The influence of antitack additives on drug release from film-coated granules

Wan, Lucy S.C.; Lai, W.F.

doi:10.1016/0378-5173(93)90007-3

Cited by 10 publications

(5 citation statements)

References 17 publications

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“…At high levels of talc, the matrix would consist primarily of talc and polymer latex. As the particle size of the polymer latex is much smaller than that of talc, consequently talc at higher levels would form the skeleton of the drug-layered matrix (12,20), thereby creating a diffusing barrier to verapamil HCL. …”

Section: Effect Of Talc Powdermentioning

confidence: 99%

“…This is accomplished during the coating process as a result of water evaporation, which generates surface tension effects and capillary forces among polymer particles (11). The slow rate of water evaporation coupled with its high latent heat of vaporization, however, is also responsible for the tackiness problems experienced with these systems (12). Therefore, talc powder has been frequently used as an inert anti-tacking agent in aqueous-based acrylic colloidal dispersions when coating either single unit dosage forms (tablets) or multiparticulate units (3,11,13).…”

Section: Introductionmentioning

confidence: 99%

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Effect of Eudragit® RS 30D and Talc Powder on Verapamil Hydrochloride Release from Beads Coated with Drug Layered Matrices

El-Malah

Nazzal

2008

AAPS PharmSciTech

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Abstract. The aim of this study was to investigate the effect of Eudragit ® RS 30D, talc, and verapamil hydrochloride on dissolution and mechanical properties of beads coated with "drug-layered matrices". This was accomplished with the aid of a three-factor multiple-level factorial design using percent drug release in 1 and 2 h, T 50 , tensile strength, brittleness, stiffness and toughness as the responses. Beads were coated in a fluidized-bed coating unit. Surface morphology and mechanical properties were evaluated by surface profilometry and texture analysis, respectively. No cracks, flaws and fissures were observed on the surfaces. The mechanical properties were dependent on the talc/polymer ratio. The release of verapamil from the beads was influenced by matrix components. Increasing the level of both talc and Eudragit decreased the percent drug released from 67% to 4.8% and from 80.7% to 6.7% in 1 and 2 h, respectively, and increased T 50 from 0.8 to 25.7 h. It was concluded that beads could be efficiently coated with "drug-layered matrices". The release of drug, however, depends on a balance between the levels of drug, talc, and polymer, whereby desired dissolution and mechanical properties could be controlled by the talc/polymer ratio and the level of drug loading.

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Section: Effect Of Talc Powdermentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Effect of Eudragit® RS 30D and Talc Powder on Verapamil Hydrochloride Release from Beads Coated with Drug Layered Matrices

El-Malah

Nazzal

2008

AAPS PharmSciTech

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“…This tackiness can create a tremendous handling problem as the coated substrates stick to each other as well as to the wall of the coating chamber. It also increases number of coating defects and impairs the yield and quality of the coated batch (12)(13)(14)(15)(16)(17)(18)(19). In case of the effervescent floating tablets, irreversible agglomeration of the tablets could damage the gas-entrapped membrane when the tablets were separated.…”

Section: Introductionmentioning

confidence: 99%

“…However, the drawback of using high amount of talc in the coating formulation includes sedimentation in the spray lines and clogging spray nozzles during coating (16). Other anti-tacking agents that have been used to reduce the tackiness of polymeric film coating formulations include glyceryl monostearate (GMS) (10,11), magnesium stearate (13,14), and silicon dioxide (16,17). Wesselling et al (10) and Petereit et al (21) reported the overcoming tackiness problem of aqueous acrylic polymer film.…”

Section: Introductionmentioning

confidence: 99%

Impact of Anti-tacking Agents on Properties of Gas-Entrapped Membrane and Effervescent Floating Tablets

et al. 2014

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Tackiness caused by the gas-entrapped membrane (Eudragit(®)RL 30D) was usually observed during storage of the effervescent floating tablets, leading to failure in floatation and sustained release. In this work, common anti-tacking agents (glyceryl monostearate (GMS) and talc) were used to solve this tackiness problem. The impact of anti-tacking agent on the properties of free films and corresponding floating tablets was investigated. GMS was more effective than talc in reducing tackiness of the film. Addition and increasing amount of anti-tacking agents lowered the film mechanical strength, but the coating films were still strong and flexible enough to resist the generated gas pressure inside the floating tablet. Wettability and water vapor permeability of the film decreased with increasing level of anti-tacking agents as a result of their hydrophobicity. No interaction between anti-tacking agents and polymer was observed as confirmed by Fourier transform infrared spectroscopy, powder X-ray diffractometry, and differential scanning calorimetry studies. Increasing amount of anti-tacking agents decreased time to float and tended to retard drug release of the floating tablets. Floating properties and drug release were also influenced by type of anti-tacking agents. The obtained floating tablets still possessed good floating properties and controlled drug release even though anti-tacking agent had some effects. The results demonstrated that the tackiness problem of the floating tablets could be solved by incorporating anti-tacking agent into the gas-entrapped membrane.

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“…Therefore, anti-tacking agents, such as simethicone, talc, and magnesium stearate, are usually added in polymer solutions in order to prevent agglomeration (37,38). However, the additives might modify drug release from the coated pellets in terms of the swelling behavior of the coated pellets in water and the potential additive-polymer interactions (39,40).…”

Section: Effect Of Pore Former Types On Coating Process (Hpc Vs Ms)mentioning

confidence: 99%

Model Drug as Pore Former for Controlled Release of Water-Soluble Metoprolol Succinate from Ethylcellulose-Coated Pellets Without Lag Phase: Opportunities and Challenges

Wang¹,

Dai²,

Chang

et al. 2014

AAPS PharmSciTech

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Abstract. The objective of the present study was to evaluate the feasibility of using model drug metoprolol succinate (MS) as a pore former to modify the initial lag phase (i.e., a slow or non-release phase in the first 1-2 h) associated with the drug release from coated pellets. MS-layered cores with high drug-layering efficiency (97% w/w) were first prepared by spraying a highly concentrated drug aqueous solution (60% w/w, 70°C) on non-pareils without using other binders. The presence of MS in ethylcellulose (EC) coating solution significantly improved the coating process by reducing pellets sticking, which often occurs during organic coating. There may be a maximum physical compatibility of MS with EC, and the physical state of the drug in the functional coating layer of EC/MS (80:20) was simultaneously crystalline and noncrystalline (amorphous or solid molecule solution). The lag phase associated with hydroxypropylcellulose (HPC) as a pore former was not observed when MS was used as a pore former. The drug release from EC/ MS-coated pellets was pH independent, inversely proportional to the coating levels, and directly related to the pore former levels. The functional coating layer with MS as a pore former was not completely stabilized without curing. Curing at 60°C for 1 day could substantially improve the stability of EC/MScoated pellets. The physical state of the drug in the free film of EC/MS (85:15) changed partially from amorphous to crystal when cured at 60°C for 1 day, which should be attributed to the incompatibility of the drug with EC.

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The influence of antitack additives on drug release from film-coated granules

Cited by 10 publications

References 17 publications

Effect of Eudragit® RS 30D and Talc Powder on Verapamil Hydrochloride Release from Beads Coated with Drug Layered Matrices

Effect of Eudragit® RS 30D and Talc Powder on Verapamil Hydrochloride Release from Beads Coated with Drug Layered Matrices

Impact of Anti-tacking Agents on Properties of Gas-Entrapped Membrane and Effervescent Floating Tablets

Model Drug as Pore Former for Controlled Release of Water-Soluble Metoprolol Succinate from Ethylcellulose-Coated Pellets Without Lag Phase: Opportunities and Challenges

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