Spherical Crystallization: A Tool to Improve the Physicochemical Properties of APIs

  • R. R Thenge Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India
  • M P Chandak Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India
  • V. S Adhao Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India

Abstract

A greater challenge in solid dosage formulation is the development of spherical agglomerates which increases the solubility and bioavailability of the drug. Spherical crystallization is “An agglomeration process that transforms crystals directly into compact spherical forms during the crystallization process.” Spherical crystallization is the novel agglomeration technique that can transform directly the fine crystals produced in the crystallization process into a spherical shape. Direct Compression of powders is simple and easy way of making tablets. In direct compression of Good Compressibility and flowability plays a major role. Spherical crystallization methods are very useful methods in which the drug crystals are modified using different solvents to directly compressible agglomerates. which cost effective and time saving. The different Techniques discussed are Crystallization method, Solvent crystallization method, Quasi- emulsion diffusion method, Ammonia Diffusion method, neutralization method, and solvent agglomeration technique. This article gives a detailed and comprehensive review about different techniques, its advantages, mechanism and application of Spherical agglomeration Technique along with its Evaluation and Characterization methods.


 

Keywords: Spherical Crystallization, Evaluation, Novel drug delivery system.

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Author Biographies

R. R Thenge, Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India

Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India

M P Chandak, Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India

Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India

V. S Adhao, Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India

Dr. Rajendra Gode College of Pharmacy, Malkapur-443101, Maharashtra, India

References

1. Rasmuson CA, Katta J. Spherical crystallization of benzoic acid. Int. J. Pharm.,1997; 348: 61-69.
2. Singh M, S Manikandan, AK Kumaraguru. Nanoparticles: A new technology with wide applications. Res. J. Nanosci. Nanotechnol.,2011; 1: 1-11.
3. Shangraw RF, Compressed tablets by direct compression. In: Lieberman HA, Lachman L, Schwartz J. B. Pharmaceutical Dosage Forms: Tablets,Marcel Dekker, New York, 1989; 1:195–246.
4. Eros I, Goczo H, Szabo-Revesz P, Farkas B, Hasznos-Nezdei M, Serwanis FS, Pintye-Hodi K, Kasa P, Antal I, Marton S. Development of spherical crystals of acetyl salicylic acid for direct tablet making. Chem. Pharm. Bull, 2000; 48(12):1877-1881.
5. Gharaei-Fathabad, E. Biosurfactants in pharmaceutical industry: A mini-review. Am. J. Drug Discovery Dev, 2011; 1: 58-69.
6. Patil SV, Sahoo SK. Pharmaoverview of spherical crystallization. Der Pharmacia Lettre 2010; 2(1)421-426.
7. Sano A, Kuriki T, Kawashima Y, Takeuchi H, Hino T, Niwa T. Particle design of tolbutamide by spherical crystallization tech. V. Improvement of dissolution and bioavailability of direct compressed tablets prepared using tolbutamide agglomerated crystals. Chem. Pharm. Bull. 1992; 40:3030-3035.
8. MM Gupta, B Srivastava, M Sharma, V Arya. Int J Pharm Res Dev., 2010; 12(2):1-10.
9. N Bharti, N Bhandari, P Sharma, K Singh; A Kumar. Asian Jof Biomedical and Pharm Sci,2013; 18(3):10-16.
10. VB Yadav, AV Yadav.Trop J Pharm Res., 2009; 8(4):361-369.
11. A Nokhodchi, M Maghsoodi, D Hassanzadeh. Iran J Pharm Res., 2007; 6(2):83-93.
12. KR Mahadik, AP Pawar, AR Paradkar, S Kadam. AAPS Pharm Sci Tech., 2004; 5(3):1-8.
