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OBJECTIVE:To optimize formulation matrix of processed Aconitum carmichaelii hydrogel patch,and to investigate its in vitro drug release.METHODS:The ratio of NP700,dihydroxyaluminum aminoacetate,tartaric acid and PVP K90 in processed A.carmichaelii hydrogel patch matrix was optimized by central composite design-response surface method (CCD-RSM) with initial adhesion,peel strength and sensory evaluation as evaluation indexes.The modified Franz diffusion cell method was used for in vitro drug release test processed A.carmichaelii hydrogel patch using accumulative release amount of six ester type alkaloids benzene [benzoyl mesaconine (BM),benzoyl aconitum (BA),benzoylhy paconine (BH),mesaconitine (MT),hypaconitine (HT) and aconitine (AT)] as evaluation indexes.RESULTS:The optimal matrix formulation was NP700-dihydroxyaluminum aminoacetate-tartaric acid-PVP K90 (1.72 ∶ 0.10 ∶ 0.02 ∶ 1.65,m/m/m/m).In validation test,the contents of six ester type alkaloids were 52.77,28.52,28.78,8.81,8.75,8.21 μg/g(RSD＜5％,n=3),comprehensive score was 118.67 ± 1.33 (RSD=4.62％,n=3).The release behavior of BM in vitro conformed to the Higuchi equation.The release behaviors of other 5 alkaloids were consistent with the Higuchi equation.12 h accumulative release amounts of BM,BA,BH,MT,HT and AT were 12.04,2.95,3.55,2.64,2.48,1.97 μg/cm2,respectively.CONCLUSIONS:The processed A.carmichaelii hydrogei patch prepared by matrix prescription is good in appearance,adhesion and in vitro release.The research can provide a basis for the development of new dosage form of processed A.carmichaelii.
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Objective To study preparation of micronized Shuanghuangpo hydrogel patch and its characteristics of transdermal penetration in vitro. Methods Micronized Shuanghuangpo hydrogel patch was prepared with some macromolecular water-soluble materials as gel base.The content of berberine was determined by HPLC method.Its transdermal penetration in vitro was determined according to the method of Chinese Pharmacopoeia 2010 edition. The rat skin penetration test in vitro was performed by modified Franz diffusion cell method. Results The hydrogel patch had constant content of berberine. Its release property in vitro conformed to Higuchi equation. The penetration of berberine in the hydrogel patch through the rat skin followed zero-order dynamics in 12 h.Its release rate was 7.934μg??(cm2)-1??h1/2 and percutaneous rate was 0.571μg??(cm2)-1??h-1. Conclusion The micronized Shuanghuangpo hydrogel patch is a new transdermal agent with sustained release property.
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To prepare Sanqi Hydrogel Patch used for setting a bone and study its transdermal permeation properties in vitro. In this paper, the appearance description, initial bonding strength, endurance bonding strength, and peel strength were taken as indexes. Based on the result of a single factor experiment, the formula for the Sanqi Hydrogel Patch was optimized by central composite design-response surface methodology. Franz diffusing cells method was chosen to study its transdermal permeability in vitro with asperosaponin VI, ginsenoside Rg1, ginsenoside Rb1, and notoginsenoside R1 as index components. The optimal ratio of the prescription was as follows: ViscomateTM NP700-Carbomer 940-PVPK90-kaoline-dihydroxyaluminum aminoacetate (1.86∶1.48∶0.49∶0.5∶0.16). Within 24 h, the transdermal rates of asperosaponin VI, ginsenoside Rg1, ginsenoside Rb1, and notoginsenoside R1 were 1.868, 4.233, 1.149, and 1.558 μ g/(cm2∙h). Sanqi Hydrogel Patch has a better release and transdermal properties and the transdermal actions are consistent with zero-order kinetics.
