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Liquid Dosage Forms

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Title: Liquid Dosage Forms


1
Liquid Dosage Forms
2
1. Pharmaceutical Solutions
3
Solutions are Dosage forms prepared by
dissolving the active ingredient(s) in an
aqueous or non aqueous solvent.
4
Solutions can be formulated for different routes
of administration Orally Syrups, elixirs,
drops In mouth and throat Mouth washes,
gargles,
throat sprays. In body cavities Douches,
enemas, ear drops,
nasal sprays. On body Surfaces Collodions,
lotions.
5
Advantages of SoIutions (1) Easier to swallow
therefore easier for children - old age -
unconscious people. (2) More quickly effective
than tablets and capsules. (3) Homogenous
therefore give uniform dose than suspension
or emulsion which need shaking. (4) Dilute
irritant action of some drugs (aspirin, Kl, KBr)
minimize adverse effects in the GIT like KCl.
6
  • Disadvantages of SoIutions
  • Bulky therefore difficult to transport and
    store.
  • (2) Unpleasant taste or odours are difficult to
    mask.
  • (3) Needs an accurate spoon to measure the dose.
  • (4) Less stable than solid dosage forms.
  • major signs of instability
  • colour change,
  • precipitation
  • microbial growth
  • chemical gas formation

7
  • Additives
  • Buffers
  • To resist any change in pH
  • Isotonicity modifiers
  • Solutions for injection
  • Application to mucous membrane
  • Large-volume solutions for ophthalmic
    application
  • Most widely used isotonicity modifiers are
    dextrose and NaCl
  • Viscosity enhancement
  • It is difficult for aqueous-based topical
    solutions to remain on the skin or in the eye
    (why?) therefore low concentrations of jelling
    agents are added to increase the viscosity of the
    product.

8
  • Preservatives
  • Solution may become contaminated for a number of
    reasons
  • Raw materials used in the manufacture of
    solutions are excellent growth media for
    bacterial substances such as gums, dispersing
    agents, sugars and flavors
  • Equipment, environment and personnel contribute
    to product contamination.
  • Consumer use may result in the introduction of
    microorganism.
  • ? a preservative should be added to the
    product
  • Preservative used should be
  • effective against a wide spectrum of
    microorganisms
  • stable for its shelf life
  • non toxic, non sensitizing
  • compatible with the ingredients in the dosage
    form
  • free of taste and odour

9
  • Preservatives may be used alone or in combination
    to prevent the growth of microorganisms.
  • Alcohols
  • Ethanol is useful as a preservative when it is
    used as a solvent.
  • It needs a relatively high concentration (gt
    10) to be effective.
  • Propylene glycol also used as a solvent in oral
    solutions and
  • topical preparations. It can function as a
    preservative in the
  • range of 15 to 30. It is not volatile like
    ethanol.
  • Acids
  • Benzoic acid and sorbic acid have low solubility
    in water.
  • They are used in a concentration range from 0.1
    to 0.5.
  • Only the non-ionized form is effective and
    therefore its use is
  • restricted to preparations with a pH below
    4.5 (WHY?).

10
  • Esters
  • Parabens are esters (methyl, ethyl, propyl and
    butyl) of p-hydroxybenzoic acid.
  • They are used widely in pharmaceutical products
    and are effective and stable over a pH range of 4
    to 8.
  • They are employed at concentrations up to about
    0.2. Frequently 2 esters are used in combination
    in the same preparation WHY?
  • To achieve a higher total concentration
  • To be active against a wider range of
    microorganisms.
  • Quaternary Ammonium Compounds
  • Benzalkonium chloride is used at a relatively low
    concentration 0.002 to 0.02.
  • This class of compounds has an optimal activity
    over the pH range of 4 to 10 and is quite stable
    at most temperatures.
  • Because of the cationic nature of this type of
    preservative it is incompatible with many anionic
    compounds.

