Solutions (Part 1) Flashcards by amanda kastel

Define pharmaceutical solutions

liquid preparations that contain one or more chemical substances dissolved in a suitable solvent OR mixture of mutually miscible solvents

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Name FIVE factors that affect solubility

-attractive forces
-repulsive forces
-van der waals forces (dipole-dipole) - dipolar molecules

-ion-dipole force
-hydrogen bond

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dipole-dipole forces are also known as…

ven der waal forces

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hydrogen bonding occurs between….

polar and non polar molecules and ions

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hydrogen bond is a hydrogen molecule attached to….

oxygen, nitrogen, or fluorine

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in a solution, what are the solutes?

medicinal agents OR additional agents (excipients) such as color, flavor, sweetness, or stability)

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to achieve the solute-solvent attraction, what has to happen?

the solute-solute forces and the solvent-solvent forces must be broken to achieve the solute-solvent attraction

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the SOLUBILITY of an agent in a particular solvent indicates what?

the maximum concentration of the drug in solution

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when is a solution said to be saturated?

when a solvent at a given temp has dissolved all of the solute possible

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what is unique about Calcium Hydroxide Topical Solution, USP?

calcium has negative heat effect. the solubility of calcium hydroxide DECREASES with rising temperature

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name the solute(s) and solvent(s) of Calcium Hydroxide Topical Solution, USP

1 solute: Calcium hydroxide (excess amount)
1 solvent: purified water

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what is the % w/v of Calcium Hydroxide Topical Solution USP?
explain

0.14% w/v
0.14 g solute in 100mL solution
this is the solubility of calcium hydroxide at room temperature
VERY LOW SOLUBILITY

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Name the solute and solvent of Potassium Iodide Oral Solution USP

1 solute: potassium iodide
1 solvent: purified water

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give the solubility of Potassium Iodide Oral Solution USP at room temp.

100% w/v
100 g of solute in 100 mL solution

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What can be changed in regards to the SOLUTE to increase solubility?

-solubilizing agent (excipient)
-using a chemical salt of the API (medicinal agent)

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Is it preferred to alter the solubility by changing the API or changing the solvent(s)?

preferred to change the solvents.

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How can the solvent be altered to adjust the solubility of a drug?

substitution (in part or whole)
ie: use of a cosolvent is done most of the time

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Explain how the SOLUTION ITSELF can be altered to adjust the solubility of the API

changing the pH or the temperature of the final solution.

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pH of the solution is adjusted based on what equation?

hendersen hasselbach equation

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why is changing the temperature of the final solution NOT really used to increase solubility?

because the solution is stored at room temperature usually and the solubility will change once the heat is removed in the laboratory setting

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Explain how altering the solution of iodine granules + purified water can increase solubility.

iodine granules by itself is not very soluble in purified water. 1 g of solute in 3000mL solution (0.033%w/v)

however, Iodine Topical Solution USP has the iodine granules (2%) and 2.4% of sodium iodide (SERVES AS A SOLUBILIZING AGENT) as the solutes and purified water as the solvent.
this makes the solution much more soluble

SOLUTES: iodine and sodium iodide (solubilizing agent; excipient)

SOLVENT: the same – purified water

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Name the USP relative terms of solubility and the meaning behind them

very soluble
freely soluble
soluble
sparingly soluble
slightly soluble
very slightly soluble
Practically insoluble/insoluble

“parts of solvent required to dissolve 1 part of the solute”

very soluble: <1
freely soluble: 1-10
soluble: 10-30
sparingly soluble: 30-100
slightly soluble: 100-1,000
very slightly soluble: 1,000-10,000
practically insoluble/insoluble: >10,000

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“parts of solvent required to dissolve 1 part of the solute”
be specific…

mL of solvent required to dissolve 1 g of solute

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Explain what happens when you convert a drug to its salt form

when a drug is converted to its salt form, the drug’s solubility in water is increased due to the “like dissolves like” principle (both are polar)

however, converting to salt form means that if alcohol is the solvent, much more of it is required to dissolve this salt form of the drug.

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what is the salt form of codeine? explain the process in getting to this point

the acceptable salt form of codeine is codeine PHOSPHATE. Codeine sulfate was originally made, but this salt form turned out to be only soluble in water, and very slightly soluble in alcohol (1,280) so, codeine phosphate was created to combat this issue of insolubility in alcohol. Codeine phosphate is freely soluble in water, and slightly soluble (325) in alcohol, which is much more acceptable than the 1,280 of codeine sulfate.

which are more soluble in alcohol -- organic bases or their corresponding salt forms?

organic bases

name the 10 POLAR GROUPS from the slides

OH CO CHO COH CH2OH COOH CHOH NO2 NH2 SO3H

Are most drugs organic or inorganic? What does organic/inorganic mean?

must drugs are organic, meaning that they contain carbon

what can you say about the solubility of monovalent molecules?

they are easily broken and have good water solubility.

rank the following according to solubility (most soluble --> least soluble) -one of the 2 ions in an ionic compound is monovalent -both the cation and anion are multivalent -both the cation and anion are monovalent

most soluble: both the cation and anion are monovalent middle: one of the 2 ions is monovalent least soluble: both the cation and anion are multivalent (double bond)

name 2 ways that we can alter solubility by altering the medicinal agent (API) itself

