237 Questions
What is the primary focus of the Research and Development (R&D) department in a pharmaceutical firm?
Pre formulation, optimization, and scale up , analtyical method development ,setting up , specification ,process validation
Which activity is NOT typically associated with the R&D department of a pharmaceutical firm?
Manufacturing large-scale production batches
In what type of environment does the R&D department usually conduct its activities?
Small scale laboratory and pilot scale up
What is a primary activity of the production department in large scale manufacturing?
Milling, mixing, granulation, tableting
What is the focus of large scale manufacturing according to :
Following the formulation and procedure developed by R&D
Which department is responsible for process validation in large scale manufacturing?
Production department
What type of testing is conducted by the Analytical labs in the QC department?
Sampling and testing semi finished and finished products
Which procedures do the Analytical labs( UV ,HPLC) in the QC department follow for testing?
Test procedures developed by R&D
What is a key responsibility of the QC department in large scale manufacturing?
Sampling and testing semi finished and finished products
What is the primary role of the QA department in large scale manufacturing?
Ensuring that GMPs are being applied
Which department is responsible for overseeing the practices followed during manufacturing Process validation?
QA department
What is the main focus of the QA department in relation to manufacturing Process validation?
Ensuring adherence to GMPs
What is the main focus of Industrial Pharmacy?
Process technology and dosage form design
What is the pharmaceutical industry looking for in formulations and process technologies?
Shorten the development time and increase product quality
What is the desired outcome of focusing on robust formulations and process technologies?
Shorten the development time and increase product quality
What is a prerequisite for conducting studies in the area of scale up and understanding pharmaceutical processes?
Close cooperation with the pharmaceutical industry
In addition to understanding and controlling pharmaceutical processes, what are the aims of the research ?
Design and develop new devices to improve pharmaceutical processes
Which of the following processes is NOT mentioned as an area of study in the text?
Crystallization techniques in drug manufacturing
What is the main objective of preformulation Formulation?
developing most stable and bioavailable dosage form that mass can be produced
What is the Formulation is
the process of developing a drug candidate into a drug product
What is the ultimate goal of the formulation process?
Developing a mass-producible stable and bioavailable drug product
What does preformulation influence?
Selection of the drug candidate itself
Which aspect of drug development is impacted by preformulation?
Selection of formulation components
What is determined as part of preformulation activities?
All of above
What does preformulation primarily influence in drug development?
Selection of the drug candidate itself
What determines the bioavailability of a drug candidate?
Physicochemical properties and interaction with excipients
In drug development, what aspect impacts the selection of a successful drug candidate for development?
Physicochemical properties and molecular structure
What is a key factor affecting how a material will be processed pharmaceutically?
Physicochemical properties of the molecule
What is the purpose of characterizing the physicochemical properties of drug candidates early in the development process?
To provide fundamental knowledge for candidate selection and dosage form design, reducing development time and costs
How can physicochemical properties of drug candidates be categorized?
Intrinsic to the molecule and derived from bulk behaviour
What is the potential outcome of characterizing physicochemical properties early in drug development?
Reduction in development time and costs
What is the primary purpose of developing a suitable assay in preformulation?
To make a 'go / no go' decision for a specific drug candidate
Why are assays developed in preformulation not rigorously validated at this stage?
To allow approximate values for decision-making
What is the main consideration when determining approximate values in preformulation assays?
Making a 'go / no go' decision for a specific drug candidate
What can color be used as an indicator of in drug batches?
Solvent presence or degradation
How can more quantitative measurements of color be obtained?
Using colorimetry
What is the subjective nature of color when describing drug batches?
It is based on individual perception
Color intensity is related to the extent of conjugated unsaturation as well as the presence of chromophores
True
All compounds that appear to have color are structurally unsaturated
False
Color in drugs is generally a function of the drug's inherent chemical structure and its level of saturation
True
Odor is a significant factor to consider in the evaluation of substance degradation.
True
Strong odors should be present in the substance to indicate degradation.
False
Any deviation from the characteristic odor of the substance should be checked for potential degradations.
True
Which factor could help suppress unpalatability in taste?
Coating
What could lead to problems in solubility and particle size when suppressing unpalatability in taste?
