Galenicals

Galenical Preparations
• Galen (Claudius Galenus-Galen of Pergamum A.D .130-200)was a Greek physician
and the great figure in Roman medical history and author of books , the drug and
remedies described in which were used almost universally for fifteen hundred
years.
Medicines prepared according to the formulae of Galen.
• The term Galenicals is now used to denote standard preparations containing
one or more active constituents of a plant and made by a process that leaves
the inert and other undesirable constituents of the plants un-dissolved.
• The term is applied to the Crude medicinal products made from animal or
vegetable drugs
• It is prepared by extraction of crude vegetable drugs (active principles)with
suitable solvent(s).

Pharmaceutical preparations are divided into:

• Galenical preparation
• Non-Galenical preparations

Types: Infusions- Decoctions- Fluid extracts- Semisolid extracts – Dry extracts- Tinctures- Medical
oils…..
 Nomenclature:
• Galenicals: Owing to Galen who discovered it.(Defined previously)
• Menstruum: Solvent used for extraction (ex. water, alcohol, ether etc)
• Marc: The inert fibrous and other insoluble materials remaining after
extraction

Need for the separation of active principles:

 Potency of the drug may be known and is more rapidly controlled.
 Deterioration by enzyme is diminished.
 Drug can easily be formulated into required dosage form
 Dosage form is more stable, elegant and palatable.
 Tablets cannot be manufactured from crude drugs.
 Injectable from crude drugs are undesirable rather very dangerous.
 Bulk (volume/amount) smaller bulk can easily be controlled/shipped and so
reduces the cost of the drug
 Extraction
Extraction involves the separation of medicinally active portions of plant or animal
tissues from the inactive or inert components by using selective solvents in
standard extraction procedures. Source of drugs: (active ingredients) may be plant
or animal .
Extraction Processes:
• Expression
• Infusion
• Decoction
• Digestion
• Maceration
• Percolation
 1.Expression:
• It is process of extraction of active constitution from the plant parts without using
solvents(menstruum).
• It is done mechanically using special type of equipments. In this method, fresh
drug is placed in a screw press or hydraulic press and strongly pressed so that
plant juice is obtained.
Examples :
• Extraction of different types of oils from plant seeds ground nut seeds, castor
seeds, teel seeds etc.
• Mainly applicable to seeds and fresh leaves
 2. Infusion
• “A product obtained when a suitably finally divided drug is treated with
either hot or cold water for a certain length of time, after which the fluid
portion is strained off and retained and the solid portion rejected.”
• “Infusions are solutions containing the readily soluble constituents of crude
drugs”
Drug:
• Crude drugs of light structure without dense tissues and containing
water-soluble constituents.
• The drug may be freshly broken, thinly sliced, cut small, or coarsely
powdered in order to facilitate the solvent penetration.
Menstruum: Always water (cold or boiling).
Time: Determined according to the amount of drug constituents to be
extracted and the ease or difficulty with which the water penetrate the drug.
Examples: Teas- Senna infusion, Infusion of senega
Process:
• It is a process of steeping or drenching a drug in water so as to extract the active principles.
• It involves pouring water over the drugs and then allowing it to keep in contact with water
for the stated period (e.g 15 min) with occasional stirring and finally filtering off the liquid.
• Fresh infusion is prepared by macerating the drug for a short period of time with cold or
hot (boiling) water.
• Concentrated infusions are prepared by a modified percolation or maceration process.

