First Lecture

Dr. Riham ElGogary, PhD.

Lecturer of Pharmaceutics and
Industrial Pharmacy

1
 What is Pharmaceutics?
 It is the area of pharmacy that deals with the
process of turning a drug into medicine, this
medicine should be safe, convenient, effective
and produces a reproducible response
 It is the science of dosage form design
 Routes of drug administration

1) Mouth (oral)
Tablets/capsules/ 2) Rectal 3) Inhalation
Oral powders/solutions/ Suppositories/enemas
syrups/suspensions

5) Topical
4) Injection (Parenterals) Ointments/creams/lotions/dusting
IV,IM,SC ampoules or vials powders/gels
 What are dosage forms
and why do we need them?
1- For the protection of a drug from the destructive influence
of oxygen or humidity

2- For the protection of a drug from the destructive influence

of gastric acid after oral administration (e.g. enteric coated
tablets)

3- To conceal the bitter, salty or offensive taste or odor of a

drug (using capsules, coated tablets, flavored syrups)

4- For topical drug administration (e.g. ointments, creams,

transdermal patches, ophthalmic, ear/nasal)
 Cont.
5- For time controlled drug action (controlled release
tablets, capsules, suspensions)

6- For insertion of a drug into one of the body orifices

(e.g. rectal and vaginal suppositories)

7- For placement of drugs directly into the bloodstream

or into the body tissues (e.g. injections)

8- For optimal drug action through inhalation therapy

(e.g. inhalants and inhalation aerosols)
Classification of
dosage forms
Semisolid
Dosage
forms

Solid
dosage
forms

Liquid dosage
forms
 Classification of liquid
dosage forms
1- Liquid dosage form
containing soluble
matter e.g. solutions

2- Liquid dosage form containing

insoluble matter called disperse
systems e.g. suspensions
emulsions, colloidal dispersions
8
 Pharmaceutical solutions
Solutions are homogeneous liquid preparations that contain one or
more chemical substances dissolved in a suitable solvent or mixture
of mutually miscible solvents (aqueous/non aqueous)

Solutions for different routes of administration

- Orally: syrups, elixirs, drop
- In mouth and throat: Mw, gargles, throat sprays
- In body orifices: Douches, enemas, ear drops
- On body surfaces: lotions, paints
- Ophthalmic solutions and parentral products are sterile dosage
forms
9
Advantages of solution
- Easy administration and swallowing than tablet and capsule.
- More rapid action (absorption) than tablet and capsules (solution>
suspension>capsule>tablet>coated tablet).
- Give accurate dose than suspension.
- Dilute the irritant action of some drugs e.g aspirin, kI , kBr, & minimize
adverse effects of KCl in GIT.
- No need to shake since there is uniform distribution of medicament.

10
Disadvantages of solution
- They are too bulky to carry, risk of loss due to
container breakage
- Need accurate spoon to measure the dose, therefore
measurement depends on accuracy and reliability of
patient
- Less stable than solid dosage forms, and more prone
to microbial growth ( pptn ,chemical and microbial
gas formation , color change are major signs of
instability)

11
 Pharmaceutical Solutions
Aqueous or non aqueous ( Water, aromatic
Choice of solvent water, Alcohols, Oils
Liquid paraffin, ether)
Buffers, viscosity enhancement, isotonicity
Other formulation modifiers, preservatives, antioxidants,
additives sweetening agents

Methods for Simple Solution- Solution by chemical

preparation reaction- Solution by extraction

Method for
manufacture Large Scale Production

Syrups, douches, enemas,

Pharmaceutical
mouthwashs,Elixirs, Spirits, Collodions,
Dosage Forms
Glycerites, Liniments, Oleo Vitamins
Detect the difference between a stored
Stability of
sample and a freshly prepared reference
Solutions
material
 Methods for preparation of solution
a) Simple solution: prepared by dissolving solute in suitable
solvent
The preparation of oral liquids extemporaneously on a small
scale is relatively straightforward.

Solid ingredients are dissolved in a quantity of the vehicle,

estimated to be sufficient by consideration of the solubility,
other liquid ingredients are added and the solution made up to
volume with the vehicle.

