9 4 3 6 4
论文已发表
注册即可获取德孚的最新动态
IF 收录期刊
- 3.3 Breast Cancer (Dove Med Press)
- 3.4 Clin Epidemiol
- 2.5 Cancer Manag Res
- 2.9 Infect Drug Resist
- 3.5 Clin Interv Aging
- 4.7 Drug Des Dev Ther
- 2.7 Int J Chronic Obstr
- 6.6 Int J Nanomed
- 2.5 Int J Women's Health
- 2.5 Neuropsych Dis Treat
- 2.7 OncoTargets Ther
- 2.0 Patient Prefer Adher
- 2.3 Ther Clin Risk Manag
- 2.5 J Pain Res
- 2.8 Diabet Metab Synd Ob
- 2.8 Psychol Res Behav Ma
- 3.0 Nat Sci Sleep
- 1.8 Pharmgenomics Pers Med
- 2.7 Risk Manag Healthc Policy
- 4.2 J Inflamm Res
- 2.1 Int J Gen Med
- 4.2 J Hepatocell Carcinoma
- 3.7 J Asthma Allergy
- 1.9 Clin Cosmet Investig Dermatol
- 2.7 J Multidiscip Healthc
已发表论文
降低刺激性微乳罗替戈汀凝胶：配方优化和在体外和体内的研究
Authors Wang Z, Mu HJ, Zhang XM, Ma PK, Lian SN, Zhang FP, Chu SY, Zhang WW, Wang AP, Wang WY, Sun KX
Published Date January 2015 Volume 2015:10 Pages 633—644
DOI http://dx.doi.org/10.2147/IJN.S74079
Received 11 September 2014, Accepted 1 November 2014, Published 14 January 2015
Background: Rotigotine is a potent and selective D1, D2, and D3 dopaminergic receptor agonist. Due to an extensive first-pass effect, it has a
very low oral bioavailability (approximately 0.5% in rats).
Purpose: The present investigation aimed to develop a microemulsion-based hydrogel for transdermal rotigotine delivery with lower application site reactions.
Methods: Pseudoternary phase diagrams were constructed to determine the region of oil in water (o/w)-type microemulsion. Central composite design was used to support the pseudoternary phase diagrams and to select homogeneous and stable microemulsions with an optimal amount of rotigotine permeation within 24 hours. In vitro skin permeation experiments were performed, using Franz diffusion cells, to compare rotigotine-loaded microemulsions with rotigotine solutions in oil. The optimized formulation was used to prepare a microemulsion-based hydrogel, which was subjected to bioavailability and skin irritancy studies.
Results: The selected formulations of rotigotine-loaded microemulsions had enhanced flux and permeation coefficients compared with rotigotine in oil. The optimum microemulsion contained 68% water, 6.8% Labrafil®, 13.44% Cremophor® RH40, 6.72% Labrasol®, and 5.04% Transcutol® HP; the drug-loading rate was 2%. To form a microemulsion gel, 1% Carbomer 1342 was added to the microemulsion. The bioavailability of the rotigotine-loaded microemulsion gel was 105.76%±20.52% with respect to the marketed rotigotine patch (Neupro®). The microemulsion gel irritated the skin less than Neupro.
Conclusion: A rotigotine microemulsion-based hydrogel was successfully developed, and an optimal formulation for drug delivery was identified. This product could improve patient compliance and have broad marketability.
Keywords: pseudoternary phase diagrams, central composite design, transdermal
Purpose: The present investigation aimed to develop a microemulsion-based hydrogel for transdermal rotigotine delivery with lower application site reactions.
Methods: Pseudoternary phase diagrams were constructed to determine the region of oil in water (o/w)-type microemulsion. Central composite design was used to support the pseudoternary phase diagrams and to select homogeneous and stable microemulsions with an optimal amount of rotigotine permeation within 24 hours. In vitro skin permeation experiments were performed, using Franz diffusion cells, to compare rotigotine-loaded microemulsions with rotigotine solutions in oil. The optimized formulation was used to prepare a microemulsion-based hydrogel, which was subjected to bioavailability and skin irritancy studies.
Results: The selected formulations of rotigotine-loaded microemulsions had enhanced flux and permeation coefficients compared with rotigotine in oil. The optimum microemulsion contained 68% water, 6.8% Labrafil®, 13.44% Cremophor® RH40, 6.72% Labrasol®, and 5.04% Transcutol® HP; the drug-loading rate was 2%. To form a microemulsion gel, 1% Carbomer 1342 was added to the microemulsion. The bioavailability of the rotigotine-loaded microemulsion gel was 105.76%±20.52% with respect to the marketed rotigotine patch (Neupro®). The microemulsion gel irritated the skin less than Neupro.
Conclusion: A rotigotine microemulsion-based hydrogel was successfully developed, and an optimal formulation for drug delivery was identified. This product could improve patient compliance and have broad marketability.
Keywords: pseudoternary phase diagrams, central composite design, transdermal
