白及多糖的制剂开发之路-The development of Bletilla striata polysaccharides pr...

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白及多糖的制剂开发之路

The development of Bletillastriata polysaccharides preparations

白及多糖，又称白及胶，是从兰科植物白及的干燥块茎中提取到的水溶性多糖。白及多糖是多个单糖（α-甘露糖、β-甘露糖和β-葡萄糖）以糖苷键连接而成的聚合物，为白及药材的主要活性成分，具有止血、促进创伤愈合、抑菌、抗溃疡、抗肿瘤等药理活性。同时，白及多糖还是一种天然无毒、无刺激的高分子材料，具有良好生物相容性和生物黏附性，既可作为制剂的主要药物，又可作为药用辅料，具有“药辅合一”的特性，在药物制剂领域开发潜力巨大。

Bletilla striata polysaccharide,also know as Hyacinthbletilla,is a water-soluble polysaccharide extracted from the dried tubers oforchid plant Bletilla striata. Bletilla striata polysaccharide is apolymercomposed of multiple monosaccharides(a-mannose， B-mannose andβ-glucose) connected byglycosidic bonds.It is the main active ingredient of Bletilla striata medicinalmaterials.It has hemostasis,promotes wound healing,and inhibits Antibacterial,anti-ulcer,anti-tumor and other pharmacologicalactivities.At the Same time， Bletillastriata polysaccharide is also a natural non-toxic，non-irritating polymer material with high bio compatibilityand bio adhesiveness.It can be used as the main medicine of preparations and as pharmaceutical adjuvant.Thefeature has great potential for development in the field ofpharmaceutical preparations.

白及多糖作为主药在药物制剂中的应用

Application of Bletilla striata polysaccharide as Main Drugin Pharmaceutical Preparation

乳膏剂

白及多糖可加速创面愈合速度，缩短创面平均愈合时间，提高伤口愈合质量，促进内皮细胞黏附与贴壁生长，并具有一定的抑菌作用，因此可用于外伤的治疗。以当归提取物和白及多糖为主药，采用乳化法制备了用于防治皮肤皲裂的瑰及乳膏。结果表明，瑰及乳膏细腻，涂展性好，成品稳定性良好，皮肤刺激性小，质量稳定可控。临床试验结果显示瑰及乳膏治疗手足皲裂症的临床有效率达91.3%。

Cream Bletilla striata polysaccharide can accelerate wound healingspeed， shorten average wound healing time，improve wound healing quality， promote endothelial celladhesion and adherence to the wall， and has a certain antibacterial effect， soit can be used for the treatment of trauma.Using angelica extract and white andpolysaccharides as the main medicine， anemulsification method was used to prepare rosettes and creams for preventing and treating skin chapped.The results showthat the rose cream is delicate， hasgood spread ability， good stability of the finishedproduct， low skin irritation， andstable and controllable quality.The results of clinical trials showed that the clinical effective rate of Rose and Cream in thetreatment of chapped hands and feet reached 91.3%.

涂膜剂

选用白及多糖、醋酸氯己定、冰片、黄柏、虎杖等为主要药物，羧甲基纤维素钠、甘油为辅料，制备出用于各种烧烫伤、皮肤感染、皮肤溃疡的复方白及涂膜剂。动物实验结果表明，该涂膜剂对于大鼠皮肤热水烫伤、大鼠皮肤水蒸气烫伤和大鼠皮肤明火烧伤模型具有良好的愈合效果。

Coating agent Using white and polysaccharides，chlorhexidine acetate， borneol，cork，polygonum cuspidatum，etc.as the main drugs， sodium carboxymethylcellulose， glycerin as auxiliary materials， the preparation of various burns and scalds， skin infections， skin ulcers compound white and coating Film agent. Animal experimentresults show that the coating agent has a good healing effect on rat skin hotwater scald， rat skin steam scald and rat skin open flame burn model.

