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Industrial pharmacy - 2nd semester summary
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Industrial pharmacy - 2nd semester summary Includes bullet points, key diagrams and images
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Semester 2 SummaryAdvanced Drug Delivery Technology
Used when- conventional delivery methods aren’t suitable, drug cant be
conventionally formed or there’s a clear advantage in producing an alternative
Need to: fool the body into up taking the drug, compromise the barrier and
create an environment at the barrier that enough drug is absorbed
Nasal
Large surface area, highly vascularised, no first pass metabolism, rapid onset,
easily assessable and delivery to brain
Nose heats and humidifies air, filters particles, has CYP450 enzymes, possible
protein absorption and rich in lymphoid tissue (IgA)
Mucociliary clearance- mucus removes substances and transports to GIT
(altered by disease state)
Mucoadhesives needed to prolong exposure time
Small non-polar molecules well absorbed
Trans-cellular and para-cellular route
Lipophilic drugs can cross via diffusion, carrier mediated or vesicle transport
Polar can sometimes pass through tight junctions
Absorption enhancement- surfactants or use of chitosan which is a bioadhesive
that opens tight junctions
Nasal vaccination- safer and can be done by non-medical professionals
Nose to brain- transport across olfactory area (nerve) via trans-cellular or para-
cellular but slow
Delivery to the Brain
Separates cerebrospinal fluid and CNS
Tight junctions
Protects brain from ion surges
Largely trans-cellular route
Para-cellular- low MW hydrophilic molecules
Trans-cellular- lipophilic or molecule that can diffuse
Transport proteins- glucose, amino acids or choline
Receptor mediated endocytosis
Cation plasma proteins
Delivery systems
Hydrophobic modifications
Amino acid/peptide carriers (p-glycoprotein efflux)
Large polar using vesicles (cation antibodies)
Lipid coated antibodies or nanoparticles (surfactants induce endocytosis)
Transient opening of tight junctions using NTs
Osmotic opening of tight junctions using hypertonic solutions
Injection in cerebrospinal fluid avoids BBB but rapid turnover back into blood
Direct injection into brain tissue (cytotoxic matrix)
Cellular replacement (viable cell transplants)
Structural Analysis of Solids
, Composition- what is the material and its constituents
Homogeneity- distribution
Mobility- how does it change in the long term
Detection of domains- size and how do they change
Correlation of molecular structure and physical properties
X-Ray Diffraction
Bragg’s law 2d(sinθ)=kλ
Only the reflected beam is detected and this follows Bragg’s
law (other cancel out)
Determination of crystallographic parameters- unit cell
dimensions and symmetry, atomic coordinates and
detecting change in the structure
Determination of physical features- crystal size,
crystallinity, lattice strain and preferred orientation of
crystals
XRD used as fingerprint compared to database but no real
structural information
Can differentiate between polymorphs as different crystal structure
Spectroscopy
Advantages- non-destructive, used with other solid state methods, distinguish
between crystalline and amorphous and automation
Basis of using EM radiation an measuring absorbance/transmission to see how
radiation is altered
IR spectroscopy
Identify crystal forms, quantify components and characterisation of forms but
interactions with other molecules
Advantages- easy to implement, cheaper and suitable for identification and
quantification
Disadvantages- complex spectra, sensitivity to API in low quantities and
ambiguity of spectra
Raman IR spectroscopy
Based on light scattering not absorption so change in polarity not sixe of dipole
Delocalised systems have higher polarisability so detectable (complementary to
IR)
Most APIs contain aromatic rings so good
Water and small molecules produces little scattering so not detected
Can differentiate between crystalline and amorphous
Structural Analysis of Solids NMR
, Transition between energy levels of nuclear spins
H=HZ+HCSA+HD+HQ+HJ
Hz- Zeeman splitting
HCSA- Chemical shift anisotropy need to remove to increase resolution
HD- Dipolar interactions
HQ- Quadrupolar interactions
HJ- Spin-spin coupling
Heteronuclear dipolar coupling
Magic angle spin θ=54.74
Magic angle spin cancels out heteronuclear dipolar and chemical shift anisotropy
Cross-polarisation- using H to enhance 13C peaks improves signal to noise ration
and sensitivity to molecular motion
Can differentiate between crystalline and amorphous
Analysis of Polymorphs
Limitations of XRD
Diffraction relies on long range order which amorphous don’t have
Electron density is the determining factor rather than positions of nuclei
Powder diffraction is less powerful than single crystal work
Disorder causes problems
Molecular mobility may cause complications
Precise location of H can be difficult especially near heavier atoms
Little to no information can be determined for amorphous
Advantages of NMR
Spectra look at local environment not long range order
Detailed information is available from microcrystalline samples
NMR can be paired with XRD to determine crystal structures
Molecular conformations and intermolecular interactions can be assessed form
chemical shifts
Information about H atoms can be determined
Molecular mobility can be obtained by relaxation times
Can analyse crystals and amorphous
Polymorphs can be identified
Solvates can also be recognised
Packaging
Primary pack- direct contact protecting the product
Secondary pack- surrounds primary pack which enables storage and transport
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