Effect of process variables on physicomechanical properties of the agglomerates obtained by spherical crystallization technique

Maghsoodi, Maryam

doi:10.3109/10837450.2010.492218

Cited by 15 publications

(18 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The bulk and tapped densities of the spherical agglomerates were lower than the corresponding value of the pure sample due to higher particle size and sphericiy. The lower density is likely to be related to the intraparticle porosity and hence the reduction in bulk density of the treated samples indicates a greater porosity within the agglomerated particles; similar finding were observed by Maghsoodi 30 and Gupta et al 41 CI for agglomerates was found to be lower when compared with the pure drug. This may be due to the formation of agglomerates.…”

Section: Micromeritic Propertiessupporting

confidence: 79%

“…This may be due to the formation of agglomerates. Fine particles with high surface to mass ratios are more cohesive than coarser particles, hence more influenced by gravitational force; similar findings were observed by Kumar et al 33 and Viswanathan et al 34 Decreased values of CI for agglomerates have better packability, indicating that they might be suitable for direct tabletting; similar findings were observed by Maghsoodi 30 and Gupta et al 41 The flow properties of the crystals were reflected by the angle of repose. It was found that the angle of repose of the agglomerates was decreased when compared with pure ibuprofen.…”

Section: Micromeritic Propertiessupporting

confidence: 74%

“…The dissolution medium used was 900 mL of gastric simulating fluid without enzymes (pH 1.2). Five milliliters of sample solution were withdrawn at predetermined time intervals (10,20,30,40,50, and 60 min) and then filtered through Whatman filter paper No: 40 and the same amount was replaced in the dissolution flask to maintain sink conditions. The amount of dissolved ibuprofen was analyzed spectrophotometrically at 221 nm.…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

See 2 more Smart Citations

Preparation and in vitro evaluation of ibuprofen spherical agglomerates

Nagaraju

Penjuri

Saritha³

et al. 2018

tjps

View full text Add to dashboard Cite

Bir anti-inflamatuvar ilaç olan ibuprofen, zayıf suda çözünürlüğü ile karakterize olup, farmakolojik etkileri sınırlar. Bu çalışmada aglomerasyonun mikromeritik özellikler ve çözünme üzerindeki etkilerinin incelenmesi amaçlanmıştır. Gereç ve Yöntemler: İbuprofen aglomeraları, su, diklorometan ve zayıf solvent olarak sırasıyla 57.5:12.5:30 oranında sıvı ve iyi çözücü köprü halindeki dimetil sülfoksit kullanılarak çözücü değiştirme yöntemi ile hazırlandı. Köprü sıvısı miktarı, ilave modu, sıcaklık ve karıştırma oranı gibi proses değişkenleri optimize edildi. Bulgular: Taramalı elektron mikroskobu çalışmaları, üretilen aglomeraların küresel olduğunu ve düzensiz şekli olduğunu göstermektedir. X-Işın Pudrası Difraksiyon spektrumu polimorfizm yokluğunu ortaya koydu. Diferansiyel tarama kalorimetrisi spektrumu, erime noktasında kristal modifikasyonun yokluğunu gösteren herhangi bir değişiklik göstermedi. Aglomeralar, saf ilaca kıyasla gelişmiş çözünürlük, çözünme hızı ve mikromeritik özellikler sergiledi. Sonuç: Anti-inflamatuvar çalışmalar Wistar suşu erkek albino sıçanlarında yürütülmüş ve ibuprofen aglomeraları saf ilaca göre daha iyi bir absorpsiyona bağlı olarak daha belirgin bir aktivite gösterdi. Saf ibuprofen ve aglomera için ülserojenik potansiyel çalışması gerçekleştirildi. İbuprofen aglomeraları ile tedavi edilen sıçanlarda daha iyi ülserojenik potansiyel gözlenmiştir. Anahtar kelimeler: İbuprofen, küresel toplanma, anti-inflamatuvar aktivite, ülserojenik potansiyel Objectives: Ibuprofen, an anti-inflammatory drug, is characterized by poor water solubility, which limits its pharmacologic effects. The present work aimed to the study the effect of agglomeration on the micromeritic properties and dissolution of ibuprofen. Materials and Methods: Ibuprofen agglomerates were prepared by solvent change method using water, dichloromethane and DMSO as poor solvent, bridging liquid and good solvent respectively in the ratio of 57.5:12.5:30. Process variables such as amount of bridging liquid, mode of addition, temperature and stirring rate were optimized. Results: SEM studies indicate that agglomerates produced were spherical and exhibit irregular shape. X-Ray Powder Diffraction spectra revealed the absence of polymorphism. DSC spectra showed no change in melting point indicating absence of crystal modification. The agglomerates exhibited improved solubility, dissolution rate and micromeritic properties compared to pure drug. Conclusion: Anti-inflammatory studies were conducted in Wistar strain male albino rats and ibuprofen agglomerates showed more significant activity than the pure drug which may be due to better absorption. Ulcerogenic potential study was carried out for pure ibuprofen and agglomerates. Better ulcerogenic potential was observed in ibuprofen agglomerates treated rats.

