ABSTRACT
Traditional Chinese medicine （TCM） effervescent tablets have the characteristics of rapid disintegration， good taste， and convenient taking， but there are some technical difficulties in the preparation and storage process， which are mainly reflected in the sticking， easy moisture absorption， poor compressibility， and poor stability. The basic physical properties of TCM powder （extract powder， raw powder） are the main cause of these technical problems， and also the key to control the quality of TCM effervescent tablets. Powder modification technology has shown good effects in solving the above problems. The author intended to review the research in the above aspects in recent years， and proposed the following strategies for applying powder modification technology to solve the problems in the production process of TCM effervescent tablets from the three aspects of raw materials， excipients and preparation intermediates：①The application of co-processing technology to the treatment of raw materials and auxiliary materials can solve the problems of sticking， poor compressibility， delayed disintegration， and poor stability. ②Using surface coating technology to treat raw materials and preparation intermediates can improve poor fluidity， poor compressibility and delayed disintegration. ③The hygroscopicity of the preparation can be reduced by using microencapsulation technology to treat the raw material. ④The inclusion technology can improve the clarity and stability of the preparation.
ABSTRACT
OBJECTIVE：To optimize the inclusion technology of volatile oil from Ganmao qingre granules. METHODS ： Guided by the concept of “quality by design ”，taking volatile oil inclusion rate and inclusion complex yield as key quality attribute，comprehensive score of above two indexes after weighting as response value ，inclusion temperature ，inclusion time ，the ratio of β-CD to volatile oil as key technology parameters ，Box-Burman response surface design was adopted to establish the design space of key technology parameters and key quality attributes. The design space was optimized and verified by 95％ confidence interval. The stability of inclusion complex was investigated preliminarily. RESULTS ：The optimal design space ，i. e. the optimal technology parameters rang ，included inclusion temperature 35-40 ℃，inclusion time 1.8-2.0 h，the ratio of β-CD to volatile oil 9.5∶1- 10∶1（g/mL）. The results of 3 validation tests showed that the volatile oil inclusion rates were all over 62％，the yields of inclusion complex were all over 75％，and the comprehensive scores were all over 80 point. The results of preliminary stability showed that the inclusion rate of volatile oil ，the yield of inclusion complex and the comprehensive score did not change significantly. The difference in evaluation indicators within 7 days was within 5％. CONCLUSIONS ：The optimized inclusion technology is feasible ， and the obtained inclusion complex is stable.
ABSTRACT
Objective: To reduce or avoid the volatilization loss of camphor (CA) in the industrialized preparation of cataplasm, using the inclusion technology of HP-β-CD. Methods: The HP-β-CD inclusion compound of CA (CA-HP-β-CD) was prepared by the constant temperature stirring method. The preparation processing of CA-HP-β-CD was optimized with inclusion efficiency as an index, and the pharmaceutical properties of CA-HP-β-CD were characterized by DSC, UV and SEM. The CA and CA-HP-β-CD were prepared to cataplasm at the industrial-scale production respectively, then the content of CA was determined and the statistical analysis was carried out. Results: The inclusion efficiency of CA-HP-β-CD for CA was (68.57 ± 1.26)% when the CA-HP-β-CD was prepared with the mass ratio of CA to HP-β-CD 1:3, the working temperature at 35 ℃ and stirring at 300 r/min for 4.0 h. The DSC, UV and SEM scans showed that there was a good compatibility between CA and HP-β-CD, and CA could be fully encapsulated by HP-β-CD and formed a stable inclusion complex of CA-HP-β-CD. Results of industrial-scale production of cataplasm for CA and CA-HP-β-CD revealed that the retention rate (actual content/feeding quantity) were (80.13 ± 1.05)% and (39.45 ± 1.38)%, respectively. And there was a statistically significant difference between them (t-test, P < 0.01), indicating that the HP-β-CD inclusion complex effectively reduce the volatilization loss of camphor CA. Conclusion: The volatilization loss of CA at the industrial-scale production of cataplasm was effectively reduced by the CA-HP-β-CD, which improves the utilization rate of CA and reduces the cost, and provides ideas and reference for the research and development of cataplasm of volatile drugs.
