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DOSAGE FORMS

Lecture \ SECOND SEMESTER

PREPARATION 17: AROMATIC AMMONIA SPIRIT


NON AQUEOUS LIQUIDS • Example: 𝑁𝑎𝑁𝑂3 + Alcohol +
𝐻2 𝐻𝑆𝑂4 → Ethyl nitrite spirit
• Non-aqueous liquids’ major phase is not
4. Distillation
water
• Brandy- fermented juice of rice
• Sometimes the Non-aqueous phase still grapes
consists water • Whisky- fermented mash of wholly
• Non-aqueous liquids do not dissolve easily germinated malted cereal grain
with water (ex. Spirits)
SPIRITS PREPARATION 17: AROMATIC AMMONIA
SPIRIT
• “Essences”
• Clear, saturated, alcoholic (over 60% Category
alcoholic content) or hydroalcoholic • Spirit
Synonyms
solution (water+ alcohol) of volatile oil or
• Smelling salts
aromatic substance
Description of Final Product
• The active ingredient in spirit like aromatic
• It is a clear, yellow solution with a strong
water may be solid, liquid, or gas ammonia odor (sharp irritating odor/ very
• Most common spirit is the aromatic water. pungent odor)
• Used internally for their medicinal value. Use/s
• Used as flavoring agent (if they do not • It is used to treat and prevent syncope
contain medicinal value) (fainting)/ the loss of consciousness.
• Stored in tight light resistant container Formulation
(amber bottle) and in a cool place— in order Original Computed
to prevent evaporation and volatilization of Amount Amount
either the alcohol or the active principle. Ammonium 34.0 g 1.02 g
carbonate
PREPARATIONS FOR SPIRITS Strong ammonia 36.0 g 1.08 g
solution
1. Simple Solution
Lemon oil 10.0 mL 0.30 mL
• Mix the volatile substance with a
Myristica oil 1.0 mL 0.03 mL
solvent.
Lavender oil 1.0 mL 0.03 mL
• Example: 65 mL volatile oil/ 1000 mL
preparation Alcohol 700.0 mL 21.00 mL
2. Solution with Maceration Purified water, 1000.0 mL 30.00 mL
• Maceration- submerging of your plant qs ad
sample/ plant material in a suitable
solvent Computations
• Macerates leaves in water to extract
the water- soluble component.
3. Chemical Reaction
• It involves reactions of two solutes to
have a resulting product.

JLF 1
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 17: AROMATIC AMMONIA SPIRIT

Procedure
1. Dissolve ammonium carbonate in strong
ammonia solution and 6 mL of purified water
2. Agitate. Stand for 24 hours
3. In another container, dissolve all the volatile
oils in alcohol
4. Gradually add the mixtures (1 and 3) together
5. Add enough water to make 30 mL
6. Stand for 24 hours. Agitating occasionally
7. If turbidity occurs, filter it
Add water to final volume 30 mL
Label
• Red label
Container
• 30 mL amber bottle
Remarks
• Preserve in tight, light resistant container, at
a temperature not exceeding 30°C. During
inhalation, place a small amount of the spirit
between your fingers to but it. Approximately
4 inches away from the nostrils, inhale the
spirit.

JLF 2
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 18: IODINE TINCTURE


EXTRACTIVES DIFFERENT TYPES OF EXTRACTIVES
• Product prepared by extraction of drug with 1. Tinctures
suitable solvent • Alcoholic/hydroalcoholic solution
prepared from vegetable or animal
Extraction drug or from chemical substance
• process of removing the active constituents • Concentration:
from a solid or liquid by means of a suitable 10-20 % potency (10-20g solute/ 100
solvent mL solvent)
• Process • They contain less than 50% alcohol
o Percolation- downward movement of content
liquid, slowly passing through a filter • Different Processes in the
o Maceration- submerging the solute; Preparation of Tinctures
submerging of plant sample in a o Simple Solution
solvent wherein you allow it to stand → Mix two solutions
for a specified time with frequent together
agitation → Ex: Iodine Tincture
o Digestion- type of maceration; with o Percolation
the aid of gentle heat during → Ex: Belladona Tincture
submerging the sample into the o Maceration
solvent → Ex: Sweet Orange
o Infusion- “blanching”; type of Peel Tincture
maceration; addition of hot water/cold • Storage of Tinctures
water o It should be stored in a tight
o Decoction- boiling for 15 minutes; light resistant container (or
used in extraction of tea amber bottle) to avoid
Extract exposure to direct sunlight
• Product in extraction and excessive heat
• 2 to 6 times more potent than crude drug o Remember that tinctures
• Three types of Extract: contains alcohol which
1. Semi liquid- has a syrupy consistency evaporates easily
due to the 20 mL solvent left 2. Fluid Extract
2. Pilular- solid extract; occurs in plastic • Very concentrated extract
mases, all solvent has been evaporated • Concentration: 1g/mL (100%
(no moisture content) concentration)
3. Dry Powder- powdered extract • Alcohol is the solvent
Example: Starchy drugs- Cassava starch,
• 100% tincture
raddish starch
• Potent, too bitter tasting (due to high
content of plant material)

JLF 1
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 18: IODINE TINCTURE


• Different Processes in the Formulation
Preparation of Tinctures Original Computed
o Percolation Amount Amount
→ Downward movement Iodine crystal 20 g 0.30 g
of the sample Sodium Iodide 24 g 0.36 g
→ Process A Alcohol 500 mL 7.50 mL
Resulting extract is Purified water, 1000 mL 15.00 mL
ready for assay qs ad
→ Process D
Hot water as Computations
menstruum (in order to
submerge the plant
material)
→ Process E
The use of longer/
narrower percolator.