Infusion pot:
1. The simplest form is coffee pot or tea pot. The drug may be placed at the bottom of the pot
,the water is added, the contents well stirred3 -4 times over the period of infusion.
2. Special pots are also used and consists of covered jar (made of earthenware, stainless-
steel, ceramic, glass, porcelain) to which is fitted at certain height a perforated tray upon
which the crude drug may be allowed to rest in water being poured over it.
3. The drug may be enclosed loosely in a small muslin bag and suspended in the jar at a
height where it will be just covered by the liquid. Stirring is not necessary.
The perforated tray or muslin bag confers two advantages:
 A-Complete extraction because when the menstruum (solvent) surrounding the drug
becomes saturated, it will sinks to the bottom due to its increased density and another
amount of fresh menstruum displace it leading to circulatory diffusion
 B- At the end of infusion time, the drug can be lifted out, leaving clear liquid which can
be strained quickly
Preparation(Fresh Dilute Infusion)
• The simplest of all methods of extraction.
• A definite weight of the crude drug in a certain state of subdivision (cut
small,coarse, powdered…) is prepared.
• The calculated amount of hot or boiling menstruum (usually water) is added
to the crude drug.
• Soak for a definite time.
• During the period of infusion, the heat should be retained in the container
and the content should be stirred.
• After the time of infusion, the liquid is poured off or strained
• Do not press or squeeze the marc otherwise colloidal cell contents may be
forced out giving a cloudy infusion.
• Such fresh infusion should be used within 12 hours after its preparation
because it gets spoiled due to bacterial and fungal growth
• e.g. Fresh infusion of Quassia.
Concentrated (stock) infusion
• To avoid rapid decomposition to which the fresh (dilute) infusions are
subjected.
• These preparations are not made by the concentration of the dilute infusion
by evaporation, since thermal treatment will result in loss of the volatile
principles.
• Prepared by double or triple maceration 8 times stronger than fresh infusion
• Concentrated infusions prepared with alcoholic menstruum or contain alcohol
as a preservative.
• Concentrated infusion are not intended to be dispensed in the concentrated
state, but upon use, are diluted with at least seven times their volume of
water
e.g Concentrated infusion of Quassia.
 Examples of infusion
• Concentrated infusion of Quassia Dilute infusion of Quassia
Quassia, cut small…………………… 80 gm
Alcohol (90%)…………………………. 250 ml
Rx.
Distilled water, cold Q.S to……..1000 ml Concentrated infusion of Quassia… 125 ml
Prepared by triple maceration. Distilled water, cold Q.S to……………1000 ml
1- Macerate Quassia with 650 ml of cold water for one Preparation: Just mix
hour, mix occasionally, strain and reserve the clear
liquid. Dose: 15 to 30 ml
2- Repeat maceration process twice, using 500 ml of
cold water for each maceration.
3- Combine second and third maceration and
evaporate to 100 ml.
4- Mix liquid 3 with liquid 1, add alcohol and adjust the
volume to 1000ml with cold distilled water
Dose: 2 to 4 ml
Alcohol is added to the final product as a preservative
Use: Anti-malaria, Appetite stimulant (bitter
stomachic).
 3. Decoction
• In this process the active principle of crude drug is extracted by boiling in water
in a specified volume of water for a defined time.”
Or
• Solutions of the water soluble constituents of plant drugs prepared by boiling
the drug with water.
• For extraction of drugs with water soluble and non- volatile constituents, and
drugs of hard and woody nature.
• Should be freshly prepared.
Preparation:
The starting ratio of crude drug to water is fixed. The volume is then brought
down to one-fourth its original volume by boiling during the extraction
procedure
• Previously sliced drug barks or wood (5 parts) is boiled with water (100
or 120 parts) in a vessel of enameled iron or earthenware for a definite
length of time (15 min.) counting from when the liquid starts to boil
with occasional stirring.
• To obtain highly concentrated decoction, boiling is continued until the
liquid reduced to a certain volume. Allow to cool to about 40ºC, press
the marc and mix the resulting liquid to the decoction.
• At the end of decoction time, decoction is strained through fine muslin
or flannel according to the nature of marc. Then, sufficient water is
passed through the strainer to produce a definite volume.

Example: Cinchona bark or wood (contains quinine)

