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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.
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Cataplasma is a new transdermal drug delivery carrier, playing a significant role in the modernization of Chinese materia medica (CMM). It can overcome many shortcomings such as inconvenient use and intense irritation in traditional adhesive plaster and black plaster. However, the development of cataplasma is restricted by some crucial factors like the types of auxiliary materials and the processing ways of volatile medicine. A total of 254 articles related to CMM cataplasma optimization and the volatile oil treatment published from 2000 to 2017 were collected and sorted in this paper. The matrix types and excipients ratio scope, the experiment design method of optimized ratio of base material, and the processing ways of volatile oil in cataplasma were summarized, and then the existing problems in these three aspects mentioned above were discussed with view to giving reference for follow-up studies.
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To optimize the matrix formulation of Chaizhi cataplasma (CC) and investigate its release and transdermal absorption properties in vitro. The optimized matrix formulation of cataplasma containing liquid herbal extract is determined by using D-optimal mixture design, with initial bonding strength, endurance bonding strength and gel strength as the evaluating indicators. Modified Franz diffusion cells were used to study the in vitro release and transdermal absorption of geniposide in CC. The optimized matrix formulation of CC contained NP700, aluminum glycinate, tartaric acid, glycerin, PVPK90 and water (9∶0.7∶0.8∶30∶5∶30.5). Cumulative release rate of geniposide in CC was (77.02±3.73)% in 24 h. The percutaneous penetration rate of geniposide was 7.25 μg•cm⁻²•h⁻¹ and the 24 h permeated amount was (156.22±4.90) μg•cm⁻². The optimized CC prepared by the D-optimal mixture design showed a good adhesion and formability. The in vitro release of the geniposide in CC was in accordance with the first order equation, while its in vitro transdermal absorption was close to the zero order equation.
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Objective: To optimize the matrix formulation of Hanbishu Cataplasma (HC) and to investigate its realease and transdermal absorption properties in vitro. Methods: To optimize the cataplasma with liquid extract by D-optimal mixture design, using initial bonding strength, endurance bonding strength, and gel strength as evaluating indicators, and to validate the optimal formulation. Modified Franz diffusion cells were used to study the in vitro release and transdermal absorption of osthole in the HC. Results: The matrix formulation of HC was as follows: NP700 6.97 g, aluminum glycinate 0.30 g, tartaric acid 0.25 g, glycerin 35.00 g, PVP K90 3.87 g, water 43.61 g, and Hanbishu liquid extract 10 g. Cumulative release rate of osthole in HC was (63.30 ± 0.05)% in 24 h. The percutaneous penetration rate of osthole was 0.16 μg/(cm2∙h) and the 24 h permeated amount was (3.61 ± 0.32) μg/cm2. Conclusion: The optimal prescription of HC optimized by D-optimal mixture design has good adhesion and formability. In vitro release characteriistics of osthole in HC conform to the first dynamical equation, and the transdermal absorption behavior is a zero-order kinetics.
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Objective: Through the studies on pilot production of the cataplasma of Chinese materia medica (CMM) containing volatile oil, to provide a rational and feasible preparation technology for the pilot production of CMM cataplasma, so as to promote the development of CMM cataplasma. Methods: The CMM containing volatile oil was extracted by steam distillation method (SDM), ethanol reflux extraction (ERE), and CO2 supercritical fluid extraction (SFE), respectively. The extracts were prepared to cataplasma in order to investigate the effects of extracting methods on the preparation process and quality of CMM cataplasma. The effects of micellar solubilization in the distilled liquid of STM on the quality of cataplasma such as adhesiveness, flexibleness, and stability were also investigated. Results: There was the significant difference among the groups of STM, ERE, and SFE on the quality of cataplasma. The extract by STM was beneficial to the preparation process and enhancement of the quality of cataplasma obviously, while the distilled liquid by STM would cause some limitations such as oil-water separation and volatile oil volatilization losses, which could contribute to obvious difference among batches. These disadvantages by STM would be overcome by the adoption of micellar solubilization technology and the stability would be increased (P < 0.01); segregation happened for the extract by ERE at room temperature, thereby, the water bath heating was needed in the preparation; this characteristics would cause the homogeneous appearance of cataplasma due to some black spots, lower flexibleness of matrix, and the preparation was not easy to control; the extract by SFE contained a lot of impurity of grease and performed half solid. As a result, it was very difficult to blend the extract by SFE with other materials uniformly, the adhesive force of cataplasma was also reduced. In addition, the cost of higher energy consumption and production was another disadvantage for SFE. Conclusion: The STM followed by micellar solubilization would be a feasible preparation technology for the pilot production of CMM cataplasma containing volatile oil, so it is worth popularizing and applying widely.
