Pharmaceutics – II

Dosage From Science:

SYRUPS
Introduction:
Due to the inability of some children and elderly people to swallow solid dosage
forms, it is fairly common today for a pharmacist to be asked to prepare an oral liquid
dosage form of a medication available in the pharmacy.

Definition:
Syrups are concentrated aqueous preparations of 85% of sugar or sugar substitute
with or without flavoring agents and medicinal substances.

OR

In medical terminology, medicinal syrups are nearly saturated solutions of 85% of

sugar in water in which medicinal substances or drugs are dissolved.

Types:
There are three types of syrups:

1. Simple Syrup:

It is 85% w/v sucrose solution in purified water (U.S.P).

2. Flavoured Syrups:

They are mostly used to improve the taste of salty, bitter, or otherwise unpleasant
mixtures.

3. Medicated Syrups:

They are of two types:

i. Made from Extractive drugs:

Here, the fluid extract of the respective medicines is mixed with the syrup.

Muhammad Muneeb
D16M137
PUCP
ii. Made from Chemicals:

This can be either by simple solution or by chemical reaction and solution. Here
the taste of the medicinal agents is greatly modified.

Examples:

 Ambroxol Syrup, USP

 Paracetamol Syrup, USP
 Erythromycin Syrup, USP

Components of Syrups:
Most of the syrups contain the following components in addition to the purified
water and any medicinal agents present:

1. Sweetening Agent (the sugar, usually sucrose, or sugar substitute used to provide
sweetness and viscosity)
2. Antimicrobial Preservatives
3. Viscosity Modifier
4. Flavorants
5. Colorants
Many types of syrups, especially those prepared commercially, contain special
solvents, solubilizing agents, thickeners, or stabilizers.

Preparation of Syrups:
Pharmaceutical syrups are produced by mixing purified water, sweeteners, active
ingredients (API), aromas, flavours and other ingredients (thickeners) etc.

There are four methods. Based on the physical and chemical properties on the
ingredients, the choice of the method is selected:

Muhammad Muneeb
D16M137
PUCP
  Solution with heat
 Agitation without heat
 Addition of sucrose to liquid medicament
 Percolation method
1. Solution with Heat:

 This method is used for the following reasons:

o When desired to prepare syrups as quickly as possible
o When the syrup components are not damage or volatilized by heat
 The procedure for this method is
o Add the sugar to the purified water and heat until solution is affected.
o Heat stable components are added to the hot syrup. Cool and made up to the
volume.
o If other components are thermo-labile they are added after cooling like
alcohol and oil.
o Avoid excessive heat because excessive heat will cause inversion of sucrose
causing discoloration.
 Specific gravity of syrup is 1.313 which is important property to identify its
concentration.
Drawbacks:

Over-heating can induce deterioration of sucrose or other component.

2. Agitation without Heat:

 To avoid the caramalization produced by heat, a syrup is prepared by this method

 Sucrose and other formulative agents are dissolved in purified water.
 Ingredients placed in a bottle of greater capacity than volume of syrup. Then
agitation is done.
 The stopper of the bottle is important, as it prevents contamination and loss during
the process
Drawbacks:

 It time consuming and hectic.

 Being concentrated and viscous, it hinders the solubility and uniform distribution
of solid substance added directly.
 However it Is yet stable compared to previous yield
3. Addition of Sucrose to Liquid Medicament:

Muhammad Muneeb
D16M137
PUCP
  The process consists of mixing the fluid extract or tincture with the water,
allowing the mixture to stand to permit the separation of the insoluble constituent.
 The filtration is done.
 After that the sucrose is dissolved in the filtrate.
 Many such tinctures and fluid extract contain alcohol soluble constituents and are
prepared with alcoholic vehicles.
4. Percolation Method:

 In this method percolator is used.

 Purified water or aqueous solution of a medicating or flavoring liquid through a
column of crystallization sucrose to dissolve.
 The percolate is collected and returned to the percolator as required until all of
sucrose has been dissolved.

Invert Syrup:
Definition:

Invert syrup is a sugar syrup composed of equal parts glucose (C6H12O6) and
fructose (C6H12O6), derived from splitting a solution of sucrose (C12H22O11) in water
(H2O) into these component parts.

