蜂蜡骨架颗粒的粒度及含蜡量对生物利用度的影响

继承和发扬祖国药剂学的成就,蜂蜡骨架颗粒可以作为口服长效剂型的一种形式,释药缓慢且均衡。颗粒的粒度及含蜡量这两种因素,独立地对生物利用度产生影响,而含蜡量起主要作用。蜂蜡来源方便,特别是食用无害而较国外近年来用作骨架材料的合成高分子物质优越。颗粒的生物利用度较原蜡丸提高很多,对一般的非剧毒药也具有实用意义。     

A new approach for preparing a controlled release ketoprofen tablets by using beeswax

Solid lipid ketoprofen micropellets (SLKM) at different drug/beeswax ratios [(1:1) and (1:2)] were prepared by emulsion congealing technique and then compressed into tablets. Ketoprofen in solid state was incorporated into the melted beeswax at 90 degrees C and the mixture was emulsified in the hot aqueous Tween 80 solution by stirring at a constant rate. The SLKM were obtained by cooling the coarse emulsion down to room temperature and filtering. Drug entrapment efficiency and particle size analysis by laser diffractometry (LD) were determined, and existence of a drug-lipid interaction was investigated by differential scanning calorimetry (DSC) on the SLKM, before being compressed into the tablets by direct compression method. Finally, in vitro release studies were performed and the release kinetics of the waxy tablets were calculated. A commercial ketoprofen retard tablet (reference: Profenid Retard 200 mg) was also examined to compare the release properties. While the data obtained from DSC were indicating absence of drug-lipid interaction in the SLKM, it was determined that 28.62% (+/-2.08), 38.60% (+/-1.91) and 47.00% (+/-1.82) of ketoprofen was released from the tablets containing (1:2) and (1:1) SLKM and Profenid Retard 200 mg in pH 7.4 phosphate buffer solution after 8 h, respectively.     

Arnebin-1 promotes the angiogenesis of human umbilical vein endothelial cells and accelerates the wound healing process in diabetic rats

Ethnopharmacological relevance

Zicao is a traditional wound healing herbal medicine that has been used for several hundred years in China. A survey of the published literatures revealed that arnebin-1, one of the naphthoquinone derivatives, played the most important role in wound healing property of this plant. However, whether arnebin-1 affects angiogenesis in vitro and has an effect on wound healing process in diabetic rats remains enigmatic. To investigate the effect of arnebin-1 with or without VEGF on proliferation, migration and tube formation of HUVECs in vitro and the effect of its topical application in the form of ointment on wound healing in a cutaneous punch wound model of alloxan-induced diabetic rats in vivo.

Materials and methods

The pro-angiogenic functions of arnebin-1 on HUVECs including proliferation, migration and angiogenesis were evaluated through MTT assay, wound healing assay, transwell assay and tube formation assay in vitro. Male Sprague-Dawley rats were injected intraperitoneally with alloxan to induce type ? diabetic rats. Three wounds were created in each rat on the dorsal surface, and then divided to be basement treated, arnebin-1 ointment treated and untreated group correspondingly. The indicators including wound closure rate and histological evaluation were investigated on day 4 and 7 post-wounding.

Results

Without VEGF, arnebin-1 did not affect the proliferation of HUVECs significantly, but had a positive effect on cell migration and tube formation. However, in the presence of minimal VEGF, Arnebin-1 could increase the proliferation, enhance the migration and promote the tube formation of HUVECs significantly. The wound closure rate was increased significantly in arnebin-1 treated group compared to that of untreated and basement treated groups in diabetic rats, and the histological evaluation also showed well organized dermal layer, reduced number of macrophages, increased number of fibroblasts, remarkable degree of neovascularization and epithelization in arnebin-1 treated group.

Conclusion

These findings suggest that arnebin-1 has a pro-angiogenic effect, and a synergetic effect with VEGF promotes the wound healing process in diabetic rats.     

蜂胶除蜡工艺对黄酮类成分含量影响的实验研究

目的 蜂胶除蜡后对蜂胶中黄酮类化合物含量的影响. 方法 选用紫外分光光度法,以芦丁为对照品,测定总黄酮含量. 结果蜂胶除蜡后,有8.5%的总黄酮类成分损失,但胶层与水层中总黄酮量仍大于未除蜡蜂胶的总黄酮量. 结论除蜡对蜂胶中总黄酮量影响不大,在其治疗心脑血管疾病复方制剂开发应用时可作为杂质除去.     

