| Draconis Sanguis is a famous traditional Chinese medicine which has being applied 1500 years. It is applied in clinic on the role of activating blood and removing stasis, hemostasis, detumescence and acesodyne and etc. Draconis sanguis flavones has been prepared common capsule which has been applied in clinic on the role of restraining venous thrombosis and focal cerebral ischemia, treating ischemic brain edema. At present study draconis sanguis flavones was selected as a model drug. According on the characteristic of angiocardiopathy, the sustained-release capsules of draconis sanguis flavones were designed. These capsules can deliver the drug slowly, reduce the fluctuation of plasma drug concentration, decrease dose and the compliance of patients could be improved. The capsules were filled with sustained release pellets which reproducibility and regularity of drug release as a kind of multiple unit dosage forms are better. The capsules were more safety than common sustained release preparation which can avoid phenomenon of sudden release.At present study the determination method of draconis sanguis flavones was established. According to the characteristic of flavones, several extraction methods were compared by the content of draconis sanguis flavones as index. As results, the content of draconis sanguis flvones is highest by light petroleum, acetone, aether, and the alkali-extraction and acid-precipitation method for extraction. The studies determine the content of lourerin A and lourerin B which are the indexes of the extractions. The studies identify the flavones of the extractions by chemical staining method and photodiode array detector (PAD).Draconis sanguis flavones are poorly water-soluble drugs and its bioavailability is lower. It is hard to prepare sustained-release capsule. In order to solve the problem, the technique of solid dispersion would be applied to prepare pellets of Draconis sanguis flavones. The technique can increase drugs dissolution and bioavailability. The determination method of pellets of draconis sanguis flavones was established. Pellets of Draconis sanguis flavones were prepared using water soluble polymers (PEG6000 and poloxamer F68 ) as carriers by the dropping method. With the dissolution and friability for index sign, single factor design and orthogonal design were applied for optimum prescription of pellet. The optimum prescriptions are as follows: the percentages of draconis sanguis flavones, poloxamer F68 and PEG6000 were 1, 2 and 1, considering on the results and the producing cost. The study examine the pellets of appearance properties, particle size distribution and weight variation. The results indicate that the quality obtained accord with regulation of pharmacopoeia. Basing on the pellets of Draconis sanguis flavones, the sustained release capsules of Draconis sanguis flavones were prepared by sustained release pellets. The sustained release pellets were coated with sustained release adjuvant to make sustained release pellets. The pellets were coated by a fluidized bed coater. By optimizing the preparation technique of the sustained release pellets, the optimum technique was found. The coating temperature was 30℃, the pulverization parameter was 1.5 bars, the sustained pellets coating fluid velocity of flow was 0.25ml/min-1.75ml/min. The optimum formulation of the sustained release membrane was the weight of EC20cps was 2.0% of the pellets'weight, the weight of PEG400 was 30% of the EC's weight and the weight of DEP was 25% of the EC's weight. The studies indicate that the release rates of sustained release capsules in different pH medium are different by the similarity factor method. The releasing mechanism of sustained release capsule of Draconis sanguis flavones was investigated by release test in vitro. The results indicate that their release profiles were best fitted to the first kinetics. The formula Ritger-Peppas indicates that the diffusion and bulk erosion occurred simultaneously in the sustained release capsule. |
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