Coating
Which method could be used to suppress unpalatability without leading to problems in solubility and particle size?
Flavors
What is assumed about the chemical structure in the context of measuring macroscopic properties of a drug candidate?
It is assumed that the chemists preparing the candidate molecules will provide this information
What does the text mention about solubility in relation to physical form?
Solubility will be dependent on the physical form (polymorph, pseudopolymorph or amorphous)
What leads to the further macroscopic properties of a drug candidate?
Intermolecular interactions
What is solubility?
The maximum quantity of solute that can dissolve in a certain quantity of solvent at a specified temperature
What forms a solution?
Solute and solvent
What is hydration in the context of solubility?
The process of dissolving solute into water as the solvent
Solubility is the maximum quantity of solvent that can dissolve in a certain quantity of solute at a specified temperature.
False
The process of dissolving a solute into a solvent is called hydration if the solvent is water.
True
The substance to be dissolved is called a solvent and the dissolving fluid in which the solute dissolves is called a solute.
False
True or false: No drug can enter systemic circulation without first being in solution?
True
True or false: Relatively insoluble compounds often exhibit complete and predictable absorption?
False
True or false: Up to 40% of drug candidates have been abandoned due to poor aqueous solubility?
True
What is the preferred solubility of the molecule for the final product assuming oral delivery in a solid form?
Exactly 10 mg mL−1
What type of formulations are initially needed for obtaining toxicity and bioavailability data in animal models?
Liquids for oral gavage or intravenous delivery
What is the minimum acceptable solubility for initial formulations used in animal models?
Greater than 1 mg mL−1
What method is usually used to determine a drug's solubility?
Equilibrium solubility method
What is the purpose of chemical analysis in determining a drug's solubility?
To determine the degree of solubility
What happens to the drug and solvent during the equilibrium solubility method?
They reach a state of balance at a constant temperature
What is frequently used to increase drug solubility?
Chemical modification into salt or ester forms
When is salt formation indicated for a drug candidate with low solubility?
When the solubility is less than 1 mg mL−1
What is required if solubility cannot be manipulated through salt formation?
A novel dosage form
Is chemical modification of the drug into salt or ester forms frequently used to increase solubility?
True
If the solubility of the drug candidate is less than 1 mg mL−1, then salt formation, if possible, is indicated.
True
If solubility cannot be manipulated through salt formation, then a novel dosage form will be required.
True
What are some parameters that determine the solubility of a compound?
Molecular size, substituent groups, degree of ionization
What must be determined for every new drug as a function of pH over the physiological pH?
Solubility
What is the maximum quantity of solvent that can dissolve in a certain quantity of solute at a specified temperature called?
Solubility
Solubility is solely determined by the molecular size of the compound.
False
The solubility of every new drug must be determined as a function of pH over the physiological pH.
True
Ionic strength and temperature do not affect the solubility of a compound.
False
What is a pharmaceutical application of solubility?
To stabilize unstable drugs
Why would solubility be used in formulating sustained release dosage forms?
To utilize poorly soluble or insoluble carriers
What is the purpose of obtaining a homogenous distribution of small amount of drugs at solid state?
To achieve uniform dispersion of drugs
Which type of drugs can be solubilized according to the text?
Oil soluble vitamins, steroid hormones, and antimicrobial agents
What is the result of solubilization of orally administered drugs, as per the text?
Improved appearance and taste
What can be combined in a single phase system in multivitamin preparations?
Both oil soluble and water soluble compounds
What can solubilization lead to?
Enhanced absorption and increased biological activity
In what dosage forms can drug absorption be increased according to the text?
Ointment bases and suppositories
What does solubilization improve according to the text?
Intestinal absorption of vitamin A
What can be used for solubilizing phenolic compounds for use as disinfectants?
Lysol and Roxenol
Which compounds are dissolved with polysorbate by solubilization?
Barbiturates and anticoagulant drugs
What does high aqueous solubility not necessarily guarantee?
Satisfactory absorption
What is the significance of understanding acid and base behavior in drug development?
It helps in determining the solubility of acidic or basic drugs, which is pH dependent
Why is it important to know how the degree of ionization of drugs may change during passage along the gastrointestinal tract?
