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PHRM 513 > Solutions in Therapy > Flashcards

Solutions in Therapy Flashcards

1
Q

Solutions

A

are liquid preparations containing one

or more chemical substances dissolved in a suitable solvent or mixture of mutually miscible solvents

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2
Q

Solutions are often classified

A

due their composition or use

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3
Q

Solution examples

A

Syrups (aqueous with sugar), hydroalcoholic (water + ethanol), elixirs, tinctures,
etc.
– Oral, otic, ophthalmic, topical, etc

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4
Q

• Since a medicinal agent is administered in solution, it is usually assumed:

A

That the agent, as well as other solutes, are soluble or at least partially aqueous
soluble

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5
Q

Since it is already in solution, it is expected that

A

absorption occurs faster than from a solid or suspension dosage form of the same medicinal agent

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6
Q

– Pharmacist is aware of the

A

solubility and stability of each solute in the solution

to avoid chemical and physical interactions that will affect the product

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7
Q

• Solubility

A

The amount of solute that can dissolve in a given quantity of solvent at
a particular temperature

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8
Q

A saturated solution is

A

one that contains the maximum quantity of dissolved solute

at a given temperature

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9
Q

Solute-solute and solvent-solvent forces must

A

be overcome by solute-solvent attractive forces for dissolution to happen

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10
Q

Solubility may be increased by selecting a

A

different solubilizing agent, different
chemical salt form, alteration of the pH of the solution or substitution in part or in
whole of the solvent

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11
Q

An increase in temperature usually results

A

in an increase in solubility

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12
Q

Prediction of solubility is based upon

A

molecular structure and functional groups

– Like dissolves like

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13
Q

Salts of monovalent cations (Na, K, Li, NH4) are generally

A

water soluble

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14
Q

Salts of divalent cations (Ca, Mg, Hg) are

A

often less soluble

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15
Q

Halogen groups and increases in molecular weight tend to

A

decrease water solubility

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16
Q

Organic compounds may be somewhat more aqueous soluble if they

A

contain

polar groups that are capable of hydrogen bonding

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17
Q

Greater the number of polar groups

A

, the better likely the aqueous solubility
Polar groups include: -OH, -CHO, -COOH, -C=O, -NO2, -NO3
, -NH2
, -SO3H

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18
Q

Choice of solvents is based upon factors such as

A

solubility, clarity, toxicity,
compatibility with other formulation components, odor, color, cost and
route of administration

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19
Q

Co-solvents are often employed

A

– To enhance solvation ability of water

– To contribute to a product’s chemical and/or physical stability

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20
Q

Examples of co-solvents

A

o Ethyl alcohol, glycerin and propylene glycol often used

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21
Q

Alcohol

A

Also called ethyl alcohol, ethanol
-94.9-96% C2H5OH v/v
-

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22
Q

Alcohol is

A

Miscible with water and is able to dissolve many water insoluble ingredients
such as drug substances, flavorants, colorants and antimicrobial preservatives

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23
Q

Ethanol may act as a

A

antimicrobial alone or with other preservatives

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24
Q

FDA limits alcohol content in OTC oral products

A

Concern about undesirable pharmacologic and toxic effects
– Limits:
❖For children < 6 years of age – 0.5%
❖For children 6-12 years of age – 5%
❖For children > 12 years of age and adults – 10%

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25
Q

Glycerin, USP

A

Also called glycerol

  • is a natural compound derived from vegetable oils or animal fat
  • Miscible with water and alcohol
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26
Q

Glycerin characteristics

A
  • Clear syrupy liquid with a sweet taste
  • Has preservative properties at higher concentrations
  • Used as a stabilizer and an auxiliary solvent in conjunction with water or alcohol
    • Used in many internal preparations
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27
Q

Propylene Glycol, USP

A

Clear, viscous liquid
• A synthetic product obtained from the hydration of propylene oxide
• Miscible with water and alcohol
• Frequently substituted for glycerin in modern pharmaceutical formulations

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28
Q

Purified Water, USP

A

s obtained from EPA compliant water treated mainly by distillation, ion exchange or reverse osmosis
- Not intended for use for parenteral administrations (i.e., injections)

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29
Q

Note abt Purified water

A

Ordinary drinking water from the tap is not acceptable for the manufacture
of most aqueous preparations because of possible incompatibilities
between dissolved solids and the medicinal agents

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30
Q

Water permitted for parenteral administration:

A

Water for Injection, USP;

Bacterostatic Water for Injection, USP; Sterile Water for Injection, USP

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31
Q

Strengths of preparations are usually expressed

A

in terms of percent strength

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32
Q

To hasten the dissolution of a slow dissolving material, one may try to:

A
  • Apply heat
  • Reduce particle size of solute
  • Use a solubilizing agent
  • Vigorously agitate mixture (effective stirring)
  • Lower viscosities of solvents if not only aqueous
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33
Q

Note:

A

Increased temperatures cannot be maintained for pharmaceuticals. Also, elevated temperatures may result in loss of volatile co-solvents (e.g., alcohol) and increase in the rate of degradation of drug or excipients.