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Objective: To optimize the prescription of Baoxieling Hydrogel Patch (BHP) using Box-Behnken test design and to investigate its transdermal absorption properties in vitro. Methods: Taking the comprehensive scores of the early adhesion, uniformity, ductility, consistence, skin adhesive ability, repeated exposing paste, and residue as response values, Box-Behnken test design was used to optimize the amounts of sodium polyacrylate NP 800, aluminum glycinate, and fillers, and to validate the optimal formulation. The percutaneous permeation of cinnamaldehyde, eugenol, evodiamine, and rutaecarpine in the optimal formulation was studied by in vitro transdermal delivery experiment with Franz diffusion cells and their contents were determined by HPLC. Results: The optimal ratio of the prescription was as follows: sodium polyacrylate NP 800-aluminum glycinate-fillers (0.82:0.02:1.56). The foremost factors were fillers and aluminum glycinate. Its transdermal absorption met zero order dynamic process. Conclusion: The optimal prescription has uniform paste, suitable consistence, easy ductility, moderate adhesion, and perfect transdermal effect. It could provide the foundation for the development of new prescription of Baoxieling.
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Objective: To explore the preparation method of glycyrrhetinic acid ethosome (GAE) hydrogel patch and to evaluate its characteristics during in vitro transdermal drug delivery. Methods: GAE was prepared by ethanol infusion method, and its entrapment efficiency, size and surface potential were investigated. Then GAE was used to prepare the hydrogel patch. The amount of penetrated glycyrrhetinic acid was determined by HPLC on modified Franz diffusion cells, and then the in vitro transdermal drug delivery of the prepared hydrogel patch was evaluated. Results: GAE had a spherical or ellipsoidal appearance and a layered structure, with an encapsulation efficiency of (75.63 ± 1. 86)%, a particle size of (106.2 ± 20.54) nm, and a surface potential of (- 41.3 ± 2.8) mV. The percutaneous delivery rate and accumulative infiltration quantity of GAE hydrogel patch were significantly higher than those of glycyrrhetinic acid hydrogel patch. The 24 h accumulative infiltration quantity of GAE hydrogel patch was 5.55 times that of the glycyrrhetinic acid hydrogel patch (t-test, P<0.01). Conclusion: Compared with glycyrrhetinic acid, GAE can significantly improve the in vitro transdermal delivery of hydrogel patch, demonstrating that ethosome hydrogel patch might be an ideal vector for transdermal delivery of glycyrrhetinic acid.
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OBJECTIVE: To prepare Nimodipine hydrogel patch and to investigate the effects of different factors on the in vitro percutaneous permeability of nimodipine.METHODS: Nimodipine hydrogel patch was prepared with sodium carboxymethylcellulose as matrix.The permeation flux of nimodipine through excised mice skin in vitro was determined using Franz diffusion cell.The content of nimodipine was measured by HPLC.Accumulative transdermal delivery of nimodipine(Q) and transdermal speed constant(Js) were calculated.The loading amounts,type of transdermal enhancer(menthol,azone and oleic acid) and their content were optimized with the value of Q and Js as index.RESULTS: The best loading amount was 4 mg?cm-2.Different transdermal enhancers were found to increase the percutaneous permeability of nimodipine.5% oleic acid had the best penetration enhancing effect.The permeation of samples containing 5% oleic acid was in accordance with the zero-order kinetics.Nimodipine hydrogel transdermal patch presented high Js of 28.10 ?g?cm-2?h-1 and Q of 342.58 ?g?cm-2 in 12 h.CONCLUSION: Nimodipine hydrogel patch has good potential for transdermal delivery.
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Objective Using the effect of microneedle array to investigate the feature and rule of transdermal drug delivery of sinomenine hydrogel patch.Methods The microneedles with different length and sinomenine hydrogel patch were prepared;The isolated rat skin was pretreated by different needle-shapes of microneedle array and different timepoints with the same needle-shape,and then sticked the sinomenine patch.The permeation rates of sinomenine were studied using a Franz diffusion cell and compared with passive diffusion of the rat skin untreated.Sinomenine content was measured by HPLC.Results The permeation rates of sinomenine via the skin pretreated with 100 and 200 ?m microneedles were 40.7 and 52.4 times to those of the untreated.The permeation rates of sinomenine via the skin pretreated 7 min with 200 ?m microneedles is 142.0 times to those of the untreated.When skins were pretreated using 200 ?m microneedles with different force, the drug permeation rates were increased with the force increasing.When the force exceeded 5 N,the drug permeation rates were equilibrium.Conclusion When transdermal drug delivery by using microneedle array-hydrogel patch,the permeation rates increase significantly.The needle-shape,skin pretreating time,and force of the microneedles play the important roles in the transdermal drug delivery.