SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

Liquid Dosage Forms
Pharmaceutical Solutions

A. General Classifications of Liquid Dosage Forms

1. Solutions
2. Dispersed Systems (Suspensions & Emulsions)

A1. Solutions
- Liq. preparations that contain one or more chemical substances dissolved in a suitable solvent or
mixture of mutually miscible solvents
- HOMOGENEOUS one-phase system consisting of two or more components
- Most commonly used liquid dosage form
- Simplest solution involves two components, solute + solvent

A2. Types of Solutions

- Classified based on use or composition

A2A. Types of Solutions based on Use A2B. Types of Solutions based on Composition
1. Oral Solution (by mouth) 1. Aqueous Solution
2. Otic Solution (by ear) 2. Non-aqueous Solution
3. Ophthalmic Solution (by eye) 3. Sterile Solution
4. Topical Solution (by skin or unswallowed)

A3. Advantages of Pharmaceutical Solutions

1. Completely homogeneous doses
2. Immediate availability for absorption and distribution (except for parenteral administration, which
is much more readily available for absorption and distribution)
3. Provides a flexible dosage form
A. Easy to swallow
B. Easy to adjust
C. Can be used by any route of administration

A4. General Rule in Preparing Solution

1. Solubility Characteristics
2. Proper Solvent - if aq. soluble, then use aq. solution
3. Salt Form - majority of formulators nowadays prefer the salt form for its enhanced solubility and
stability

A5. Intermolecular Forces That Affect Solubility

- Attractive forces between atoms lead to the formation of molecules and ions
- These forces, which are developed between like molecules, are responsible for the physical state
(solid, liquid, gas) of the substance under given conditions
- These forces can be broken by application of higher temperature

PREPARED BY: Prince Leander Rally B. Palalon 1

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

A5A. Common Intermolecular Forces

Intermolecular Forces Description

Dipole-dipole or Van der Waals Interxn where the negative pole of one molecule points towards the
Forces positive pole of the other

Polar to polar interactions

One of the weakest interactions

Ion-dipole Interaction Results of an electrostatic interaction between charged ion and a

molecule that has a dipole

It is an attractive force that is commonly found in solutions, especially

ionic compounds dissolved in polar liquids

Hydrogen Bonding Involves strongly electronegative atoms such as oxygen, nitrogen,

fluorine

NOTE: When molecules interact, attractive and repulsive forces are in effect

NOTE: When a solute dissolves, the substance’s intermolecular forces of attraction must be overcome by
forces of attraction between the solute and the solvent molecules. This entails breaking the solute-solute forces
and solvent-solvent forces to achieve the solute-solvent attraction

A5B. Solubility
- State when the total amount of solute in the solution and excess particles reach equilibrium
- As grams of solute dissolving milliliters of solvent
- E.G. 1 g of NaCl dissolves in 2.8 mL of water

A5B1. Solubility Table

Descriptive Term Parts of Solvent Required for 1 Part of Solute

Very Soluble <1

Freely Soluble 1-10

Soluble 10-30

Sparingly Soluble 30-100

Slightly Soluble 100-1000

Very Slightly Soluble 1000-10000

Practically Insoluble or Insoluble >10000

PREPARED BY: Prince Leander Rally B. Palalon 2

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

A6. Solvents Used for Liquid Preparations

1. Alcohol, USP
2. Glycerin, USP
3. Propylene Glycol, USP
4. Purified Water, USP

A6A. Alcohol, USP

- AKA Ethyl Alcohol or Ethanol
- MOST USEFUL SOLVENT in Pharmacy, next to water
- Used as primary solvent for many organic compounds
- Recognized as a solvent in the formulation of oral pharmaceutical products

- Properties:
A. 94.9% - 96% ethanol v/v at 15.56°C (standard temp. to assay an alcohol) - Absolute Alcohol
B. 99.5% (Dehydrated Alcohol) (Water-free) (no such thing as 100%)

- If orally taken, alcohol concentration is at 12% and below, which is the allowable intake for
pharmaceutical solutions. 5% is for pharmaceutical oral solutions with medication. 70%+ is for
topical application. There is no 100% as they are unstable and evaporate easily