PREPARATION 18: IODINE TINCTURE


Procedure
Category 1. Dissolve NaI in small amount of water
• Topical Tincture (Solution 1)
Synonyms 2. Add I2 crystal in alcohol (Based on the
• Tincture of Iodine, Tinctura Iodi, Soluto Iodi, computed amount of alcohol; Solution 2)
Spiritucae Weak Solution of Iodine 3. Mix together Solution 1 to 2.
Description of Final Product 4. Add enough purified water to complete the
• The tincture has a reddish brown color which volume of 15 mL.
produce stain on the skin Label
Use/s • Red Label
• This is a popular local anti-infective/ anti- Container
microbial agent applied topically to the skin • 15 mL amber bottle
in general household first aid procedure. It is Remarks
also used as germicide and fungicide. • The method of preparation used was simple
solution. The alcohol used was 49% diluted
alcohol. Sodium iodide acted as a solubilizing
agent of the poorly solubilized iodine crystal.
It should be stored in a tight container to
prevent the loss of alcohol

SPECIAL NOTES
Sodium iodide
• Solubilizing agent (increase solubility of the
iodine crystals)

JLF 2
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 18: IODINE TINCTURE


• Used to stabilize the tincture and make it
miscible with water in all proportions
• Prevents the formation of ethyl iodide
• Helpful in this formulation, instead of reacting
with alcohol, your I2 crystals will react with
NaI to increase its solubility rather than
reacting with your alcohol to produce Ethyl
iodide

Iodine
• NaI will react with I2 to form NaI3 thus, I2 will
not react with alcohol, ethyl iodide, aldehyde,
and hydrogen iodide.
Ethyl iodide
• Ethyl iodide will decrease the activity of the
iodine
• Without NaI, Iodine will only react with ethyl
alcohol and it will produce your ethyl iodide
• Ethyl iodide decreases the bacteriostatic
activity of your Iodine
• If hydroiodic acid was formed, the solution
would be moved when applied to wounds

JLF 3
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 19: CAMPHORATED SOAP LINIMENT


NON-AQUEOUS LIQUIDS FACTORS THAT AFFECT THE SELECTION OF
VEHICLE
• Refers to the preparation where the solvent
used is not water 1. Desired Action
• Ex: Alcohol (plain alcohol), hydroalcoholic • How will you use the liniment?
solutions (water + alcohol) 2. Solubility of the component in various
• When we use a hydroalcoholic preparations, solvents
the substances that is being dissolved in the • The solubility of the substances or
HA solution, will have faster solubility than the solute must be considered in
dissolving it in water or alcohol alone the preparation of the liniment
• The substance must be dissolved
LINIMENTS in the vehicle
TYPES OF LINIMENT ACCORDING TO THE
• From latin “linere”- to anoint
VEHICLE USED
• Solution or mixture of various substance in
oil, alcoholic solution of soap or emulsion 1. Alcoholic Liniments
intended for external application • Vehicle: Alcohol
• One of the vehicle used is oil • Desired Action: Intended generally
• Applied with friction and rubbing/ massaging for their rubefacient, counterirritant,
to the affected area and that is why they are mild astringent, and penetrating
called “embrocation” effect.
• The oil and soap base provides ease of • Rubefacient- substance for topical
application and massage application; cause irritation then
• Not intended to be applied in broken produces redness to the skin.
skin/wounds/ bruised skin, because there is a - Causes irritation because of the
tendency of excessive irritation dilation of the capillaries and
• They should be stored in a tight container increase in blood circulation
• Counter irritant- produce irritation or
discomfort that can now divert the
attention from another
- agent applied locally to produce
superficial inflammation with the
object of reducing inflammation in
deeper adjacent structures
• Mild astringent- tightens pores
• Penetrating effect- they penetrate to
the deeper parts of the skin
• Alcoholic liniments penetrates the
skin readily than the oil base because
it is not as thick as the oil base.

JLF 1
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 19: CAMPHORATED SOAP LINIMENT


2. Oily Liniments
• Vehicle: Oil Computations
• Milder in action but are more useful
when massage is desired
• Used as protecting coating depending
on the ingredient in the preparation
and it should not be applied on
bruises and broken skin
• The solvent may be fixed oils (almond
oil, peanut oil, sesame oil, or
cottonseed oil) or volatile oil
(wintergreen oil, turpentine oil) or
combination of the two
• Volatile oil- liquids that easily
evaporates; do not stain
Procedure
• Fixed oils- produces stain 1. Dissolve camphor and rosemary oil in alcohol

