Solutions PDF
Solutions PDF
LECTURE: SOLUTIONS
SOLUTIONS
OVERVIEW ● Solutes – considers the active ingredients, excipients
I Solutions especially the colorants, flavorants and sweetener
II Solutions According To Use (natural or artificial)
III Solutions According To Composition
IV Solubility Advantages Disadvantages
V Kinds of Solutions
VI Advantages Of Ethyl Alcohol As A Solvent ● Self administration ● Dosing Accuracy
VII Limitations set by FDA as to the Alcoholic ● Easy to swallow (oral) (large disadvantage
Contents of OTC Oral Preparations ● Patient Compliance of solutions due to
VIII Different Alcohols or Solvents for Liquid (due to flavor and different size
Preparations ease of swallowing) spoons or improper
IX How Most Pharmaceutical Solutions are ● Uniformity of dose reading of cups)
Prepared ● Microorganisms and
X How Strengths of Pharmaceutical Preparation contamination
are Expressed: (since dispensed in
A. Percent Strength multi-dose
B. Ratio Strength containers)
● Handling,
XI A. Ways Oral Solutions are made packaging, shipping
Extemporaneously ● Heavy liquids, large
B. Methods Under Solution by volumes, and
Extraction breakable
C. Examples of Oral Solutions by containers
Category
XII Oral Rehydration Solutions/Salts (ORS) PHYSICOCHEMICAL TERMS
XIII Oral Colonic Lavage Solution
XIV Magnesium Citrate Oral Solution ● Solutions may be prepared from any combination of a
XV Sodium Citrate and Citric Acid Oral Solution solid,liquid, and gas, the three states of matter.
XVI Most Syrups Contain the Following
Components in Addition to the Purified Water PHARMACEUTICAL TERMS
and Any Medicinal Agents Present:
A. Sugar ● Liquid preparations that contain one or more chemical
B. Antimicrobial Preservatives substances dissolved in a suitable solvent or mixture
C. Flavorants of mutually miscible solvents.
D. Colorants
XVII Sucrose Based and Non-Sucrose Based II. SOLUTIONS ACCORDING TO USE
Syrups ORAL SOLUTIONS
XVIII Syrup Preparation Methods
XIX Elixirs ● In liquid form and is administered in the mouth.
XX Topical Preparations ● Has flavorants and colorants to make the medication
XXI Common Extraction Methods more attractive and palatable.
XXII Products Formed from Extractives ● ORS: Distributed as powder, need to incorporate
needed amount of water to make it into a solution.
I. SOLUTIONS ● Examples:
○ Oral Rehydration Solutions,
● Has a lot of classifications depending on uses and ○ Oral Colonic Lavage Solution
composition. ○ Magnesium Citrate Oral Solution
● Can be prepared by extracting active constituents
from crude drugs. OTIC SOLUTIONS (EAR DROPS)
● In Pharmacy, interest in solutions for the most part are
limited to solutions of a solid and a liquid. ● Treatment for outer ear bacterial infections.
● Less frequently, a gas solute in a liquid solvent. ● It works by preventing the growth of bacteria and
fungus in the ears that may also cause pain and
SOLUTION PROCESS discomfort for the patient.
● Examples: Ofloxacin Otic Solutions
● The formation of a solution (in basic terms) involves:
○ Solutes (drugs, color, flavoring, sweeteners) OPHTHALMIC SOLUTIONS (EYE DROPS)
+
○ Liquid Solvent (water, oil, alcohol, ● Treatment for eye bacterial infections and works by
propylene glycol) = stopping its growth.
○ Solution ● Examples: Tobramycin Dexamethasone (Opidex)
● The solute must be soluble in the chosen solvent.
HYDROALCOHOLIC ETHEREAL
VII. LIMITATIONS SET BY THE FDA AS TO THE ● Concern has been expressed over the undesired
ALCOHOLIC CONTENTS OF OTC ORAL PREPARATIONS pharmacologic and potential toxic effects of alcohol
when ingested in pharmaceutical products,
● The U.S. Food and Drug Administration (FDA) has particularly by children.
proposed that insofar as possible, manufacturers of ○ Thus, the U.S. The Food and Drug
over-the-counter (OTC) oral drug products restrict the Administration (FDA) has proposed that
use of alcohol and include appropriate warnings in the insofar as possible manufacturers of
labeling. over-the-counter (OTC) oral drug products
restrict the use of alcohol and include
appropriate warnings in the labeling.
