The Tablets Preparation And Part Of Action Research Of Betaine Hydrochloride

AimsResearch the effervescent tablets prescription, preparation process and method of betaine hydrochloride. Establish preliminary quality evaluation method then evaluate its quality. Observe the effervescent pharmacological tablets and the acute toxicity reaction of Research betaine. To provide experimental basis and the research and development of betaine hydrochlorideMethodsFirstly, the quality evaluation and determination of hydrochloride effervescent tabletsIn the process of the preparation of effervescent tablets, first of all, the dosage of the fixed betaine hydrochloride, a comprehensive evaluation of the disintegration time limit brittle broken degree of exterior factors such as hardness, select effervescent agent filler lubricant, the kinds of adhesive by orthogonal design method to optimize the prescription and the preparation process. Determine the best prescription preparation quality and simple prescription.According to the appendix IA of Chinese pharmacopoeia 2010. Evaluate the quality of preparation then establish standards, the quality and effervescent tablets of betaine hydrochloride.Secondly, The nerve pharmacological effects and acute toxicity studies of Betaine hydrochloride1 Sedative hypnotic experimentBetaine effervescent tablets to approach to the study of the central nervous system function in mice:①select similar weight 50 kunming mice, male and female half, were randomly divided into 5 groups, respectively, betaine low concentration group(0.29g·kg-1)betaine concentration group(0.58g·kg-1) betaine high concentration group(1.16g·kg-1)positive control group(diazepam2.0mg·kg-1) blank control group(NS), drug lavage after30 min to adapt the box into the activity in mice after 5 min, records within five minutes after 30 min 60 min min 90 number of self-help activities in mice, as a sedative effect observation index.②Same grouping, lavage 30 min after the treatment, each group of mice celiac injection of sodium pentobarbital, 25 mg·kg-1 in turn are reflected in mice within 30 minutes more than 1 min on the number of mice as sleep index, continuous observation self medicine end to appear in mice sleep time to sleep and sleep only the number of indicators as betaine hydrochloride hypnotic effects. ③the same grouping, lavage for 30 min after intraperitoneal injection of sodium pentobarbital 40 mg·kg-1, record each time of mice celiac injection of sodium pentobarbital, are reflected and recovery time, calculate the pentobarbital sodium hypnosis incubation period(from celiac injection of the drug to turn positive reflex disappearing time) and hypnotic time(from flip is reflection are reflected to the recovery time interval.2 Anti-seizure test Grouped in the same way, the same way of administration, oral administration after30 min, each group of mice were injected intraperitoneally(ip) injection Nikethamide150mg·kg-1, recording each group of mice convulsions and death, the incubation period is calculated convulsions and death, as betaine hydrochloride nikethamide resistance in mice induced convulsions indicators.3 Analgesic test①Light radiate a spin method: screening in the normal pain domain 50 kunming mice,random points 5 low betaine concentration group(0.29g·kg-1) betaine concentration group(0.58g·kg-1) betaine high concentration group(1.16g·kg-1) positive control group(acetylsalicylic acid solution 400mg·kg-1) blank control group(NS), dosing 30 min after 60 min using a radiant heat meter measure the pain threshold, calculate the pain threshold increase percentage(%). ② With the same grouping method, lavage 30 min after the treatment, each group of mice intraperitoneal injection(IP) 0.6% acetic acid solution, the dose of 0.1ml·10g-1record groups appear within 10 min mice body torsion reaction on the number of animals and the number of twist body computing analgesia percentage and percentage inhibition of body torsion reaction.4 Acute toxicity test To fill the maximum concentration and maximum capacity for mice gastric betaine hydrochloride effervescent tablets solution, observe the daily mice poisoning symptoms and deaths, record within 7 days of deaths in mice.Results1. Hydrochloride effervescent tablets of the result of determination of the optimum process of preparation and levels① According to the experimental results show that: with the rapid depletion of granulating of betaine hydrochloride effervescent tablets prepared by the best, the best prescription for: betaine hydrochloride(10%) tartaric acid(22%), sodium bicarbonate(28%), lactose(17.5%) of mannitol(17.5%), sodium chloride(2%), polyethylene glycol6000(3%) 3% of polyvinylpyrrolidone anhydrous ethanol liquid right amount, to produce quality inspections of betaine hydrochloride effervescent tablets, disintegration time limit weight difference brittle broken degrees are conform to the requirement of Chinese pharmacopoeia.