CN1686089A - 一种可直接压片的木糖醇颗粒及其制备方法 - Google Patents
一种可直接压片的木糖醇颗粒及其制备方法 Download PDFInfo
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Abstract
本发明提供了一种主要组成为木糖醇和聚乙烯吡咯烷酮的可直接压片的木糖醇颗粒及其制备方法。木糖醇是一种具有营养和医疗价值的甜味物质,也是人体糖代谢的正常中间体。由于木糖醇是一种多羟基结构化合物,自身易吸潮成团,一般难以压制成片剂口服(或口含)使用。本发明经过多次试验,采用新的组合配方及方法制成颗粒,颗粒色泽均一,而且稳定性好,口感好,防龋齿,直接压片后的木糖醇片既可以口服,也可以口含,能使口腔保持一定pH值环境,有利于口腔卫生。同时按本发明制成的木糖醇颗粒解决了单纯服用木糖醇时易产生的腹泻肠气等不良现象。
Description
本发明涉及医药保健及食品领域,是一种将木糖醇制成可直接压片的颗粒及其制备方法,该颗粒中含有木糖醇和聚乙烯吡咯烷酮,此外还可以含有山梨醇和羟丙基甲基纤维素等。
木糖醇是一种具有医药生理能的甜味物质,化学名为戊五醇,分子式C5H12O5,是一种白色结晶粉末,甜度与蔗糖相近,但热量比蔗糖低,人体吸收迅速,既是健康人群日常糖的代用品,又是糖尿病人的营养剂和治疗剂。后来人们发现木糖醇能调节口腔牙床的PH值和对抗口腔微生物发酵,从而防止牙齿脱矿,因而有特殊的防龋功能,欧美及日本等许多国家,已将其做成各种剂型,如片剂、颗粒、口香糖口含糖块及口嚼糖片等。在我国,用木糖醇制成的辅助治疗药品“木糖醇输液”及口香糖已在市场销售。
木糖醇有较强的吸湿性,但熔点低,将其制成颗粒及压制成片剂有较大的困难,普遍缺陷和问题是颗粒容易粘连成块、片剂易粘片,硬度不够,保存期短。由此原因,木糖醇片剂及适宜的木糖醇颗粒至今未能商业化大生产来满足消费者的需用求。
本发明涉及的木糖醇颗粒及其组合成份和制备方法,该颗粒既可直接口服使用,又能用于直接压片,颗粒外观色泽均一,稳定性好、口感好,压成的片剂崩解时间短,且不易松片破碎。该颗粒防龋齿,不会产生单独服用木糖醇后的腹泻或胀气现象。
本发明提供了一种可直接压片的木糖醇颗粒,其特征在于该颗粒主要组成为:木糖醇和聚乙烯吡咯烷酮,其中木糖醇和的聚乙烯吡咯烷酮的含量按重量计为:木糖醇90.0~99.0%,聚乙烯吡咯烷酮0.1~5.0%。
在本发明的木糖醇颗粒中还含有山梨醇,其中各组分的含量按重量百分比为:木糖醇90.0~99.0%,聚乙烯吡咯烷酮0.1~5.0%,山梨醇为0.1~5.0%。
此外,在本发明的木糖醇颗粒中还可以含有羟丙基甲基纤维素。
大量的文章报导证明,由于木糖醇熔点低,将其直接或与其他辅助载体混合制粒后压片时,一般不容易压制成硬度合宜的片剂,普遍存在的缺陷是片子松软,不易储存服用。本发明人经长期深入研究和大量试验后,认为聚乙烯吡咯烷酮是非常适宜的辅助载体,再加一定比例的生理上可接受的附加物,如山梨醇等,混合后制粒压片,就可以避免上面提到的不利影响,而是经多次试验,压成的片剂稳定性好,符合片剂的硬度值和崩解度等各项指标要求,而且大大减少了单独服用木糖醇时易引起的肠泻胀气等现象。
聚乙烯吡咯烷酮是一种较优良的粘合剂,它可与多种物质,特别是含有氨基、羟基的化合物形成络合物,从而大大增强了母体化合物(如木糖醇)的稳定性,但不改变母体化合物的生理活性作用。发明人有选择地添加合宜比例的聚乙烯吡咯烷酮,优选的聚乙烯吡咯烷酮是K30-K90(例如,其中K30的平均分子量为25000~40000,K60的平均分子量为160000,K90的平均分子量为360000),这样制成的片子非常理想。
此外,优选的是在本发明的木糖醇颗粒中,羟丙基甲基纤维素与山梨醇的总重量百分比不低于0.2%。
羟丙基甲基纤维素是一种纤维素醚,其粘度使范围比较大。粘度值不适合,则制成的颗粒长时期储存人时会发生粘连,本发明人选择的粘度值在20~650MP·S之间。
本发明还提供了一种可直接压片的木糖醇颗粒的制备方法,其特征在于:将木糖醇粉碎成后,与粉碎好的山梨醇混合,再与胶状聚乙烯吡咯烷酮水溶液混合,用湿法制粒而成。
本发明木糖醇颗粒优选的制备方法是:其特征在于:(1)将木糖醇粉碎成60~90目(250~160微米),与粉碎好的山梨醇混合,(2)将羟丙基甲基纤维用乙醇水溶液溶解,(3)将聚乙烯吡咯烷酮用水溶解使成胶状溶液,与羟丙基甲基纤维素溶液混合,并将此混合溶液在搅拌下加到上述木糖醇与山梨醇的混合粉中,用湿法制粒而成。
