Pharmaceutical compounding I - WordPress.com · Pharmaceutical compounding I ... 2/5/2017 Pharmaceutical Compounding 17 Liniments ... • Advantages of extractives

University of Sulaimani School of Pharmacy Dept. of Pharmaceutics Pharmaceutical Compounding

Pharmaceutical compounding I Solutions using mixed solvent systems: Spirits, Elixirs and Extracted Products

Dr. rer. nat. Rebaz H. Ali

2/5/2017 Pharmaceutical Compounding 2

Outlines

• Spirit

• Elixir

• Miscellaneous liquid preparations

• Extracted products


Spirit

• Spirits are alcoholic or hydroalcoholic solutions of volatile substances. The volatile

substances in the majority of cases are volatile oils.

• The volatile oil content of the official spirits is much greater than of the corresponding

aromatic waters.

• The alcohol content varies from the lower percentage as in Ammonia Spirit 62-68%, to

the highest percentage as in Camphor Spirit 80-87%.

• When mixed with water or with an aqueous preparation, they form a milky preparation.

• For medicinal purposes, spirits may be taken orally, applied externally, or used by

inhalation.

• Depending on the materials, spirits may be prepared by simple solution, solution by

maceration, or distillation.


Official spirits

• Peppermint spirit: is used as a carminative and flavor. Given orally in small doses

usually 1 ml.

• Preparation:

• Leaves are macerated in water to remove tannins,

xanthophylls, and other principles soluble in water, this

aqueous extract is discarded.

• The leaves are expressed and then macerated in alcohol.

The alcohol dissolves the chlorophyll so that the final

product has a bright green color.


Official spirits

• Aromatic Ammonia spirit: is prepared from ammonium carbonate and strong

ammonia.

• It is used orally as an antacid and carminative, is also used as a stimulant to revive

conscious state after fainting, through inhalation.


Official spirit cont.

• Camphor spirit: this is a simple solution of 10% of camphor in alcohol.

• Usually it's applied to cold sores.

• It could be used in case of insect bite, muscle pain, and to relieve cough.


Outlines

• Spirit

• Elixir




Elixir

• Elixirs

• They are sweetened hydroalcoholic solutions containing flavoring materials and,

usually, medicinal substances.

• In the official elixirs, the alcohol content varies from 4 to 40 percent; which is

enough alcohol to keep volatile oils or the medical substances in solution.

• The sugar content in elixir is lower than that of syrups.

• Elixirs are usually less sweet and less viscous and are less effective than syrups in

masking the taste of medicinal substances.

• Because of their hydroalcoholic character, elixirs are

better able than aqueous syrups to maintain both

water-soluble and alcohol-soluble components in

solution.


Elixir cont.

• Elixirs containing more than 10% to 12% of alcohol are usually self-preserving and

do not require the addition of an antimicrobial agent.

• Elixirs should be stored in tight, light-resistant containers and protected from excessive

heat

• A disadvantage

• For children and for adults who choose to avoid alcohol is their alcoholic content.

• Nonmedicated Elixir

• Addition of a therapeutic agent.

• Dilution of an existing medicated elixir.


Elixir cont.

• Medicated Elixir

• Most official and commercial elixirs contain a single therapeutic agent.

• Antihistaminics; like Chlorpheniramine Maleate, Diphenhydramine HCl.

• Sedative and Hypnotics: like Phenobarbital, Secobarbital.

• Expectorants: like Terpin hydrate, Terpin Hydrate and Codeine.

• These elixirs cannot be diluted with much water or the slightly water-soluble

terpin hydrate will precipitate.

• These elixirs contain the highest percentage of alcohol (39 to 44%) of all elixirs in

order to keep the terpin hydrate in solution.

• Miscellaneous: digoxin, dexamethasone, acetaminophen, hyoscyamine sulfate


Outlines

• Spirit

• Elixir


• Douches

• Enemas

• Liniments

• Collodions



Douches

• Douches are an aqueous solution directed against a part or into a

cavity of the body. It functions as a cleansing or antiseptic agent.

• Pharyngeal douches are used to prepare the interior of the throat

for an operation and cleanse it in suppurative conditions.

• Douches are often dispensed in the form of a powder with

directions for dissolving in a specified quantity of water (usually

warm).

• Vaginal douches are the most common type of douche and are used

for cleansing the vagina and hygienic purposes.


Douches cont.

• The ingredients used in vaginal douches:

• Antimicrobial agents, such as benzalkonium chloride, the parabens,

• Anesthetics or antipruritics, such as phenol or menthol.

• Astringents, such as zinc sulfate or potassium alum,

• Chemicals to alter the pH, such as sodium bicarbonate or citric acid.

• Aromatics, for example, menthol, thymol, eucalyptol.


Outlines

• Spirit

• Elixir


• Douches

• Enemas

• Liniments

• Collodions



Enemas

• Enemas are solutions administered rectally for the local effects of the medication

(e.g., hydrocortisone) or for systemic absorption (e.g., aminophylline).

• Corticosteroids are administered as retention enemas as adjunctive treatment of

some patients with ulcerative colitis.

• Also they may possess anthelmintic, nutritive, sedative, or they may contain

radiopaque substances for examination of the lower bowel.


Enemas

• For evacuation enema, Sodium chloride, sodium bicarbonate,, glycerin, docusate

potassium, and light mineral oil are used in enemas to evacuate the bowel.

• They could be used alone or in combination with irritants, such as soap.


Liniments

• Liniments are alcoholic or oleaginous solutions or emulsions of various medicinal

substances intended to be rubbed on the skin.