AGE RANGE ALLOWED ALCOHOLIC % ○ For OTC oral products intended for children
FOR OTC ORAL under 6 years of age, the recommended
PREPARATIONS alcohol content limit is 0.5%.
○ For products intended for children 6 to 12
For OTC products intended 0.5% years of age, the recommended limit is 5%
for children under 6 years ○ For products recommended for children over
of age 12 years of age and for adults, the
recommended limit is 10%.
For products intended for 5%
children 6 - 12 years of DILUTED ALCOHOL
age
● Diluted Alcohol, NF, is prepared by mixing equal
For products recommended 10% volumes of Alcohol, USP, and Purified Water, USP.
for children over 12 years ○ The final volume of such mixtures is not the
of age and adults sum of the individual volumes of the two
components because the liquids contract
VIII. DIFFERENT ALCOHOLS OR SOLVENTS FOR LIQUID upon mixing.
PREPARATIONS ● The final volume is generally about 3% less than
ALCOHOL / ETHYL ALCOHOL what would otherwise be expected.
○ Thus, when 50 mL of each component is
● Next to water, alcohol is the most useful solvent in combined, the resulting product measures
pharmacy. approximately 97 mL.
● It is used as a primary solvent for many organic ● The strength of Diluted Alcohol, NF, is not exactly
compounds. half that of the more concentrated alcohol but slightly
○ Together with water, it forms a hydro greater, approximately 49%.
alcoholic mixture that dissolves both ● Diluted alcohol is a useful hydro alcoholic solvent in
alcohol-soluble and water-soluble various pharmaceutical processes and preparations.
substances, a feature especially useful in the
extraction of active constituents from crude RUBBING ALCOHOL
drugs.
○ By varying the proportion of the two agents, ● The product is volatile and flammable and should be
the active constituents may be selectively stored in a tight container remote from fire.
dissolved and extracted or allowed to ● Synonym: alcohol rubbing compound
remain behind, according to their particular ○ contains about 70% ethyl alcohol by
solubility characteristics in the menstruum. volume, the remainder consisting of water,
● Alcohol, USP, is 94.9% to 96.0% C2H5OH by volume denaturants with or without color additives
(i.e., v/v) when determined at 15.56°C, the US and perfume oils, and stabilizers.
government's standard temperature for alcohol ● You can buy rubbing alcohol with a concentration of
determinations. 70% or 99% isopropyl alcohol.
● Dehydrated Alcohol, USP, contains not less than ○ Experts say 70% is actually better for
99.5% C2H5OH by volume and is used when an disinfecting. It has more water, which helps
essentially water-free alcohol is desired. it to dissolve more slowly, penetrate cells,
● Alcohol has been well recognized as a solvent and and kill bacteria.
excipient in the formulation of oral pharmaceutical ● The disinfecting power of rubbing alcohol drops at
products. concentrations higher than 80%-85%.
○ Certain drugs are insoluble in water and ● Each 100 mL must contain not less than 355 mg of
must be dissolved in an alternative vehicle. Sucrose octaacetate or 1.4 mg of denatonium
● Alcohol is often preferred because of its miscibility benzoate, bitter substances that discourage
with water and its ability to dissolve many accidental or abusive oral ingestion.
water-insoluble ingredients, including drug ● According to the Internal Revenue Service, U.S.
substances, flavorants, and antimicrobial Treasury Department, the denaturant employed in
preservatives. rubbing alcohol is formula 23-H
○ Alcohol is frequently used with other ○ Composed of 8 parts by volume of acetone
solvents, such as glycols and glycerin, to ○ 1.5 parts by volume of methyl
reduce the amount of alcohol required. isobutyl/ketone
● It is also used in liquid products as an antimicrobial ○ 100 parts by volume of methyl alcohol
preservative alone or with parabens, benzoates, isobutyl ketone
sorbates and other agents. ○ 100 parts by volume of ethyl alcohol
○ The use of this denaturant mixture makes ● It may also be found in eardrop products, jellies and
the separation of ethyl alcohol from the creams for topical use, in expectorants for congestion,
denaturants virtually impossible with suppositories, and gel capsules.
ordinary distillation apparatus.
