PubMed · 13610705
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F C BLUBAUGH, J R ZAPAPAS, M C SPARKS. 1958. An enteric compression coating. I. In vitro studies.. https://pubmed.ncbi.nlm.nih.gov/13610705/
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Effects of micromeritic properties (bulk, tapped and particle density, particle size and shape) on the flow rate through circular orifices are investigated, for three pharmaceutical excipients (Lactose, Emcompress and Starch) separated in four sieve fractions, and are modeled with the help of artificial neural networks (ANNs). Eight variables were selected as inputs and correlated by applying the Spearman product-moment correlation matrix and the visual component planes of trained Self-Organizing Maps (SOMs). Back-propagation feed-forward ANN with six hidden units in a single hidden layer was selected for modeling experimental data and its predictions were compared with those of the flow equation proposed by. It was found that SOMs are efficient for the identification of co-linearity in the input variables and the ANN is superior to the flow equation since it does not require separate regression for each excipient and its predictive ability is higher. Besides the orifice diameter, most influential and important variable was the difference between tapped and bulk density. From the pruned ANN an approximate non-linear model was extracted, which describes powder flow rate in terms of the four network's input variables of the greatest predictive importance or saliency (difference between tapped and bulk density (x(2)), orifice diameter (x(3)), circle equivalent particle diameter (x(4)) and particle density [equation in text].
PURPOSE: To study the effects of two lipid excipients, Peceol and Gelucire 44/14 on the in vitro pancreatic lipase activity. METHODS: A 50 microL reaction mixture, consisting of 45 microL (3H) triolein as the radiolabeled substrate, 2.5 microL Peceol or Gelucire 44/14 (0.05-0.5%), either alone or in combination, 2.5 microL colipase (100 microg/mL), and 2.5 microL pancreatic lipase (1 mg/mL), was incubated for 10 min at room temperature. At the end of incubation, the reaction was stopped by the addition of an extraction solvent containing chloroform, methanol, and n-heptane (12.5:14:10), and the mixture vortexed briefly. Subsequently, 250 microL of 50 mM sodium carbonate was added and the aqueous and organic phase separated by centrifugation for 5 min at 1000 g. One hundred microliters of the supernatant was transferred to a scintillation counter and then radioactivity measured after the addition of 3.6 mL of scintillation fluid. Pancreatic lipase activity was determined by measuring the amount of free fatty acid released into the incubation medium and expressed as micromol free fatty acid released/min. RESULTS: When used alone, Peceol inhibited the pancreatic lipase activity significantly in a concentration-dependent manner, with a maximum inhibition of 57% at 0.4% of the excipient [p < 0.05, one-way analysis of variance (ANOVA)]. Similarly, Gelucire 44/14 alone caused inhibition of lipase activity in a concentration-dependent manner. However, the maximum inhibition (30%) was smaller in magnitude compared with the former agent. When the two excipients were used in combination, the inhibitory effects on the enzyme activity were similar to those observed with the individual agents (p < 0.05, one-way ANOVA). However, the maximum inhibition of 30% was lower than that observed with Peceol alone. CONCLUSIONS: The results from this study suggest that these lipid excipients inhibit in vitro pancreatic lipase activity and should be taken into consideration when developing oral formulations using these agents.
Talc is widely used as a glidant (flow regulator) for powders. This study highlights the characteristics that confer to talcs new end use properties in improving the lubrication function during compression. We studied the contribution of texture, mean diameter (D50), and specific surface area on the residual die pressure, the ejection pressure, the lubrication index, and the tablet hardness. Different textures were studied: microcrystalline, macrocrystalline, and moderately macrocrystalline talc grade. The compression parameters were improved according to the texture. D50 varies from 0.62 to 15 microm. As D50 decreases, the lubrication performance is improved. Finally, the specific surface area of talcs was studied. This last characteristic of talcs was shown as the most relevant parameter in determining lubrication ability.