ABSTRACT
Objective To investigate the preparation process of Kucha gynecological gel and prepare a temperature-sensitive in situ gel capable of rapid phase change in vagina. Methods Poloxamer P188 and Poloxamer P407 were used as gel matrix, Lactic acid and sodium lactate were used as the acid buffer solution. The central composite design was performed to optimize the prescription and technology, and the gelation temperature (GT), gelation time, and the effects of different acid buffer solutions on GT, gel stability, and related rheological properties were determined. Results Within a certain concentration range, the gelation temperature was gradually increased with the increase of poloxamer 188 concentration, and the gelation temperature was gradually decreased with the increase of poloxamer 407 concentration, and the optimized prescription by central composite design was poloxamer P188 with a concentration of 3.51% and poloxamer P407 with a concentration of 17.16%. The addition of different buffers has a deviation of 5% of the gelation temperature of the gel in vitro, but the variation in the vaginal fluid is large. The gelation temperatures of the citric acid-sodium citrate buffer and the lactic acid-sodium lactate buffer solution in the vaginal fluid were 68.5 ℃ and 35.8 ℃, respectively, and the rheological data showed that the gel retained better in vivo. Conclusion The Kucha gynecological gel preparation corresponded with the model employed by central composite design, and the screened process can prepare situ gels with good retention and stable properties.
ABSTRACT
<p><b>OBJECTIVE</b>To prepare colon-targetting tablets of total alkaloids of Sophora alopecuroides and evaluate the effect of pectins of different degree of esterification (DE) on sophoridine release profiles in-vitro.</p><p><b>METHOD</b>Wet granulation technique was employed to prepare petin-based matrix tablets, then tablets were coated the optimal formulation with Kollicoat MAE 30 DP based on the optimal formulation and analysed their release.</p><p><b>RESULT</b>Coated formulation E could target total alkaloids of S. alopecuroides to colon and various DE of pectin exerted different effects on sophoridine release. The release of low DE pectin-based matrix tablets coating with Kollicoat MAE 30 DP approximatedly fitted zere-order eqution, which was erosion depended.</p><p><b>CONCLUSION</b>Low DE pectin-based matrix tablet coating with Kollicoat MAE 30 DP can deliver sophoridine to colon, hence improve the effectiveness of sophoridine.</p>