PREPARATION 18: CAMPHORATED SOAP


LINIMENT
Category
• Alcohol based liniment
Synonyms • Since camphor is an organic compound and
• Linimentum camphores El saponis, Soap rosemary oil is an oil, it is soluble in alcohol.
Liniment, Liquid Opadel doc
Description of Final Product 2. In a separate container, dissolve grated soap
• Clear, colorless to yellow solution. It has odor in 9 mL purified water
of camphor (naphthalene balls)
Use/s
• This is products used as rubefacient. It has a
counterirritant effect and it has better
penetration. It is also used as local anesthetic
for sprain and rheumatism
Formulation
Original Computed
• Soap is a water soluble substance
Amount Amount
Camphor 45 g 1.35 g 3. Mix the 2 solution and allow it to stand for 24
Soap 60 g 1.80 g hours in a cool place
Rosemary oil 10 mL 0.30 mL
Alcohol 700 mL 21.00 mL
Purified water, 1000 mL 30.00 mL
qs ad

JLF 2
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 19: CAMPHORATED SOAP LINIMENT

• The solution must be set aside for 24


hours to ensure complete saturation

4. Filter and add water to complete volume (up


to 30 mL)

• The solution must filtered to prevent


turbidity
Label
• Red Label
Container
• 15 mL amber bottle
Remarks
• The method of preparation used was simple
agitation without the aid of heat.
• Official hand soap should be used.
• Warning: If soap made from animal oils are
used gelatinization will occur

JLF 3
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 20: MINERAL OIL EMULSION


EMULSION b. Vegetable –
acacia,
1. Two phase system in which one liquid is
tragacanth,
dispersed in the form of small globules
Chondrus, pectin,
throughout another liquid in which it is immiscible.
2. One immiscible liquid is intimately dispersed in carrageenan
another liquid in droplets. Two immiscible liquid • Synthetic
is added, particularly oil and water. a. Finely Divided
Solid – Mg(OH)2
(magnesium
hydroxide),
Al(OH)3
(aluminum
hydroxide), and
Magnesium
trisilicate
b. Colloid – Kaolin,
bentonite magma
c. Anionic – SLS
(sodium lauryl
sulfate)
d. Cationic –
Benzalkonium
3 COMPONENTS OF EMULSION chloride
e. Non-ionic – PEG
1. Dispersed liquid – smaller amount 400, Spans and
a. Internal phase Tween
b. Discontinuous phase (Polysorbate)
2. Dispersion medium – liquid vehicle in larger f. Amphoteric -
amount Lecithin
a. External phase b. Dispersing or Stabilizing agent
b. Continuous phase
3. Intermediate agent – also referred to as TYPE OF EMULSION
emulsifier or molecules that have two different
ends which are the head that forms a chemical 1. Simple – O/W – used internally; W/O
bond with water (hydrophilic – water loving), a. Oil in Water - oil – internal phase while
while the tail (hydrophobic – water hating) forms water – external phase ; preparation in
a chemical bond with oil but not with water. this type are used internally
a. Emulsifying agent b. Water in Oil – water is the dispersed
Type of Emulsifying Agent: phase while oil is the dispersion medium;
• Natural this simple type of emulsion are
a. Animal – gelatin, macroemulsions (with particle size
egg yolk, casein, from 1-100 mm) and the appearance is
woolfat, opaque.
cholesterol

MEL 1
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 20: MINERAL OIL EMULSION


Particle size: [100-1000 A (1A = 0.1 nm)]
*Meaning that 1000 A is equivalent to 100 nm.

METHOD OF PREPARATION
1. Wet or English Dictates the nature
Of emulsion (O/W
or W/O)
2. Dry gum or Continental
External phase – contains larger amount
Primary nucleus – the similarity of both
Internal phase – contains smaller amount
methods are they are prepared in one direction
2. Multiple
(e.g., clockwise trituration method all throughout
a. O/W/O (oil-water-oil)
the procedure with the aid of mortar and pestle),
• Contains both oil in water
creamy, sticky mixture with cracking sound. Both
and water in oil type and
preparations are considered good by using the
this requires use of at
ratio, 4:2:1 (4 parts of Oil, 2 parts of Water: 1 part
least two surfactants or
of Emulsifying Agent).
two emulsifying agents in
order to stabilize the
English method – uses an emulsifying agent
system.
but you have to add water first to form mucilage.
• One with a low Consequently, the oil is slowly incorporated to
hydrophilic-lipophilic
form the emulsion.
balance for the HLB value
of the emulsifying agent to Dry gum method – the emulsifying agent
stabilize the primary water
(acacia) is mixed with the oil before the addition
in oil type of emulsion. of water.
• And the other stabilizing
agent for the system is 3. Bottle or Forbes Volatile oil (2:2L2 – done
with high HLB value to by shaking vigorously). The emulsion is
stabilize the secondary oil prepared directly in the container itself.
in water type.
b. W/O/W (water-oil-water) The emulsifying agent (acacia) is mixed with the
• Contains both water in oil oil before the addition of water. A portion of 2
and oil in water type of the parts of volatile oil is added with 2 parts of water
simple emulsion. and 1 part of emulsifying agent.
• Also requires the use of
two emulsifying agents in
order to stabilize the
system.
3. Microemulsion
a. thermodynamically stable – separation
won’t happen even in the long period of
time, thus it is the most stable of the three
b. dispersed phase is in very small globules
c. has an appearance of transparent

