DISSOLUTION ENHANCEMENT OF LANSOPRAZOLE USING COCRYSTALLIZATION
Objective: Lansoprazole (LPZ) is a Biopharmaceutics Classification System Class II drug. It has low solubility and high permeability, so its rate of
dissolution is a rate-limiting step for drug absorption. This study aimed to improve the dissolution rate of LPZ by forming cocrystals, using nicotinamide
(NCT) as the conformer.
Methods: Cocrystals of LPZ were produced using the solvent evaporation and solvent-drop grinding methods with a molar ratio of 1:1 and 1:2.
The cocrystals were characterized using Fourier-transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), and differential scanning
calorimetry (DSC). The solubility and dissolution of the LPZ cocrystals were examined in distilled water.
Results: FTIR was used to confirm the formation of hydrogen bonds between LPZ and NCT. DSC and XRD studies showed the formation of crystals
from cocrystals and a decrease of the melting point of the cocrystals. The dissolution study revealed that the cocrystals could increase the LPZ
dissolution rate by up to 8.4-fold compared with pure LPZ.
Conclusion: LPZ cocrystal formation with NCT was successful in increasing the dissolution rate of LPZ.
biopharmaceutics classification system. New scientific approaches to
international regulatory standards. Eur J Pharm Biopharm 2000;50:3-12.
2. Chaudhary A, Nagaich U, Gulati N, Sharma VK, Khosa RL.
Enhancement of solubilization and bioavailability of poorly soluble
drugs by physical and chemical modifications: A recent review. J Adv
Pharm Educ Res 2012;2:32-67.
3. Ensom MH, Decarie D, Sheppard I. Stabillity of lansoprazole in
extemporaneously compounded suspensions for nasogastric or oral
administration. Can J Hosp Pharm 2007;60:184-91.
4. Mendiratta C, Kadam V, Pokharkar V. Lansoprazole solid dispersion
using a novel amphiphilic polymer soluplus. J Chem Pharm Res
5. Lu Y, Guo T, Qi J, Zhang J, Wu W. Enhanced dissolution and stability
of lansoprazole by cyclodextrin inclusion complexation: Preparation,
characterization, and molecular modeling. AAPS Pharm Sci Tech
6. Shargel L, Yu AC. Applied Biopharmaceutics and Pharmaceutics.
3rd ed. Connecticut: Appleton and Lange; 2005.
7. Qiao N, Li M, Schlindwein W, Malek N, Davies A, Trappitt G.
Pharmaceutical cocrystals: An overview. Int J Pharm 2011;419:1-1.
8. Sekhon BS. Pharmaceutical co-crystals a review. ARS Pharm
9. Fábián L, Hamill N, Eccles KS, Moynihan HA, Maguire AR,
McCausland L, et al. Cocrystals of fenamic acids with nicotinamide.
Cryst Growth Des 2006;11:3522-8.
10. Sevukarajan M, Thanuja B, Sodanapalli R, Nair R. Synthesis and
characterization of a pharmaceutical co-crystal: (Aceclofenac:
Nicotinamide). J Pharm Sci Res 2011;3:1288-93.
11. Weyna DR, Shattock T, Vishweshwar P, Zaworotko MJ. Synthesis and
structural characterization of cocrystal and pharmaceutical cocrystal:
Mechanochemistry vs slow evaporation from solution. Crystal Growth
12. Okram ZD, Kanakapura B, Jagannathamurthy RP, Basavaiah VK.
Development of a simple uv-spechtrophotometric method for the
determination of lansoprazole and study of its degradation profile.
Quim Nova 2012;35:386-91.
13. Yamamoto K, Tsutsumi S, Ikeda Y. Establishment of cocrystal cocktail
grinding method for rational screening of pharmaceutical cocrystals. Int
J Pharm 2012;437:162-71.
14. Shan N, Zaworotko MJ. The role of cocrystals in pharmaceutical
science. Drug Discov Today 2008;13:440-6.
15. Yu M, Sun L, Li W, Lan Z, Li B, Tan L, et al. Investigation of structure
and dissolution properties of a solid dispersion of lansoprazole in
polyvinylpyrrolidone. J Mol Struct 2011;1005:70-7.
This work is licensed under a Creative Commons Attribution 4.0 International License.