11
  • Antioxidants
  • Vitamins, essential oils almost all fats and
    oils can be oxidized. Oxidation reaction can be
    initiated by
  • 1. heat maintain oxidizable drugs in a cool
    place
  • 2. light use of light- resistant container
  • 3. heavy metals (e.g. Fe, Cu) effect of trace
    metals can be
  • minimized by using citric acid or
    ethylenediamine tetraacetic
  • acid (EDTA) i.e. sequestering agent .
  • Antioxidants as propyl octyl esters of gallic
    acid, tocopherols or vitamin E, sodium sulfite,
    ascorbic acid (vit. C) can be used.
  • Sweetening agents
  • Sucrose is the most widely used sweetening agent.
  • Advantages Colourless, highly water soluble,
    stable over a wide pH range (4-8), increase the
    viscosity, masks both salty and bitter taste, has
    soothing effect on throat.
  • Polyhydric alcohols (sorbitol, mannitol and
    glycerol) possess sweetening power and can be
    used for diabetic preparations.

12
  • Flavours and perfumes
  • Mask unpleasant taste or odour
  • Enable the easy identification of the product.
  • Natural products fruit juices, aromatic oil
    (peppermint, lemon)
  • Artificial perfumes are cheaper, more readily
    available and
  • more stable than natural products.

13
Stability of solutions Both physical and chemical
stability of solutions in their containers is
very important A solution must retain its
clarity, colour, odour, taste and viscosity over
its shelf life.
14
Classification of Solutions According to Vehicle
(a) Aqueous solutions (b) Non-aqueous
solutions Aqueous Solutions Aqueous
solutions are homogeneous mixtures that are
prepared by dissolving a solid, liquid or gas in
an aqueous medium (vehicle). Vehicle This may
be water, aromatic water or extracts.
15
WATER Water is used both as vehicle and as a
solvent for the desired flavoring or medicinal
ingredients. Advantages Tasteless, odourless,
lack of pharmacological activity, neutral and
very cheap Tap Water It is not permitted to
use tap water for the dispensing of
pharmaceutical dosage forms due to its possible
bacterial contamination and the presence of
dissolved salts that destroy the active
ingredients or enhance their decomposition.
Freshly Boiled and Cooled Water Boiling is
seldom used to destroy vegetative bacteria. But,
on storage for long time spores may yield
vegetative microorganism.
16
  • Purified Water
  • Must be used for most pharmaceutical operations
    and in all the tests and assays.
  • Such water is prepared by distillation,
    deionization or reverse osmosis.
  • "Hard" waters are those that contain the Ca and
    Mg cations.
  • Alkaline" waters are those that contain
    bicarbonates as the major impurity.
  • Ultraviolet energy, heat or filtration (Millipore
    filtration) can be used to remove or kill the
    microorganisms present in the water.
  • Water for injection
  • Must be used for the formulation of parental
    solutions.
  • It is obtained by sterilizing pyrogen-free
    distilled water.

17
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18
  • Aromatic Waters
  • Aromatic waters (medicated waters) are clear,
    saturated aqueous solution of volatile oils or
    other aromatic or volatile substances.
  • They are used principally as flavored or perfumed
    vehicles.
  • Volatile oils solutions represent an
    incompatibility problem of
  • salting out. This occurs after the
    incorporation of a very soluble
  • salt in their solution.
  • Aromatic water will deteriorate with time
    therefore
  • - should be made in small quantities
  • - protected from intense light and excessive
    heat by storing
  • in air tight, light resistant containers.
  • If they become cloudy or otherwise deteriorate
    they should be
  • discarded. Deterioration may be due to
    volatilization, decomposition or mould growth.
  • There are 2 official methods of preparation

19
  • (a) Distillation process (Stronger Rose Water NF)
  • Adv. most satisfactory method Dis. slow
    and expensive
  • The drug should be coarsely ground and mixed with
    sufficient
  • quantity of purified water in the
    distillation unit.
  • After distillation any excess oil in the
    distillate is removed by
  • filtration.
  • Drug should not be exposed to the action of
    direct heat during
  • distillation otherwise, the odour of the
    carbonized substance
  • will be noticeable in the distilled aromatic
    water.
  • If the volatile principle in the water are
    present in small
  • quantities the distillate is returned several
    times to the still with
  • fresh portions of drug.
  • (b) Solution process (Peppermint water)
  • Aromatic water may be prepared by shaking
    volatile substance with purified water. The
    mixture is set aside for 12 hours filtered.
    Talc (inert) may be used to increase the surface
    of the volatile substance, insure more rapid
    saturation of the water and act as a filter aid.

