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?

Milling, mixing, granulation, tableting Signup and view all the answers

What is the focus of large scale manufacturing according to :

Following the formulation and procedure developed by R&D Signup and view all the answers

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

Production department Signup and view all the answers

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

Sampling and testing semi finished and finished products Signup and view all the answers

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

Test procedures developed by R&D Signup and view all the answers

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

Sampling and testing semi finished and finished products Signup and view all the answers

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

Ensuring that GMPs are being applied Signup and view all the answers

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

QA department Signup and view all the answers

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

Ensuring adherence to GMPs Signup and view all the answers

What is the main focus of Industrial Pharmacy?

Process technology and dosage form design Signup and view all the answers

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

Shorten the development time and increase product quality Signup and view all the answers

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

Shorten the development time and increase product quality Signup and view all the answers

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

Close cooperation with the pharmaceutical industry Signup and view all the answers

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

Design and develop new devices to improve pharmaceutical processes Signup and view all the answers

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

Crystallization techniques in drug manufacturing Signup and view all the answers

What is the main objective of preformulation Formulation?

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

What is the Formulation is

the process of developing a drug candidate into a drug product Signup and view all the answers

What is the ultimate goal of the formulation process?

Developing a mass-producible stable and bioavailable drug product Signup and view all the answers

What does preformulation influence?

Selection of the drug candidate itself Signup and view all the answers

Which aspect of drug development is impacted by preformulation?

Selection of formulation components Signup and view all the answers

What is determined as part of preformulation activities?

All of above Signup and view all the answers

What does preformulation primarily influence in drug development?

Selection of the drug candidate itself Signup and view all the answers

What determines the bioavailability of a drug candidate?

Physicochemical properties and interaction with excipients Signup and view all the answers

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

Physicochemical properties and molecular structure Signup and view all the answers

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

Physicochemical properties of the molecule Signup and view all the answers

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 Signup and view all the answers

How can physicochemical properties of drug candidates be categorized?

Intrinsic to the molecule and derived from bulk behaviour Signup and view all the answers

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

Reduction in development time and costs Signup and view all the answers

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

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

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

To allow approximate values for decision-making Signup and view all the answers

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

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

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

Solvent presence or degradation Signup and view all the answers

How can more quantitative measurements of color be obtained?

Using colorimetry Signup and view all the answers

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

It is based on individual perception Signup and view all the answers

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

True Signup and view all the answers

All compounds that appear to have color are structurally unsaturated

False 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

True Signup and view all the answers

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

True Signup and view all the answers

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

False Signup and view all the answers

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

True Signup and view all the answers

Which factor could help suppress unpalatability in taste?

Coating Signup and view all the answers

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

Coating Signup and view all the answers

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

Flavors Signup and view all the answers

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 Signup and view all the answers

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

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

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

Intermolecular interactions Signup and view all the answers

What is solubility?

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

What forms a solution?

Solute and solvent Signup and view all the answers

What is hydration in the context of solubility?

The process of dissolving solute into water as the solvent 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.

False Signup and view all the answers

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

True 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.

False Signup and view all the answers

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

True Signup and view all the answers

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

False Signup and view all the answers

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

True 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?

Exactly 10 mg mL−1 Signup and view all the answers

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

Liquids for oral gavage or intravenous delivery Signup and view all the answers

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

Greater than 1 mg mL−1 Signup and view all the answers

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

Equilibrium solubility method Signup and view all the answers

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

To determine the degree of solubility Signup and view all the answers

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

They reach a state of balance at a constant temperature Signup and view all the answers

What is frequently used to increase drug solubility?

Chemical modification into salt or ester forms Signup and view all the answers

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

When the solubility is less than 1 mg mL−1 Signup and view all the answers

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

A novel dosage form Signup and view all the answers

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

True 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.

True Signup and view all the answers

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

True Signup and view all the answers

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

Molecular size, substituent groups, degree of ionization Signup and view all the answers

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

Solubility 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?

Solubility Signup and view all the answers

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

False Signup and view all the answers

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

True Signup and view all the answers

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

False Signup and view all the answers

What is a pharmaceutical application of solubility?

