Saturated Solutions and Solubility
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Questions and Answers

Which statement best describes a saturated solution?

  • A solution with no undissolved solute present.
  • A solution in which there is a dynamic equilibrium between dissolved and undissolved solute at a given temperature. (correct)
  • A solution containing solute at a concentration below the saturation point at a given temperature.
  • A solution where the solute concentration exceeds the saturation point at a given temperature.

Solubility, in quantitative terms, refers to the rate at which a solute dissolves in a solvent.

False (B)

Briefly explain the significance of maintaining a constant temperature during the solubility determination process.

Temperature affects solubility

The spontaneous interaction of two or more substances to form a homogenous dispersion is known as ______ or dissolution process.

<p>solvation</p> Signup and view all the answers

Match each solution type with its correct definition:

<p>Saturated Solution = Contains the maximum amount of solute that can dissolve at a given temperature. Unsaturated Solution = Contains less solute than the maximum amount that can dissolve at a given temperature. Supersaturated Solution = Contains more solute than the maximum amount that can dissolve at a given temperature; unstable.</p> Signup and view all the answers

Which of the following is NOT a reason why understanding solubility is important for a pharmacist?

<p>Predicting patient compliance based on taste. (B)</p> Signup and view all the answers

A true solution is a heterogeneous dispersion of solute and solvent.

<p>False (B)</p> Signup and view all the answers

What is the role of the solvent in a true solution?

<p>dispersion medium</p> Signup and view all the answers

The process by which a drug becomes available to reach sites of absorption and interact with therapeutic targets is known as ______.

<p>distribution</p> Signup and view all the answers

Which of the terms refers to the substance that is dispersed or dissolved in a solution?

<p>Solute (D)</p> Signup and view all the answers

What is one of the primary reasons for pharmacists to study solubility?

<p>To select the best solvent(s) for a drug or mixture of drugs. (C)</p> Signup and view all the answers

Understanding drug solubility is irrelevant to predicting its ADME (Absorption, Distribution, Metabolism, Excretion) properties.

<p>False (B)</p> Signup and view all the answers

Match the following terms with their descriptions:

<p>Solute = Dispersed substance in a solution Solvent = Dispersion medium of a solution True Solution = Homogenous mixture of two or more components Distribution = Process of drug reaching sites of absorption</p> Signup and view all the answers

Based on the graph, which compound's solubility is most affected by changes in pH?

<p>Oxytetracycline (amphoteric) (A)</p> Signup and view all the answers

Salt formation is a strategy used to decrease the solubility of a drug.

<p>False (B)</p> Signup and view all the answers

Based on the solvent polarity scale, which solvent would be most effective at dissolving organic salts?

<p>Water (B)</p> Signup and view all the answers

Name two chemical properties of solutes that can be inferred from their chemical structure and that may affect solubility.

<p>Ionizable groups or polar groups or lipophilic groups</p> Signup and view all the answers

The crystal structure of a solute can be either __________ or crystalline.

<p>amorphous</p> Signup and view all the answers

Non-polar solvents are effective at reducing the attraction between ions of strong electrolytes.

<p>False (B)</p> Signup and view all the answers

What type of intermolecular forces enables non-polar solvents to dissolve non-polar solutes?

<p>van der Waals forces</p> Signup and view all the answers

Why is it important to consider the different crystal forms (polymorphs) of a drug?

<p>Different forms may have different solubility and stability. (B)</p> Signup and view all the answers

Ester formation is used to decrease solubility.

<p>False (B)</p> Signup and view all the answers

According to the reading, solubility generally ______ with an increase in temperature.

<p>increases</p> Signup and view all the answers

Match the solvent with the type of solute it is most likely to dissolve:

<p>Water = Inorganic salts Ethyl alcohol = Waxes Hexane = Fixed oils</p> Signup and view all the answers

Match each pH range with the most suitable description of Indomethacin's solubility changes, based on the figure:

<p>pH 2-4 = Solubility is low and relatively constant pH 6-8 = Solubility slightly increases pH 10-12 = Solubility significantly increases</p> Signup and view all the answers

Which factor related to the chemical structure of a drug is LEAST likely to be relevant when predicting its solubility?

<p>The color of the compound (B)</p> Signup and view all the answers

Which structural feature of a solute would most enhance its solubility in polar solvents?

<p>The presence of multiple polar groups (A)</p> Signup and view all the answers

Mineral oil is a polar solvent.

<p>False (B)</p> Signup and view all the answers

List three factors influencing the solubility of solid/liquid systems.

<p>Temperature, Solvent, pH</p> Signup and view all the answers

Which of the following is NOT a type of solution of pharmaceutical importance mentioned?

