| Leech is the animal of Hirudo aipponica Whitman,Whitmaniapigra uhitman or Whitmania acranulaata Whman who belongs to Annelida.It is Bitter salty in flavour,mild in property,slightly poisonous,and belongs to liver meridian.TCM considered it had the functions of promoting blood circulation to remove blood stasis,promoting menstruation.It mainly contained hirudin, heparin,anti-thromboxane,protein,amino acid,peptide,histamine analogs and so on.Its main pharmacological effects were inhibited coagulation,antithrombin and so on.The application of treatment of cardio-cerebrovascular disease in modern clinical practice was of significant curative effect.This paper studied on the preparation technology of making the leeches into soft hydrophilicity capsules.The really research contents were the selection of processed products of leeches,the extraction,refining,concentration and desiccation of leeches,the preliminary study on the prescription technique of soft capsule,the study of the quality standard and stability of the restricted substance in the soft capsule.This paper selected the optimum processed products of leeches by testing the activity of the different processed products using the enzyme-titration. The experimental results showed that the activity of the antithrombin in the sun drying products of leeches was obviously higher than in the sand fired products.As this paper used the sun drying products to study on the preparation of soft capsules.To screen the extraction solvent this paper used the activity of anticoagulation and exacting rate as the koxsada indexes,adopted orthogonal test design to select the extraction technology of leeches and the optimum technology parameters of refining,concentration and desiccation.The experiment results showed that the best extraction condition was to crush the dry leeches powder into coarse particle with the size of 0.5-1.0cm,to soak for 4h with water,to be extracted by water for 3 times,the first time was 10 times water 2h,the second and the third time were 8 times water 1.5h,to complicate the decoction,to filter and concentrate to a relative density of 1.20～1.25,to add ethanol to 70%,to mix intensively and stand for 24h,to filter and recycle ethanol,to decompressing concentrate and dry in -0.09MPa 80℃.Using the fluidity of the restricted substance as index,the preliminary study of the prescription technique of soft capsule indicated that the optimum proportion of leeches extraction and medium was 1:2.This experiment also investigated the characters of the restricted substance in different temperature,the result showed that the restricted substance with good flowability in 15℃or above.Using the substance mobility and leaching rate of flexible rind in PEG as indexes to select the plasticizer and disintegrant of lorica,result showed the best plasticizer was the mixture of glycerol and sorbitol,and the PEG400 can improve the dissolve rate and the disintegration of soft capsule.To study on the stability of the preparation,this paper established the TLC method to identify the soft capsule of leeches.This method featured simple operation,significant results and noninterference of excipient.This paper established the method of determining the titer of antithrombin in the preparation.This method featured noninterference of excipient and good repeatability.This paper adopt Micro-Kjeldahl Method to test the nitrogen content in the substeance.In the stability test part,this paper testified by sample at room temperature and in heating and accelerating condition to investigate the stability of the substance in the soft capsule.Results showed that it kept excellent characters and biological activity in 6 months.Using the formaldehyde content as the index,investigate the influence of the substances and various excipients in the prescription to the stability of the soft capsule. Results indicated that there is a little formaldehyde content in the substance and its excipients and it changed little. |
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