chapter 1 Preformulation

What is the primary focus of the Research and Development (R&D) department in a pharmaceutical firm?

Which activity is NOT typically associated with the R&D department of a pharmaceutical firm?

In what type of environment does the R&D department usually conduct its activities?

What is a primary activity of the production department in large scale manufacturing?

What is the focus of large scale manufacturing according to :

Which department is responsible for process validation in large scale manufacturing?

What type of testing is conducted by the Analytical labs in the QC department?

Which procedures do the Analytical labs( UV ,HPLC) in the QC department follow for testing?

What is a key responsibility of the QC department in large scale manufacturing?

What is the primary role of the QA department in large scale manufacturing?

Which department is responsible for overseeing the practices followed during manufacturing Process validation?

What is the main focus of the QA department in relation to manufacturing Process validation?

What is the main focus of Industrial Pharmacy?

What is the pharmaceutical industry looking for in formulations and process technologies?

What is the desired outcome of focusing on robust formulations and process technologies?

What is a prerequisite for conducting studies in the area of scale up and understanding pharmaceutical processes?

In addition to understanding and controlling pharmaceutical processes, what are the aims of the research ?

Which of the following processes is NOT mentioned as an area of study in the text?

What is the main objective of preformulation Formulation?

What is the Formulation is

What is the ultimate goal of the formulation process?

What does preformulation influence?

Which aspect of drug development is impacted by preformulation?

What is determined as part of preformulation activities?

What does preformulation primarily influence in drug development?

What determines the bioavailability of a drug candidate?

In drug development, what aspect impacts the selection of a successful drug candidate for development?

What is a key factor affecting how a material will be processed pharmaceutically?

What is the purpose of characterizing the physicochemical properties of drug candidates early in the development process?

How can physicochemical properties of drug candidates be categorized?

What is the potential outcome of characterizing physicochemical properties early in drug development?

What is the primary purpose of developing a suitable assay in preformulation?

Why are assays developed in preformulation not rigorously validated at this stage?

What is the main consideration when determining approximate values in preformulation assays?

What can color be used as an indicator of in drug batches?

How can more quantitative measurements of color be obtained?

What is the subjective nature of color when describing drug batches?

Color intensity is related to the extent of conjugated unsaturation as well as the presence of chromophores

All compounds that appear to have color are structurally unsaturated

Color in drugs is generally a function of the drug's inherent chemical structure and its level of saturation

Odor is a significant factor to consider in the evaluation of substance degradation.

Strong odors should be present in the substance to indicate degradation.

Any deviation from the characteristic odor of the substance should be checked for potential degradations.

Which factor could help suppress unpalatability in taste?

What could lead to problems in solubility and particle size when suppressing unpalatability in taste?

Which method could be used to suppress unpalatability without leading to problems in solubility and particle size?

What is assumed about the chemical structure in the context of measuring macroscopic properties of a drug candidate?

What does the text mention about solubility in relation to physical form?

What leads to the further macroscopic properties of a drug candidate?

What is solubility?

What forms a solution?

What is hydration in the context of solubility?

Solubility is the maximum quantity of solvent that can dissolve in a certain quantity of solute at a specified temperature.

The process of dissolving a solute into a solvent is called hydration if the solvent is water.

The substance to be dissolved is called a solvent and the dissolving fluid in which the solute dissolves is called a solute.

True or false: No drug can enter systemic circulation without first being in solution?

True or false: Relatively insoluble compounds often exhibit complete and predictable absorption?

True or false: Up to 40% of drug candidates have been abandoned due to poor aqueous solubility?

What is the preferred solubility of the molecule for the final product assuming oral delivery in a solid form?

What type of formulations are initially needed for obtaining toxicity and bioavailability data in animal models?

What is the minimum acceptable solubility for initial formulations used in animal models?

What method is usually used to determine a drug's solubility?

What is the purpose of chemical analysis in determining a drug's solubility?

What happens to the drug and solvent during the equilibrium solubility method?

What is frequently used to increase drug solubility?

When is salt formation indicated for a drug candidate with low solubility?

What is required if solubility cannot be manipulated through salt formation?

Is chemical modification of the drug into salt or ester forms frequently used to increase solubility?

If the solubility of the drug candidate is less than 1 mg mL−1, then salt formation, if possible, is indicated.

If solubility cannot be manipulated through salt formation, then a novel dosage form will be required.

What are some parameters that determine the solubility of a compound?

What must be determined for every new drug as a function of pH over the physiological pH?

What is the maximum quantity of solvent that can dissolve in a certain quantity of solute at a specified temperature called?

Solubility is solely determined by the molecular size of the compound.

The solubility of every new drug must be determined as a function of pH over the physiological pH.

Ionic strength and temperature do not affect the solubility of a compound.

What is a pharmaceutical application of solubility?

Why would solubility be used in formulating sustained release dosage forms?

What is the purpose of obtaining a homogenous distribution of small amount of drugs at solid state?

Which type of drugs can be solubilized according to the text?

What is the result of solubilization of orally administered drugs, as per the text?

What can be combined in a single phase system in multivitamin preparations?

What can solubilization lead to?

