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Drug Dev Ind Pharm. 2012 Sep;38(9):1068-76. doi: 10.3109/03639045.2011.638302. Epub 2011 Dec 10.

Development and evaluation of sustained-release Compritol® 888 ATO matrix mini-tablets.

Author information

1
School of Pharmacy & Biomolecular Sciences, Liverpool John Moores University, Liverpool, UK. m.roberts1@ljmu.ac.uk

Abstract

CONTEXT:

Sustained-release mini-tablets are a potentially suitable for paediatric drug delivery or as multi-particulate dosage forms.

OBJECTIVE:

To evaluate the potential for developing lipophilic matrix mini-tablets and to assess the effects of Compritol® 888 ATO concentration on drug release from differently sized mini-tablets prepared by direct compression.

METHODS:

A formulation comprising theophylline as a model soluble drug, 15% w/w Compritol® 888 ATO as the inert matrix-forming agent, with dibasic dicalcium phosphate anhydrous and lactose as diluents was evaluated by producing 12 mm tablets at a range of compression speeds and forces. The same formulation and further formulations with 25, 35 or 45% w/w Compritol® 888 ATO were evaluated by producing 2, 3 and 4 mm mini-tablets.

RESULTS AND DISCUSSION:

Drug release from matrix tablets was sustained over a period of 12 hours and release rate varied according to the compression force and speed employed. The rate of drug release from matrix mini-tablets was more rapid and increasing Compritol® 888 ATO concentration resulted in slower release rates. The rate of drug release from matrix mini-tablets was inversely proportional to mini-tablet size (2 mm > 3 mm > 4 mm). Drug release from the matrix tablets and mini-tablets followed square-root of time kinetics.

CONCLUSION:

Tailored drug release from matrix mini-tablets may achieved by altering the size of mini-tablet or level of Compritol® 888 ATO in the formulation and this may have potential in the development of paediatric formulations or multi-particulate dosage forms.

PMID:
22149472
DOI:
10.3109/03639045.2011.638302
[Indexed for MEDLINE]

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