○ This discourages the illegal removal for use ISOPROPYL RUBBING ALCOHOL
as a beverage of the alcoholic content
rubbing alcohol. ● First commercial synthetic alcohol
● Denatonium is therefore often used in rubbing ○ Chemists at the Standard Oil Company of
alcohol as an inactive ingredient. New Jersey (later Exxon Mobil) first
● Denatonium benzoate is used to denature ethanol produced it in 1920 while studying petroleum
so that it is not treated as an alcoholic beverage with by-products.
respect to taxation and sales restrictions. ○ It is easily synthesized from the reaction of
● Rubbing alcohol is employed as a rubefacient propylene with sulfuric acid, followed by
externally hydrolysis.
○ soothing rub for bedridden patients ● Isopropyl alcohol is easily oxidized to acetone.
○ germicide for instruments ● about 70% by volume isopropyl alcohol, the
○ skin cleanser prior to injection remainder consisting of water with or without color
○ It is also used as a vehicle for topical additives, stabilizers, and perfume oils.
preparations. ● Isopropyl alcohol is mixed with water for use as a
rubbing-alcohol antiseptic.
GLYCERIN ● It is used in aftershave lotions, hand lotions, and other
● cosmetics.
● Glycerin is a clear syrupy liquid with a sweet taste. ● It is also used as an inexpensive solvent for
● It is miscible with both water and alcohol. cosmetics, drugs, shellacs, and gums, as well as for
● As a solvent, it is comparable with alcohol, but denaturing ethanol (ethyl alcohol)
because of its viscosity, solutes are slowly soluble ● Added to wet gas, it helps to prevent separation and
in it unless it is rendered less viscous by heating. freezing of a water layer.
● Has preservative qualities. ● It is used externally as
● Produced through: ○ A rubefacient
○ Saponification ○ Soothing rub
○ Hydrolysis, ○ and as a Vehicle for topical products
○ and Transesterification of triglycerides ● This preparation and a commercially available 91%
● Synthetic glycerin can be produced by propylene isopropyl alcohol solution are commonly employed by
● USP glycerine is commonly available commercially at diabetic patients in preparing needles and syringes for
anhydrous glycerol content levels of 96%, 99.0% hypodermic injections of insulin and for disinfecting
and 99.5%. the skin.
○ Concentrations above 99.5% are also ● The main difference between isopropyl alcohol and
available commercially. rubbing alcohol is the concentration;
● It is often used as a stabilizer and as an auxiliary ○ Concentration of Isopropyl Alcohol is 100%
solvent in conjunction with water or alcohol. ○ Concentration of Rubbing Alcohol is less
● It is used in many internal preparations. because of the addition of water.
● In the medical and pharmaceutical industries, ○ Otherwise, the two liquids have the same
glycerin is used as a lubricant and humectant. properties: antibacterial and antiseptic.
○ Used for the treatment of severely increased
eye pressure PROPYLENE GLYCOL
● Used in many skin-care products that help prevent
dry skin as moisturizer. ● A colorless, odorless, tasteless and viscous liquid,
● Used for the preparation of cough syrups. is miscible with water and alcohol.
● Used for the production of toothpaste. ● It is a useful solvent with a wide range of applications
● Glycerin is moderately antimicrobial and antiviral and and is frequently substituted for glycerin in modern
can therefore be used for wound treatment. pharmaceutical formulations.
● An 85% glycerin solution is known to show ○ This means that it’s used to dissolve other
bactericidal and antiviral effects and glycerin-treated substances (usually solid) without changing
wounds generally display decreased inflammation their fundamental structure or composition.
after an approximate time frame of 2 hours. ● It can dissolve some substances better than water
● Because of this, it is commonly used in wound care and is also good at retaining moisture.
materials, including hydrogel sheets based on ● Concentrations above 25% v/v in water provide a
glycerin for burns and other wound care products. biostatic function.
