ENHANCEMENT SOLUBILITY AND DISSOLUTION RATE OF PARACETAMOL AND IBUPROFEN BY COAMORPHOUS PARTICLES USING MICROWAVE TECHNIQUE
ENHANCEMENT SOLUBILITY AND DISSOLUTION RATE
Objective: The objective of the present study was to the preparation of a coamorphous (COAM) system of paracetamol (PA) (Biopharmaceutics Classification System [BCS] Class-III) and ibuprofen (IB) (BCS Class-II) for enhancement of solubility and dissolution of IB.
Methods: The COAM system was prepared by chemical electric magnetic field microwave-assisted method. Several batches with different concentrations of COAM PA and IB were prepared at constant temperature, pressure, and holding time. Solubility studies were carried out in different pH condition and the batch, which show the highest increase in solubility 98.00%. COAM samples were characterized by solubility, dissolution, Fourier transform infrared (FTIR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC) studies.
Results: FTIR results showed evidence of molecular interactions between both the drugs. Maximum increase in aqueous solubility of IB was seen 500:200 mg dose ratio (COAM) batch E in phosphate buffer 7.4. The COAM system increased solubility of IB about 98.70%. The solubility and dissolution rate of IB were also enhanced. In vitro drug release study, 100% of the drug was released within 120 min. Thus, saturation solubility and dissolution rate of IB were found significant improved unlike PA. XRD and DSC results confirmed amorphization of IB. FTIR results evidenced hydrogen bonding interactions between both the drugs. In accelerated stability studies, powder XRD and DSC results demonstrated insignificant changes, thus confirming successful stabilization of IB by PA.
Conclusion: Hence, it concluded that the study of COAM of PA and IB successfully prepared by microwave-assisted method to enhance solubility, dissolution, stability, and bioavailability.
2. Shinde S, Patil S, Mevekari F, Satpute A. An approach for solubility enhancement: Solid dispersion. Int J Adv Pharma Sci 2010;1:299-310.
3. Saleki-Gerhardt A, Stowell JG, Byrn SR, Zografi G. Hydration and dehydration of crystalline and amorphous forms of raffinose. J Pharm Sci 1995;84:318-23.
4. Adahalli SB, Talluri M. Formulation and evaluation of tablet prepared by coamorphous system containing anti-hypertensive and anti-hyperlipidemic drug. Int J Pharm Pharm Sci 2016;8:182-93.
5. Li Y, Han J, Zhang GG, Grant DJ, Suryanarayanan R. In situ dehydration of carbamazepine dihydrate: A novel technique to prepare amorphous anhydrous carbamazepine. Pharm Dev Technol 2000;5:257-66.
6. Okamoto P, Lam N. Physics of crystal-to-glass transformations. Solid State Phys 1999;52:1-135.
7. Descamps M, Willart J, Dudognon E, Caron V. Transformation of pharmaceutical compounds upon milling and comilling: The role of Tg. J Pharm Sci 2007;96:1398-407.
8. Potthast H, Dressman JB, Junginger HE, Midha KK, Oeser H, Shah VP, et al. Biowaiver monographs for immediate release solid oral dosage forms: Ibuprofen. J Pharm Sci 2005;94:2121-31.
9. Dudognon E, Danède F, Descamps M, Correia NT. Evidence for a new crystalline phase of racemic ibuprofen. Pharm Res 2008;25:2853-8.
10. Pramanik T, Padan SK. Microwave irradiated green Biginelli Reaction employing apple, promraganate and grape juice as eco-friendly reaction medium. Int J Pharm Pharm Sci 2016;8:396-8.
11. Caron V, Willart JF, Lefort R, Derollez P, Danède F, Descamps M, et al. Solid state amorphization kinetic of alpha lactose upon mechanical milling. Carbohydr Res 2011;346:2622-8.
12. Terada K, Kitano H, Yoshihashi Y, Yonemochi E. Quantitative correlation between initial dissolution rate and heat of solution of drug. Pharm Res 2000;17:920-4.
