Show simple item record

dc.contributor.authorKaialy, Waseem
dc.contributor.authorLarhrib, Hassan
dc.contributor.authorChikwanha, Brian
dc.contributor.authorShojaee, Saeed
dc.contributor.authorNokhodchi, Ali
dc.date.accessioned2017-06-14T12:34:22Z
dc.date.available2017-06-14T12:34:22Z
dc.date.issued2014-04-10
dc.identifier.citationAn approach to engineer paracetamol crystals by antisolvent crystallization technique in presence of various additives for direct compression. 2014, 464 (1-2):53-64 Int J Pharm
dc.identifier.issn1873-3476
dc.identifier.pmid24480534
dc.identifier.doi10.1016/j.ijpharm.2014.01.026
dc.identifier.urihttp://hdl.handle.net/2436/620513
dc.description.abstractParacetamol is a popular over-the-counter analgesic and a challenging model drug due to its poor technological and biopharmaceutical properties such as flowability, compressibility, compactibility and wettability. This work was aimed to alter the crystal habit of paracetamol from elongated to polyhedral-angular via particle engineering whilst maintaining the stable polymorphic form (form I: monoclinic form). The engineered paracetamol crystals obtained in the present investigation showed better technological and biopharmaceutical properties in comparison to the commercial paracetamol. Engineered paracetamol crystals were obtained using antisolvent crystallization technique in the presence of various concentrations (0.1, 0.5 and 1%, w/w) of additives, namely, polyvinyl alcohol (PVA), Avicel PH 102 (microcrystalline cellulose), Brij 58, methylcellulose (MC) and polyethylene glycol having different molecular weights (PEGs 1500, 6000 and 8000). Paracetamols crystallized in the presence of Avicel (or physically mixed with Avicel), Brij 58 and PEG 6000 demonstrated the best compactibility over a range of compaction pressures. Brij-crystallized paracetamol provided the fastest dissolution rate among all the paracetamol batches. Paracetamols crystallized in the presence of PVA or Avicel, or physically mixed with Avicel demonstrated a reduced degree of crystallinity in comparison to the other paracetamols. This study showed that the type, the grade and the concentration of additives could influence the physical stability such as flow, crystallinity and polymorphic transformation of paracetamol, the technological and biopharmaceutical properties of paracetamol. Stable polymorphic form of paracetamol with optimal tableting characteristics can be achieved through particle engineering.
dc.language.isoen
dc.subjectParticle engineering
dc.subjectAntisolvent crystallization;
dc.subjectParacetamol; Additives
dc.subjectCompactibility;
dc.subjectCrystal habit
dc.subject.meshAcetaminophen
dc.subject.meshChemical Engineering
dc.subject.meshCompressive Strength
dc.subject.meshCrystallization
dc.subject.meshParticle Size
dc.subject.meshPolymers
dc.subject.meshSolubility
dc.subject.meshSolvents
dc.titleAn approach to engineer paracetamol crystals by antisolvent crystallization technique in presence of various additives for direct compression.
dc.typeJournal article
dc.identifier.journalInternational journal of pharmaceutics
html.description.abstractParacetamol is a popular over-the-counter analgesic and a challenging model drug due to its poor technological and biopharmaceutical properties such as flowability, compressibility, compactibility and wettability. This work was aimed to alter the crystal habit of paracetamol from elongated to polyhedral-angular via particle engineering whilst maintaining the stable polymorphic form (form I: monoclinic form). The engineered paracetamol crystals obtained in the present investigation showed better technological and biopharmaceutical properties in comparison to the commercial paracetamol. Engineered paracetamol crystals were obtained using antisolvent crystallization technique in the presence of various concentrations (0.1, 0.5 and 1%, w/w) of additives, namely, polyvinyl alcohol (PVA), Avicel PH 102 (microcrystalline cellulose), Brij 58, methylcellulose (MC) and polyethylene glycol having different molecular weights (PEGs 1500, 6000 and 8000). Paracetamols crystallized in the presence of Avicel (or physically mixed with Avicel), Brij 58 and PEG 6000 demonstrated the best compactibility over a range of compaction pressures. Brij-crystallized paracetamol provided the fastest dissolution rate among all the paracetamol batches. Paracetamols crystallized in the presence of PVA or Avicel, or physically mixed with Avicel demonstrated a reduced degree of crystallinity in comparison to the other paracetamols. This study showed that the type, the grade and the concentration of additives could influence the physical stability such as flow, crystallinity and polymorphic transformation of paracetamol, the technological and biopharmaceutical properties of paracetamol. Stable polymorphic form of paracetamol with optimal tableting characteristics can be achieved through particle engineering.


Files in this item

Thumbnail
Name:
Publisher version

This item appears in the following Collection(s)

Show simple item record