○ With the exception of third-degree burns, ● It is used in injectable medications, like lorazepam,
glycerin is licenced for all forms of wound and in some creams and ointments that are applied
treatment and is used to package the donor to the skin, such as corticosteroids.
skin that is used in skin grafts. ● Due to its chemical properties, it is also found in a
○ It can also be noted that there is no wide variety of hygiene and cosmetic products.
authorized topical therapy for third-degree ● Propylene glycol is also used as a carrier in drug
burns and this restriction is also not limited to formulations.
glycerin ○ Active ingredients can be formulated in it and
● Glycerin is used as a sweetener in syrups, lozenges, delivered to the body through it.
and as an excipient in eyewash solutions. ● It is used to dilute and stabilize medicines.
● Used in different forms of drugs including oral drugs ● It is also used for the rinsing of equipment and for the
like capsules and tablets, topical drugs like creams preparation of cleaning solutions.
and gels, and intravenous (injected) drugs.
IX. HOW MOST PHARMACEUTICAL SOLUTIONS ARE
PURIFIED WATER PREPARED
● Naturally occurring water exerts its solvent effect on ● Most pharmaceutical solutions are unsaturated with
most substances it contacts and, thus, is impure, solute.
containing varying amounts of dissolved inorganic ○ Thus, the amounts of solute to be dissolved
salts, usually sodium, potassium, calcium, are usually well below the capacity of the
magnesium, and iron; chlorides; sulfates; and volume of solvent employed.
bicarbonates, along with dissolved and undissolved
organic matter and microorganisms. ● Pharmaceutical solutions are made by dissolving a
● Water in most cities and towns where water is purified solute into a solvent.
for drinking usually contains less than 0.1% of total ○ The solutes can be one or more active
solids, determined by evaporating a 100-mL sample ingredients or excipients that are
to dryness and weighing the residue (which homogeneously dispersed at the molecular
weighs<100 mg). level in the solvent.
● Drinking water must meet the U.S. Public Health ○ The solvent can be a single liquid excipient
Service regulations with respect to bacteriologic or a combination of miscible liquids.
purity. ○ On an industrial scale, solutions are
● Acceptable drinking water should be clear, colorless, prepared in large mixing vessels with ports
odorless, and neutral or only slightly acidic or for mechanical stirrers (Fig. 13.1). When
alkaline. heat is desired, thermostatically controlled
○ The deviation from neutral being due to the mixing tanks may be used.
nature of the dissolved solids and gasses
(carbon dioxide contributing to the acidity ● For oral drug delivery, it is important that the
and ammonia to the alkalinity of water). solvents used are safe for peroral consumption and
● Ordinary drinking water from the tap is not appropriate for complete solubilization of the drug and
acceptable for the manufacture of most aqueous solutes.
pharmaceutical preparations or for the ● Additional excipients may be needed for flavor, color,
extemporaneous compounding of prescriptions sweetening, pH adjustments, preservation, and
because of the possible chemical incompatibilities viscosity.
between dissolved solids and the medicinal agents ● Some chemical agents in a given solvent require an
being added. extended time to dissolve.
● Signs of such incompatibilities are precipitation: ○ To hasten dissolution, a pharmacist may
discoloration, and occasionally effervescence. employ one of several techniques, such as
○ Its use is permitted in washing, in extraction applying heat, reducing the particle size of
of crude vegetable drugs, in preparation of the solute, using a solubilizing agent, and/or
certain products for external use, and when subjecting the ingredients to vigorous
the difference between tap water and purified agitation.
water is of no consequence. ● Most chemical agents are more soluble at elevated
● Naturally, when large volumes of water are required to temperatures than at room temperature or below
clean pharmaceutical machinery and equipment, tap because an endothermic reaction between the
water may be economically employed so long as a solute and the solvent uses the energy of the heat to
residue of solids is prevented by using purified water enhance dissolution.
as the final rinse or by wiping the water dry with a ○ However, elevated temperatures cannot be
meticulously clean cloth. maintained for pharmaceuticals, and the net
● Purified Water, USP, is obtained by distillation, ion effect of heat is simply an increase in the
exchange treatment, reverse osmosis, or other rate of solution rather than an increase in
suitable process. solubility.
