Effect of magnesium stearate or calcium stearate as additives on dissolution profiles of diltiazem hydrochloride from press-coated tablets with hydroxypropylmethylcellulose acetate succinate in the outer shell

Fukui, Eiji; Miyamura, Nobuteru; Kobayashi, Masao

doi:10.1016/s0378-5173(01)00580-4

Cited by 28 publications

(9 citation statements)

References 15 publications

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“…As can be seen in Fig. 2 increasing Magnesium stearate concentration decreases tensile strength of the tablets, as previous research has shown (Fukui et al 2001). This tensile strength decrement can be explained by reduction of inter-particulate bonding caused by formation of lubricant around carrier particles.…”

Section: Resultssupporting

confidence: 75%

Transparent computational intelligence models for pharmaceutical tableting process

Khalid

Tuszyński

Kazemi

et al. 2016

Complex Adapt Syst Model

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Purpose Pharmaceutical industry is tightly regulated owing to health concerns. Over the years, the use of computational intelligence (CI) tools has increased in pharmaceutical research and development, manufacturing, and quality control. Quality characteristics of tablets like tensile strength are important indicators of expected tablet performance. Predictive, yet transparent, CI models which can be analysed for insights into the formulation and development process. Methods This work uses data from a galenical tableting study and computational intelligence methods like decision trees, random forests, fuzzy systems, artificial neural networks, and symbolic regression to establish models for the outcome of tensile strength. Data was divided in training and test fold according to ten fold cross validation scheme and RMSE was used as an evaluation metric. Tree based ensembles and symbolic regression methods are presented as transparent models with extracted rules and mathematical formula, respectively, explaining the CI models in greater detail. Results CI models for tensile strength of tablets based on the formulation design and process parameters have been established. Best models exhibit normalized RMSE of 7 %. Rules from fuzzy systems and random forests are shown to increase transparency of CI models. A mathematical formula generated by symbolic regression is presented as a transparent model. Conclusions CI models explain the variation of tensile strength according to formulation and manufacturing process characteristics. CI models can be further analyzed to extract actionable knowledge making the artificial learning process more transparent and acceptable for use in pharmaceutical quality and safety domains.

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Section: Resultssupporting

confidence: 75%

Transparent computational intelligence models for pharmaceutical tableting process

Khalid

Tuszyński

Kazemi

et al. 2016

Complex Adapt Syst Model

View full text Add to dashboard Cite

show abstract

“…This mixture was stirred for 24 h to allow total release of the drug. After filtration through a 0.45 m filter membrane, the solution was assayed using ultraviolet (UV) spectrophotometry (Helios , Thermo ® , England) at a wavelength of 265 nm for diltiazem [20] and 264 nm for ibuprofen. The assay for drug content was performed in triplicate for each formulation.…”

Section: Drug Contentmentioning

confidence: 99%

Chitosan-Polycarbophil Complexes in Swellable Matrix Systems for Controlled Drug Release

Chen²,

Hamman³

2007

CDD

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A prerequisite for progress in the design of novel drug delivery systems is the development of excipients that are capable of fulfilling multifunctional roles such as controlling the release of the drug according to the therapeutic needs. Although several polymers have been utilised in the development of specialised drug delivery systems, their scope in dosage form design can be enlarged through combining different polymers. When a polymer is cross-linked or complexed with an oppositely charged polyelectrolyte, a three-dimensional network is formed in which the drug can be incorporated to control its release. The swelling properties and release kinetics of two model drugs with different water solubilities (i.e. diltiazem and ibuprofen) from monolithic matrix tablets consisting of an interpolyelectrolyte complex between chitosan and polycarbophil are reported. Matrix tablets consisting of this polymeric complex without drug or excipients exhibited extremely high swelling properties that are completely reversible upon drying. The drug release from matrix systems with different formulations depended on the concentration of the chitosan-polycarbophil interpolyelectrolyte complex and approached zero order release kinetics for both model drugs. The chitosan-polycarbophil interpolyelectrolyte complex has demonstrated a high potential as an excipient for the production of swellable matrix systems with controlled drug release properties.

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“…Consequently, this phenomenon is attributed to the coating effect of the drugs by the hydrophobic Precirol ATO 5, which leads to a drug-release delay from the microcapsules. 28 Therefore, the use of Precirol ATO 5 is useful for the sustained release behaviors of hydrophilic microcapsules.…”

Section: Resultsmentioning

confidence: 99%

Influence of glyceryl palmitostearate on release behaviors of hydroxypropyl cellulose microcapsules containing indomethacin by W/O emulsion

Kim

Park

2011

Macromol. Res.

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Hydrophilic hydroxypropyl cellulose (HPC) microcapsules containing the indomethacin model drug were prepared using the water in oil (W/O) emulsion method. The effect of hydrophobic glyceryl palmitostearate (Precirol ATO 5) on the release behavior as well as the drug loading and encapsulation efficiency of the indomethacin-loaded microcapsules was investigated as a function of the Precirol ATO 5 content. The microcapsules formed showed stable and spherical forms, whose particle sizes ranged from about 20 to 152 µm. X-ray diffraction analyses indicate that the indomethacin in the microcapsules was distributed in the form of molecular or very small crystals. The drug loading and encapsulation efficiency of the microcapsules slightly increased with increasing surfactant and Precirol ATO 5 content. In the dissolution test, pure HPC microcapsules showed rapid drug release, whereas HPC microcapsules containing Precirol ATO 5 showed a slower release rate. This behavior might be attributable to the hydrophobic Precirol ATO 5 coating on indomethacin, leading to the delayed effect on drug release in the medium.

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Effect of magnesium stearate or calcium stearate as additives on dissolution profiles of diltiazem hydrochloride from press-coated tablets with hydroxypropylmethylcellulose acetate succinate in the outer shell

Cited by 28 publications

References 15 publications

Transparent computational intelligence models for pharmaceutical tableting process

Transparent computational intelligence models for pharmaceutical tableting process

Chitosan-Polycarbophil Complexes in Swellable Matrix Systems for Controlled Drug Release

Influence of glyceryl palmitostearate on release behaviors of hydroxypropyl cellulose microcapsules containing indomethacin by W/O emulsion

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