20
  • Methods of Preparation of Solutions
  • (a) Simple Solution
  • (b) Solution by Chemical Reaction
  • (c) Solution by Extraction
  • (a) Simple Solution
  • Solutions of this type are prepared by dissolving
    the solute in a suitable solvent (by stirring or
    heating).
  • The solvent may contain other ingredients which
    stabilize or solubilize the active ingredient
    e.g. solubility of Iodine is 1 2950 in water
    however, it dissolves in presence of KI due the
    formation of more soluble polyiodides (KI.I2
    KI.2I2 KI3.I3 KI.4I4) . Strong Iodine
    Solution USP (Lugol's SoIution).

21
(b) Solution by Chemical Reaction These solutions
are prepared by reacting two or more solutes with
each other in a suitable solvent e.g. Calcium
carbonate and lactic acid used to prepare Calcium
lactate mixture. WHY? (c) Solution by
Extraction Plant or animal products are prepared
by suitable extraction process. Preparations of
this type may be classified as solutions but more
often, are classified as extractives. Extractives
will be discussed separately.
22
  • Pharmaceutical Solutions
  • Aqueous
  • Douches
  • Enemas
  • Gargles
  • Mouthwashes
  • Nasal washes
  • Juices
  • Sprays
  • Otic solutions
  • Inhalations
  • Sweet /or Viscid
  • Syrups
  • Honeys
  • Mucilages
  • Jellies
  • Nonaqueous
  • Elixirs
  • Spirits
  • Collodions
  • Glycerins
  • Liniments
  • Oleo Vitamin

23
Aqueous Pharmaceutical Solutions
24
  • Douches
  • Douche is an aqueous solution, which is directed
    against a part or into a cavity of the body.
  • It functions as a cleansing or antiseptic agent.
  • Eye douches are used to remove foreign particles
    and discharges from the eyes. It is directed
    gently at an oblique angle and is allowed to run
    from the inner to the outer corner of the eye.
  • Pharyngeal douches are used to prepare the
    interior of the throat for an operation and to
    cleanse it in supportive conditions.
  • Similarly, there are nasal and vaginal douches.
  • Douches most frequently dispensed in the form of
    a powder with directions for dissolving in a
    specified quantity of water.

25
  • Enemas
  • These preparations are rectal injections employed
    to
  • evacuate the bowel (evacuation enemas),
  • influence the general system by absorption
    (retention enemas) e.g. nutritive, sedative or
    stimulating properties
  • affect locally the site of disease (e.g.
    anthelmintic property)
  • they may contain radiopaque substances for
    roentgenographic examination of the lower bowel.
  • Retention enemas are used in small quantities
    (about 30ml) and are thus called retention
    microenema.
  • Starch enema may be used either by itself or as a
    vehicle for other forms of medication

26
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27
  • Gargles
  • Gargles are aqueous solutions frequently
    containing antiseptics, antibiotics and/or
    anesthetics used for treating the pharynx
    (throat) and nasopharynx by forcing air from the
    lungs through the gargle, which is held in the
    throat subsequently, the gargle is expectorated.
  • Many gargles must be diluted with water prior to
    use. Although mouthwashes are considered as a
    separate class of pharmaceuticals many are used
    as gargles, either as is, or diluted with water.
  • The product should be labeled so that it cannot
    be mistaken for preparations intended for
    internal administration.

