173 Questions
What do reformulation studies in drug development help predict?
Dissolution rates
Why are compatibility studies important in drug development?
To assess the drug's compatibility with excipients and packaging materials
Why is understanding bulk density essential for tablet formulation?
It helps determine the amount of powder that can fit in a space
What do flow properties evaluate in drug powder?
Uniform mixing and precise dosing
Why is the melting point of a drug important in formulation development?
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What is the primary method for determining the kinetic solubility of a drug?
Dissolving the drug in DMSO and adding water, then filtering and measuring concentrations using UV or LC/MS techniques
Which method helps identify polymorphic and amorphous forms of a drug based on solubility?
Thermodynamic solubility
What type of drug molecules are more lipid-soluble and absorb more effectively?
Un-ionized
What does the Henderson-Hasselbach equation estimate for a weak acid or base at a given pH?
Ionization
What does the partition coefficient ($log P$) indicate about a drug?
Drug lipophilicity, with higher values indicating increased drug cross-linking
What does the partition coefficient (log P) indicate about a drug's ability to cross the biological cell membrane?
The higher the log P value, the greater the drug's ability to cross the biological cell membrane
What is the primary method for determining the concentration of a compound in each phase for calculating the partition coefficient?
High Performance Liquid Chromatography (HPLC)
What property is highly desirable for drug absorption, according to the text?
An optimal balance between lipophilicity and solubility
What does the Noyes-Nernst equation describe?
The dissolution rate of solids in a given medium under fixed hydrodynamic conditions
What does the intrinsic dissolution rate (IDR) depend on?
Both solubility and surface area
What parameter influences the dissolution rate of a drug substance?
Surface area
What is the definition of the dissolution rate of a drug substance?
$dC / dt = k1C_s$ where $k1$ is the intrinsic dissolution rate constant and $dC / dt$ is the intrinsic dissolution rate (mg · cm2 /s)
What is drug formulation?
The process of determining the best way to deliver an active ingredient
What is the next step after developing the formulation and dosage form?
Conducting preclinical and clinical studies
What are pharmaceutical excipients classified according to?
Function they perform
What are most new drugs marketed as?
Tablets and capsules
Which process is involved in direct compression for tablet manufacturing?
Milling of APIs and excipients
What is the main advantage of direct compression in tablet manufacturing?
Economical process with fewer unit operations
What is the primary limitation of direct compression in tablet manufacturing?
Challenging formulation for high dose APIs with poor flowability
What characteristic makes direct compression ideal for moisture or heat sensitive APIs?
Elimination of moisture and heat treatment
Which method involves spraying of liquid binder onto the fluidized powder bed followed by drying?
Fluidized bed granulation
What is a disadvantage of high shear granulation?
Mechanical degradation (fragile particles)
What process variable may affect the granulation process in high shear granulation?
Impeller & chopper speed
Which type of APIs are not suitable with wet granulation method?
Moisture and heat sensitive APIs
What is an advantage of fluidized bed granulation?
Offers continuous drying
What affects fluidized bed granulation process?
Fluidising air flow rate/gas velocity
What does high shear granulation involve?
Mixing and spraying of binder liquid on powder bed using a spray nozzle
What is a disadvantage of fluidized bed granulation?
Problems with reproducibility
Which method is suitable for handling fine or dusty powders and improving the compressibility of powders?
Wet granulation
What is the primary advantage of dry granulation over wet granulation?
Cost-effectiveness due to fewer required steps
What does dry granulation aim to prevent in powder blends for oral solid dosage forms?
Segregation
Which process involves compression of powder mixture into large tablets or ribbons?
Dry granulation
What is a primary disadvantage of wet granulation compared to dry granulation?
Time-consuming and complex process
What type of APIs is dry granulation suitable for?
Heat-sensitive APIs
What is the primary purpose of measuring the concentration of a drug in the blood?