洗剂

从白及多糖的止血、促进溃疡愈合的药理作用出发，以白及多糖为主药，乙醇为溶剂，再辅以羧甲基纤维素钠增强缓释效果，制备了用于口腔溃疡的复方白及洗剂，其胶液粘附性高，成膜较好，厚度适中。

lotion Starting from the pharmacological effects of Bletilla striatapolysaccharides to stop bleeding and promote ulcer healing， Bletilla striata  polysaccharides are used as the main medicine，ethanol is the solvent， andcarboxymethylcellulose sodium is supplemented to

enhance the slow-release effect， and a compound  Bletillastriata for oral ulcers is prepared.And lotion， itsglue has high adhesiveness， good film formation andmoderate thickness.

散剂

白及多糖自身具有收敛止血、消肿生肌、保护组织的作用，可用于止血产品的开发。采用冷冻干燥法将白及多糖与改良淀粉进行复合，制备了白及止血粉。经实验结果表明，白及止血粉的止血效果良好，不会引起豚鼠皮肤刺激性和过敏性反应，可以降解完全，具备良好生物相容性。

Powder Bletilla striata polysaccharides have the functions of astringent hemostasis， swelling and muscle growth， and tissue protection， and can be used forthe development of hemostatic products.By freeze-drying method，Bletilla striata polysaccharide andmodified starch were compounded to prepare Bletilla striata hemostaticpowder.Experimental results show that Bletilla striata hemostatic powder has a good hemostatic effect， does not cause guinea pigskin irritation and allergic reactions， can be completely degraded， and has good bio compatibility.

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柔性脂质体

采用薄膜蒸发-超声分散法制备的白及多糖柔性脂质体，包封率大于85%，载药量在12%左右，药物利用率大于55%，很好地解决了由白及多糖较好的水溶性导致的透皮吸收效果较差的问题。

Flexible liposome The flexible liposome of Bletilla striata polysaccharideprepared by thin film evaporation-ultrasonic dispersion method has an encapsulation rategreater than 85%， drug loading is about 12%， and the drug utilization rate is greater than 55%， which is a good solution for Bletilla striata polysaccharides.Theproblem of poor transdermal absorption caused by its water solubility.

口腔黏附片

利用白及多糖的生物黏附性和药理活性，采用冷冻干燥法制备的白及多糖口腔黏附片在实验结果中表明，4%的白及多糖和7%甘油混合制成的口腔黏附片具有优秀的理化特性，该口腔黏附片可促进口腔溃疡模型家兔的口腔黏膜损伤修复。

Oral Adhesive Tablets Taking advantage of the bio adhesive and pharmacologicalactivities of white and polysaccharides， the oral adhesive tablets of white and polysaccharides prepared by freeze-drying methods how that the oral adhesive tablets madeby mixing 4%of white and polysaccharides and 7%glycerin have excellentperformance.Physical and chemical properties， the oral adhesive tablet can promote oral mucosal damage and repair in rabbits with oral ulcers.

白及多糖作为辅料在药物制剂中的应用

The application of Bletilla striata polysaccharide asexcipients in pharmaceutica preparations

凝胶剂的基质

·      以沙棘籽油为原料，白及多糖为凝胶骨架材料，采用高压均质乳化技术使沙棘籽油以微粒形式分散于白及多糖凝胶液中，制成了O/W型凝胶乳剂。实验结果表明，白及多糖促进了沙棘籽油微粒在皮肤上的涂布分散，抑制了油滴的聚集，使其具有良好的涂布性和舒适性。另外，制成凝胶乳剂后可避免沙棘籽油与外界环境接触，从而防止沙棘籽油的氧化变质。

Gel matrix Using seabuckthorn seed oil as the raw material and Bletilla striatapolysaccharide as the gel skeleton material， the seabuckthorn seed oil is dispersed in the Bletilla striatapolysaccharide gel liquid in the form of particles by high-pressure homogeneous emulsification technology to make an O/W gel emulsion.The experimental resultsshowed that Bletilla striata polysaccharides promoted the coating anddispersion of seabuckthorn seed oil particles on the skin， inhibited the aggregation of oil droplets， and made it have good coating properties and comfort.In addition， the gel emulsion can prevent the Seabuckthorn seed oil from contacting the externalenvironment， thereby preventing the seabuckthorn seed oil from oxidative deterioration.