-change it to its salt form -change functional groups

name the 4 general rules of solubility for organic molecules

1. Molecules with 1 polar functional group are usually soluble to a TOTAL CHAIN LENGTH OF 5 CARBONS 2. Molecules having branched chains are more soluble than corresponding straight chain compound 3. Water solubility DECREASES with an increase in MW 4. Increased structural similarity between solute and solvent gives increased solubility

true or false molecules having 1 polar functional group are usually soluble to a total chain length of 6 carbons

FALSE --- 5 carbons

True or false: molecules having branched chains are more soluble than the corresponding straight chain compound

TRUE

true or false: water solubility increases with increasing molecular weight

FALSE -- water solubility DECREASES with an increase in molecular weight

true or false: compounds with similar dielectric constants will have better solubility than compounds with differing dielectric constants

TRUE remember: like dissolves like

name the alcohols in order of number of carbons, from 1 carbon - 10 carbons

methanol ethanol propanol butanol pentanol hexanol heptanol octanol (idk 9?) decanol

Name 7 solvents for liquid preparations

Alcohol, USP Diluted alcohol, NF Rubbing alcohol Glycerin, USP Isopropyl rubbing alcohol Propylene Glycol, USP Purified water, USP

Is Alcohol, USP a product or an ingredient (API)

PRODUCT -- you can tell by the capital A and the USP after it

Alcohol, USP contains what compound?

Ethyl alcohol, also known as ethanol

what is the PRIMARY SOLVENT for organic compounds?

alcohol

Describe the % V/V of Alcohol, USP

94.9-96% v/v of ethanol it is a HYDROALCOHOLIC MIXTURE. the remaining ~5% is made up of water

WHY is Alcohol, USP not 100% v/v of ethanol?

because it is more stable at 95%. In a sealed container of 100% alcohol, it will become 95% when opened and exposed to the air

name the alcohol-content limits that exist in OTC oral products

in children <6 years old --- 0.5% limit in children 6-12 years old --- 5% limit in people >12 years old ---- 10% limit

Explain what Diluted Alcohol, NF is

Diluted Alcohol, NF is a mixture of EQUAL VOLUMES of Alcohol, USP (the PRODUCT) and Purified Water, USP (PRODUCT)

Diluted Alcohol, NF is a useful ____ solvent

HYDROALCOHOLIC

true or false: In Diluted Alcohol, NF, the final volume of the mixture is the sum of the individual volumes of the 2 components

FALSE Diluted Alcohol, NF has the contraction effect. the final volume is reduced ~3% from the sum

Is Rubbing Alcohol used topically or orally?

topically

Explain the contents of Rubbing Alcohol (the PRODUCT)

70% by volume of dehydrated ethyl alcohol (100% alcohol. NOT the product Alcohol USP which is 95%) the remaining 30% consists of water and denaturants

WHY are there denaturants in rubbing alcohol?

the denaturants make the separation of alcohol from the denaturants impossible with ordinary distillation apparatus. -discourages illegal removal and usage as an alcoholic beverage

What is Rubbing Alcohol used as? (he said in class that this is very important to know)

Used as a rubefacient and germicide to prevent the growth of bacteria on the skin

Name the components of Glycerin, USP

glycerol

Which has the HIGHEST viscosity -- alcohol, water, or glycerol?

glycerol

What does auxiliary solvent mean? what is often used as an auxiliary solvent with water or alcohol?

co-solvent; Glycerol, USP

Explain the physical characteristics of Glycerin, USP

higher viscosity than alcohol and water it is a clear, syrupy liquid -- therefore, it is good to use when we use simple syrup

does Glycerin, USP have preservative activity?

it technically does, but it's only a 1:1 ratio

true or false glycerin is often used as a stabilizer

true

Explain the contents of Isopropyl Rubbing Alcohol

70% by volume of isopropyl alcohol, the remainder is water.

Contrast Rubbing Alcohol and Isopropyl Rubbing Alcohol

Rubbing Alcohol is 70% ethanol while Isopropyl Rubbing Alcohol is 70% isopropyl alcohol Isopropyl Rubbing Alcohol is less dehydrating and preferred for diabetics. It is also better than ethyl alcohol in germicidal activity

which is used in preparing needles and syringes for hypodermic injections of insulin and for disinfecting the skin: -Rubbing Alcohol or -Isopropyl Rubbing Alcohol

Isopropyl Rubbing Alcohol

Name the uses for Isopropyl Rubbing Alcohol

rubefacient, germicidal activity, soothing rub, vehicle for topical products, AND in preparing needles and syringes for hypodermic injections of insulin and for disinfecting the skin

what is the substitute for Glycerin, USP?

Propylene Glycol, USP

Propylene Glycol, USP can be nicknamed..

PPG

Name 4 ways in which Propylene Glycol, USP is similar to Glycerin, USP

-higher viscosity than alcohol and water -preservative activity -stabilizer -auxiliary solvent with alcohol or water

which is used 1st -- Glycerin or PPG?

Glycerin. PPG is only used if there is a problem

true or false both Glycerin, USP and Propylene Glycol, USP are miscible in both water and alcohol

TRUE -- remember -- they are often used as auxiliary (co) solvents with them

Purified Water, USP is more free of solid impurities than drinking water. Give the altering percentages

0.001% impurity vs 0.1% impurity

how many preparation methods of purified water are there? name them

3 methods of preparing purified water: -distillation -ion-exchange -reverse osmosis

can Purified Water, USP be used for parenteral administration?

NO -- use Water for Injection, Bacteriostatic Water, or Sterile Water PURIFIED WATER CANNOT BE USED

Solutions (Part 1) Flashcards

(70 cards)