Name:  Recommended by the content for OTC drugs:

Pharmaceutical Dosage  6 to 12 yrs. Of age: 0.5%

Chapter 13: Solutions  Over 12 yrs.: 5%
Solutions  Adults: 10%
 Liquid preparations containing one or more chemical substances  Diluted Alcohol, NF (49%)
dissolved in a suitable solvent or mixture of mutually miscible solvents  Produced by mixing equal amount of water and alcohol
 Prepared from a combination of solid, liquid, and gas  Upon mixing the volume is 3% less because liquids contract
 According to use: oral, otic, ophthalmic, or topical  Hydroalcoholic solvent in pharmaceutical processes and
 According to composition: preparations
 Syrups: aqueous solutions containing sugar  Rubbing Alcohol (79% ethyl alcohol)
 Elixirs: sweetened hydroalcoholic solutions  Other components: denaturants with or without color
 Spirits: solutions of aromatic materials additives, perfume oils, and preservatives
 Tinctures or fluid extracts: active constituents from crude  Composed of 8 parts of volume of acetone, 1.5 parts of
drugs methyl iso-butyl ketone, and 100 parts of ethyl alcohol
 Tincture: alcoholic or hydroalcoholic  Denatorium benazoate is added to prevent accidental or
 Injections: parenteral preparations (sterile and pyrogen-free) abusive ingestion
 Use: rubefacient, soothing rub, germicide, skin cleaner,
 Preparations where the medicinal agents are intended to provide vehicle
systemic effects:  Synonym: alcohol rubbing component
 Oral solutions, syrups, elixirs, spirits and tinctures  Glycerin, USP
 Absorption is rapid than suspension or solid  Clear, syrupy liquid with a sweet taste
dosage forms of the same medicinal agent  Miscible with water and alcohol
 Information utilized in formulation or compounding a  With its viscosity: solutes are slowly soluble
pharmaceutical solution:  Not mixed with oxidizing agents (KMnO4, KClO3): will form
 Solubility and stability of solutes to the solvent an explosive combination
 Avoided in the formulation or compounding:  Preservative, stabilizer and auxiliary solvent, internal
 Combination of medicinal or pharmaceutical preparations
agents resulting in chemical or physical  Isopropyl Rubbing Alcohol
interactions affecting therapeutic quality or  70% by volume isopropyl alcohol and the remainder
stability  Denaturants with or without color additives, perfume oils and
Solubility stabilizers
 Attractive forces between atoms:  Rubefacient, soothing rub, vehicle, preparing needles and
 Lead to formulation of molecules and atoms syringes (diabetic patients) for hypodermic injections of
 Attractive forces between molecules: insulin and skin disinfectant
 Causes them to cohere  Propylene Glycol, USP
 “Like dissolves like”  Viscous liquid miscible with water and alcohol
 Dipole-dipole or Vander Waal’s forces  Useful solvent and substitute for glycerin
 Associated with the weak reactions Solvent for Liquid Preparation
 Saturated solution  Purified Water, USP
 When a solvent at a given temperature has dissolved all of  Naturally occurring water exerts solvent effect on most
the solute substance it contacts (impure) containing amount of:
 Increase in temperature (important factor) increases solubility  Dissolved inorganic salts: Na, K, Ca, Mg, Fe, Cl,
 Factors affecting solubility SO4, & HCO3
 Temperature, pressure and pH, particle size and extent of  Dissolved and undissolved organic mater
agitation  Microorganisms
 Positive heat of solution  Obtained by distillation, ion exchange, and reverse
 Chemicals absorb heat when they are dissolved resulting in osmosis
increased solubility with increased temperature  Ion exchange
o Makes use of filter membranes in
 Negative heat of solution
 Decrease in solubility with a rise in temperature removing contaminants
o Advantages over distillation:
 Solubility expressed as grams of solute dissolving in mL of solvent
(g/mL) permit ease of operation,
Kinds of Solutions minimal maintenance, and more
mobile facility
 Aqueous
 Reverse Osmosis
 Water-based, water as main solvent
o Pressurized steam of water is
 Non-aqueous
 Not water but another solvent passed parallel to the inner side
 Hydroalcoholic: alcohol as main solvent of a filter membrane core
o Elixirs and spirits Preparation of Solution
 Most pharmaceutical preparation solutions
 Oleaginous: oil as main solvent
 Unsaturated with solute
o Liniment and toothache drops
 The strengths of pharmaceutical preparations
 Ethereal: ether as the main solvent
 Expressed in % strength
o Collodion
 For very dilute preparations ration strengths
Solvent for Liquid Preparations
 Several techniques to hasten dissolution
 Alcohol, USP: Ethyl Alcohol, ethanol (94.9 – 96.0% ethanol by volume)
 Applying heat
 Most useful solvent next to water
 Reducing the particle size of the solute
 Hydroalcoholic mixture with water
 Using a solubilizing agent
 Miscible with water
 Subject the ingredients to vigorous agitation
 Dissolve other water-insoluble ingredients
 Solutions intended for oral administration contain
 Used with other solvents: glycols and glycerin to reduce the
 Flavorants and colorants
amount of alcohol required
 When needed:
 Antimicrobial preservative
 Stabilizers of medicinal agents
 Toxic effects when ingested in pharmaceutical products by