To assess the duration of action and effectiveness of the drug
What is the key factor influencing dissolution rate in oral dosage forms?
Particle size and solubility at gastric pH
What is the role of API in pharmaceutical formulation?
API is responsible for providing therapeutic effect
What is the significance of understanding dissolution rate in drug formulation?
To assess bioavailability and absorption rate of the drug
What is the purpose of enteric coated or gastro resistant tablets?
To protect the drug from degrading in the stomach and release drugs under intestine pH conditions
What do suffixes such as CR (controlled release) and SR (sustained release) indicate for prolonged release preparations?
They indicate the release characteristics of the preparation
What happens if tablets modified with active coatings are broken, crushed, or chewed?
The coating's integrity is destroyed, leading to dose dumping
What does repeated action indicate for modified release forms?
Rapid drug release
What type of dosage forms are enteric coated or gastro resistant tablets?
Solid oral dosage forms
What do delayed release dosage forms provide?
A coating that is insoluble in stomach acid conditions
What characteristic makes tablets coated or formulated to prolong release different from other tablets?
They have a higher amount of API than standard dosage forms
What is the primary function of suffixes such as XL (once daily dosing) for prolonged release preparations?
To reduce dosing frequency by providing once daily dosing
Which route allows for precise, accurate, and rapid delivery of APIs?
Intravascular
Which method involves drug absorption through the skin for controlled delivery into the systemic circulation?
Transdermal
Which route of administration involves an injection of fluid into the lower bowel by way of the rectum?
Rectal
What is the primary difference between suspensions and emulsions?
Suspensions mix solid particles with liquids, while emulsions involve one liquid in another
What is the function of syrups in pharmaceutical suspensions?
Contain sucrose or sugar for convenience
What is a key advantage of using pharmaceutical suspensions for drug administration?
Quicker absorption rates
What is necessary for treating patients unable to obtain commercially produced medications?
Extemporaneous compounding
What is the primary role of tertiary packaging in pharmaceutical products?
Ensuring supply chain integrity
Which environmental hazard can cause physical changes, chemical changes, and contamination to pharmaceutical products?
Moisture
What is the main function of primary packaging in pharmaceutical products?
Stability protection
What is the most crucial aspect of an ideal drug pack according to the text?
Product protection from light and moisture
Which primary packaging material is known for its inertness, ease of closure, and easy cleaning?
Glass
What is the most common primary packaging material known for its flexibility, low density, and lightweight nature?
Plastic
Which factor significantly influences medication adherence according to the text?
Packaging type
What is the main reason behind the reduction in the use of metals as packaging material?
Sophistication and customization
What is the purpose of developing anti-tamper seals for pharmaceutical packaging materials?
To ensure product stability and safety
Which secondary packaging material is primarily used for better stacking, display, and physical protection?
Paper/card
What is the most common primary packaging material known for its successful history due to inertness, ease of closure, and easy cleaning?
Glass
What is the primary purpose of tertiary packaging in pharmaceutical products?
Enabling bulk transportation of cartons from the warehouse
What does high shear granulation involve?
Spraying of liquid binder onto a fluidized powder bed followed by drying
Why is understanding bulk density essential for tablet formulation?
To evaluate the flow properties of the tablet powder
What is the significance of understanding dissolution rate in drug formulation?
To prolong the release of the medication
What is the preferred metal for packaging in pharmaceuticals?
Aluminium
Which of the following is a disadvantage of using plastics as primary packaging materials?
Chemical interaction with drug components
What can lead to reduced adherence to medication?
Restricted access to medicines
What is the primary purpose of anti-tamper seals in pharmaceutical packaging materials?
Improving product stability
Which secondary packaging material is primarily used for better stacking and display?
Paper/card
What measure can be taken to aid adherence to medication?
Using devices for physical limitations
What is a disadvantage of blister packs for drug administration?
Causing swallowing issues
What is a potential risk associated with permeation of a pharmaceutical product?