膜剂的成膜材料

·      白及多糖具有良好的物理机械强度和粘附性，是优良的成膜材料。既可单独作为成膜材料，也可与甲壳胺、聚乙烯醇、甲基纤维素钠、海藻酸钠等药用高分子材料复配，制备新型复合膜。尤其通过改变和调整成膜材料的配比和组成后，可灵活控制药物的释放速度，达到缓释和速释的目的。白及多糖和聚乙烯醇结合制成的氢溴酸眼用膜具有缓释作用，可有效减少给药次数，延长药效。将甲基纤维素钠和白及胶制备成双层膜，具有速释的止痛消炎作用。

Film-forming material of film agent Bletilla striata polysaccharide has good physical andmechanical strength and adhesion， and isan excellent film-forming material.It can be used as a film-forming materialalone， or it can be compounded with medicinal polymermaterials such as chitosan， polyvinyl alcohol， sodiummethylcellulose， sodium alginate， etc.to prepare a new type of composite film.Especially by changing and adjusting the ratioand composition of the film-forming materials， the release rate of the drug can be flexibly controlled to achieve the purpose of sustained release and immediaterelease.The hydro b romic acid ophthalmic film made from the combination of Bletillastriata polysaccharide and polyvinyl alcohol has as low-release effect， which can effectively reduce the number of administrations and prolong the drug effect.The sodiummethylcellulose and Bletilla striata gum are prepared into a double-layer film， which has quick-release analgesic and anti-inflammatory effects.

生物黏附制剂的黏附材料

·       白及多糖对胃黏膜有很强的黏附性，在损伤模型大鼠胃内的滞留时间较正常大鼠胃内滞留时间长，其黏附性与白及多糖的浓度呈正相关。将白及多糖细粉与阿莫西林混匀，以PVP乙醇溶液为黏合剂，制备了阿莫西林白及多糖生物黏附缓释胶囊。研究结果表明，白及多糖在体内外均有良好的生物黏附性和功能缓释性，可作为生物黏附制剂和缓释制剂的辅料。

Adhesive materials for bio adhesive preparations Bletilla striata polysaccharide has strong adhesion togastric mucosa.The residence time in the stomach of injured model rats islonger than that of normal rats， andits adhesion is positively correlated with the concentration of Bletillastriata  polysaccharide.The Bletillastriata  polysaccharide powder andamoxicillin were mixed， and the PVP ethanol solutionwas used as the binder to prepare the amoxicillin white and polysaccharide bio adhesive sustained-release capsules.The research resultsshow that Bletilla striata polysaccharides have good bio adhesion and functionalslow-release properties both in vivo and invitro， and can be used as excipients for bio adhesive preparations and sustained-release preparations.

血管栓塞剂的载体材料

·      有研究团队以白及多糖为主要基质，研制了一种用于颅内动脉瘤栓塞的液态栓塞剂，作用于兔颈总动脉侧壁动脉瘤，证明了栓塞剂的可行性。利用这一特性，白及多糖常被用作栓塞剂的基质。通过肝细胞癌大鼠模型证实了白及多糖栓塞剂能够阻断肝癌供血动脉和侧枝循环的功效，能有效抑制肝癌的生长和复发。将白及多糖作为化疗药物丝裂霉素C的载体，制成白及多糖丝裂霉素C混悬剂，进行了犬肾动脉栓塞后的药代动力学研究，发现白及多糖作为药物载体具有缓释效果，是一种新型化疗性栓塞剂。

