In-process crystallization of acidic drugs in acrylic microparticle systems: Influence of physical factors and drug-polymer interactions

Journal of Pharmaceutical Sciences

Volumn 100, Issue 8, 2011, Pages 3284-3293

  Alhnan, Mohamed A ^a   Basit, Abdul W ^a  

^a UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

Calorimetry (DSC); Emulsion solvent evaporation; Enteric polymers; Methacrylic acid methyl methacrylate; Microencapsulation; Microspheres; Non steroidal anti inflammatory drugs (NSAIDs); Oral drug delivery; Stability; Thermal analysis

Indexed keywords

ACRYLIC ACID; DRUG CARRIER; EUDRAGIT; INDOMETACIN; KETOPROFEN; MICROPARTICLE; MICROSPHERE; NAPROXEN; PARACETAMOL; PLASTICIZER; POLYMER; SALICYLIC ACID; UNCLASSIFIED DRUG;

ARTICLE; CRYSTALLIZATION; DRUG INTERACTION; DRUG RELEASE; DRUG SOLUBILITY; EMULSION; EVAPORATION; GLASS TRANSITION TEMPERATURE; MICROENCAPSULATION;

EID: 79955113999     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.22572     Document Type: Article

References (23)

1. Bodmeier R, Huagang C. 1989. Preperation and characterization of microspheres containing the anti-inflammatory agents, indomethacin, ibuprofen and ketoprofen. J Control Release 10:167-175.
2. Chandran S, Sanjay KS, Asghar LF. 2008. Microspheres with pH modulated release: Design and characterization of formulation variables for colonic delivery. J Microencapsul 26(5):420-431.
3. Mateovic T, Ratnik M, Bogataj M, Mrhar A. 2005. Determination of microsphere solidification time in the solvent evaporation process. J Microencapsul 22:81-90.
4. Kilicarslan M, Baykara T. 2003. The effect of the drug/polymer ratio on the properties of the verapamil HCl loaded microspheres. Int J Pharm 252:99-109.
5. Yang YY, Chia HH, Chung TS. 2000. Effect of preparation temperature on the characteristics and release profiles of PLGA microspheres containing protein fabricated by double-emulsion solvent extraction/evaporation method. J Control Release 69:81-96.
6. Li WI, Anderson KW, Mehta RC, Deluca PP. 1995. Prediction of solvent removal profile and effect on properties for peptide-loaded PLGA microspheres prepared by solvent extraction/ evaporation method. J Control Release 37:199-214.
7. Li WI, Anderson KW, Deluca PP. 1995. Kinetic and thermodynamic modeling of the formation of polymeric microspheres using solvent extraction/evaporation method. J Control Release 37:187-198.
8. Jenquin MR, Liebowitz SM, Sarabia RE, McGinity JW. 1990. Physical and chemical factors influencing the release of drugs from acrylic resin films. J Pharm Sci 79:811-816.
9. Mortada LM, Bostanian LA, Salib NN. 1990. Interactions of oxyphenbutazone with polyvinylpyrrolidone. Pharmazie 45: 350-354.
10. Crowley KJ, Zografi G. 2003. The effect of low concentrations of molecularly dispersed poly(vinylpyrrolidone) on indomethacin crystallization from the amorphous state. Pharm Res 20:1417-1422.
11. Matsumoto T, Zografi G. 1999. Physical properties of solid molecular dispersions of indomethacin with poly(vinylpyrrolidone) and poly(vinylpyrrolidone-co-vinyl-acetate) in relation to indomethacin crystallization. Pharm Res 16:1722-1728.
12. Yoshioka M, Hancock BC, Zografi G. 1995. Inhibition of indomethacin crystallization in poly(vinylpyrrolidone) coprecipitates. J Pharm Sci 84:983-986.
13. Miyazaki T, Yoshioka S, Aso Y, Kojima S. 2004. Ability of polyvinylpyrrolidone and polyacrylic acid to inhibit the crystallization of amorphous acetaminophen. J Pharm Sci 93:2710-2717.
14. Thompson C, Davies MC, Roberts CJ, Tendler SJ, Wilkinson MJ. 2004. The effects of additives on the growth and morphology of paracetamol (acetaminophen) crystals. Int J Pharm 280:137-150.
15. Fuji M, Hasegawa J, Kitajima H, Matsumoto M. 1991. The soild dispersion of benzodiazepins with phosphatidylcholine-effect of benzodiazepins on the formation of solid dispersion. Chem Pharm Bull (Tokyo) 39:3013-3017.
16. Konno H, Taylor LS. 2006. Influence of different polymers on the crystallization tendency of molecularly dispersed amorphous felodipine. J Pharm Sci 95:2692-2705.
17. Kendall R, Alhnan MA, Nilkumhang S, Murdan S, Basit AW. 2009. Fabrication and in vivo evaluation of highly pH-responsive acrylic microparticles for targeted gastrointestinal delivery. Eur J Pharm Sci 37:284-290.
18. Alhnan MA, Cosi D, Murdan S, Basit AW. 2010. Inhibiting the gastric burst release of drugs from enteric microparticles: The influence of drug molecular mass and solubility. J Pharm Sci 99:4576-4583.
19. Kaneniwa N, Otsuka M, Hayashi T. 1985. Physicochemical characterization of indomethacin polymorphs and the transformation kinetics in ethanol. Chem Pharm Bull (Tokyo) 33:3447-3455.
20. Borka L. 1974. The polymorphism of indomethacine. New modifications, their melting behavior and solubility. Acta Pharm Suec 11:295-303.
21. Nilkumhang S. 2008. Preparation and evaluation of microparticles to target drugs to different regions of the gastrointestinal tract. London, UK: The School of Pharmacy, University of London.
22. Evonik Degussa. 2004. Specifications and test methods for Eudragit® L100 and Eudragit® S100.
23. El-obdeid HA, Al-Badr AA. 1985. Acetaminophen. In Analytical profiles of drug substances 14; Florey K, Ed. Academic Press Limited, London, UK. pp 555-557.