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[Objective] The aim of this study is to investigate the mechanism and curative effect of cataplasma of Artemisia Argyi by supercritical CO 2 fluid extraction to rat weight, foot swel ing, interleukin-1β, interleukin-17 and tumor necrosis factor-αin the adjuvant arthritis rat models;and afford theoreti-cal evidence for clinical work.[Methods]50 healthy male SD rats were randomly divided into 5 groups:Control group, Model group, Low-dose treatment group, Medium-dose treatment group, High-dose treatment group. Model and al treatment goups took CFA for model ing. After establishing animal models of AA rats, the first group and second group used cataplasm without active drug ingredients. Other groups were given treatment according to dif-ferent drug doses. Assess the joint swel ing degree at different times. Measure the arthritic index and rat weight in two weeks. After 21 days ,detect the cy-tokines level of IL-lβ,IL-17 and TNF-α from the rat's serum and examine the pathological changes of joint observed by HE . [Results]Cataplasma of Artemisia Argyi by supercritical CO2 fluid extraction can significantly reduce rat foot swel ing of the ankle joint pathology ,reduce arthritis score and slow down the weight loss,meanwhile,effectively improve the general daily behavior of rats. The standard of IL-1β,IL-17,TNF-α in serum can be decreased by cataplasma of Artemisia Argyi by supercritical CO2 fluid extraction. The pathological result showed: in the treatment group,the rats synovial hyperplasia the vesselwing reduced, the inflammatory cel infiltration was more decreased than the model group. [Conclusion]The result showed that the cataplasma of Artemisia Argyi by supercritical CO2 fluid extraction had an obvious effect in treating RA. The mechanism was probably that it regulated the immune dis-order of RA.
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This study was aimed to observe the analgesia of curing-injury Cataplasma and discuss the Nav1 . 7 expression in dorsal root ganglion ( DRG ) in model rats with formaldehyde-induced inflammatory pain . A total of 36 Sprague-Dawley rats were divided into three groups, which were the blank control group (n = 12), model group ( n = 12 ) , and treatment group ( n = 12 ) . The blank control group was without any treatment . The model group was injected with 0 . 1 mL 5% saline formalin on the left rear foot . The treatment group was applied with curing-injury Cataplasma on the left rear foot 24 h before the injection of 0 . 1 mL 5% saline formalin in the establishment of animal model . The behavior reactions to pain of model rats were observed . Dubuisson score was recorded and compared . Meanwhile , L3-6 DRG was collected from rats in each group . The expres-sion of Nav1 . 7 was detected by real-time quantitative PCR and western blot . The results showed that the pain reaction integral in the treatment group was lower than the model group ( P < 0 . 05 ) . Results from the real-time quantitative PCR showed that the relative expression of Nav1 . 7 mRNA in the model group was more than the treatment group . And the relative expression of Nav1 . 7 mRNA in the treatment group was more than the blank control group . There was significant difference among three groups ( P < 0 . 05 ) . There was no statistical difference at the three time points within three groups. Results from the western blot showed that the relative expression of Nav1 . 7 in the model group was more than the treatment group . And the expression of Nav1 . 7 in the treatment group was more than the blank control group . There was significant difference among three groups (P < 0.05). There was no statistical difference at the three time points within three groups. It was concluded that the curing-injury Cataplasma can alleviate inflammatory pain response in rats, and have certain analgesia effect . Meanwhile , it can influence Nav1 . 7 expression in DRG in model rats with formaldehyde-induced inflam-matory pain .