In what dosage forms can drug absorption be increased according to the text?

What does solubilization improve according to the text?

What can be used for solubilizing phenolic compounds for use as disinfectants?

Which compounds are dissolved with polysorbate by solubilization?

What does high aqueous solubility not necessarily guarantee?

What is the significance of understanding acid and base behavior in drug development?

Why is it important to know how the degree of ionization of drugs may change during passage along the gastrointestinal tract?

Why is determining the pKa of a drug considered an important step in preformulation characterization?

Understanding acid and base behavior is extremely important in drug development

The solubility of an acidic or basic drug is not pH dependent

The pKa of a drug is not a significant factor in preformulation characterization

True or false: The Henderson Hasselbalch equations allow calculation of the extent of ionization of a drug as a function of pH, if the pKa is known?

True or false: When the pH is significantly below the pKa (by at least 2 pH units), a weakly acidic drug will be completely unionized?

True or false: When the pH is significantly above the pKa (by at least 2 pH units), a weakly acidic drug will be virtually fully ionized?

What happens when the pH is significantly below the pKa for a weakly acidic drug?

What occurs when the pH is significantly above the pKa for a weakly acidic drug?

What does the Henderson Hasselbalch equations allow calculation of?

What is the impact of degree of ionization on solubility?

What is the purpose of determining pKa values in preformulation?

Why is modern automated instrumentation for determining pKa values considered extremely useful?

In preformulation, why is it important to know how a molecule will distribute itself between aqueous and fatty environments?

What is the primary consideration in determining approximate values in preformulation assays?

Why is understanding acid and base behavior important in drug development?

What is commonly used as a simple solvent model to mimic the biological lipid bilayers?

Why is it difficult to develop an analytical method to measure actual partitioning between complex lipophilic phases in a physiological environment?

What does n-Octanol aim to mimic in the context of drug partitioning?

Log P values can only be determined experimentally, not calculated from the chemical structure of the drug candidate.

Group additivity functions are used to calculate Log P values from the chemical structure of the drug candidate.

Group additivity functions are not used to calculate Log P values from the chemical structure of the drug candidate.

Log P values can be determined experimentally or can be calculated from the chemical structure of the drug candidate by means of group additivity functions.

Solubility is solely determined by the molecular size of the compound.

Color intensity is related to the extent of conjugated unsaturation as well as the presence of chromophores

Hygroscopicity refers to the tendency of a substance to repel water from its immediate environment.

An increase in water content can often decrease the rate of chemical degradation of the active ingredient.

Wet powders will become more cohesive and flowability is increased.

What is the term for the tendency of a substance to attract water from its immediate environment?

What happens to the flowability of wet powders as their water content increases?

How does an increase in water content affect the rate of chemical degradation of the active ingredient in a substance?

What happens to an amorphous matrix when it absorbs water?

What effect does absorption of water have on freeze-dried amorphous powder?

What extreme outcome can result from absorption of water by amorphous materials?

How does hygroscopicity affect the compression characteristic, granulation, and hardness of the final product?

Why is hygroscopicity important in aerosol applications?

What aspect of drug stability does hygroscopicity affect?

What is the primary reason for ensuring the stability of salt forms with respect to environmental humidity?

Which salts are highlighted as examples of being so hygroscopic that they will dissolve in the water they absorb?

Why must the stability of salt forms with respect to environmental humidity be assured?

What is the appropriate action if water absorption is likely to cause a detrimental change in physicochemical properties of a drug candidate?

What is typically involved in protecting a drug candidate or product from detrimental changes due to water absorption?

In case of potential detrimental changes due to water absorption, what is the recommended approach for protecting the drug candidate or product?

Ephedrine & Hyoscymine are hygroscopic in nature

Physostigmine is not hygroscopic in nature

Hygroscopic & Deliquescent substances absorb moisture from the air.

Pilocarpine is not hygroscopic in nature.

Glycerinated gelatin & PEG base of suppository are not hygroscopic in nature.

Efflorescent substances lose water of hydration when exposed to air.

Cocaine is an efflorescent substance.

Atropine is a hygroscopic substance.

Is water uptake usually determined through a change in mass?

Does TGA measure mass as a function of temperature?

Does DVS measure mass as a function of humidity at a constant temperature?

What are some of the physicochemical properties that differ between different physical forms of a drug?

Why is the solid state considered the most important when developing a drug candidate into a drug product?

What is the significance of understanding the different physical forms of a drug in drug development?

What is polymorphism in the of crystallization?

What is the form with the highest melting temperature called in polymorphism?

Why is it important to select the best form of a polymorph for development?

What is the defining characteristic of the stable form in polymorphism?

Why is it tempting to consider formulating only the stable polymorph of a drug?

What happens to all metastable forms over time in relation to the stable form?

What can the presence of the B form or the C form of chloramphenicol palmitate dramatically reduce?

What is the preferred option for development if the stable polymorph shows acceptable bioavailability?

What is not necessarily straightforward when it comes to selection of polymorphic form?

What does DSC data help differentiate in polymorphs?

What can the heat of fusion, determined by DSC, be used to calculate?