Where viscous solvents are included it is more effective to use

the less viscous vehicles for the initial dissolution.

Where mixed solvents are used as the vehicle, each solid should
be dissolved in the appropriate solvent and then mixed in a
manner designed to avoid precipitation
e.g1 Calcium hydroxide solution U.S.P (lime water):-
- Shake 3 gm of Ca (OH)2 with 1000ml of cool, purified water (exothermic). Excess
Ca (OH)2 is allowed to settle out and the clear supernatant liquid is dispensed
- The soln must be kept in well filled &closed container to avoid co2 which
precipitate CaCO3, the solution should be kept in cold places (25° C) to increase
solubility of Ca(OH)2
- Used as astringent, and as protective in several types of lotions
- Used orally as source of calcium, mild antacid
b) Solution by chemical reaction:-
Prepared by reacting 2 or more solutes with each other in a suitable solvent.
e.g1 Lugols’ solution (Strong Iodine soln)
- Iodine is insoluble in water so solubilizing agent is used. It dissolves in presence
of KI due to formation of polyiodide complex (KI3 ).
- Dissolve 50g I2 in 100 ml purified water containing 100g of Kl then sufficient
14
purified H20 is added portion wise to make 1000 ml of soln.
- Used as topical germicide and treatment of hypothyroidism

15
e.g.2 Aluminum subacetate soln USP (Topical astringent) :

Rx
Aluminum Sulfate 145g
Acetic Acid 160mL
Calcium Carbonate 70g
Purified Water, a sufficient quantity,
to make 1000mL

Dissolve the Aluminum Sulfate in 600mLof cold water, filter the solution, and add the
Calcium Carbonate gradually, In several portions, with constant stirring. Then slowly add
the Acetic Acid, mix, and set the mixture aside for 24hours.
Filter the product with the aid of vacuum if necessary, returning the first portion of the
filtrate to the funnel. Wash the magma on the filter with small portions of cold water, until
the total filtrate measures 1000mL.
C) Solution by Extraction:-
Plant or animal products are prepared by extraction with a selective solvent
(extractives).

16
 Oral solutions
The pharmacist may be asked to dispense a commercially prepared
oral solution:
- Dilute the concentration of a solution (pediatric form of an adult
product)
- Reconstitution of a dry powder mixture.
- Extemporaneously compound an oral solution from bulk
components.

Knowledge of the solubility and stability of the medicinal agents and the solvents
employed in the commercial products → inform the patient of mixing the
solution with juice, milk, or other beverages upon administration.
17
Ammonium Chloride Oral Solution BP
An example of an oral solution

... “ Ammonium chloride oral solution

needs to prepared extemporaneously
and may not be readily available.”
 Solvent selection
- Selection of the proper solvent depends on the chemical characteristics of the
drugs (solutes), clarity, low toxicity, viscosity, compatibility with other
formulative ingredients, chemical inertness, palatability, odor, color, economy.
- In most cases the preferred solvent is water
- Sometimes when water is used as the primary solvent, an auxiliary solvent is
also employed to augment the solvent action of water or to contribute to a
product’s chemical or physical stability (such as alcohol, glycerin, propylene
glycol)
- Solvents such as acetone, ethyl oxide and isopropyl alcohol are too toxic to be
permitted in preparations taken internally.
19
 Some solvents used for oral solutions
Purified water, USP:
Used as a vehicle or solvent for most active ingredients or flavors.
advantages: tasteless, odorless, no pharmacological activity and cheap
non irritant for external use
Tap water:- Not used in pharmaceutical DF because it is contaminated by bacteria
and dissolved salts that may destroy active ingredients
Freshly boiled and cooled water:-
Used to destroy vegetative bacteria but on storage spores yield vegetative m.o., also
dissolved salts that may destroy active ingredients still exist
Purified water:
must be free from anions, cations .

20
N.B.
- (tap water) is not generally acceptable because of the chemical
incompatibilities that may result from the combination of dissolved
solids present and the medicinal agents being added.
- Signs of such incompatibilities are precipitation, discoloration.
-Its use is permitted in the washing and in the preparation of certain
products for external use.
-Water for Injections: Pyrogen-free distilled water, sterilized
immediately after collection and is used for parenteral preparations.