To understand the impact of pH on the solubility and absorption of drugs
Why is determining the pKa of a drug considered an important step in preformulation characterization?
It helps in understanding the extent of ionization over a range of pH values
Understanding acid and base behavior is extremely important in drug development
True
The solubility of an acidic or basic drug is not pH dependent
False
The pKa of a drug is not a significant factor in preformulation characterization
False
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
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
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?
True
What happens when the pH is significantly below the pKa for a weakly acidic drug?
The drug will be completely unionized
What occurs when the pH is significantly above the pKa for a weakly acidic drug?
The drug will be virtually fully ionized
What does the Henderson Hasselbalch equations allow calculation of?
Extent of ionization of a drug as a function of pH
What is the impact of degree of ionization on solubility?
It increases solubility
What is the purpose of determining pKa values in preformulation?
To understand acid and base behavior of the drug
Why is modern automated instrumentation for determining pKa values considered extremely useful?
It can determine pKa values with very small amounts of drug
In preformulation, why is it important to know how a molecule will distribute itself between aqueous and fatty environments?
To determine the drug's solubility in different physiological conditions
What is the primary consideration in determining approximate values in preformulation assays?
The drug's solubility and partitioning behavior
Why is understanding acid and base behavior important in drug development?
To understand how pH affects the drug's solubility and absorption
What is commonly used as a simple solvent model to mimic the biological lipid bilayers?
n-Octanol
Why is it difficult to develop an analytical method to measure actual partitioning between complex lipophilic phases in a physiological environment?
Complexity and numerousness of the lipophilic phases
What does n-Octanol aim to mimic in the context of drug partitioning?
Short chain hydrocarbons in biological lipid bilayers
Log P values can only be determined experimentally, not calculated from the chemical structure of the drug candidate.
False
Group additivity functions are used to calculate Log P values from the chemical structure of the drug candidate.
True
Group additivity functions are not used to calculate Log P values from the chemical structure of the drug candidate.
False
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.
True
Solubility is solely determined by the molecular size of the compound.
False
Color intensity is related to the extent of conjugated unsaturation as well as the presence of chromophores
True
Hygroscopicity refers to the tendency of a substance to repel water from its immediate environment.
False
An increase in water content can often decrease the rate of chemical degradation of the active ingredient.
False
Wet powders will become more cohesive and flowability is increased.
False
What is the term for the tendency of a substance to attract water from its immediate environment?
Hygroscopicity
What happens to the flowability of wet powders as their water content increases?
It is reduced
How does an increase in water content affect the rate of chemical degradation of the active ingredient in a substance?
It often increases the rate of chemical degradation
What happens to an amorphous matrix when it absorbs water?
Plasticization of the matrix and major structural change
What effect does absorption of water have on freeze-dried amorphous powder?
It often causes structural collapse
What extreme outcome can result from absorption of water by amorphous materials?
Crystallization
How does hygroscopicity affect the compression characteristic, granulation, and hardness of the final product?
It decreases compression characteristic and granulation but improves hardness
Why is hygroscopicity important in aerosol applications?
It enhances the chemical stability of hydrolysable drugs in aerosols
What aspect of drug stability does hygroscopicity affect?
Chemical stability in aqueous environments
What is the primary reason for ensuring the stability of salt forms with respect to environmental humidity?
To avoid the dissolution of the corresponding free acid or base
Which salts are highlighted as examples of being so hygroscopic that they will dissolve in the water they absorb?
Potassium hydroxide and magnesium chloride
Why must the stability of salt forms with respect to environmental humidity be assured?
To prevent chemical degradation of the salt forms
What is the appropriate action if water absorption is likely to cause a detrimental change in physicochemical properties of a drug candidate?
Select suitable packaging and advise the patient on correct storage
What is typically involved in protecting a drug candidate or product from detrimental changes due to water absorption?
Selection of suitable packaging and advising the patient on correct storage
In case of potential detrimental changes due to water absorption, what is the recommended approach for protecting the drug candidate or product?
Selecting suitable packaging and advising on correct storage
Ephedrine & Hyoscymine are hygroscopic in nature
True
Physostigmine is not hygroscopic in nature
False
Hygroscopic & Deliquescent substances absorb moisture from the air.
