Liquid Dosage Forms

Leigh Don T. Villanueva, RPh

De La Salle Medical and Health Sciences Institute
PH-PHR 214 A.Y. 2020-2021
Liquid Dosage Forms
• Prepared using pharmaceutically and therapeutically
acceptable vehicles
• Active ingredient(s) may be
• _________ in an aqueous or nonaqueous solvent or
combination
• __________ in the medium
• ___________ in an appropriate medium
• ___________ in either the oil or water phase

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Liquid Dosage Forms
• can be formulated for different routes of administration

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Advantages
• dose can be ________ adjusted by dilution
• can readily be administered to _____________________

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Advantages
• extracts eliminate the need to isolate the drug in pure form,
allow several ingredients to be given from a single source, and
permit the preliminary study of drugs from natural sources
• used to minimize ______________ in the gastrointestinal tract

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Consideration for using Liquid Dosage Forms
• purpose of the drug
• internal or external use
• concentration of the drug
• selection of the vehicle
• physical and chemical stability of the drug and its excipients
• preservation of the preparation
• use of appropriate excipients

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solutions
Solution
• _____________ mixture that is prepared by dissolving a
solid, liquid or gas in another liquid
• the molecules of the solute are dispersed among those
of the solvent

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Principle Involved
• Solubility

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Principle Involved
• Factors that affect Solubility
• Temperature
• Solute & Solvent properties
• Pressure
• pH
• Physical Agitation

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solubility Rules
• Inorganic Molecules
• Both ions are monovalent
• One ion is monovalent
• Both ions are multivalent
• Common salts of alkali metals
• Ammonium and Quaternary Ammonium salts

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solubility Rules
• Inorganic Molecules
• Nitrates, nitrites, acetates, chlorates, and lactates
• Sulfates, Sulfites, and thiosulfate
• Chlorides, bromides, iodides
• Acid Salts corresponding to an insoluble salts

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solubility Rules
• Inorganic Molecules
• Hydroxides and Oxides other than alkali metals
• Sulfides
• Phosphates, carbonates, silicates, borates, and
hypochlorites

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solubility Rules
• Organic Molecules
• One polar group; <5 C
• Branched Chain
• Increase in MW
• Increased structural similarity between solute and solvent

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solvents
• Alcohol, USP
• Primary solvent for most organic compounds
• Antimicrobial Preservative
• Water miscible and has the ability to dissolve water insoluble
substances

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solvents
• Diluted Alcohol, NF
• Mixed equal volumes of Alcohol, USP and Purified Water, USP
• Useful Hydroalcoholic Solvent

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solvents
• Rubbing Alcohol
• 70% Ethanol by volume
• Each 100 mL must contain NLT 355 mg Sucrose
Octoacetate or 1.4mg of denatonium benzoate

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solvents
• Glycerin, USP
• Clear, syrupy liquid with a sweet taste
• Miscible to both water and alcohol

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solvents
• Isopropyl Rubbing Alcohol
• 70% Isopropyl Alcohol by volume
• Commonly employed by diabetic patients for syringes

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solvents
• Propylene Glycol, USP
• Viscous Liquid miscible with water and alcohol

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solvents
• Purified Water, USP
• Obtained by Distillation, Ion Exchange, Reverse Osmosis or
other suitable process

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Advantages of Solutions
• Easy to Swallow
• Immediate Absorption
• Homogenous
• Reduced gastric irritation

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Disadvantages of Solutions
• Transport and Storage inconvenience
• Poor stability
• Inaccurate dose
• Inability to mask taste

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Techniques to increase solubility of Solutes
• Application of Heat
• Reducing Particle Size of solute
• Using a solubilizing agent
• Subjecting the ingredients to vigorous agitation

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Types of Solution
Type of Solution
• Aqueous Solutions
• Sweet or Other Viscid Aqueous Solutions
• Non-aqueous Solutions

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Aqueous Solutions
• Water
• Aromatic Waters
• Aqueous Acids
• Solutions
• Douches
• Enemas
• Gargles
• Mouthwashes

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Aqueous Solutions
• Juices
• Nasal Solutions
• Otic Solutions
• Irrigation Solutions

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Water
• Major Ingredient
• Vehicle, solvent for flavoring

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Aromatic Waters
• Medicated Waters
• Clear, Aqueous solutions saturated with volatile
oils or other aromatic or volatile substances
• Flavoring; Perfuming
• Ex: Peppermint Water, USP; Stronger Rose Water,
USP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Dilute acids
• Aqueous solutions of concentrated acids diluted
with purified water
• Ex. Diluted Hydroalcoholic, USP; Diluted Acetic
Acid