21
Methods of preparation of purified water

1- Distillation
Methods of preparation of purified water
A- Distillation
- The first amount of distillate is discarded as it contains volatile
substances and the last amount in the still is discarded as it
contains heavy metals, and also since distillation to dryness will
decompose the remaining solid impurities in the last portion
leading to contamination of the previously collected distillate
- Distilled water is not sterile (to be sterile the condenser should be
sterile)
- To be sterile, it must be subjected to sterilization process e.g. UV
energy, heat or Millipore filtration.
23
B- Ion exchange (Deionization or demineralization)
Passage of water through a column of cation and anion exchangers, consisting of
water insoluble, synthetic, polymerized phenolic, carboxylic, amino, or
sulfonated resins of high molecular weight.
(a) Cation, or acid exchangers, which permit the exchange of the cations (Ca++,
iron, mg) in the tap water with hydrogen ion from the resin
H-Resin + M+ + X- + H2O → M-Resin + H+ + X- + H2O
(b) Anion, or base exchange resins, which permit the removal of anions.
Resin – NH2 + H+ + X- + H2O → Resin – NH2 .HX + H2O (pure)
Deionized water is not sterile and can be sterilized by Heat, filtration (Millipore
filter) or uv energy .

24
C- Reverse osmosis
-A pressurized stream of water is passed parallel to the inner side of a filter
membrane core. Reverse osmosis removes virtually all pyrogens, organic
molecules, and 90-99% of all ions.
Reverse osmosis (RO) is a filtration
method that removes many types of
large molecules and ions from
solutions by applying pressure to the
solution when it is on one side of a
selective membrane. The result is
that the solute is retained on the
pressurized side of the membrane
and the pure solvent is allowed to
pass to the other side. To be
"selective," this membrane should
not allow large molecules or ions
through the pores (holes), but should
allow smaller components of the
solution (such as the solvent) to pass
freely. 25
2- Alcohol
- Low mol. weight alcohol associate like water (form H-bond).
- High DEC ( less than water)
- Used as Co solvent to increase solubility of non-electrolytes.
a) Ethyl alcohol:- (contains 5% water) (CH3CH2OH)
- Not hydrolyze drug & microrganism can’t grow in it (solution keep almost
indefinitely) since it has antimicrobial and co-preservative action
- Selective solvent as it dissolves: Resin – volatile oil – alkaloid – glycoside (active
ingredients) & not dissolve : gum – albumin – starch (inert constituents) so
useful extraction of crude drugs
- Mixture of water and alcohol in different proportions are termed hydroalcoholic
solutions (diluted alcohol is 50% alcohol and 50% water).
- It does not dissolve fixed oil (except castor oil).
26
Alcohol USP is 94.9%-96% C2H5OH v/v

Advantages of alcohol:
Solvent for water insoluble drugs or excipients such as flavorants and preservatives
Miscible with water
It is used in combination with other solvents such as glycerin to reduce the amount
of alcohol required
Used as antimicrobial preservative

Disadvantages of alcohol:
Potential toxic effects when ingested in products (especially for children). The
recommended doses for alcohol in children under 6 years is 0.5 %, 6-12 years is
5%, over 12 years is 10%
b) Absolute alcohol (dehydrated alcohol) 100%
- Free from water so has greater range of solvent power
- used in research – analysis
c) Isopropyl alcohol (CH3CHOHCH3)
- Toxic so used externally only.
- Contains not more than 1% water
- Used in some liniments and lotions

28
3- Glycerin
- Excellent solvent (comparable with alcohol).
- Preservative in high conc (above 20%).
- It dissolves fixed oil, Vegetable acid , pepsin , tannin
- it is not selective as it dissolves gum – starch – soluble
carbohydrate
- Owing to its high viscosity, solutes are slowly soluble in it
Has special value as:
- Simple solvent.
- Preservative.
- Stabilizer.
29
4- Propylene glycol

- Substitute for glycerin

- Viscous liquid, miscible with water – acetone- chloroform &
ether
- immiscible with fixed oil & dissolves many essential oil
- inhibit mould growth as ethyl alcohol

30