Carrier material for vascular embolic agents A research team has developed a liquid embolic agent forintracranial aneurysm embolization using Bletilla striata  polysaccharides as the main matrix， which acts on rabbit common carotid artery sidewall aneurysms， proving the feasibility of embolization agents.Taking advantage of this feature， Bletilla striata  polysaccharides are often used as abase forembolic agents.The rat model of hepatocellular carcinoma proved that Bletillastriata  polysaccharide embolizationagent can block the blood supply arteries and collateral circulation of livercancer， and can effectively inhibit the growth andrecurrence of liver cancer.Bletilla striata polysaccharide was used as the carrier of the chemotherapy drug mitomycinC to prepare Bletilla striata polysaccharide mitomycin Csuspension.The pharmacokinetic study aftercanine renal artery embolization was carried out， and Bletillastriata  polysaccharide was found as thedrug carrier It has as low-release effect and is a new type of chemotherapeuticembolic agent.

包合材料

白及多糖是由甘露糖和葡萄糖聚合而成，含有大段的α螺旋结构，具有包合物的基本结构。采用白及多糖包合结构不稳定的有效成分，可增加其稳定性，使药物具有一定的缓释效果。采用水溶液法制备粉末状的白及多糖丹皮酚包合物经实验得出：白及多糖可与丹皮酚形成完整的包合物。

Clathrate material Bletilla striata polysaccharide is formed by the polymerizationof mannose and glucose.It contains a large a-helix structure and has the basicstructure of an inclusion compound.The use of white and polysaccharides to incorporateactive ingredients with unstable inclusion structures can increase its stabilityand enable the drug to have a certain slow-release effect.The aqueous solutionmethod was used to prepare a powdered inclusion compound of Bletilla striatapolysaccharide paeonol.The experiment showed that： Bletilla striata polysaccharide can form a complete inclusion compound with paeonol

白及多糖的开发，路阻且长

白及多糖来源丰富，价廉易得，具有止血、促进创伤愈合、抑菌、抗溃疡、抗肿瘤等药理活性，同时表现出良好的生物可降解性、生物相容性以及结构可修饰性，在药物递送系统和伤口敷料以及其他生物材料上的应用中表现出巨大潜力和应用前景。

The development of Bletilla striata polysaccharides has longroads and obstacles Bletilla striata polysaccharides are rich in sources， cheap and easy to obtain， have pharmacological activities such as hemostasis， promote wound healing， antibacterial， anti-ulcer，anti-tumor， etc.， and show goodbiodegradability， bio compatibility and structural modification.It has shown great potential andapplication prospects in the application of drug delivery systems， wound dressings and other biologicalmaterials.

需要注意的是，白及多糖成分的结构复杂，提取和纯化过程中尚不存在固定的工艺参数，结构尚未做到完全解析，质量控制方法尚不完善，结构特征和功能药效的关系也尚未阐明，这些影响了白及多糖相关制剂的进一步开发与利用。而目前白及多糖的剂型研究多集中于制剂的制备过程和制剂的体外表征研究中，对于制剂的药效学、药动学及临床研究较少，因此白及多糖相关制剂的产品开发和产业化进程还有很长的路要走。

It should be noted that the structure of Bletilla striatapolysaccharide components is complex，there are no fixed process parameters in the extraction andpurification process， the structure has not yet beenfully resolved， the quality control method is not yet complete， and therelationship between structural features and functional efficacy has not yet been established.It is clarified that these haveaffected the further development and utilization of white andpolysaccharide-related preparations.At present，research on the dosage form of Bletilla striata polysaccharides is mostlyfocused on the preparation process and invitro characterization ofpreparations.There are few pharmacodynamics， pharmacokinetics and clinical studies of preparations.

Therefore， theproduct development and industry of Bletilla striata  polysaccharide-related preparations Thetransformation process still has along way to go.

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