1 - Intro to Dosage Form Design Flashcards
Define drug
Agent for diagnosis, mitigation, treatment, cure, or prevention of disease
What are the 3 chemical classes of all medications?
- Inorganic
- Organic
- Biological
What is the major goal of drug delivery?
To obtain the highest drug effects in the simplest administration way
What is a dosage form?
- Physical form consisting of active ingredient(s) and pharmaceutical excipients
- Stable, safe, attractive, easy to produce/use
- Unit dose
Why do we have to design different dosage forms?
- Prevent from degradation
- Conceal flavour, taste, or odour
- Facilitate mass production
- Use accurate dose
- Provide product choice
- Enhance therapeutic outcome
What are the 6 stages of drug development?
1) New chemical entity
2) Preclinical studies
3) Investigational new drug
4) Clinical trials
5) New drug application
6) Post-marketing
What is involved in the “new chemical entity” stage of drug development?
Finding of a compound as a potential drug candidate, including chemical synthesis, extraction, separation, and purification
What is involved in the “preclinical studies” stage of drug development?
- Preliminary investigation on the suitability of a new chemical entity as a therapeutic agent
- Early stage includes physical and chemical characterization, pharmacological and toxicological evaluations and in vivo behaviours
- Later stage involves long-term toxicity, formulation dev’t and assessment, and preparation for new drug product launch
What is involved in the “investigational new drug application” stage of drug development?
- Submission of basic info of a new chemical compound for review
- Clinical studies in humans can commence only after approval of IND application
What is involved in the “clinical trials” stage of drug development?
- Phase 1 – drug safety in 20-100 subjects
- Phase 2 – drug efficact in 100’s of subjects
- Phase 3 – drug efficacy and dose evaluation in 1000’s of subjects
What is involved in the “new drug application” stage of drug development?
Submission of complete info of a chemical entity for review by health authority
How long does each stage of drug development take?
About 2-3 years, so entire process can take 10-15 years
What are some in vitro tests? What is the goal of these tests?
- Goal = to assess basic characteristics of a chemical compound
- Physical/chemical properties
- Drug/excipient interactions
- Stability considerations
- Production feasibilities
What are the 4 stages that every drug undergoes?
Absorption, distribution, metabolism, and excretion
What is bioequivalency?
Bioavailability comparison of different formulations, products, or batches of the same active ingredient
What are the most popular formulations?
- Tablets/capsules = 60%
- Sterile products = 15%
- Solutions = 15%
- All other products = 10%
____ formulations are always the first choice because ______
- Solid
- Easy and cheap to make
What can be accomplished by modifying drug release rate?
- Sustain drug absorption in GI
- Prolong systemic drug effects
- Reduce administration frequency
- Minimize potential adverse effects
What can be accomplished by formulating an injectable?
- Deliver drug directly into blood
- Optimize drug bioavailability
- Achieve fast drug action
Which formulations provide the fastest absorption of nitroglycerin?
IV, buccal, and sublingual
What is the easiest application of nitroglycerin?
Transdermal
What are some factors that must be considered before an appropriate preparation can be put into large-scale production?
- Physicochemical properties (solubility, particle size, salt form, pH, pKa)
- Biological characteristics (ADME)
- Route of administration
- Excipient properties (interaction, dissolution, disintegration, drug release)
Which characteristics do suspending agents affect?
- Stability
- Dose accuracy
What characteristics do emulsifiers affect?
- Emulsion type
- Particle size
- Stability
What characteristics do binders affect?
- Disintegration
- Dissolution
- Bioavailability
What characteristics do lubricants affect?
- Dissolution
- Bioavailability
How is most data on drug doses obtained?
From various animal studies and then extrapolated into doses appropriate for human applications
What factors must be considered when deciding drug dose?
- Toxic dose
- ADME
- Subject conditions
- Drug interactions
- Tolerance/dependence
- Patient compliance
What are advantages to computer-aid drug design?
- Reduce time and resource
- Eliminate in vivo testing
- Focus on functional groups
- Minimize side effects and toxicity
What are some improvements that can be made to bioavailability?
- Increase drug absorption
- Reduce drug metabolism
- Eliminate drug degradation
- Prolong drug retention
- Direct drug to specific sites
What are advantages to controlled drug release or specific-site drug targeting?
- Reduce administration frequency
- Minimize potential adverse drug effects
- Increase therapeutic outcomes
- Provide more product choices
What are the goals for dosage form development?
- Most effective result
- Most appropriate form
- Most convenient application
- Most acceptable approach
- Most economic production
