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公开(公告)号:US20110217340A1
公开(公告)日:2011-09-08
申请号:US13059462
申请日:2009-07-24
CPC分类号: A61K9/1694 , A61K9/1623 , A61K9/1635 , B01J2/04
摘要: A process for the production of a soluble composition comprising a water-insoluble active which comprises either the steps of: a) providing a liquid mixture comprising: i) a dissolved water-insoluble active, ii) a dissolved water-soluble carrier, iii) a solvent for each of the active and the carrier, and b) spray-granulating the mixture to remove the, or each, solvent and obtain a substantially solvent-free nano-dispersion of the water-insoluble active in the carrier said water-insoluble active being in nano-particles having a size range of 999-20 nm; or, the steps of: a) providing a substantially solvent-free powder comprising a water-insoluble active dispersed in a water soluble carrier, said water-insoluble active being in nano-particles having a size range of 999-20 nm, and, b) spray-granulating the powder to obtain larger and denser particles. The invention also relates to solvent-free, granular products with a particle size in the range 20 microns to 10 mm and a bulk-density of greater than 0.4 g/cm3 comprising a water-soluble carrier material, the carrier material having dispersed therein a water-insoluble active, wherein on addition of water the carrier dissolves to form an aqueous dispersion of the active with a peak (z-average) particle size of below 800 nm, preferably below 500 nm and more preferably below 200 nm. The invention also relates to an analogous “reverse” process in which the active is water soluble and the carrier is oil soluble.
摘要翻译: 一种用于生产包含水不溶性活性物质的可溶性组合物的方法,其包括以下步骤:a)提供液体混合物,其包含:i)溶解的水不溶性活性物质,ii)溶解的水溶性载体,iii) 用于活性物质和载体中的每一种的溶剂,以及b)将混合物喷雾造粒以除去溶剂或每种溶剂,并获得载体中不溶于水的活性物质的基本上无溶剂的纳米分散体,所述水不溶性 活性纳米颗粒的尺寸范围为999〜20nm; 或者步骤:a)提供基本上无溶剂的粉末,其包含分散在水溶性载体中的不溶于水的活性物质,所述水不溶性活性物质的尺寸范围为999-20nm, b)将粉末喷雾造粒以获得更大和更致密的颗粒。 本发明还涉及粒径在20微米至10毫米范围内的无溶剂颗粒状产品,其中堆积密度大于0.4克/厘米3,包含一种水溶性载体材料,载体材料已分散在其中 其中在加入水时,载体溶解以形成具有低于800nm,优选低于500nm,更优选低于200nm的峰(z-平均)粒度的活性物质的水分散体。 本发明还涉及类似的“反向”方法,其中活性物质是水溶性的并且载体是油溶性的。
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公开(公告)号:US20120135058A1
公开(公告)日:2012-05-31
申请号:US13365830
申请日:2012-02-03
申请人: Doris Angus , David John Duncalf , Andrew James Elphick , Alison Jayne Foster , James Long , Steven Paul Rannard , Dong Wang
发明人: Doris Angus , David John Duncalf , Andrew James Elphick , Alison Jayne Foster , James Long , Steven Paul Rannard , Dong Wang
IPC分类号: C08L39/06 , A61K8/81 , A01P3/00 , C09B67/38 , A01N25/10 , A61Q5/00 , B82Y40/00 , B82Y30/00 , B82Y5/00
CPC分类号: A61K9/1617 , A01N25/04 , A61K9/10 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/19 , A61K31/167 , Y02A50/411 , A01N43/54 , A01N53/00 , A01N31/16 , A01N37/18
摘要: The invention provides process for making contra-soluble nano-dispersions of at most sparingly-soluble materials in a soluble carrier material comprising the steps of: (i) providing a single phase mixture of: (a) a solvent or a mixture of miscible solvents wherein at least one of the solvents is an aqueous solvent and at least another solvent is a non-aqueous solvent, (b) at least one carrier material soluble in solvent (a), said carrier material being also contra-soluble to payload material (c) and solid at ambient temperature, (c) at least one a payload material which is soluble in solvent (a), and, (ii) freeze-drying the mixture to remove solvent (a) and thereby obtain the carrier material (b) in solid form with payload (c) dispersed therein as nanoparticles.