● It has fewer solid impurities than ordinary drinking ● An increased rate is satisfactory to the pharmacist
water. because most solutions are unsaturated anyway and
○ When evaporated to dryness, it must not do not require a concentration of solute above the
yield more than 0.001% of residue (1 mg of normal capacity of the solvent at room temperature.
solids per 100 mL of water). ● Pharmacists are reluctant to use heat to facilitate
● It is intended for use in the preparation of aqueous solution, and when they do, they are careful not to
dosage forms except those intended for parenteral exceed the minimally required temperature, for many
administration (injections). medicinal agents are destroyed at elevated
○ Water for Injection, USP; Bacteriostatic temperatures and the advantage of rapid solution may
Water for Injection, USP; or Sterile Water for be completely offset by drug deterioration.
Injection, USP, is used for injections. ○ If volatile solutes are to be dissolved or if the
● It is intended for use in formulation of medicines that solvent is volatile (as is alcohol), the heat
are not intended to be sterile and apyrogenic. would encourage the loss of these agents to
● It is widely used for oral and topical products and in the atmosphere and must therefore be
granulation processes for tablets and capsules. avoided.
● It is also the feed water for the production of water for ● Pharmacists are aware that certain chemical agents,
injection (WFI) and for pharmaceutical grade clean particularly calcium salts, undergo exothermic
steam. reactions as they dissolve and give off heat.
MILLENDEZ, OLAVE, ORTEGA, PANDAN, PARRONE, SALVATIERRA, & TERO
PHA619 LECTURE: SOLUTIONS
○ For such materials, the use of heat would ● Applicable dosage forms are aromatic waters and
actually discourage the formation of a lotions.
solution.
○ The best pharmaceutical example of this PERCENT WEIGHT IN WEIGHT (%w/w)
type of chemical is calcium hydroxide,
● Grams of constituent in 100 g of preparation
which is used in the preparation of Calcium
● Example
Hydroxide Topical Solution, USP. Calcium
○ 1% w/w = 1 g constituent in 100 g
hydroxide is soluble in water to the extent of
preparation
140 mg/100 mL of solution at 25°C (about
● Applicable dosage forms are ointments, creams and
77°F) and 170 mg/100 mL of solution at
suppositories.
15°C (about 59°F).
○ Obviously, the temperature at which the
RATIO STRENGTH
solution is prepared or stored can affect the
concentration of the resultant solution.
● The concentration of weak solutions or liquid
● In addition to or instead of raising the temperature of
preparations is frequently expressed in terms of ratio
the solvent to increase the rate of solution, a
strength.
pharmacist may choose to decrease the particle size
● Ratio strength is merely another way of expressing
of the solute.
the percentage strength of solutions or liquid
○ This may be accomplished by comminution
preparations (and, less frequently, of mixtures of
(grinding a solid to a fine state of
solids).
subdivision) with a mortar and pestle on a
● The ratio and percentage strengths of any solution or
small scale or industrial micronizer on a
mixture of solids are proportional, and either is easily
larger scale.
converted to the other by the use of proportion.
○ The reduced particle size increases the
surface area of the solute.
○ If the powder is placed in a suitable vessel RATIO OF STRENGTH TO WEIGHT IN VOLUME
(e.g., a beaker, graduated cylinder, bottle) (- : — w/v)
with a portion of the solvent and is stirred or ● Grams of constituent in stated milliliters of preparation
shaken, as suited to the container, the rate of ● Example
solution may be increased by the continued ○ 1:1000 w/v = 1 g constituent in 1000 mL
circulation of fresh solvent to the drug’s preparation
surface and the constant removal of newly
formed solution from the drug’s surface.
RATIO OF STRENGTH TO VOLUME IN VOLUME
X. HOW STRENGTHS OF PHARMACEUTICAL
PREPARATIONS ARE EXPRESSED (- : — v/v)
● Milliliters of constituent in milliliters of preparation
● The strengths of pharmaceutical preparations are ● Example
usually expressed in terms of percent strength, ○ 1:1000 v/v = 1 mL constituent in 1000 mL
although for very dilute preparations, expressions of preparation
ratio strength may be used.