28
  • Mouthwashes
  • Mouthwashes can be used for therapeutic
    cosmetic purposes
  • Therapeutic mouthwashes can be formulated to
    reduce plaque, gingivitis, dental caries and
    stomatitis.
  • Cosmetic mouthwashes may be formulated to reduce
    bad breath through the use of antimicrobial
    and/or flavoring agents.
  • Mouthwashes are used as a dosage form for a
    number of specific problems in the oraI cavity
    e.g.
  • mouthwashes containing
  • combination of antihistamines, hydrocortisone,
    nystatin and tetracycline have been prepared for
    the treatment of stomatitis,
  • a painful side effect of
    cancer therapy.
  • Allopurinol used for the treatment of stomatitis,
  • pilocarpine for xerostoma (dry mouth)
  • tranexamic acid for the prevention of bleeding
    after oral
  • surgery.
  • carbenoxolone for the treatment of orofacial
    herpes simplex
  • infections

29
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30
  • Mouthwashes generally contain four groups of
    excipients
  • AIcohols (10-20 in MW) ? may function as a
    preservative.
  • aids in masking the unpleasant taste of active
    ingredients,
  • functions as a solubilizing agent for some
    flavoring agents
  • Humectants such as glycerin and sorbitol (5-20
    in MW)
  • increase the viscosity of the preparation
  • enhance the sweetness of the product
  • improve the preservative qualities of the
    product.
  • Surfactants Non ionic and anionic surfactants
    aid in the solubilization of flavors and in the
    removal of debris by providing foaming action.
    Cationic surfactants such as cetylpyridinium
    chloride are used for their antimicrobial
    properties, but these tend to impart a bitter
    taste.
  • Flavours are used in conjunction with alcohol
    and humectants to overcome disagreeable tastes.
    The principle flavoring agents are peppermint,
    cinnamon, menthol or methyl salicylate.
  • CoIouring agents also are used in these
    products.

31
  • Nasal Solutions
  • Nasal solutions are usually aqueous solutions
    designed to be administered to the nasal passages
    in drops or sprays.
  • Ephedrine Sulfate or Naphaxoline Hydrochloride
    Nasal Solution USP are administered for their
    local effect to reduce
  • nasal congestion
  • Lypressin Nasal Solution USP for its systemic
    effect for the

  • treatment of diabetes insipidus
  • The current route of administration of peptides
    and proteins is limited to parental injection
    because of inactivation within the GIT. As a
    result there is considerable research on
    intranasal delivery of these drugs such as
    insulin.
  • Intranasal drug administration offers rapid
    absorption to the systemic circulation. This
    route is safe and acceptable alternative to the
    parental administration

32
There is a direct route of transport from the
olfactory region to the central nervous system
(CNS) without prior absorption to the circulating
blood. The olfactory receptor cells are in
contact with the nasal cavity and the CNS and
they provide a rout of entry to the brain that
circumvents the blood brain barrier
33
  • Commercial nasal preparations include
    antibiotics, antihistamines and drugs for asthma
    prophylaxis.
  • Current studies indicate that nasal sprays are
    deposited in the pharynx with the patient in an
    upright position.

Pharynx
  • Drops spread more extensively than the spray and
    three drops cover most of the walls of the nasal
    cavity, with the patient in a supine position and
    head tilted back and turned left and right.

34
  • Nasal decongestant solutions are employed in the
    treatment of rhinitis of the common cold and for
    allergic rhinitis (hay fever) and for sinusitis.

Sinuses are air-containing cavities in certain
bones of the skull
35
  • Their frequent use or their use for prolonged
    periods may lead to chronic edema of the nasal
    mucosa, i.e. rhinitis medicainentosa, aggravating
    the symptom that they are intended to relieve.
    Thus, they are best used for short periods of
    time used for short periods of time (no longer
    than 3 to 5 days).
  • Nasal solutions are prepared so that they are
    similar in many respects to nasal secretions, so
    that normal ciliary action is maintained thus
    aqueous nasal solutions usually are isotonic and
    slightly buffered to maintain a pH of 5.5 to 6.5.