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34
Q

Ratio strength weight in volme

A

-:- w/v Grams of constituent in stated milliliters of preparation

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35
Q

Dry mixtures for solution

A

Some drugs have insufficient stability in aqueous solution for an extended
shelf-life, e.g., antibiotics
• These products are provided as dry powder or granule form for reconstitution immediately prior to dispensing
- This dry powder contains all of the formulative components except for the
solvent

36
Q

Dry powder: Once reconstituted, the solution remains

A

stable for a certain labeled period
(7 to 14 days) when stored in the refrigerator; this period is sufficient for
the completion of the regimen prescribed

37
Q

Solutions intended for oral administration may contain

A

– Flavors and colors to make them more palatable and attractive
– Stabilizers to maintain chemical and physical stability
– Preservatives to prevent growth of microorganisms

38
Q

Pharmacist may be called on to

A

– Dispense a commercially prepared solution
– Dilute the concentration of a prepared solution (e.g., to make a pediatric
solution from an adult product)
– Prepare a reconstituted solution
– Extemporaneously compound an oral solution from bulk ingredients

39
Q

Oral rehydration solutions

A

Rapid fluid loss associated with diarrhea can lead to dehydration and death
- common in young children and elderly
-

40
Q

Why would you need oral rehydration solutions

A

Small intestine secretes far more fluid and electrolytes than normal exceeding the amount
the large intestine can reabsorb; the fluid loss, mainly extracellular fluid, leads to progressive
loss of blood volume and hypovolemic shock

41
Q

Goal of Oral rehydration solutions

A

o Usually effective in treatment of mild volume depletion: 5-10% body weight
o Available OTC – Typically as a powder that is added to a specific amount of water

42
Q

Oral rehydration solutions example

A

Pedialyte (Abbott)

43
Q

Oral colonic lavage solution

A

To prepare for procedures such as a colonoscopy, the bowel must be cleared;
material remaining in the bowel results in problems during the procedure
-Bowel clearance entails oral administration of a balanced solution of
electrolytes with PEG-3350
-Product needs to be refrigerated after reconstitution

44
Q

PEG

A

acts as the osmotic agent in the GI and the balanced electrolyte concentration results in virtually no net absorption or secretion of ions
o A large volume (4 L) of this solution is administered

45
Q

Magnesium citrate oral solution

A

Also known as, citrate or citrate of magnesia
– An essentially colorless, effervescent liquid having a sweet, acidulous taste and
a lemon flavor
– During preparation, liquid is boiled; final solution may be sterilized
– Employed as a saline laxative that is best taken refrigerated

46
Q

Sodium citrate and citric acid oral solution

A

Citric acid and sodium citrate solution
– Used as a systemic alkalinization for patients with need of maintaining alkaline urine for the treatment of cystine calculi (a type of kidney stone)
– Also used as an adjuvant in treatment of gout

47
Q

Syrups

A

Concentrated, viscous aqueous preparations of sugar or sugar substitute with or without flavoring agents and medicinal substances
- helps w taste

48
Q

Most commonly sugar employed in syrups

A

sucrose

- Sorbitol, glycerin, propylene glycol, methylcellulose, hydroxyethylcellulose – Often substituted for sucrose

49
Q

Non-medicated or flavored vehicles

A

Syrups containing flavoring agents, but no
drug
- Can be used in reformulating a medication only available in a solid form
– Drug stability, solubility and bioavailability must be considered, case-by-case
– Can be prepared as either solution or suspension

50
Q

Note abt syrup

A

Water-soluble, aqueous-stable drug may be added to a flavored syrup provided
other components of the formulation are also compatible

51
Q

Most syrups contain

A
52
Q

High sugar concentrations –

A
  • Strongly resistant to microbial growth, as it ties up water
  • Antimicrobial preservatives
  • Water-soluble flavors and colors
    – Water
    – Drug – Water-soluble, aqueous-stable
    – Other solvents (e.g., alcohol), solubilizing agents, thickeners and/or stabilizers, if
    needed
53
Q

Formulation note

A

Use of minimal amount of free water to dissolve solids minimizes chance of microbial growth

54
Q

Elixirs

A

Clear, sweetened hydroalcoholic oral solutions
• Contain less sugar than syrups – Therefore, less sweet and less viscous
• Flavorings and colorings to increase patient acceptance

55
Q

Alcohol content dependent upon the aqueous solubility of the components

A

Poorer the

water solubility, the higher the proportion of alcohol

56
Q

Elixir co-solvents

A

Glycerin and propylene glycol

57
Q

Elixirs with 10-12% alcohol are

A

usually self-preserving

58
Q

Elixir storage

A

should be stored in tight, light resistant containers and protected from excessive heat
- most often observed in extemporaneous compounding

59
Q

Tinctures

A

Alcoholic or hydroalcoholic solutions prepared from vegetable materials or chemical substances
• Oral and topical administration, depending on the tincture

60
Q

Tinctures contain

A

15-80% alcohol
– Keeps extractives in solution
– Protects against microbial growth – Self-preserved
– Sometimes co-solvents needed to enhance stability and/or solubility of solutes

61
Q

Tinctures storage

A

Need to be kept in tightly stoppered, light resistant containers protected from excessive temperatures due to alcohol content

62
Q

Spirits

A

Alcoholic/hydroalcoholic solutions of volatile substances (usually oils)

  • Alcohol concentration – Generally > 60%
  • Normally when mixed with water, volatile substances separate out and solution forms a milky preparation
63
Q

Spirits uses?

