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active
transport of drugs:
Carriage
of a solute across a biological membrane, which requires a suitable carrier and
the expenditure of energy.
adjuvant:
1.
Additive with no intended pharmacological action, used in the formulation of
dosage forms. 2. In pharmacology,
a substance added to a drug to speed or increase the action of the main
component. 3. In immunology, a substance (such as aluminum hydroxide) or an
organism (such as killed mycobacterium) that increases the response to an
antigen. IUPAC Pharmaceutics
adjuvants vaccines:
An
adjuvant is a substance that is formulated as part of a vaccine to enhance
its ability to induce protection against infection. The word “adjuvant”
comes from the Latin adjuvare and means “to help.” Adjuvants help activate
the immune system, allowing the antigens — pathogen components that elicit
an immune response — in vaccines to induce long-term protective immunity.
NIH, NIAID
https://www.niaid.nih.gov/research/vaccine-adjuvants
antibody drug conjugates: Biologics
bioavailability:
1.
Ratio of the systemic exposure from extravascular (ev) exposure to that
following intravenous (iv) exposure as described by the equation: where F is
the bioavailability, A and B are areas under the (plasma)
concentration-time curve following ev and iv administration,
respectively, and Dev and Div are the administered ev and iv
doses. 2. Relative amount of the administered dose of a drug that reaches
systemic circulation from a certain dosage form in comparison to the
amount that reaches the systemic circulation by iv administration. See
also relative bioavailability.
[7,12]
As indicated in Chapter 21 CFR (Codes of Federal
Regulations) Part 320.1, bioavailability of a drug is defined as the
extent and rate to which the active drug ingredient or active moiety from
the drug product is absorbed and becomes available at the site of drug
action. The extent and rate of drug absorption are usually measured by the
area under the blood or plasma concentration-time curve (AUC) and the
maximum concentration (Cmax), respectively. For drug products that are not
intended to be absorbed into bloodstream, bioavailability may be assessed
by measurements intended to reflect the rate and extent to which the
active ingredient or active moiety is absorbed and becomes available at
the site of action. A comparative bioavailability study refers to the
comparison of bioavailabilities of different formulations of the same drug
or different drug products. As indicated in Chow and Liu (2008),
the definition of bioavailability has evolved over time with different
meanings by different individuals and organizations [1].
For example, differences are evident in the definitions by Academy of
Pharmaceutical Sciences in 1972, the Office of Technology Assessment (OTA)
of the Congress of the United States in 1974, and the 1984 Drug Price
Competition and Patent Restoration Act which is amendments to the Food,
Drug, and Cosmetic Act. For more discussion regarding the definition of
bioavailability, see [2-4].
Bioavailability and Bioequivalence in Drug Development. Wiley Interdiscip
Rev Comput Stat. 2014;6(4):304-312.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4157693/
bioequivalence:
a term in pharmacokinetics used
to assess the expected in vivo biological
equivalence of two proprietary preparations of a drug. If two products are said
to be bioequivalent it means that they would be expected to be, for all intents
and purposes, the same. ... Birkett (2003) defined bioequivalence by stating
that, "two pharmaceutical products are bioequivalent if they are
pharmaceutically equivalent and their bioavailabilities (rate
and extent of availability) after administration in the same molar dose are
similar to such a degree that their effects, with respect to both efficacy and
safety, can be expected to be essentially the same. Pharmaceutical equivalence
implies the same amount of the same active substance(s), in the same dosage
form, for the same route of administration and meeting the same or comparable
standards."[1]
For The World
Health Organization (WHO) "two
pharmaceutical products are bioequivalent if they are pharmaceutically
equivalent or pharmaceutical alternatives, and their bioavailabilities, in terms
of rate (Cmax and tmax) and extent of absorption (area under the curve), after
administration of the same molar dose under the same conditions, are similar to
such a degree that their effects can be expected to be essentially the same" [2].
