Improvement of flowability, compressibility and dissolution of aceclofenac by emulsion solvent diffusion with polyethylene glycol.
Keywords:
Spherical crystallization, Compressibility, Polyethylene glycolAbstract
Aim: The objective behind this study is to improve the compressibility, flowability, packability and dissolution rate of aceclofenac by preparing spherical crystals using quasi emulsion solvent diffusion method.
Materials and Method: Spherical agglomerates of aceclofenac were effectively prepared using acetone, dichloromethane and 0.1 N HCl as good solvent, bridging liquid and poor solvent respectively with different concentrations of polyethylene glycol 6000 in poor solvent.
Results: Prepared agglomerates were spherical with enhanced fragmentation and less elastic recovery. Particle size, flowability, compactibility, packability, solubility and dissolution rate of agglomerates were preferably improved for direct compression compared with raw crystal of aceclofenac. X-ray powder diffraction and differential scanning calorimetry study indicated slight amorphization of drug during recrystallization but not associated with any chemical transition indicated by Fourier transforms infrared spectra.
Conclusion: The present research improved tableting properties and dissolution characteristics of aceclofenac.
Downloads
References
Szabo RP, Goczo H, Pintye HK, Kasa P, Eros I, Hasznos NM, et
al. Development of spherical crystal agglomerates of an aspartic
acid salt for direct tablet making. Powder Technol. 2001; 114(1-
:118-24.
Kawashima Y, Furukawa K, Takenaka H. The physicochemical
parameters determining the size of agglomerate prepared by the
wet spherical agglomeration technique. Powder Technol. 1981;
:211-6.
Guillory JK. Generation of polymorphs, hydrates, solvates
and amorphous solids. In: Brittain HG, ed. Polymorphism in
pharmaceutical solids. New York: Marcel Dekker; 1999:183–226.
Patil SV, Sahoo SK. Spherical Crystallization: a method to
improve tabletability. Research J Pharm and Tech. 2009; 2
(2):234–7.
Yadav AV, Yadav VB. Designing of pharmaceuticals to
improve physicochemical properties by spherical crystallization
technique. J Pharm Res. 2008; 1(2):105–12.
Pawar AH, Pawar AP, Mahadik KR, Paradkar AR. Evaluation
of tableting properties of agglomerates obtained by spherical
crystallization of trimethoprim. Indian J Pharm Sci. 1998;
(1):24-8.
Kawashima Y, Okumura M, Takenaka H. The effects of temperature on the spherical crystallization of salicylic acid. Powder Technol. 1984; 39(1):41–7.
Gordon MS, Chowhan ZT. Manipulation of naproxen particle morphology via the spherical crystallization technique to achieve directly compressible raw material. Drug Dev Ind Pharm. 1990; 16(8):1279-90.
Paradkar AR, Pawar AP, Mahadik KR, Kadam SS. Spherical crystallization: a novel particle design technique. Indian Drugs. 1994; 31(6):229–33.
Paradkar AR, Pawar AP, Chordiya JK, Patil VB, Ketkar AR. Spherical crystallization of celecoxib. Drug Dev Ind Pharm. 2002; 28(10):1213-20.
Martindale: The extra pharmacopoeia. 33 ed. London: Pharmaceutical Press; 2002.
Ghosh S, Barik BB. Formulation and in vitro evaluation of once daily sustained release formulation of Aceclofenac. Trop J Pharm Res. 2010; 9(3):265-73.
Carr RL. Evaluating flow properties of solids. Chem Engg. 1965; 72(2):163-8.
Lachman L, Liberman HA, Konig JL. Theory and Practice of Industrial Pharmacy. 3ª ed. London: PA, Lea and Febiger, Philadelphia; 1986.
Heckel RW. An analysis of powder compaction phenomenon. Trans Metal Sci. AIME. 1961; 221:1001-8.
Heckel RW. Density-pressure relationships in powder compaction. Trans Metal Sci. AIME. 1961; 221:671-5.
Armstrong NA, Hainess-Nutt RF. Elastic recovery and surface area changes in compacted powder system. Powder Technol. 1974; 9(5-6):287-90.
Kawakita K, Ludde KH. Some considerations on powder equations. Powder Technol.1971; 4(2):61–8.
Ali N, Maryam M, Davood HZ, Mohammad BJ. Preparation of agglomerated crystals for improving flowability and compactibility of poorly flowable and compactible drugs and excipients. Powder Technol. 2007; 175(2):73–81.
Downloads
Published
How to Cite
Issue
Section
License
The articles, which are published in this journal, are subject to the following terms in relation to the rights of patrimonial or exploitation:
- The authors will keep their copyright and guarantee to the journal the right of first publication of their work, which will be distributed with a Creative Commons BY-NC-SA 4.0 license that allows third parties to reuse the work whenever its author, quote the original source and do not make commercial use of it.
b. The authors may adopt other non-exclusive licensing agreements for the distribution of the published version of the work (e.g., deposit it in an institutional telematic file or publish it in a monographic volume) provided that the original source of its publication is indicated.
c. Authors are allowed and advised to disseminate their work through the Internet (e.g. in institutional repositories or on their website) before and during the submission process, which can produce interesting exchanges and increase citations of the published work. (See The effect of open access).