The document discusses the preformulation of celecoxib. It provides details on the chemical and physical properties of celecoxib, including its chemical formula, molecular weight, solubility, and stability aspects when formulated in capsule and suspension dosage forms. Stability studies showed the capsule and suspension formulations were stable for up to 12 months and 93 days, respectively, when stored under specified conditions. The conclusion discusses developing a celecoxib nanocrystalline solid dispersion using wet media milling to enhance oral bioavailability.
2. Physicochemical parameters
Chemical properties
• Chemical Formula : C17H14F3N3O2S
• IUPAC Name :
4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H
-pyrazol-1-yl]benzene-1-sulfonamide
• Molecular Weight : 381.4
• Monoisotopic Mass : 381.07588236
• Hydrogen Bond Donor Count : 1
• Hydrogen Bond Acceptor Count : 7
• Rotatable Bond Count : 3
• Complexity : 577
Physical properties
• Color / form : pale yellow solid
• Melting Point : 529.0±60.0
• Boiling Point : 157-159
• Solubility : Poorly soluble “In water, 4.3
mg/L at 25 °C”
• Vapor Pressure : 1.19X10-9 mm Hg
at 25°C
• pKa : 11.1
• LogP : 3.53
3. Stability aspects
• For capsule dosage form
Stability data on the product are provided for 4 pilot-scale batches of each capsule
strength stored at 25°C/60% RH (12 months) and 40°C/75% RH (6 months). Ther
e are No clear changes or trends were observed. All parameters remain within the
specified limits at accelerated and long-term storage conditions.
• So the proposed shelf-life of 2 years is acceptable
• Photostability studies showed that the capsules are not sensitive to light.
• For Suspension dosage form packaged in amber PVC bottles were stable for up to
93 days when stored at 5°C or 23°C.
• also shelf-life could be enhanced by Nano emulsion formulation to become 2.38
years.
4. Ahmed Ibrahim 18006
Conclusion
CLX-NC was successfully prepared using the chosen PV
P VA64 and SDS as the combined stabilizers, and furthe
r optimized,using a central composite ,was found to have
an adequate particle distribution and no substantial cryst
alline change occur. Quality evaluation indicated that CL
X-NC could provide excellent physical stability during six
months’ storage
Journal Name
pharmaceutics
Year of publication
11 July 2019
Delivery system
Solid Dispersions compressed tablet
Excipients
Celecoxib (CLX), used as micronized crystallin
e power, was purchased from Yijing Industrial
Co. Ltd. Hydroxypropylmethylcellulose acetate
succinate and hydroxypropylcellulose. Polyviny
lpyrrolidone—polyvinyl acetate copolymers and
polyvinylpyrrolidone were generouslyprovided b
y BASF. Sodiumdodecyl sulfate (SDS), used a
ssecondary stabilizer. Milli-Q water.
Aim to
Enhanced Oral Bioavailabili
ty of Celecoxib Nanocrystal
line Solid Dispersion based
on Wet Media Milling Tech
nique: Formulation,Optimi
zation and In Vitro/In Vivo
Evaluation
to develop and optimize CLX nanocrystalline(C
LX-NC) solid dispersion prepared by the wet m
edium millingtechnique combined with lyophiliz
ation to enhance oral bioavailability
5. Ahmed Hamdy Ali 18015
Conclusion
development of a solid dispersion system to improve
patient compliance and safety with respect to poorly
water-soluble celecoxib (CXB)
Journal Name
pharmaceutics
Year of publication
2019
Delivery system
solid dispersion system
Excipients
CXB and SPAN 80 .Cremophor RH40, Poloxamer 188,
Poloxamer 407, and Soluplus . Labrafac PG, Labrafil M
1944 CS, Labrasol, Plurol Oleique CC497, and Transcut
ol HP were obtained from Gattefosse . Ryoto sugar ester
L-1695 and P-1670 were kindly provided by Mitsubishi-K
asei Chemical Co. Heweten 101 (microcrystalline cellulo
se) and Pharmatose 200M (Lactose)
Aim to
Development and Evaluati
on of Poorly Water-Soluble
Celecoxib as Solid Dispersi
ons Containing Nonionic S
urfactants Using Fluidized-
Bed Granulation
to develop a solid dispersion system with improved
dissolution, absorption, and patient compliance of poorly
water-soluble celecoxib (CXB)
6. Ibrahim saad 18003
Conclusion
new development of solid formulation for celecoxib is still
desirable. Dry elixir (DE) formulation is an efficient
dosage form for oral delivery to circumvent problems
such as low solubility, dissolution and bioavailability of
BCS class drug II.9–11 The loaded materials in the DE
system are very quickly dissolved in GI media due to the
cosolvent effect of ethanol and water, resulting in both an
enhaned dissolution and oral bioavailability
Journal Name
journal of Nanoscience and Nanotechnology
Year of publication
2019
Delivery system
dry elixir system
Excipients
Celecoxib- ethanol – Water – dextrin – sodium –
lauryl sulfate
Aim to
Improved
Dissolution
and Oral
Bioavailability
of Celecoxib
by a Dry Elixir
System
Enhancing the dissolution rate and oral bioavailability of
celecoxib. DE system has been used for improving
solubility, oral bioavailability of poorly water-soluble
drugs.
7. Ahmed ismail
Conclusion
developing a direct compression tablet formulation of CEL
using the DMSO solvate of CEL, which exhibits better flow
ability and tabletability than the commercial Form III CEL.
CEL also releases more quickly from the tablet than CEL c
apsules. The formulation develops a predictive techniques
for assessing powder flowability and tableting performance.
