Name: Pharmaceutical DosageChapter 13: Solutions

Elixirs Clear, sweetened hydroalcoholic solutions for

oral use Less viscous since they contain a lower

proportion of sugar and consequently less effective than syrups

Maintain both water soluble and alcohol soluble components in solutions than aqueous syrups

Excipients: Sweetened with sucrose or sucrose

syrups, some sorbitol, glycerin or artificial sweeteners

High alcoholic content requires artificial sweeteners usually saccharin

Flavorants to increase palatability and coloring agents to enhance their appearance

Kinds of Elixirs Medicated

Elixir with active ingredient Example: terpin hydrate elixir

Non-medicated Useful to the pharmacist's in

extemporaneous filling of Rx involving: Addition of a therapeutic agent Dilution of an existing medicated

elixir Example: iso-alcoholic elixir

Advantages of elixirs over the counterpart solid dosage form:

Flexibility and ease of administration Disadvantage

For patients who choose to avoid alcohol

Preparation of Elixirs By simple solution with agitation Administration of two or more liquid

ingredientsKinds of elixirs

Antihistamine elixirs Useful in the symptomatic relief of certain

allergies disorder Other adverse effects include dryness of

the nose, throat and mouth, dizziness and disturbed concentration

Digoxin elixir Contain 4.5 to 5.25mg of digoxin per 100ml

of elixir Oral adult dose as cardiotonic agent: 1.5

mg on initial and 0.5 as maintenance therapy

Obtained from leaves of digitalis lanataTinctures

Hydroalcoholic solution prepared from vegetable materials or from chemical substances

Have a potency of 10-20% Prepared by simple solution Alcohol content ranging from 15-80%

Protects solution from microbial growth

Never mixed with liquids because the solute may precipitate

Undergo photochemical changes: exposure to light Tightly stoppered Stored in a light-resistant containers

Specific Methods of Preparation of Tincture Simple solution

Chemical substances as active ingredient Example: iodine tincture, thiomerosal

Tincture Percolation

"process P" Example: belladonna tincture

Maceration "process M"

Compound Benzoin Tincture Prepared by maceration in alcohol of 10%

benzoin and lesser amount of aloe, storax, and tolu balsam totaling about 24% of starting material

Used as a protectant to toughen skin in treatment of bed sores, ulcers cracked nipples and tissues of the lips and anus

Serves as delivery vehicle of podophyllum in treatment of visceral warts

Thimerosal Tincture Similar with thimerosal topical solution except

that sodium chloride and sodium borate are absent from the tincture and the vehicle of the tincture is water, acetone and about 50% alcohol

Monoethanolamine and ethylenediamine are used as stabilizers

Effective because of its chelating action on metallic impurities that may be present at time of preparation

Iodine Tincture Sodium iodide reacts with iodine to form

sodium triiodide which prevents formation of ethyl iodide. NaI + I2 --> NaI3

Ethyl iodide will decrease the anti-microbial property of tincture NaI: solubilizing agent

Prepared by dissolving 2% iodine crystals and 2.4% sodium iodide

Advantage: water solution Popular local anti-infective agent Reddish brown stain on the skin Local anti-infective agent: brownish red color

stains on the skinTopical Solutions and Tinctures

Topical solution Employed as an aqueous vehicle Prepared by simple solution dissolving

some by chemical reaction and maceration Topical tinctures

Alcoholic vehicleAluminum Acetate Topical Solution

Colorless and has a faint odor and sweetish, astringent taste used in dermatologic lotions, creams and pastes

Aluminum Subacetate Topical Solution Ratio of aluminum oxide to acetic acid

Subacetate solution: 1:2:3:51

Acetate solution: 1:3:5:2 Subacetate is stronger of the two.