children
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  Preservative (prevents growth of
microorganisms)
Oral Solutions and Preparation for Oral Solution
 Dry mixtures for solution or reconstitution
 Number of medicinal agents (antibiotics) with
insufficient stability in aqueous solution to meet extent
shelf-life periods
 7-14 days: expiration date after filling with a suitable
solvent
Example:
 Cloxacilin Sodium for Oral Solution, USP
o Anti-infective
 Penicillin V Potassium for Oral Solution,
USP
o Anti-infective
 KCl for Oral Solution, USP
o K Supplement
 Oral solutions
 Pediatric form of an adult product
 Reconstituting a dry powder mixture/extemporaneously
compound an oral solution from bulk components
 Oral rehydration solutions
 Rapid fluid loss associated with diarrhea lead to:
 Dehydration
 Ultimately death in some patients
particularly the infants
 Effective in treatment of patients with mild volume
depletion 3 to 10% of body weight
 OTC, inexpensive and use diminished the incidence of
complications associated parentally administered
electrolytes solution
 Typical oral rehydration solution contains:
 45 mEq Na, 20 mEq Cl, 30 mEq Citrate and
25 g dextrose
 Never mixed with or given with other electrolyte-
containing liquids:
 Milk
 Fruits
 Commercial oral electrolyte solution:
 Prevents dehydration or achieve rehydration
Examples:
o Pedialyte solution
o Rehydrate solution
 Oral colonic lavage solution
 Administration of oral laxative:
 Magnesium citrate or bisacodyl the night
before
 Cleansing enema administered 2 to 4 hours
prior to the procedure
 Alternative method to prepare the gastrointestinal tract:
 Requires less time and dietary restriction
and obviates cleansing enemas
 Entails oral administration of: balanced
solution of electrolytes with PEG
 Adult dose: 4L, 240 ml per 10 minutes until 4L is
achieved
 Magnesium citrate oral solution
 Citrate or citrate of magnesia
 Colorless to slightly yellow clear effervescent liquid,
sweet acidulous taste and lemon flavor
 Excellent medium for the growth of molds and any
molds spores: must be killed to remain stable
 Always been troublesome:
 Tendency to deposit a crystalline solid upon
standing
 Sodium citrate and citric acid oral solution
 Contains sodium citrate 100 mg and citric acid 67 mg in
each millimeter of aqueous solution
Syrups
 Concentrated aqueous preparations of a sugar or sugar substitute
with or without flavoring agents and medicinal substances
 Serves as:
 Pleasant tasting vehicle for medicinal substances in:
 Extemporaneous compounding of
prescription
 Preparation of a standard formula for a
medicated syrup
 Commercially prepared medicated syrups:
 By combining:
 Sucrose
 Purified water
 Flavoring
 Coloring agents
 The therapeutic agent
 Other ingredients
 Clear aqueous saturated solution of sugar commonly sucrose
 1.313: specific gravity
 85%w/v or 65%w/w
 High osmotic pressure
 Maybe:
 Medicated: with active ingredient
 Non-medicated
Components of Syrup
 Sucrose or sugar substitute
 Provide sweetness and viscosity
 Antimicrobial preservatives
 Flavorants
 Colorants
Sucrose Based and Non-sucrose Based Syrups:
 Sucrose: sugar most frequently employed in syrups
 Special circumstances: replaces by other sugar
substances:
 Sorbitol
 Glycerin
 Prophylene glycol
 Replaced by nonglycogenetic substances
 Methylcellulose or hydroxyl ethylcellulose
 Most syrups contain 60 to 80% sucrose
 Efficient nutrient medium for growth of microorganisms
 Concentrated sugar solution
 Resistant to microbial growth
 Syrup NF 26 (Simple Syrup) prepared by:
 Dissolving 85g of sucrose in purified water to make
100 ml of syrup
Antimicrobial Agent
 The amount of preservative
 Varies with the proportion of water available for
growth:
 Benzoic acid: 0.1-0.2%
 Sodium Benzoate: 0.1-0.2%
 Methylparabens, proplyparabens and
butylparabens, totaling to 1%
Flavorant
 Synthetic flavorant or with naturally occurring materials such as
volatile oils (e.g. orange oil), vanillin, and others
Colorant
 Enhance the appeal of the syrup
 Correlates with the flavorant employed
Method of Preparation of Syrups
 Solution of the ingredients with the aid of heat (fastest)
 Solution of the ingredients with agitation without the use of heat,
or the simple admixture of liquid components (slowest)
 Addition of sucrose to a prepared medicated liquid or to a flavored
liquid
 Percolation of either the source of medicating substance or of the
sucrose
Solution with the Aid of Heat
 Sugar added to the purified water and heat is applied
 Syrup when overheated
 Becomes amber colored as the sucrose caramelizes
 Excessive heating convert syrups into its inversion form
(Excessive heat  Inversion  Caramelization)
 Medicinal agents destroyed by elevated temperature
Solution by Agitation Without Aid of Heat
 Dissolves with purified water
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  Ingredients in a vessel larger than the volume of syrup  Undesirable or unnecessary components of
to be prepared permitting thorough agitation of the corresponding syrup
mixture  Removed by mixing the tincture or fluid extract with
Addition of Sucrose to a Medicated Liquid or to Flavored Liquid water
 Alcohol-soluble components

