CO-CRYSTALS OF CARVEDILOL: PREPARATION, CHARACTERIZATION AND EVALUATION

CO-CRYSTALS OF CARVEDILOL

  • RAJU THENGE School of Pharmacy, Dr. A. P. J. Abdul Kalam University, Indore (M. P), India
  • RAKESH PATEL School of Pharmacy, Dr. A. P. J. Abdul Kalam University, Indore (M. P), India
  • NANDU KAYANDE Thakur Shiv Kumar Singh Memorial Pharmacy College, Burhanpur, (M. P), India.
  • NILESH MAHAJAN Dadasaheb Balpande College of Pharmacy, Besa-Nagpur, Maharashtra, India

Abstract

Carvedilol an antihypertensive drug, exhibit poor solubility and dissolution rate. Hence an attempt has been made to prepare the Co-crystals of Carvedilol to increase the solubility and dissolution rate by solvent evaporation method using coformer such as succinic acid, fumaric acid and oxalic acid. The prepared Co-crystals were evaluated for  solubility, dissolution rate and micromeritic properties. The Co-crystals were characterized by scanning electronic Microscopy (SEM), FT-Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffractometry (XRD). The CAR-SA Co-crystal, CAR-FA Co-crystals and CAR-OA Co-crystals showed increased in solubility and dissolution rate compared to pure Carvedilol. The Co-crystals formed with coformer have showed improved micromeritic properties. SEM clearly showed the formation of new solid phase with the coformer. The FT-IR spectra indicate the shifting of characteristic peak in the Co-crystals but does not showed any interaction between the coformer used. DSC data showed the change in the endotherm with the melting points of Co-crystals. XRD spectra indicate the notified difference in the 2θ and the intensity of the peaks. Hence the Co-crystal formation could be helpful to improve the solubility, dissolution and micromeritic properties of Carvedilol.

Keywords: Carvedilol, Co-crystals, Solubility, FT-IR, Dissolution rate, Micromeritic properties.

Author Biographies

NANDU KAYANDE, Thakur Shiv Kumar Singh Memorial Pharmacy College, Burhanpur, (M. P), India.

Principal

NILESH MAHAJAN, Dadasaheb Balpande College of Pharmacy, Besa-Nagpur, Maharashtra, India

Professor

References

1. Aakeroy CB, Forbes S, Desper J. Using co-crystals to systematically modulate aqueous solubility and melting behavior of an anticancer drug. J Am Chem Soc 2009;131:17048–9.
2. Ramanathan T. Ed. Mass spectrometry in drug metabolism and pharmacokinetics. John Wiley and Sons, Inc., Hoboken, NJ; 2009. p. 1–4.
3. Rasenack N, Hartenhauer H, Muller BW. Microcrystals for dissolution rate enhancement of poorly water-soluble drugs. Int J Pharm 2003;254:137–45.
4. Hong JY, Kim JK, Song YK, Park JS, Kim CK. A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption. J Controlled Release 2006;10:332–8.
5. Chowdary KPR, Pavan Kumar A. Recent research on formulation development of BCS class II drugs, a review. Int Res J Pharm Appl Sci 2013;3:173-81.
6. RR Thenge, VB Patond, NM Mahajan, VS Adhao, PV Ajmire, LN Barde, et al. ‘Preparation and characterization of co-crystals of diacerein. Indo J Pharm 2017;28:34-41.
7. S Mirza, I Miroshnyk, J Heinamaki, J Yliruusi. Co-crystals: an emerging approach for enhancing the properties of pharmaceutical solids. Dosis 2008;24:90–6.
8. Sevukarajan M, Tanuja B. Synthesis and characterization of pharmaceutical cocrystals. (Aceclofenac-Nicotinamide) J Pharm Sci Res 2011;3:1288-93.
9. V Yadav, AS Shete, AP Dabke, PV Kulkarni, SS Sakhare. Co-crystals: a novel approach to modify physicochemical properties of active ingredients. Ind J Pharma Sci 2009;71:359–70.
10. Rajurkar VG, Nagare AS, Ghawate V. Tablet formulation and enhancement of aqueous solubility of efavirenz by solvent evaporation co-crystal techniques. Med Chem 2015;S2:002.3
11. Instrumental methods of analysis. 7th edition. by Willard, Merritt, Dean and Settle; 1989. p. 796.
12. Palermo PJ. Handbook of modern pharmaceutical analysis. Ahuja S, Scypinski S. eds. Academic Press: San Deigo, USA; 2001. p. 243-4.
13. Yuvraja K, Khanam J. Enanhancement of carvedilol solubility by solid dispersion techniques using cyclodextrin, a water-soluble polymer and hydroxyl acid. J Pharm Biomed Anal 2014;96:510-20.
14. Thenge RR. Crystal modification of aceclofenac by spherical crystallization to improve solubility dissolution rate and micromeritic properties. J Pharma Res 2012;5:974-7.
15. Planinsek O, Kovacic B, Vrecer F. Carvedilol dissolution improvement by preparation of solid dispersions with porous silica. Int J Pharm 2011;406:41-8.
16. Hiendrawan S, Hartanti AW, Veriansyah B, Widjojokusumo E, Tjandrawinata RR. Solubility enhancement of ketoconazole via salt and cocrystal formation. Int J Pharm Pharm Sci 2015;7:160-4.
17. Chadha R, Saini A, Arora P, Chanda S, Dharamvir Singh Jain. Cocrystal of efavirenz with selected conformers: preparation and characterization. Int J Pharm Pharm Sci 2012;4:244-50.
18. Hiendrawan S, Veriansyah B, Widjojokusumo E, Soewandhi SN, Wikarsa S, Tjandrawinata RR. Simultaneous cocrystallization and micronization of paracetamol-dipicolinic acid cocrystal by supercritical antisolvent (SAS). Int J Pharm Pharm Sci 2016;8:89-98.
19. F Rahman, AN Winantari, Siswandono, D Setyawan. Comparison study of grinding and slurry method on the physicochemical characteristic of acyclovir–succinic acid cocrystal. Asian J Pharm Clin Res 2017;10:153-8.
20. M Raghuram, MS Alam, M Prasad, CH Khanduri. Pharmaceutical cocrystal of prulifloxacin with nicotinamide. Int J Pharm Pharm Sci 2014;6:180-4.
Statistics
118 Views | 16 Downloads
Citatons
How to Cite
THENGE, R., PATEL, R., KAYANDE, N., & MAHAJAN, N. (2019). CO-CRYSTALS OF CARVEDILOL: PREPARATION, CHARACTERIZATION AND EVALUATION. International Journal of Applied Pharmaceutics, 12(1), 42-49. https://doi.org/10.22159/ijap.2020v12i1.35640
Section
Original Article(s)