13. Einfal T, Planinšek O, Hrovat K. Methods of amorphization and investigation of the amorphous state. Acta Pharm 2013;63:305-34.
14. Nokhodchi A, Aliakbar R, Desai S, Javadzadeh Y. Liquisolid compacts: The effect of cosolvent and HPMC on theophylline release. Colloids Surf B Biointerfaces 2010;79:262-9.
15. Hancock BC, Zografi G. Characteristics and significance of the amorphous state in pharmaceutical systems. J Pharm Sci 1997;86:1-2.
16. Laitinen R, Löbmann K, Strachan CJ, Grohganz H, Rades T. Emerging trends in the stabilization of amorphous drugs. Int J Pharm 2013;453:65 79.
17. Benedict C, Jibiri N, Bede E, Anusionwu B, Orji C, Alisi C. Effect of ingestion of microwaved foods on serum anti-oxidant enzymes and vitamins of albino rats. Sci Dir 2017;10:148-51.
18. Estevez R, Lopez PS, Luna D, Bautista F. Microwave-assisted etherification of glycerol with tert-butyl alcohol over amorphous organosilica-aluminum phosphate. Sci Dir 2017;213:42-52.
19. Bello A, Fashedemi O, Barzegar F, Madito M, Momodu DY, Masikhwa TM, et al. Microwave synthesis: Characterization and electrochemical properties of amorphous activated carbon-MnO2 nanocomposite electrodes. J Alloys Compd 2016;681:293-300.
20. Löbmann K, Laitinen R, Grohganz H, Gordon KC, Strachan C, Rades T, et al. Coamorphous drug systems: Enhanced physical stability and dissolution rate of indomethacin and naproxen. Mol Pharm 2011;8:1919-28.
21. Löbmann K, Strachan C, Grohganz H, Rades T, Korhonen O, Laitinen R, et al. Co-amorphous simvastatin and glipizide combinations show improved physical stability without evidence of intermolecular interactions. Eur J Pharm Biopharm 2012;81:159-69.
22. Dengale SJ, Ranjan OP, Hussen SS, Krishna BS, Musmade PB, Gautham Shenoy G, et al. Preparation and characterization of co-amorphous ritonavir-indomethacin systems by solvent evaporation technique: Improved dissolution behavior and physical stability without evidence of intermolecular interactions. Eur J Pharm Sci 2014;62:57-64.
23. Laitinen R, Löbmann K, Grohganz H, Strachan C, Rades T. Amino acids as co-amorphous excipients for simvastatin and glibenclamide: Physical properties and stability. Mol Pharm 2014;11:2381-9.
24. Wairkar S, Gaud R. Co-amorphous combination of nateglinide-metformin hydrochloride for dissolution enhancement. AAPS PharmSciTech 2016;17:673-81.
25. Surati M, Jauhari S, Desai K. A brief review: Microwave assisted organic reaction. Scho Res Lib 2012;4:645-61.
26. Paradkar A, Ambike AA, Jadhav BK, Mahadik KR. Characterization of curcumin-PVP solid dispersion obtained by spray drying. Int J Pharm 2004;271:281-6.
27. Giron D, Remy P, Thomas S, Vilette E. Quantitation of amorphicity by microcalorimetry. J Therm Anal 1997;48:465-72.
28. Craye G, Löbmann K, Grohganz H, Rades T, Laitinen R. Characterization of amorphous and co-amorphous simvastatin formulations prepared by spray drying. Molecules 2015;20:21532-48.
29. Savolainen M, Kogermann K, Heinz A, Aaltonen J, Peltonen L, Strachan C, et al. Better understanding of dissolution behaviour of amorphous drugs by in situ solid-state analysis using Raman spectroscopy. Eur J Pharm Biopharm 2009;71:71-9.
This work is licensed under a Creative Commons Attribution 4.0 International License.
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.