A6A1. Advantages & Disadvantages of Alcohol, USP

Advantages Disadvantages

Miscibility with water Undesired pharmacologic effect

Ability to dissolve many water-soluble ingredients

(e.g. flavorants, APIs)

Used with other solvent (e.g. glycol or glycerin) that Potential toxic effect (particularly in children)
allows reduction of the amount of alcohol required

As antimicrobial preservative

A6A2. Alcohol Content Limit for OTC Oral Products intended for children

Alcohol Content Age

0.5% Children under 6 yrs of age

5% 6 to 12 yrs of age

10% Over 12 yrs of age and adults

NOTE: Beyond 10% is for alcoholic beverages

A6A3. Alcohol Preparations Available

1. Diluted Alcohol, NF 3. Isopropyl Alcohol
2. Rubbing Alcohol

PREPARED BY: Prince Leander Rally B. Palalon 3

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

A6A4. Diluted Alcohol, NF

- Mixture of Alcohol, USP and Purified Water, USP
- Conc.: 49%
- Hydroalcoholic solvent in various pharmaceutical processes and preparations

A6A5. Rubbing Alcohol (Alcohol Rubbing Compound)

- Contains about 70% ethyl alcohol or isopropyl alcohol by volume and the remainder consisting of
water, denaturants and stabilizers
- Formulation:
A. 355 mg sucrose octa-acetate or 1.4 mg denatonium benzoate for each 100 mL
B. Bitter substances (to discourage oral consumption)
- Denaturant Agent: Formula 23-H
A. Composition:
1. Acetone
2. Methyl isobutyl ketone
3. Ethyl alcohol
- The denaturant’s purpose in the formulation:
1. Discourage the illegal removal for use as a beverage of the alcoholic content
2. Impossible separation of ethyl alcohol from the denaturants with ordinary distillation
apparatus

A7. Glycerin, USP or Glycerol

- Characteristics:
A. Clear syrupy liquid with sweet taste
B. Miscible with water and alcohol
- Uses:
A. Stabilizer
B. Auxiliary solvent in conjunction with water and alcohol
- Comparable to alcohol in their preservative qualities
- 1 is water, 2 is ethanol, 3 is glycerin

A8. Propylene Glycol, USP

- Characteristics:
A. Viscous liquid
B. Miscible with water and alcohol
- Uses:
A. Solvent
B. Substitute for Glycerin in pharmaceutical formulations

A9. Purified Water, USP

- Most commonly used solvent for drug solutions
A. Purified Water, USP
B. Water for Injection, USP
C. Bacteriostatic Water for Injection, USP
D. Sterile Water for Injection, USP
E. Sterile Water for Inhalation, USP
F. Sterile Water for Irrigation, USP

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SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

A9A. Methods Employed in Preparing Purified Water

Method Process

Distillation Method Uses: Distillation apparatus

Result: Distilled water

Ion-Exchange Method Uses: Ion-exchange equipment

Result: Deionized water

Reverse Osmosis Uses: Cross-flow or tangential flow membrane filtration

Result: Concentrates/Permeates

A9A1. Ion-Exchange Method

- Passes water through a column of cation and anion exchangers consisting of water-insoluble synthetic
polymerized phenolic, carboxylic, amino or sulfonated resins
- Two types of resins:
A. Cations or acid exchangers w/c permit the exchange of cations in solution with hydrogen ion
B. Anions or base exchange resins w/c permit the removal of anions
- Advantages:
1. Elimination of Heat
2. Permit ease of operation
3. Minimal maintenance
4. More mobile facility

A9A2. Reverse Osmosis

- Pressurized stream of water is passed parallel to the inner side of a filter membrane
(semi-permeable) core

NOTE: Tap water must not be used in pharmaceutical products as it may contain impurities

A10. Cross Flow Membrane Particle Removal Ranges

Term Range

Microfiltration 0.1 to 2 micrometers (bacteria)

Ultrafiltration 0.01 to 0.1 micrometers (virus)

Nano-filtration 0.001 to 0.01 micrometers (Org. compounds in the MW of 300-1000)

Reverse Osmosis Less than 0.001 micrometers

PREPARED BY: Prince Leander Rally B. Palalon 5

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

A11. Different Types of Water (According to British Pharmacopoeia)

