Stable Co-crystals of Glipizide with Enhanced Dissolution Profiles: Preparation and Characterization.
Present study deciphers preparation of co-crystals of lipophilic glipizide by using four different acids, oxalic, malonic, stearic, and benzoic acids, in order to achieve enhanced solubility and dissolution along with stability. All co-crystals were prepared by dissolving drug and individual acids in the ratio of 1:0.5 in acetonitrile at 60-70°C for 15 min, followed by cooling at room temperature for 24 h. FT-IR spectroscopy revealed no molecular interaction between acids and drug as the internal structure and their geometric configurations remain unchanged. Differential scanning calorimetry revealed closer melting points of raw glipizide and its co-crystals, which speculates absence of difference in crystallinity as well as intermolecular bonding of the co-crystals and drug. PXRD further revealed that all the co-crystals were having similar crystallinity as that of raw glipizide except glipizide-malonic acid co-crystals. This minor difference in the relative intensities of some of the diffraction peaks could be attributed to the crystal habit or crystal size modification. SEM revealed difference in the crystal morphology for all the co-crystals. Micromeritic, solubility, dissolution, and stability data revealed that among all the prepared co-crystals, glipizide-stearic acid co-crystals were found superior. Hence, it was concluded that glipizide-stearic acid co-crystals could offer an improved drug design strategy to overcome dissolution and bioavailability related challenges associated with lipophilic glipizide.
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Narendra Kumar
NK
Pandey
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Hans Raj
HR
Sehal
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Varun
V
Garg
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Tejasvi
T
Gaur
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Bimlesh
B
Kumar
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India. singhsachin23@gmail.com.
Sachin Kumar
SK
Singh
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Monica
M
Gulati
Department of Pharmaceutics, J.S.S. College of Pharmacy, Rocklands, Ooty, Tamilnadu, 643001, India.
K
K
Gowthamarajan
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Palak
P
Bawa
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Sarvi Yadav
SY
Rajesh
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Parth
P
Sharma
School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, 144 401, India.
Rakesh
R
Narang
D002152:Calorimetry, Differential Scanning; D003460:Crystallization; D005913:Glipizide / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods; D013229:Stearic Acids / Q000737:chemistry
D013229:Stearic Acids; C031183:stearic acid; D005913:Glipizide
co-crystals; dissolution; glipizide; solubility; stability