36
  • Sprays
  • Sprays are solutions of drugs in aqueous vehicles
    and are applied to the mucous membrane of the
    nose and throat by means of an atomizer
    nebulizer.
  • The spray device should produce relatively coarse
    droplets if the action of the drug is to be
    restricted to the upper respiratory tract. Fine
    droplets tend to penetrate further into the
    respiratory tract than is desirable.

37
  • Many of the older sprays were prepared by
    dissolving drug in light liquid petrolatum. This
    vehicle may retard the normal ciliary action of
    the nasal mucosa and if drops of oil enter the
    trachea, can cause lipoid pneumonia. Therefore
    aqueous sprays, which are isotonic with nasal
    secretions and of approximately the same pH are
    to be preferred (WHY?). Such sprays may contain
    antibiotics, antihistamines, vasoconstrictors,
    alcohol, and suitable solubilizing and wetting
    agents.
  • They are used for the treatment of allergy and/or
    vasodilatation (congestion) that occur with
    common cold.

38
  • Otic Solutions
  • The main classes of drugs used for topical
    administration to the ear include local
    anesthetics, e.g. benzocaine antibiotics e.g.
    neomycin and anti-inflammatory agents, e.g.
    cortisone.
  • These preparations include the main types of
    solvents used, namely glycerin or water.
  • The viscous glycerin vehicle permits the drug to
    remain in the ear for a long time.
  • Anhydrous glycerin, being hygroscopic, tends to
    remove moisture from surrounding tissues, thus
    reducing swelling.
  • Viscous liquids like glycerin or propylene glycol
    either are used alone or in combination with a
    surfactant to aid in the removal of cerumen (ear
    wax).
  • In order to provide sufficient time for aqueous
    preparations to act, it is necessary for the
    patient to remain on his side for a few minutes
    so the drops do not run out of the ear.

39
For a Middle Ear InfectionWhile the person
receiving Otic solution lies on his/her side, the
person giving the drops should gently press the
(TRAGUS (4 times in a pumping motion. This will
allow the drops to pass through the hole or tube
in the eardrum and into the middle ear.
For an Ear Canal Infection While the person
receiving the medication lies on his/her side,
the person giving the drops should gently pull
the outer ear upward and backward. This will
allow the ear drops to flow down into the ear
canal.
40
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41
Sweet /or Viscid Pharmaceutical Solutions
42
These include Syrups, Honeys, Mucilages, and
Jellies. All of these preparations are viscous
liquids or semisolids. The sweetness and viscid
appearance are given by sugars, polyols, or
polysaccharides (gums). SYRUPS Syrups are
concentrated solutions of sugar such as sucrose
in water or other aqueous liquid. simple syrup
when water is used alone for making syrup.
medicated syrup when the aqueous preparation
contains some
added medicinal substance flavored syrup which
contains aromatic or pleasantly
flavored substances and is intended to
be used as a vehicle
or flavor for prescriptions
43
  • Polyols (e.g. glycerin or sorbitol) may be added
    to
  • - retard crystallization of sucrose or
  • - increase the solubility of added ingredients.
  • Alcohol often is included as
  • - preservative
  • - solvent for volatile oils.
  • Syrups possess remarkable masking properties for
    bitter and saline drugs.
  • It is important that the concentration of sucrose
    approaches but not quite reach the saturation
    point, WHY?
  • In dilute solutions sucrose provides an excellent
    nutrient for molds, yeasts, and other
    microorganisms.
  • In concentration of 65 by weight or more the
    solution will retard the growth of such
    microorganisms (WHY?).
  • A saturated solution may lead to crystallization
    of a part of the sucrose under conditions of
    changing temperature.

