PMCCPMCCPMCC

Search tips
Search criteria 

Advanced

 
Logo of aapspharmspringer.comThis journalToc AlertsSubmit OnlineOpen Choice
 
AAPS PharmSciTech. 2005 September; 6(3): E359–E366.
Published online 2005 October 14. doi:  10.1208/pt060345
PMCID: PMC2750380

Dry granulation and compression of spray-dried plant extracts

Abstract

The purpose of this research was to evaluate the influence of dry granulation parameters on granule and tablet properties of spray-dried extract (SDE) fromMaytenus ilicifolia, which is widely used in Brazil in the treatment of gastric disorders. The compressional behavior of the SDE and granules of the SDE was characterized by Heckel plots. The tablet properties of powders, granules, and formulations containing a high extract dose were compared. The SDE was blended with 2% magnesium stearate and 1% colloidal silicon dioxide and compacted to produce granules after slugging or roll compaction. The influences of the granulation process and the roll compaction force on the technological properties of the granules were studied. The flowability and density of spray-dried particles were improved after granulation. Tablets produced by direct compression of granules showed lower crushing strength than the ones obtained from nongranulated material. The compressional analysis by Heckel plots revealed that the SDE undergoes plastic deformation with a very low tendency to rearrangement at an early stage of compression. On the other hand, the granules showed an intensive rearrangement as a consequence of fragmentation and rebounding. However, when the compaction pressure was increased, the granules showed plastic deformation. The mean yield pressure values showed that both granulation techniques and the roll compaction force were able to reduce the material's ability to undergo plastic deformation. Finally, the tablet containing a high dose of granules showed a close dependence between crushing strength and the densification degree of the granules (ie, roll compaction force).

Keywords: Dry granulation, Maytenus ilicifolia, spraydried extracts, Heckel plot, tableting

Full Text

The Full Text of this article is available as a PDF (400K).

Selected References

These references are in PubMed. This may not be the complete list of references from this article.
1. Souza KCB, Petrovick PR, Bassani VL, González Ortega G. The adjuvants Aerosil 200 and Gelita-Sol-P influence on the technological characteristics of spray-dried powder fromPassiflora edulis var.flavicarpa. Drug Dev Ind Pharm. 2000;26:331–336. doi: 10.1081/DDC-100100361. [PubMed] [Cross Ref]
2. Diaz L, Souto C, Concheiro A, Gomez-Amozy LM, Martinez-Pacheco R. Evaluation of Eudragit E as excipient in tablets of dry plant extract. STP Pharma Sci. 1986;2:105–109.
3. Souza TP, Bassani VL, González Ortega G, Dalla Costa TCT, Petrovick PR. Influence of adjuvants on the dissolution profile of tablets containing high dose of spray-dried extract ofMaytenus ilicifolia. Pharmazie. 2001;56:730–733. [PubMed]
4. Plaizer-Vercamen JA, Bruwier C. Evaluation of excipients for direct compression of the spray-dried extract ofHarpogaphytum procumbens. STP Pharma Sci. 1986;2:525–530.
5. Rocksloh K, Rapp FR, Abu Abed S, et al. Optimization of crushing strength and disintegration time of a high-dose plant extract tablet by neural network. Drug Dev Ind Pharm. 1999;25:1015–1025. doi: 10.1081/DDC-100102264. [PubMed] [Cross Ref]
6. Eggelkraut-Gottanka SG, Abu Abeb S, Müller W, Schmidt PC. Roller compaction and tabletting of St. John's wort plant dry extract using gap width and force controlled roller compactor, I: granulation and tabletting of eight different extract batches. Pharm Dev Technol. 2002;7:433–445. doi: 10.1081/PDT-120015046. [PubMed] [Cross Ref]
7. Miller RW. Roller compaction technology. In: Parikh DM, editor. Handbook of Pharmaceutical Granulation Technology. New York, NY: Marcel Dekker; 1997. pp. 99–150.
8. Freitag F, Kleinebude P. How do roll compaction/dry granulation affect the tablet behavior of inorganic materials? Comparison of four magnesium carbonates. Eur J Pharm Sci. 2003;19:281–289. doi: 10.1016/S0928-0987(03)00133-7. [PubMed] [Cross Ref]
9. Bultmann JM. Multiple compaction of microcrystalline cellulose in a roller compactor. Eur J Pharm Biopharm. 2002;54:59–64. doi: 10.1016/S0939-6411(02)00047-4. [PubMed] [Cross Ref]
10. Heckel RW. An analysis of powder compaction phenomena. Trans. Metal. Sci. AIME. 1961;221:1001–1008.
11. Heckel RW. Density-pressure relationship in powder compaction. Trans. Metal. Sci. AIME. 1961;221:671–675.
12. Rue PJ, Rees JE. Limitations of the Heckel relation for predicting powder compaction mechanisms. J Pharma Pharmacol. 1978;30:642–643. [PubMed]
13. Ilkka J, Paronen P. Prediction of the compression behavior of powder mixtures by the Heckel equation. Int J Pharm. 1993;94:181–187. doi: 10.1016/0378-5173(93)90022-8. [Cross Ref]
14. Mitrevej A, Faroongsarng D, Sinchaipanid N. Compression behavior of spray dried starch. Int J Pharm. 1996;140:61–68. doi: 10.1016/0378-5173(96)04576-0. [Cross Ref]
15. Kochhar SK, Rubinstein MH, Barnes D. The effects of slugging and recompression on pharmaceutical excipients. Int J Pharm. 1995;115:35–43. doi: 10.1016/0378-5173(94)00250-9. [Cross Ref]
16. Horisawa E, Danjo K, Sunada H. Influence of granulating method on physical and mechanical properties: compression behavior and compactibility of lactose and microcrystalline cellulose granules. Drug Dev Ind Pharm. 2000;26:583–593. doi: 10.1081/DDC-100101273. [PubMed] [Cross Ref]
17. Petrovick PR, Carlini E. Antiulcerogenic preparation fromMaytenus ilicifolia and obtainment process. Brazil patent PI 994 502. March 6, 1999.
18. Darstellung von Korn-(teilchen-)-grössenverteilungen—RRSB-Netz. Berlin, Germany: Beuth Verlag; 1997. pp. 191–193.
19. European Pharmacopoeia. Strasbourg, France: Council of Europe; 1997.
20. Hausner HH. Friction conditions in a mass of metal powder. Int J Powder Mettall. 1967;3:7–13.
21. Carr RL. Evaluating flow properties of solids. Chem Engineer. 1965;72:163–168.
22. Guyot JC, Arnaud P, Becourt P, et al. Commentaires Relatifs aux Méthodes Générales d'analyse des Formes Orales Solides Récemment Introduites dans les Pharmacopées Française et Européene. Rapport d'une Commision SFSTP. STP Pharma Pratiques. 1995;5:482–494.
23. Dressler JA, Wagner KG, Wahl MA, Schmidt PC. Comparison of incremental and inductive displacement transducers on an eccentric tablet press. Pharm Ind. 2001;53:886–893.
24. European Pharmacopoeia Supplement. Strasbourg. France: Council of Europe; 2001.
25. Rees JE, Rue PJ. Time-dependent deformation of some direct compression excipient. J Pharm Pharmacol. 1978;30:601–607. [PubMed]

Articles from AAPS PharmSciTech are provided here courtesy of American Association of Pharmaceutical Scientists