Used as astringent wash and wet dressingCalcium Hydroxide Topical Solution (Lime Water)

More soluble in cold water than hot water Stored in well-filled tightly stoppered

containers to determine the absorption of carbon monoxide and kept in cool places

Only supernatant is dispersed Used as astringent

Sprays Aqueous or oleaginous solutions in the form of

coarse droplets or as finely divided solids applied topically to nasopharyngeal tract or to the skin

Break up a solution into small particles effectively sprayed of to facilitate the spraying of a powder

Advantage over conventional spray Prevents drawback contamination of nasal

fluids into the bottle after administrationVaginal and Rectal Solutions

Vaginal douches For irrigation and cleansing of the vagina

Rectal solutions Retention enemas

Corticosteroids or continuous drip as adjunctive treatment of some patients with ulcerative colitis

Evacuation enemas Used to cleanse the bowel Agents: solution of sodium phosphate and

sodium biphosphate, glycerin and docusate potassium and light mineral oil

Component of Douche Powders Boric acid or sodium borate Astringents: (e.g.) potassium, alum, ammonium

alum, zinc sulfate Antimicrobials: (e.g.) oxyquinolone sulfate,

povidone iodine Quaternary ammonium compounds: (e.g.)

benzethonium chloride Detergents: (e.g) sodium lauryl sulfate Oxidizing agents: sodium perborate Salts: (e.g.) sodium citrate, sodium chloride Aromatics: (e.g.) menthol, thymol, eucalyptol,

methyl salicylate, phenolTopical Oral (Dental) Solutions

Benzocaine: topical anesthetic For temporary relief of pain, soreness,

and irritation in the mouth associated with teeth, orthodontic appliances new or poorly fitting dentures and canker sores

Camphorated parachlorophenol: dental anti-infective

Used in dentistry by sterilization of deep root canals

Carbamide peroxide topical solution: dental anti-infective

Chemo-mechanical cleansing and darkening agent

Cetylpyridinium chloride solution and cetylpyridinium chloride lozenges: local anti-infective

A freshening mouth cleanser

Have benzyl alcohol as a local anesthetic in soothing throat irritations

Erythrosine sodium topical solution and erythrosine sodium soluble tablets

Solution applied to teeth to reveal remaining plaque tablet same affect but not swallowed

Eugenol: dental analgesic Applied topically to dental cavities and

dental protective Pale yellow solution having an aromatic

odor of clove and a spicy taste Lidocaine oral spray: topical dental anesthetic Nystatin oral suspension: antifungal

For oral fungal infections by retaining in the mouth as long as possible before swallowing

Saliva substitutes: electrolytes in a carboxymethylcellulose base

Relief of dry mouth and throat in xerostomia

Sodium fluoride oral solution and tablets: dental caries prophylactic

Applied to the teeth or when drinking water that does not contain adequate fluoride, a dilute solution may be swallowed

Tablets containing sodium fluoride 1.1 or 2.2 mg are chewed or swallowed as required

Sodium fluoride and phosphoric acid gel and sodium fluoride and phosphoric acid topical solution: dental caries prophylactic

Gel and solutions applied to teeth Triamcinolone acetonide dental paste: topical

anti-inflammatory agent Applied to the oral mucous membranes

as a 0.1% pasteMiscellaneous Solutions

Aromatic waters Clear, aqueous solution saturated with

volatile oil or other aromatic or volatile substances

Prepared from a number of volatile substances including orange flower oil, peppermint oil, rose oil, anise oil, spearmint oil, wintergreen oil, camphor and chloroform

Very low solubility in water Used for perfuming and for flavoring

Diluted acids Aqueous solutions prepared by diluting

the corresponding concentrated acids with purified water

Concentrated acid expressed in: percent weight to weight (w/w%): number of grams of solute per 100g of solution

Concentrated HCl Not less than 15g and not more than

38g solute per 100g of acid (36.5%w/w in strength)

Diluted HCl 9.3g and 10.3g solute per 100ml

solution (10%w/v in strength)Spirits

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Alcoholic or hydroalcoholic solutions of volatile substances with or without medicinal substances

High alcoholic concentration: over 60% Pharmaceutically as flavoring agent for

therapeutic value of the aromatic solute Prepared by simple solution, solution by

maceration or distillationMethods of Preparations of Spirits

Simple solution Aromatic ammonia spirit

Maceration Peppermint spirit

Chemical reaction Ethyl nitrite spirit

Distillation Brandy: distillation of fermented fruit of

grapes Whisky: distillation of fermented malt

cereal grainsNon-aqueous Solutions

Liniments Embrocation Medicinal substitution intended to be

rubbed on the skin Alcohol as a vehicle: useful when

rubefacient, counterirritant or penetrating action is desired

Oleaginous liniments are less irritating to the skin than alcoholic liniments

For external use (not to be applied to the broken skin and open wounds)