在本发明木糖醇颗粒的制备方法中,聚乙烯吡咯烷酮用水溶解制成胶状物后使用,羟丙基甲基纤维素用0~10%的乙醇水溶液制成胶状液体。
本发明选用的配方及物料比例,主料辅料按规定进行预加工处理,按工艺次序混合,湿法制粒,经干燥后即得木糖醇颗粒,用于直接压片,该压片片剂的各项性能指标,均优于对照品木糖醇片剂。
实施例一
取木糖醇96克,粉碎成80~90目;再取山梨醇2克粉碎成100~120目后加到木糖醇粉中,混合20分钟使均匀;取聚乙烯吡咯烷酮2克,用适量水溶解制成胶状溶液;将山梨醇与木糖醇粉混合物加入到制成的聚乙烯吡咯烷酮胶状溶液中,混合,用16目制粒,20目整粒,80℃以下烘干,测定含水量合格后包装即得。
实施例二
取粉碎后过100筛的木糖醇95克,再取山梨醇3克并粉碎过100目筛,两者混合后备用;将1.5克羟丙基甲基纤维素用5%的乙醇溶液溶解后与1.0克的聚乙烯吡咯烷酮水溶液混合后加到上述木糖醇与山梨醇的混合粉中,混合制粒,用18~20目整粒,80℃以下烘干,检验合格后分装即得。
实施例三
取木糖醇94.5克,粉碎后过100目筛;取聚乙烯吡咯烷酮2克,用于溶解后制成胶状溶液;再取山梨醇3.5克粉碎成90~100目后加到粉碎过筛的木糖醇粉中,加入配好的聚乙烯吡咯烷酮胶性溶液,混合物后制粒,在70~80℃左右烘干,检验使含水份在1.0%以下,分装即得。
实施例四
取木糖醇94克和山梨醇3.5克,分别粉碎各自过100目筛后混合备用,将2.0克的羟丙基甲基纤维用8%乙醇水溶液溶解,再将0.5克的聚乙烯吡咯烷酮用水溶解使成胶状溶液后,与羟丙基甲基纤维素溶液混合,将此混合溶液在搅拌下加到上述木糖醇与山梨醇的混合粉中,混合后用16目制粒,20目整粒,80℃以下烘干即得。
对照实施例一
取木糖醇96克,粉碎后过100目筛,另取山梨醇2克,粉碎过100目筛。取羧甲基纤维素钠2克,用适量水溶解。将上述木糖醇与山梨醇粉混合物后加入羟甲基纤维素钠胶体溶液,混合制粒,80℃以下烘干,用20目整粒后检验,合格后分装。
对照实施例二
取粉碎后、过90~100目筛的木糖醇96克与2克淀粉混合,用2克羧甲基纤维素钠制成的胶状溶液混合后制粒,制得的颗粒在70~80℃下烘干,检验合格后分装。
试验一
直接压片的木糖醇颗粒制得的片剂对照试验
1、供试品片:木糖醇片(根据本发明制备的颗粒压制)
A、批号:041001,数量:3800片(按实施例一方法制得的颗粒压制而成)
B、批号:041002,数量:4500片(按实施例二方法制得的颗粒压制而成)
C、批号:041003,数量:4300片(按实施三方法制得的颗粒压制而成)
2、对照品片:木糖醇羧甲基纤维素钠片
A、批号:041011-1,数量:4000片(按对照实施例一方法制得的颗粒压制而成)
B、批号:041011-2,数量:4500片(按对照实施例二方法制得的颗粒压制而成)
3、崩解时限、溶出度对照试验结果:见下表
4、结论:从表中看出,按本发明实施的木糖醇颗粒压成的片剂,其崩解时限和溶出度都比对照的木糖醇片要好得多,即崩解时限缩短二分之一,溶出度高出15%左右。
试验II:
聚乙烯吡咯烷酮粘度值的选择试验
分别用同一厂商生产的、不同粘度规格的聚乙烯吡咯烷酮(K15、20、30、40、60、90、100、120),按本发明实施例一的方法,用木糖醇及山梨醇制成颗粒压制的片剂,其片剂硬度及崩解时限进行比较试验,结果见下表:
聚乙烯吡咯烷酮根据其中化学结构组成的差别,其K值不一样。从试验情况来看,K值大则硬度大,崩解时限长,K值小则反之。而符合标准的片剂,则要求硬度较大而崩解时限越小越好。在可选择的范围内,我们选择K30-K90。从表中数据可以看出,比较满意。
Claims (10)
1、一种可直接压片的木糖醇颗粒,其特征在于该颗粒主要组成为:木糖醇和聚乙烯吡咯烷酮。
2、权利要求1的木糖醇颗粒,其中木糖醇和的聚乙烯吡咯烷酮的含量按重量计为:木糖醇90.0~99.0%,聚乙烯吡咯烷酮0.1~5.0%。
3、权利要求1的木糖醇颗粒,该颗粒中还含有山梨醇。
4、权利要求3的木糖醇颗粒,其中各组分的含量按重量百分比为:木糖醇90.0~99.0%,聚乙烯吡咯烷酮0.1~5.0%,山梨醇为0.1~5.0%。
5、权利要求3或4的木糖醇颗粒,该颗粒中还含有羟丙基甲基纤维素。
6、权利要求1的木糖醇颗粒,其中聚乙烯吡咯烷酮优选为K30-K90。
7、权利要求5的木糖醇颗粒,其中羟丙基甲基纤维素的粘度为20~650mp·S。
8、权利要求5的木糖醇颗粒,其中羟丙基甲基纤维素与山梨醇的总重量百分比不低于0.2%。
