chapter 1 Preformulation
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Questions and Answers

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

  • Human resources management
  • Financial planning and budgeting
  • Marketing and sales strategies
  • Pre formulation, optimization, and scale up , analtyical method development ,setting up , specification ,process validation (correct)

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

  • Process validation
  • Analytical method development
  • Manufacturing large-scale production batches (correct)
  • Setting up specifications for raw materials

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

  • Small scale laboratory and pilot scale up (correct)
  • Administrative offices
  • Large-scale industrial production units
  • Logistics and distribution centers

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

    <p>Milling, mixing, granulation, tableting</p> Signup and view all the answers

    What is the focus of large scale manufacturing according to :

    <p>Following the formulation and procedure developed by R&amp;D</p> Signup and view all the answers

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

    <p>Production department</p> Signup and view all the answers

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

    <p>Sampling and testing semi finished and finished products</p> Signup and view all the answers

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

    <p>Test procedures developed by R&amp;D</p> Signup and view all the answers

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

    <p>Sampling and testing semi finished and finished products</p> Signup and view all the answers

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

    <p>Ensuring that GMPs are being applied</p> Signup and view all the answers

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

    <p>QA department</p> Signup and view all the answers

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

    <p>Ensuring adherence to GMPs</p> Signup and view all the answers

    What is the main focus of Industrial Pharmacy?

    <p>Process technology and dosage form design</p> Signup and view all the answers

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

    <p>Shorten the development time and increase product quality</p> Signup and view all the answers

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

    <p>Shorten the development time and increase product quality</p> Signup and view all the answers

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

    <p>Close cooperation with the pharmaceutical industry</p> Signup and view all the answers

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

    <p>Design and develop new devices to improve pharmaceutical processes</p> Signup and view all the answers

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

    <p>Crystallization techniques in drug manufacturing</p> Signup and view all the answers

    What is the main objective of preformulation Formulation?

    <p>developing most stable and bioavailable dosage form that mass can be produced</p> Signup and view all the answers

    What is the Formulation is

    <p>the process of developing a drug candidate into a drug product</p> Signup and view all the answers

    What is the ultimate goal of the formulation process?

    <p>Developing a mass-producible stable and bioavailable drug product</p> Signup and view all the answers

    What does preformulation influence?

    <p>Selection of the drug candidate itself</p> Signup and view all the answers

    Which aspect of drug development is impacted by preformulation?

    <p>Selection of formulation components</p> Signup and view all the answers

    What is determined as part of preformulation activities?

    <p>All of above</p> Signup and view all the answers

    What does preformulation primarily influence in drug development?

    <p>Selection of the drug candidate itself</p> Signup and view all the answers

    What determines the bioavailability of a drug candidate?

    <p>Physicochemical properties and interaction with excipients</p> Signup and view all the answers

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

    <p>Physicochemical properties and molecular structure</p> Signup and view all the answers

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

    <p>Physicochemical properties of the molecule</p> Signup and view all the answers

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

    <p>To provide fundamental knowledge for candidate selection and dosage form design, reducing development time and costs</p> Signup and view all the answers

    How can physicochemical properties of drug candidates be categorized?

    <p>Intrinsic to the molecule and derived from bulk behaviour</p> Signup and view all the answers

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

    <p>Reduction in development time and costs</p> Signup and view all the answers

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

    <p>To make a 'go / no go' decision for a specific drug candidate</p> Signup and view all the answers

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

    <p>To allow approximate values for decision-making</p> Signup and view all the answers

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

    <p>Making a 'go / no go' decision for a specific drug candidate</p> Signup and view all the answers

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

    <p>Solvent presence or degradation</p> Signup and view all the answers

    How can more quantitative measurements of color be obtained?

    <p>Using colorimetry</p> Signup and view all the answers

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

    <p>It is based on individual perception</p> Signup and view all the answers

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

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

    All compounds that appear to have color are structurally unsaturated

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

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

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

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

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

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

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

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

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

    Which factor could help suppress unpalatability in taste?

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

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

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

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

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

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

    <p>It is assumed that the chemists preparing the candidate molecules will provide this information</p> Signup and view all the answers

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

    <p>Solubility will be dependent on the physical form (polymorph, pseudopolymorph or amorphous)</p> Signup and view all the answers

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

    <p>Intermolecular interactions</p> Signup and view all the answers

    What is solubility?

    <p>The maximum quantity of solute that can dissolve in a certain quantity of solvent at a specified temperature</p> Signup and view all the answers

    What forms a solution?

    <p>Solute and solvent</p> Signup and view all the answers

    What is hydration in the context of solubility?