Name Derivation:

The concentration of sugar syrup can be measured by passing polarized light (light
whose waves are all aligned in a single plane which can be measured before and after it
enters the syrup) through the solution and measuring the degree of light wave rotation
upon exiting. A solution of pure sucrose will rotate the light 66.5 degrees to the right,
and as the sucrose is converted into glucose and fructose the exiting light will begin
rotating to the left. A fully converted sugar will have an exit rotation of 39 degrees to the
left. This inversion of the rotation from right to left gives the converted syrup its name.

Other Names:

 Inverted syrup
 Trimoline

Process:

Sucrose is a disaccharide, which indicates that it is composed of two simpler

monosaccharides (glucose and fructose). By heating a solution of sucrose in water, a

Muhammad Muneeb
D16M137
PUCP
hydrolysis reaction is induced which splits the disaccharide into its two component parts.
By adding an acid catalyst such as lemon juice (10ml per kg sugar) or cream of tartar (1g
per kg sugar), the reaction can be accelerated. Pastry chefs often make invert syrup by
cooking sucrose syrup with an acid until thicker syrup is formed (e.g., boiling a
sucrose/acid solution for 20 minutes at 237°F). Invert syrup can be made in varying
thicknesses based on the ratio of sugar to water, and can be converted to varying degrees
(up to about 85% glucose/fructose) based on the reaction time.

Naturally Occurring Forms:

 Honey
 Jams

Color:

Light to medium gold

Taste:

Noticeably sweeter than sucrose

Advantages:

 Invert syrup will resist crystallization longer than sucrose syrup.

 If invert syrup begins to solidify, it can be re-liquefied by warming gently.
 Invert syrup creates products that are smoother and less granular than sucrose
syrup.
 Invert syrup retains more moisture than sucrose syrup, so it adds preservative
qualities to products and has a longer shelf life.
 Invert syrup is an important ingredient in low-fat goods, as it replaces the moisture
content that would be provided by fat.
 All constituent sugars (sucrose, glucose, and fructose) support fermentation, so
invert syrup can be fermented as easily as sucrose syrup.

Factors to be taken in Consideration:

The manufacturing process must achieve the following factors:

 Dissolving of the sugars to form a syrup

 Hydration of powdered ingredients
 Blending ingredients of widely different viscosity
Muhammad Muneeb
D16M137
PUCP
  Suspension or dissolving of active ingredients
 The end product must be smooth, agglomerate-free and homogeneous.
 Equipment should conform to GMP standards

Packaging of Syrup:
Syrup, as a pharmaceutical product requires safe, secure and tamper - proof
handling while packaging. Packaging of syrups needs to ensure complete protection from
contamination and microbial growth. Our inevitable packaging support assures the safe
and secure packaging of syrups so as to ensure their extended shelf life.

The general process of packaging is:

 Filling
 Sealing
 Capping
 Coding & labeling
 Wrapping

Process Involved in Syrup Packaging:

 Empty Bottles are rinsed though Air-jet cleaning.

 After complete cleaning, bottles are tested & transferred ahead for filling.
 Filling machines with their automatic piston fills the bottles with accurate volume
of syrup.
 Capping is done on bottle through capping machines.
 Plastic or aluminum capsules are bound over the neck of the bottle for secure
sealing.
 Important details regarding packaging date & expiry date are printed on bottles.

Advantages of Syrups:

 Appropriate for any patient, whatever the age is.

 The most natural and easiest route of administration.
 Economical and safe to the patient.
 No nursing is required, which means the patient can take it with no help.
 The liquid dosage form is expected for certain types of products like cough
medicines.
Disadvantages of Syrups:

 Delayed onset of action because absorption takes time.

 Not suitable in emergency and for unconscious patients.
Muhammad Muneeb
D16M137
PUCP
 Not convenient for a patient with a gastrointestinal disorder such as diarrhea,
constipation, ulceration, and hyperacidity in stomach.
 Can’t avoid first pass metabolism.

Muhammad Muneeb
D16M137
PUCP