ABSTRACT
OBJECTIVE： To establish the method for content determination of ligustilide and to optimize the extraction technology of volatile oil and inclusion technology in Quhan zhufeng granules. METHODS： HPLC method was adopted. The determination was performed on Waters C18 column with mobile phase consisted of methanol-water （70 ∶ 30， V/V） at the flow rate of 1 mL/min. The detection wavelength was set at 327 nm， and the column temperature was 30 ℃. The sample size was 10 μL. Using yield of volatile oil and the content of ligustilide as index， with soaking time， the amount of adding water and extraction time as factors， the extraction technology was optimized by orthogonal test. Using inclusion rate， the yield of inclusion compound and yield of volatile oil as index， with ratio of volatile oil to β-cyclodextrin， inclusion temperature and inclusion time as factors， the inclusion technology of volatile oil was optimized by orthogonal test. RESULTS： The linear range of ligustilide was 0.4-4 μg（r＝0.999 9）； RSDs of precision， stability and reproducibility tests were all lower than 2％ （n＝6）. The recoveries were 96.75％-102.03％（RSD＝2.06％，n＝6）. The optimal extraction technology of volatile oil included 10-fold water （mL/g）， soaking for 15 min， extracting for 8 h. Average yield of volatile oil was 0.310 7％， and average content of ligustilide was 0.418 0 mg/g. The optimal inclusion technology of volatile oil included ratio of β-cyclodextrin and volatile oil was 1 ∶ 8 （mL/g）； inclusion temperature was 50 ℃； inclusion time was 3 h. Average inclusion rate was 69.43％， and the yield of inclusion compound was 58.89％； the yield of volatile oil was 14.15％. CONCLUSIONS： Established determination method is simple， accurate and stable. The optimal extraction technology of volatile oil and inclusion technology are stable and feasible.
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OBJECTIVE:To optimize the inclusion technology of Eugenol-β-cyclodextrin (β-CD) inclusion complex,and to identify and characterize it. METHODS:With the molar ratio of eugenol to β-CD,inclusion temperature and inclusion time as fac-tors,using the yield of inclusion compounds as index,the inclusion technology was optimized by orthogonal test. The formation of inclusion compound was identified by the spectra change of FT-IR,XRD and 1H NMR. Its structure was characterized by 1H RO-ESY NMR. RESULTS:The optimized inclusion conditions were that the molar ratio of eugenol to β-CD was 1.0:1;inclusion tem-perature was 60 ℃;inclusion time was 2.0 h. And the yield of inclusion compound was 73.86%(RSD=0.17%,n=3). 1H NMR results ofβ-CD and its inclusion complex indicated that the optimum qualitative ratio of the inclusion complex was 1.0:1. The inter-molecular interaction between eugenol and β-CD was confirmed by the spectrum analysis of FT-IR and XRD. 1H ROESY NMR re-sults indicated the structure of inclusion complex mainly was that the phenyl of eugenol was in the cavity of β-CD,the vinyl was outside. CONCLUSIONS:The inclusion technology is reasonable and feasible,and can be used for the inclusion of eugenol andβ-CD. The formation of inclusion compound is confirmed by the spectrum analysis.
ABSTRACT
Objective To optimize extraction technology for volatile oil of Pogostemon cablin in the second traditional veterinary drugs anti-stress granule.Methods The single factor was used to investigate the concentration and amount of the ethanol before inclusion of volatile oil.The L9(34) orthogonal design was used to optimize the factors in the process of inclusion.Results The optimal of technology method was that volatile oil was dissolved with 95% EtOH by 1:20(mL/mL),the ratio of oil and ?-CD was 1:8,?-CD was prepared the concentration of 10%,ultrasound pool was at 40 ℃,2.0 h.Conclusion The optimized process is stable and adjustable quality.