    <p>The process of dissolving solute into water as the solvent</p> Signup and view all the answers

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

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

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

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

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

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

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

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

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

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

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

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

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

    <p>Exactly 10 mg mL−1</p> Signup and view all the answers

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

    <p>Liquids for oral gavage or intravenous delivery</p> Signup and view all the answers

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

    <p>Greater than 1 mg mL−1</p> Signup and view all the answers

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

    <p>Equilibrium solubility method</p> Signup and view all the answers

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

    <p>To determine the degree of solubility</p> Signup and view all the answers

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

    <p>They reach a state of balance at a constant temperature</p> Signup and view all the answers

    What is frequently used to increase drug solubility?

    <p>Chemical modification into salt or ester forms</p> Signup and view all the answers

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

    <p>When the solubility is less than 1 mg mL−1</p> Signup and view all the answers

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

    <p>A novel dosage form</p> Signup and view all the answers

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

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

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

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

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

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

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

    <p>Molecular size, substituent groups, degree of ionization</p> Signup and view all the answers

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

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

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

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

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

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

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

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

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

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

    What is a pharmaceutical application of solubility?

    <p>To stabilize unstable drugs</p> Signup and view all the answers

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

    <p>To utilize poorly soluble or insoluble carriers</p> Signup and view all the answers

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

    <p>To achieve uniform dispersion of drugs</p> Signup and view all the answers

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

    <p>Oil soluble vitamins, steroid hormones, and antimicrobial agents</p> Signup and view all the answers

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

    <p>Improved appearance and taste</p> Signup and view all the answers

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

    <p>Both oil soluble and water soluble compounds</p> Signup and view all the answers

    What can solubilization lead to?

    <p>Enhanced absorption and increased biological activity</p> Signup and view all the answers

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

    <p>Ointment bases and suppositories</p> Signup and view all the answers

    What does solubilization improve according to the text?

    <p>Intestinal absorption of vitamin A</p> Signup and view all the answers

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

    <p>Lysol and Roxenol</p> Signup and view all the answers

    Which compounds are dissolved with polysorbate by solubilization?

    <p>Barbiturates and anticoagulant drugs</p> Signup and view all the answers

    What does high aqueous solubility not necessarily guarantee?

    <p>Satisfactory absorption</p> Signup and view all the answers

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

    <p>It helps in determining the solubility of acidic or basic drugs, which is pH dependent</p> Signup and view all the answers

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

    <p>To understand the impact of pH on the solubility and absorption of drugs</p> Signup and view all the answers

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

    <p>It helps in understanding the extent of ionization over a range of pH values</p> Signup and view all the answers

    Understanding acid and base behavior is extremely important in drug development

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

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

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

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

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

    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?

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

    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?

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

    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?

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

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

    <p>The drug will be completely unionized</p> Signup and view all the answers

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

    <p>The drug will be virtually fully ionized</p> Signup and view all the answers

    What does the Henderson Hasselbalch equations allow calculation of?

    <p>Extent of ionization of a drug as a function of pH</p> Signup and view all the answers

    What is the impact of degree of ionization on solubility?

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

    What is the purpose of determining pKa values in preformulation?

    <p>To understand acid and base behavior of the drug</p> Signup and view all the answers

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

    <p>It can determine pKa values with very small amounts of drug</p> Signup and view all the answers

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

    <p>To determine the drug's solubility in different physiological conditions</p> Signup and view all the answers

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

    <p>The drug's solubility and partitioning behavior</p> Signup and view all the answers

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

    <p>To understand how pH affects the drug's solubility and absorption</p> Signup and view all the answers

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

    <p>n-Octanol</p> Signup and view all the answers

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

    <p>Complexity and numerousness of the lipophilic phases</p> Signup and view all the answers

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

    <p>Short chain hydrocarbons in biological lipid bilayers</p> Signup and view all the answers

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

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

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

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

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

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

    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.

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

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

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

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

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

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

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

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

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

    Wet powders will become more cohesive and flowability is increased.

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

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

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

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

    <p>It is reduced</p> Signup and view all the answers

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

    <p>It often increases the rate of chemical degradation</p> Signup and view all the answers

    What happens to an amorphous matrix when it absorbs water?

    <p>Plasticization of the matrix and major structural change</p> Signup and view all the answers

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

    <p>It often causes structural collapse</p> Signup and view all the answers

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

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

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

    <p>It decreases compression characteristic and granulation but improves hardness</p> Signup and view all the answers

    Why is hygroscopicity important in aerosol applications?

    <p>It enhances the chemical stability of hydrolysable drugs in aerosols</p> Signup and view all the answers

    What aspect of drug stability does hygroscopicity affect?

