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Objective:To prepare Danshen extract and Danshen capsules, and study on its stability under high humidity, high temperature and light conditions.To determine the hygroscopicity of Danshen capsules and its intermediates. Method:The contents of danshensu, rosmarinic acid, lithospermic acid and salvianolic acid B in Danshen extract and Danshen capsules were determined by UPLC, the detection wavelength was 280 nm and the mobile phase was 0.05% phosphoric acid aqueous solution(A)-acetonitrile(B)for gradient elution(0-2 min, 93% -79.2% A;2-6 min, 79.2% -75% A;6-9 min, 75% -65% A;9-10.5 min, 65% -10% A;10.5-11 min, 10% -93% A).The critical relative humidity(CRH) was calculated and hygroscopic isothermal curve was drawn by determining the moisture absorption and weight gain of Danshen capsules and its intermediates. Result:The fluctuation of contents of these four phenolic acids in Danshen extract and Danshen capsules was within±10% and no significant change trend after placing at temperature of 40℃, relative humidity of 75% and 92.5%, light intensity of (4 500±500) Lx for 10 days.The change rates of danshensu in Danshen extract and Danshen capsules under 60℃ were 47.45% and 32.24%, and change rates of salvianolic acid B were -6.39% and -9.64%, respectively.The hygroscopic investigation showed that CRH of starch-based pellets was 58.5%, CRH of Danshen extract was 72.34%, CRH of coated pills was 72.85%, and CRH of Danshen capsules was 73.55%. Conclusion:High temperature has effect on stability of phenolic acids in Danshen extract and Danshen capsules, in order to ensure the quality of them, high temperature environment should be avoided.In order to prevent excessive moisture absorption of Danshen capsules and its intermediates, the relative humidity in the production and storage environment should be controlled below the corresponding CRH.
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OBJECTIVE:To study the formulation of Xiqingguo buccal tablet,optimize the proportion and quantity of main materials. METHODS:Using appearance,hardness,dissolution and taste as investigation indexes,orthogonal design was adopted to optimize the proportion and quantity of main thinner(lactose,mannitol),wetting agent(ethanol),lubricant(magnesium stea-rate),flavoring agent(aspartame),and critical relative humidity was detected. RESULTS:By wet granulation,the optimal formu-lation were as follows as the ratio of lactose and mannitol was 1:3,ethanol volume fraction was 60%,the dosage of menthol, magnesium stearate,aspartame and orange essence was 0.4%,0.9%,2.0%,0.4%;it was proven that the total score of 3 batches of samples were 2.67,2.67,2.70 (RSD=0.65%,n=3),respectively. The critical relative humidity of granule was 60%. CON-CLUSIONS:The Xiqingguo buccal tablet prepared by optimal prescription meets the requirements.
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Objective:To confirm the relative humidity conditions of preparation of Hericium Erinaceus and Lumbricus ( HD) bio-transformation and the longest operation time under the conditions through the study on hygroscopicity of dry extract powder. Methods:The solution was prepared respectively in the environment with various humidity, and the moisture absorption rate and critical relative humidity ( CRH) of dry extract powder of HD biotransformation were measured, and then the mathematical model was built and the curves of moisture percentage vs relative humidity was drawn. The parameters of moisture absorption rate, and the relative humidity and operation time with the moisture percentage up to 5% were calculated. The analytic geometry and linear regression method were used to calculate CRH, so as to determine the air humidity control range and the conditions for the production and storage process. Results:The moisture absorption of HD dry extract powder could reach 5% when exposed to the air respectively with the relative humidity of 66. 0%, 80. 8%, 88. 2% and 99. 0% for 7. 088, 3. 953, 2. 892 and 0. 661 h. When the moisture percentage reached 5%, the rela-tive humidity and the shortest time was 50. 84% and 9. 937 h, respectively. The CRH of the dry extract powder of HD biotransforma-tion was 68. 12%. Conclusion:When the dry extract powder of HD biotransformation is under preparation, the relative humidity of en-vironment should be controlled below 50. 84% with the operation time shorter than 9. 937 h, or the relative humidity is controlled below 68. 12% with the operation time shorter than 6. 810 h. Under the above conditions, the moisture absorption rate of HD dry extract pow-der can be controlled below 5%, which does not affect the preparation.