44
When heat is used in the preparation of syrups,
there is almost certain to be an inversion of a
slight portion of the sucrose. C12H22O11
2 C6H12O6 Sucrose heat acid Invert sugar
(dextrose and levulose) The speed of
inversion is greatly increased by acids (why ?)
the hydrogen ion acts as a catalyst in this
hydrolytic reaction. Invert sugar ? is more
readily fermentable than sucrose ? tend to darken
in color ? retard the oxidation of other
substances. The levulose formed during inversion
is sweeter than sucrose therefore the resulting
syrup is sweeter than the original syrup. When
syrup is overheated it caramelizes.
45
  • Invert Syrup
  • It is prepared by hydrolyzing sucrose with
    hydrochloric acid and neutralizing the solution
    with Ca or Na carbonate.
  • The sucrose in the 66.7 w/w solution must be at
    least 95 inverted.
  • The invert syrup, when mixed in suitable
    proportions with syrup, prevents the deposition
    of crystals of sucrose under most conditions of
    storage.

46
  • Preparation of Simple Syrup
  • (a) Solution with heat
  • This is the usual method of making syrups
  • in the absence of volatile agents or those
    injured by heat
  • when it is desirable to make the syrup rapidly.
  • The sucrose is added to the purified water or
    aqueous solution and heated until dissolved, then
    strained and sufficient purified water added to
    make the desired weight or volume.
  • Excessive heating in the preparation of syrups
    must be avoided to prevent inversion of sucrose,
    with increased tendency to fermentation. Syrups
    cannot be sterilized by autoclaving without
    caramelization (yellow color).
  • The specific gravity of syrup is an important
    property to identify its concentration. Syrup has
    a specific gravity of about 1.313, which means
    that each 100 ml of syrup weighs 1313 g.

47
  • (b) Agitation without Heat
  • This process is used in those cases where heat
    would cause loss of valuable volatile
    constituents.
  • The syrup is prepared by adding sucrose to the
    aqueous solution in a bottle of about twice the
    size required for the syrup. This permits active
    agitation and rapid solution.
  • The stoppering of the bottle is important, as it
    prevents contamination and loss during the
    process.

48
  • (c) Addition of a Medicating Liquid to syrup
  • This method is resorted to in those cases in
    which fluid extracts, tinctures, or other liquids
    are added to syrup to medicate it.
  • Syrups made in this way usually develop
    precipitates since alcohol is often an ingredient
    of the liquids thus used and the resinous and
    oily substances dissolved by the alcohol
    precipitate when mixed with syrup.
  • A modification of this process consists of mixing
    the fluid extract or tincture with the water,
    allowing the mixture to stand to permit the
    separation of insoluble constituents, filtering
    and then dissolving the sucrose in the filtrate.
  • ?This procedure is not permissible when the
    precipitated
  • ingredients are the valuable medicinal
    agents.

49
  • (d) Percolation
  • In this procedure, purified water or an aqueous
    solution is permitted to pass slowly through a
    bed of crystalline sucrose, thus dissolving it
    and forming a syrup a pledget of cotton is placed
    in the neck of the percolator
  • If necessary, a portion of the liquid is repassed
    through the percolator to dissolve all of the
    sucrose.
  • This method is used for the preparation of Syrup
    USP.

50
  • Preservation of Syrups
  • The USP suggests that syrups be kept at a
    temperature not above 25C.
  • Preservatives such as glycerin, methyl paraben,
    benzoic acid and sodium benzoate may be added to
    prevent bacterial and mold growth, particularly
    when the concentration of sucrose in the syrup is
    low.
  • The concentration of preservative is proportional
    to the free water.
  • The official syrups should be preserved in well
    dried bottles and stored in a cool dark place.

51
  • Dextrose-Based Syrups
  • Dextrose may be used as a substitute for sucrose
    (WHEN?) in syrups containing strong acids in
    order to eliminate the discoloration associated
    with inversion.
  • Dextrose forms a saturated solution in water at
    70 w/v, which is less viscous than simple syrup.
  • It dissolves more slowly than sucrose and is less
    sweet Preservatives are required to improve the
    keeping qualities of such syrups. Glycerin is
    added in 30 to 45 v/v as preservative.

