OBJECTIVE  To optimal the prescription of Hu Li San Gel(HLS-G) and evaluate it in vitro, as well as to evaluate its anti-inflammatory and analgesic effects.

METHODS The HLS-G formulation was optimized using orthogonal tests with viscosity, spreadability, greasiness, endpoint water loss and stability as indicators. Solubility, moisture and rheological properties were also evaluated. The effects of azone(AZ), propylene glycol(PG) and menthol(MT) on the expression of lobetyolin(LOB), notoginsenoside R1(NG-R1), ginsenoside Rg1(G-Rg1), 8-deacetyl yunaconitine(8D-YNA), yunaconitine(YNA), and ginsenoside Rb1(G-Rb1) were investigated for in vitro percutaneous permeation, and the best the optimal permeation promoter was selected. The anti-inflammatory and analgesic effects of HLS-G were further evaluated using the mouse auricular swelling model and the acetic acid torsion model.

RESULTS The preferred HLS-G formulation was carbomer 940 0.9 g, pH 7.0 and glycerol 6.0 g with good swelling, moisturising and rheological properties. The preferred optimum osmotic promoter was 5% PG, and the 24 h cumulative osmolality of the six compositions was (214.02±0.04), (447.94±0.08), (183.50±0.03), (31.38±0.10), (21.18±0.12) and (657.42±0.05) μg·cm⁻², respectively. Meanwhile, HLS-G significantly inhibited xylene-induced ear swelling in mice and reduced serum levels of inflammatory factors IL-6, IL-1β and TNF-α in mice; at the same time, it was able to prolong the latency period of acetic acid-induced writhing, reduce the number of writhings and reduce serum levels of PGE₂, 5-HT and IL-1β in mice.

CONCLUSION The optimized HLS-G has good transdermal permeability and anti-inflammatory and analgesic activity, which provides a basis for the development of HLS into a topical preparation and an idea for the secondary development of ethnomedicine.