| Now among the drugs made from Ligustrazine in market, injection has many shortages, such as,the injection is not convenience to use and results in pain at the injecting position, it also has the acute toxicity and anaphylaxis. Tablets and capsules have the insufficiencies on absorption and bioavailability, and they are not easy to deglut and difficult to decrease the dosage for the elderly. In the studies, Ligustrazine Hydrochloride is used to make into a new dosage form–guttate pills by the introduction of solid dispersion technology which can be taken both orally and buccally and has the advantages of high bioavailability, low side effects, and convenience for use. Main studies are as follows:The study was made on the basis of preliminary screening groundsubstance and condensing agent, the prescriptions and preparation processes of the drug were optimized and defined by orthogonal design. The validation of three lots of samples proved that the preparation process was stable and feasible. The conditions for the storage of the samples were also inspected.The material state of the dripping pills were identified by DSC, X-RAY, IR, SEM. It is found that some of the Ligustrazine Hydrochloride appeared in the state of dispersal molecules, some of them appeared as the micro-crystals. This indicates that it has changed into solid dispersion system during the procedure of preparation.The quality of the dripping pills is evaluated synthetically by quality specification, vitro dissolution and relative bioavailability, which shows that it is stable and controllable. The vitro bioavailability and vivo relative bioavailability of the dripping pills is improved significantly compared with that of the tablets.The result of the study proves that the preparation process of the dripping pills is stable and the quality of the pills is controllable. The Ligustrazine Hydrochloride dripping pills has the advantages of immediate effect and high bioavailability compared with other oral solid preparations.
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