Metoclopramide Dihydrochloride Injection Preparation

We got metoclopramide dihydrochloride crystal from metoclopramide, then, consulted the standard of injection, prepared metoclopramide dihydrochloride injection. Finally we carried through security experiment,stability experiment, pharmacodynamics experiment and pharmacokinetics experiment.1 The preparation of metoclopramide dihydrochloride crystal: Compare three different technics in order to gain the best technics. First, dissolved metoclopramide by hydrochloric acid, secondly surged four hours, thirdly vaporized 40 minutes at 25℃,then, air-dry 6 hours, finally gained the flav crystal. According to the means of codex to confirm it.2 The preparation of metoclopramide dihydrochloride injection and quality: according to the standard of injection, we prepared metoclopramide dihydrochloride injection. The average rate of recovery is 100.13%, the variance is 0.56%, the pH is 4.0, the value of osmotic pressure is 286mOsM, injection was eligibility after examined in bacterium. The linear relationship was found when the metoclopramide dihydrochloride concentrations ranged from 1μg/ml to 10μg/ml, A=0.0339C+0.0142, R2=0.99543 The stability of metoclopramide dihydrochloride injection: in the study of light speedup, the difference of content was not notability, only the colour of the injection seems a litter yellow; in the study of speedup and longtime study, the difference of content was not notability too; the result of classic isothermal kinetic study shows: lgK=11.73-5060.9/T, t1/10=2.15, the expiration date was 2.15 year.4 The security of metoclopramide dihydrochloride injection: pyrogen examine was negative, thrill experiment show it has a litter stimulate to muscle and was not notability to blood vessel, hemolysis experiment was negative, the value of LD50 was 409.64mg/kg, minimum lethal dose was 800mg/kg, which was one-hundred times of normal dose.5 The pharmacodynamics of metoclopramide dihydrochloride injection: Take metoclopramide dihydrochloride injection as experiment group and acetylcholine as positive control group, in vitro, intestine's squirm was recorded by four-channel physiological recorder, and the squirm frequencies and scopes of experiment group from 4.32 and 4.1mm to 4.95 and 7.5mm, the squirm frequencies and scopes of control group from 4.13 and 4.2mm to 5.16 and 9.8mm. The effect of metoclopramide dihydrochloride injection on gastric emptying and small intestine propulsion was studied by giving mice the semisolid nutrient paste. Result show that the gastric emptying was from 29.88±5.15 to 16.11±3.76 and the small intestine...