• Liniments with an alcoholic or hydroalcoholic vehicle are useful when rubefacient,

counterirritant, or penetrating action is desired.

• Oleaginous liniments are employed primarily when massage is desired.

• All liniments should bear a label indicating that they are suitable only for external use

and must never be taken internally.

• Other liniments contain antipruritics, astringents, emollients, or analgesics


Collodions

• Collodion is a clear or slightly opalescent viscous liquid prepared by dissolving pyroxylin

(4%w/v) in a 3:1 mixture of ether:alcohol.

• The solution is highly volatile and flammable

• Pyroxylin is a mixture of nitric and sulfuric acids on cotton

• It has the appearance of raw cotton when dry but is harsh to the touch.

• Collodions are intended for external use.

• When applied to the skin the solvent rapidly evaporates,

leaving a filmy residue of pyroxylin.


Collodions cont.

• This provides an occlusive protective coating to the skin

• Salicylic acid collodion is a 10% solution of salicylic acid in flexible collodion.

• It is used for its keratolytic effects, especially in the removal of corns from the

toes.


Outlines

• Spirit

• Elixir



• Extraction methods

• Tincture, fluidextract, extract and resin


Extracted products

• Crude drugs are vegetable or animal drugs that have undergo no other processes

than collection, cleaning, and drying.

• Tinctures, fluidextracts, and extracts are the pharmaceutical products most

commonly prepared from extractives.

• Advantages of extractives

• Extraction concentrates the active constituents of a crude drug and removes

from it the unwanted matter.

• More potent

• More palatable

• More conveniently for administration

• Comminution of the crude is often desirable.


Extracted products cont.

• For extraction, use of water alone is discouraged:

• Most active plant constituents are complex organic chemical compounds that

are less soluble in water.

• It dissolves undesirable constituents like starches, coloring principles, and

tannins.

• It serves as good growth media for molds, yeasts, and bacteria.

• Hydroalcoholic mixtures are the most widely employed menstrua.

• Methods of extraction

• Maceration

• Percolation


Extraction methods

A. Maceration

• It is a process in which the 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.

• For drugs containing little or no cellular material, such as aloe, and Tolu, which

dissolve almost completely in the menstruum, maceration is the most efficient

method of extraction.

• After the appropriate time has elapsed, the system is

filtered to remove undissolved material.

• The solvent used is called the menstruum, and the

undissolved portion is called the marc.


• One approach suggested to overcome this difficulty is to enclose the crude drug in a

permeable membrane or sack, as in a tea bag.

• Decoction; involves placing plant material in water, boiling for about 15 minutes, and

expressing and straining the remaining marc to obtain a maximum amount of water-

soluble principles.

Extraction methods cont.


• Digestion: is maceration with continued heating, the temperature is usually maintained

between 40 and 60 oC.

• Infusion: is macerating the drug with cold water followed by the addition of boiling

water.


B. Percolation

• Percolation is as a process in which a comminuted drug is

extracted of its soluble constituents by the slow passage of a

suitable solvent through a column of the drug.

• The extraction apparatus termed a percolator, with the collected

extractive called the percolate


• Percolation offers the opportunity to extract principles exhaustively with a minimum of

solvent.

• Exhaustive extraction can be monitored by:

• Loss of color in extracted solvent system.

• Loss of bitter taste characteristic of alkaloids.



Outlines

• Spirit

• Elixir



• Extraction methods

• Tincture, fluidextract, extract and resin


Tinctures

• Tinctures are defined in the USP as alcoholic or hydroalcoholic solutions prepared

from vegetable materials or from chemical substances (Iodine Tincture).

• When they are prepared from chemical substances (iodine), tinctures are prepared

by simple solution.

• When they prepared from vegetable , it prepared by maceration and percolation.

• The potency is 10%

• Cardamom tincture: carminative and flavor

• Belladonna tincture: antispasmodic


Fluidextracts

• The USP defines fluidextract is a liquid preparations of vegetable drugs, containing

alcohol as a solvent or as a preservative, or both.

• Each mL contains the therapeutic constituents of 1 g of the standard drug that it

represents.

• Senna fluidextract: used as purgative.

• Belladonna fluidextract:

• Glycyrrhiza fluidextract:

• It is able to moisten the mucous membranes, which includes the respiratory

system, the urinary tract and the digestive system.


Extracts

• Extracts are concentrated of animal or vegetable drugs which first have been extracted.

• They are potent preparations, usually 2 to 6 times as potent as a weight basis as the

crude drug.

• In most cases, after percolation the volume is reduced by evaporation of solvent.

• The extent of removal of the solvent determines the final physical character of the

extract:

• Semi-liquid extracts with a syrup consistency.

• Pilular extracts with a plastic consistency; like Pure

Clycyrrhiza Extract.

• Powdered extracts, brought to complete dryness; like

Cascara Sagrata Extract

• Relief constipation


Extracts cont.

• For potent products, adjustment of potency is accomplished by the addition of inert

diluents.

• Liquid glucose is often used for the pilular extracts

• Starch is added to powdered extracts.


Resins

• Resins are solid preparations consisting of the resinous constituents of vegetable

matter.

• They are soluble in alcohol and in most organic solvents but insoluble in water.

• Alcoholic solution is concentrated and poured into water.

• The precipitated resin, subsequently washed with water, dried and powdered.

• Podophyllum resin is a cytotoxic agent and is used to treat the genital warts.


Resins

• Oleo resins are combinations of volatile oils and naturally occurring resins and are

generally found by cutting into the trunks of trees in which they occur.

• Capsicum oleoresin

• Capsaicin is used in medicated creams and lotions to relieve muscle or joint pain


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