Uses: Treatment of fever, malaria and as an appetite stimulant. Also used in
anemia, indigestion, gastrointestinal disorders, general fatigue.
Comparison between infusion and decoction
 4.Digestion
• This process is a modified maceration in which extraction of drug is carried out at
a higher temperature at which the active ingredients are not adversely affected.
• Use of higher temperature provides for enhanced solvent action of menstruum.
If the menstruum is readily volatilized at the temperature employed, a reflux
condenser is attached to the vessel so that the solvent may get condensed,
recovered and returned to the container.
• This process is applicable to thermostatic one. It is also known as accelerated
maceration.
• Not applicable to volatile menstruum
• e.g:- gum, resin…..
 5.Meceration
• The term maceration comes from the Latin macerare, meaning to soak. It is a
process in which the properly comminuted drug is permitted to soak in the
menstruum until the cellular structure is softened and penetrated by the
menstruum and the soluble constituents are dissolved.
• Particle size of drug should be coarsed or moderately coarse & not fine.
• A closed vessel is recommended, to prevent loss of the menstruum.
• Maceration process involves the separation of medicinally active portions of
the crude drugs.
• In the maceration process, the drug to be extracted is generally placed in a
wide-mouth container with the prescribed menstruum, the vessel is
stoppered tightly, and the contents are agitated repeatedly over a period
usually ranging from 2 to 14 days. The agitation permits the repeated flow of
fresh solvent over the entire surface area of the comminuted drug.
Types of maceration:
1. Simple maceration (for organized drugs),
2. Maceration with adjustment (for unorganized drugs)
3. Multiple maceration (for concentrated preparations)
Various types of maceration process:
1.Simple maceration: a process for the tinctures made from organized drugs like roots, stems,
leaves
• Drug is placed with the whole of the menstruum in a closed vessel for 7 days, shaking
occasionally. After 7 days liquid is strained and marc is pressed. The pressed liquid is mixed with
strained liquid, then filtered to make a clear liquid. Final volume is not adjusted.
• Ex:- Tincture of Orange
2.Modified maceration (Maceration with adjustment) : A process for the tinctures made from
unorganized drugs like gums, resins .
• The drug is placed with 4/5 th of the menstruum in a closed vessel for a period of 2-7 days with
occasional shaking. After 7 days the liquid is filtered and the final volume is made up by the
remaining menstruum. The marc is not pressed.
• Ex:- Tincture of Tolu Compound tincture of Benzoin Tincture of Myrrh
3. Multiple maceration: multiple maceration is adopted to achieve maximum extraction of active
constituents from drug if the drugs having high % of active substances. The process is carried out in
the same way as simple maceration process, but the menstruum used is divided into 2 parts in
Double maceration and 3 parts in Triple maceration
• Double maceration process:The drug is macerated twice by using the
menstruum which is divided into 2 parts, in which the same volume is
used for each maceration
• Triple Maceration Process: The drug is macerated thrice by using the
menstruum which is divided into 3 parts, in which the same volume is
used for each maceration.
 7.Percolation
• The term percolation, from the Latin per, meaning through, and colare, meaning to strain,
may be described generally as a process in which a comminuted drug is extracted of its
soluble constituents by the slow passage of a suitable solvent through a column of the drug.
• The drug is packed in a special extraction apparatus termed a percolator, with the collected
extractive called the percolate.
Types of percolation
Percolation can be performed by these three methods which are mentioned below;
1.Simple percolation process
2. Percolation process for concentrated preparations (Reserved percolation and Modified
percolation
3. Continuous hot percolation / Soxhlet Extraction / Soxhlation
Simple Percolation Process
a) Size reduction
b) Imbibition or moistening of crude drug :It is done with a suitable solvent and allowed to
stand for 4 hours in closed container. The drug will swells up and the menstruum will get
into the cell wall of the crude drug.
c) Packing: After imbibition the imbibe drug is evenly packed into the percolator.
d) Maceration: After packing of the crude drug sufficient amount of the menstruum is added
to saturate the material and close the percolator with a lid.
e) Percolation: After 24 hours, the tap of the percolator is opened and collected liquid is
allowed to drip down at a controlled speed till 3/4 volume is collected. More menstruum is
added so that marc does not become dry.
. Reserved percolation
1st portion (about 3/4 of the final product) of the percolate containing maximum active principles is
reserved.
• Subsequent percolation is completed until drug is exhausted but the last 1/4th of final volume is
collected separately.
• 2nd dilute part is evaporated to get the syrupy consistency which is then mixed with reserved
portion and final volume is adjusted with menstruum.
• Generally alcohol is used as menstruum.
Examples: liquid extract of liquorice.
3. Continuous extraction:
• This process is used for those drugs where the penetration of the menstruum into the cellular tissues is
very slow,
• the solute is not readily soluble into the solvent and the quantity of the menstruum is very less.
• In such cases Soxhlet extractor is used where small volume of hot menstruum is passed over the drug
time and again to dissolve out the active constituents until the drug is exhausted. The process is known
as Soxhlation
 In normal extraction process, concentrated preparations are made followed by evaporation of
solvent. Continuous extraction combines two operations i.e. evaporation and condensation.
 Condensed liquid is returned to the drug to continue extraction. So with the help of temperature
smaller volumes of solvent may be used and process is called “continuous extraction.”
• Some volume of the solvent is used again and again using special apparatus.
• A continuous extraction may be;
1) Continuous hot extraction
2) Continuous cold extraction
 Extractive preparations
• After the separation of the active constituents form the crude drug,
the active principles are ready to use in the form of;
• Extracts
• Fluid extracts
• Tinctures
 EXTRACTS
Definition:
• “Extracts are concentrated preparations of vegetable or animal drugs
obtained by removal of the active constituents of the respective drugs with
suitable menstruum, evaporation of all or nearly all of the solvent, and
adjustment of the residual masses or powders to the prescribed
standards.”
Properties
• Extracts are potent preparations, usually between two and six times as
potent on a weight basis as the crude drug.
Objective/Function:
• Their function is to provide in small amounts and in convenient way, stable
physical form of the medicinal activity and character of the bulkier plants
that they represent. As such, they have use in product formulation.
Types of extracts:
There are three major types or forms of the extracts;
I. Semisolid or semiliquid of syrupy consistency e.g. hyoscyamus extract.
II. Plastic masses known as pilular or solid extract e.g. glycyrrhiza extract.
III. Dry powder known as powdered extracts e.g. belladonna extract.
• Powdered extracts are used in solid dosage forms i.e. tablets, capsule, powders,
granules etc. and the pilular extracts are used in plastic dosage forms, ointments
and suppositories
Preparation of extracts
1.Extracts made by percolation
• Extracts can be made by various methods but most of the extracts are
prepared mainly by percolation.
• Percolate is concentrated by;
• Evaporating whole of the drug solution in case of thermostable drug.
• Under reduced pressure in case of thermolabile drugs.
• Reserved percolation in case of thermolabile preparations.
• Continuous extraction both hot and cold.
2. Extracts made by reserved percolation:
All are liquid preparations prepared by taking alcohol as menstruum. Products are
adjusted to the specified volume, while the unreserved portion is evaporated
under reduced pressure.
Example: Liquid extract of belladonna, Liquid extract of ipecacuanha etc.