MEL 2
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 20: MINERAL OIL EMULSION


PROBLEMS ENCOUNTERED IN PREPARING METHOD OF IDENTIFYING EMULSION
EMULSION (Based on Stability)
1. Drop Dilution Test – add water (drop)
1. Creaming • Homogenous -> O/W
• temporary separation of the 2 phases -> • The emulsion is diluted with oil or water
shake again (that once it is shaken, it will • If the emulsion is O/W, it is diluted with
disperse again the globules into the water and it will remain unchanged or
dispersion medium) stable (since water is the dispersing
• Aggregates of globules of the internal medium meaning O/W emulsion can
phase that rise to the top before it falls to easily be diluted with an aqueous
the bottom of the emulsion. solvent; but if its diluted with oil, the
• Referred as an upward creaming and emulsion will break since oil and water is
downward creaming. not miscible with each other)
2. Cracking or Breaking • If the emulsion is W/O, it is diluted with
• Total separation of the 2 phase (two oil and it will remain unchanged or stable
immiscible liquids) with coalescence since oil will remain dispersed all
• The protective sheet around the globules throughout the preparation. However, if
are completely destroyed and the oil water is added, there will be separation
tends to coalesce. of the layer.
• Cracking and coalescence are examples
of irreversible process - no matter how
much shaking, it will not return into a good
emulsion
• Coalescence – process in which 2 or
more droplets merge together to form a
single large droplets
• Flocculation – is the process wherein
the disperse particle come together but
does not fuse (will not form into large
globules)– when shaken it will still be
considered as good emulsion
3. Phase inversion 2. Dye Solubility Test
• Evaporation of water; change of water • Oil soluble -> Sudan red -> W/O
from Oil in Water to Water in Oil due to o In an oil soluble dye when Sudan
evaporation Red is used and the continuous
• If there is an evaporation in: phase appears red then it is W/O
• O/W type – the amount of water in the type (since Sudan red is oil
dispersion medium lessens and that soluble so it will be dispersed in
water become the dispersed phase the continuous phase which is the
because the amount of water is smaller oil).
than that of the oil. Making the oil the • Water soluble -> Amaranth green ->
dispersion medium. Then, transforming O/W
into the W/O type. o In this test, an emulsion is mixed
with water soluble dye and
observed under the microscope

MEL 3
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 20: MINERAL OIL EMULSION


o If the continuous phase appears florescence (since oil can absorb UV
red, the emulsion is O/W (since light).
water is in the external phase and • O/W - If an emulsion upon exposure to
the dye will dissolve in it) UV radiation shows only spotty
o If the globules appears to be red, fluorescence then the type of emulsion is
then the emulsion is W/O type oil in water type (right picture)
because the dispersion medium
now is colorless.

3. Electric Conductivity Test


• Water conduct electricity -> O/W
o In an assembly: a pair of electrons
PREPARATION 20: MINERAL OILEMULSION
is connected to electric bulb and
the electron is dip into an I. Category
emulsion • Oral emulsion
o If the emulsion is O/W type, the II. Synonyms
test will be positive (electric bulb • Liquid petrolatum emulsion
glows since water is the III. Description of Final Product
dispersion medium and it • It has a whitish yellow color
conducts electric current). IV. Use/s
o If the emulsion is W/O type, the • The emulsion is employed as a
test will be negative (will not lubricating cathartic (substances that
glow since oil is the dispersion soften stool/feces and the intestinal wall)
medium and does not conduct with a usual dose of 30mL
electric current). V. Formulation:
Ingredients Original Computed
Amount Amount

Mineral Oil 500 mL 15 mL

Acacia 125 g 3.75 g

Syrup 100 mL 3 mL

Vanillin 40 mg 1.2 mg

Alcohol 60 mL 1.8 mL
4. Fluorescence Test
• Oil can absorb UV light -> W/O Purified 1000 mL 30.00 mL
water, qs ad
• W/O - If an emulsion upon exposure to
UV radiation shows a continuous

MEL 4
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION 20: MINERAL OIL EMULSION


VI. Computation • Alcohol as a preservative
• The emulsion is much more palatable
than the unemulsified oil.

VII. Procedure
• Dry gum
i. Triturate mineral oil
ii. Add emulsifying agent in portion
and triturate
iii. Add water and triturate
iv. Add syrup in portion in trituration
v. Add vanillin, previously dissolved
in alcohol, in portion with
trituration
vi. Add enough water to 30mL
• Wet gum
i. Triturate emulsifying agent
ii. Add water (all at once) and
continue triturating
iii. Add oil in portion with trituration
iv. Add syrup in portion with
trituration
v. Add vanillin previously in portion
dissolved in alcohol in portion with
trituration
vi. Add enough water to make 30mL
VIII. Label
• White label with shake well
IX. Container
• 30mL wide mouthed amber bottle
X. Remarks
• Mineral oil as cathartic
• Acacia as a suspending or an
emulsifying agent
• Syrup as sweetening agent
• Vanillin as a flavorant

MEL 5
DOSAGE FORMS
Laboratory \ SECOND SEMESTER

INTERACTIVE ACTIVITY ON PREPARATION 17-20


1. Spirit is a clear, saturated, alcoholic, or · Maceration – usually submerged for 36 to 72
hydroalcoholic solution of a volatile or aromatic hours
substance. · Digestion – heating at low temperature
· Infusion – commonly used in tea bags
Ans: True · Decoction – boiling for 15 minutes

· Volatile oil/Aromatic substance (solute) 5. Tinctures have 100% potency.