RATIO OF STRENGTH TO WEIGHT IN WEIGHT
PERCENTAGE STRENGTH (- : — w/w)
● The symbol % used without qualification (as with w/v, ● Grams of constituent in stated number of grams of
v/v, or w/w) means: preparation
○ Percent weight in volume for solutions or ● Example
suspensions of solids in liquids, and for ○ 1:1000 w/w = 1 g constituent in 1000 g
solutions of gasses in liquids. preparation
○ Percent volume in volume for solutions of
liquids in liquids.
○ Weight in weight for mixtures of solids and
semisolids.
XI. WAYS ORAL SOLUTIONS ARE MADE EXAMPLES OF ORAL SOLUTIONS BY CATEGORY
EXTEMPORANEOUSLY
WAYS DEFINITION
XVI. SYRUPS
● Conc. aqueous preparations of a sugar or sugar
substitute with or without flavoring agents and
medicinal substances.
● Syrups containing flavoring agents but not medicinal
substances are called non medicated or flavored
vehicles (syrups).
● These syrups are intended to serve as
pleasant-tasting vehicles for medicinal substances to
be added in the extemporaneous compounding of
prescriptions or in the preparation of a standard
formula for a medicated syrup, which is a syrup
containing a therapeutic agent
● The inability of some children and elderly people to
swallow solid dosage forms, it is fairly common today
for a pharmacist to be asked to prepare an oral liquid
dosage form of a medication available in the
pharmacy only as tablets or capsules. In these
instances, drug solubility, stability, and bioavailability
must be considered case by case.
● The liquid dosage form selected for compounding
may be a solution or a suspen- sion, depending on
the chemical and physical characteristics of the
particular drug and its solid dosage form.
● Medicated syrups are commercially pre- pared from
the starting materials, that is, by combining each of
the individual components of the syrup, such as
sucrose, purified water, flavoring agents, coloring
agents, the therapeutic agent, and other necessary
and desirable ingredients.
● Syrups provide a pleasant means of administering a
liquid form of a disagreeable-tasting drug. They are
particularly effective in the administration of drugs to
youngsters, since their pleasant taste usually
dissipates any reluctance on the part of the child to
take the medicine.
● Certain flavored syrups have an acidic medium,
whereas others may be neutral or slightly basic, and
the proper selection must be made to ensure the
stabil- ity of any added medicinal agent.
● The most frequently found types of medications
administered as medicated syrups are antitussive
agents and antihistamines
XVIII. SYRUP PREPARATION METHODS ● On a small scale, sucrose and other formulative
agents may be dissolved in purified water by placing
● Syrups are most frequently prepared by one of four the ingredients in a vessel larger than the volume of
general methods, depending on the physical and syrup to be prepared, permitting thorough agitation
chemical characteristics of the ingredients. These of the mixture.
methods include the following: ● This process is more time-consuming than the use of
● Sucrose is the sugar most frequently employed in heat, but the product has maximum stability.
syrups, although in special circumstances, it may be ● Huge glass-lined or stainless steel tanks with
replaced in whole or in part by other sugars or mechanical stirrers or agitators are employed in
substances such as sorbitol, glycerin, and large-scale preparation of syrups.
propylene glycol.
● In some instances, all glycogenetic ADVANTAGE
substances/sucrose based (materials converted to
● For substance that are heat sensitive
glucose in the body), are replaced by non
glycogenetic substances/non-sucrose based,
such as methylcellulose or hydroxyethylcellulose. DISADVANTAGE
○ These two materials are not hydrolyzed and ● Slower
absorbed into the bloodstream, and their use
results in an excellent syrup-like vehicle for ADDITION OF SUCROSE TO A MEDICATED LIQUID OR TO
medications intended for use by diabetic A FLAVORED LIQUID
patients and others whose diet must be
controlled and restricted to non glycogenetic ● Involves the simple mixture of sugar and a
substances prepared medicated liquid, usually a fluid extract
or tincture.