3. Extracts prepared by maceration:

In this process whole drug is macerated in whole of the solvent.
Example: Liquid extract of senna, compound extract of colocynth.

4. Extracts made my digestion:

Digestion process is rarely exploited for the preparation of the extracts.
Example: Extract of malt, it helps in the digestion of fatty food due to the presence
of enzymes in it.
5. Extract of animals:
Extraction is accomplished by using appropriate process and solvent.
Example: Extract of ox bile, Extract of Liver.

Packaging and Storage of Extracts:

They must be packaged in;
• Wide mouth containers or plastic tubes and closely tight to prevent loss of
moisture which would result in it’s becoming hard and unstable for use.
• They must be kept at cool and dry place.
 FLUID EXTRACTS
“Fluid extracts are liquid extracts of vegetable drugs that contain alcohol as a
solvent, preservative, or both.”
Properties
• Fluid extracts are prepared by percolation so that each milliliter contains the
therapeutic constituents of 1 g of the standard drug.
• Because of their high drug content, fluid extracts are sometimes referred to as
“100% tinctures.”
• Fluid extracts of potent drugs are usually 10 times as concentrated, or potent,
as the corresponding tincture. For example, the usual dose of tincture
belladonna is 0.6 mL; the equivalent dose of the more potent fluid extract is
0.06 mL.
• Many fluid extracts are considered too potent for self-administration by
patients, so they are almost never prescribed.
• Many fluid extracts are simply too bitter. Hence,most fluid extracts are
modified by either flavoring or sweetening agents.
 TINCTURES
“Tinctures are alcoholic or hydroalcoholic solutions prepared from vegetable
materials or from chemical substances.”
Properties
• A product is called tincture when it contains 45% v/v or more alcohol. Tincture
ipecacanha is an exemption containing about 23% v/v of alcohol. Generally a
tincture contains alcohol ranging 20% - 90% v/v alcohol.
• They vary in method of preparation, strength of the active ingredient, alcoholic
content, and intended use in medicine or pharmacy.
Preparation of tinctures:
They are considered stable preparations as they have sufficient amount of alcohol
to resist the microbial growth. Tinctures can be prepared by various methods;
1. By Dilution/ Simple Solution:
• Tinctures can be prepared by the dilution method from the concentrated
extracts. Solute is dissolved in the solvent with agitation, and then filtered off.
Example: Iodine, Thimerosal, Green soap tinctures.
2. By Maceration:
Tinctures can also be prepared by;
• . From the maceration of organized drugs e.g. Tincture of Aurantii
• From the maceration of unorganized drugs e.g. Tincture of benzoin, Tincture of myrrh.
3. By percolation:
Tinctures can also be prepared by the percolation of the crude drug in percolator.
• Example: Tincture of Belladonna, Tincture of Digitalis.

