Study Of Allicin Hydroxypropyl-β-cyclodextrin Inclusion Compound Intestines Dissolving Capsule In Pharmaceutics

Allicin is a broad-spectrum antibiotic, in our country medicine has a long history, it is the main garlic biological active ingredients, have lower blood pressure, fall hematic fat, reduce coronary atherosclerosis, cancer prevention and cure of cancer, antivirus, inhibit platelet accumulation effect and so on. Allicin is the main effective ingredients volatile garlic, its have the stronger antimicrobial and inhibiting tumor cell growth and prevention and cure atherosclerosis effects, and make known good development prospect of garlic. Because of volatile allicin, bad smell, soluble in water, which greatly limits the defects in its clinical application range and degree. At present, although have allicin tablets and capsules in clinical application, but preparation when used materials shortage, largely influenced the curative effect of allicin, such as previously reported in the literature to play many useβ-cyclodextrins for closure material will be after closure allicin, preparation into capsule or tablet, and preparations run to gut, intestinal fluid has not enough,β-cyclodextrins itself in the water solubility is small, so limiting the closure of the dissloution allicin with absorption. This study adopts HP-β-CD for closure materials, can resolve the allicin volatile, and it doesn't affect closure things dissolve out of allicin and absorption, will closure made intestines dissolving capsule thing, and overcome the smell of allicin, very irritating with stomach development prospect, at present, has not been seen similar reports in the literature. In order to get higher closure process of production rate, this experiment using orthogonal design method of allicin, hydroxypropyl-β-cyclodextrins closure rate for the research, the optimum best technological conditions. This topic to modern pharmacy for guiding principle, formulations theory combined with clinical needs and requirements.use modern pharmaceutical technology of allicin closure, which explored the preparation research. Previous research has made major pharmacodynamic effect, the results show that allicin, drug use safe reliable. This topic is in ordinary preparations primarily, optimize the allicin closure of content closure process, determine for its with capsule formulations, and its preparation process and quality control are studied, the drug delivering to in vitro, and the results showed that the probes the in vitro dissloution obvious, faster than the functionalities allicin tablet and allicin intestines dissolving capsule, preliminary reached this topic research purposes.1. Closure content closure process selection and research According to allicin and hydroxypropy-βcyclodextrins physicochemical properties and closure methodology comparison, eventually process route for grinding method worked. Orthogonal experimental method with many indexes, and screened grinding method considering the best closure process:1mL allicin with 1mL anhydrous alcohol dissolving,4mL slowly add to the water dissolved 12g hydroxypropyl-β-cyclodextrins assessments, grinding 2h mortar, buy vacuum drying oven after 50℃in dry 4h. The results show that the closure process retrieval rate is high, reliable and practical.2. Closure that allicin extraction technology researchExplore that closure of allicin extraction method and reagents choice, the results show that the organic solvent extraction closurerate that allicin steam distillation method obviously higher than. Meanwhile on different elution and extraction solvent of allicin hydroxypropyl-βcyclodextrin entrapped complex closure rate mensuration analysis was studied and established the accurate closure rate determination methods. Using different solvents for closure surfaces were not closure of free medicine, and for elution that closure already closure medicine extraction solvent, to select the right thing for closure in combination of the determination of effective ingredients. Results show that different solvents on closure content free of allicin elution and elution drug losses and closure when that the effective ingredients, there was a big difference between taking effect. Elution efficiency:petroleum ether< ethyl acetate< ether, Extraction efficiency:hexane> acetic acid> ethanol. So choose polarity small petroleum ether as elution solvent, polarity big is hexane as extraction solvent.3. Closure content intestines dissolving capsule production process and quality standards According to the properties and drug preparation in technology and clinical medication requirements, determine its formulations for capsule. Will preparation good allicin hydroxypropyl - beta entrapped cyclodextrin complex, crushing, screening, will have 60 orders powder fills at 0 drug, intestines dissolving capsule shells, each grain of outfit 0.45 g. Investigation under different conditions of quality index drug changes over time, is for the packing of the drugs, the confirmation and preservation condition of the validity of establishing provides the basis.Through the determination of moisture absorption rate to determine the critical relative humidity for 74%, relatively suitable for production. In preparations by TLC method was used to identify effective ingredients, results, good separation result, controlled spots without interference. For closure by GC methods that are intestines dissolving capsule content determination, studies show that more quantitative method used simple, reliable, accurate, and can be used as a control this product immanent quality indicators. According to the measuring results, and developed a batch sample, the content of allicin every capsules, temporary limit shall be not less than containing allicin 7.17 mg.4. Research into the dynamics of drugs and in vitro drug deliveringDrug dynamics is the principles of dynamics and mathematical method by studying the drug in the body, the dynamic behavior and quantitative change rules for the clinical application of scientific, choose the appropriate dosage forms and formulate rational dose provide the scientific basis. This research build the allicin hydroxypropyl-β-cyclodextrin entrapped complex intestines dissolving capsule body analysis for allicin, through GC method index component determination of allicin in plasma of rabbit, in its content of dynamic characteristics of a drug in the body is reserached. Results show that allicin closure content intestines dissolving capsule in rabbit in a relatively short time, body function with other the functionalities of formulations allicin effect-acting fast, compared to its further development of scientific foundation laid. With the accumulation of allicin dissloution percentage were for the study index, or scenedesmus allicin tablet, capsule and ordinary allicin preparations of this study in vitro dissloution, show that the research preparations in vitro dissloution significantly faster than the functionalities other forms.5. Closure content intestines dissolving capsule preliminary stability studyDrug stability is the clinical efficacy and safety of main index. This topic established intestines dissolving capsule GC content determination methods, inspects the preparations preliminary stability, results show that the content determination method is feasible, high efficiency, error (days error, requirements, daytime error) Long-term stability experiments show that this preparation, good stability and its expiration date provisionally as two years.