摘要翻译: 本发明提供了在可溶性载体材料中制备至多微溶性材料的可溶性纳米分散体的方法,其包括以下步骤:(i)提供单相混合物:(a)溶剂或可混溶溶剂的混合物 其中所述溶剂中的至少一种是水性溶剂,并且至少另一种溶剂是非水溶剂,(b)至少一种可溶于溶剂(a)的载体材料,所述载体材料也与所述载体材料 c)和环境温度下的固体,(c)至少一种可溶于溶剂(a)的有效载荷材料,和(ii)冷冻干燥该混合物以除去溶剂(a),从而获得载体材料 ),其中有效载荷(c)作为纳米颗粒分散在其中。
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公开(公告)号:US20120134940A1
公开(公告)日:2012-05-31
申请号:US13365826
申请日:2012-02-03
申请人: Doris Angus , David John Duncalf , Andrew James Elphick , Alison Jayne Foster , James Long , Steven Paul Rannard , Dong Wang
发明人: Doris Angus , David John Duncalf , Andrew James Elphick , Alison Jayne Foster , James Long , Steven Paul Rannard , Dong Wang
IPC分类号: C08L29/04 , C08L39/04 , A61K47/32 , A01N25/04 , A61K8/81 , A61Q5/12 , C11D3/37 , A61Q17/04 , D06P5/00 , C11D3/395 , A61Q13/00 , A23L1/22 , A61Q19/00 , A01P7/04 , A01P1/00 , A61P31/00 , C08L39/06 , B82Y5/00 , B82Y99/00
CPC分类号: A61K9/1617 , A01N25/04 , A61K9/10 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/19 , A61K31/167 , Y02A50/411 , A01N43/54 , A01N53/00 , A01N31/16 , A01N37/18
摘要: The invention provides process for making water-soluble nano-dispersions of water-insoluble materials in a water-soluble carrier material comprising the steps of: (i) providing a single phase mixture of: (a) a non-aqueous solvent or a mixture of miscible non-aqueous solvents, (b) at least one carrier material soluble in non-aqueous solvent (a), said carrier material being also soluble in water and solid at ambient temperature, (c) at least one water-insoluble payload material which is soluble in non-solvent (a), and, (ii) drying the mixture to remove solvent (a) and thereby obtain the carrier material (b) in solid form with payload (c) dispersed therein as nanoparticles, wherein the product of the drying step is water dispersible to give an aqueous solution of (b) and an aqueous nano-dispersion of (c).
摘要翻译: 本发明提供在水溶性载体材料中制备水不溶性材料的水溶性纳米分散体的方法,其包括以下步骤:(i)提供单相混合物:(a)非水溶剂或混合物 的混溶性非水溶剂,(b)至少一种可溶于非水溶剂(a)的载体材料,所述载体材料在环境温度下也可溶于水和固体,(c)至少一种不溶于水的有效载荷材料 其可溶于非溶剂(a),和(ii)干燥混合物以除去溶剂(a),从而获得固体形式的载体材料(b),其中有效载荷(c)分散在其中作为纳米颗粒,其中产物 的干燥步骤是水分散,得到(b)的水溶液和(c)的水性纳米分散体。
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公开(公告)号:US20090175953A1
公开(公告)日:2009-07-09
申请号:US12309306
申请日:2007-06-29
申请人: Doris Angus , David John Duncalf , Andrew James Elphick , Alison Jayne Foster , James Long , Steven Paul Rannard , Dong Wang
发明人: Doris Angus , David John Duncalf , Andrew James Elphick , Alison Jayne Foster , James Long , Steven Paul Rannard , Dong Wang
IPC分类号: A61K9/16 , C09K3/00 , B01J13/00 , C09B67/08 , A01N43/653 , A01N37/50 , A01N31/16 , A01N53/00 , A01P1/00 , A01P3/00
CPC分类号: A61K9/1617 , A01N25/04 , A61K9/10 , A61K9/1635 , A61K9/1641 , A61K9/1652 , A61K9/19 , A61K31/167 , Y02A50/411 , A01N43/54 , A01N53/00 , A01N31/16 , A01N37/18
摘要: The invention provides process for making contra-soluble nano-dispersions of at most sparingly-soluble materials in a soluble carrier material comprising the steps of: (i) providing a single phase mixture of: a) a solvent or a mixture of miscible solvents, b) at least one carrier material soluble in solvent (a), said carrier material being also contra-soluble to payload material (c) and solid at ambient temperature, c) at least one a payload material which is soluble in solvent (a), and, (ii) drying the mixture to remove solvent (a) and thereby obtain the carrier material (b) in solid form with payload (c) dispersed therein as nanoparticles.
摘要翻译: 本发明提供了在可溶性载体材料中制备至多微溶性材料的可溶性纳米分散体的方法,其包括以下步骤:(i)提供单相混合物:a)溶剂或可混溶溶剂的混合物, b)可溶于溶剂(a)的至少一种载体材料,所述载体材料在环境温度下也可溶于有效载荷材料(c)和固体,c)至少一种可溶于溶剂(a)的有效载荷材料, ,和(ii)干燥混合物以除去溶剂(a),从而获得固体形式的载体材料(b),其中有效载荷(c)作为纳米颗粒分散在其中。
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公开(公告)号:US20110217381A1
公开(公告)日:2011-09-08
申请号:US13061533
申请日:2009-08-03
IPC分类号: A61K9/14 , A61K31/4545 , A61P43/00
CPC分类号: A61K9/1694 , A61K9/1652 , A61K9/5161
摘要: The present invention provides a substantially solvent-free nano-dispersion of an active in a carrier, wherein the carrier comprises an enteric carrier soluble at intestinal pH, but insoluble at stomach pH, and wherein the enteric carrier comprises at least 50% by weight of the nano-dispersion; and processes for the preparation of a substantially solvent-free nano-dispersion of an active in a carrier.
摘要翻译: 本发明提供了一种载体中活性物质的基本上无溶剂的纳米分散体,其中载体包含可在肠pH下溶解但在胃pH下不溶的肠溶载体,其中肠载体包含至少50重量% 纳米分散体; 以及用于制备载体中活性物质的基本上无溶剂的纳米分散体的方法。
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