (for use on skin) and ophthalmic preparations are all solutions.
4. No need to shake the container. Unlike suspensions as the active ingredient is
dissolved within the vehicle.
5. Facilitate swallowing in difficult cases (e.g. infants or the elderly). It is easier for
patients to take solution
Disadvantages of
Pharmaceutical Solutions
1. Drug stability is reduced in Sol by hydrolysis or oxidation. For this reason, Sol. is
commonly having a shorter expiry date than equivalent solid dosage forms.
2. It is difficult to mask unpleasant tastes.
3. A major disadvantage; they are much larger and bulkier, difficult to transport.
Liquids packed in glass bottles are obviously prone to breakage and cause loss of
the preparation.
4. Technical accuracy is needed to measure the dose on admin. patient accuracy in
measuring a dose is required.
5. Some drugs are poorly soluble so it is necessary to alter vehicle or drug form in
order to formulate a convenient prep.
6. A measuring device is needed for admin. so need to be supplied to the patient
to be able to measure an accurate dose
Pharmaceutical
Oral solution
Ophthalmic solution
Nasal solution
Mouth wash
SYRUP
INTRODUCTION
1. Syrup are concentrate aqueous preparation og sugar and sugar substitute with or without
flavouring agents and medicinal substances.
2. Syrup provide pleasant mean of administering a liquid form
3. Any water soluble drug that is stable in aqoues solution may be added to a flavoured syrup.
4. However care must be exercise to ensure compatibility between the drug substance and the
other formulative components of the syrup.
TYPES
1.Medicated syrup
Preparing by combining APIs, sucrose , purified water ,flavouring agents , coloring agents and
other necessary ingredients .
2.Non medicated syrup
Syrup containing flavouring agents but donot medicinal substances are called non medicated or
flavouring syrup
Syrup Intented to serve as pleasant tasting vehicles
E.g :cocoa syrup
Orage syrup
Simple syrup
According to BP
67.7% W/V
According to USP
85% W/V
Components
1.Sugar
Sucrose is motly used sugar in syrups .other subtances are sorbitol,glycerine ,methylcellulose
and hydroxyl ethylcellulose
Sucrose is alternative agents are used for attaining the proper viscosity.
Mask the taste of drug
Soothing effect on the irritated tissues of the throat .
Stability of aqueous sucrose solutions:
In order to formulate syrup properly, one must consider the
properties of the basic vehicle particularly its stability, sucrose is
subjected to two degradative pathways in aqueous solution
fermentation and hydrolysis.

Preservative used in syrup include benzoic acid ,butyl


paraben ,sorbic acid ,glycerin ,alcohol etc. benzoates ,butyl
paraben ,sorbic acid are most effective in acidic solution ,they in
effective as preservative in alkaline solution mixtures of parabens
are frequently employed to take advantage of their potentiating
effect
Flavoring agents
Most syrup are flavoured synthetic or with naturally occurring
materials ,i-e orange , vanillin
Coloring agents
To enhance the appeal of syrup a coloring agents that correlates
with flavouring employed i.e green with mint , brown with
chocolate .
Incompatibilities:
1. If a preparation containing high concentration of alcohol
sucrose will crystallize, simple syrup can tolerate 10%
alcohol without crystallization.
2. When solution containing pectin are mixed with sucrose
syrup .Gellation is observed since sucrose partially
dehydrate pectin.
3. When syrup dehydrated with aqueous solution the necessity
for additional preservative should be considered
Preparation of syrup
Syrups are most frequently prepared by one of four general methods, depending on the physical
and chemical characteristics of the ingredients. Broadly stated, these methods are
a) Solution of the ingredients with the aid of heat.
b) Solution of the ingredients by agitation without the use of heat or the simple admixture of
liquid components.
c) Addition of sucrose to a prepared medicated liquid or to a flavored liquid.
d) Percolation of either the source of the medicating substance or the sucrose. Sometimes syrup
is prepared by more than one of these methods, and the selection may simply be a matter of
preference on the part of the pharmacist
Steps in syrup preparation
Write out the formula
Calculate the quantities
Prepare the label
Weighing all ingredient
Reduce particle size of solid if necessary
Solid is dissolved in the required amount of solvents
Make the final volume
Packing
Labeling
Dispense
a) Solution of the
ingredients with the aid of
heat
Syrups are prepared by this method when it is desired to prepare the
syrup as quickly as possible and when the syrup’s components are
not damaged or volatilized by heat.