Table 13.5: Examples of Oral Solutions by Category

Representative Commercial
Oral Solution Concentration of Commercial Product Comments
Products

Antidepressant

Nortriptyline HCl Pamelor Oral Solution (Novartis) 10mg nortriptyline/5ml Tricyclic antidepressant

Fluoxetine HCl Prozac Liquid (Dista) 20mg fluoxetine/5ml For depression, obsessive compulsive disorder

Antiperistaltic

For diarrhea. Diphenoxylate is related structurally and

Diphenoxylate HCl, 2.5mg diphenoxylate HCl, 0.025mg pharcologically to the opioid meperidine. Atropine
Lomotil Liquid (Searle)
atropine sulfate atropine sulfate/5ml sulfate in subtherapeutic amounts discourages (by
virtue of side effects) deliberate overdosage

Imodium A-D Liquid (McNeil For diarrhea in adults and children aged 6 years and
Loperamide HCl 1mg loperamide HCl/5ml
Consumer Products) older. Structurally related to haloperidol.

Antipsychotics

Haloperidol Haloperidol Oral Solution 2mg haloperidol/ml Primarily for severe neuropsychiatric conditions when
oral medication is preferred and tablets and capsules
Perphenazine Perphenazine Oral Solution 16mg perphenazine/5ml are impractical. Concenreted solutions used by adding
desired amount of concentrate bt calibrated dropper to
soup or a beverage.
  Thiothixene HCl Navane concentrate (Pfizer)

Bronchodilator

Alcohol-free solution for treatment of bronchial

Theophylline Oral Solution
Theophylline 80mg theophylline/15ml asthma and reversible bronchospasm associated with
(Roxane)
chronic bronchitis and emphysema.

Cathartics

Magnesium citrate equivalent to 1.55-1.9

Magnesium Citrate, USP   Discussed in text.
g/100ml magnesium oxide

2.4g monobasic sodium phosphate, 0.9g

Sodium phosphate Phospho-Soda (Fleet)  
dibasic sodium phosphate/5ml

Corticosteroid

Synthetic adrenocortical steroid with mainly

Prenisolone sodium 5mg prednisolone (as sodium
Pediapred Oral Solution (Medeva) glucocorticoid properties indicated for endocrine,
phosphate phosphate)/5ml
rheumatic, collagen, allergic, and other disorders.

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Dental caries protectant      

Prophylaxis of dental caries; for use when community

Sodium fluoride Pediaflor Drops (Boss) 0.5 mg/ml
water supply is inadequately fluoridated.

Electrolyte replenisher

For hypopotassemia (low blood level of potassium).

Condition may be prompted by severe or chronic
20 mEq KCl/15ml in flavored aqueous
Potassium chloride KaoChlor 10% Liquid (Adria) diarrhea, low dietary intake of potassium, increased
vehicle
renal excretion of potassium, other causes. Solution is
diluted with water or fruit juice.

Fecal softener

Usually 50-200mg measured by calibrated dropper,

mixed with milk, fruit juice, other liquid to mask taste.
Softens fecal mass by lowering surface tension,
Docusate sodium Colace syrup (Shire) 10mg docusate sodium/ml permitting normal bowel habits, particularly in
geriatric, pediatric cardiac, obstetric, and surgical
patients. Taken for several days or until bowel
movements are normal.

Hematinic

For prevention and treatment of iron deficiency

anemias. Usual propylactic dose 0.3 or 0.6ml,
Fer-In-Sol Drops (Mead Johnson
Ferrous sulfate 15mg/0.6ml measured by calibrated dropper, mixed with water or
Nutritional)
juice. Dosage for intended primarily for infants and
children.

Histamine H2 antagonist

Tagamet HCl Liquid (SmithKline For peptic ulcer disease, pathologic hypersecretory
Cimetidine HCl 300mg/ml
Beecham) conditions, e.g., ZollingerEllison syndrome.

Opioid agonist analgesic

For relief of severe pain; detoxification, maintenance

Methadone HCl Methadone HCl (Roxane) 1 or 2 mg/ml
treatment of opioid addiction.

Vitamin D

Water-insoluble ergocalciferol (vitamin D2) in

propylene glycol. Usual propylactic dose about 400U;
Ergocalciferol Calciferol Drops (Schwarz) 8,000 U/ml
therapeutic dose may be as high as 200,000-500,000
U daily in treating rickets.

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