True
Pilocarpine is not hygroscopic in nature.
False
Glycerinated gelatin & PEG base of suppository are not hygroscopic in nature.
False
Efflorescent substances lose water of hydration when exposed to air.
True
Cocaine is an efflorescent substance.
False
Atropine is a hygroscopic substance.
True
Is water uptake usually determined through a change in mass?
True
Does TGA measure mass as a function of temperature?
True
Does DVS measure mass as a function of humidity at a constant temperature?
True
What are some of the physicochemical properties that differ between different physical forms of a drug?
Solubility, dissolution rate, and crystal habit
Why is the solid state considered the most important when developing a drug candidate into a drug product?
It has the greatest impact on physicochemical properties relevant to drug development
What is the significance of understanding the different physical forms of a drug in drug development?
It impacts bioavailability and therapeutic effectiveness
What is polymorphism in the of crystallization?
When a compound can crystallize to more than one unit cell
What is the form with the highest melting temperature called in polymorphism?
Stable polymorphic form
Why is it important to select the best form of a polymorph for development?
Different polymorphs have different physicochemical properties
What is the defining characteristic of the stable form in polymorphism?
It is the only form at a thermodynamic position of equilibrium
Why is it tempting to consider formulating only the stable polymorph of a drug?
To ensure no change in polymorph on storage
What happens to all metastable forms over time in relation to the stable form?
They eventually convert to the stable form
What can the presence of the B form or the C form of chloramphenicol palmitate dramatically reduce?
Bioavailability
What is the preferred option for development if the stable polymorph shows acceptable bioavailability?
The stable polymorph
What is not necessarily straightforward when it comes to selection of polymorphic form?
Selection of polymorphic form
What does DSC data help differentiate in polymorphs?
Thermodynamic information
What can the heat of fusion, determined by DSC, be used to calculate?
Solubility
What thermodynamic information does DSC provide about polymorphs?
Stability and metastability
Does DSC data differentiate polymorphs based on their melting points and heats of fusion?
True
Can DSC identify which polymorph is stable and which polymorphs are metastable?
True
Is the heat of fusion determined by DSC used to calculate ideal solubility?
True
What can make it difficult for molecules to orient themselves into repeating arrays in amorphous materials?
High molecular weight
In what scenario do molecules forming the solid phase not have sufficient time to align in amorphous materials?
Rapid solid phase formation
What factor can contribute to difficulty in orienting molecules in amorphous materials?
Derivatized polymer as active ingredient
What term is used to describe a solid phase produced by disrupting a preexisting crystal structure with a localized force?
Amorphous
Why do amorphous materials usually have appreciably higher solubilities and faster dissolution rates than their crystalline equivalents?
They have no lattice energy and are essentially unstable
What advantage do amorphous materials offer as an alternative to salt selection to increase the bioavailability of poorly soluble compounds?
They have higher solubilities and faster dissolution rates
What are manufacturing processes frequently affected by?
Particle size and shape
What properties can affect the movement, blending, and compression of powders in manufacturing processes?
Solubility and particle size
Which factor is not typically involved in the influence of powder properties on manufacturing processes?
Thermal conductivity
How is particle shape most easily determined?
By visual inspection with a microscope
When is scanning electron microscopy a better option for determining particle shape?
For spray dried or micronized powder
What makes it difficult to define the particle size of irregularly shaped particles?
The lack of spherical shape
What are the shapes of powder particle size?
All of above
Why should each new drug candidate be tested with the smallest particle size during preformulation?
To facilitate preparation of homogeneous samples and maximize the drug’s surface area for interactions
What does preformulation aim to achieve in relation to drug particles?
Facilitate preparation of homogeneous samples and maximize the drug’s surface area for interactions
Which processes are controlled by surface area in preformulation?
Dissolution and Surface morphology of the drug particles
Particle size and surface area are inversely related: True or false?
True
Smaller drug particles have greater surface area: True or false?
True
Hygroscopic substances repel water from their immediate environment: True or false?
False
increased surface area leads to faster dissolution: True or False
True
High surface area most often reflects a relatively small particle size: true
True
Small particles agglomerate more readily: true
True
Increased surface area leads to slower dissolution: true
False
Particle size distribution and shapes do not affect the chemical and physical properties of drug substances.