Ans: False
Nature of Volatile oil:
o They evaporate quickly. · Tinctures – 10-20%
o Has an odor · Fluid extracts – 100%
o Dosage form that contains a volatile · Both are hydroalcoholic/alcoholic.
oil/aromatic substance: aromatic water · To achieve 100% potency, allow it to
completely evaporate. 1:1 ratio. No more
Difference between spirits and aromatic water solvent present.
as to solvent:
o Water as the solvent for aromatic water 6. Percolation process that uses hot water as
o Alcohol as the solvent for spirits or a menstruum.
combination of alcohol and water. A. Process A
B. Process D
· Hydroalcoholic C. Process E
o Water + alcohol = hydroalcoholic D. None of the choices
o There are substances wherein they
are soluble in water and in alcohol. 7. What is the use of Iodine Tincture?
o Has the ability to extract more Ans: Local anti-infective, germicide,
substance fungicide
· Spirit and aromatic water are same in terms
of solute but different in solvent. · Anti-infective
· Saturated o Against germs and fungi
o Maximum amount of solute dissolved · IDE – directly kill. Germicidal.
in maximum solvent · Static – stop the growth

2. Produce from fermented juice of ripe grapes.


Ans: Brandy 8. it can decrease the bacteriostatic activity of
Iodine Tincture.
3. It is used to treat and prevent syncope. A. Ethyl Iodide
Ans: Aromatic Ammonia Spirit B. Iodine
C. Sodium Iodide
4. It is a process with aid of gentle heat. ● Prevents the action of iodine as
A. Maceration bacteriostatic agent: Ethyl iodide
B. Digestion ● Iodine - anti-infective
C. Infusion
D. Decoction 9. Liniments are applied with friction and rubbing
to the affected area.
● Liniment - to anoint
● Referred as “embrocation”

GT, CJO, EFL


DOSAGE FORMS
Laboratory \ SECOND SEMESTER

INTERACTIVE ACTIVITY ON PREPARATION 17-20


10. Oily Liniments - liniments that are milder in 12. Three (3) components of Emulsion:
their action but are more useful when massage is 1. Dispersed Liquid
desired. 2. Dispersion Medium
● Oily liniments are desired when massage is 3. Intermediate Agent
desired because of its greasy character.
● Alcoholic liniments are intended mainly as ● Dispersed Liquid - referred to as “internal
rubefacient, counterirritant, and mild phase” or “discontinuous phase”
astringent. ○ Little amount
○ Also has a penetrating effect to the ○ Can be in liquid or oil form
skin than the oil-based ● Dispersion Medium - referred to as
● Oily liniments are used as protective coating. “external phase” or “continuous phase”
○ Not to be applied with bruises and ○ Greater amount as compared to
wounds. dispersed liquid
● Fixed oils or volatile oils are used as ○ Cannot be in liquid or oil form
solvents in oily liniments. ● Intermediate agent - referred to as
“emulsifying agent” or “dispersing agent” or
11. Uses of Camphorated Soap Liniment: “stabilizing agent”
1. Rubefacient ○ Binds dispersed liquid and dispersion
2. Counterirritant medium
3. Local anesthetic for sprain and rheumatism ○ Hydrophilic head, hydrophobic tail

● Rubefacient - substances applied topically 13. Natural or Synthetic Emulsifying Agent


(with local effect) that produces redness of a. Acacia: natural – vegetable origin
the skin which will cause dilation of the b. Benzalkonium chloride: synthetic
capillaries and increases blood circulation –cationic
○ When blood circulation increases, c. Egg Yolk: natural; animal origin
pain will be relieved in the site of d. SLS (Sodium Lauryl Sulfate): synthetic
application. – anionic
○ Pain will only be relieved when e. Magnesium: synthetic – finely divided
capillaries dilate and blood circulation solid
increases.
● Counterirritant - substance that produce 14. Method of preparation that uses volatile
local action with irritant effect on the site as oil in a 2:2:1 ratio
to where you applied the preparation
○ Intended to relieve the irritation in Answer: c. Bottle method
another part.
● Local anesthetic - anesthetic effect will only
be in the site of application

