Study On Gastrodin Sustained-Release Suspension

Research Context Gastrodin is one of the effective components of Chinese traditional medicine gastrodia elata. Its main function is used to treat the disease of heart head blood-vessel. With cerebrovascular disease incidence is higher and higher, as a traditional Chinese medicine preparations, curative effect,low toxicity, will have broad application prospects. But so far, more and more research literature about its slow-release preparation, such as:sustained-release skeleton slice, coating zyban, slow release micro pill,osmotic pump, etc., but the real sale controlled-release formulation is few and far between, for the most part for injection, tablet, oral liquid, etc.This research hopes to develop a slow-release dry suspension agent, is expected to meet the patients' medical needs. Will first gastrodia elata was prepared using ethyl cellulose solid dispersion, to release degree as the index, to screen the best prescription and preparation process, and then dry suspension agent is prepared. With vertigo mice model to evaluate its slow release effect, the results show that the slow-release effect.Main contents1. Investigation of the physical and chemical properties of gastrodia elata,establish analysis method, is advantageous to the subsequent solid dispersions of preparation and release study.2. Preparation of gastrodine solid dispersions, determined by factors that influence the biggest single factor, optimization orthogonal experiment was used for the best prescription and technology.3. preparation of gastrodine Sustained-release dry suspension agent and test its stability, and the dry suspension agent meets the requirements.4.Vertigo mice model was established to evaluate the slow-release effect of dry suspension agent.Methods1. preformulation study.With reference to the requirements of the "Chinese pharmacopoeia" in 2015 the fourth, set up the analysis method for the determination of gastrodine content and release degree determination method, the results accord with the requirement of related.2.Orthogonal experiment optimization gastrodine solid dispersions.With ethanol as solvent, drugs and ethyl cellulose were dissolved,preparation of gastrodine slow-release solid dispersions, through orthogonal experiment, the cumulative in vitro release percentage as an index, to screen the best prescription and preparation technology.3.The preparation and quality evaluation of Gastrodia elata slow-release dry suspension agent.Gastrodia elata solid dispersions and other auxiliary materials through 80 mesh sieve, sedimentation volume and dispersion as evaluation index, commonly used six suspended aid. Under the condition of high temperature, high humidity and strong light irradiation, examine the stability of the slow-release preparation by dry suspension agent,accelerated test and long-term test research shows that the preparations slow-release dry mixing the long-term stability of the suspension.4. The evaluation of slow-release effect about gastrodia elata slow-release of dry suspension agent ueing kunming male mice as experimental animals, first set up toavoid electric shock in mice conditioned reflex, to rotate the mice produce dizziness, vertigo mice to avoid electric shock time for incubation period, after giving gastrodine, because of gastrodine can resist the dizziness, the mice will shorten the incubation period, compared with common preparation, incubation period to change over time to evaluate preparation gastrodine slow-release slow-release effect of dry suspension agent.Results1. Gastrodia elata in ph1.2 hydrochloric acid solution, PH6.8 phosphate buffer solution, the stable within 24 h, to establish the content determination method of linear relationship meets the requirements(r =0.999), precision, daytime precision, recovery and release content determination method meets the requirements.2. This study selected ethyl cellulose(EC) viscosity of 20 m Pa S,gastrodia elata and slow-release carrier material ratio of 1:3, hole agent dosage for control-released carrier materials of 1.5%, crushing sieving particle size is 80 mesh, the preparation of the solid dispersion of fitness over 12 h drug release in vitro and drug release curve of pseudo-first-order release equation.3. Gastrodia elata solid dispersions and other auxiliary materials all through 80 mesh sieve, mixing of dry suspension agent prepared directly,its final prescription for: gastrodia elata solid dispersions(including gastrodine 25 mg), suspended aid HPMC K10M(50 mg), taste masking agent mannitol(300 mg), a sweetener xylitol(210 mg), aromatic osmanthus fragrance(5.5 mg), flow aid colloidal silica(3.5 mg).4. The establishing of animal model of dizziness can intuitive response of homemade gastrodine slow-release of sustained-release effect of dry suspension agent. In mice, it can slow release for 8 h, the method issimple and clear, does not need complex high-end equipment,slow-release preparation by dry suspension agent has certain sustained-release effect.Conclusions1. For preparation of ethyl cellulose solid dispersion of gastrodia elata, in vitro release form, it has certain sustained release effects.2. Homemade gastrodine slow-release dry suspension agent of preparation technology is simple, materials used in common, the price is reasonable, good stability.3. Gastrodine slow-release dry suspension agent in vertigo mice model study showed that compared with common preparation, it has certain sustained release effects.