AIM: To prepare a complex of hyaluronic acid (HA) and phospholipids (PL), and study the improvement effect of PL on the oral absorption of HA. METHODS: The complex of HA-PL (named Haplex) was prepared by film dispersi...AIM: To prepare a complex of hyaluronic acid (HA) and phospholipids (PL), and study the improvement effect of PL on the oral absorption of HA. METHODS: The complex of HA-PL (named Haplex) was prepared by film dispersion and sonication method, its physico-chemical properties were identified by infrared spectra and differential scanning calorimetry (DSC). The oral absorption of Haplex was studied. Thirty-two healthy rats were divided into 4 groups randomly: (1) a normal saline (NS) control group; (2) an HA group; (3) a mixture group and (4) a Haplex group. After intragastric administration, the concentration of HA in serum was determined. RESULTS: The physico-chemical properties of Haplex were different from HA or PL or their mixture. After Haplex was administered to rats orally, the serum concentration of HA was increased when compared with the mixture or HA control groups from 4 h to 10 h (P < 0.05). The △AUC0-12 h of Haplex was also greater than that of the other three groups (P < 0.05). CONCLUSION: The method of film dispersion and sonication can prepare HA and PL complex, and PL can enhance the oral absorption of exogenous HA.展开更多
Cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally.This work was to mask the bitter taste of CA and enhance its oral bioavailability.Dry suspensions were prepared...Cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally.This work was to mask the bitter taste of CA and enhance its oral bioavailability.Dry suspensions were prepared by means of wet granulation method and solid dispersion method.Binders,suspending agents and other compositions involved in the formulation were optimized.The differential scanning calorimetry(DSC)analysis indicated that CA was amorphous in the solid dispersion with stearic acid as the carrier,which contributed to an improvement of the dissolution rate.Taste evaluation was performed by three volunteers and taste masking was successfully achieved by the methods mentioned above.A pH 7.0 phosphate buffer was adopted to study the in vitro dissolution performance of the three formulations,i.e.,two self-made dry suspensions and the commercial one.With a better release characteristic and a satisfying taste masking ability,the solid dispersion suspension was selected as the optimal formulation for the further pharmacokinetic study in beagle dogs.The values of Cmax and AUC0e12 for the solid dispersion suspension were about 1.78-fold and 2.17-fold higher than these of reference suspension,respectively.The obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability.展开更多
Osteoarthritis (OA) means inflammation of the joints, with the symptoms of joint pain, stiffness, and swelling of the joints. It is a degenerative disease that appears to be caused by both biomechanical and bio-chemic...Osteoarthritis (OA) means inflammation of the joints, with the symptoms of joint pain, stiffness, and swelling of the joints. It is a degenerative disease that appears to be caused by both biomechanical and bio-chemical factors. Intra-articular (IA) injection treatment is one of the main treatment methods for OA because of its positive effect in reducing joint pain and increasing joint mobility. IA injection of xanthan gum (XG) could protect the joint cartilage, relieve the synovitis and reduce the OA progression in experiment OA. The injection of XG may have a long-lasting effect in the joint cavity, which could avoid frequent IA injections. However, for the development of this potential therapy, further studies such as the effective long-term pain relief properties, the detailed action mechanism and the pharmacokinetics of the XG injection will be conducted. This article briefly reviewed the preparation, safety evaluation, pharmacodynamics and possible action mechanism of XG injection, and come up with the ideas for further development of this potential therapy for OA.展开更多
Taking lotus flavones as the research object, cytotoxicity was evaluated by MTT test, inhibitory effects onthe activity of tyrosinase was studied, and DPPH scavenging experiments were carried out. Lotus flavoneswere u...Taking lotus flavones as the research object, cytotoxicity was evaluated by MTT test, inhibitory effects onthe activity of tyrosinase was studied, and DPPH scavenging experiments were carried out. Lotus flavoneswere used in a formula of skin cream and facial whitening effects were examined. Results shows that lotusflavones are exhibited no cytotoxicity at a concentration equal or less than 1%, and it can decrease the activityof tyrosinase at a concentration between 0.02%~0.30%. Lotus flavones can scavenge DPPH radical. The skincream containing lotus flavones declines facial melanin content. Lotus flavones have good biological safety andare suitable in cosmetics as whitening agents.展开更多