13. M Ueda, Y Nakamura, H Makita, Y Imasato, Y Kawashima. Chem Pharm Bull., 1990; 38(9):2537-2541.
14. A Sano, T Kuriki, Y Kawashima, H Takeuchi,THino; T Niwa. Chem Pharm Bull., 1992; 40 (10):3030-3035.
15. M Dixit, PK Kulkarni, PSC Bose, R Reddy. Int J of Pharm Res and Dev2010; 2(9):33-43.
16. Patil SV, Sahoo SK. Pharmoverview of spherical crystallization Res Library.Der Pharmacia Lettre, 2010; 2 (1): 421-426.
17. Kulkarni PK, Nagavi PG. Ind. Jr. Pharm. Eudc, 2002; 36(2):66-73.
18. Jain SK, Chourasia MK, Jain NK, Jain S. Preparation and characterization of agglomerates of flurbiprofen by spherical crystallization Tech.Ind. J. Pharm. Sci, 2003; 65(3):287-291.
19. Deshpande MC, Mahadik KR, Pawar AP and Paradkar AR. Evaluation of spherical crystallization as particle size enlargement Tech for aspirin Ind.JPharmSci, 1997 59(1):32-34.
20. Jarosz PJ and Parrott EL. Compression of granule strength and tablet tensile strength. J Pharm. Sci, 72(5), 1983, 530-534.
21. Bhadra S, Kumar M, Jain S, Agrawal S and Agrawal GR.Spherical crystallization of Mefenamic acid. Pharmaceutical Technology, 2004:66-76.
22. Chourasia MK, Jain SK, Jain S. and Jain NK. Preparation and characterization of agglomerates of Flurbiprofen by spherical crystallization technique. Ind. JPharm Sci, 2003:287-291.
23. Kaur H, Mariappan TT and Singh S. Behavior of uptake of moisture by drugs and excipients under accelerated conditions of temperature and humidity in the absence and presence of light, various drug substances, Part-III, 2009.
24. Gupta VR, Srinivas M, Patel MM, Jani GK. Spherical crystals of Celecoxib to improve the solubility, dissolution rate and micromeritic properties. Acta Pharm. 2007; 57:173-184.
25. Gohle MC, Parikh RK, Shen H, Rubey RR. Improvement in flowability and compressibility of Ampicilline Trihydrate by spherical crystallization. Ind J Pharm Sci. 2003; 634-37.
26. Hector GP, Jorge B, Carlo A. Preparation of Norfloxacin spherical agglomerates using the ammonia diffusion system. J Pharm Sci. 1998; 87(4):519-23.
27. Yadav VB, Yadav AV. Polymeric Recrystallized agglomerates of Cefuroxime Axetil prepared by Emulsion Solvent Diffusion Tech Trop. J Pharm. Res.2009; 8(4):361-369.
28. Yadav Venkat and Yadav Adhikrao; “Directly compressible roxithromycin recrystallizedagglomerates by solvent change Tech”. Scholars Res Library der Pharmacia Lettre 2010; (1)2:25-40.
29. Deshpande M.C, Mahadik K.R, Pawar A.P, Paradkar A.R; “Evaluation of spherical crystallization as particle size enlargement Tech for Aspirin”. IntJof PharmSci.1997; (1)53:32-34.
30. N. Usha, S. Mutalik, M. S. Reddy and A. K. Ranjith, Preparation and, in vitro, preclinical and clinical studies of Aceclofenac spherical agglomerates, Eur. J. Pharm. Biopharm.2008;70:674–683
31. H. Goczo, P. Szabo-Revesz, B. Farkas, M. Hasznos-Nezdei, S.F. Serwanis, A.K. Pintye-Hodi, P. Kasa, Jr., I. Eros, I. Antal and S.Marto, Development of spherical crystals of acetylsalicylic acid for direct tablet-making, Chem. Pharm. Bull.2000; 48:1877–1881.
32. Bausch A, Leuenberger H. Wet spherical agglomeration of proteins as a new method to prepare parenteral fast soluble dosage forms. Int J Pharm. 1994; 101:63-70.
33. P. Di Martino, C. Barthelemy, F. Piva, E. Joiris, G. F. Palmieri and S. Martelli, Improved dissolution behavior of fenbufen by spherical crystallization, Drug Dev. Ind. Pharm.1999; 25:1073–1081.
34. J bilou M, Ettabia A, Guyot-Hermann, AM, Guyot JS. Ibuprofen agglomeration prepared by phase separation. Drug Dev Ind Pharm. 1990; 25(3):297-305.
35. Pawar, A. Paradkar, S. Kadam and K. Mahadik, Crystallo-co-agglomeration: A novel technique to obtain ibuprofen-paracetamol agglomerates, AAPS Pharm.Sci.Tech.5, 2004):44.
36. Pawar, A. R. Paradkar, S. S. Kadam and K. R. Mahadik, Effect of polymers on crystallo-co-agglomeration of ibuprofen-paracetamol: Factorial design, Ind. J. Pharm. Sci. 2007; 69:658–664.
