Crystallo-co-agglomeration: A novel particle engineering technique

Anant R Paradkar, Atmaram P Pawar

Abstract


Crystallo-co-agglomeration (CCA) is a novel particle engineering/design technique developed by Kadam et al, to overcome the limitations of spherical crystallization (SC). Basically, it’s single step process used for size enlargement of single, two or more, small dose or large dose drugs, in combination with or without diluent. The process of CCA involves simultaneous crystallization and agglomeration of drug/s with/without excipients/s from good solvent and/or bridging liquid by addition of a non-solvent.Till date CCA has been applied for spherical agglomeration of talc, bromhexine hydrochloride–talc, ibuprofen–talc, ibuprofen–paracetamol, and naproxen–starch. The spherical agglomerates obtained by CCA can be used as intact beads (encapsulated spansules) or directly compressible tablet intermediates having satisfactory micromeritic (flowability), mechanical (friability, crushing), compressional (compressibility, compactibility), and drug
release properties. Modified drug release from agglomerates and compacts thereof can be achieved using suitable polymer composition in the process design. Thus, it can be concluded that, CCA is a simple and cost effective process, which can be
tailor-made for particle design of all majority of drugs and combinations thereof.


Full Text:

PDF

References


Kawashima Y. Spherical crystallization as a novel particle design

technique for oral drug delivery system. Chin Pharm J 1989;41:

-72.

Lachman L, Liberman HA, Kanig JL. Theory and Practice of Industrial

Pharmacy. 2nd ed. Philadelphia, USA: Lea & Febiger; 1976. p. 317-24.

Woodruff CW, Nuessle NO. Effect of processing variables on particles

obtained by extrusion-spheronisation processing. J Pharm Sci

;61:787-90.

Lachman L, Liberman HA, Kanig JL. Theory and Practice of Industrial

Pharmacy. 2nd ed. Philadelphia, USA: Lea & Febiger; 1976. p. 338-9.

Piera D, Mara S, Etienne JG. The spray drying of acetazolamide as a

method to modify crystal properties and to improve compression

behaviour. Int J Pharm 2001;213:209-21.

Asker AF, Beeker CH. Some spray -dried formulations of

sulfaethylthiadiazole for prolonged-release medication. J Pharm Sci

;55:90-4.

Aerger JS, Price R. Processing of spherical crystalline particles via a novel

solution atomisation and xtallisation by sonication (SAXS) technique.

Pharm Res 2004;21:372-81.

Paradkar AR, Maheshwari M, Chauhan B. Preparation and evaluation

of ibuprofen beads by melt solidification technique. Int J Pharm

;255:33-42.

Paradkar AR, Maheshwari M, Jahagirdar HA. Melt sonocrystallisation

of ibuprofen: Effect on crystal properties. Eur J Pharm Sci 2005;25:

-8.

Jayasankar A, Somwangthanaroj A. Cocrystal formation during

cogrinding and storage is mediated by amorphous phase. Pharm Res

;23:2381-92.

Kawashima Y, Okumura M, Takenaka H. Spherical crystallization: Direct

spherical agglomeration of salicylic acid during crystallization. Science

;216:1127-8.

Kadam SS, Mahadik KR, Paradkar AR. A process for making agglomerates

for use as or in a drug delivery system. Indian Patent 183036;1997.

Kadam SS, Mahadik KR, Paradkar AR. A process for making agglomerates

for use as or in a drug delivery system. Indian Patent 183481;1997.

Tapia C, Buckton G, Newton J. Factors influencing the mechanism of

release from sustained release matrix pellets produced by extrusion-

spheronization. Int J Pharm 1993;92:211-8.

Neau SH, Chow MY, Durrani MJ. Fabrication and characterization of

extruded and spheronized beads containing carbopol 974P NF resin.

Int J Pharm 1996;131:47-55.

Goskonda SR, Hileman GA, Upadrashta SM. Controlled release pellets

by extrusion-spheronization. Int J Pharm 1994;111:89-97.

Jorgensen K, Christensen FN, Jacobsen L. Dissolution stability of

multiparticulate controlled release tablets. Int J Pharm 1997;153:1-11.

Umprayn K, Chitropas P, Amarekajom S. Development of terbutaline

sulfate sustained-release coated pellets. Drug Dev Ind Pharm

;25:477-91.

Kojima M, Nakagami H. Development of controlled release matrix

pellets by annealing with micronized water-insoluble or enteric

polymers. J Control Release 2002;82:335-43.

Bechgaard H, Hegermann NG. Controlled-release multiple-units and

single-unit doses: a literature review. Drug Dev Ind Pharm 1978;4:

-67.

Tang SK, Chan LW, Heng WS. Coating of multiparticulates for sustained

release. Am J Drug Deliv 2005;3:17-8.

Freely LC, Khosla R, Davis SS. Investigating the gastric emptying of

different sizes of non- disintegrating tablets in humans using gamma

scintigraphy. J Pharm Pharmacol 1987;39:31-7.

Bechgaard H. Critical factors influencing gastrointestinal absorption:

What is the role of pellets? Acta Pharm Technol 1982;28:149-57.