To stabilize unstable drugs Signup and view all the answers

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

To utilize poorly soluble or insoluble carriers Signup and view all the answers

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

To achieve uniform dispersion of drugs Signup and view all the answers

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

Oil soluble vitamins, steroid hormones, and antimicrobial agents Signup and view all the answers

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

Improved appearance and taste Signup and view all the answers

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

Both oil soluble and water soluble compounds Signup and view all the answers

What can solubilization lead to?

Enhanced absorption and increased biological activity Signup and view all the answers

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

Ointment bases and suppositories Signup and view all the answers

What does solubilization improve according to the text?

Intestinal absorption of vitamin A Signup and view all the answers

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

Lysol and Roxenol Signup and view all the answers

Which compounds are dissolved with polysorbate by solubilization?

Barbiturates and anticoagulant drugs Signup and view all the answers

What does high aqueous solubility not necessarily guarantee?

Satisfactory absorption Signup and view all the answers

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 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?

To understand the impact of pH on the solubility and absorption of drugs Signup and view all the answers

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 Signup and view all the answers

Understanding acid and base behavior is extremely important in drug development

True Signup and view all the answers

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

False Signup and view all the answers

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

False 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?

True 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?

True 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?

True Signup and view all the answers

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

The drug will be completely unionized Signup and view all the answers

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

The drug will be virtually fully ionized Signup and view all the answers

What does the Henderson Hasselbalch equations allow calculation of?

Extent of ionization of a drug as a function of pH Signup and view all the answers

What is the impact of degree of ionization on solubility?

It increases solubility Signup and view all the answers

What is the purpose of determining pKa values in preformulation?

To understand acid and base behavior of the drug Signup and view all the answers

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

It can determine pKa values with very small amounts of drug 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?

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

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

The drug's solubility and partitioning behavior Signup and view all the answers

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

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

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

n-Octanol 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?

Complexity and numerousness of the lipophilic phases Signup and view all the answers

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

Short chain hydrocarbons in biological lipid bilayers Signup and view all the answers

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

False Signup and view all the answers

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

True 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.

False 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.

True Signup and view all the answers

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

False Signup and view all the answers

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

True Signup and view all the answers

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

False Signup and view all the answers

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

False Signup and view all the answers

Wet powders will become more cohesive and flowability is increased.

False Signup and view all the answers

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

Hygroscopicity Signup and view all the answers

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

It is reduced 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?

It often increases the rate of chemical degradation Signup and view all the answers

What happens to an amorphous matrix when it absorbs water?

Plasticization of the matrix and major structural change Signup and view all the answers

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

It often causes structural collapse Signup and view all the answers

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

Crystallization Signup and view all the answers

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

It decreases compression characteristic and granulation but improves hardness Signup and view all the answers

Why is hygroscopicity important in aerosol applications?

It enhances the chemical stability of hydrolysable drugs in aerosols Signup and view all the answers

What aspect of drug stability does hygroscopicity affect?

Chemical stability in aqueous environments Signup and view all the answers

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 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?

Potassium hydroxide and magnesium chloride Signup and view all the answers

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

To prevent chemical degradation of the salt forms 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?

Select suitable packaging and advise the patient on correct storage Signup and view all the answers

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 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?

Selecting suitable packaging and advising on correct storage Signup and view all the answers

Ephedrine & Hyoscymine are hygroscopic in nature

True Signup and view all the answers

Physostigmine is not hygroscopic in nature

False Signup and view all the answers

Hygroscopic & Deliquescent substances absorb moisture from the air.

True Signup and view all the answers

Pilocarpine is not hygroscopic in nature.

False Signup and view all the answers

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

False Signup and view all the answers

Efflorescent substances lose water of hydration when exposed to air.

True Signup and view all the answers

Cocaine is an efflorescent substance.

False Signup and view all the answers

Atropine is a hygroscopic substance.

True Signup and view all the answers

Is water uptake usually determined through a change in mass?

True Signup and view all the answers

Does TGA measure mass as a function of temperature?

True Signup and view all the answers

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

True Signup and view all the answers

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

Solubility, dissolution rate, and crystal habit Signup and view all the answers

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 Signup and view all the answers

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

It impacts bioavailability and therapeutic effectiveness Signup and view all the answers

What is polymorphism in the of crystallization?