    <p>Chemical stability in aqueous environments</p> Signup and view all the answers

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

    <p>To avoid the dissolution of the corresponding free acid or base</p> Signup and view all the answers

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

    <p>Potassium hydroxide and magnesium chloride</p> Signup and view all the answers

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

    <p>To prevent chemical degradation of the salt forms</p> Signup and view all the answers

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

    <p>Select suitable packaging and advise the patient on correct storage</p> Signup and view all the answers

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

    <p>Selection of suitable packaging and advising the patient on correct storage</p> Signup and view all the answers

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

    <p>Selecting suitable packaging and advising on correct storage</p> Signup and view all the answers

    Ephedrine & Hyoscymine are hygroscopic in nature

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

    Physostigmine is not hygroscopic in nature

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

    Hygroscopic & Deliquescent substances absorb moisture from the air.

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

    Pilocarpine is not hygroscopic in nature.

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

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

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

    Efflorescent substances lose water of hydration when exposed to air.

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

    Cocaine is an efflorescent substance.

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

    Atropine is a hygroscopic substance.

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

    Is water uptake usually determined through a change in mass?

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

    Does TGA measure mass as a function of temperature?

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

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

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

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

    <p>Solubility, dissolution rate, and crystal habit</p> Signup and view all the answers

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

    <p>It has the greatest impact on physicochemical properties relevant to drug development</p> Signup and view all the answers

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

    <p>It impacts bioavailability and therapeutic effectiveness</p> Signup and view all the answers

    What is polymorphism in the of crystallization?

    <p>When a compound can crystallize to more than one unit cell</p> Signup and view all the answers

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

    <p>Stable polymorphic form</p> Signup and view all the answers

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

    <p>Different polymorphs have different physicochemical properties</p> Signup and view all the answers

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

    <p>It is the only form at a thermodynamic position of equilibrium</p> Signup and view all the answers

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

    <p>To ensure no change in polymorph on storage</p> Signup and view all the answers

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

    <p>They eventually convert to the stable form</p> Signup and view all the answers

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

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

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

    <p>The stable polymorph</p> Signup and view all the answers

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

    <p>Selection of polymorphic form</p> Signup and view all the answers

    What does DSC data help differentiate in polymorphs?

    <p>Thermodynamic information</p> Signup and view all the answers

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

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

    What thermodynamic information does DSC provide about polymorphs?

    <p>Stability and metastability</p> Signup and view all the answers

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

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

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

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

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

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

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

    <p>High molecular weight</p> Signup and view all the answers

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

    <p>Rapid solid phase formation</p> Signup and view all the answers

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

    <p>Derivatized polymer as active ingredient</p> Signup and view all the answers

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

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

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

    <p>They have no lattice energy and are essentially unstable</p> Signup and view all the answers

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

    <p>They have higher solubilities and faster dissolution rates</p> Signup and view all the answers

    What are manufacturing processes frequently affected by?

    <p>Particle size and shape</p> Signup and view all the answers

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

    <p>Solubility and particle size</p> Signup and view all the answers

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

    <p>Thermal conductivity</p> Signup and view all the answers

    How is particle shape most easily determined?

    <p>By visual inspection with a microscope</p> Signup and view all the answers

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

    <p>For spray dried or micronized powder</p> Signup and view all the answers

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

    <p>The lack of spherical shape</p> Signup and view all the answers

    What are the shapes of powder particle size?

    <p>All of above</p> Signup and view all the answers

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

    <p>To facilitate preparation of homogeneous samples and maximize the drug’s surface area for interactions</p> Signup and view all the answers

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

    <p>Facilitate preparation of homogeneous samples and maximize the drug’s surface area for interactions</p> Signup and view all the answers

    Which processes are controlled by surface area in preformulation?

    <p>Dissolution and Surface morphology of the drug particles</p> Signup and view all the answers

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

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

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

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

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

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

    increased surface area leads to faster dissolution: True or False

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

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

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

    Small particles agglomerate more readily: true

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

    Increased surface area leads to slower dissolution: true

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

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

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

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

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

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

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

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

    <p>Fine materials are more readily bioavailable than coarse materials</p> Signup and view all the answers

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

    <p>Size and shape influence the flow and mixing efficiency of powders and granules</p> Signup and view all the answers

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

    <p>Fine materials are less susceptible to attack from atmospheric oxygen and humidity than coarse materials</p> Signup and view all the answers

    How does particle size influence the stability of dispersions?

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

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

    <p>It increases bioavailability and therapeutic effectiveness</p> Signup and view all the answers

    In what type of formulation is particle size relevant?

    <p>Inhaler formulation and ophthalmic formulation</p> Signup and view all the answers

    Particle size influences dissolution

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

    Particle size influences stability of dispersions

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

    Particle size influences bioavailability and therapeutic effectiveness

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

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

    <p>Measurement of the angle of repose and measurement of bulk density</p> Signup and view all the answers

    Why must powders have good flow properties in pharmaceutical manufacturing?