Devereux JE, Newton JM, Short MB. The influence of density on the

gastrointestinal transit of pellets. J Pharm Pharmacol 1990;42:500-1.

Clarke GM, Newton MJ, Short MD. Gastrointestinal transit of pellets of

differing size and density. Int J Pharm 1993;100:81-92.

Tuleu C, Andrieux C, Boy P, Chaumeil JC. Gastrointestinal transit of

pellets in rats: Effect of size and density. Int J Pharm 1999;180:123-31.

Paradkar AR, Mahadik KR, Pawar AP. Spherical crystallization a novel

particle design technique. Indian Drugs 1998;31:283-99.

Jadhav NR. Studies on applications of crystallo-co-agglomeration

technique in pharmaceutical formulations [doctoral thesis], Bharati

Vidyapeeth University, Pune 2009.

Jadhav NR. Studies on agglomerates of bromhexine hydrochloride

loaded talc prepared by crystallo-co-agglomeration [masters thesis],

University of Pune 1998.

Pawar AP, Paradkar AR, Kadam SS, Mahadik KR. Agglomeration of

ibuprofen with talc by novel crystallo-co-agglomeration technique.

AAPS PharmSciTech 2004;5:1-6.

Pawar AP, Paradkar AR, Kadam SS, Mahadik KR. Crystallo-co-

agglomeration: A novel process to obtain ibuprofen-paracetamol

agglomerates. AAPS PharmSciTech 2004;5:1-8.

Gadekar SE. Studies on preparation of bromhexine hydrochloride

loaded talc agglomerates by wet agglomeration technique [Masters

thesis], University of Pune; 1997.

Pawar AP. Studies on spherical crystallisation of various pharmaceuticals

[Doctoral thesis], University of Pune; 1999.

Kawashima Y, Aoki S, Takenaka H, Miyake Y. Preparation of spherically

agglomerated crystals of aminophylline. J Pharm Sci 1984;73:1407-10.

Limzerwala RB. Optimization of the wet agglomeration of talc [Masters

thesis], University of Pune; 1996.

Ganjian F, Cutie AJ, Jochsaberger T. In vitro adsorption studies of

cimetidine. J Pharm Sci 1980;69:352-53.

Maghsoodi M, Omid T, Martin GP, Nokhodchi A. Particle design of

naproxen-disintegrant agglomerates for direct compression by a

crystallo-co-agglomeration technique. Int J Pharm 2008;351:45-54.

Rao RP. Studies on talc agglomeration process [Masters thesis],

University of Pune; 1997.

Jagdale SC. Studies on evaluation of crystallo-co-agglomerates of

bromhexine hydrochloride loaded talc [Masters thesis], University of

Pune; 2000.

Kawashima Y, Handa T, Hirofumi T, Okumura M. Effects of polyethylene

glycol on size of agglomerated crystals of phenytoin prepared by

the spherical crystallization technique. Chem Pharm Bull (Tokyo)

;34:3403-7.

Kawashima Y, Handa T, Tekeuchi H, Okumara M, Katou H, Nagata

O. Crystal modification of phenytoin with polyethylene glycol for

improving mechanical strength, dissolution rate and bioavailability

by spherical crystallization technique. Chem Pharm Bull (Tokyo)

;34:3376-83.

Jadhav NR, Pawar AP, Paradkar AR. Design and evaluation of deformable

talc agglomerates prepared by crystallo-co-agglomeration technique

for generating heterogeneous matrix. AAPS PharmSciTech 2007;8:1-7.

Pawar AP, Paradkar AR, Kadam SS, Mahadik KR. Effect of polymers on

crystallo-co-agglomeration of ibuprofen-paracetamol: Factorial design.

Indian J Pharm Sci 2007;69:654-8.

Sanghavi NM, Sivanand R, Kotwaney HN. Dissolution pattern of

miniscular sulfisoxazole. Ind J Pharm Sci 1979;41:116-7.

Alsaidan SM, Abdulhakeem AA, Eshra AG. Improved dissolution rate

of indomethacin by adsorbents. Drug Dev Ind Pharm 1998;24:389-94.

Aulton ME, Dyer AM, Khan KA. The strength and compaction of

millispheres: The design of a controlled-release drug delivery system

for ibuprofen in the form of a tablet comprising compacted polymer-

coated millispheres. Drug Dev Ind Pharm 1994;20:3069-104.

Lin K, Peck GE. Development of agglomerated talc, I: Evaluation of

fluidized bed granulation parameters on the physical properties of

agglomerated talc. Drug Dev Ind Pharm 1995;21:159-73.

Lin K, Peck GE. Development of agglomerated talc, II: Optimization of

the processing parameters for the preparation of granulated talc. Drug

Dev Ind Pharm 1995;21:447-60.

Ho T, Hersey JA. Granulation using the agglomerative phase of

comminution. Powder Technol 1979;23:191-5.

Patki SR. Extended release beads of felodipine prepared by crystallo-co-

agglomeration technique [Masters thesis], Kolhapur: Shivaji University;

Shouche PV. Use of talc beads as coating substrates [Masters thesis],

Kolhapur: Shivaji University; 2009.




DOI: http://dx.doi.org/10.22377/ajp.v4i1.115

Refbacks

  • There are currently no refbacks.