Type of Water Use

Purified Water Preparation of medicines that do not have to be

sterile and apyrogenic

Highly Purified Water Preparation of medicines where water of high

biological quality is needed, except where water for
injections is required

Water for Injections Medicines for parenteral administration

Must be pyrogen-free

Sterilized Water for Injections Medicines for parenteral administration

Water has been sterilized by heat
Suitably packaged

B. Preparation of Solutions
1. Simple Solution
2. Chemical Reaction
3. Solution by Extraction

B1. Simple Solution

- Prepared by dissolving the solute in most of the solvent, mixing until dissolved then adding sufficient
solvent to bring the solution up to the proper volume
- Most basic method
- However, complete dissolution does not always occur

B2. Chemical Reaction

- Prepared by reacting two or more solutes with each other in a suitable solvent
- Commonly employed when one of the API/solute is not completely soluble with the solvent, so with
the addition of another ingredient which is used to aid the dissolving/solubility of the API/solute

B3. Solution by Extraction

- Vegetable or animal origin are often extracted with suitable solvent
- Commonly employed when dealing with either vegetable or animal source of drugs

B4. Several Techniques to Hasten Dissolution

1. Applying heat
2. Reducing the particle size
3. Using a solubilizing agent
4. Vigorous agitation

C. Examples of Pharmaceutical Solutions

1. Oral Solution 5. Vaginal & Rectal Solutions
2. Syrup 6. Topical Tincture
3. Topical Solutions 7. Non-aqueous Solution
4. Elixir 8. Miscellaneous Solutions

PREPARED BY: Prince Leander Rally B. Palalon 6

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

C1. Oral Solutions & Preparations for Oral Solutions

- Most solutions intended for oral administration contain flavorants, colorants, stabilizers &
preservatives. Flavorants & colorants make the medication more attractive and palatable. Stabilizers
to maintain the chemical and physical stability of the medicinal agent. Preservatives to prevent the
growth of microorganisms in the solution

- Liquid pharmaceuticals are formulated such that the patient receives the usual dose of the
medication in a conveniently administered volume as 5, 10 and 15 mL

- Oral solutions constitute a dry mixture and a suitable solvent

C1A. Dry Mixture for Solution

- Medicinal agents w/ insufficient stability in aqueous solution to meet the extended shelf life period
are produced in a dry mixture for solution to be reconstituted

- Unstable when in prolonged contact with aqueous solution, lifespan of 7 days if unrefrigerated, 14 if
refrigerated

- Formulative components:
A. Drug D. Buffers
B. Flavorant
C. Colorant

C1A1. Dispensing Note for Dry Mixture for Solution

- Once reconstituted, dry mixture solution remains stable when stored in the refrigerator for a labeled
period of 7-14 days since it will be degraded
- In case the medication remains after the patient completes the course of therapy, patient should be
instructed to discard the remaining portion

C1B. Examples of Oral Solutions

1. Oral Rehydration Solution (ORS)
2. Oral Colonic Lavage Solution (OCLS)
3. Magnesium Citrate Oral Solution (MCOS)
4. Sodium Citrate & Citric Acid Oral Solution (SCCAOS)

C1B1. Oral Rehydration Solution

- Given to replace/replenish the rapid fluid loss or dehydration associated with diarrhea
- The loss of fluid during diarrhea is accompanied by depletion of sodium, potassium & bicarbonate
ions. These can be replenished by the ORS. EX. Gatorade
- GOAL: Replace lost fecal water

A. Typical ORS Contains (for 1000 mL)

- 45 mEq sodium
- 20 mEq potassium
- 35 mEq chlorides
- 30 mEq citrate
- 25 g dextrose

PREPARED BY: Prince Leander Rally B. Palalon 7

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

B. Counseling
- Product should be dissolved in 1L of water
- Products should not be mixed with or given with other electrolyte-containing liquids such as
milk or fruit juices due to increased number of components and cause electrolyte imbalance
- Discourage the production of homemade versions of electrolyte solutions, as they may cause
hypernatremia or worsen the diarrhea

C1B2. Oral Colonic Lavage Solution

- Used in preparation of the bowel for procedures such as colonoscopy, aids in the removal of the
content of the colon