52
  • Artificial Syrups (Non-Nutritive Syrups)
  • intended as substitutes for syrups and are to be
    administered to persons who must regulate their
    sugar and/or calorie intake accurately. e.g.
    persons suffering from diabetes mellitus.
  • Some early formulae included glycerin, however,
    glycerin and propylene glycol are glycogenetic
    substances, i.e. they are materials which are
    converted into glucose in the body.
  • An example of nonnutritive syrup is Diabetic
    Simple Syrup. It contains compound sodium
    cyclamate (6 cyclamate sodium and 0.6 saccharin
    sodium)
  • However, the cyclamate studies showed that the
    sweetener could produce cancer in animals and, as
    a result, this substance was removed from a wide
    variety of products. Similar studies have been
    carried out on saccharin. Much research has been
    done to find a safe synthetic substitute for
    sucrose. As a result, aspartame which is about
    200 times sweeter than sucrose, is being used now
    in many commercial preparations as the sweetening
    agent.

53
  • Sorbitol-Based Syrups
  • Sorbitol which is hexahydric alcohol made by
    hydrogenation of glucose has been used in the
    preparation of syrup.
  • It is used mostly in the form of a 70 w/w
    aqueous solution.
  • Sorbitol solution is not irritating to the
    membrane of the mouth and throat and does not
    contribute to the formation of dental carries.
  • Sorbitol is metabolized and converted to glucose
    however, it is not rapidly absorbed from the GlT
    as sugars. No significant hyperglycemia has been
    found (WHY?) it may be used as component of
    non-nutritive vehicles.
  • Sorbitol solution does not support mold growth.
    Preservative should be used in solution
    containing less than 60 w/w sorbitol.
  • It is chemically stable and inert with respect to
    drugs and other ingredients used in
    pharmaceutical perpetration.

54
Sorbitol
Glucose
55
  • HONEYS
  • Are thick liquid preparations. At one time,
    before sugar was available, honey was used as a
    base, instead of syrup.
  • There are few official preparations containing
    honey. e.g. Oxymel, or" acid honey "'is a mixture
    of acetic acid, water and honey
  • MUCILAGES
  • The official mucilages are thick viscid, adhesive
    liquids, produced by dispersing gum (acacia or
    tragacanth) in water.
  • Mucilages are used as suspending agents for
    insoluble substances in liquids their colloidal
    character and viscosity prevent immediate
    sedimentation.
  • Synthetic agents e.g. carboxymethylcellulose
    (CMC) or polyvinyl alcohol are nonglycogenetic
    and may be used for diabetic patients.

56
  • Jellys
  • Preparations having a jelly-like consistency.
    They are prepared also from gums.
  • Are used as lubricants for surgical gloves and
    catheters
  • Lidocaine HCl Jelly USP is used as a topical
    anaethetic.

57
Non-Aqueous Pharmaceutical Solutions
58
  • Advantages
  • If the drug is not completely soluble or unstable
    in aqueous medium it may be necessary to use an
    alternative non-aqueous solvent.
  • Oily solutions of drugs are often used for depot
    therapy e.g. in muscles
  • It is essential to test
  • toxicity irritancy flammability cost
    stability and compatibility of solvents to avoid
    problems
  • Solvents such as acetone, benzene and petroleum
    ether are not used for internal products.
  • Internal products may contain ethanol, glycerol,
    propylene glycol certain oils.
  • For parental products the choice is very limited

