Sintering of wax for controlling release from pellets

Singh, R.J.; Poddar, Sushilkumar S.; Chivate, Amit

doi:10.1208/pt0803074

Cited by 36 publications

(35 citation statements)

References 16 publications

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“…The prepared tablets were then subjected to thermal treatment by placing on aluminum foil and subjecting to sintering (3,8,13) at 80°C for 1, 2, and 3 h in hot air oven (Labhosp, Mumbai).…”

Section: Sintering Of Matrix Tabletsmentioning

confidence: 99%

Mechanistic Evaluation of the Effect of Sintering on Compritol® 888 ATO Matrices

Rao¹,

Ranpise²,

Borate³

et al. 2009

AAPS PharmSciTech

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Abstract. The present research studied the effect of sintering technique in the development of a controlled release formulation for ketorolac tromethamine. The method consisted of mixing drug and wax powder (Compritol® 888 ATO) along with lactose as diluent and talc as lubricant followed by direct compression at room temperature. The compressed fluffy matrices were kept at 80°C for 1, 2, and 3 h for sintering. The sintered tablets were characterized by their physical parameters and in vitro dissolution profile. The sintering time markedly affected the drug release properties of Compritol® 888 ATO matrices. It is notable that the release rate of ketorolac tromethamine from matrices was inversely related to the time of sintering. This may be due to the increase in the extent and firmness of sintering which further compacts the mass so that drug release is affected. Contact angle measurement and scanning electron microscopy analysis indicated that heat treatment caused the wax to melt and redistribute. This redistributed wax formed a network-like structure in which the drug along with lactose is entrapped. This particular formed matrix is responsible for retarding the drug release. Fourier transform infrared spectroscopy results did not show any drug-wax interaction due to sintering. Differential scanning calorimetric and powder X-ray diffraction studies ruled out the occurrence of solid solution and polymorphic changes of the drug. Drug release from the wax tablets with or without sintering was best described by the Higuchi equation.

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Section: Sintering Of Matrix Tabletsmentioning

confidence: 99%

Mechanistic Evaluation of the Effect of Sintering on Compritol® 888 ATO Matrices

Rao¹,

Ranpise²,

Borate³

et al. 2009

AAPS PharmSciTech

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“…In the procedure, 20 g of matrix granules were placed in the drum of an Erweka friabulator (Heusenstamm, Germany) rotating at 20 rev per min for 10 min. The matrix granules were then screened through a 60# sieve to remove the fines generated (Nasipuri and Omotosho, 1985;Eichie et al, 2005;Singh et al, 2007). Hence, the hardness-friability index was calculated using the equation below: %HFI = F A /F B ×10; where F A and F B are weights after and before friability determination respectively.…”

Section: Hardness-friability Index (Hfi)mentioning

confidence: 99%

“…This finding is in conformity with previous literature (Rao et al, 2001;Rao et al, 2003). The retardation in drug release on sintering may be due to softening of the wax particles during sintering and hence penetrated the empty spaces, forming a continuous layer around the drug particles in the matrix granules (Singh et al, 2007). This resulted in a decrease of the drug particles surface to the dissolution medium resulting in drug retardation from the matrix granules.…”

Section: Uhumwangho M U; Ramana Murthy K Vmentioning

confidence: 99%

Release Characteristics of Diltiazem Hydrochloride Wax-Matrix Granules – Thermal Sintering Effect

Uhumwangho¹,

Ramana²

2011

Journal of Applied Sciences and Environmental Management

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ABSTRACT:The aim of this study was to investigate the release characteristics of matrix (non-disintegrating) granules consisting of diltiazem hydrochloride (model drug) and glyceryl behenate (a wax matrix forming polymer) for sustained release application using sintering technique. The granules of diltiazem hydrochloride-wax matrix were prepared by melt granulation technique. This was formed by triturating the drug powder with a melted glyceryl behenate (drug: wax ratio, 3:1). The granules were subsequently sintered at 60 and 70 0 C for 1, 1.5 and 3h. The unsintered and sintered wax matrix granules of diltiazem hydrochloride were evaluated for physicochemical parameters and in vitro dissolution studies. The dissolution data were subjected to analysis using different mathematical models namely -zero order flux, first order, Higuchi square root of time, then Korsmeyer and Peppas model. Fourier-Transform Infrared Spectroscopy (FTIR) was carried out to investigate any chemical interactions between the drug and the added recipients before and after sintering. There was increased drug release retardation of diltiazem hydrochloride-wax matrix granules with sintering. The retardation depended on the temperature and duration of sintering. For instance, formulations sintered at 60 and 70°C for a period of 1.5h gave maximum release (m∞), time to attain maximum release (t∞) and dissolution rate (m∞/t∞) of 96. 1%, 95.2%, 5h, 9h, 19.2%h -1 and 10.6%h -1 respectively. The drug release was by Higuchi controlled diffusion mechanism and it followed Fickain diffusion mechanism (n<0.45). Sintering technique enhanced the extent of drug retardation from the systems studied. There was no chemical interaction between the model drug and the added recipients as shown in the FTIR studies. @JASEM

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“…After completing the test, the pellets were gently tapped on ASTM # 60 mesh to remove the powdered fines and the retained pellets were carefully collected and weight loss was measured. The HardnessFriability Index (%HFI) (Singh et al, 2007) was calculated using equation 1:…”

Section: Hardness-friability Indexmentioning

confidence: 99%

In vitro and in vivo evaluations of ketoprofen extended release pellets prepared using powder layering technique in a rotary centrifugal granulator

et al. 2011

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In the present study, an extended release pellet dosage form of ketoprofen was prepared using powder layering technique. A combination of ethyl cellulose (45 cps) and shellac polymers was used as a binder (12% w/w polymer) during drug layering and an extended release coating (1:3 ratio at 2%, 4% and 7% w/w polymer) within the same apparatus. The coated pellets were characterized for sphericity, Hardness-Friability Index, and drug content, and also underwent scanning electron microscopy. In vitro dissolution was performed in 900 mL of phosphate buffer (pH 6.8) using paddle apparatus at 100 rpm. Ethyl cellulose and shellac when used as binders during drug loading did not extend ketoprofen release beyond 3 h. However, coating of the drug loaded pellets using ethyl cellulose and shellac resulted in an extended release profile of about 10 h. Using Higuchi's model and the Korsmeyer equation, the drug release mechanism from the pellets was found to be an anomalous type involving diffusion and erosion. Scanning electron microscopy was used to visualize the pellet morphology and drug release mechanism during dissolution testing. In vivo evaluations of the extended release pellets in rats indicated a significant increase in the time to reach maximum concentration (t(max)) and extent of absorption (AUC(0-∞)) compared to the ketoprofen immediate release tablet blend dispersed and dosed. In conclusion, extended release pellets of ketoprofen could perform therapeutically better than conventional dosage forms, leading to improved efficacy for a prolonged period.

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Sintering of wax for controlling release from pellets

Cited by 36 publications

References 16 publications

Mechanistic Evaluation of the Effect of Sintering on Compritol® 888 ATO Matrices

Mechanistic Evaluation of the Effect of Sintering on Compritol® 888 ATO Matrices

Release Characteristics of Diltiazem Hydrochloride Wax-Matrix Granules – Thermal Sintering Effect

In vitro and in vivo evaluations of ketoprofen extended release pellets prepared using powder layering technique in a rotary centrifugal granulator

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