In this method, the sugar is generally added to the purified water,
and heat is applied until the sugar is dissolved.
Then, other heat-stable components are added to the hot syrup, the
mixture is allowed to cool, and its volume is adjusted to the proper
level by the addition of purified water.
b) By agitation
To avoid heat-induced inversion of sucrose, syrup may be prepared
without heat by agitation.
On a small scale, sucrose and other formulative agents may be
dissolved in purified water by placing the ingredients in a vessel larger
than the volume of syrup to be prepared, permitting thorough
agitation of the mixture.
This process is more time-consumingg than the use of heat, but the
product has maximum stability.
c)Addition of Sucrose to a
Medicated Liquid or to a
Flavored Liquid
•Occasionally, a medicated liquid, such as a tincture or fluidextract, is
employed as the source of medication in the preparation of syrup.
•Many such tinctures and fluidextracts contain alcohol-soluble
constituents and are prepared with alcoholic or hydroalcoholic
vehicles.
•If the alcohol-soluble components are desired medicinal agents,
some means of rendering them water soluble is employed.
Percolation In the
percolation method
Either sucrose may be percolated to prepare the syrup or the source of the medicinal
component may be percolated to form an extractive 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.
The drug ipecac, which consists of the dried rhizome and roots of Cephaëlis ipecacuanha,
contains the medicinally active alkaloids emetine, cephaline, and psychotrine.
 These alkaloids are extracted from the powdered ipecac by percolation with a hydroalcoholic
solvent
Application of Syrups
Syrups are intensely sweet vehicles which lack significant amount of alcohol
and can function to mask the taste otherwise salty or bitter drugs.
Their effectiveness as vehicle is due also to their high viscosity and mouth feel
qualities .
Syrups are often described as having body and smoothness.
 For these reason important advantage of syrup is their acceptability and wide
variety of flavors they constitute the vehicle most widly used for pediatric
medication
ELIXIRS
INTRODUCTION
oElixirs are clear, sweetened, flavoured, hydro- alcoholic
solutions to be taken orally.
oAn elixir contains at least one active ingredient .
oElixirs are less sweet and less viscous than syrups.
Components
Alcohol 5-40%
Sweetener (sucrose , sorbitol, glycerine, artificial sweetener)
Flavouring agents and colouring agents
Elixir containing more then 10-12% of alcohol usually not required an
antimicrobial agents.
Types
A) Medicated
Medicated elixir contain at least one active ingredient.

B) Non medicated
Non medicated elixir are used as a vehicle ,and dilution of an existing medicated elixir .
In selecting as a vehicle , solubility and stability of a drug in water and alcohol is concerned .
The proportion of alchol should be only slightly above the amount needed to maintain the drug solution .
When we have dilute an existing mediated elixir ,the diluent should have the same alcoholic
concentration , flavour and color.
E.g: Aromatic elixir, bezaldehyde elixir and isoalcoholic elixir.
Preparation
Simple dissolutions or mixtures of two or more liquids can be used to prepare elixirs after
the ingredients have been dissolved in their respective solvents.
Those that are alcohol-soluble will dissolve in alcohol, and those that are water-soluble will
dissolve in water.
Aqueous solutions are added to alcoholic solutions to maintain the strength of the alcohol.
Once the desired volume has been reached , the mixture is made into ice cream.
In this stage, some of the flavoring agents can separate from the product due to the
reduction in alcohol strength.
Once the elixir is allowed to stand for a while, oil globules begin to precipitate.
The filtrate is then added.
The excess oils are absorbed by talc.
The resulting product is clear after filtration.
Advantages
Elixirs are better than syrup for maintaining both water and alcohol soluble
components.