GT, CJO, EFL


DOSAGE FORMS
Laboratory \ SECOND SEMESTER

INTERACTIVE ACTIVITY ON PREPARATION 17-20


● Bottle method: uses the 2:2:1 ratio, ● Phase inversion -instability of the emulsion
wherein 2 parts oil, 2 parts water, and 1 part wherein oil-in-water type turns to
of emulsifying agent are used. water-in-oil type.
● Both wet and dry methods follow the 4:2:1
ratio wherein 4 parts of oil, 2 parts of water,
and 1 part of emulsifying agent are used.
● Home-based ingredients: oil (10mL), water
(10mL), egg yolk (5mL)
● In Forbes Bottle method, volatile oil is
being utilized.
● In Wet method, water is added first to the
gum, followed by the oil that is added portion
by portion.
● In Dry method, oil is added first to the gum,
Home-based Experiment
followed by the water that is added all at
once. Notes:
● On bottle:
15. Problem of emulsion with a temporary - Use flint wide mouth bottle
separation of the 2 phases - Specimen bottle can be used
- Don’t use jar
Answer: a. Creaming - Use 30 or 60mL bottle to provide space
on shaking, but the total amount of the 3
● Creaming has two types: ingredients will be 25mL (To make
- Upward creaming: globules rise to the 25mL)
upper surface; happens when oil is less ● On oil:
dense than the water - Use ordinary oil if volatile oil is not
- Downward creaming: globules are in available (label as oil only)
the lower portion; happens when oil is - If ordinary oil is used, shake it longer
denser than the water - Scented oil can be used
● Creaming is a reversible process. Since two ● Home-based Experiment Title: DIY Emulsion
or more globules are not fused into one
larger unit, cream can be easily re-dispersed
(into good emulsion) by agitation.
● In cracking and breaking, total separation
of 2 layers occurs.
● Coalescence - fusion of globule that result
in the formation of large clumps of globules.

GT, CJO, EFL


DOSAGE FORMS 619
Laboratory \ SECOND SEMESTER

PREPARATION 21: CHALK MIXTURE

MIXTURES V. Formulation
• Aqueous liquid preparation which contains which Precipitated chalk 60 g 0.9 g
lesson (Insoluble solid)
contains suspended (suspensoid) insoluble solid
substances. Glycerin 100 mL 1.5 mL
• Aqueous liquid preparation means that the (Viscosity modifier/
thickening agent; ensures
dispersing medium is water.
that precipitated chalk
• The insoluble substance maybe help in suspension remain suspended in the
by the use of suitable suspending or thickening agent mixture)
(aka viscosity modifying agents) since the insoluble Cinnamon water 400 mL 6 mL
substance does not make the mixture very viscous. Purified water, qs ad 1000 mL 15.0 mL

INSOLUBLE SUBSTANCES
• Should be in very finely divided state and it must be Computations
lesson
uniformly distributed throughout the preparation. 60 𝑔 𝑥
𝑃𝑟𝑒𝑐𝑖𝑝𝑖𝑡𝑎𝑡𝑒𝑑 𝑐ℎ𝑎𝑙𝑘 = =
• The particle size shouldIN
be adequately reduced 1000 𝑚𝐿 15 𝑚𝐿

• Accomplished by the use of colloid mill, special 𝑥 = 0.9 𝑔


methods of precipitation and suspending agent 100 𝑚𝐿 𝑥
𝐺𝑙𝑦𝑐𝑒𝑟𝑖𝑛 = =
1000 𝑚𝐿 15 𝑚𝐿
Reasons for having the insoluble substance in a finer 𝑥 = 1.5 𝑚𝐿
state of subdivision: 400 𝑚𝐿 𝑥
• Enables the insoluble substance to become more 𝐶𝑖𝑛𝑛𝑎𝑚𝑜𝑛 𝑤𝑎𝑡𝑒𝑟 = =
1000 𝑚𝐿 15 𝑚𝐿
active as adsorbents and protectives while in contact 𝑥 = 6 𝑚𝐿
with inflamed areas or surfaces
• Suspended more readily and settle out slowly.
Hence, it will ensure that there will be uniform doses VI. Procedure:
of suspended particles. 1. Triturate the calcium carbonate (chalk)
• Increase palatability with the use of colloidal with 5mL water.
suspending agent. i. Amount of purified water in the
first step is dependent on the
PREP 21: CHALK MIXTURE desire volume of the
I. Category: Medicated Mixture preparation.
lesson ii. 5mL is good for 15 mL chalk
II. Synonyms: Mixture de Creta, Mistura Cratae
III. Description of Final Product: A whitish mixture mixture.
containing suspended, insoluble solid 2. Add glycerin (thickening agent/viscosity
substance. modifier) and levigate.
IV. Use/s: This is used as antacid and atidiarrheal 3. Add cinnamon water and triturate.
agent. 4. Transfer mixture in a graduated cylinder
5. Wash mortar with purified water, add
washings to the cylinder.

SURNAME/S 1
DOSAGE FORMS 619
Laboratory \ SECOND SEMESTER

PREPARATION 21: CHALK MIXTURE

• To ensure that all the mixture


has been obtained from the
mortar.
6. Add enough water to complete the
volume.
VII. Container: Flint bottle
• Volume/size should be suitable to the
amount prepare
• 15mL chalk mixture = 15 mL flint bottle
VIII. Label: White label with shake well
• Orally taken
• There are insoluble solid substances
dispersed or suspended in the mixture
so the patient should shake the
preparation first before taking the drug
to ensure that the suspensoids are
uniformly distributed throughout the
preparation.
IX. Remarks: The method of preparation used was
simple hydration. Glycerin is used as a viscosity
agent/modifier or thickening agent.
• Glycerin increases viscosity of the
preparation.