Biological hazards
What is the primary purpose of measuring the concentration of a drug in the blood?
To assess the therapeutic effectiveness and safety of the drug
What characteristic makes tablets coated or formulated to prolong release different from other tablets?
They exhibit delayed onset of action
What is a potential risk associated with permeation of a pharmaceutical product?
Decreased bioavailability of the drug
Why are compatibility studies important in drug development?
To evaluate the stability and interaction of drug components
What is the primary purpose of the 'Yellow Card Scheme' mentioned in the text?
To report potential side effects of any medicine
What is the significance of the 'List of Medicines Under Additional Monitoring' maintained by MHRA and EMA?
It identifies medicines that require additional post-market surveillance
What does obtaining a patent for a new medicine allow a company to do?
Produce the medicine exclusively for the duration of the patent
What is the purpose of assembling data into a 'Dossier' for a marketing authorization application (MA)?
To present evidence for the safety and efficacy of the new product
What is the primary reason why generic drugs are less expensive than branded drugs?
They undergo a less intensive research and drug development process
What is the crucial requirement for a generic medicine to be considered equivalent to the branded drug?
Demonstrating bioequivalence and having the same therapeutic effect as the brand-name drug
What is the main difference in the development process between generic drugs and new drugs?
Generic drugs do not require pre-clinical testing and clinical trials
In what instances might patients be prescribed branded anti-epileptic medicines instead of generic ones?
When the patient cannot be switched between branded and generic medicines
What is the purpose of the Orphan Drugs scheme?
To encourage the development of drugs for rare diseases
Why is it more difficult to undertake clinical trials for paediatric medicines?
Due to the unpredictable long-term effects of new substances in a growing body
What benefits can manufacturers of orphan drugs access?
Assistance with development of trial protocol, scientific advice, 10 year market exclusivity
Why do 90% of the medicines given to children lack sufficient testing for efficacy and safety?
They are only licensed for adults and not specifically tested in children
What is the primary focus of Quality Risk Management (QRM) within a Pharmaceutical Quality System (PQS)?
Identifying and controlling hazards that may affect the quality of the product
What is a key requirement of a Pharmaceutical Quality System (PQS) in relation to the development of medicinal products?
Continuous improvement and development throughout the product's life cycle
What is a primary responsibility of a manufacturer regarding the sale or supply of medicinal products?
Ensuring each batch has been produced and controlled in accordance with regulatory requirements
What does it mean for pharmaceutical products to be 'continually improved and developed throughout its life cycle' as mentioned in the text?
Ongoing enhancement of product safety and efficacy
What is the primary aim of Quality Assurance (QA) in pharmaceutical development?
To ensure the quality required for the intended use of pharmaceutical products
Which organization published a vision in 2003 to create single, harmonized global quality standards based on good science and risk management principles?
The International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH)
What is the primary role of the MHRA in pharmaceutical development?
To oversee regulatory authority in pharmaceutical development
What is the main purpose of the 'The International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use' (ICH)?
To create single, harmonized global quality standards based on good science and risk management principles
What is the difference between Quality Assurance (QA) and Quality Control (QC) in pharmaceutical products?
QA ensures the quality required for intended use while QC focuses on product inspection and testing
What is the primary responsibility of the 'The International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use' (ICH) in relation to worldwide pharmaceutical development?
Producing guidelines about drug development and influencing regulatory authorities
What is the primary responsibility of the 'The International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use' (ICH) in relation to worldwide pharmaceutical development?
Setting standards for clinical trial design and conduct
What characteristic makes tablets coated or formulated to prolong release different from other tablets?
Drug dissolution profile
What property is highly desirable for drug absorption, according to the text?
High solubility in water
What does the Noyes-Nernst equation describe?
The relationship between surface area and dissolution rate
Which factor plays a significant role in the choice of dosage form for incorporating drugs?
Drug properties, administration route, patient characteristics, and therapeutic goals
What is the main advantage of extended-release formulations?