The United States Food
and Drug Administration (FDA) has defined bioequivalence as, "the absence of
a significant difference in the rate and extent to which the active ingredient
or active moiety in pharmaceutical equivalents or pharmaceutical alternatives
becomes available at the site of drug action when administered at the same molar
dose under similar conditions in an appropriately designed study."[3]
Wikipedia accessed 2018 Nov 6
https://en.wikipedia.org/wiki/Bioequivalence
When two formulations
of the same drug or two drug products are claimed bioequivalent, it is
assumed that they will provide the same therapeutic effect or that they
are therapeutically equivalent. In this case, most people interpret that
they can be used interchangeably. Two drug products are
considered pharmaceutical equivalents if they contain identical amounts of
the same active ingredient. Two drugs are identified as pharmaceutical
alternatives to each other if both contain an identical therapeutic
moiety, but not necessarily in the same amount or dosage form or as the
same salt or ester. Two drug products are said to be bioequivalent if they
are pharmaceutical equivalents (i.e., similar dosage forms made, perhaps,
by different manufacturers) or pharmaceutical alternatives (i.e.,
different dosage forms) and if their rates and extents of absorption do
not show a significant difference to which the active ingredient or active
moiety in pharmaceutical equivalents or pharmaceutical alternatives become
available at the site of action when administered at the same molar dose
under similar conditions in an appropriately designed study.
Bioavailability and Bioequivalence in Drug Development. Wiley Interdiscip
Rev Comput Stat. 2014;6(4):304-312.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4157693/
biological availability:
The extent to which the active ingredient of a drug dosage form becomes
available at the site of drug action or in a biological medium believed to
reflect accessibility to a site of action. MeSH 1979
biopharmaceutics: The
study of the chemical and physical properties
of drugs, and the relationship between
these, dosage, and activity
Wiktionary
https://en.wiktionary.org/wiki/biopharmaceutics
biologics
formulation:
Optimizing Biologics
Formulation Development January
20-21, 2020 • San Diego, CA
formulation challenges of emerging modalities, new strategies for
predictive analysis at this stage, exciting new analytical methodologies and
accelerating and the best practices being employed to overcome formulation
challenges.
https://www.chi-peptalk.com/biologics-formulation/
Blood-Brain Barrier June
19-20, 2018
• Boston, MA | Antibodies and
new drugs that are promising for treating brain diseases and disorders are often
limited by poor brain exposure. Research is focused on examining new ways to
deliver drugs to the brain, including gene therapy and treatment of the BBB’s
microvessels. Cambridge Healthtech Institute’s Fourth Annual Blood-Brain
Barrier conference will focus on the key areas of understanding BBB
transport and dysfunction in disease through a series of case studies and
cutting-edge research presentations. This conference will address questions
surrounding BBB permeability, blood flow, translational research, and biomarkers
of BBB breakdown. Special attention will be paid to in vivo models and tools
that are available to investigate BBB transport and pathology in disease. The
conference will also provide updates from the industry on antibody delivery and
transport across the BBB.
Blood Brain Barrier
and
CNS Drug Discovery
Strategies and Tools
to Address Hurdles in CNS Drug Discovery
APRIL 12, 2019 San DIEGo CA
The blood-brain barrier (BBB) plays a critical role in brain homeostasis –
a function it does so well that scientists and drug developers continue to
grapple with the challenges of delivering drugs into the brain to treat
devastating and life-threatening diseases such as brain cancer and
neurodegenerative disorders. As we understand more about the state of the
BBB in a healthy and a disease-challenged brain, novel strategies, methods
and tools are developed to design and study brain-penetrant molecules. https://www.drugdiscoverychemistry.com/Blood-Brain-Barrier-Inhibitors/
carrier-mediated
drug transport: Transfer
of a drug across a membrane by a transporter (often a protein) constituent of
the cytosol membrane. Also known as active transport as opposed to
passive diffusion/absorption. IUPAC
cosolvent:
Vehicle
(often ethanol) used in combination to increase the solubility of drugs.
Frequently, the solubility of a drug in a mixed solvent system is greater than
can be predicted from its solubility in each solvent component separately. IUPAC
crystalline:
Term
that describes a solid of regular shape and the presence of three-dimensional
order on the level of atomic dimensions, for a given molecule. Note 1:
Crystallinity may be detected by diffraction techniques, heat-of-fusion
measurements, etc. Note 2: Crystalline forms are often preferred, over amorphous
forms, in pharmaceutical dosage forms, due to uniformity,
reproducibility, and sometimes lack of hygroscopicity IUPAC
dosage
form:
Formulated
preparation
of molecules/drugs that are rarely if ever suitable for administration to
patients
drug delivery: refers
to approaches, formulations, technologies, and systems for transporting a pharmaceuticalcompound
in the body as needed to safely achieve its desired therapeutic
effect.[1] It
may involve scientific site-targeting within the body, or it might involve
facilitating systemic pharmacokinetics;
in any case, it is typically concerned with both quantity and duration of
drug presence. Drug delivery is often approached via a drug's chemical
formulation, but it may also involve medical devices or drug-device
combination products. Drug delivery is a concept heavily integrated with dosage
form and route
of administration, the latter
sometimes even being considered part of the definition.[2]
Wikipedia accessed 2018 Nov 5
https://en.wikipedia.org/wiki/Drug_delivery
drug
delivery system: Sophisticated
dosage form, which, by its construction, is able to modify/control the
availability of the drug substance to the body by temporal or spatial
considerations. controlled release, extended release, delayed release, delayed
action, dosage form, depot, embedding, gradual release, fast release or immediate
release, i.e., conventional dosage form, implants, liposome, long-acting,
modified release, prolonged action, pulsatile release
drug-eluting
stent: Refers
to a stent with an active drug that is intended to produce a
therapeutic effect (e.g., reduction of restenosis) [13].