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Solutions
• Liquid preparations that contain one or more soluble
chemical substances dissolved in water
• Preparation of Solutions
• Simple Solutions
• Solution by Chemical Reaction
• Solution by Extraction

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Douches
• Aqueous solution directed against a part or into
a cavity of the body using bulb syringes
• Powders or tablets with directions for dissolution
• Cleansing or antiseptic agents

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Enemas
• Rectal Injection
• Used as
• Evacuation Enema
• Retention enema

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Gargles
• Aqueous solutions frequently containing antiseptics,
antibiotics, and/or anesthetics used for treating the
_____________________ by forcing air from the lungs through the
gargle that is held in the throat and then the gargle is
subsequently expectorated
• Examples: Potassium Chlorate and Phenol Gargle, PC; Isodine

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Mouthwashes
• Aqueous solutions often in concentrated form containing one
or more active ingredient and used by swishing the liquid in the
oral cavity
• Usually contains alcohols, surfactants, flavors, and coloring
agents

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Juices
• Aqueous preparation from fresh ripe fruit or with artificial
flavors
• Used in making syrups

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Nasal Solutions
• Aqueous solutions designed to be administered to the nasal
passages in drops or sprays
• Drops spread more extensively than sprays
• Sprays

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Otic Solutions
• Aural Solutions
• Aqueous solution for topical application in the ear as drops
• May contain analgesics, anti-inflammatory agents, antibiotics
for the removal of cerumen
• Examples: Antipyrine and Benzocaine Otic Solution, USP;
Neomycin and Polymyxin B Sulfates and Hydrocortisone Otic
Solutions, Sodium Bicarbonate Eardrops, BP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Irrigation Solutions
• Aqueous solutions used to wash or bathe surgical incisions,
wounds or body tissues
• Must be isotonic, sterile, and pyrogen-free
• Ex: Acetic Acid Irrigation, USP; Sodium Chloride Irrigation

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Sweet or other Viscid Aqueous Solutions
• Viscous liquids or semisolid that are sweet or viscid and may
contain sugars, polyols, or polysaccharides (gums)
• Syrups
• Honeys
• Mucilages
• Jellies

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Syrups
• Concentrated aqueous preparations of sugar or
sugar substitute with or without flavoring agents
and medicinal substances usually for children
and elderly people
• Flavored Vehicle; Medicated Syrup
• May contain glycerin or sorbitol to prevent
crystallization or to increase solubility of added
ingredients
PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Syrups
• Components: Sugar, Antimicrobial Preservatives,
flavorant, Colorant
• Methods of Preparation

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Preservation of Syrups
• Quantities consumable within a few months
• Use low temperature
• No supersaturation
• Add preservatives
• Glycerin, methylparaben, benzoic acid, sodium benzoate

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Honeys
• Thick liquid preparations with honey as a base
• Example: Squill Oxymel, BP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Mucilages
• Thick, viscid, adhesive liquids produced by dispersing gum in
water, or by extracting the mucilaginous principles from
vegetable substances with water
• Prone to decomposition and the viscosity is decreased on
storage
• Not in quantities larger than immediate use
• Aid in suspending insoluble substances in liquids
• Ex: Acacia Mucilage, NF; Tragacanth Mucilage, BPC

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Non-aqueous
Solutions
Nonaqueous Solutions
• Includes alcoholic and hydroalcoholic solutions, ethereal
solutions, glycerin solutions, oleaginous solutions, inhalations
and inhalants
• Collodions
• Elixirs
• Glycerins
• Inhalations and inhalants
• Liniments
• Oleovitamins
• Spiris
• Toothache drops

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Collodions
• Liquid preparations of pyroxylin in a solvent
mixture of ethyl ether and ethanol applied to the
skin using a soft brush or other suitable
applicator, leaving a film after the solvent has
evaporated

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Elixirs
• Clear, Sweetened hydroalcoholic solutions
intended for oral use and are usually flavored to
enhance their palatability
• Non-medicated; Medicated
• Dry Elixirs are in development for improved
absorption

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Elixirs vs. Syrups
• Elixirs are usually less viscous
• Contains lower proportion of sugar
• Better at maintaining hot water-soluble and
alcohol soluble components
• Stable characteristics and the ease of
preparation

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Elixirs vs. Solid Dosage Forms
• Advantage: Flexibility and ease of dosage
administration to patients who have difficulty in
swallowing
• Disadvantage: Alcoholic Content

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Elixir Preparation
• Simple Solution with agitation and/or Admixture
of two or more liquids
• Alcohol-soluble and water-soluble components
are dissolved separately
• Aqueous Solution is added to the alcoholic
solution

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Elixir Preparation
• If cloudy, stand for a number of hours

