Expanding the Crystal Structure Landscape of Pravastatin Complexes: Tuning Solubility, Diffusion, and Pharmacokinetics
Richu Bagya Varsa S,
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Lasya Priya Katukam,
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Goutam Kumar Kole
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et al.
Crystal Growth & Design,
Journal Year:
2024,
Volume and Issue:
24(12), P. 5309 - 5323
Published: June 1, 2024
Pravastatin
(PRV),
a
lipid-lowering
medication,
is
prescribed
to
treat
cardiovascular
disease
and
dyslipidemia.
Due
its
low
permeability
high
solubility,
the
biopharmaceutics
classification
system
(BCS)
class
III
drug
exhibits
poor
bioavailability.
To
overcome
bottlenecks
of
PRV,
novel
complexes
with
Zn
Cu
along
zwitterionic
cocrystal
l-proline
(PRO)
were
synthesized.
These
new
solid
forms
characterized
by
SC-XRD,
PXRD,
DSC,
TGA,
FT-IR,
DVS,
SEM
images.
Rietveld
refinement
was
used
obtain
3D
coordinates
PRV–Na–PRO
ionic
hydrate
from
high-resolution
PXRD
data.
PRV–Cu
obtained
substituting
PRV
sodium
salt
Cu/Zn
metal.
In
hydrate,
each
Na
metal
coordinated
carboxylates
(2)
PRO
(1)
three
water
molecules
result
in
an
octahedron
geometry.
two
carboxylate
anions
molecules,
forming
square
pyramidal
The
PRV–Zn
complex
maintains
octahedral
geometry
using
four
coordination
molecules.
exhibited
higher
solubility
(1.7-fold)
diffusion
profile
(1.1-fold)
compared
commercial
PRV–Na
whereas
PRV–Cu/Zn
showed
controlled
release.
Surprisingly,
enhanced
peak
plasma
concentration
Cmax
(50
fold)
AUC
(14.4
during
pharmacokinetics
study
rats.
stability
supported
ground-state
optimization
energy
calculations.
Unlike
moisture-sensitive
PRV–Zn/Cu
far
superior
moisture
may
offer
extended
On
other
hand,
significantly
improved
bioavailability
can
be
commercialized
following
proper
formulation
that
offers
stability.
Language: Английский
Crystals, Crystallization and X-ray Techniques: Pharmaceutical Application
Research Journal of Pharmacy and Technology,
Journal Year:
2025,
Volume and Issue:
unknown, P. 1906 - 1912
Published: April 12, 2025
Within
pharmaceutical
manufacturing,
crystallization
is
one
of
the
most
extensively
used
and
vital
unit
operation.
Mass
transfer
a
solute
from
liquid
solution
to
pure
solid
known
as
crystallization,
it
chemical
process
solid-liquid
separation.
It
result
particles
rapidly
arranging
themselves
into
regular
geometric
patterns
or
repetitive
order.
Because
combines
particle
generating
purification
single
process,
beneficial
isolation
step
for
manufacturing.
Nearly
all
products
developed
involving
fine
chemicals,
such
colors,
explosives,
photographic
materials,
need
crystallize
during
manufacturing
operations,
over
90%
contains
bioactive
medicinal
product
items
excipients
in
crystalline
form.
Without
acquiring
supersaturation
not
achieve.
There
are
many
types
equipment,
which
often
on
basis
methods
achieving
suspending
growing
crystals.
Probably
important
characteristics
governing
size,
shape,
hardness
impurities.
crystals
because
techniques
involve
drugs
with
improved
physiochemical
properties.
A
crucial
variety
uses
crystallization.
Purification,
enhanced
processing
traits,
physical
stability,
ease
handling,
prolonged
release,
separation
entrapped
constituents
primary
drivers
Language: Английский
Three Indomethacin cocrystals: preparation, characterization and formation thermodynamics
Ying Zhang,
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Jingjing Liu,
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Ling Yin
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et al.
Process Safety and Environmental Protection,
Journal Year:
2025,
Volume and Issue:
unknown
Published: May 1, 2025
Language: Английский
The Peculiar H-Bonding Network of 4-Methylcatechol: A Coupled Diffraction and In Silico Study
Mattia Lopresti,
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Luca Palin,
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Giovanni Calegari
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et al.
Molecules,
Journal Year:
2024,
Volume and Issue:
29(10), P. 2173 - 2173
Published: May 7, 2024
The
crystal
structure
of
4-methylcatechol
(4MEC)
has,
to
date,
never
been
solved,
despite
its
very
simple
chemical
formula
C7O2H8
and
the
many
possible
applications
envisaged
for
this
molecule.
In
work,
gap
is
filled
4MEC
obtained
by
combining
X-ray
powder
diffraction
first
principle
calculations
carefully
locate
hydrogen
atoms.
Two
molecules
are
present
in
asymmetric
unit.
Hirshfeld
analysis
confirmed
reliability
solved
structure,
since
two
show
rather
different
environments
H-bond
interactions
directionality
strength.
packing
characterised
a
peculiar
bond
network
with
hydroxyl
nests
formed
adjacent
octagonal
frameworks.
It
noteworthy
that
observed
short
contacts
suggest
strong
inter-molecular
interactions,
further
inter-crystalline
aggregation
microscopic
images,
indicating
growth,
crystallization
attempts,
single
aggregates
taller
than
half
centimetre
and,
often,
spherical
shapes.
These
peculiarities
induced
presence
methyl
group
4MEC,
parent
compound
catechol,
similarity,
shows
standard
layered
alternating
hydrophobic
polar
layers.
