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OBJECTIVE: To optimize the formulation of citalopram hydrobromide (CTH ) thermosensitive nasal gel and further evaluate its in vitro properties. METHODS: With gelling temperature and gelling time as evaluating indexes, central composite design-response surface and single factor experimental design method were used to optimize the formulation of CTH thermosensitive nasal gel by using poloxamer 407(F127) and carbomer 940 (CP940) as gel materials. Meanwhile, nasal mucosa permeation enhancer for CTH was then sieved by using Franz diffusion cell and ex vivo sheep nasal mucosa as experimental model. Finally, CTH thermosensitive nasal gel was prepared with cold method and then its in vitro properties was evaluated. In vitro cumulative erosion and cumulative release rate of the drug thermosensitive nasal gel were investigated by membrane-free dissolution method and dialysis membrane method, respectively. Moreover, the effect of temperature and pH on the viscosity of the drug nasal gel formulation was also evaluated. RESULTS: The optimal formulation of the thermosensitive nasal gel consisted of CTH 8.0%, F127 20.27%, CP940 0.17%, DM-β-CD 3.0%, ethylparaben 0.05% and distilled water. The gelling temperature, gelling time and pH of the drug thermosensitive nasal gel were found to be about 32.5 ℃,42 s and 5.0, respectively. The in vitro cumulative erosion and cumulative release percentage were both greater than 90% in 55 min and furthermore there was good linear correlation between these two parameters (r=0.998 6). Additionally, in vitro cumulative release of the drug from the gel formulation was determined to be 92% within 8 h, which conformed to Higuchi kinetic equation. Furthermore, the viscosity of the drug nasal gel was influenced by temperature as well as pH in different extent. CONCLUSION: The optimized formulation of the CTH thermosensitive nasal gel with central composite design-response surface method and single factor design method shows suitable gelling temperature, gelling time, pH value for nasal preparation and obvious in vitro drug sustained release characteristics.
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Aim To study the therapeutic effect of re-combinant human acidic fibroblast growth factor (rh-aFGF) carbomer 940 gel in the treatment of skin wound healing in type I diabetic rats. Methods Two types of skin trauma models, namely, full-thickness wound and scalded wound,were established in a model of type I diabetes mellitus using STZ-induced SD rats. The rats were divided into control group, vehicle group,90 AU rh-aFGF gel group and 270 AU rh-aFGF gel group in each skin wound models. The wound area and wound healing rate were used to evaluate the thera-peutic effect. The growth of fibroblasts, fibrocytes, collagen fibers and vessel capillaries in the wound was observed using HE staining and analysed by semi-quantitative score. Results The rh-aFGF carbomer gel significantly reduced the traumatic area as well as promoted the wound healing rate of the skin trauma model of SD rats of type I diabetes mellitus (P <0.05). HE staining showed that rh-aFGF carbomer gel significantly promoted the pathological score of fibro-blasts and collagen fibers(P<0.05). Conclusions rh-aFGF carbomer gel might play a protective role in micro-environment of wound and rh-aFGF, which could benefit for proliferation of fibroblasts and colla-gen, therefore promoting the healing process of skin wound in SD rats with type I diabetes mellitus, and it might be expected to be a new preparation for the treat-ment of chronic trauma in diabetes mellitus.
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OBJECTIVE:To optimize base material compositions and preparation technology for compound ciprofloxacin gel.METHODS:4factors,ciprofloxacin,carbomer-940,glycerine,triethanolamine(in formula dosages)were selected as variable factors,the stability of the preparation was taken as the index for investigation and table L 9 (3 4 )was used to conduct the orthogonal experiment.RESULTS:The optimum base material composition and technology were the following,ciprofloxacin0.3%,carbomer-9401%,glycerine7.5%,triethanolamine2%.CONCLUSION:The compound ciprofloxacin gel prepared based on the optimized technology is in conformity with the specification stated in Chinese Pharmacopoeia(2000).