- EX. PEG-ES - balanced solution of electrolytes w/ polyethylene glycol, example of Oral Colonic
Lavage Solution (OCLS)

- MOA: Act as osmotic agent in GIT and balance electrolyte concentration

- DOSE: 4 L (4,000 mL) solution
- USE: Management of acute iron overdose in children

Counseling
1. Drink 240 mL of solution every 10 minutes until 4 L is consumed in preparation for
colonoscopy
2. Advised to drink each portion quickly
3. Should not have taken any food 3-4 hours before beginning to take the solution
4. No solid foods be taken by the patient for at least 2 hours before the solution is administered
as it defeats the purpose of the OCLS
5. No foods except clear liquid are permitted after this product is administered and prior to
examination
6. Stored in refrigerator after reconstitution

NOTE: After taking the 4L, the 1st bowel movement will occur in one hour

C2. Syrups
- Concentrated aq. preparations of a sugar or sugar substitute with or without flavoring agents and
medicinal substances

C2A. Types of Syrups

1. Non-medicated Syrup
- No API, flavored vehicle only
- Serve as pleasant tasting vehicle for medicinal substances
- They may or may not contain flavorant since it is made up of sugar

2. Medicated Syrup
- Prepared by combining sucrose, purified water, flavoring agent, coloring agent, therapeutic
agent and other ingredients desirable for the preparation
- Employed for the therapeutic purpose

3. Simple Syrup - beginning of all syrups

PREPARED BY: Prince Leander Rally B. Palalon 8

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

C2B. Advantages of Syrups

1. Provide pleasant means of administering a liquid form of a disagreeable-tasting drug
2. Particularly effective in the administration of drug to youngsters due to their pleasant taste
3. Contains little or no alcohol that adds to their favor among parents

C2C. Components of Syrups

A. Sucrose or sugar substitute
- Sucrose is the sugar most frequently employed. Sugar substitutes include sorbitol, glycerin
or propylene glycol
B. Antimicrobial preservative
- Commonly used are benzoic acid (COMMONLY-ADDED) (0.1% to 0.2%), sodium benzoate
(0.1% to 0.2%), combination of methyl and propylparaben (0.1%)
C. Flavorants
- Masks the unpleasant taste. Flavored with synthetic flavorants or with naturally-occurring
volatile materials, such as volatile oils. Commonly-employed are orange oil & vanillin
D. Colorants
E. Special solvents, solubilizing agents, thickeners, stabilizers (OPTIONAL)

NOTE: Alcohol is added to syrups to help dissolve the alcohol-soluble ingredients, but is not present in the
final product

C2D. Syrup, NF
- AKA Simple Syrup
- Prepared by dissolving 85 g of sucrose in enough purified water to make 1000 mL of syrup

C2D1. Characteristics of Syrup, NF

- Inherently stable and resistant to the growth of microorganisms
- Has a specific gravity of 1.313
- Self-preservative at conc. of 85%

C2E. Sorbitol Solution, USP

- Non-sucrose based syrup
- Contains 64% by weight of Polyhydric Alcohol Sorbitol

C2F. Preparation of Syrups

1. Solution with the aid of heat
2. Agitation without the use of heat
3. Reconstitution
4. Percolation

C2F1. Solution w/ Aid of Heat

- Desired method to prepare the syrup as quickly as possible and when the syrup’s components are not
damaged or volatilized by heat
- Heat facilitates the rapid dissolution of the sugar and certain other components of the syrup

- Process:
A. Sugar is added to purified water and heat is applied until sugar is dissolved
B. Other heat-stable components are added to the hot syrup then the mixture is allowed to cool
and volume is adjusted with addition of purified water

PREPARED BY: Prince Leander Rally B. Palalon 9

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

A. CAUTION must be exercised:

- PREVENT hydrolytic rxn of sucrose which is INVERSION which provides fructose and
glucose
- Caramelization

B. Properties
- Syrups cannot be sterilized by autoclaving
- Store in a tight container

C2F2. Solution by Agitation w/o the use of Heat

- Used to avoid heat-induced inversion of sucrose
- Process:
A. Sucrose and other formulative agents are dissolved in purified water in a vessel larger than
the volume of syrup to be prepared permitting thorough agitation

- Disadvantage & Advantage:

A. More time consuming BUT product has MAXIMUM stability

- Large/Intermediate Scale of Preparation: Bottle Shaker

- Small Scale of Preparation: Manual Shaking to dissolve the solutes in the solvent

- Solid Agents are to be added to a syrup:

A. Solid agents are dissolved first in minimal amount of purified water and incorporate the
resulting solution into syrup

- If solid substances are added directly:

A. They dissolve slowly because of the viscous nature of the syrup and it does not permit the
solid substance to distribute readily throughout the syrup

C2F3. Percolation
- 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
- Combination of simple solution & Solution by Extraction
- EX.
A. Ipecac Syrup
- Prepared by adding glycerin and syrup to an extractive of powdered ipecac obtained
by percolation

C3. Topical Oral (Dental) Solutions

A. Mouthwashes
- Are aq. solutions used for deodorant, refreshing or antiseptic effect or for control of plaque

B. Gargles
- Are aq. solutions used for treating the pharynx and nasopharynx by forcing air from the
lungs through the gargle which is held in the throat

PREPARED BY: Prince Leander Rally B. Palalon 10

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

C4. Elixir
- Non-aq. solution due to it being more of alcohol (Alcohol Content: 10% to 20%)
- Clear, sweetened hydroalcoholic solutions intended for oral use and usually flavored to enhance their
palatability
- Less sweet and viscous compared to syrup as it contains a lower portion of sugar, due to this, elixirs
are preferred sometimes over syrup due to sugar content

C4A. Types of Elixir

A. Non-medicated Elixir
- Employed as vehicles

B. Medicated Elixir
- Used for the therapeutic effect of the medicinal substance they contain

C4B. Advantages & Disadvantages of Elixir

Advantages Disadvantages

Less sweet and less viscous Less effective in masking the taste of medicinal
substances

Better in maintaining both water-soluble and Alcohol content (which can cause toxicity)
alcohol-soluble components in solution

C4C. Characteristics of Elixir & Sweeteners of Elixir

A. Proportion of alcohol in elixirs varies because individual components have different water and
alcohol solubility
B. Each elixir requires a specific blend of alcohol and water to maintain all of the components in
solution

SWEETENERS:
A. Sucrose or sucrose syrup
B. Sorbitol
C. Glycerin
D. Artificial sweeteners

NOTE: Elixirs with more than 10% to 20% of alcohol are considered as self-preserving and do not require
the addition of antimicrobial preservatives. Recommended dose of elixir is at 5-10 mL for adults

C4D. Preparations of Elixirs

- Elixirs are prepared usually by simple solution w/ agitation or by admixture of two or more liquid
ingredients
- Process:
A. Alcohol-soluble and water-soluble components are prepared separately in alcohol and
purified water
B. Aq. solution is then added to the alcoholic solution. Aq. is added to alcohol to maintain the
highest possible alcoholic strength at all times and to have minimal separation of
alcoholic-soluble components
C. Completely mixed, the mixture is made to the volume with specified solvent or vehicle

PREPARED BY: Prince Leander Rally B. Palalon 11

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

D. Characteristics of the final mixture will be CLOUDY due to the separation of some flavoring
oils by the reduced alcoholic concentration
E. If this occurs, elixir is usually permitted to stand or prescribed for a number of hours to
ensure saturation and permit the oil globules to coalesce so that they may be more easily
removed by filtration
F. TALC is used as filter aid in the preparation of elixirs
G. IMPORTANT CHARACTERISTIC is CLARITY

C5. Tinctures
- Non-aq. solution
- Are alcoholic or hydroalcoholic solutions prepared from vegetable materials or from chemical
substances
- Vary in terms of:
A. Method of Preparation
B. Strength of API
C. Alcoholic Content
D. Intended Use in Medicine or Pharmacy

A. Methods
A. Chemical Substances - Simple Solution
B. Vegetable Materials - Percolation

Alcohol Content: 15% to 80%

B. Characteristics
A. Must be tightly stoppered, stored in light-resistant container protected from sunlight and not
exposed to excessive temperatures due to its alcohol content

C. Examples of Tinctures
1. Paregoric, USP
- Camphorated opium tincture
- Oral
- Obsolete due to Opium

2. Laudanum, USP
- Opium tincture
- More potent than Paregoric, USP
- AKA Opium Tincture, USP
- Oral
- Obsolete due to Opium