SOLUTION WITH THE AID OF HEAT ● Many such tinctures and fluid extracts contain
alcohol-soluble constituents and are prepared with
● Syrups are prepared by this method when it is desired alcoholic or hydroalcoholic vehicles.
to prepare the syrup as quickly as possible and ● If the alcohol-soluble components are desired
when the syrup’s components are not damaged or medicinal agents, some means of rendering them
volatilized by heat. water soluble is employed.
● In this method, the sugar is generally added to the ● If the alcohol-soluble components are undesirable or
purified water, and heat is applied until the sugar is unnecessary components of the corresponding syrup,
dissolved. they are generally removed by mixing the tincture
○ Then, other heat-stable components are or fluid extract with water, allowing the mixture to
added to the hot syrup, the mixture is stand until separation of the water-insoluble agents is
allowed to cool, and its volume is adjusted to complete, and filtering them from the mixture.
the proper level by the addition of purified ● The syrup prepared through this method is not
water. self-preserving
● If heat labile agents or volatile substances, such as
volatile flavoring oils and alcohol, are to be added, PERCOLATION
they are generally added to the syrup after the
sugar is dissolved by heat, and the solution is ● A percolator or column is utilized.
rapidly cooled down to room temperature. ● The percolator will allow the slow passage of water
through the bed of crystalline sucrose that will
ADVANTAGE eventually dissolve into sugar.
● Either sucrose or the source of the medicinal
● Fast
component may be percolated to form an extractive to
which sucrose or syrup may be added.
DISADVANTAGE ● This method is two (2) separate procedures:
● Excessive heating will cause inversion of sucrose → 1. Preparation of the Extractive of the Drug
glucose + fructose (sweeter, with an increase 2. Preparation of the Syrup
tendency to ferment) PRINCIPLE
○ Will taste more sour upon long-standing for
● When water is added, it will wet the sucrose and it will
several days
slowly be dissolved (principle of maceration)
● Caramelize, yellowish to brownish color
● Once dissolved, it will permeate to the cotton as
○ Caramelization is the process of heating
percolate
sugar at a higher temperature so that the
○ Percolate: clear liquid obtained after
water will be removed and sugar is broken
percolation
down into glucose and fructose and then
● Percolate will flow downward, due to gravity, to the
afterward, it will reform into a complex
receiver
polymer producing a sweet, nutty, or
buttery-flavored and golden brown to dark
XIX. ELIXIRS
brown liquid
● Elixirs are clear, sweetened hydroalcoholic solutions
SOLUTION BY AGITATION WITHOUT THE AID OF HEAT
intended for oral use and are usually flavored to
enhance their palatability.
● To avoid heat-induced inversion of sucrose, a syrup
may be prepared without heat by agitation.
KINDS OF ELIXIRS
VAGINAL SOLUTIONS/DOUCHES
NON-MEDICATED ELIXIRS MEDICATED ELIXIRS
● Used for their hygienic effects
● A few douche powders containing specific therapeutic
Employed as vehicles Employed for the
anti-infective agents such as those mentioned in the
therapeutic benefit of the
discussion of vaginal suppositories are used against
medicinal agent
monilial and trichomonal infections.
