Novel Approach to DPI Carrier Lactose with Mechanofusion Process with Additives and Evaluation by IGC
The effect of lactose carrier surface property on the inhalation profile of dry powder inhaler (DPI) was eval-uated using a micronized drug (Compound A) by inverse gas chromatography (IGC). Mechanofusion with magnesium stearate (Mg-St) or sucrose stearate increased the line particle fraction (FPF),...
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Published in | Chemical & Pharmaceutical Bulletin Vol. 54; no. 11; pp. 1508 - 1514 |
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Main Authors | , , , , |
Format | Journal Article |
Language | Japanese |
Published |
Pharmaceutical Society of Japan
2006
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Online Access | Get full text |
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Summary: | The effect of lactose carrier surface property on the inhalation profile of dry powder inhaler (DPI) was eval-uated using a micronized drug (Compound A) by inverse gas chromatography (IGC). Mechanofusion with magnesium stearate (Mg-St) or sucrose stearate increased the line particle fraction (FPF), considered to be due to de-crease in the interaction between Compound A and the lactose carrier. The effect of Compound A concentration on FPF was smaller in mechanofusion-processed lactose compared to intact lactose, especially when processed with Mg-St. The relationship between the IGC parameters of the lactose and FPF was also investigated. FPF in-creased as both the dispersive component of the surface energy and acidity similarity between the lactose carri-ers and Compound A increased. Although further investigation is necessary, it could be suggested that acidity similarity decreases the interaction between Compound A and lactose, thus contributing to the increase in the FPF. In conclusion, (1) mechanofusion with Mg-St or sucrose stearate could be an effective method to improve FPF of a DPI drug formulation; (2) IGC would be a valuable method to investigate the interaction between a drug and the DPI carrier; and (3) a relationship between surface acidity and inhalation profile was suggested. |
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ISSN: | 0009-2363 1347-5223 |