3. Iodine Tincture
- Has iodine content
- Topical

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SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

C5A. Topical Tinctures

C5A1. Iodine Tincture

- Prepared by dissolving 2% iodine crystals and 2.4% sodium iodide in an amount of alcohol equal to
half the volume of tincture
- Local anti-infective agent
- Reddish-brown color produces stain in the skin, useful in delineating the application over the affected
skin area
- Stored in a tight container to prevent loss of alcohol
- Prepared by chemical reaction

C5A2. Compound Benzoin Tincture

- Prepared by maceration in alcohol of 10% benzoin and lesser amount of Aloe, storax and tolu balsam
totalling 24% of starting material
- Categorized as PROTECTANT

C5A3. Thimerosal Tincture

- Has the same general remarks about thimerosal topical solution except sodium chloride and sodium
borate are absent and the vehicle are water, acetone & 50% alcohol

C5B. Topical Solutions & Tinctures - Preparation

- Topical solutions = Aq. solutions
- Maceration = hydroalcoholic solutions
- Prepared by:
A. Simple dissolving/solution
B. Chemical reaction
C. Maceration (Extraction)

C5B1. Examples of Topical Solutions

1. Sprays
2. Aluminum Acetate Topical Solution
3. Aluminum Subacetate Topical Solution
4. Calcium Hydroxide Topical Solution
5. Coal Tar Topical Solution
6. Hydrogen Peroxide Topical Solution
7. Chlorhexidine Gluconate Solution
8. Povidone-Iodine Topical Solution
9. Thimerosal Topical Solution

C6. Spirits
- Are alcoholic or hydroalcoholic solutions of volatile substances
- AKA Essenses
- Alcohol Content: Over 60%
- USE: Flavoring Agent (if conc. is lowered) & Medicinally for the Therapeutic Value of Aromatic
Solute
- Methods of Preparation:
A. Simple Solution
B. Solution by Maceration
C. Distillation

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SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

C9A. Examples of Spirits

1. Aromatic Ammonia Spirit
2. Camphor Spirit
3. Compound Orange Spirit
4. Peppermint Spirit

C10. Vaginal & Rectal Solutions

Solutions Intended Use

Vaginal Douches For irrigation cleansing of vagina

Retention Enemas Influences the general system by absorption or

affect a local disease

Imaging or Radiopaque Media

Evacuation Enemas Used to cleanse the bowel

C11. Aromatic Waters

- No longer in widespread use
- Are clear, aq. solutions saturated with volatile oils or other aromatic or volatile substances
- USE: Perfumery
- Examples:
1. Orange Flower Oil 5. Spearmint Oil
2. Peppermint Oil 6. Wintergreen Oil
3. Rose Oil 7. Camphor
4. Anise Oil 8. Chloroform - Obsolete

C12. Sprays
- May be defined as aq. or oleaginous solutions in the form of coarse droplets or as finely divided solids
to be applied topically, most usually in the nasopharyngeal tract or the skin
- Advantages:
A. Non-invasive
B. Quickness w/ medication delivery systemically

D. Non-Aqueous Solutions

D1. Ethereal Solutions

- Contains essences or essential oils or ether oils

D2. Oleaginous Solutions

- More oils

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SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

Non-Aqueous Solutions Description Example

Liniments Alcoholic/Oleaginous solutions or Hydroalcoholic Liniment

emulsions of various medicinal - Rubefacient,
substances intended to be rubbed counterirritant, or
on the skin penetrating action

Oleaginous Liniment
- Massage

Collodions Liquid preparations composed of Pyroxylin

pyroxylin dissolved in a solvent - AKA nitrocellulose or
mixture (comp. of alcohol & soluble cotton gun
ether) with or without medicinal - Obtained by the action of
substances a mixture of nitric and
sulfuric acids on cotton
To be used externally
Flexible Collodion
- Combination of
pyroxylin, 10% salicylic
acid, 2% camphor & 3%
castor oil

