Bioavailability and pharmacokinetics of sorafenib suspension, nanoparticles and nanomatrix for oral administration to rat.

Sorafenib is slightly absorbed in the gastrointestinal tract due to its poor solubility in water. To improve its absorption, a novel nanoparticulate formulation-nanomatrix was used in the study. The nanomatrix was a system prepared from a porous material Sylysia(®) 350 and a pH sensitive polymer Eudragit(®). The formulations were optimized by orthogonal design (L(9)(3(4))) and their bioavailability were evaluated in rat, comparing to pH-sensitive Eudragit nanoparticles and suspension of sorafenib. In the formulations, the ratio of sorafenib to Eudragit(®) S100 was found to be more important determinant of the sorafenib bioavailability than the ratio of sorafenib to Sylysia(®) 350. As for the bioavailability, the AUC(0-36 h) of sorafenib nanomatrix was 13-33 times to that of sorafenib suspension, but only 16.8% to 40.8% that of Eudragit(®) S100 nanoparticles. This may be resulted from the different drug dispersion degree, release character and bioadhension activity. However, because all the materials used in the nanomatrix formulation are commonly adjuvant, safe, easy to get and cheap, above all, the nanomatrix formulation can solve the stability and scaling up problems in the nanoparticles, it had potential to develop into a product in the future.

[Effect of ligustrazine, synthetic borneol on lasting time of ciliary movement].

OBJECTIVE: To study the using of the method in vitro and in vivo of lasting time of ciliary movement in ligustrazine, synthetic borneol. METHODS: (1) Method in vitro-The lasting time of ciliary movement was observed with forty-fold optical microscope after dropping liquid medicine on exteacorporeal frog palate mucosa. Then mucosa was cleared. It was observed whether the ciliary movement was recovered and the lasting time was recorded from recovering to stopping once again. (2) Method in vivo-Liquid medicine or normal saline was dropped on frog palate mucosa by contacting thirty minutes. Then mucosa was cleared. The lasting time of ciliary movement was observed with forty-fold optical microscope by separating palate mucosa. RESULTS: Relatively percentage of lasting time of ciliary movement of ligustrazine in vitro and in vivo was 9.8%, 87.3%; The relatively percentage of synthetic borneol in vitro and in vivo was 9.3%, 89.5%. CONCLUSION: The method in vitro and in vivo of lasting time of ciliary movement can be the one of the selecting ways of Chinese drug's toxicity of nasal mucosa, and it have virtues and defects respectively. Ligustrazine, synthetic borneol have significantly toxical effect on exteacorporeal lasting time of ciliary movement.