An investigation into the effect of formulation variables and process parameters on characteristics of granules obtained by in situ fluidized hot melt granulation

Mašić, Ivana; Ilić, Ilija; Dreu, Rok; Ibrić, Svetlana; Parojčić, Jelena; Đurić, Zorica

doi:10.1016/j.ijpharm.2011.12.013

Cited by 25 publications

(18 citation statements)

References 40 publications

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“…For this granulation method, the drying step, which is required after wet granulation, is eliminated, hence the process time and energy requirements are significantly reduced. Since no liquids are used, HMG has the possibility to agglomerate moisture-sensitive materials [11,12].…”

Section: Introductionmentioning

confidence: 99%

Quantitative and qualitative use of thermal analysis for the investigation of the properties of granules during fluid bed melt granulation

Regdon

Korteby

2017

J Therm Anal Calorim

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This study describes a novel approach for the use of thermal analysis to study the aftermath of the fluid bed melt granulation process and to depict the growth mechanism of the granules by quantifying the enthalpies of the granules at every physicochemical change using DSC and their mass loss through TG coupled to MS for a qualitative determination of the composition and amount of the evolved gases for the corresponding fragment ion. The experiments were made in-situ with lactose monohydrate and two viscosity grades of PEG (2000 and 6000) as meltable binders with different contents and size fractions. DSC showed the presence of a beta lactose endotherm peak after the melting of alpha lactose and a proportional increase in its intensity with the increase of the particle size and the content of the binder, which suggested a relation with the agglomeration growth. Interestingly, TG and MS showed a larger reduction in the water content from lactose with the increase in the binder particle size, making it possible to evaluate the dehydration during the melt granulation. Indeed, during the distribution mechanism the low binder particle size and viscosity exposed lactose to a high heat transfer from the fluidizing air. However, a high binder particle size results in lactose immersed in the PEG particles, causing water to be trapped inside the granules and hence a larger reduction in water mass loss indicating the immersion mechanism. Therefore, thermal analysis is a promising tool for granulation growth control.

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Section: Introductionmentioning

confidence: 99%

Quantitative and qualitative use of thermal analysis for the investigation of the properties of granules during fluid bed melt granulation

Regdon

Korteby

2017

J Therm Anal Calorim

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“…Along with an optimal dissolution rate, taste masking is often an important objective in formulation development ( 33 , 43 , 196 , 197 ). This is usually evaluated in sensory studies with trained volunteers ( 33 , 198 – 200 ). Some studies also involve cats, which are sensitive to bitterness and scorn bitter food with insufficient taste masking ( 197 ).…”

Section: Characterization Methods Challenges and Controlling Strategmentioning

confidence: 99%

Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations

2015

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Lipid excipients are applied for numerous purposes such as taste masking, controlled release, improvement of swallowability and moisture protection. Several melting techniques have evolved in the last decades. Common examples are melt coating, melt granulation and melt extrusion. The required equipment ranges from ordinary glass beakers for lab scale up to large machines such as fluid bed coaters, spray dryers or extruders. This allows for upscaling to pilot or production scale. Solvent free melt processing provides a cost-effective, time-saving and eco-friendly method for the food and pharmaceutical industries. This review intends to give a critical overview of the published literature on experiences, formulations and challenges and to show possibilities for future developments in this promising field. Moreover, it should serve as a guide for selecting the best excipients and manufacturing techniques for the development of a product with specific properties using solvent free melt processing.