This study exemplifies the benefits of combining crystal en
gineering and materials science to enable the efficient dev
elopment of high quality tablet products.
Journal Name
International Journal of pharmaceutics
Year of publication
2021
Delivery system
Direct compress ion tablet
Excipients
- Celecoxib - DMSO - FMC Biopoly
mer –Philadelphia - Mannitol - SLS
- Mg St
Aim to
Direct compression tablet
formulation of celecoxib
enabled with a
pharmaceutical solvate
Improve flow and denisty of DC tablet
celecoxib by adding (DMSO) solvate
8. Abadeer shenouda 18001
Conclusion
The results show that Liquisolid technology Combined
with ball milling is an efficient tool for enhancing the
dissolution of poorly water soluble drugs
Journal Name
Journal of pharmaceutical innovation.
Year of publication
2022
Delivery system
Classic Liquisolid
Excipients
* PVP * Micro crystaline cellulose * Silica
Aim to
Combining liquid and cogri
nding technique to enhanc
e the dissoluti on rate of ce
lecoxib
Enhance the dissoluti on rate of poorly water soluble drugs .
9. Abrar osama
Conclusion
Bead milling method can be used as for the preparation of
the nanoparticles in nano-scale from the drug powders of
several microns in size. Milled celecoxib nanosuspension
has enhanced dissolution profiles of over 80 times compar
ing to micron sized celecoxib powder, leading to improve
bioavailability. So, the celecoxib nanosuspension is a goo
d option as an alternative dosage form of celecoxib. This f
ormulation may improve in vitro dissolution and oral absor
ption of lipophilic drugs with similar properties to celecoxib.
Journal Name
Journal of Nanoscience and Nanotechnolo gy
Year of publication
2019
Delivery system
Nanosus pension
Excipients
Celecoxib Tween80 -HPMC -Dow Chemical
Aim to
Preparation and Characteri
zation of Celecoxib Nanosu
spension Using Bead Millin
g
The aim of this study is to develop nanosuspe nsion fo
r improved dissolution of poorly watersoluble celecoxib
10. Ahmed elgamal 18014
Conclusion
The present study demonstrated that at equivalent lipid do
ses, increasing the drug saturation above equilibrium solu
bility resulted in an increased in vivo bioavailability of celec
oxib from single component LBDDS relative to the corresp
onding nonsupersaturated LBDDS. Using the in vitro Perm
eapadR model, while supersaturation in LBDDS did not re
veal higher flux across the biomimetic membrane
Journal Name
European Journal of Pharmaceutical Sciences
Year of publication
2020
Delivery system
Lipidbased drug delivery systems
Excipients
buprofen Capmul MCM C8 Maisine CC Labrasol ALF
Porcine pancreatic lipase 4x USP, calcium chloride dih
ydrate CaCl2⋅2H20, 4- bromophenylboronic acid (4- B
BBA) and maleic acid
Aim to
Exploring impact of supersa
turated lipidbased drug deli
very systems of celecoxib
on in vitro permeatio n acr
oss Permeapa dR membran
e and in vivo absorption
to explore supersaturat ed versus nonsupersaturat ed li
pidbased systems at equivalent lipid doses, on in vivo bi
oavailabilit y in rats and on in vitro permeation across a
biomimetic Permeapad R membrane to establish a pote
ntial in vivo - in vitro correlation.
11. Asmaa alaa
Conclusion
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Journal Name
European jurnal of Pharmaceutics and Biopharmaceutica
Year of publication
2022
Delivery system
tablet
Excipients
Celecoxib PVP -HPMC -VA Microcrystalline Cellulose
Mannitol Crospovidone Mg st NaH2 Po4,
Aim to
Development of a multipart
iculate drug delivery syste
m for in situ amorphisation
The aim of this study is to develop drug delivey system
of poor watersoluble colocxibe by multiparticulate drug
delivey in situ amorphisation
12. Ahmed sahry 18017
Conclusion
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Journal Name
pharmaceutics
Year of publication
2022
Delivery system
solid dispersion
Excipients
Lactosemon ohydrate (75%) & microcrystal linecellulo
se (25%) - crosslinkedP VP - Mgstearate - crosslinked
NaCMC - SLS
Aim to
Synthesis of Celecoxib
Eutectic Mixture Particles vi
a Supercritica l CO2 Process
and Celecoxib Immediate R
elease Tablet Formulatio n
by Quality by Design Appro
ach
Developed a therapeutic eutectic system for CEL whic
h is a promising approach for oral delivery to enhance
bioavailability
13. Amir nageh 18007
Conclusion
In a ternary ASDs consisting of CEL, CoPVP, and TP
GS, the presence of CEL improved the miscibility bet
ween TPGS and CoPVP. TPGS improved the propert
ies of CEL ASDs during dissolution by enhancing the
powder wetting and by facilitating the formulation of C
EL nanoparticles. CEL ASDs containing 20% TPGS d
emonstrated the fastest dissolution and the highest d
egree of supersaturation in both non-sink
Journal Name
Journal of Drug Delivery Science and Technology.
Year of publication
2019
Delivery system
Amorphous solid dispersions.
Excipients
Copovidone. polyethylene glycol 1000 succinate..To
copherol
Aim to
Effect of surfactant level on
properties of celecoxib am
orphous solid Dispersions.
to explore the influence of Dα-tocopheryl polyethylen
e glycol 1000 succinate (vitamin E TPGS) on the pro
perties of celecoxib (CEL) amorphous solid dispersio
ns (ASDs).
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