Protective effects of D-002 on experimentally induced gastroesophageal reflux in rats

AIM:To investigate the effects of beeswax alcohols(D-002)on the esophageal damage induced by gastroesophageal reflux(GER)in rats.METHODS:Sixty male rats were randomized into six groups(10 rats/group):a negative control and five groups with experimentally induced GER:a positive vehicle control,three treated with D-002(25,100 and 200mg/kg,respectively),and one with omeprazole 10 mg/kg.All treatments were given by gastric gavage.One hour after dosing,GER was produced by simultaneous ligation of the pyloric end and the forestomach.Esophageal lesions index(ELI),gastric secretion volume and acidity,and esophageal malondialdehyde(MDA)and sulfhydryl(SH)group concentrations were measured.Statistical significance was considered at P<0.05.RESULTS:As compared to the negative control,the positive control group exhibited increased ELI(5.2±0.33 vs 0±0,P=0.0003),gastric secretion volume(2.69±0.09 vs 0.1±0.0,P=0.0003)and acidity(238±19.37 vs 120.0±5.77,P=0.001),and esophageal concentrations of MDA(2.56±0.1 vs 1.76±0.28,P=0.001)and SH groups(1.02±0.05 vs 0.56±0.08,P=0.0003).D-002(25,100 and 200 mg/kg)reduced ELI(3.36±0.31,2.90±0.46 and 2.8±0.23,respectively)vs the positive control(5.2±0.33)(P=0.004;P=0.002;P=0.001,respectively).There were no significant changes in acidity with D-002 treatment,and only the highest dose reduced the volume of the gastric secretion(1.92±0.25)vs the positive control(2.69±0.09,P=0.013).D-002(25,100 and 200 mg/kg)lowered the esophageal MDA(2.05±0.16,1.98±0.22and 1.93±0.22,respectively)(P=0.01;P=0.03;P=0.03,respectively)and SH group concentration(0.87±0.06,0.79±0.08 and 0.77±0.06,respectively)(P=0.04;P=0.04;P=0.02)vs the positive control(2.56±0.10 and 1.02±0.05,respectively).Omeprazole decreased ELI(2.54±0.47),gastric secretion volume(1.97±0.14)and acidity(158.5±22.79),esophageal MDA(1.87±0.13)and SH group(0.72±0.05)concentrations vs the positive control(P=0.002;P=0.001;P=0.02;P=0.003;P=0.002,respectively).CONCLUSION:Acute oral administration of D-002 decreased macroscopic esophageal lesions and oxidative stress in rats with experimentally induced GER,without modifying gastric secretion acidity.     

顶空-气质联用测定黑龙江地产蜂蜡中挥发性成分

目的:研究蜂蜡挥发性成分。方法:采用顶空-气质联用手段进行测定,利用ChemStation、AMDIS、NIST05库相结合的方法对分离得到的化合物进行结构鉴定,应用相对峰面积法计算相对百分含量。结果:分离得到色谱峰34种,确定了其中29种化合物,其中大部分成分在蜂蜡中首次报道。结论:应用顶空气-质联用技术能够全面、便捷测定蜂蜡中挥发性成分。     

The effects of Beeswax,Olive oil and Butter impregnated bandage on burn wound healing

BackgroundBeeswax, Olive oil and Butter (BOB) are nutritive products that could support wound healing by adsorption to bandage. This study demonstrated the therapeutic effects of BOB on second degree burn.MethodsSecond degree burn model was created in rats. Experimental groups were assigned to Healthy, Burn, Silver Sulfadiazine (SS) and BOB. The effects of BOB were evaluated on skin regeneration, vesicles and bullae and fibroblast activity by histopathological analyses and wound contraction percent were determined. Transforming Growth Factor-Beta1 (TGF-β1) and Vascular Endothelial Growth Factor-alpha (VEGF-α) mRNA expressions were analyzed with Real Time-Polymerase Chain Reaction. All parameters analyzed at 3rd, 7th, 14th days.ResultsThe BOB treatment increased TGF-β1 and VEGF-α expressions compared to Burn group. The histopathological analyses showed that epidermis and dermis layers injured due to burn. BOB treatment augmented the regeneration of these layers and increased fibroblast activity and keratinization which are play important role on the new blood vessels production. Also with the BOB treatment we showed wound contraction levels were higher than Burn and SS treatment.ConclusionThis study demonstrated that beeswax–olive oil–butter mixture impregnated bandage treatment in a second-degree burn rat model improved burn wound healing and encouraged skin renewal via modulating tissue TGF-β1 and VEGF-α.     

GC法测定蜂蜡总烷醇中两种烷醇的含量

采用气相色谱法，对蜂蜡主要成分二十八烷醇、三十烷醇进行了含量测定。测定条件为１ｍ×３ｍｍ不锈钢柱，以ＣｈｒｏｍｏｓｏｒｂＷＡＷＤＭＣＳ为填料，１．５％ＯＶ－１７和１．５％ＳＥ－３０为固定相；柱温为２９５℃；进样品、检测器（ＦＩＤ）温度分别为３２０℃。结果表明，方法准确、稳定、重现性好，可作为蜂蜡总烷醇或其制剂的含量测定。     

Clinical and mycological benefits of topical application of honey, olive oil and beeswax in diaper dermatitis

Twelve infants suffering from diaper dermatitis were treated four times daily for 7 days with a mixture containing honey, olive oil and beeswax. The severity of erythema was evaluated on a five-point scale. Three infants had severe erythema and ulceration, four had moderate erythema, and five had moderate erythema with maceration. The initial mean lesion score of 2.91 +/- 0.79 declined significantly (p < 0.05) to 2.0 +/- 0.98 (day 3), 1.25 +/- 0.96 (day 5) and 0.66 +/- 0.98 (day 7). Candida albicans was isolated initially from four patients, but from only two patients after treatment. This topical treatment was safe and well-tolerated, and demonstrated clinical and mycological benefits in the treatment of diaper dermatitis.