Applied with rubbingTypes of Liniments

Alcoholic Faster effect Ability to penetrate skin faster To relieve pain Example: Efficascent Oil

Oily Milder action than alcoholic liniment Example: Omega Pain

Non-aqueous Solutions Collodions

A clear or slightly opalescent viscous liquid prepared by dissolving pyroxylin in a 3:1 solvent mixture of ether and alcohol with or without added medicinal substances

For external use: applied to skin with a fine camel’s hair brush or glass applicator, the solvent rapidly evaporates, leaving a filmy residue of pyroxylin

Forms a protectant film on application to the skin and volatilization of the solvent Highly volatile and flammable Useful in holding the edges of an

incised wound together Flexible collodion

Prepared by adding 2% camphor (makes product water proof) and 3% castor oil

Castor oil is the cause of its flexibility Apply the coating over bandages or

stitched incisions to make them water proof and to protect them from external stress

Salicylic collodion 10% solution of salicylic acid in flexible

collodion Used for its keratolytic effects,

especially in removal of corns from the toes

Irritates normal healthy skin Pyroxylin

Soluble gun cotton, collodion cotton Obtained by the action of a mixture of

nitric and sulfuric acids on cotton, consists chiefly of cellulose tetranitrate

1 part soluble in 25 parts of a mixture of 3 volumes of ether and 1 volume of alcohol

Also soluble in acetone and glacial acetic acid

Extraction Withdrawal of desired constituents from

crude drugs through the use of selected solvents in which the desired selected constituents are soluble

Crude drugs: vegetable or animal drugs that have undergone no other processes than collodion, cleaning and drying

Extractives: product of extraction containing varying numbers of constituents

In drug extraction: Menstruum: solvent or solvent mixture

o Hydroalcoholic mixture: inherent protection against microbial contamination and helps prevent separation of extracted material on standing

o Glycerin Cosolvent with water or

alcoholic menstruum and prevent inert materials from precipitating upon standing

Prevents separation of lannin and tannin oxidation products in extractives

Contributes to the stability of pharmaceutical extractive

Marc: plant residue exhaustedExample Preparations Prepared by Extraction Processes

Fluid extract Too potent, too bitter tasting,

unpalatable to be accepted by the patient

Modified by flavorants or sweetening agents

Not used in medical practice Liquid preparations of vegetable drugs

by percolation Use: drug source component of other

liquid dosage 3 processes:

Process A Entails exhaustive percolation with an

alcoholic or hydroalcoholic menstruum Example: senna fluidextract

Process B or D Used in the preparation of fluidextract

with boiling water as the menstruum

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and alcohol generally added to the concentrated percolate as preservative.

A heat resistant or metallic percolator is used.

Example: Aromatic cascara sagrada Process C and E

Intended to facilitate total drug extraction by collecting 1000ml of percolate from each 1000g of drug uses long marrow column of drug and percolation under pressure

Official Preparation Glycyrrhiza fluidextract: Licorice Root

Fluidextract: flavoring agent Eriodietyon fluidextract : Yerba Santa

Fluidextract: cathartic Cascara Sagrada Fluidextract: Rhammus

Pushiana Fluidextract Aromatic Cascara Sagrada Fluidextract Senna Fluidextract – Fluidextractum Sennae

Example Preparations Prepared by Extraction Processes

Extracts Concentrated preparations of vegetable or

animal drugs obtained by the removal of the active constituents of the respective drugs with suitable solvent

Syrupy Add solvent system to drug, either

macerate or percolate Obtain through evaporation

2 to 6 times more potent than crude drug Extract are made in 3 forms:

Syrupy semiliquido 20 ml of solvent system is

remained removing all or most of the menstruum

Pilular plastic consistencyo Plastic consistency, nearly all

solvent has evaporatedo Preferred in compounding a

caustic dosage form: ointment, paste, or pliable material facilitates compounding

Powdered extract: dry extract by removal of all menstruum

o Vegetable drug material which are starchy

o Preferred in compounding of powders capsules and tablets

Extractive Drug products obtained by extracting animal or

vegetable drug with suitable solvent system Methods of preparation:

Maceration: soaking in solvent Decoction: boiling for 15 minutes Percolation: soaking using percolator Infusion: hot or cold water Digestion: applying gentle heat

Nasal Decongestant Solution Treatment of rhinitis of the common cold, for

sinusitis

Table 13.8: Examples of Medicated Elixirs by CategoryElixir Commercial Product Comments

Adrenocortical steroid Dexamethasone

Dexamethasone Elixir Synthethic analogue of hydrocortisone,

about 30 times more potent. Commercial elixir is packaged with a calibrated dropper for accurate measurement of small doses; intended primarily for children; also has utility for adults with trouble swallowing tablets. Used for many indications: rheumatoid arthritis, skin disease, allergies, inflammatory conditions. Commercial product contains 5% alcohol.