<p>Gas/gas solutions (C)</p> Signup and view all the answers

The ability of two liquids to mix in all proportions, forming a homogenous solution, is known as ______.

<p>miscibility</p> Signup and view all the answers

Polymorphism in drug crystals affects which of the following physical properties most directly due to differences in bond energy?

<p>Melting point (A)</p> Signup and view all the answers

Complexation of a drug using complexing agents generally leads to a decrease in the drug's water solubility.

<p>False (B)</p> Signup and view all the answers

Define the term 'partition coefficient' and explain what it measures.

<p>The partition coefficient is the ratio of a drug's concentration in two immiscible solvents at equilibrium, typically octanol and water. It measures the drug's relative solubility in these solvents, indicating its lipophilicity or hydrophilicity.</p> Signup and view all the answers

The use of __________ with many drugs can form inclusion complexes that have a higher water solubility.

<p>cyclodextrine</p> Signup and view all the answers

Match the technique with its application in drug characterization:

<p>Kp = Physicochemical measurement of drug permeability X-ray diffraction = Analysis of crystal structure in polymorphism Distribution coefficient (K) = Quantifies drug partitioning between two immiscible liquids</p> Signup and view all the answers

Which of the techniques is NOT a method for measuring drug permeability?

<p>Spectroscopic (A)</p> Signup and view all the answers

A high partition coefficient (K) generally indicates that a drug is more soluble in water than in octanol.

<p>False (B)</p> Signup and view all the answers

Explain how temperature can affect the partition coefficient of a drug.

<p>Temperature can influence the solubility of a drug in each phase, altering the equilibrium concentrations and therefore changing the partition coefficient. Higher temperatures may increase solubility in one or both phases, shifting the distribution.</p> Signup and view all the answers

The distribution coefficient, K, is calculated by the concentration in solvent 1 (C1) divided by the __________ in solvent 2 (C2).

<p>concentration</p> Signup and view all the answers

What is the primary reason for using complexation in drug formulation?

<p>To increase drug water solubility (D)</p> Signup and view all the answers

Which of the following is NOT a parameter used in the Biopharmaceutical Classification System (BSC)?

<p>Particle Size (C)</p> Signup and view all the answers

A drug with high permeability and low solubility is classified as a Class I drug according to the Biopharmaceutical Classification System.

<p>False (B)</p> Signup and view all the answers

According to the BSC, a drug is considered highly soluble when its highest dose strength is soluble in how much aqueous media (in mL)?

<p>250</p> Signup and view all the answers

For an immediate release product to be considered rapidly dissolving, no less than _____% of the labeled amount of the drug substance must dissolve within 15 minutes.

<p>85</p> Signup and view all the answers

A drug is determined to be highly permeable when the extent of absorption in humans is what percentage, or greater, of the administered dose?

<p>90% (C)</p> Signup and view all the answers

Match the BSC Class with its primary characteristic related to oral bioavailability:

<p>Class I = Ideal for oral administration, no expected bioavailability issues Class II = Dissolution is the rate-limiting step for bioavailability Class III = Rapid release from the dosage form is critical due to low permeability Class IV = Poor oral bioavailability, often requiring alternative routes of administration</p> Signup and view all the answers

Which BSC class is likely to benefit most from formulation approaches that enhance drug dissolution?

<p>Class II (B)</p> Signup and view all the answers

The Biopharmaceutical Classification System (BSC) can be used to guide chemical modifications during lead optimization to improve a drug's physicochemical properties.

<p>True (A)</p> Signup and view all the answers

Which of the following drugs is classified as a Class IV drug, indicating poor oral bioavailability?

<p>Furosemide (B)</p> Signup and view all the answers

For a drug to be considered 'highly soluble' under BSC guidelines, at what pH range must it exhibit the required solubility in aqueous media?

<p>pH 1 to 7.5 (D)</p> Signup and view all the answers

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Flashcards

Solubility

The maximum amount of a substance that can dissolve in a given amount of solvent at a specific temperature.

Importance of Solubility

Helps in selecting the best solvent for a drug, overcoming formulation problems, and understanding drug action.

Solubility's Role in ADME

Determines if a drug can reach absorption sites, interact with targets, and undergo metabolism/excretion.

True Solution

A homogenous mixture of solute(s) and solvent(s) forming one phase.

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Solute

The substance that is dispersed or dissolved in a solvent.

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Solvent

The medium in which a solute is dissolved (can be aqueous or non-aqueous).

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Factors Affecting Solubility

Factors like pH, temperature, and the presence of other substances can affect how well something dissolves.

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Electrolytes

Drugs that dissociate into ions when dissolved, affecting their solubility depending on pH.