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“…Pri upotrebi veziva većeg viskoziteta, rast granula se može odvijati sporije i biti relativno ograničen. Afinitet veziva ka površini čestica praška može uticati na način formiranja i rast granula (26). Zhai i saradnici (27) su pokazali da se sa porastom kontaktnog ugla kapi otopljenog veziva na površini čvrstog materijala smanjuje obim aglomeracije, odnosno veličina aglomerata i njihova otpornost na habanje i lomljenje.…”

Section: Vrsta Sredstva Za Vezivanjeunclassified

“…Kukec i saradnici (59) su postigli poboljšanje u brzini i obimu rastvaranja karvedilola primenom granulacije topljenjem u mikseru/granulatoru velike brzine i uređaju tipa fluidizirajućeg sistema. Postupak granulacije topljenjem primenjen je za izradu granula, odnosno tableta sa trenutnim oslobađanjem paracetamola (14,26,30), kao i granula sa pH-zavisnim oslobađanjem paracetamola (60). Primenom hidrofobnih sredstava za vezivanje pri granulaciji topljenjem u mikseru/granulatoru velike brzine (16,61) ili uređaju tipa fluidizirajućeg sistema (6,26) moguće je postići produženo oslobađanje aktivne supstance na relativno jednostavan način.…”

Section: Primena Granulacije Topljenjemunclassified

“…Postupak granulacije topljenjem primenjen je za izradu granula, odnosno tableta sa trenutnim oslobađanjem paracetamola (14,26,30), kao i granula sa pH-zavisnim oslobađanjem paracetamola (60). Primenom hidrofobnih sredstava za vezivanje pri granulaciji topljenjem u mikseru/granulatoru velike brzine (16,61) ili uređaju tipa fluidizirajućeg sistema (6,26) moguće je postići produženo oslobađanje aktivne supstance na relativno jednostavan način. Literaturni podaci ukazuju na mogućnost primene ovog postupka uz upotrebu hidrofobnih sredstava za vezivanje za izradu flotirajućih granula/peleta sa produženim oslobađanjem (62)(63)(64).…”

Section: Primena Granulacije Topljenjemunclassified

See 1 more Smart Citation

Melt granulation as an alternative technique in solid dosage forms manufacture

Aleksić¹,

Djuriš²,

Cvijić³

et al. 2015

Arh farmaciju

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Konvencionalne metode granulacije pokazuju brojne nedostatke što je razlog za sve veće interesovanje i ulaganje u razvoj alternativnih metoda. Granulacija topljenjem predstavlja alternativnu metodu koja ima značajan potencijal za primenu u proizvodnji čvrstih farmaceutskih oblika. Podrazumeva primenu vezivnih sredstava koja imaju relativno nisku temperaturu topljenja (50 do 100°C), a čiji rastop omogućava aglomeraciju čestica praška. Kako rastvarač nije potreban, izbegava se faza sušenja, pa su broj procesnih koraka i troškovi smanjeni u odnosu na tradicionalni postupak vlažne granulacije. Postupak je pogodan za aktivne supstance podložne hidrolizi, a izborom odgovarajućeg vezivnog sredstva može se primeniti za izradu preparata sa modifikovanim ili trenutnim oslobađanjem, uz poboljšanje bioraspoloživosti slabo rastvorljivih aktivnih supstanci, kao i u cilju maskiranja gorkog ukusa. Granulacija topljenjem se može izvoditi u uređajima koji se uobičajeno koriste za vlažnu granulaciju, kao što su mikseri/granulatori velike brzine, uređaji tipa fluidizirajućeg sistema, ekstruderi. Brojni faktori formulacije, procesni parametari, kao i faktori vezani za dizajn i vrstu opreme mogu uticati na mehanizam aglomeracije i karakteristike dobijenih granula. Dobro kontrolisan postupak granulacije topljenjem podrazumeva podrobno poznavanje i razumevanje uticaja ovih faktora, zbog čega ova oblast i dalje zahteva intenzivan, a često i multidisciplinarni istraživački rad.

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An investigation into the effect of formulation variables and process parameters on characteristics of granules obtained by in situ fluidized hot melt granulation

Cited by 25 publications

References 40 publications

Quantitative and qualitative use of thermal analysis for the investigation of the properties of granules during fluid bed melt granulation

Quantitative and qualitative use of thermal analysis for the investigation of the properties of granules during fluid bed melt granulation

Solvent-Free Melting Techniques for the Preparation of Lipid-Based Solid Oral Formulations

Melt granulation as an alternative technique in solid dosage forms manufacture

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