Dissolution and mechanical behaviors of recrystallized carbamazepine from alcohol solution in the presence of additives

Nokhodchi, Ali; Bolourtchian, N.; Dinarvand, Rassoul

doi:10.1016/j.jcrysgro.2004.10.158

Cited by 45 publications

(35 citation statements)

References 23 publications

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“…The effect of mechanical stress can result in an increase in the intensity of free electrons at the particle surface thereby increasing the surface free energy of powders dramatically [35]. XRPD showed characteristic diffraction peaks for CBZ form III ( -form) at 2 of 10.5, 12.95 and 15.2 (Figure 5a) [36,37]. The XRPD pattern of the pure CBZ and the ground CBZ displayed similar diffraction patterns.…”

Section: Electrostatic Properties Of Physical Mixture and Solid Dispementioning

confidence: 92%

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

et al. 2016

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An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine, Powder Technology (2016Technology ( ), doi: 10.1016Technology ( /j.powtec.2016 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.A C C E P T E D M A N U S C R I P T AbstractOne of strategies adopted to improve the dissolution rates of poorly soluble drugs is by co-grinding the drug with a hydrophilic carrier. However, the introduction of mechanical forces during th e grinding process can lead to changes in the physicochemical characteristics as well as an increase in the surface free energy of the ground particles, which causes an alteration in the electrostatic properties of these particles. The solid state characteristics of glucosamine hydrochloride (GLU) and carbamazepine (CBZ) and their co-ground mixtures were studied using DSC, XRPD and SEM.These revealed that polymorphic transformations occurred due to the grinding process. The influence of grinding time on the triboelectrification properties of the formulations was also studied.Both pure CBZ and GLU powders were predominantly electro-positively charged and their charging properties increased with increasing grinding time. CBZ:GLU physical mixtures exhibited complicated bipolar charging behaviour, however, when subjected to grinding, these mixtures demonstrated mainly electronegative charge properties. The influence of both grinding time and CBZ content within CBZ:GLU mixtures were examined. The value of net-electronegative-charge density of CBZ:GLU mixtures was shown to increase with grinding time and /or when increasing the percentage proportion of CBZ up to 30 % w:w. This study helps to provide information about the handling of these formulation and gives a formulator tools to ascertain appropriate ratios for handling and possible simultaneous dissolution improvements.

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Section: Electrostatic Properties Of Physical Mixture and Solid Dispementioning

confidence: 92%

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

et al. 2016

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“…Namely, untreated and SAS CO 2 treated CBZ samples were investigated for changes in the particle size distribution, morphology and crystalline structure. According to the literature, CBZ is known to have at least four anhydrous polymorphic forms: triclinic form (Form I), trigonal form (Form II), monoclinic form (Form III), and C-centered monoclinic form (Form IV) (21,23,25). O'Brien et al gave a detailed analysis of the four anhydrate polymorphic forms (26).…”

Section: Sas Co 2 System Operation Proceduresmentioning

confidence: 99%

Self-built Supercritical CO2 Anti-solvent Unit Design, Construction and Operation using Carbamazepine

et al. 2008

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Abstract. The purpose of this study was to design and build a supercritical CO 2 anti-solvent (SAS) unit and use it to produce microparticles of the class II drug carbamazepine. The operation conditions of the constructed unit affected the carbamazepine yield. Optimal conditions were: organic solution flow rate of 0.15 mL/min, CO 2 flow rate of 7.5 mL/min, pressure of 4,200 psi, over 3,000 s and at 33°C. The drug solidstate characteristics, morphology and size distribution were examined before and after processing using X-ray powder diffraction and differential scanning calorimetry, scanning electron microscopy and laser diffraction particle size analysis, respectively. The in vitro dissolution of the treated particles was investigated and compared to that of untreated particles. Results revealed a change in the crystalline structure of carbamazepine with different polymorphs co-existing under various operation conditions. Scanning electron micrographs showed a change in the crystalline habit from the prismatic into bundled whiskers, fibers and filaments. The volume weighted diameter was reduced from 209 to 29 μm. Furthermore, the SAS CO 2 process yielded particles with significantly improved in vitro dissolution. Further research is needed to optimize the operation conditions of the self-built unit to maximize the production yield and produce a uniform polymorphic form of carbamazepine.

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“…The crystallization technique can change the habit-crystal form and particle size. The nature and extent of these changes depend on the crystallization conditions such as type of crystallization medium (2).…”

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confidence: 99%

“…The presence of small amounts of an effective additive in the crystallization medium can dramatically change the crystal size and shape. There are several reports of changing the crystal habit or polymorphism in the presence of impurities during crystallization of carbamazepine (2). The objective of this study was to achieve improved physicomechanical properties of carbamazepine powder through recrystallization from aqueous solutions at different pH values.…”

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Improvement of physicomechanical properties of carbamazepine by recrystallization at different pH values

et al. 2009

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The morphology of crystals has an appreciable impact role on the physicochemical properties of drugs. Drug properties such as flowability, dissolution, hardness and bioavailability may be affected by crystallinity behaviours of drugs. The objective of this study was to achieve an improved physicomechanical property of carbamazepine powder through recrystallization from aqueous solutions at different pH values. For this purpose, carbamazapine was recrystallized from aqueous solutions at different pH values (1, 7, 11). The morphology of crystals was investigated using scanning electron microscopy; X-ray powder diffraction (XRPD) was used to identify polymorphism; thermodynamic properties were analyzed using differential scanning calorimetery (DSC). Dissolution rate was determined using USP dissolution apparatus. Mechanical behavior of recrystallized carbamazepine powders was investigated by making tablets under different compaction pressure and measuring their hardness. SEM studies showed that the carbamazepine crystallization in different media affected the morphology and size of carbamazepine crystals. The shape of carbamazepine crystals changed from flaky or thin plate-like to needle shape. XRPD and DSC results ruled out any crystallinity changes occurring due to the temperature during recrystallization procedure or pH of crystallization media. The crushing strength of tablets indicated that all of the recrystallized carbamazepine samples had better compactiblity than the original carbamazepine powder. In vitro dissolution studies of carbamazepine samples showed a higher dissolution rate for carbamazepine crystals obtained from media with pH 11 and 1. Carbamazepine particles recrystallized from aqueous solutions of different pH values (all media) appeared to have superior mechanical properties to those of the original carbamazepine sample.

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Dissolution and mechanical behaviors of recrystallized carbamazepine from alcohol solution in the presence of additives

Cited by 45 publications

References 23 publications

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

An assessment of triboelectrification effects on co-ground solid dispersions of carbamazepine

Self-built Supercritical CO2 Anti-solvent Unit Design, Construction and Operation using Carbamazepine

Improvement of physicomechanical properties of carbamazepine by recrystallization at different pH values

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