Easy preparation
More stable
Flexibility
Easy of administration
Disadvantages
Less effective than syrup in masking the drug .
Alcohol content.
Addiction
Sedation and dizziness
Ignition
Spirit
Introduction
Are alcoholic or hydro alcoholic solutions of volatile principle, mostly volatile
oils.
Spirits could be classified according alcoholic or hydro alcoholic solutions of
volatile principle, mostly volatile oils.
Spirits could be classified according to their uses:
1. Therapeutic spirits: which contain therapeutic volatile substances.
2. Flavouring spirits: which contain flavouring volatile substances.
Preparation
Spirits were prepared by distillation, but nowadays they are prepared
by dissolving the volatile substances in alcohol.
» The amount of volatile substance in spirits varies greatly and no
fixed percentage can be given, but in all cases, volatile substances in
the spirits are more than that of aromatic water (clear aqueous
solution saturated with volatile oils (e.g. rose oil, Peppermint oil), or
other aromatic or volatile substances eg. camphor)
» Amount of alcohol differ from one spirit to another, the lowest
amount of alcohol found in internal spirits as (aromatic spirit of
ammonia) which contain 62-68% alcohol while (camphor spirit) which is
used externally contain 80-87%.
» Spirits when taken orally, they are generally mixed with portion of
water to reduce the pungency effect.
» In preparation of spirits we must keep in mind that the oil dissolved in
alcohol is precipitated causing turbidity when the solutions are mixed
with water other than specified in the formula, so all equipment should
be dry and filter paper should be moisten with alcohol.
» Spirits should be stored in light resistant containers and in cool place
to prevent evaporation of alcohol and volatilization of volatile
substance or active ingredients and to limit oxidative changes
Methods of preparation
1. Simple solution method
2. Maceration
3. Chemical reaction
4. Distillation
Aromatic spirit of ammonia
Rx Ammonium carbonate
34 g Dilute solution of ammonia
90 ml Oil of lemon
10 ml Oil of lavender
1 ml Oil of Myristica
1 ml Alcohol 700 ml
D.W Q.S 1000 ml
Method: Dissolve the solid agent in dilute solution of ammonia with little
amount of water , while the oil dissolved in alcohol also with little amount of
water, and then add the aqueous solution into alcoholic one after filtering each
one. Note: In preparation of aromatic spirit of ammonia we make filtration due
to the presence of water with alcohol that lead to precipitation of volatile oil
Uses of official spirits
1. Carminative
2. Antacid
3. Mild reflex circulatory stimulant
4. Flavouring agent
Difference between elixirs and syrups
1. Elixirs are usually less sweet and less viscous than syrups because
they contain a lower proportion of sugar and consequently are
less effective than syrups in masking the taste of medicinal
substances, hence required flavoring agent.
2. Elixirs are better than aqueous syrups to maintain both water
soluble and alcohol soluble components in solution because of
their hydroalcoholic character.
3. From manufacturing stand point, elixirs are preferred over syrup
due to their stability and ease of preparation (by simple solution
Mouthwash
Introduction
mouthwashes are antiseptic solutions intended to reduce
the microbial load in the mouth.
Ingredients
There are many active ingredients used in various types of mouthwash, each with its own effects and benefits.
They include
Cetylpyridinium chloride : It is added to mouthwash to reduce bad breath.
Chlorhexidine : It can be used to help control plaque and gingivitis and generally can’t be bought without a
prescription.
Essential oils : Helps control plaque and gingivitis
Fluoride : It is used to help prevent tooth decay
Peroxide : Helps teeth whitening
Sodium Fluoride : used for preventing tooth decay and helping decrease teeth sensitivity.
Eucalyptus : help prevent plaque and gingivitis2
Hydrogen peroxide : used for teeth whitening and is highly effective in penetrating the hard tissues of the teeth
Types
1. cosmetic mouthwash
2. Fluoride mouthwash
3. Antiseptic mouthwash
4. Natural mouthwash
5. Whitening mouthwash
THANK YOU

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