    <p>To fill tablet presses or capsule filling machines and ensure blend uniformity</p> Signup and view all the answers

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

    <p>Small volumes allow for more accurate assessment at an early stage</p> Signup and view all the answers

    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?

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

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

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

    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?

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

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

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

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

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

    Tablets are rarely made from the drug alone: true

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

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

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

    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

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

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

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

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

    <p>Plastic properties</p> Signup and view all the answers

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

    <p>Facilitates bond formation during fragmentation</p> Signup and view all the answers

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

    <p>To ensure it can be tableted effectively</p> Signup and view all the answers

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

    <p>It acts as a plasticizer</p> Signup and view all the answers

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

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

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

    <p>Deform plastically</p> Signup and view all the answers

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

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

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

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

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

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

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

    <p>Industrial Pharmacy</p> Signup and view all the answers

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

    <p>Selection of tools</p> Signup and view all the answers

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

    <p>all of the above</p> Signup and view all the answers

    Which of the following is a type of quality control except

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

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

    <p>Walk through</p> Signup and view all the answers

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

    <p>Quality Audit</p> Signup and view all the answers

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

    <p>No particular requirement</p> Signup and view all the answers

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

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

    Which assay is used to determine the pKa property using:

    <p>b+c</p> Signup and view all the answers

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

    <p>all of the above</p> Signup and view all the answers

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

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

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

    <p>Both A and B</p> Signup and view all the answers

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

    <p>B+C</p> Signup and view all the answers

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

    <p>Very soluble</p> Signup and view all the answers

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

    <p>30 - 100</p> Signup and view all the answers

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

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

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

    <p>Cream-yellow</p> Signup and view all the answers

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

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

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

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

    Study Notes

    Research and Development (R&D) in Pharmaceuticals

    • Focuses on developing new drug formulations and processes.
    • Typically does NOT handle large-scale production activities.
    • Conducts research in innovative and controlled laboratory environments.

    Production in Large Scale Manufacturing

    • Primary activity involves producing pharmaceutical products on a large scale.
    • Responsible for ensuring efficiency and compliance with regulations.

    Quality Control and Quality Assurance

    • Process validation is overseen by the Quality Assurance (QA) department.
    • Analytical labs in the Quality Control (QC) department conduct various testing, including potency and purity assessments.
    • QC labs utilize procedures like UV and HPLC (High-Performance Liquid Chromatography) for testing.
    • A key responsibility of the QC department is to ensure product quality and regulatory compliance.
    • The main role of the QA department is to oversee manufacturing processes and validations.

    Industrial Pharmacy Focus

    • Concentrates on robust formulations and process technologies.
    • Pharmaceutical industry seeks efficient formulations that ensure API stability and enhance bioavailability.
    • Aims include successful scale-up and understanding of pharmaceutical processes.

    Preformulation in Drug Development

    • Main objective is to prepare optimal formulations before clinical testing.
    • Influences the drug's release, absorption, and therapeutic effectiveness.
    • Determines key parameters such as solubility and stability.

    Physicochemical Properties

    • Characterization of properties influences drug processing and formulation success.
    • Early assessment of physicochemical properties can predict product behavior and performance.
    • A suitable assay in preformulation helps establish validation criteria for drug testing.

    Solubility Considerations

    • Solubility is defined as the maximum amount of solute that can dissolve in a solvent at a specific temperature.
    • Solvation occurs during hydration, particularly when water is the solvent.
    • High aqueous solubility is crucial for oral drug delivery.
    • Up to 40% of drug candidates may fail due to poor solubility, impacting absorption.

    Salt Formation and Drug Candidates

    • Salt formation is a common method to enhance solubility.
    • If low solubility persists, alternative formulation strategies (like novel dosage forms) are necessary.
    • The chemical structure of drug candidates can impact their processing and solubility.

    Ionic Behavior and pH Considerations

    • Understanding acid-base behavior is vital for predicting drug performance in different physiological environments.
    • The Henderson-Hasselbalch equation is essential for calculating drug ionization levels at varying pH.
    • Drug ionization significantly affects solubility, absorption, and therapeutic efficacy.

    Solubilization and Absorption

    • Solubilization improves drug absorption, particularly for orally administered drugs.
    • Polysorbate is often used to solubilize phenolic compounds.
    • While high aqueous solubility can aid absorption, it does not guarantee therapeutic effectiveness.

    Important True/False Statements

    • True: No drug can enter systemic circulation without first being in solution.
    • True: The Henderson-Hasselbalch equation allows the calculation of ionization extent based on pH and pKa.
    • False: Solubility is solely determined by the molecular size of the compound.

    Summary of Key Points

    • Robust formulations are essential for successful drug development.
    • Physicochemical property characterization at an early stage can significantly influence therapeutic development.
    • Salt formation and understanding pH behavior are critical components in enhancing drug solubility and bioavailability.

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    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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