Background While intra-articular injection of sinomenine hydrochloride has a therapeutic effect on osteoarthritis, it has a short half-life, and is thermolabile and photolabile. The aim of this research was to evaluat...Background While intra-articular injection of sinomenine hydrochloride has a therapeutic effect on osteoarthritis, it has a short half-life, and is thermolabile and photolabile. The aim of this research was to evaluate the sustained-release of sinomenine hydrochloride from an injectable sinomenine hydrochloride and sodium hyaluronate compound （CSSSI） and its therapeutic effect in a rabbit model of osteoarthritis following intra-articular injection. Methods An injectable compound consisting of 1% sodium hyaluronate and 2.5% sinomenine hydrochloride was prepared and kept as the experiment group, and 2.5% sinomenine hydrochloride was prepared and kept as the control group. The cumulative mass release was measured at different time points in each group in vitro. Sixty-five male Zelanian rabbits were randomly divided into five groups： 15 （30 knees） each for the control, sodium hyaluronate, sinomenine hydrochloride, and CSSSI groups respectively, and five （10 knees） for the modeling group. Papain was injected into both knees of each rabbit for model establishment. Subsequently, 0.2 ml of the corresponding drugs was injected into the articular cavities of the remaining experiment groups, while the control group was treated with 0.2 ml normal saline. All groups were treated once a week for 4 weeks. Seven days after the last treatment, knees were anatomized to perl^orm pathological observations and Mankin＇s evaluation of the synovium. Four groups were compared using the SPSS 13.0 software package. Results In the in vitro sustained-release experiments, 90% of the drug was released in the experiment group 360 minutes following the injection. Comparison of the Mankin＇s evaluations of the four groups illustrated statistical discrepancies （P 〈0.05）. In further paired comparisons of the CSSSI group vs. modeling control/sodium hyaluronate/sinomenine hydrochloride groups, statistical significance was uniformly obtained. Moreover, sodium hyaluronate and sinomenine hydrochloride treatments showed significant improvement over the modeling control （P 〈0.05）, whereas sodium hyaluronate vs. sinomenine hydrochloride comparison failed to reach significance （P 〉0.05）. Conclusions CSSSI has a sustained-release effect on sinomenine hydrochloride. Intra-articular injection of CSSSI was significantly better than the sole sodium hyaluronate or sinomenine hydrochloride for the treatment of osteoarthritis in a rabbit model.展开更多
基金the Natural Science Foundation of Shandong Province, China. No. Y2005C31
文摘AIM: To prepare a complex of hyaluronic acid (HA) and phospholipids (PL), and study the improvement effect of PL on the oral absorption of HA. METHODS: The complex of HA-PL (named Haplex) was prepared by film dispersion and sonication method, its physico-chemical properties were identified by infrared spectra and differential scanning calorimetry (DSC). The oral absorption of Haplex was studied. Thirty-two healthy rats were divided into 4 groups randomly: (1) a normal saline (NS) control group; (2) an HA group; (3) a mixture group and (4) a Haplex group. After intragastric administration, the concentration of HA in serum was determined. RESULTS: The physico-chemical properties of Haplex were different from HA or PL or their mixture. After Haplex was administered to rats orally, the serum concentration of HA was increased when compared with the mixture or HA control groups from 4 h to 10 h (P < 0.05). The △AUC0-12 h of Haplex was also greater than that of the other three groups (P < 0.05). CONCLUSION: The method of film dispersion and sonication can prepare HA and PL complex, and PL can enhance the oral absorption of exogenous HA.
基金the National Nature Science Foundation of China(No.81173008)from Project for Excellent Talents of Liaoning Province(No.LR20110028)from Program for New Century Excellent Talents in University(No.NCET-12-1015).
文摘Cefuroxime axetil(CA)is an ester prodrug of cefuroxime with an unpleasant taste when administrated orally.This work was to mask the bitter taste of CA and enhance its oral bioavailability.Dry suspensions were prepared by means of wet granulation method and solid dispersion method.Binders,suspending agents and other compositions involved in the formulation were optimized.The differential scanning calorimetry(DSC)analysis indicated that CA was amorphous in the solid dispersion with stearic acid as the carrier,which contributed to an improvement of the dissolution rate.Taste evaluation was performed by three volunteers and taste masking was successfully achieved by the methods mentioned above.A pH 7.0 phosphate buffer was adopted to study the in vitro dissolution performance of the three formulations,i.e.,two self-made dry suspensions and the commercial one.With a better release characteristic and a satisfying taste masking ability,the solid dispersion suspension was selected as the optimal formulation for the further pharmacokinetic study in beagle dogs.The values of Cmax and AUC0e12 for the solid dispersion suspension were about 1.78-fold and 2.17-fold higher than these of reference suspension,respectively.The obtained results demonstrated that the solid dispersion can efficiently mask the bitter taste of CA and significantly enhance its oral bioavailability.