What thermodynamic information does DSC provide about polymorphs?

Does DSC data differentiate polymorphs based on their melting points and heats of fusion?

Can DSC identify which polymorph is stable and which polymorphs are metastable?

Is the heat of fusion determined by DSC used to calculate ideal solubility?

What can make it difficult for molecules to orient themselves into repeating arrays in amorphous materials?

In what scenario do molecules forming the solid phase not have sufficient time to align in amorphous materials?

What factor can contribute to difficulty in orienting molecules in amorphous materials?

What term is used to describe a solid phase produced by disrupting a preexisting crystal structure with a localized force?

Why do amorphous materials usually have appreciably higher solubilities and faster dissolution rates than their crystalline equivalents?

What advantage do amorphous materials offer as an alternative to salt selection to increase the bioavailability of poorly soluble compounds?

What are manufacturing processes frequently affected by?

What properties can affect the movement, blending, and compression of powders in manufacturing processes?

Which factor is not typically involved in the influence of powder properties on manufacturing processes?

How is particle shape most easily determined?

When is scanning electron microscopy a better option for determining particle shape?

What makes it difficult to define the particle size of irregularly shaped particles?

What are the shapes of powder particle size?

Why should each new drug candidate be tested with the smallest particle size during preformulation?

What does preformulation aim to achieve in relation to drug particles?

Which processes are controlled by surface area in preformulation?

Particle size and surface area are inversely related: True or false?

Smaller drug particles have greater surface area: True or false?

Hygroscopic substances repel water from their immediate environment: True or false?

increased surface area leads to faster dissolution: True or False

High surface area most often reflects a relatively small particle size: true

Small particles agglomerate more readily: true

Increased surface area leads to slower dissolution: true

Particle size distribution and shapes do not affect the chemical and physical properties of drug substances.

The biopharmaceutical behavior of solid drugs is not influenced by their particle size distribution and shapes.

The effect of particle size distribution and shapes is limited to the physical properties of solid drugs.

How does the physical form of a drug influence its bioavailability?

How does size and shape of tablets influence powders and granules?

How does material size relate to stability and interaction with atmospheric factors?

How does particle size influence the stability of dispersions?

What impact does particle size have on bioavailability and therapeutic effectiveness?

In what type of formulation is particle size relevant?

Particle size influences dissolution

Particle size influences stability of dispersions

Particle size influences bioavailability and therapeutic effectiveness

What are the two most relevant methods of assessment at the preformulation stage for powder flow?

Why must powders have good flow properties in pharmaceutical manufacturing?

Why are methods required during preformulation that only need small volumes of powder?

Is the angle of repose, Carr’s index, and the Hausner ratio useful in predicting bulk properties when only a small amount of test material is available?

Are the Carr’s index and the Hausner ratio calculated from measurements of bulk density?

Are the angle of repose, Carr’s index, and the Hausner ratio the most useful parameters in predicting bulk properties when only a small amount of test material is available?

Compaction properties are usually very poor for most drug powders, but tablets are rarely made from the drug alone: true

Compaction is a result of the compression and cohesion properties of a drug: true

Tablets are rarely made from the drug alone: true

Excipients play a more significant role in tablet properties than the drug itself for low dose drugs: true

Once the dose of a drug increases to more than 50 mg, the compaction characteristics of the drug greatly influence the overall tablet properties: true

The majority of the tablet comprises excipients for low dose drugs, making the properties of the drug less important: true

What type of properties should a material to be tableted preferably have?

Why is brittleness considered a beneficial characteristic for a material to be tableted?

What is the purpose of understanding the compaction properties of a drug candidate at the preformulation stage?

What role does water play in altering mechanical properties of high dose drugs?

In preformulation, what should happen to excipients if a high dose drug behaves plastically?

What should excipients do if a high dose drug does not behave plastically in preformulation?

Water content can act as a plasticizer, altering mechanical properties of high dose drugs: true or false?

If a high dose drug behaves plastically, the excipients should deform plastically: true or false?

Water frequently acts as a plasticizer, altering mechanical properties of high dose drugs: true or false?

Which of the statements from the Department of a pharmaceutical firm except:

Which of the following is a type of quality assurance that involves :

Which of the following is a type of quality assurance that involves :

Which of the following is a type of quality control except

Which of the following is a type of quality control that involves:

Which of the following is a type of quality control except :

What is the requirement of sample for determining the hygroscopicity property?

What is the requirement of sample for determining the solubility property?

Which assay is used to determine the pKa property using:

Which property is used to determine assay with using HPLC,Plus suitable storage condition?

What is the abbreviation of the technique that measures the surface area of particles?

What is the name of the index that measures the compressibility of a powder?

What technique is used to measure the excipient compatibility of a drug?

What is the term for a solute that requires less than one part of solvent for one part of solute?

What is the range of parts of solvent required for one part of solute for a sparingly soluble solute?

Which of the following solutes is most likely to be insoluble in water?

What is the color of the substance that has a sulfurous odour and a bitter taste?

What is the taste of the substance that has a shiny color and a fruity odour?

What is the odour of the substance that has an off-white color and an acidic taste?