②To produce the quality inspections effervescent tablets,the disintegration time limit, the difference of weight, brittle broken degrees of betaine hydrochloride are conform to the requirement of Chinese pharmacopoeia. Accelerated test is expected to product is valid for 2 years.2. Central nervous system effects of acute toxicity studies in mice and the results of betaine effervescent①In research hydrochloride effervescent tablets of autonomic activities in mice was adopted while calming effect experiment, the experimental results show that: compared with control group, diazepam in mice after 30 min 60 min free activities have obvious inhibitory effect of betaine hydrochloride of low concentration(0.29g·kg-1) and the concentration(0.58g·kg-1) compared with control group can reduce the frequency of autonomic activities in mice but there is no statistically significant downward trend, but high concentration group of betaine hydrochloride(1.16g·kg-1), after two hours of autonomic activities in mice have significant inhibition(P < 0.01). ② In the study of hypnotic experiments in mice, positive control group significantly less sleep time of mice,increase the sleep of mice with rat; But in the three concentrations of betaine, only a high concentration of betaine can significantly reduce the sleep time of mice and sleep rate(* P< 0.05); The rest of the two groups with have shorten the sleep time of mice the trend of increase the rate of falling asleep, but not statistically significant. ③ After injection of pentobarbital sodium, compared with the control group, positive control group could significantly shorter latency in mice hypnotic, sleep time is extended; three concentrations of Betaine can also significantly increase the sleep time of mice, but only the high concentration group hypnosis can significantly shorten the latency of mice(P <0.01).④In Nikethamide convulsive injection experiment, compared with control group, the Ukrainian sodium pentobarbital group can greatly increase the latency of seizures in mice reduces mortality in mice; betaine high, medium and low concentrations can significantly reduced mortality and convulsions latency(P <0.01) in mice.⑤Method and the use of drift Study twisting body analgesic effect of betaine on mice. The results showed that: In the tail flick test, compared with the control group, positive control group at 30 min, 60 min after administration the mice were extended field of pain, betaine can be extended only at high concentrations of the two time points after after drug pain domain(P <0.05), although the extension of the two remaining concentration trend but not statistically significant. In writhing, compared with the control group, the three concentrations of betaine can reduce writhing in mice and increased with dose concentration decreases. Betaine prove effervescent analgesic effect in mice. ⑥ Acute toxicity studies in mice, used as betaine concentration increased, compared with the control group, the mortality rate of mice also gradually increased.Conclusions1 The use of non-Shui granulation prepared betaine hydrochloride effervescent best,and the best process: acid betaine(10%), tartaric acid(22%), sodium bicarbonate(28%),lactose(17.5%), mannitol(17.5%), sodium chloride(2%), polyethylene glycol 6000(3%),2% ethanol solution of polyvinylpyrrolidone amount of acid betaine(10%), tartaric acid(22%), sodium bicarbonate(28%), lactose(17.5%), mannitol(17.5%), sodium chloride(2%), polyethylene glycol 6000(3%), 2% ethanol solution of polyvinylpyrrolidone amount.2 To produce the quality inspections effervescent tablets,the disintegration time limit,the difference of weight, brittle broken degrees of betaine hydrochloride are conform to the requirement of Chinese pharmacopoeia. Accelerated test is expected to product is valid for2 years.3 Betaine effervescent sedative, hypnotic, anticonvulsant, analgesic pharmacological effects.4 The maximum tolerance of Mice stomach betaine hydrochloride is 1.05 g/kg...