False
The biopharmaceutical behavior of solid drugs is not influenced by their particle size distribution and shapes.
False
The effect of particle size distribution and shapes is limited to the physical properties of solid drugs.
False
How does the physical form of a drug influence its bioavailability?
Fine materials are more readily bioavailable than coarse materials
How does size and shape of tablets influence powders and granules?
Size and shape influence the flow and mixing efficiency of powders and granules
How does material size relate to stability and interaction with atmospheric factors?
Fine materials are less susceptible to attack from atmospheric oxygen and humidity than coarse materials
How does particle size influence the stability of dispersions?
It increases stability
What impact does particle size have on bioavailability and therapeutic effectiveness?
It increases bioavailability and therapeutic effectiveness
In what type of formulation is particle size relevant?
Inhaler formulation and ophthalmic formulation
Particle size influences dissolution
True
Particle size influences stability of dispersions
True
Particle size influences bioavailability and therapeutic effectiveness
True
What are the two most relevant methods of assessment at the preformulation stage for powder flow?
Measurement of the angle of repose and measurement of bulk density
Why must powders have good flow properties in pharmaceutical manufacturing?
To fill tablet presses or capsule filling machines and ensure blend uniformity
Why are methods required during preformulation that only need small volumes of powder?
Small volumes allow for more accurate assessment at an early stage
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?
True
Are the Carr’s index and the Hausner ratio calculated from measurements of bulk density?
True
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?
True
Compaction properties are usually very poor for most drug powders, but tablets are rarely made from the drug alone: true
True
Compaction is a result of the compression and cohesion properties of a drug: true
True
Tablets are rarely made from the drug alone: true
True
Excipients play a more significant role in tablet properties than the drug itself for low dose drugs: true
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
True
The majority of the tablet comprises excipients for low dose drugs, making the properties of the drug less important: true
True
What type of properties should a material to be tableted preferably have?
Plastic properties
Why is brittleness considered a beneficial characteristic for a material to be tableted?
Facilitates bond formation during fragmentation
What is the purpose of understanding the compaction properties of a drug candidate at the preformulation stage?
To ensure it can be tableted effectively
What role does water play in altering mechanical properties of high dose drugs?
It acts as a plasticizer
In preformulation, what should happen to excipients if a high dose drug behaves plastically?
Fragment
What should excipients do if a high dose drug does not behave plastically in preformulation?
Deform plastically
Water content can act as a plasticizer, altering mechanical properties of high dose drugs: true or false?
True
If a high dose drug behaves plastically, the excipients should deform plastically: true or false?
False
Water frequently acts as a plasticizer, altering mechanical properties of high dose drugs: true or false?
True
Which of the statements from the Department of a pharmaceutical firm except:
Industrial Pharmacy
Which of the following is a type of quality assurance that involves :
Selection of tools
Which of the following is a type of quality assurance that involves :
all of the above
Which of the following is a type of quality control except
Trainings
Which of the following is a type of quality control that involves:
Walk through
Which of the following is a type of quality control except :
Quality Audit
What is the requirement of sample for determining the hygroscopicity property?
No particular requirement
What is the requirement of sample for determining the solubility property?
Chromophore
Which assay is used to determine the pKa property using:
b+c
Which property is used to determine assay with using HPLC,Plus suitable storage condition?
all of the above
What is the abbreviation of the technique that measures the surface area of particles?
BET
What is the name of the index that measures the compressibility of a powder?
Both A and B
What technique is used to measure the excipient compatibility of a drug?
B+C
What is the term for a solute that requires less than one part of solvent for one part of solute?
Very soluble
What is the range of parts of solvent required for one part of solute for a sparingly soluble solute?
30 - 100
Which of the following solutes is most likely to be insoluble in water?
Oil
What is the color of the substance that has a sulfurous odour and a bitter taste?
Cream-yellow
What is the taste of the substance that has a shiny color and a fruity odour?
Sweet
What is the odour of the substance that has an off-white color and an acidic taste?
Pungent
Test your knowledge of the departments in a pharmaceutical firm with a focus on Research and Development (R&D), including pre-formulation, optimization, scale-up, and analytical method development.
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