● For irrigation and cleansing for vagina
May be useful to the Most official and commercial
● Examples:
pharmacist in the elixirs contain a single
○ Vagisil
extemporaneous filling of therapeutic, meaning the
○ Summer’s eve douche
prescriptions involving dosage of that single drug
○ Norforms
(a) the addition of a may be increased or
○ KY Silk
therapeutic agent to a decreased by simply taking
pleasant-tasting vehicle and more or less of the elixir
(b) dilution of an existing
COMPONENTS:
medicated elixir 1. Boric acid or sodium borate
2. Astringents: potassium, alum, ammonium alum, and
EXAMPLES OF ELIXIRS zinc sulfate
3. Antimicrobials: oxyquinoline sulfate and
EXAMPLES USES povidone-iodine
4. Quaternary ammonium compounds: benzethonium
Antihistamine Useful primarily in the symptomatic chloride
Elixirs relief of certain allergic disorders 5. Detergents: sodium lauryl sulfate
6. Oxidizing agents: sodium perborate
Barbiturate Sedative and hypnotic agents that are 7. Salts: sodium citrate and sodium chloride
Sedative and used to produce various degreesj of 8. Aromatics: menthol, thymol, eucalyptol, methyl
Hypnotic Elixirs central nervous system depression salicylate, and phenol
Phenobarbital ● In low dosage, sedative. rfs RECTAL SOLUTIONS: RETENTION ENEMAS AND
Elixir ● In higher dosage, hypnotics EVACUATION ENEMAS
MISCELLANEOUS SOLUTIONS: AROMATIC WATER ● Since an equal amount of water is 50g, it means the
● Clear, aqueous solutions saturated with volatile oils water measures 50mL
or other aromatic or volatile substances. ● Since the water is equal volume to the other liquid,
○ Aromatic waters are no longer in the liquid also measures 50mL
widespread use. ● Volume represented by 27.39 g of the concentrated
○ Concentration of concentrated HCl and HCl may be similarly determined by dividing the
Diluted HCl weight of the concentrated acid by its specific gravity
and equating the weight of an equal volume of water
MISCELLANEOUS SOLUTIONS: DILUTED ACIDS to the volume of the acid:
● Aqueous solutions prepared by diluting the
corresponding concentrated acids with purified
water.
PREPARATION:
● To prepare a diluted acid from a concentrated one, it ● Since 23.41g measures 24.31 mL and is equal in vol.
is necessary first to calculate the amount of solute ● To the concentrated acid, the latter also measures
required in the diluted product. 23.41 mL, this is the amount required to prepare 100
○ Then the amount of concentrated acid mL of the 10% w/v diluted acid
required to supply the needed amount of ● Once done, this formula may be used to calculate the
solute can be determined. concentrated acid required in the preparation of a
● HCl contains not < 35 g and not more than 38 g of specific volume of the corresponding diluted acid:
solute, therefore considered to be 36.5% w/w
strength on average.
● Diluted hydrochloric acid contains 9.5 to 10.5 g of
solute per 100 mL of solution and is therefore
considered to be approximately 10% w/v in strength.
● If you want to prepare 100 mL of diluted HCl from the DILUTED HCL:
concentrated acid, 10g of solute is needed.
● Recalculating the preparation of 100 mL of diluted
hydrochloric acid from the concentrated acid gives the
following:
EXTRACTS
Concentrated preparations of
vegetable or animal drugs
XXI. COMMON EXTRACTION METHODS obtained by removal of the active
MACERATION constituents of the respective
● A process in which the properly comminuted drug drugs with suitable menstrua,
is permitted to soak in the menstruum until the evaporation of all or nearly all of
cellular structure is softened and penetrated by the the solvent, and adjustment of
menstruum and the soluble constituents are the residual masses or powders
dissolved. to the prescribed standards.
● In the maceration process, the drug to be extracted
is generally placed in a wide-mouthed container
● Extracts are potent preparations, usually between
with the prescribed menstruum, the vessel is
two and six times as potent on a weight basis as the
stoppered tightly, and the contents are agitated
crude drug.
repeatedly over a period usually ranging from 2 to 14
● They contain primarily the active constituents of
days.
the crude drug, with a great portion of the inactive
● The agitation permits the repeated flow of fresh
constituents and structural components of the crude
solvent over the entire surface area of the
drug having been removed.
comminuted drug.
● Their function is to provide in small amounts and
in convenient, stable physical form the medicinal
PERCOLATION
activity and character of the bulkier plants that they
● A process in which a comminuted drug is extracted
represent.
of its soluble constituents by the slow passage of
● As such, they have use in product formulation.
a suitable solvent through a column of the drug.
● In the manufacture of most extracts, percolation is
● The drug is packed in a special extraction
employed to remove the active constituents from the
apparatus termed a percolator, with the collected
drug.
extractive called the percolate.
● Most drug extractions are performed by percolation, a
process whereby coffee is routinely prepared.
● In the process of percolation, the flow of the
menstruum over the drug column is generally
downward to the exit orifice, drawn by the force of
gravity as well as the weight of the column of liquid.
ORAL ADMINISTRATION:
● Teaspoon
● Tablespoon
● Dropper
● Pre Calibrated measuring device