SURNAME/S 2
DOSAGE FORMS
Lecture \ SECOND SEMESTER

PREPARATION
Preparation22:
22:ALUMINUM HYDROXIDE
Aluminum H droxide GelGEL

GELS
Ge layer. It affects both red and blue
I Introduction
d ci litmus paper slightly but is not
Suspension, in a water medium of reddened by phenolphthalein.
insoluble drugs in hydrated form U e/ :
wherein, the particle si e It is used primarily as an antacid,
approaches or attain colloidal knowing it contains hydroxide,
dimension (without systemic alkalosis) in the
Thixotrophy - displaced higher management of hyperacidity, peptic
viscosity in a semi solid state on ulcer, gastritis and esophagitis. It is
standing and become low viscous also used as skin protectant and
liquid upon agitation. mild astringent. May cause
If undistributed for some time, they constipation.
may become semisolid or gelatinous
with some small amount of water FORMULATION:
separating on standing, if
distributed/shaken/ agitated, they ORIGINAL COMPUTED
Original Computed
liquefy AMOUNT Amount
Amount AMOUNT
Very fine particle si e- in colloidal
dimension, to achieve large surface Ammonium 800 g 212g g
and thus maximum adsorption alum
capacity
Sodium 1000 g 15 g
May contain peppermint oil, glycerin, Carbonate
sorbitol, sucrose, saccharin or other
suitable flavor and preservative in a Peppermint 0.01%0.01 (0.01
0.01% % 0.01%
0.003 g
total amount of not exceeding 0.5% oil g / 100 mL) (0.003 g)

Sodium 0.1% (0.1 g 0.1%


0.03(0.03
g
Pe aai 22: A i
PreparationH22:
d ide Ge 0.1%
0.1 %
ben oate / 100 mL) g)
A Aluminim
i HHydroxide
d Gel
ide Ge
Ca eg : Purified 2000 mL 30 mL
Medicated gel water, qs ad
S :
Colloidal Aluminum Hydroxide; Pe e i i : suspending agent
Amphojel; Alternagel S di be a e: preservative
De c i i f Fi a P d c : Wa e : vehicle
This preparation is a white, viscous S di ca b a e: produces hydroxide
preparation from which a small A i a : can cause constipation
amount of water may be separated
on standing. It is translucent in a thin
___________________________________________________________________________
-
JDML 11 1
DOSAGE FORMS
Lecture \ SECOND SEMESTER

Preparation
PREPARATION 22:22: AluminumHYDROXIDE
ALUMINUM H droxide Gel
GEL

8. Suspend residue in 30mL purified water


C ai : flavored with peppermint oil and preserve
with sodium ben oate
9. Homogeni e resulting gel

Labe :
White label with shake well note to
attain uniform content
C ai e :
60mL wide mouth amber bottle
Re a k :
The method of preparation used was
Here is how tha Hydroxide produced: chemical reaction. It produces no
systemic alkalosis.
Aluminum compounds decrease the
From the sodium carbonate, put it in a hot absorption of certain drugs because
60 mL water to reproduce Sodium they form a Kelate with other metals
Hydroxide plus Carbon dioxide. like antibiotics - tetracycline.Also, it
decreases the adsorption of
P ced e aluminum compounds when you
1. Calibrate final bottle to 30mL take the product because it contains
2. Dissolve sodium carbonate in 60mL hot Calcium. Do not eat metal products
water & filter; as this preparation is together with dairy products.
suspension, therefore, there will be a lot of It also interferes with the deframing
insoluble substances in the gel. So, Sodium action of simethicone.
carbonate will become Sodium hydroxide in These compounds are also
the making. constipating. Sodium ben oate is
3. Dissolve alum in 30mL of hot water used as a preservative.
4. Filter the alum solution in the carbonate
solution
5. Add 60mL hot water with stirring to allow
gas / Carbon dioxide escape from the
solution for 5 minutes.
6. Dilute to 1200mL with cold water. Stand.
Decant
7. Filter and wash residue with 10mL cold
water

-
___________________________________________________________________________

JDML 21 2
DOSAGE FORMS 619
Laboratory \ SECOND SEMESTER

PREPARATION 23: CALAMINE LOTION

LOTION 𝑍𝑛𝑆𝑂4 + 𝑆𝑢𝑙𝑓𝑢𝑟𝑎𝑡𝑒𝑑 𝑃𝑜𝑡𝑎𝑠ℎ (𝐾2 𝑆3 )