Finally,
complexity
peculiarity
growth
features
explain
why
could
not
be
structural
analysis.
Language: Английский
Pharmaceutical cocrystals: Unlocking the potential of challenging drug candidates
Journal of Drug Delivery Science and Technology,
Journal Year:
2024,
Volume and Issue:
unknown, P. 106572 - 106572
Published: Dec. 1, 2024
Language: Английский
PREPARATION, CHARACTERISATION, EVALUATION AND DFT ANALYSIS OF CILNIDIPINE-L-PHENYLALANINE COCRYSTAL
International Journal of Applied Pharmaceutics,
Journal Year:
2023,
Volume and Issue:
unknown, P. 365 - 372
Published: Nov. 7, 2023
Objective:
The
objective
of
this
study
was
to
prepare,
characterise
and
evaluate
pharmaceutical
cocrystals
Cilnidipine
using
L-phenylalanine
as
the
coformer
enhance
aqueous
solubility
Cilnidipine.
It
also
proposed
mechanism
cocrystal
formation
based
on
Density
Functional
Theory
(DFT)
Gaussian
software.
Methods:
To
overcome
limitation
poor
Cilnidipine,
a
1:1
prepared
by
liquid
assisted
grinding
(LAG)
technique.
resultant
were
characterised
Fourier
transform-infrared
spectroscopy
(FTIR),
powder
X-ray
diffraction
(PXRD),
differential
scanning
calorimetry
(DSC)
field
emission
electron
microscopy
(FE-SEM).
They
evaluated
for
their
saturation
in
water.
studied
at
DFT
level
theory.
Results:
band
broadening
the–NH
and–NO
peaks
FTIR
spectra
indicated
hydrogen
bonds
cocrystals.
A
single
sharp
melting
endotherm
218.40
°C
DSC
curve
confirmed
appearance
new
PXRD
pattern
showed
crystalline
phase.
FE-SEM
analysis
above
findings.
exhibited
3.31
folds
enhancement
solubility.
intrmolecular
bonding
between
the–NO
and–NH
L-phenylalanine.
Conclusion:
present
demonstrated
successful
approach
enhancing
poorly
water-soluble
drug
cocrystallisation
technique
coformer.
Language: Английский
Structural analysis of anti-retroviral drug raltegravir and its potential impurity C: investigation of solubility and stability
T. K. S. Fayaz,
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Hemanth Kumar Chanduluru,
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Puja Lal
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et al.
CrystEngComm,
Journal Year:
2023,
Volume and Issue:
26(4), P. 517 - 531
Published: Dec. 13, 2023
An
anhydrous
form
of
raltegravir
and
two
crystalline
phases
its
impurity
C
were
obtained
during
solid
screening
their
crystal
structures
are
reported
with
variable
conformations.
Language: Английский
Noncovalent Derivatization
Elsevier eBooks,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Jan. 1, 2024
SYNERGISTIC BIOGENIC SYNTHESIS OF ZINC NANOPARTICLES BY PROBIOTICS SACCHAROMYCES CEREVISIAE AND LACTOBACILLUS FERMENTUM FOR FARM ANIMAL HEALTH AND NUTRITION
Sudhair Abbas Bangash,
No information about this author
Sadia Sardar,
No information about this author
Qudsia Begum
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et al.
Journal of Population Therapeutics and Clinical Pharmacology,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Jan. 1, 2024
Probiotics,
such
as
Lactobacillus
fermentum
and
Saccharomyces
cerevisiae,
play
a
crucial
role
in
catalyzing
the
biogenesis
of
nano-minerals,
offering
transformative
solution
to
enhance
nutrient
absorption
farm
animals
promote
agricultural
sustainability.
This
research
aims
synthesize
ZnO
nanoparticles
using
Probiotic
assessing
their
antibacterial
efficacy
against
MDR
pathogens
investigating
impact
Nano
zinc
supplementation
on
growth
blood
parameters
goats.
Utilizing
analytical
methods
Fourier
transform
infrared
spectroscopy
(FT-IR),
scanning
electron
microscopy
(SEM),
X-ray
diffraction
analysis
(XRD),
ultraviolet–visible
(UV–Vis),
produced
NPs
were
characterized,
revealing
distinct
bonds
structural
features.
nanoparticles,
highlighted
through
FTIR
(emphasizing
N-H
stretching
at
1450-1500
cm-1
nanoparticle
stretches
400-800
cm-1),
SEM
(revealing
micro-sized
bioconjugates
with
dimensions
100–120
nm),
XRD
(confirming
hexagonal
crystal
structure
approximately
36.50
degrees),
demonstrated
significant
activity.
Goats
treated
exhibited
substantial
weight
gain
over
12
weeks
(Initial
BW:
29.2±0.48
kg;
Final
Body
Weight
-
Treatment
C:
40.99±0.58
kg,
ZnO-1:
43.39±0.45
ZnO-2:
44.05±0.43
kg),
limited
physiological
effects,
except
for
notable
variations
immunoglobulins
(IgA,
IgG)
among
treatment
groups
(p
=
0.006
p
0.003,
respectively).
Notably,
displayed
activity
(ZnO-1
E.
cloacae:
13mm,
A.
baumannii:
12mm;
ZnO-2
S.
aureus:
12mm,
P.
aeruginosa:
12mm),
indicating
remarkable
antimicrobial
potency.
environmentally
friendly
cost-effective
approach
synthesizing
holds
promise
diverse
biomedical
applications.
Language: Английский