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Nonmedicated Elixirs
• Useful to the pharmacist in the extemporaneous
filling of prescriptions involving the addition of a
therapeutic agent to a pleasant-tasting vehicle
and dilution of an existing medicated elixir

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Medicated Elixirs
• Employed for the therapeutic benefit of the
medicinal agent
• Most official and commercial elixirs contain only
one therapeutic agent
• Ex: Dexamethasone Elixir, USP; Phenobarbital
Elixir USP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Glycerins
• Glycerites
• Solutions or mixtures of medicinal substances in not less than
50% by weight of glycerin
• Extermely viscous and jelly-like
• Hygroscopic

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Inhalations
• Drugs or solutions or suspensions on one or more drug
substances administered by the nasal or oral respiratory route
for local or systemic effect

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Inhalations
• Nebulizers are used if the solution give fine and uniform-sized
droplets so that the mist reaches the bronchioles
• Metered-dose inhalers are propellant-driven drug suspensions
or solutions in liquefied-gas propellant with or without a
cosolvent and are intended for delivering metered doses of the
drug to the respiratory tract

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Inhalations
• In the BP, inhalations are solutions or suspensions of one or
more active ingredients that may contain an inert, suspended
diffusing agent
• intended to release volatile constituents for inhalation, either
when placed on a pad or when added to hot but not boiling
water
• Example: Benzoin Inhalation BP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Inhalants
• special class of inhalations consisting of drugs or combination
of drugs that, by virtue of their high vapor pressure, can be
carried by an air current into the nasal passage where they
exert their effect

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Liniments
• Alcoholic or oleaginous solutions/emulsions of
medicinal substance intended to be rubbed on the skin
only
• Intended for external application and must be labeled
“For External Use Only”; rubbed onto the affected area
(embrocations)

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Oleovitamins
• Fish-liver oils diluted with edible vegetable oil or solutions of
the indicated vitamins or vitamin concentrates in fish-liver oil
• Example: Oleovitamin A and D, Concentrated Vitamin A Solution
PC

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Spirits
• Alcoholic or hydroalcoholic solutions of volatile
substances
• Used pharmaceutically as flavoring agents and
medicinally for the therapeutic value of aromatic
solute
• Should be stored in tight, light-resistant
containers and in a cool place

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Spirits
• Prepared by
• simple solution
• solution with maceration
• chemical reaction
• distillation
• Dilution with aqueous solutions or liquids of low alcoholic
content may result to turbidity or precipitation
• Examples: Aromatic Ammonia Spirit BP, Soap Spirit BP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Extracts
Extracts
• Products obtained from plant or animal tissue by extraction
• Extractive Preparation
• Tinctures
• Fluidextract
• Extracts

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
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
• Methods
• Maceration
• Percolation
• Digestion
• Infusion
• Decoction

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Tinctures
• Alcoholic or hydroalcoholic solutions prepared
from vegetable materials or from chemical
substances
• Alcohol content: 15 to 80%

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Tinctures
• The alcoholic content acts as an antimicrobial
and keeps the alcohol-soluble extractives in
solution
• Cannot be mixed with liquids too diverse in
solvent character because solute may precipitate

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Tinctures
• Two general process of preparation
• Process P
• Process M
• Example: Compound Benzoin Tincture USP,
Sweet Orange Peel Tincture USP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Fluidextract
• Liquid preparations of vegetable drugs, containing alcohol as a
solvent or as a preservative, or both, so made that, unless
otherwise specified in an individual monograph, each, mL
contains the therapeutic constituents of 1 g of the standard
drug that it represents
• BP term is Liquid Extract

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Fluidextract
• Three methods of Preparation
• Process A
• Process E
• Process D
• Example: Cascara Sagrada Fluidextract, USP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Extract
• Concentrated preparations of vegetable or animal drugs
obtained by the removal of the active constituents of the
respective drugs with suitable menstrual, evaporation of all or
nearly all of the solvent, and adjustment of the residual masses
or powders to the prescribed standards

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Extract
• 3 Forms
• Semiliquids or liquids of syrupy consistency
• Plastic masses
• Pillular or solid extracts
• For ointments and suppositories
• Pure Glycyrrhiza Extract USP
• Dry powders
• Powdered extracts
• Capsules, powders, tablets
• Belladonna Extract USP

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
Reference
• Ansel, Howard, et al. Pharmaceutical Dosage Forms
and Drug Delivery Systems. 10th ed. USA: Lippincott
Williams & Wilkins, 2014.

PH-PHR 214: Dosage Forms, Drug Delivery Systems, and Medical Devices
 Thank you for listening

Leigh Don T. Villanueva, RPh

De La Salle Medical and Health Sciences Institute
PH-PHR 214 A.Y. 2020-2021