An approach to engineer paracetamol crystals by antisolvent crystallization technique in presence of various additives for direct compression.

2.50
Hdl Handle:
http://hdl.handle.net/2436/620513
Title:
An approach to engineer paracetamol crystals by antisolvent crystallization technique in presence of various additives for direct compression.
Authors:
Kaialy, Waseem; Larhrib, Hassan; Chikwanha, Brian; Shojaee, Saeed; Nokhodchi, Ali
Abstract:
Paracetamol 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.
Citation:
An 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
Journal:
International journal of pharmaceutics
Issue Date:
10-Apr-2014
URI:
http://hdl.handle.net/2436/620513
DOI:
10.1016/j.ijpharm.2014.01.026
PubMed ID:
24480534
Type:
Article
Language:
en
ISSN:
1873-3476
Appears in Collections:
FSE

Full metadata record

DC FieldValue Language
dc.contributor.authorKaialy, Waseemen
dc.contributor.authorLarhrib, Hassanen
dc.contributor.authorChikwanha, Brianen
dc.contributor.authorShojaee, Saeeden
dc.contributor.authorNokhodchi, Alien
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 Pharmen
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.en
dc.language.isoenen
dc.rightsArchived with thanks to International journal of pharmaceuticsen
dc.subjectParticle engineeringen
dc.subjectAntisolvent crystallization;en
dc.subjectParacetamol; Additivesen
dc.subjectCompactibility;en
dc.subjectCrystal habiten
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.en
dc.typeArticleen
dc.identifier.journalInternational journal of pharmaceuticsen

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