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Objective To investigate the effects of moisture-proof materials and contents on hygroscopicity of Yixinshu Capsules; To improve moisture-proof function of Yixinshu Capsules. Methods The hygroscopicity performance of Yixinshu Capsules was analyzed with the indexes of moisture absorption rate and critical relative humidity (CRH), and effects of soluble starch, maize starch, dextrin, lactose, mannitol, calcium hydrogen phosphate, ethylcellulose, microcrystalline cellulose, hypromellose and low-substituted hydroxypropyl cellulose on hygroscopicity of Yixinshu Capsules were compared. The effects of optimized excipients and capsule contents after granulation on hygroscopicity of Yixinshu Capsules were tested. Results Lactose, microcrystalline cellulose and mannitol were the most appropriate moisture-proof excipients for Yixinshu Capsules with balanced moisture absorption rate of 18.04%, for which the best proportion of Yixinshu Capsules to excipients was 1 to 0.1 (wt%). The balanced moisture absorption rate of the powders were 14.87%, 14.39%, and 15.38%, respectively, whereas the granules were 10.75%, 10.29%, and 11.13%, respectively. Conclusion The selected excipients can effectively reduce the hygroscopic rate of the Yixinshu Capsules, and its granules can promote the moisture resistance of Yixinshu Capsules.
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Objective: To optimize the processing conditions of Maxing Antitussive and Antiasthmatic Grannule (MAAG). Methods: The influence of different excipients including lactose, soluble amylum, and dextrine, and usage amount of soluble amylum to hygroscopicity of powdered extract was investigated; Processing conditions were optimized by orthogonal test, flowability, and hygroscopicity were investigated. Taking forming rate, solubility, and absorption rate as indexes, the materials added prescription varieties, ratio, and optimum molding process were screened. Results: The particles sugar plus dextrin as excipients were superior to dextrin or sugar or soluble starch as excipient particles; The optimized conditions were obtained with: main drug-accessories (1:2), accessories for the dextrin-powdered sugar (1:1), with 80% ethanol as wetting agent which accounted for 14% of the main drug. Conclusion: The selected accessories in MAAG is reasonable and forming process is feasible. This research provides the basis for the establishment of forming technique and control of production environment of MAAG.
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Objective To optimize the forming process of Wuzibushen Capsules. Methods Category and ratio of accessories were investigated by taking moisture absorption percentage as index. The inspected angle of repose, bulk density and critical relative humidity were also investigated. Results Starch was used as the excipien. Remedium cardinale and starch in the ratio of 1.15∶1.25 was more appropriate, 60% alcohol was added, dried at 60 ℃. Granules had a good fluidity, critical relative humidity was about 62%. Conclusion The forming technology was reasonable and provide reliable basis for production.
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OBJECTIVE: To study optimal formulation process of Rutongning granule. METHODS: The ratio of main components to excipients was optimized with hygroscopicity,granulation and dissolubility index. RESULTS: The optimal ratio of extract powder to saccharose was 1 ∶ 1.5. The made granules were characterized with low hygroscopicity, high granulation,high dissolubility and low cost. And its critical relative humidity was 65%. CONCLUSION: The study provides theory evidence for formulation process of Rutongning granule and the control of production environment.
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[Objective]To ascertain the best formulation process of Tangkening Granule. [Method]By determinating hygroscopicity, granulation and dissolubility, the appropriate recipient and its formula are selected. [Results]The best excipient is 1∶0.5. The made granules have low hygroscopicity and high granulation and high dissolubility. And its critical relative humidity is 70%. [Conclusion]The experimental results provide the basis of the ascertainment of formulation process and the control of product inviroment of Tangkening Granule.
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Objective:To increase the critical relative humidity(CRH) of Qubi granule,thus to improve its humidity resistance. Methods:The best prescription of Qubi granule was optimized by comparative method,and to determine its critical relative humidity. Results:The old prescription of the Qubi granule's CRH was 50%.With new prescription,the Qubi granule’ s CRH was 61%. the latter has increased by 11% as compared with the former . Conclusion:Considering above result,there is a hope to improve the hygroscopicity of Qubi granule.
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Objective: To improve the physical properties of micromeritics of the extracts of Fengshilin capsule, such as anti moisture. Methods: Critical relative humidity, absoption curve of moisture, angle of repose were used as the norms of the research. The suitable excipients and formulation process of Fengshilin capsule have been sieved. Results: It was feasible that the combined excipients of microcystalline cellulose and starch (in a ratio of 1∶1) were mixed with the extract powder. The absorption of moiture of the extract powder was improved. The humidity of mass production and store was lower than 45%. Conclusion: The research has been found to be an effective in the process of Fengshilin capsule.