Analgesic, antipyretic Acetaminophen Children’s Tylenol Elixir Reduction of pain and lowering of fever

particularly in patients sensitive to or unable to take aspirin. Elixir especially useful for pediatric patients and is alcohol free.

Anticholinergic,antispasmodic Hyoscyamine sulfate Levsin Elixir Used to control gastric secretions, visceral

spasm, hypermotility, abdominal cramps. Commercial product contains 20%

Antihistamine Diphenhydramine HCl Elixir Diphenhydramine HCl Elixir Antihistamines are used for a variety of

allergic reactions e.g. perennial and seasonal allergic rhinitis, allergic skin manifestations of urticaria. Reactions of insect bites. Commercial product contains 5.6% alcohol.

Antipsychotic Fluphenazine HCl Fluphenazine HCl Elixir Management of psychotic disorders.

Cardiotonic

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Digoxin Lanoxin Pediatric Elixir Among other effects, increase force of myocardial contraction. Used in congestive heart failure, atrial fibrillation, other cardiac conditions. Commercial product contains 10% alcohol.

Sedative, hypnotics Butabarbital sodium

Phenobarbital

Butisol sodium Elixir

Phenobarbital Elixir

In low dosage, sedatives;in higher dosage,hypnotics. Butabarbital sodium elixir contains 7% alcohol; Phenobarbital elixir contains 14% alcohol.

Table 13.9: Examples of Solutions Applied to SkinSolution Corresponding

Commercial ProductVehicle Category and Comments

Aluminum acetate - Aqueous AstringentAluminum subacetate - Aqueous AstringentCalcium hydroxide (limewater)

- Aqueous Astringent

Chlorhexidine Gluconate

Hibiclens Skin Cleanser (Stuart)

Skin wound and general skin cleanser, surgical scrub, preoperative skin preparation. Effective for gram-positive and gram-negative bacteria such as Pseudomonas aeruginosa.

Clindamycin phosphate Cleocin T topical Solution (Pharmacia & Upjohn)

Isopropyl alcohol, water Treatmentof acne vulgaris.

Clotrimazole Lotrimin Solution (Schering)

PEG 400 Antifungal

Coal tar (liquor carbonis detergens; LCD)

- Alcohol Antieczematic; antipsoriatic

Erythromycin Erymax Topical Solution (Allergan Helbert)

Polyethylene glycol/ acetone/ alcohol

Treatment of acne vulgaris.

Fluocinolone acetonide Synalar Topical Solution (Syntex)

Propylene glycol Adrenocortical steroid (topical anti-inflammatory)

Fluorouracil Efudex Topical Solution (Roche)

Propylene glycol Antineoplastic (actinic keratoses)

Hydrogen peroxide - Aqueous Topical anti-infectiveHydroquinone Melanex Topical

Solution (Neutrogena Dermatologies)

Water, alcohol, propylene glycol

temporary bleaching of hyperpigmented skin, e.g., chloasma, melasma

Minoxidil Rogaine Topical Solution (Pharmacia & Upjohn)

Alcohol, water, propylene glycol

Long-term topical treatment of male pattern baldness by stimulating hair growth.

Povidone iodine Betadine Solution (Purdue Frederick)

Aqueous Topical anti-infective

Tolnaftate Tinactin Solution (Schering-Plough)

Polyethylene glycol Topical antifungal

Table 13.10: Examples of Tinctures Applied to the SkinTincture Vehicle Category and Comments

Green Soap Tincture Alcohol Detergent. Also contains 2% lavender oil as perfume.

Iodine Tincture Alcohol, water Topical anti-infectiveCompound Benzoin Tincture Alcohol Topical protectant. Prepared by

maceration in alcohol.

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Pharmaceutical DosageChapter 13 – Quiz: Try it!