Salicylic Acid Collodion

D3. Oleaginous Liniment Solvents

1. Almond Oil
2. Cottonseed Oil
3. Peanut Oil
4. Wintergreen Oil - most common
5. Sesame Oil
6. Turpentine Oil

NOTE: All liniments should bear a label indicating “FOR EXTERNAL USE” or “SHAKE WELL”

D4. Extraction Methods for Preparing Solutions

A. Extraction
B. Crude Drug
C. Extractive
D. Marc
E. Tincture, fluidextract & extracts

D4A. Extraction
- Process of withdrawing the desired constituents from crude drugs through the use of selected solvents
in which the desired constituents are soluble

D4B. Crude Drug

- Vegetable or animal drugs that have undergone no other processes than collection, cleaning & drying

D4C. Extractive
- Product of extraction process

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SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

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D4D. Marc
- Solid and undissolved portion
- Plant residue

D4E. Tincture, Fluidextract & Extracts

- MOST COMMON pharmaceutical products that is prepared from extractive

NOTE: The solvent system used in extraction are selected on the basis of their capacity to dissolve the
maximum amount of desired active constituent and the minimum amount of undesired constituent

D4F. Menstruum
- Solvent or solvent mixture
- Either alcohol (ethanol is most used, methanol is used sometimes), or water

E. Methods of Extraction
A. Maceration
1. Decoction
2. Digestion
3. Infusion
B. Percolation

E1A. Decoction
- For water soluble and heat-stable constituent of crude drugs
- Extracted by boiling in water

E1B. Digestion
- Same with decoction but with gentle heat, not in boiling water

E1C. Infusion
- Dilute solutions are readily soluble infusions like making tea
- Short maceration of drug through cold/boiling water

E2. Factors Affecting the Method of Extraction

1. Nature of the Crude Drugs
- For maceration & percolation
2. Adaptability to Various Extraction Methods
3. Interest in Obtaining Complete or Nearly Complete Extraction of the Drug

E3. Maceration
- Softens the plant tissue and dissolve the active constituent
- From the latin word “macerare” meaning to “soak”
- Conducted at 15℃ to 20℃ for 3 days or until the soluble matter is dissolved
- 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
- Process:
1. Drug to be extracted is placed in a wide-mouthed container with prescribed menstruum
2. Vessel is stoppered tightly and the contents are agitated repeatedly over a period ranging
from 2-14 days

PREPARED BY: Prince Leander Rally B. Palalon 16

SUBJECT: Pharmaceutical Dosage Forms, Drug Delivery Systems & Medical Devices

INSTRUCTOR: Ms. Rhona Joy Enriquez

E4. Percolation
- Separate the extractive form of the Marc
- “Per” meaning “through” & “colare” meaning to “strain”
- Process in which a comminuted drug is extracted of its soluble constituents by slow passage of
suitable solvent through a column of the drug
- Special extraction apparatus: PERCOLATOR
- Flow of menstruum over the drug column is downward to the exit orifice, drawn by the force of
gravity
- EX. Traditional way of making coffee

F. Fluidextracts
- Are liq. preparations of vegetable drugs prepared by percolation
- Contain alcohol as solvent, preservative and made to have 1 g of the therapeutic constituent is
present in each mL
- Disadvantage:
A. Too potent to be safely self-administered
B. Too bitter tasting

F1. Extracts
- Conc. preparations of animal or vegetable drugs obtained by removal of the active constituents of the
respective drugs with suitable menstrua evaporation of all or nearly all oil the solvent and
adjustment of the residual masses or powders to the prescribed standards
- Potent preparations, usually between 2x & 6x as potent on a weight basis as the crude drug
- Contain primarily the active constituents with a great portion of inactive constituents and structural
components

F2. Three Forms of Extracts

1. Semi-liquid Extract
- Those of a syrupy consistency prepared without the intent of removing all or even most of
the menstruum
- Most common to be obtained in the laboratory

2. Pilular
- Solid extracts of plastic consistency prepared with nearly all of the menstruum removed

3. Powdered Extract
- Prepared to be dry by the removal of all of the menstruum insofar as is feasible or practical

NOTE: In the extraction of crude drugs, combination of maceration and percolation is employed

NOTE: Pilular & powdered extract differ only by the slight amount of remaining solvent in the former
preparations

PREPARED BY: Prince Leander Rally B. Palalon 17