→ 𝑍𝑛𝑆 + 2𝑆 + 𝐾2 𝑆𝑂4
• Liquid suspension or dispersion intended for
3. Clear Solution – in which the active ingredient is
external application to the body
a water soluble substance
• Can also be used for the topical delivery of
Example: Dimethisoquin hydrochloride lotion
medication such as antibiotics, antiseptics,
antifungals, corticosteroids anti-acne agents, PREPARATION 23: CALAMINE LOTION
soothing and protecting agents such as I. Category: Medicated suspension
acrylamide. II. Synonyms: Lotio Calaminae
• Many medicated shampoos are lotions; lotions III. Description of Final Product: A liquid
have an advantage that they be spread thinly as suspension or dispersion that is pink in color
compared to the previous formulation (like IV. Use/s: This is employed chiefly as an
creams and ointment) astringent, antipruritic, topical protectant
• They may economically cover a larger area and soothing lotion for sunburn, treatment
compared to creams and ointments for ivy poisoning, etc. It is often prescribed
• Applied without friction by dermatologist to give opacity and a flesh
• Insoluble matter are finely divided as particles like color to lotions, skin protectant.
approaching colloidal dimension (too small) are V. Formula
more soothing to inflamed areas & are more Original Computed
effective in contact with the infected area Ingredient Function
Amount Amount
• Can carry medications, can be the vehicle for Calamine 80 g 2.4 g Skin Protectant
medications Zinc Oxide 80 g 2.4 g Skin Protectant
• Lotions are preferred over semi-solid Humectant
Glycerin 20 mL 0.6 mL
preparation because of non-greasy character (moisturizing agent)
(compared to cream and ointment) and their Bentonite Stabilizer and
250 mL 7.5 mL
increased spreadability over large areas of skin. Magma Suspending Agent
Calcium Vehicle (contains
METHOD OF PREPARATION Hydroxide, 1000 mL 30.0 mL astringent
1. Triturating the ingredient to a smooth paste qs ad properties)
and then cautiously adding the remaining liquid
phase (with the use of high speed mixers & VI. Computation
homogenizers)
Example: Calamine Lotion – consist of finely
divided insoluble solids held in more or less
permanent suspension by the presence of
suspending agents/or surface active agent.
2. By chemical interaction in the liquid
Example: White lotion – must be freely
prepared & does not contain suspending agent

KDP 1
DOSAGE FORMS 619
Laboratory \ SECOND SEMESTER

PREPARATION 23: CALAMINE LOTION

VII. Procedure
1. Dilute bentonite magma with an equal
volume of calcium hydroxide topical
solution
2. Mix calamine and zinc oxide alternately
with glycerin to form a smooth paste
3. Add 7.5mL of diluted magma
4. Triturate and add the remaining magma
5. Add enough calcium hydroxide topical
solution to complete volume
VIII. Label: Red Label with shake well
IX. Container: 15 mL plastic prescription bottle
with sufficient room to able vigorous
shaking.

KDP 2
DOSAGE FORMS 619
Laboratory \ SECOND SEMESTER

PREPARATION 24: CAPTOPRIL SUSPENSION

SUSPENSION PHA 619


SAMPLE SCENARIO
• is a liquid preparation wherein solid particles are • Assume that the prescription is 300 mcg/kg t.i.d
lesson
dispersed throughout a liquid phase. • Give enough for 10 days.
• Usually used if the active ingredient is not stable in a • Patient’s weight = 66 lbs.
solution • Average weight of the 6 tablets of Captopril = 1,284
• can be further defined as a preparation that mg
contains finely broken down drug particles V. FORMULATION
(suspensoid) with a uniform distribution throughout Captopril tablet 270 mg (1156 mg
a vehicle in which the drug displays a minimum crushed 50 mg tabs)
degree of solubility. Cherry flavorant 2 mL
Disodium edetate 150 mg
Simple syrup, q.s ad 150 mL
CHARACTERISTICS OF A GOOD
SUSPENSION NSIO
VI. COMPUTATION
• lesson
The suspended particles should not settle rapidly
and sediment produced must be easily re-
suspended by the use of moderate amount of
shaking.
o So that the patient will get a uniform
dose when taking a suspension.
• Easy to pour yet not watery and no grittiness.
• Pleasing odor, color, and palatability.
• Physically, chemically, and microbiologically stable.
• Parenteral/ophthalmic suspension should be
sterilizable.

PREP 24: CAPTOPRIL SUSPENSION


I. Category : Suspension
II. Synonyms : N/A (Since Captopril is a generic
name, it doesn’t have synonyms. But it has
brand names such as Capoten)
III. Description of Final Product : Clear,
colorless syrup suspension
IV. Use/s: Captopril is intended for the
treatment of essential hypertension; It is
also indicated for chronic heart failure.

JNL 1
DOSAGE FORMS 619
Laboratory \ SECOND SEMESTER

PREPARATION 24: CAPTOPRIL SUSPENSION

VII. PROCEDURE PHA 619


1. Weigh six tablets of Captopril (50 mg).
2. Crush the six tablets in a mortar and weigh
1,156 mg of this crushed tablet powder.
3. Place the weighed tablet powder in a clean
mortar.
4. Weigh 150 mg of disodium edetate and place it
in the mortar.
5. Add small amounts od purified water to
moisten the powder.
6. Slowly add approximately 20 mL of syrup to the
mortar with trituration.
7. Transfer the mixture to a 6-ounce prescription
bottle that has been pre-calibrated to 150 mL.
8. Rinse out the mortar using the simple syrup and
transfer the remainder to the prescription
bottle. Add 2 mL of the cherry flavoring agent
until the solution reaches the calibration mark
on the bottle with simple syrup.
9. Label the bottle and dispense.

VIII. Label: White with “Shake well before use”


IX. Container: Narrow mouth amber bottle

Notes:

Captopril tablet

• Active ingredient

Cherry flavorant

• Flavoring agent

Disodium edetate

• Used as a stabilizer
• Needed in doing liquid preparations

Simple syrup

• Vehicle

JNL 2

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