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Objective To compare the rapeutic effects of different acupoint combination applied with Rheumatoid Arthritis Cata-plasma on nuclear factor-? ? expression of CIA rats. Methods Induced arthritis rats back were endermic injected with type Ⅱ bovine collogen as animal models. There were five groups for comparison. NF-? ?, interleukin-1? (IL-1?) and tumor necrosis factor-? (TNF-?) of synovial cell clear supernatant liquid were observed. Results NF-? ?, IL-1? and TNF-? scores in therapy groups were steped down. The scores of systematic selection (distant and near coordination) of acupoints was the most close to normal group. Conclusion Rheumatoid Arthritis Cata-plasma can down-regulation the expression of nuclear factor-?? and correlated cell factor density of CIA rats synovial cell and repress positive feedback. Therapeutic effect of distant and near coordination of acupoints is better than distant selection and local selection of acupoints, probably by treating appearance and substance simultaneously to multitarget effect.
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Objective: To optimize a preparation technology for pyretic arthralgia cataplasma. Methods: The preparation technology were studied by a uniform design experiment in which NP-700, tartaric acid, PVP, dihydroxyaluminum aminoacetate, glycerol, water and medicinal powder were factors and viscosity, infiltration, gel mobility and gel strength were indices. Results: The best ratio of this cataplasma matrix was NP-700:tartaric acid:PVP:dihydroxyaluminum aminoacetate: glycerol:water:powder = 4.0:0.2:1.0:0.1:25.0:35.0:2.0. According to optimized formula, to prepare the poultice, then to spread the poultice uniformly onto non-woven fabrics, cover CPP membrane and pack after 1 week at room temperature. Conclusion: Pyretic arthralgia cataplasma was well moldable and its process technology was feasible.
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Objective To study the effects on electroporation of Qingfengteng cataplasma transdermal absorption and describe the characteristics of animal pharmacokinetics of it.Methods Two-chamber diffusion cell was used and the plasma drug concentration was determined by HPLC.The application of AIC theory to analysis of the compartmentally based model of sinomenine transdermal delivery by electroporation.Results The Cmax,Ka,and AUC0→∞ of electroporation was larger than those of passive diffusion;t1/2(Ka)and tmax of electroporation were reduced compared with passive diffusion.The drug concentration-curve equation were C=2.884?(e-0.056 t-e-0.232 t)and C=2.512?(e-0.058 t-e-0.149 t)for electroporation and passive diffusion,respectively.Conclusion The change of in vivo drug concentration of Qingfengteng calaplasma transdermal absorption by electroporation could be analized in accordance with mammillary one-compartment open model.The etrectroporation technology could sharply enhance the bioavalibility compared with the passive diffusion.
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AIM:To study the prepartion of Ruanganxiaoshui Cataplasma and it's percutaneous absorption in vitro as well as dissolvability in vitro. METHODS: In the experiment,orthogonal test was used to optimize the preparation.Meanwhile,with the help of azole and propylene alcohol the percutaneous absorption of ginsenoside Rg_1 from the cataplasma carriers in vitro was determined by Franz's diffusion cell and HPLC,as well as dissolution rate in vitro. RESULTS: The percutaneous absorption rate of ginsenoside Rg_1 through rat skin in vitro was 0.394 ?g/cm~2/h.And the dissolution process fitted to first order model. CONCLUSION: The Cataplasma carriers possess a good drug dissolution property.To add compound penetration enhancers is one of the effective methods for raising percutaneous absorption.
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OBJECTIVE:To prepare Xiaozhong zhitong cataplasma,establish a method for its quality control and to observe its clinical efficacy on orthopedic patients(30 cases).METHODS:Based on the precompounded prescription order of Xiaozhong zhitong powder with water soluble polymer substance as base material which were evenly mixed with the drug extractives before being applied on non-woven fabric to prepare Xiaozhong zhitong cataplasma.The clinical efficacy was compared between the trial group(Xiaozhong zhitong cataplasma) and the control group(Xiaozhong zhitong powder).RESULTS:The prepared Xiaozhong zhitong cataplasma had smooth surface and uniform thickness,with a satisfactory stability achieved within 3 months at a dosage of 0.715 6 g?100 cm-2.The total effective rate in the trial group(93.3%) was significantly higher than in the control group(76.7%)(P