文摘Osteoarthritis (OA) means inflammation of the joints, with the symptoms of joint pain, stiffness, and swelling of the joints. It is a degenerative disease that appears to be caused by both biomechanical and bio-chemical factors. Intra-articular (IA) injection treatment is one of the main treatment methods for OA because of its positive effect in reducing joint pain and increasing joint mobility. IA injection of xanthan gum (XG) could protect the joint cartilage, relieve the synovitis and reduce the OA progression in experiment OA. The injection of XG may have a long-lasting effect in the joint cavity, which could avoid frequent IA injections. However, for the development of this potential therapy, further studies such as the effective long-term pain relief properties, the detailed action mechanism and the pharmacokinetics of the XG injection will be conducted. This article briefly reviewed the preparation, safety evaluation, pharmacodynamics and possible action mechanism of XG injection, and come up with the ideas for further development of this potential therapy for OA.
文摘Taking lotus flavones as the research object, cytotoxicity was evaluated by MTT test, inhibitory effects onthe activity of tyrosinase was studied, and DPPH scavenging experiments were carried out. Lotus flavoneswere used in a formula of skin cream and facial whitening effects were examined. Results shows that lotusflavones are exhibited no cytotoxicity at a concentration equal or less than 1%, and it can decrease the activityof tyrosinase at a concentration between 0.02%~0.30%. Lotus flavones can scavenge DPPH radical. The skincream containing lotus flavones declines facial melanin content. Lotus flavones have good biological safety andare suitable in cosmetics as whitening agents.
文摘Background While intra-articular injection of sinomenine hydrochloride has a therapeutic effect on osteoarthritis, it has a short half-life, and is thermolabile and photolabile. The aim of this research was to evaluate the sustained-release of sinomenine hydrochloride from an injectable sinomenine hydrochloride and sodium hyaluronate compound （CSSSI） and its therapeutic effect in a rabbit model of osteoarthritis following intra-articular injection. Methods An injectable compound consisting of 1% sodium hyaluronate and 2.5% sinomenine hydrochloride was prepared and kept as the experiment group, and 2.5% sinomenine hydrochloride was prepared and kept as the control group. The cumulative mass release was measured at different time points in each group in vitro. Sixty-five male Zelanian rabbits were randomly divided into five groups： 15 （30 knees） each for the control, sodium hyaluronate, sinomenine hydrochloride, and CSSSI groups respectively, and five （10 knees） for the modeling group. Papain was injected into both knees of each rabbit for model establishment. Subsequently, 0.2 ml of the corresponding drugs was injected into the articular cavities of the remaining experiment groups, while the control group was treated with 0.2 ml normal saline. All groups were treated once a week for 4 weeks. Seven days after the last treatment, knees were anatomized to perl^orm pathological observations and Mankin＇s evaluation of the synovium. Four groups were compared using the SPSS 13.0 software package. Results In the in vitro sustained-release experiments, 90% of the drug was released in the experiment group 360 minutes following the injection. Comparison of the Mankin＇s evaluations of the four groups illustrated statistical discrepancies （P 〈0.05）. In further paired comparisons of the CSSSI group vs. modeling control/sodium hyaluronate/sinomenine hydrochloride groups, statistical significance was uniformly obtained. Moreover, sodium hyaluronate and sinomenine hydrochloride treatments showed significant improvement over the modeling control （P 〈0.05）, whereas sodium hyaluronate vs. sinomenine hydrochloride comparison failed to reach significance （P 〉0.05）. Conclusions CSSSI has a sustained-release effect on sinomenine hydrochloride. Intra-articular injection of CSSSI was significantly better than the sole sodium hyaluronate or sinomenine hydrochloride for the treatment of osteoarthritis in a rabbit model.
