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Research Article

The effect of ion-pair formation combined with penetration enhancers on the skin permeation of loxoprofen

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Pages 1550-1557 | Received 09 Sep 2014, Accepted 25 Oct 2014, Published online: 11 Nov 2014

Figures & data

Figure 1. Structures of loxoprofen (A) and its active metabolite (B).

Figure 1. Structures of loxoprofen (A) and its active metabolite (B).

Figure 2. Effect of various organic amines on in vitro permeation of LOXO across the rabbit skin from IPM (n = 4).

Figure 2. Effect of various organic amines on in vitro permeation of LOXO across the rabbit skin from IPM (n = 4).

Table 1. Permeation parameters of LOXO with and without organic amines in IPM through rabbit skin and corresponding physicochemical properties (n = 3 or 4).

Figure 3. Relationship between the log Ko/w of LOXO with organic amines and ER values.

Figure 3. Relationship between the log Ko/w of LOXO with organic amines and ER values.

Figure 4. Relationship between the log Ko/w of LOXO with organic amines and log Ko/w of organic amines.

Figure 4. Relationship between the log Ko/w of LOXO with organic amines and log Ko/w of organic amines.

Figure 5. Infrared spectra of LOXO with or without equimolar amines in CHCl3.

Figure 5. Infrared spectra of LOXO with or without equimolar amines in CHCl3.

Figure 6. Effect of various organic amines on in vitro permeation of LOXO across the rabbit skin from PSA (n = 4).

Figure 6. Effect of various organic amines on in vitro permeation of LOXO across the rabbit skin from PSA (n = 4).

Table 2. Permeation parameters of LOXO with and without organic amines in PSA through rabbit skin (n = 4).

Figure 7. Effect of LOXO–TEA combination with penetration enhancers on the permeation through rabbit skin from PSA (n = 4).

Figure 7. Effect of LOXO–TEA combination with penetration enhancers on the permeation through rabbit skin from PSA (n = 4).

Figure 8. Effects of different concentration of IPM on percutaneous absorption of LOXO–TEA patch compared with the LOXONA® plaster (n = 4).

Figure 8. Effects of different concentration of IPM on percutaneous absorption of LOXO–TEA patch compared with the LOXONA® plaster (n = 4).

Table 3. The permeation parameters of LOXO–TEA with various enhancers (n = 3 or 4).

Table 4. The permeation parameters of LOXO–TEA with different concentration of IPM, compared with the listed LOXONa® plaster (n = 3 or 4).

Figure 9. The profiles of swelling degree (%) of different groups in the experiment of adjuvant induced arthritis in rats (A) left side; (B) right side.

Figure 9. The profiles of swelling degree (%) of different groups in the experiment of adjuvant induced arthritis in rats (A) left side; (B) right side.

Table 5. The result of analgesic effect of LOXO patch on the pain induced by acetic acid in mice (mean ± SD, n = 10).

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