show abstract

Section: Micromeritic Propertiessupporting

confidence: 79%

Section: Micromeritic Propertiessupporting

confidence: 74%

Section: In Vitro Dissolution Studiesmentioning

confidence: 99%

See 1 more Smart Citation

Preparation and in vitro evaluation of ibuprofen spherical agglomerates

Nagaraju

Penjuri

Saritha³

et al. 2018

tjps

View full text Add to dashboard Cite

show abstract

“…There has also been a wide range of studies on the physiochemical, mechanical, and micromeritic properties of the spherical agglomerates to assess the possibility of direct tableting of the agglomerates. [17][18][19][20][21][22][23][24] However, none of the aforementioned studies looked into the interplay between the operating conditions and the trade-off between the size distribution and properties of spherical agglomerates and the size distribution of constituting internal crystals. In almost all previous spherical crystallization systems, crystallization and 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 60 7 agglomeration occurred simultaneously; offering little or no control in tailoring the internal crystal size versus external agglomerate size.…”

Section: Introductionmentioning

confidence: 98%

Process Intensification through Continuous Spherical Crystallization Using a Two-Stage Mixed Suspension Mixed Product Removal (MSMPR) System

Peña

Nagy

2015

Crystal Growth & Design

View full text Add to dashboard Cite

Of utmost importance in the crystallization of active pharmaceutical ingredients (APIs) in the pharmaceutical industry is to produce crystals of good physical, processing, and biopharmaceutical properties. The definition of good physical properties depends on what the end goal and the drug formulation that the crystals will be a part of, but often processing and biopharmaceutical properties are competing interests. In most cases, the crystallization process is tailored to improve downstream process efficiency rather than improve drug molecule efficacy in the human body. Herein a novel concept and method to help satisfy both processing and biopharmaceutical interests is proposed, which is based on performing crystallization and spherical agglomeration in a two-stage continuous mixed suspension mixed product removal (MSMPR) system. With the suitable operating mode, the system enables to decouple the nucleation and growth from the agglomeration mechanisms, while performing efficient continuous manufacturing of particles with desired properties. Decoupling will offer more degrees of freedom for the control of each mechanism. This in turn provides the means by which properties in the nucleation/growth stage can be tailored to those of most biopharmaceutical benefit and efficacy (e.g. bioavailability, dissolution, morphology) while allowing the agglomeration stage to be tailored to produce spherical agglomerates of the most processing efficiency (e.g. filtering, drying, friability).

show abstract

“…Zhang and coworkers have recently reported that the mean particle size of cefotaxime sodium spherical agglomerates increased with an increase of the poor solvent chloroform content in the crystallization system, and at the same time the particle size distribution became narrower, which can be ascribed to higher supersaturation and more effective crystallization and agglomeration (31). In that study, the temperature and agitation speed had no notable impact on the agglomerated particle size, while in another study (34) higher temperature resulted in smaller particle size and increased density of agglomerated carbamazepine.…”

Section: Spherical Agglomerationmentioning

confidence: 81%

Spherical crystallization of drugs

Kovačič¹,

Vrečer²,

Planinšek³

2012

Acta Pharmaceutica

View full text Add to dashboard Cite

The solid state properties of pharmaceutical compounds have a decisive impact on dosage form development, stability, and in vivo performance of the drug. Many pharmaceutical drugs are problematic per se due to their inappropriate physical and mechanical properties and poor aqueous solubility. The micromeritic properties of drug particles, such as shape and size, are of essential importance for the formulation of solid high--dose units (1). The particle size of poorly soluble drugs is always an issue due to its impact on dissolution properties. Micronized drug particles (smaller than 10 mm) have a large specific area and provide a way to improve the dissolution rate (2), but high energy input during the micronization process gives rise to increased free surface energy, electrostatic tendencies, and thus poor flowability and/or compressibility of powders and low bulk density (3), which makes them difficult to use in downstream processing in the pharmaceutical industry such as direct tablet-making or capsule-filling processes. In addition, micronized drug substances tend to agglomerate and the increase in surface area is not always reflected in improved dissolution (4). Spherical crystallization of drugs is the process of obtaining larger particles by agglomeration during crystallization. The most common techniques used to obtain such particles are spherical agglomeration and quasi-emulsion solvent diffusion. Ammonia diffusion systems and crystallo-co-agglomeration are extensions of these techniques. By controlling process parameters during crystallization, such as temperature, stirring rate, type and amount of solvents, or excipient selection, it is possible to control the formation of agglomerates and obtain spherical particles of the desired size, porosity, or hardness. Researchers have reported that the particles produced have improved micromeritic, physical, and mechanical properties, which make them suitable for direct compression. In some cases, when additional excipients are incorporated during spherical crystallization, biopharmaceutical parameters including the bioavailability of drugs can also be tailored.

show abstract

Effect of process variables on physicomechanical properties of the agglomerates obtained by spherical crystallization technique

Cited by 15 publications

References 23 publications

Preparation and in vitro evaluation of ibuprofen spherical agglomerates

Preparation and in vitro evaluation of ibuprofen spherical agglomerates

Process Intensification through Continuous Spherical Crystallization Using a Two-Stage Mixed Suspension Mixed Product Removal (MSMPR) System

Spherical crystallization of drugs

Contact Info

Product

Resources

About