Controlled and sustained drug release
In what instances might patients be prescribed branded anti-epileptic medicines instead of generic ones?
When there are concerns about the bioequivalence of generic versions
What is the primary significance of incorporating drugs into various dosage forms?
Influencing drug bioavailability and absorption
What is the main purpose of targeted drug delivery through creams, ointments, patches, and gels?
Aiming drug delivery to specific sites within the body
Why are oral liquids and dispersible tablets preferred for pediatric and geriatric patients?
They are easier to administer than other dosage forms
What is a significant factor in determining the intended route of administration for a drug's dosage form?
Therapeutic goals
What do preformulation studies in drug development help predict?
Dissolution rates
Why are compatibility studies important in drug development?
To assess the drug's compatibility with excipients and packaging materials
What do flow properties evaluate in drug powder?
Uniform mixing and precise dosing
Which method helps identify polymorphic and amorphous forms of a drug based on solubility?
Thermodynamic solubility
What does the partition coefficient (logP) indicate about a drug?
Drug lipophilicity, with higher values indicating increased drug cross-linking
What does the solubility of a drug determine?
Drug's bioavailability
What plays a significant role in determining the appropriate dosage form for a drug?
Drug's physicochemical properties
What aspect of pharmaceutical formulation significantly impacts the administration and absorption of medications?
Administration and absorption
What do preformulation studies help select appropriate methods for in drug development?
Drug's physicochemical properties
What do analytical methods developed during formulation development and quality control help with?
Accurate quantification
What is essential to understand for tablet formulation in terms of bulk density?
Amount of powder that can fit in a space
What is the primary purpose of tertiary packaging in pharmaceutical products?
To enable bulk transportation in cartons from the warehouse
Why is understanding bulk density essential for tablet formulation?
To improve the compressibility of powders
What does the partition coefficient ($log P$) indicate about a drug's ability to cross the biological cell membrane?
Its ability to be absorbed effectively by lipid-soluble molecules
What characteristic makes tablets coated or formulated to prolong release different from other tablets?
Their ability to release drug slowly over an extended period
What is a primary disadvantage of using plastics as primary packaging materials?
Their permeability to moisture, oxygen, and CO2
What do reformulation studies in drug development help predict?
The stability and safety of the product
What affects fluidized bed granulation process?
Moisture, temperature, pressure, light, and atmospheric gases
What benefits can manufacturers of orphan drugs access?
Exclusivity, tax credits, and marketing subsidies
What does the Yellow Card Scheme mentioned in the text primarily focus on?
Reporting adverse drug reactions and side effects
'What does repeated action indicate for modified release forms?
The ability to release drug slowly over an extended period
What is a disadvantage of using wet granulation compared to dry granulation?
Requirement for drying processes which can increase production time and cost
What does the partition coefficient (log P) indicate about a drug's ability to cross the biological cell membrane?
The higher the log P value, the greater the drug's ability to cross the biological cell membrane
What property is highly desirable for drug absorption, according to the text?
An optimal balance between lipophilicity and solubility
What does the Noyes-Nernst equation describe?
The dissolution rate of solids in a given medium under fixed hydrodynamic conditions
What does the intrinsic dissolution rate (IDR) depend on?
Both solubility and surface area
What is drug formulation?
The process of determining the best way to deliver an active ingredient
What is the next step after developing the formulation and dosage form?
Evaluating the safety and efficacy of the drug product in humans
What are pharmaceutical excipients classified according to?
Function they perform
Which method is used for tablet formulation that compresses tablets from powder blends of API with excipient and lubricant, reducing the number of unit operations required?
Direct compression
What are granulation techniques used for?
To increase density
What does dry granulation involve?
Involves mechanical compression or compaction of powder mixture with binder to facilitate particle agglomeration
What is tablet formulation method does not require operations like feeding, blending, milling, granulation, drying, and coating?
