Release Solid Dispersions

Aiming at the cure of vertebral artery type of cervical spondylosis (also called cervical vertigo) which is common in cervical spondylosis, and paroxysmal vertigo caused by Qi stagnation and Blood stasis, and Blood stagnation due to Qi deficiency, or Phlegm accumulated by stagnant Blood, activating Qi and Blood circulation system was selected as a basic principle for treatment. Through systematic research, modern compound sustained-release preparation Jing Yunting sustained-release capsules were prepared by sustained-release solid-dispersion techniques. Jing Yunting sustained-release capsules is composed of Chinese herbs Rhizoma Chuanxiong and Radix pueriae. Here is the abstract of our research:The genuine crude drugs of Rhizoma Chuanxiong originate from Sichuan. Owing to the angle of rational utilization of resource, and the physical and chemical nature of the alkaloid of its main effective position, we confirmed the conditions of the pharmaceutical-process of total alkaloid of Rhizoma Chuanxiong by single factor tests (ANOVA): put sour liquid (PH 2-3) which cubage is 2 times of the drug powder in the percolation vat, then, soak in the same pH value sour water for 24 hours. Percolate it, at the rate of 4-5ml/kg. Then, collect the percolating liquid which 6 times of cubage of crude drugs is needed.By the systematic comparison of the differences among the macroporous absorb resin and the refined purification craft of the strong-acid ion exchange resin, and weak-acid ion exchange resin, as well as ion exchange resin, we carried on the separation purification craft of drawing liquid of total alkaloid of Rhizoma Chuanxiong by associating the macroporous absorb resin with ion exchange technique innovatively. Eluting and screening by single factor test, we lastly confirmed the Rhizoma Chuanxiong total alkaloid separate purification craft. Which is: regulate the solution pH value of the percolate of Rhizoma Chuanxiong to 2-3, then set it still. Then, be filtrated by D₁₀₁macroporous absorb resin post. After that, collect the post liquid, and regulate its pH to be neutral value. Through Model A ion exchange resin post, wash the percolate with water at 3BV/h speed to neutral. And then be eluted by 5% of the M of 2 times as much as that of beds' cubage which has solved the difficult point in the total alkaloid refined purification craft of Rhizoma Chuanxiong. Purify the liquid by passing it through the anhydrous ethanol and Dioi resin. And freeze drying it after eluting and concentrating the liquid which have got the effective position of total alkaloid of Rhizoma Chuanxiong. This sets up the quality level of the total alkaloid intermedia of Chuanxoing that has offered an important way for comprehensive utilization of the Rhizoma Chuanxiong.We has got the total flavonoids of Radix pueriae, and set up quality level, and offered the qualified intermedia for preparation of sustained-release capsule by distilling liquid from 50% ethanol, absorbing the resin to separate by the AB-8 macroporous absorb resin, eluting 70% of the ethanol, and spraying and desiccating after the eluting liquid was concentrated.The proportions of compatibility of two kinds of intermedia are decided to be 1:2, and a daily quantity is 200mg by studying the influence on the model rat's blood rheology index of "blood clot" of intermedia, and consideration of the result of the test in drug effect as a basis. Depending on the research of preparation of shaping craft, the solubility of total alkaloid of Rhizoma Chuanxiong is better than that of extracts of Radix pueriae. And, considering the clinical need and advantage of dispersing technology of solid, EC is regarded as carriers and HPMC is regarded as releasing controller, sustained-release solid dispersion was prepared by evaporating solvent. And by using the external accumulating releasing degree of the total alkaloid of Rhizoma Chuanxiong and total Flavonoids of the Radix pueriae as the index, the best preparation prescription by single factor test (ANOVA) is that EC: HPMC: Medicine equals 3:0.5:1. About the dispersed state of medicine in sustained-release solid dispersion, X-ray diffraction test, DSC test, and infrared spectrum scanning and so on, are all indicates the medicine exists within the molecular and mini-crystal state mainly in...