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Objective:To study the in vitro transdermal permeability of nifedipine nanoemulsion ( NFNE) containing different per-meation enhancers to lay foundation for the development of transdermal nifedipine preparation. Methods: Franz diffusion cells were used to study the transdermal enhancement of NFNE with different transdermal enhancers ( Azone, oleic acid, TMC20, TMC40, TMC60). Results:The in vitro transdermal effect of NFNE was better than that of nifedipine (NF). The order of in vitro transdermal permeation enhancement was as follows: azone > oleic acid > TMC60 > TMC40 > TMC20, while the water-soluble transdermal permeation enhancers had faster effect. Conclusion:For NFNE, fat-soluble transdermal permeation enhancers have better effect.
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Objective To study the effects of microemulsion/ethosomes on transdermal absorption properties and efficacy of Huoxue Zhitong Cataplasm. Methods The improved Franz diffusion cells were used for the in-vitro permeation experiment with rat skins as the barriers, which was used to evaluate the transdermal absorption properties. In the erxeriment, the contents of paeonol, eugenol and methyl salicylate were used as markers, and detected by ultra performance liquid chromatography to evaluate the transdermal absorption effects. The anti-inflammatory and analgesia activity were evaluated through the writhing plate experiments. Results The cumulative release rate of paeonol in Huoxue Zhitong Cataplasm, Microemulsion Huoxue Zhitong Cataplasm and Ethosomes Huoxue Zhitong Cataplasm were, in order, 65.30%, 61.30%and 60.20%in 24 h;eugenol were, in order, 51.08%, 54.71% and 55.66% in 24 h; methyl salicylate were, in order, 49.20%, 65.17% and 72.15% in 24 h. Furthermore, Microemulsion Huoxue Zhitong Cataplasm high-dose group and Ethosomes Huoxue Zhitong Cataplasm medium-dose group had good effects on reducing the inflammatory exudate of peritoneal capillary and capillary permeability (P<0.05) in animal models. Conclusion Huoxue Zhitong Cataplasm based on microemulsion/ethosomesnano-technology has good transdermal absorption properties and efficacy.
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The purpose of this paper was to study the pre-mixed materials of emulsion gel. Accessories were screened and formula was designed with the most common use, low cost and simple process as the standards. Experiments were designed by central composite design-response surface methodology (ccd-rsm). 8.0.6 Trial Design-Expert was used for data processing and analysis, and subjective scores were used as the index to draw the three-dimensional effect surface and 2D contour maps. It was determined that the optimal ranges were A (carbomer 940)： 0.05-0.065 g; B (castor oil)： 1.00-1.12 mL; C (poly polysorbate-80)： 0.15 mL. The optimal formula was as follows： carbopol 0.057 5 g, castor oil 1.1 mL, polysorbate-80 0.15 mL. The formulated substrate was studied on its preliminary stability and rheology characteristics, such as viscosity and thixotropy. Then with the optimal formula as substrate, emulsion type gel was prepared respectively with 98% rutin, 98% berberine hydrochloride, and 98% berbamine hydrochloride as the main component. With 0.9% normal saline as the absorption solution, the results showed that the ransdermal flux of the three formulations of 1 h was all less than 1%. The results indicated that this substrate had the potential to be developed into a premixed material. The emulsion type gel matrix made from this formula had a good appearance, stability to certain extent, appropriate viscosity and thixotropy, and showed no skin irritation in 1 h.
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Objective To optimize the formulation of Dihydroartemisinin ointment and study its characteristics of penetration enhancers.Method A method of transdermal experiment in vitro was established for DHA.The penetration rate in vitro was examined by HPLC,and coincided the DHA cumulative permeation curve with the Higuchi equation.Result The penetration rate of DHA from DHA ointment made up of water-soluble carbopol and Azone was the highest in all formulations,up to 27.262 ?g/(h?cm2).The cumulative permeation curve which coincided with the Higuchi equation was better.Conclusion The formulation which made up of water-soluble carbopol and Azone was optimized.
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Object To screen the prescriptions of JIUFEN SPRAY Methods Four prescriptions were primarily obtained from 19 prescriptions of JIUFEN SPRAY on the basis of their stability and spraying effect, then the obtained four prescriptions were screened further according to transdermal rate of them Results Prescription 17th was considered to be the best as its high stability, spraying effect and transdermal rate Conclusion The optimal prescription of JIUFEN SPRAY consisted of 20% alcohol solution of sample, 3% borneol and 5% glycerine