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

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

Stable polymorphic form Signup and view all the answers

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

Different polymorphs have different physicochemical properties Signup and view all the answers

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

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

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

To ensure no change in polymorph on storage Signup and view all the answers

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

They eventually convert to the stable form Signup and view all the answers

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

Bioavailability Signup and view all the answers

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

The stable polymorph Signup and view all the answers

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

Selection of polymorphic form Signup and view all the answers

What does DSC data help differentiate in polymorphs?

Thermodynamic information Signup and view all the answers

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

Solubility Signup and view all the answers

What thermodynamic information does DSC provide about polymorphs?

Stability and metastability Signup and view all the answers

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

True Signup and view all the answers

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

True Signup and view all the answers

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

True Signup and view all the answers

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

High molecular weight Signup and view all the answers

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

Rapid solid phase formation Signup and view all the answers

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

Derivatized polymer as active ingredient 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?

Amorphous Signup and view all the answers

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 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?

They have higher solubilities and faster dissolution rates Signup and view all the answers

What are manufacturing processes frequently affected by?

Particle size and shape Signup and view all the answers

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

Solubility and particle size Signup and view all the answers

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

Thermal conductivity Signup and view all the answers

How is particle shape most easily determined?

By visual inspection with a microscope Signup and view all the answers

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

For spray dried or micronized powder Signup and view all the answers

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

The lack of spherical shape Signup and view all the answers

What are the shapes of powder particle size?

All of above Signup and view all the answers

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 Signup and view all the answers

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 Signup and view all the answers

Which processes are controlled by surface area in preformulation?

Dissolution and Surface morphology of the drug particles Signup and view all the answers

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

True Signup and view all the answers

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

True Signup and view all the answers

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

False Signup and view all the answers

increased surface area leads to faster dissolution: True or False

True Signup and view all the answers

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

True Signup and view all the answers

Small particles agglomerate more readily: true

True Signup and view all the answers

Increased surface area leads to slower dissolution: true

False Signup and view all the answers

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

False Signup and view all the answers

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

False Signup and view all the answers

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

False Signup and view all the answers

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

Fine materials are more readily bioavailable than coarse materials Signup and view all the answers

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

Size and shape influence the flow and mixing efficiency of powders and granules Signup and view all the answers

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 Signup and view all the answers

How does particle size influence the stability of dispersions?

It increases stability Signup and view all the answers

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

It increases bioavailability and therapeutic effectiveness Signup and view all the answers

In what type of formulation is particle size relevant?

Inhaler formulation and ophthalmic formulation Signup and view all the answers

Particle size influences dissolution

True Signup and view all the answers

Particle size influences stability of dispersions

True Signup and view all the answers

Particle size influences bioavailability and therapeutic effectiveness

True Signup and view all the answers

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 Signup and view all the answers

Why must powders have good flow properties in pharmaceutical manufacturing?

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

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

Small volumes allow for more accurate assessment at an early stage 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?

True Signup and view all the answers

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

True 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?

True 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

True Signup and view all the answers

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

True Signup and view all the answers

Tablets are rarely made from the drug alone: true

True Signup and view all the answers

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

True 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

True 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

True Signup and view all the answers

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

Plastic properties Signup and view all the answers

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

Facilitates bond formation during fragmentation Signup and view all the answers

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

To ensure it can be tableted effectively Signup and view all the answers

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

It acts as a plasticizer Signup and view all the answers

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

Fragment Signup and view all the answers

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

Deform plastically Signup and view all the answers

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

True Signup and view all the answers

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

False Signup and view all the answers

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

True Signup and view all the answers

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

Industrial Pharmacy Signup and view all the answers

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

Selection of tools Signup and view all the answers

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

all of the above Signup and view all the answers

Which of the following is a type of quality control except

Trainings Signup and view all the answers

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

Walk through Signup and view all the answers

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

Quality Audit Signup and view all the answers

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

No particular requirement Signup and view all the answers

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

Chromophore Signup and view all the answers

Which assay is used to determine the pKa property using:

b+c Signup and view all the answers

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

all of the above Signup and view all the answers

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

BET Signup and view all the answers

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

Both A and B Signup and view all the answers

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

B+C 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?

Very soluble 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?

30 - 100 Signup and view all the answers

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

Oil Signup and view all the answers

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

Cream-yellow Signup and view all the answers

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

Sweet Signup and view all the answers

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

Pungent 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.