Direct compression (DC)
What is the primary reason for wet granulation not being suitable for moisture and heat-sensitive APIs?
Ideal pH conditions for API stability
What is the main characteristic that makes direct compression ideal for moisture or heat-sensitive APIs?
Elimination of moisture and heat treatment
What is a primary advantage of dry granulation over wet granulation?
Prevention of segregation of APIs
What is a disadvantage of fluidized bed granulation?
Problems with reproducibility
What affects the fluidized bed granulation process?
Fluidising air flow rate/gas velocity
What is the key factor influencing dissolution rate in oral dosage forms?
Drug molecular structure and solubility at gastric pH
What do delayed release dosage forms provide?
Delayed drug release
What does the partition coefficient ($log P$) indicate about a drug's ability to cross the biological cell membrane?
$log P$ value indicates lipid solubility and absorption effectiveness
'What does repeated action indicate for modified release forms?'
Rapid release
What is a disadvantage of blister packs for drug administration?
Limited protection from external factors
What is the primary function of suffixes such as CR (controlled release) and SR (sustained release) for prolonged release preparations?
To reduce dosing frequency by providing once daily dosing
What does repeated action indicate for modified release forms?
Rapid drug release
What is the significance of understanding dissolution rate in drug formulation?
To assess bioavailability and absorption rate of the drug
What characteristic makes tablets coated or formulated to prolong release different from other tablets?
They have a higher amount of API than standard dosage forms
What is necessary for treating patients unable to obtain commercially produced medications?
Extemporaneous compounding
Which method involves drug absorption through the skin for controlled delivery into the systemic circulation?
Transdermal delivery
What is the primary responsibility of 'The International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use' (ICH) in relation to worldwide pharmaceutical development?
Ensuring harmonization of technical requirements for drug registration
What can lead to reduced adherence to medication?
High cost of medication
What is a primary disadvantage of wet granulation compared to dry granulation?
Risk of oxidation of sensitive drugs
What affects fluidized bed granulation process?
Particle size and solubility at gastric pH
What is the primary difference between suspensions and emulsions?
Suspensions mix solid particles with liquids while emulsions involve one liquid in another
Why is understanding bulk density essential for tablet formulation?
To ensure proper flow properties during manufacturing processes
Study Notes
- Segregation of APIs in powder blends can be reduced by careful formulation design, including selection of excipients and ordered mixing.
- Dry granulation is a technique used to improve the flowability, compactability, and prevent segregation of powder blends for oral solid dosage forms.
- Dry granulation process can be performed using roller compaction or slugging methods, with following steps: milling of APIs and excipients, blending of powder mix, compression of powder mixture into large tablets or ribbons, milling of tablets or ribbons, and mixing with lubricant and disintegrating agent.
- Dry granulation is suitable for APIs that are sensitive to solvents, heat, and moisture, and is more cost-effective than wet granulation due to fewer required steps.
- Wet granulation is another common method for manufacturing oral solid dosage forms, which involves wet massing of API and excipients with a granulation liquid (with or without polymeric binder), followed by wet sizing and drying, with following steps: milling of APIs and excipients, mixing of powder mix, agglomeration of solution binder with powder mix, drying of moist granules, milling of dry granules, and mixing of screened granules.
- Wet granulation is suitable for handling fine or dusty powders, improving the compressibility of powders, and preventing segregation of APIs, as well as improving the dissolution of hydrophobic drugs.
- However, wet granulation requires many expensive equipments and a large space due to multiple unit operations, and is a time-consuming and complex process, especially during the drying phase.
- Wet granulation is not suitable for moisture and heat sensitive APIs.
- Both dry and wet granulation methods require feeders for continuous manufacturing.
Test your knowledge of preformulation studies, which are essential for understanding the physical and chemical properties of drug substances. These studies help in selecting appropriate formulation methods, predicting dissolution rates, assessing chemical stability under varying environmental conditions, and designing drug formulations for specific routes of administration.
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