IUPAC
drug targeting: A strategy aiming
at the delivery of a compound to a particular tissue of the body. IUPAC
Medicinal Chemistry
micelle(s):
Aggregates
of
colloidal dimensions (i.e., association of colloids) formed reversibly from amphiphile
molecules. [3] Note 1: A
micelle is thus a structural unit of the dispersed phase (surfactant) in
an emulsion, suspension, or a gel; a unit whose repetition
in three dimensions constitutes the micellar structure of the gel; it does not
denote the individual particles in free suspension or solution, or the unit
structure of a crystal. Note 2: Arrangements of groups of
molecules of hydrophobic liquids in aqueous environment, formed by surface-active
agents. [7] See also critical
micelle concentration. IUPAC
microfiltration:
Pressure-driven,
membrane-based separation process in which particles and dissolved
macromolecules
molecular
pharmaceutics:
Molecular Pharmaceutics publishes the results
of original research that contributes significantly to the molecular mechanistic
understanding of drug delivery and drug delivery systems.,,, Scientific areas
within the scope of the journal include physical and pharmaceutical chemistry,
biochemistry and biophysics, molecular and cellular biology, and polymer and
materials science as they relate to drug and drug delivery system efficacy. American Chemical Society,
About Molecular Pharmaceutics http://pubs.acs.org/page/mpohbp/about.html
Broader term: pharmaceutics
nanodelivery:
Nanomaterials
for targeted delivery are uniquely capable of localizing delivery of
therapeutics and diagnostics to diseased tissues. The ability to achieve high,
local concentrations of drugs or image contrast agents at a target site provides
the opportunity for improved system performance and patient outcomes along with
reduced systemic dosing.
Targeted
Nanodelivery of Drugs and Diagnostics,
Margaret
A. Phillips, Martin L. Gran, and Nicholas A. Peppas, Nano Today 2010 April 1
5(2)”143-150
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2882307/
nanoencapsulation:
Formation
of nanoparticles encapsulating a drug. IUPAC
Pharmaceutics
parenteral:
administration of drugs, parenteral route
Method of introducing substances into an
organism, avoiding the gastrointestinal tract [1].
Note 1:
Parenteral routes
may be employed whenever enteral routes are contraindicated or inadequate.
Note 2:
Parenteral administration includes some conventional (intravenous,
intramuscular,
subcutaneous) and
some special (intradermal, intraventricular, etc.) routes.
Note 3: Parenteral
products can be solutions, suspensions, and
emulsions. They are presented as
sterile products. It
is commonly used to imply administration by
injection or infusion.
See also
administration.
IUPAC Pharmaceutics
pharmaceutics:
Science
of preparation of drugs, dosage forms, and drug delivery
systems taking into account the pharmacokinetics and pharmacodynamics
of the drug as well as its physical and chemical properties. IUPAC
pharmacodelivery:
Site-directed pharmacodelivery is a desirable but elusive goal.