9、一种可直接压片的木糖醇颗粒的制备方法,其特征在于:将木糖醇粉碎成后,与粉碎好的山梨醇混合,再与胶状聚乙烯吡咯烷酮水溶液混合,用湿法制粒而成。
10、权利要求9的木糖醇颗粒的制备方法,其特征在于:(1)将木糖醇粉碎成60~90目(250~160微米),与粉碎好的山梨醇混合,(2)将羟丙基甲基纤维用乙醇水溶液溶解,(3)将聚乙烯吡咯烷酮用水溶解使成胶状溶液,与羟丙基甲基纤维素溶液混合,并将此混合溶液在搅拌下加到上述木糖醇与山梨醇的混合粉中,用湿法制粒而成。
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US11/885,147 US20080161417A1 (en) | 2005-05-08 | 2006-05-08 | Xylitol Granules Capable of Directly Being Compressible Into Tablets and Preparation Process Thereof |
EP06741800A EP1852109A4 (en) | 2005-05-08 | 2006-05-08 | XYLITOL PELLETS THAT CAN BE TRANSFORMED DIRECTLY IN TABLETS AND PROCESS FOR THE PREPARATION THEREOF |
PCT/CN2006/000905 WO2006119697A1 (fr) | 2005-05-08 | 2006-05-08 | Granules de xylitol pouvant etre transformes directement en comprimes et procede de preparation associe |
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WO2008017220A1 (fr) * | 2006-08-01 | 2008-02-14 | Beijing Jianjian Kangkang Bio-Tech.Co., Ltd | Produit à mâcher soluble à base de xylitol et de café, et procédé de préparation dudit produit |
WO2008052426A1 (fr) * | 2006-11-03 | 2008-05-08 | Anhui Fukang Pharmaceutical Co., Ltd | Comprimé sucré à base de xylitol et son procédé de préparation |
WO2008125035A1 (fr) * | 2007-04-11 | 2008-10-23 | O'laughlin Fine Chemicals (Kunshan) Co., Ltd | Granulés édulcorants |
CN102429885A (zh) * | 2011-12-30 | 2012-05-02 | 山东力诺科峰制药有限公司 | 一种dc-木糖醇及其制备方法 |
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CN109512789A (zh) * | 2018-11-22 | 2019-03-26 | 浙江华康药业股份有限公司 | 一种可直接压片的高纯度粒状木糖醇及其制备方法 |
CN112312912A (zh) * | 2018-06-27 | 2021-02-02 | 第一三共株式会社 | 含有二胺衍生物的颗粒 |
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IT1396118B1 (it) * | 2009-09-23 | 2012-11-16 | Eridania Sadam S P A | Composizione dolcificante. |
CN112352958A (zh) * | 2020-11-09 | 2021-02-12 | 安阳市豫鑫木糖醇科技有限公司 | 一种木糖醇制粒的生产工艺 |
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ZA869191B (en) * | 1986-01-07 | 1987-07-29 | Warner Lambert Co | Polyvinylpyrrolidone-containing coating for comestibles |