A

As flavoring agents, e.g., Peppermint Spirit

– For medicinal purposes, e.g., Camphor Spirit for topical administration

64
Q

Generally, the topical solutions employ an_____, whereas the

topical tinctures characteristically employ an______

A
  1. Aqeuous vehicle

2. Alcoholic vehicle

65
Q

Sprays

A

Aqueous or oleaginous solutions administered topically

– Coarse droplets or fine solids applied via spray bottles or atomizers

66
Q

Sprays characteristics

A

Usually to nasopharyngeal tract (e.g., congestions and inflammation) or skin
o Insulin and glucagon may be administered nasally
o Anti-infective and antifungal are examples of skin sprays

67
Q

Coal tar topical solution

A

An alcoholic solution containing 20% coal tar and 5% polysorbate 80
– Final content is 81-86% alcohol
– Diluted formulation used as a local antieczematic for topical skin conditions

68
Q

Chlorhexidine gluconate solution

A

A broad spectrum antiseptic used as a surgical scrub, hand wash, skin wound and antiplaque, antigingivitis
mouth wash

69
Q

Povidone iodine topical solution

A

Chemical complex of iodine and polyvinylpyrrolidine (PVP)
-Approximately 10% iodine available to be released when applied to skin
– Used as a surgical scrub and non-irritating antiseptic

70
Q

Thimerosal topical solution

A

Water soluble organic mercury antibacterial
o Buffered to maintain alkalinity (pH ~10) for stability
o Solution protected from light

71
Q

Thimerosal topical solution uses

A

Was used mainly to disinfect skin prior to surgery and as a first aid to abrasions
and wounds
– Was used as a preservative in vaccines and other biologic products
– Withdrawn from the market

72
Q

Vaginal solutions (Douches)

A

Concentrated powders – Usually diluted or prepared as solutions by patient
– For irrigation, hygienic cleansing of the vagina
– Some douches contain therapeutic anti-infective agents

73
Q

Rectal solutions

A

– Retention enemas

- Evacuation enemas

74
Q

Retention enemas –

A

For local effects or systemic absorption
o Minimizes undesirable GI effects seen in oral administration
o Blood levels usually obtained within 30 minutes following instillation

75
Q

Evacuation enemas

A

To cleanse the bowel

76
Q

Non-aqueous solutions

A

Liniments

Collodions

77
Q

Liniments

A

Alcoholic or oleaginous liquid preparation intended to be rubbed with friction and
massaged onto the skin
may be solutions, emulsions or suspensions depending upon the materials and
preparation procedure
➢FOR EXTERNAL USE ONLY

78
Q

Alcoholic liniments –

A

Used when rubefacient, counterirritant or penetration action is desired

79
Q

Oleagineous liniments

A

Primarily employed when massage is desired; less irritating to skin than
alcoholic liniments

80
Q

Collodions

A

Mainly solutions of pyroxylin in vehicle of alcohol and ether with or without drug
– Painted/applied to skin and allowed to dry to form a somewhat flexible film used to
occlusively protect the skin or retain a dissolved drug in contact with skin for a
prolonged period of time
➢FOR EXTERNAL USE ONLY

81
Q

Principal methods of drug extraction

A

Maceration

Percolation

82
Q

Maceration

A

o Process in which the properly comminuted drug is permitted to soak in solvent until the
soluble material is dissolved
o Material is placed in a stoppered vessel and the material is soaked and repeatedly
agitated for a period of time, usually 2-14 days
o Alternative method is to place material in a porous cloth bag that is suspended in
solvent until all soluble material is dissolved
o Maceration is usually conducted at 15-20 °C

83
Q

Percolation

A

Process in which a comminuted drug is extracted by the slow passage of solvent
through a column of the drug

84
Q

Advantages of solutions

A
  • The drug is already dissolved in solvent
    system; drug action can be rapid
  • Dose uniformity and specific volumes can
    be measured accurately allowing for flexible
    dosing
  • Oral solutions are usually easily swallowed
    as opposed to solid dosage forms
  • Generally, easy to manufacture
85
Q

DisAdvantages of solutions

A
  • Drug instability is increased when drug is in
    solution
  • Bulky and less convenient for patients to
    transport compared to solid dosage forms
  • Many drugs are insoluble or poorly soluble
    in water
  • Measuring device needed for administration

PHRM 513 (13 decks)

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