Endothelium and epithelium create formidable barriers to endogenous molecules
as well as targeted therapies in vivo. Deidre P. MacIntosh et. al,
Targeting endothelium and its dynamic caveolae for tissue-specific transcytosis in
vivo: A pathway to overcome cell barriers to drug and gene delivery, PNAS 99
(4): 1996-2001, Feb. 19, 2002 http://www.pnas.org/cgi/content/full/99/4/1996
polymorph:
Solid
material that exists at least in two different molecular arrangements, i.e.,
distinctly different crystal species. Note 1: The differences
between polymorphs disappear in solution or in the vapor phase. Note 2:
Solubility, melting point, density, crystal shape, crystal structure, and some
other physical properties often differ from one polymorph to the other. IUPAC
Pharmaceutics
preformulation:
Exploratory
activity that begins early in pharmaceutics, involving studies designed
to determine the compatibility of excipients with the active substance
for a biopharmaceutical; physicochemical and bioanalytical investigation
in support of promising experimental formulations. [21] IUPAC
Pharmaceutics
protein delivery:
It
is a safe bet that if a therapeutic protein is bringing in big money and its
patent is nearing expiration, someone somewhere with a clever technology is
planning a market invasion based on improving how the protein is delivered. targeted
drug delivery: sometimes
called smart drug delivery,[1] is
a method of delivering medication to
a patient in a manner that increases the concentration of
the medication in some parts of the body relative to others. This means of
delivery is largely founded on nanomedicine, which plans to employ nanoparticle-mediated
drug delivery in order to combat the downfalls of conventional drug
delivery. These nanoparticles would be loaded with drugs and targeted to
specific parts of the body where there is solely diseased tissue, thereby
avoiding interaction with healthy tissue. The goal of a targeted drug
delivery system is to prolong,
localize, target and have a protected drug interaction with the diseased
tissue. The conventional drug
delivery system is the absorption of
the drug across a biological
membrane, whereas the targeted
release system releases the drug in a dosage form. The advantages to the
targeted release system is the reduction in the frequency of the dosages
taken by the patient, having a more uniform effect of the drug, reduction
of drug side-effects,
and reduced fluctuation in circulating drug levels. The disadvantage of
the system is high cost, which makes productivity more difficult and the
reduced ability to adjust the dosages. Wikipedia accessed 2018 Nov 5
https://en.wikipedia.org/wiki/Targeted_drug_delivery
therapeutic equivalence: Approved Drug Products with
Therapeutic equivalence evaluations "Orange Book"
https://www.fda.gov/drugs/informationondrugs/ucm129662.htm
Drug delivery
resources
IUPAC
definitions are reprinted with the permission of the International Union of Pure
and Applied Chemistry.
Evolving Terminology for Emerging Technologies
Comments? Questions?
Revisions?
Mary Chitty MSLS
mchitty@healthtech.com
Last revised
January 07, 2020
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Related glossaries include Biologics Drug
Discovery & development
Also known as bioavailability.
Advancing CNS Biotherapeutics and Crossing the
Blood-Brain Barrier
January 14-15, 2019 • San Diego, CA
the hottest topics
and biggest opportunities in discovering and developing highly efficacious
therapeutic agents against CNS disorders and innovative strategies for
delivering therapies across the blood-brain barrier (BBB), new research on topics such as the biologics for CNS
targets and biomarkers, brain cancer,
neurodegeneration, neuroinflammation, neuroimmunology, alteration of CNS/BBB
barriers due to injury or disease, preclinical models, neuroimaging, tools for
prediction of brain penetration, and updates from the industry on topics such as
antibody delivery and vector-mediated transport across BBB.
The Journal of Drug Targeting publishes
papers and reviews on all aspects of drug delivery and targeting for molecular
and macromolecular drugs including the design and characterization of carrier
systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo
applications of these drugs. Papers
are not restricted to drugs delivered by way of a carrier, but also include
studies on molecular and macromolecular drugs that are designed to target
specific cellular or extra-cellular molecules. As such the journal publishes
results on the activity, delivery and targeting of therapeutic peptides/proteins
and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids
(e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes),
as well as aptamers, mononucleotides and monoclonal antibodies and their
conjugates. The diagnostic application of targeting technologies as well as
targeted delivery of diagnostic and imaging agents also fall within the scope of
the journal. In addition, papers are sought on self-regulating systems, systems
responsive to their environment and to external stimuli and those that can
produce programmed, pulsed and otherwise complex delivery patterns.
Aims and Scope, Journal of Drug Targeting, Taylor & Francis
http://www.tandfonline.com/action/journalInformation?show=aimsScope&journalCode=idrt20
microsphere:
Solid
spherical particles of micron-size range, used as matrix dosage forms. IUPAC
polymorphic
transition: Transition
of a solid crystalline phase to another phase having the same chemical
composition but a different crystal structure. Note: The
transition may occur at a characteristic temperature and pressure, called the
inversion point.
[3,20] IUPAC
Pharmaceutics
polymorphism:
Existence
of two or more different crystal structures for the same compound. IUPAC
Search
the Orange Book Database
https://www.accessdata.fda.gov/scripts/cder/ob/index.cfm
IUPAC, Glossary of terms related to pharmaceutics, Pure and
Applied Chemistry 81, 971–999, 2009, http://www.iupac.org/publications/pac/pdf/2009/pdf/8105x0971.pdf
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