US5536526A (en) * | 1988-01-11 | 1996-07-16 | Cultor Ltd. | Xylitol-based binding and diluting agent and a process for the production thereof |
US5204115A (en) * | 1990-12-12 | 1993-04-20 | Suomen Xyrofin Oy | Directly compressible xylitol and method |
US5846568A (en) * | 1996-09-19 | 1998-12-08 | Xyrofin Oy | Directly compressible lactitol and method |
AU739767B2 (en) * | 1997-10-15 | 2001-10-18 | Merck Patent Gmbh | Production of a directly compressible tabletting aid |
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IT1305308B1 (it) * | 1999-03-26 | 2001-05-04 | Biosint S P A | Granulato ad alto contenuto di l-carnitina o alcanoil-l-carnitina,particolarmente adatto alla produzione di compresse per compressione |
US6264983B1 (en) * | 1999-09-16 | 2001-07-24 | Rhodia, Inc. | Directly compressible, ultra fine acetaminophen compositions and process for producing same |
CN1108107C (zh) * | 2000-01-11 | 2003-05-14 | 赵力 | 木糖醇含片及其制造方法 |
US7118765B2 (en) * | 2001-12-17 | 2006-10-10 | Spi Pharma, Inc. | Co-processed carbohydrate system as a quick-dissolve matrix for solid dosage forms |
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-
2005
- 2005-05-08 CN CN2005100682552A patent/CN1686089B/zh not_active Expired - Fee Related
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2006
- 2006-05-08 WO PCT/CN2006/000905 patent/WO2006119697A1/zh not_active Application Discontinuation
- 2006-05-08 EP EP06741800A patent/EP1852109A4/en not_active Withdrawn
- 2006-05-08 US US11/885,147 patent/US20080161417A1/en not_active Abandoned
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CN1686089B (zh) | 2010-08-18 |
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WO2006119697A1 (fr) | 2006-11-16 |
EP1852109A4 (en) | 2010-05-12 |
US20080161417A1 (en) | 2008-07-03 |
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