Preparation Of Betaine Hydrochloride Tablets And Study On Its Pharmacokinetics And Relative Bioavailability

The molecular formula of betaine contains3methyl groups, and the methyl group as donor participate in tricarboxylic acid cycle, so betaine could be applied in syndrome short of methyl group. This research have discussed preparation method, quality standard of betaine, and provide theoretical basis for development of betainePart one preparation of Betaine hydrochloride tabletsObjectiveTo prepare betaine hydrochloride tabletMethodsAccording to physicochemical property of betaine and though screening diluent, adhesion agent, emollient to confirm betaine hydrochloride tablet preparationResultsBetaine hydrochloride tablet preparation are betaine hydrochloride, amylum, lactose, microcrystalline cellulose,6%starch syrup, magnesium stearate.ConclusionThe design of betaine hydrochloride tablet preparation is reasonable, preparation technology is simple and steady.Part two The quality standard research of betaine hydrochloride tabletObjectiveMake quality standard of betaine hydrochloride tabletMethodsAccording to the requirementof<Chinese Pharmacopoeia>, evaluate appearance, quality standard, friability, solubility, microbial limit of tablet. ResultsThe quality standard of betaine hydrochloride tablet correspond with <Chinese Pharmacopoeia>ConclusionThe method of quality control standard is simple, accuracy, and could be applied to quality control standard.Part three Establish HPLC measurement of betaine in serum samplesObjectiveApplying sedimentation of protein draw betaine of serum. Use Hypersil amino column(250×4.6mm,5μm), acetonitrile-water-three ethylamine(85:5:0.1) as moving phase(flow rate is1.0ml/min-1), and use evaporative light-scattering detector test betaine of serum(The drift tube temperature is86℃, flow rate of carrier gas is2.2L/min and nitrogen pressure is0.5MPa.ResultsLimit of detection of this method is0.0675μg and limit of quantitation is0.28μg. Repetitive test:three degrees value(high, middle, low) of RSD%are2.08%,6.09%,5.12%.6-day stability test:intra-day RSD%value are9.86%,5.9%and5.1%, inter-day RSD value was9.47%,5.79%,4.25%respectively. The average of absolute recovery of three different concentration are96.20%、88.96%、88%。elative standard deviation RSD are1.8%,6.93%and15.20%respectively.ConclusionDetermination method of betaine pharmacokinetics and bioequivalence studyPart four Research of betaine hydrochloride tablets in the pharmacokineticsObjectiveEvaluate bioequivalence between experimental betaine hydrochloride tablets and foreign public tablet.MethodsFeed wistar rats two kinds of betaine tablet by lavage through cross experiment, and apply HPLC-ELSD to test blood concentration and calculateResults:Apply SPSS17.0statistical analysis software to analyses the data from experiment. Use t-test analyses two groups of data at different time points. P<0.05show the differences has statistically significance. Use both sides t-test analyse bioavailability F (105.41+17.86), and P>0.05show the difference has no statistically significant difference.95%confidence interal (95%-97.58%) is equivalent.ConclusionThere was no statistically significant difference test preparation and reference preparation, for the biological equivalent preparation.Part five Study acute toxicity of betaine hydrochloride tabletsObjectiveDiscussed safety of the experimental betaine hydrochloride medicationMethodsMice were intragastrically administered with betaine hydrochloride tablets (2.52g/kg). Observe the mise situation of weight increase and survival and organs have or not abnormal.ResultsAll the mise had no abnormal at the time when were intragastrically administered with betaine hydrochloride tablets, and all the mise were survived during14days. Weight increase, mental activity and all kinds of vital signs were normal, and internal organs had no abmormal.ConclusionBetaine hydrochloride is low acute toxicity and safety...