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Quantitative Solubility

The maximum solute concentration in a solvent at a specific temperature, forming a saturated solution.

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Qualitative Solubility

The spontaneous interaction of substances forming a homogenous dispersion (molecular or ionic).

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Saturated Solution

A solution where dissolved and undissolved solute are in dynamic equilibrium at a given temperature.

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Unsaturated Solution

A solution with a solute concentration lower than required for complete saturation at a given temperature.

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Supersaturated Solution

A solution containing more dissolved solute than it can normally hold at a given temperature; unstable.

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pH and Solubility

Acids increase solubility at higher pH, while bases increase solubility at lower pH.

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Solute Chemical Structure

Ionizable groups, polar groups, and lipophilic groups affect solubility.

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Salt Formation

Salts can improve a drug's solubility, dissolution rate, and stability compared to the free acid or base form.

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Ester Formation

Esters can modify drug solubility and duration of action; they are formed by combining an alcohol and an acid.

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Amorphous vs. Crystalline

Amorphous forms generally have higher solubility and dissolution rates compared to crystalline forms.

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Crystal Polymorphism

Different crystal forms (polymorphs) of a drug can have different solubility, stability, and bioavailability.

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Possible precipitation upon storage?

Refers to the potential change of crystal structure that can affect drug performance.

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Amphoteric

A substance that can act as both an acid and a base.

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Solvent Polarity

A measure of a solvent's ability to dissolve various chemical compounds; affects solute solubility.

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Polar Solvents

Water and alcohols; dissolve polar solutes via hydrogen-bond formation and acid-base reactions. Have high Dielectric Constant (DEC).

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Non-Polar Solvents

These cannot reduce attraction between ions or form hydrogen bonds. They can dissolve non-polar solutes through induced dipole interactions and weak van der Waals forces.

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Types of Solutions

Include gas/liquid, solid/liquid, and liquid/liquid solutions; all used in pharmaceuticals.

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Temperature's effect on solubility

In general, solubility increases when temperature increases which can be explained by dissolution energetics.

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Temperature Coefficient

Indicates how much the solubility of a solute changes with temperature.

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Solute Solubility Examples

Organic and inorganic salts are highly soluble, while fixed oils, fats, and petrolatum hydrocarbons are very low.

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High DEC

The dielectric constant (DEC).

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Polymorphism

The ability of a substance to exist in multiple crystalline forms, affecting physical properties but not chemical properties.

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Complexation

The process of adding complexing agents to a drug to increase its water solubility, often resulting in more polar drug complexes.

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Drug Permeability

A measure of how easily a drug diffuses through biological membranes, indicating its suitability for oral administration.

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Partition Coefficient (K)

The ratio of a drug's concentration in two immiscible solvents at equilibrium, indicating its relative affinity for each solvent.

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Distribution Phenomenon

The distribution of a drug between two immiscible liquids until each phase is saturated, described by the ratio of concentrations.

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Complexation Definition

Adding complexing agents to produce more water-soluble forms of drugs, often using cyclodextrine.

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Drug Permeability Definition

Provides information on drug diffusion through biological membranes and oral administration suitability.

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Partition Coefficient

Ratio of drug concentrations in two immiscible liquids, indicating affinity.

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Distribution Phenomenon

Drug distributes between immiscible liquids until saturated in each.

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Partition Coefficient (Ko/w)

Ratio of drug in octanol vs. water at equilibrium. Limitations: association, dissociation, temperature.

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Biopharmaceutical Classification System (BSC)

A system that uses solubility, permeability, and dissolution to predict oral drug bioavailability.

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High Intestinal Permeability (BSC)

Indicates if a drug can be absorbed well enough in the intestine (90% or more compared to IV).

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High Aqueous Solubility (BSC)

Indicates a high solubility when the highest dose strength dissolves in 250 mL or less of aqueous media, across a pH range of 1 to 7.5.

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Rapid Dissolution (BSC)

An immediate-release product dissolves quickly when at least 85% of the drug is released within 15 minutes under specific USP conditions.

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BSC Class I

High permeability, high solubility. Ideal for oral administration with no bioavailability issues.

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BSC Class II

High permeability, low solubility. Dissolution limits bioavailability, affected by formulation.

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BSC Class III

Low permeability, high solubility. Rapid release from dosage form is critical.

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BSC Class IV

Low permeability, low solubility. Poor oral bioavailability, often requires alternative routes.

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Lead Optimization (BSC)

Enhancing drug properties through chemical modifications to improve drug characteristics.

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Bioavailability Indicator (BSC)

Predicts how well a drug will be absorbed when taken orally.

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