59
This section is devoted to four groups of
non-aqueous solutions 1. alcoholic or
hydroalcoholic solutions, e.g. elixirs and
spirits, 2. ethereal solutions, e.g. the
collodions 3. glycerin solutions, e.g. the
glycerites, 4. oleaginous soIutions e.g. the
liniments, medicated oils, oleo- vitamins,
sprays, and toothache drops.
60
  • ELIXIRS
  • Are clear, pleasantly flavored, sweetened
    hydroalcoholic liquids intended for oral use.
  • They are used as flavors and vehicles e.g.
    Dexamethasone Elixir USP and Phenobarbital Elixir
    USP.
  • The main ingredients in elixirs are ethanol and
    water but glycerin, sorbitol, propylene glycol,
    flavoring agents, preservatives, and syrups are
    often used in the preparation of the final
    product.
  • EIixirs contain ethyl alcohol, however, the
    alcoholic content will vary greatly, from elixir
    containing only a small quantity to those that
    contain a considerable portion as a necessary aid
    to solubility
  • An elixir may contain water and alcohol soluble
    ingredients.

61
  • Incompatibility of elixir
  • Alcohol precipitates water soluble substances
    e.g. tragacanth, acacia agar and many inorganic
    salts from aqueous solutions.
  • If an aqueous solution is added to an elixir, a
    partial precipitation of ingredients may occur.
    This is due to the reduced alcoholic content of
    the final preparation.

62
  • SPIRITS
  • Alcoholic or hydroalcoholic solutions of volatile
    substances. The active ingredient may be gas,
    liquid or solid.
  • Spirits may be used internally for their
    medicinal value, by inhalation but is mostly used
    as flavouring agents.
  • Spirits should be stored in tight,
    light-resistant containers and in a cool place,
    WHY?
  • Spirits are preparation of high alcoholic
    strength and when diluted with aqueous solutions
    or liquids of low alcoholic content turbidity may
    occur, WHY?

63
  • COLLODIONS
  • Are liquid preparations containing pyroxylin (a
    nitrocellulose) in a mixture of ethyl ether and
    ethanol.
  • They are applied to the skin by means of a soft
    brush or other suitable applicator and, when the
    ether and ethanol have evaporated, leave a film
    of pyroxylin on the surface.
  • The official medicated collodion, Salicylic Acid
    Collodion USP, contains 10 w/v of Salicylic
    Acid in Flexible Collodion USP and is used as a
    keratolytic agent in the treatment of corns and
    warts.
  • Collodion is made flexible by the addition of
    castor oil and camphor.

64
  • GLYCERINS
  • Glycerins or glycerites are solutions or mixtures
    of medicinal substances in not less than 50 by
    weight of glycerin.
  • Most of the glycerins are extremely viscous.
  • Glycerin is a valuable pharmaceutical solvent
    forming permanent and concentrated solutions not
    otherwise obtainable.
  • Glycerin is used as the sole solvent for the
    preparation of Antipyrine and Benzocaine Otic
    Solution USP. As noted under Otic Solutions,
    glycerin alone is used to aid in the removal of
    cerumen.
  • Glycerins are hygroscopic and should be stored
    in tightly closed containers.

65
  • LINIMENTS
  • Are solutions or mixtures of various substances
    in oil, alcoholic solutions of soaps, or
    emulsions.
  • They are intended for external application and
    should be so labeled.
  • They are applied with rubbing to the affected
    area, the oil or soap base providing for ease of
    application and massage.
  • Alcoholic liniments are used generally for their
    rubefaciant and counterirritant effects. Such
    liniments penetrate the skin more readily than do
    those with an oil base.
  • The oily liniments are milder in their action and
    may function solely as protective coatings.
  • Liniments should not be applied to skin that are
    bruised or broken.

66
Rubefacient a substance for external application
that produces redness of the skin e.g. by causing
dilation of the capillaries and an increase in
blood circulation. Counterirritant a medicine
applied locally to produce superficial
inflammation in order to reduce deeper
inflammation
67
  • OLEO VITAMINS
  • Oleo vitamins are fish liver oils diluted with
    edible vegetable oil or solutions of the
    indicated vitamins (usually vitamins A and D).
  • The indicated vitamins are unstable in the
    presence of rancid oils and, therefore, those
    preparations, should be stored in small, tight
    containers, preferably under vacuum or under an
    atmosphere of an inert gas, protected from light.
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