Minitabletting: improving the compactability of paracetamol powder mixtures

Lennartz, Peter; Mielck, Jobst B.

doi:10.1016/s0378-5173(98)00206-3

Cited by 104 publications

(53 citation statements)

References 21 publications

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“…In contrast, minitablets (Thomson et al, 2009, Stoltenberg and, pellets (Kayumba et al, 2007) and granules (Mambrini and Kibleur, 2013) may be preferred alternatives when formulating new dosage forms for children providing the required drug stability, and dose accuracy as well as flexibility. Some children seem to prefer uncoated tablets to suspensions, syrups or powders (van Riet-Nales et al, 2013) but the age at which they are able to swell minitablets (2-3 mm diameter (Lennartz and Mielck, 1998)) remains undetermined and probably varies with the individual. Recent studies showed that round uncoated tablets are well accepted by 1 to 4 year old children (van Riet-Nales et al, 2013), while others deemed their usage safe in children as young as 2 years old (Thomson et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the ability of powdered milk to produce minitablets containing paracetamol for the paediatric population

Pinto

Brachkova

Fernandes

et al. 2016

Chemical Engineering Research and Design

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The work aims at evaluating the usefulness of powdered milk as a drug matrix for the production of minitablets specifically designed for children. Mixtures made of powdered milk, paracetamol, mannitol, sodium croscarmellose and magnesium stearate (evaluated for flow properties, cohesiveness and caking tendency) were compacted into beams (evaluated for deformation, elasticity and stiffness) and minitablets (evaluated for uniformity of mass, thickness, tensile strength and paracetamol mean dissolution time) and a 2 3 factorial design performed. The increase on milk fraction in the formulation improved the compressibility of paracetamol and hardness of compacts, reducing weight variation and paracetamol release. A marked decrease on the dissolution time was observed as sodium croscarmellose was added to the milk rich formulations. The increase of the compression force resulted in the production of thinner compacts but had little effect on dissolution time. The production of beams has shown that deformation, bending strength and stiffness increased with both milk and compaction pressure, and decreased with sodium croscarmellose, whereas elasticity decreased when all variables increased. Tensile strength and mean dissolution time described minitablets well, unlike compaction force. The study has proved that powdered milk is suitable for the production of minitablets by direct compression of poor compressible drugs. Highlights-Powdered milk can be used as a matrix to deliver poorly compressible drugs.-Minitablets can be produced by direct compression of drug and powdered milk.-Materials' behaviour is different as powders, compacts or tablets.-The complexity of milk materials justifies unexpected outcomes for compacts and tablets.-Mean drug dissolution time was the most sensitive parameter to assess tablets' performance.

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Section: Introductionmentioning

confidence: 99%

Evaluation of the ability of powdered milk to produce minitablets containing paracetamol for the paediatric population

Pinto

Brachkova

Fernandes

et al. 2016

Chemical Engineering Research and Design

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“…To achieve swallowing appropriateness and uniform unit dose strength, mini-tablet is a suitable candidate. Minitablet is defined as a tablet with a diameter less than 3 mm (20). A recent study conducted by Thomson et al illustrated that out of 100 preschoolers, no one suffered the potential of choke caused by swallowing placebo mini-tablets and up to 86% of 5-year-old children swallowed mini-tablets successfully (21).…”

Section: Introductionmentioning

confidence: 99%

Development of a Mini-Tablet of Co-Grinded Prednisone–Neusilin Complex for Pediatric Use

et al. 2013

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Abstract. The purpose of this study is to enhance the dissolution rate of prednisone by co-grinding with Neusilin to form a complex that can be incorporated into a mini-tablet formulation for pediatrics. Prednisone-Neusilin complex was co-grinded at various ratios (1:1, 1:3, 1:5, and 1:7). The physicochemical properties of the complex were characterized by various analytical techniques including: differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), scanning electron microscope (SEM), particle size, surface area, solubility, and dissolution rate. The co-grinded prednisone-Neusilin complex (1:7) was blended with other excipients and was formulated into a 2-mm diameter mini-tablet. The minitablets were further evaluated for thickness, weight, content uniformity, and dissolution rate. To improve taste masking and stability, mini-tablets were coated by dip coating with Eudragit® EPO solution. DSC and XRPD results showed that prednisone was transformed from crystalline state into amorphous state after co-grinding with Neusilin. Particle size, surface area, and SEM results confirmed that prednisone was adsorbed to Neusilin's surface. Co-grinded prednisone-Neusilin complex (1:7) had a solubility of 0.24 mg/ mL and 90% dissolved within 20 min as compared to crystalline prednisone which had a solubility of 0.117 mg/mL and 30% dissolved within 20 min. The mini-tablets containing co-grinded prednisoneNeusilin complex (1:7) exhibited acceptable physicochemical and mechanical properties including dissolution rate enhancement. These mini-tablets were successfully dip coated in Eudragit® EPO solution to mask the taste of the drug during swallowing. This work illustrates the potential use of co-grinded prednisone-Neusilin to enhance solubility and dissolution rate as well as incorporation into a mini-tablet formulation for pediatric use.

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“…Minitablets are tablets with a diameter equal to or smaller than 2-3 mm (Lennartz & Mielck, 1998). As multiple-unit dosage forms, the minitablets present several advantages over conventional single-unit dosage forms, such as dose flexibility, high degree of dispersion in the gastrointestinal tract, and thus minimizing irritation due to high local drug concentrations, reproducible bioavailability (Graffner et al, 1986) and uniform plasma levels.…”

Section: Introductionmentioning

confidence: 99%

Preparation of multiple-unit floating-bioadhesive cooperative minitablets for improving the oral bioavailability of famotidine in rats

Zhu

et al. 2014

Drug Delivery

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The aims of this study were to prepare fine famotidine-containing floating-bioadhesive cooperative minitablets and to investigate the possibility of using those minitablets as a delivery system for promoting the oral bioavailability of famotidine. Nine minitablet formulations were designed using hydroxypropylmethylcellulose (HPMC K4M) as releaseretarding polymers, Carbopol 971P as bioadhesive materials and sodium bicarbonate (NaHCO 3 ) as gas formers. The prepared 3 ± 0.02 mm minitablets were evaluated in terms of their swelling ability, floating behavior, bioadhesion test and in vitro release. The optimized minitablets (F6) containing HPMC K4M (50.00%, w/w), Carbopol 971P (10.00%, w/w) and NaHCO 3 (10.00%, w/w) were found to float in 1 min and remain lastingly buoyant over a period of 8 h in vitro, with excellent bioadhesive properties (20.81 g) and sustained drug release characteristics (T 50% ¼ 46.54%) followed one-order model. In addition, plasma concentration-time profiles from pharmacokinetic studies in rats dosed with minitablets showed 1.62-fold (p50.05) increased absorption of famotidine, compared to the market tablets XinFaDing Õ . These studies demonstrated that the multiple-unit floating-bioadhesive cooperative minitablets may be a promising gastro-retentive delivery system for drugs that play a therapeutic role in the stomach.

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Minitabletting: improving the compactability of paracetamol powder mixtures

Cited by 104 publications

References 21 publications

Evaluation of the ability of powdered milk to produce minitablets containing paracetamol for the paediatric population

Evaluation of the ability of powdered milk to produce minitablets containing paracetamol for the paediatric population

Development of a Mini-Tablet of Co-Grinded Prednisone–Neusilin Complex for Pediatric Use

Preparation of multiple-unit floating-bioadhesive cooperative minitablets for improving the oral bioavailability of famotidine in rats

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