Disadvantages:
 Unpleasant tasting
 Physician will prefer single drug tablets , capsules etc instead of preparation from plants
 High alcohol content

• Uses of Tinctures:
 Per oral e.g. Tincture of Ayrantii.
 Externally e.g. Tincture of Iodine.
 Inhalation e.g. Tincture of bezoin co.
 As flavoring agent e.g. Lemon tincture, compound cardamom tincture.
Storage of Tinctures:
• Because of high alcoholic contents ,tinctures must be tightly stoppered and not exposed
to excessive temperature
• Because the constituents found undergo a photochemical change , they must be stored
in light resistant container.
AROMATIC WATERS
• “Aromatic water is also called medicated water, defined in the USP as; clear, saturated
aqueous solutions of volatile oils or other aromatic or volatile substances.
• Concentrated aromatic waters also contain alcohol from 52 – 56 % v/v.

Preparation of aromatic waters:

There are four important methods which are mainly used;
1. Distillation
2. Solution method
3. Alternative solution method
4. From Concentrated Water(Dilution method

1. Distillation method:
• It is the old, the slowest and the most expensive method. Proportion of drugs in distillate
is different in different drugs. Example: Stronger rose water is prepared by distillation
process.
2. Solution method:
• Aromatic waters can also be prepared by the repeatedly shaking for 15 minutes.
(Certain volume/ amount for e.g. 2ml or 2g of volatile oil/ aromatic substance with
1000ml of water.)
• The resultant solution is set aside at least for 12 hours.
• Then filtered off the solution through wet filter paper. Example: Chloroform water,
Camphor water.
3. Alternative solution method:
• In this method aromatic water is prepared by thoroughly incorporating (about 15g
)talc or purified siliceous earth or pulped filter paper into the volatile oil.
• Purified distilled water (about 1000ml) is added and then whole is agitated for 10
minutes.
• Then filtered it off through wet filter paper.
• Filtering aid is provided to form a layer on filter paper to facilitate filtration.
• The treatment subdivide the oil particles, the finely divided oil rapidly dissolved to
form a saturated solution.
• Note: these incorporated agents are also called “distributing agents.”
From Concentrated Water :
• These products are alcoholic, non aqueous preparations containing 2% of volatile oils. They are 40
times stronger than the ordinary aromatic waters. Many volatile oils contain aromatic part and non-
aromatic part.
• The aromatic portion is much more soluble in a weak alcohol than the non-aromatic portion. Hence
when a solution of the oil in 90% alcohol is diluted with a limited amount of water the aromatic portion
of the oil remains in solution while the non-aromatic portion is precipitated off, separating as an oily
layer.
• Therefore 50 g of talc is added for 1000 ml of preparation, which acts as a distributing agent, and will
absorb the non-aromatic part. The solution is agitated and set aside for a few hours and filtered.
• Example: Concentrated waters dill, cinnamon, and caraway etc.
Storage of aromatic waters:
 Air tight container
 Light resistant container
 Non- alkaline
 Controlled Temperature
Uses of aromatic waters:
• Aromatic waters are pharmaceutical aid and used principally for perfuming and
flavoring the formulation.
• They can be used as an excipients or bases or vehicles for formulation of other
pharmaceutical preparations.
• Aromatic waters may be used for some special purposes like,
(a) Camphor water has been used as the vehicle in ophthalmic solutions owning to its ability to
contribute refreshing and stimulating effect to the preparation.
(b) Rose water has an antioxidant activity. The Rose water cleanses, tones and protects skin
from harmful environmental impacts.
(c) Hamamelis water known as witch hazel is employed as a rub, perfume and as an astringent
in various cosmetic preparations, particularly in after-shave lotions.
(d) Chloroform water has been used as preservative apart from its flavoring nature.