| Skipjack peptide is a kind of peptide extracted from the skipjack,and it exerts a significant role on lowering the uric acid level according to existing reports.However,direct oral administration of skipjack peptide is not acceptable because of its strong fishy smell.Therefore,there is an urgent need to improve the dosage form for taste masking.In this article,firstly,the extrusion-spheronization was selected as the technology of granulation.Next,fluidized bed technology was used for coating the obtained granules.And we selected suitable suspending agent and release regulator to make granule.At last,skipjack peptide's release studies were carried out,and we combine the volunteers taste evaluation and GC-MS as the taste masking evaluation method.At first,studies were made on skipjack peptide's micromeritics.Malvern 2000 laser particle size analyzer was used to measure skipjack peptide's average size.The average size was 13.560 ?m,and the repose angle of skipjack peptide was 32.7 ± 0.6°.When skipjack peptide was put in 25 ?,65%RH for 24 hours,the moisture absorption was 23.92 ± 0.26 %.Then studies on the assay method of skipjack peptide were made,and the BCA kit was selected as the optimum method.At the same time,we detected the amino acid,and detemined the amino acid composition of skipjack peptide.The GC-MS was used to detect the origin of the fishy smell from skipjack peptide,and the volatility component is(2-Aziridinylethyl)amine.The extrusion-spheronization was applied for granulation.When 50% ethanol was selected as adhesion agent,and the weight ratio of skipjack peptide and microcrystalline cellulose(MCC)was 3:7,particles with uniform particle size distribution could be obtained,and the average size of the particles was 150 ?m-250 ?m.The repose angle of granules was 32.4 ± 0.5°,and when granules were put in 25 ? 65%RH for 24 hours,moisture absorption was 8.35 ± 0.12%.For coating,fluidized bed technology was applied(the air intake temperature is 40 ?,atomizing pressure is 0.16 MPa,fan volume is 8 Hz,fluid velocity is 8 r/min).Colocon enteric coating powder was used as the coating material,and coating weight gain was about 60%.After coating,about 90% microcapsules' size were distributed among 250 ?m-450 ?m.The drug loading efficiency of microcapsules was 20.60%,and the repose angle was 28.2 ± 0.4°.And when granules were put in 25 ? 65%RH for 24 hours,moisture absorption was 2.02 ± 0.17%.Citric acid was chose to regulate the release of skipjack peptide,and the brewing temperature and the concentration of citric acid were evaluated.The best brewing temperature was 50 ? and the citric acid concentration was 0.5%.Furthermore,the guar gum was chose as the best suspending agent,and the appropriate concentration was 0.75%.Granules' release in gastric juice and intestinal juice were investigated,25.43% skipjack peptide was released in gastric juice after 1 h,and 48.32% after 2 h.90% skipjack peptide was released in intestinal juice after 30 min,and 1 h later,almost all skipjack peptide was released.GC-MS method was developed to evaluate taste masking effect,and measured the taste masking effect of different concentration of citric acid.When the concentration was 0.5%,the fishy smell released only 20% of the same amount skipjack peptide.19 healthy volunteers were chose to taste 10 mg/ml skipjack peptide solution and 10 g skipjack peptide granules among 200 ml water,and then they gave scores.The results indicated that the skipjack peptide granules had a good taste masking effect. |
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