37. Pawar A, Paradkar A, Kadam S, Mahadik K. Agglomeration of Ibuprofen with Talc by Novel Crystallo-Co- Agglomeration Technique. AAPS Pharm SciTech, 2004; 5(4):1-6.
38. Mudit Dixit, PK Kulkarni1. Spherical agglomeration of Indomethacin by solvent change method. Int J of Pharma Res and Dev, 2005; 2(9):33-43.
39. Kawashima Y. Devof spherical crystallization tech and its application to pharmsystems. Arch Pharm. Res.1984; 7(2):145-151.
40. F. Espitalier, B. Biscans and C. Laguerie, Particle design Part B: batch quasi-emulsion process and mechanism of grain formation of ketoprofen, Chem. Eng. J.1997; 68:103–114.
41. Chavda V, Maheshwari RK. Tailoring of ketoprofen particle morphology via novel crystallo-coagglomeration technique to obtain a directly compressible material, Asian J. Pharm,2008; 2(1):61-67.
42. S. Bhadra, M. Kumar, S. Jain, S. Agrawal and G. P. Agrawal, Spherical crystallization of mefenamic acid, Pharm. Technol. 2004: 66–76.
43. M. Maghsoodi, O. Taghizadeh, G. P. Martin and A. Nokhodchi, Particle design of naproxen-disintegrant agglomerates for direct compression byacrystallo-co-agglomeration Tech, IntJPharm.2008; 351:45–54.
44. Viswanathan CL, Kulkarni SK, Kolwankar DR. Spherical agglomeration of mefenamic acid and Nabumetone to improve micromeritics and solubility: A Technical AAPS Pharm Sci Tech.2006; 7(2):48.
45. M Dixit, PK Kulkarni. Preparation and characterization of spherical agglomerates of Piroxicam by neutralization method. American J of drug discovery and dev, 2011:1-12.
46. Martino P.D, Cristofaro R.D, Joiris E., Filippo G.P, Sante M; “Improved compression properties of propyphenazone spherical crystals”, IntJ of Pharm 2000; 197:95–106.
47. Kawashima Y, Aoki S, Takenaka H, Miyake Y; “Preparation of spherically agglomerated crystals of aminophylline”. Jof PharmSci 1984; (10)73:1407-10.
48. Bos AS, Zuiderweg FJ. Size of agglomerates in batch wise suspension agglomeration. Chem Eng Res Des. 1987; 65a: 187.
49. Bermer GG, Zuiderweg FG. Proceedings of international symposium of fine particles. AIME. 1992:1524-46.
50. Sano, T. Kuriki, Y. Kawashima, T. Hino and T. Niwa, Particle design of tolbutamide by the spherical crystallization technique. III. Micromeritic properties and dissolution rate of tolbutamide spherical agglomerates prepared by the quasi-emulsion solvent diffusion method and the solvent change method, Chem. Pharm. Bull.1990; 38:733–739.
51. Kawashima Y, Cui F, Takeuchi H, Niwa T, Hino T, Kiuchi K. Parameters determining the agglomeration behavior and the micromeritic properties of spherically agglomerated crystals prepared by the spherical crystallization technique with miscible solvent systems. Int. J. Pharm, 1995; 119(2):139-147.
52. Yadav VB, Yadav AV. Effect of Different Stabilizers and Polymers on Spherical Agglomerates of Gresiofulvine by Emulsion Solvent Diffusion (ESD) System. Int. J. Pharm. Tech. Res., 2009; 1(2):149-150.
53. Kawashima Y, Niwa T, Takeuchi H, Hino T, Itoh Y, Furuyama S, Characterization of polymorphs of Tranilast anhydrate and Tranilast monohydrate when crystallization by two solvents changes spherical crystallization Tech. J. Pharm. Sci., 1991; 80(5):472-78.
54. Miss Bhosale Bhakti Bhimarao, Mr. D. M. Shivale Preparation and characterization of spherical crystals of valsartan for direct compression method Int J of Pharm Res and Dev, 2009; 1:4.
55. Kumar S, Chawla G, Bansal A. Spherical Crystallization of Mebendazole to Improve Processability. Pharm. Dev. Technol.2008; 13(6):559-568.
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How to Cite
Thenge, R., Chandak, M., & Adhao, V. (2020). Spherical Crystallization: A Tool to Improve the Physicochemical Properties of APIs. Asian Journal of Pharmaceutical Research and Development, 8(3), 104-110. https://doi.org/https://doi.org/10.22270/ajprd.v8i3.727