Review of Solubilization Techniques for a Poorly Water-Soluble Drug: Carbamazepine

Mittapalli Pavan Kumar; G. Y. Srawan Kumar; Shashank Apte; Yamasani Madhusudan Rao

Abstract

Solubility behavior of drugs remains one of the most challenging aspects in formulation development. With the introduction of various solubility improvement techniques it should be possible to overcome solubility-linked issues. Several years of research and various novel techniques for improvement of drug solubility have resulted in only a few marketed products. There are various techniques that were studied in depth to improve carbamazepine (CBZ) solubility. Several in vitro and in vivo studies have shown significant improvement in dissolution and bioavailability of CBZ. This article begins with an overview of the historical background and definitions of the various techniques, including the novel ones. The second part of the article is devoted to the techniques, materials used, procedures, and characterization of various developed formulations. The current review is further extended specifically to drug dissolution in relation to drug crystalline in various solubilization approaches.

Footnotes

Abbreviations
AUC
Area under curve
βCD
Beta cyclodextrin
BCS
Biopharmaceutical classification system
CBZ
Carbamazepine
C_max
Maximum plasma concentration
CO₂
Carbondioxide
CR
Controlled release
DMPC
L-α-dimyristoylphosphatidylcholine
DMPG
L-α-dimyristoylphosphatidylglycerol
DSC
Differential scanning calorimetry
DSPC
L-α-distearoylphosphatidylcholine
DTA
Differential thermal analysis
EPC
egg phosphatidylcholine
FT-IR
Fourier transform infrared
HPβCD
Hydroxypropyl beta cyclodextrin
HPMC
Hydroxypropyl methylcellulose
HSM
Hot state microscopy
IDR
Intrinsic dissolution rate
LD
Laser diffraction
PCS
Photon correlation spectroscopy
PEG
Polyethylene glycol
PM
Physical mixture
PVP-CL
Cross linked polyvinyl pyrrolidone/crospovidone
PVP
Polyvinyl pyrrolidone
SCF
Super critical fluid
SD
Solid dispersions
SDS
Sodium dodecyl sulphate
SEM
Scanning electron microscopy
SGF
Simulated gastric fluid
SIF
Simulated intestinal fluid
STG
Sodium starch glycollate
TGA
Thermal gravimetry analysis
T_max
Time to reach maximum concentration
Vitamin E TGPS
D-alpha-tocopheryl polyethyleneglycol 1000 succinate
XRD
X-ray diffraction

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