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Aim: To study the hydrofluoroalkane-driven(HFA-134a) salbutamol sulfate (SS) MDI formulation compositions and the respiratory tract absorption in rats. Methods: Solubility determination and orthogonal design were used to aid the screening of non-CFC SS MDI formulations. Rats were exposed to SS MDI via intubation inhalation. Fluorescent HPLC detection was developed to determine plasma SS concentration in rats given the selected SS MDI formulations. Analysis of the plasma drug level-time profiles was performed by the statistical moment approach. Results: Stable and homogeneous non-CFC SS MDI formulations were obtained. The developed HPLC method was validated and used to assay SS levels in the rats after inhalation of the MDI. AUC ratios of the SS/HFA-134a-driven MDI formulation to the reference SS MDI and CFC SS MDI formulation were 109. 86% and 135. 54%, respectively. Conclusion: It is proven that the absorption of the HFA-134a SS MDI formulation in rats is equivalent to the simulant formulation commercially available oversea and better than CFC formulation.
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Aim Effect of various absorption enhancers on the insulin colonic absorption was investigated. Methods The hypoglycemic effect was examined after colon delivery of INS SOL co administered with various absorption enhancers and the pharmacological bioavailability (PA) was calculated. Results INS SOL (5 U?kg -1 ) containing eucalyptol, sodium caprate, sodium deoxycholate and menthol significantly decreased the blood glucose level ( P
ABSTRACT
Objective To develop a novel synergism compound suspension concentrate of niclosamide and chlorphoxim (Co-SCN) and sdudy its characteristics. Methods Niclosamide and chlorphoxim were milled by a ball mill and mixed with different amounts of wetting agent. disper-sant agent, thickener, and water etc. , to develop Co-SCN, and the pH value, thickener, grain size were evaluated. The ultraviolet absorption spectrum of niclosamide and chlorphoxim were measured. The content of niclosamide and chlorphoxim in the solution were assayed by HPLC. Results Co-SCN was a gray thickener fluidity liquid. It was very easy to disperse and could be mixed with water in any proportion. Its pH was 8. 65 and thickener was 137 mpa? s. The grain sizes (diameter) were from 0. 138-19. 953 ?m. Of them more than 95. 6% was smaller than 10 ?m and more than 82. 24% was smaller than 5 ?m. There were three peaks of ultraviolet absorption spectrum for niclosamide: 210, 234 nm and 334 nm respectively. One peak of chlorphoxim was at 269 nm. The novel formulation contained 20.64% niclosamide and 5.26% chlorphoxim. The suspension stability of Co-SCN was 100% for 2 hours and 89. 14% for 4 hours, and otherwise WPN in water was speedy sediment. Conclusion The novel synergism compound suspension concentrate of niclosamide and chlorphoxim is a stable quality and standard formulation.
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Objective:To study possibility of traditional Chinese drug preparation of controlled drug delivered to the colonic region. Methods: After the herbs was extracted and refined, micropills was produced with pectin selected as coating material and thallium monochloride was as internal standard substance. Results: The preparation was testified to attain schedule colon target. Conclusions: This research provided a way for traditional Chinese drug preparation of colon targeting.