Identify:(1) _______________ Clear, sweetened hydroalcoholic solutions for oral use(2) _______________ Alcoholic or hydroalcoholic solutions of volatile substances with or without medicinal

substances(3) _______________ Clear, aqueous solution saturated with volatile oil or other aromatic or volatile substances(4) _______________ Aqueous solutions prepared by diluting the corresponding concentrated acids with purified

water(5) _______________ Drug products obtained by extracting animal or vegetable drug with suitable solvent system(6) _______________ Concentrated preparations of vegetable or animal drugs obtained by the removal of the active

constituents of the respective drugs with suitable solvent(7) _______________ Aqueous or oleaginous solutions in the form of coarse droplets or as finely divided solids

applied topically to nasopharyngeal tract or to the skin(8) _______________ Hydroalcoholic solution prepared from vegetable materials or from chemical substances(9) _______________ Treatment of rhinitis of the common cold, for sinusitis

Matching Type:Set 1

(A) Calcium Hydroxide Topical Solution (Lime Water)(B) Compound Benzoin Tincture(C) Thimerosal Tincture(D) Aluminum Acetate Topical Solution(E) Iodine Tincture(F) Aluminum Subacetate Topical Solution(G) Vaginal douches(H) Evacuation enemas(I) Rectal solutions

(a) ___ Serves as delivery vehicle of podophyllum in treatment of visceral warts(b) ___ Used as a protectant to toughen skin in treatment of bed sores, ulcers cracked nipples and tissues of the

lips and anus(c) ___ Stored in well-filled tightly stoppered containers to determine the absorption of carbon monoxide and kept

in cool places(d) ___ For irrigation and cleansing of the vagina(e) ___ Retention enemas(f) ___ Popular local anti-infective agent(g) ___ Colorless and has a faint odor and sweetish, astringent taste used in dermatologic lotions, creams and

pastes(h) ___ Monoethanolamine and ethylenediamine are used as stabilizers(i) ___ Effective because of its chelating action on metallic impurities that may be present at time of preparation(j) ___ Used as astringent(k) ___ Used as astringent wash and wet dressing(l) ___ Used to cleanse the bowel

Set 2(A) Aromatics(B) Astringents (C) Antimicrobials (D) Quaternary ammonium compounds (E) Detergents (F) Oxidizing agents(G) Salts(H) Component of douche powders

(a) ___ Oxyquinolone sulfate, povidone iodine(b) ___ Boric acid or sodium borate(c) ___ Sodium citrate, sodium chloride(d) ___ Benzethonium chloride(e) ___ Sodium perborate(f) ___ Sodium lauryl sulfate(g) ___ Menthol, thymol, eucalyptol, methyl salicylate, phenol

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(h) ___ Potassium, alum, ammonium alum, zinc sulfate

Set 3(A)Benzocaine(B)Camphorated parachlorophenol(C)Carbamide peroxide topical solution(D) Cetylpyridinium chloride solution and cetylpyridinium chloride lozenges(E)Erythrosine sodium topical solution and erythrosine sodium soluble tablets(F) Eugenol(G) Lidocaine oral spray(H) Nystatin oral suspension(I) Saliva substitutes(J) Sodium fluoride oral solution and tablets(K)Triamcinolone acetonide dental paste(L) Sodium fluoride and phosphoric acid gel and sodium fluoride and phosphoric acid topical solution

(a)___ Topical anti-inflammatory agent(b)___ Topical anesthetic(c) ___ Electrolytes in a carboxymethylcellulose base(d)___ Dental anti-infective(e)___ Local anti-infective(f) ___ Dental caries prophylactic(g)___ Dental analgesic(h)___ Topical dental anesthetic

Odd Man Out: Put a check that does not belong to the group.(A) ___ Adrenocortical steroid ___ Children’s Tylenol ___ Elixir ___ Dexamethasone Elixir(B) ___ Phenobarbital ___ Butisol Sodium Elixir ___ Hypnotics ___ Fluphenazine HCl(C) ___ Antipsychotic ___ Hyoscyamine sulfate ___ Anticholinergic ___ Levsin Elixir(D) ___ Anticholinergic ___ Children’s Tylenol Elixir ___ Antipyretic ___ Acetaminophen(E) ___ Detergent ___ Alcohol, water ___ Green Soap ___ Tincture Alcohol

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