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    • 4. 发明授权
    • Highly loaded amorphous efavirenz composition and process for preparing the same
    • 高度无定形的依法韦仑组合物及其制备方法
    • US09114170B2
    • 2015-08-25
    • US13843224
    • 2013-03-15
    • ISP Investments Inc.
    • Yunxia BiMohammed Abdul RahmanJames David LesterThomas DurigRandy Bull
    • A61K31/536C07D265/14A61K47/38A61K47/32B29C43/00A61K9/14A61K9/16
    • A61K47/38A61K9/146A61K9/1635A61K31/536A61K47/32B29C43/003
    • A stable and high loading ternary solid dispersion composition comprising (a) about 50% wt. to about 90% wt. of amorphous Efavirenz; (b) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone (PVP), a first polymer; (c) about 1% wt. to about 30% wt. of a water-soluble second polymer; and (d) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Also discloses a high loading ternary composition comprising (a) a solid dispersion composition comprising (i) about 50% wt. to about 90% wt. of amorphous Efavirenz; (ii) about 10% wt. to about 50% wt. of polyvinyl pyrrolidone, a first polymer; (b) about 1% wt. to about 30% wt. of a water-soluble second polymer blended with solid dispersion of composition of (a); and (c) optionally about 0.1% wt. to about 50% wt. of at least one pharmaceutically acceptable excipient. Additionally discloses a method for preparing solid dosage forms comprising (i) amorphous Efavirenz and (ii) polyvinyl pyrrolidone (PVP), a first polymer; (iii) a water-soluble second polymer; and (iv) optionally, at least one pharmaceutical excipients.
    • 一种稳定且高负载的三元固体分散体组合物,其包含(a)约50重量% 至约90重量% 的无定形依非韦伦; (b)约10重量% 至约50重量% 聚乙烯吡咯烷酮(PVP),第一聚合物; (c)约1重量% 至约30重量% 的水溶性第二聚合物; 和(d)任选地约0.1重量% 至约50重量% 的至少一种药学上可接受的赋形剂。 还公开了一种高负载三元组合物,其包含(a)固体分散体组合物,其包含(i)约50重量% 至约90重量% 的无定形依非韦伦; (ii)约10重量% 至约50重量% 聚乙烯吡咯烷酮,第一聚合物; (b)约1重量% 至约30重量% 与(a)的组合物的固体分散体共混的水溶性第二聚合物; 和(c)任选地约0.1重量% 至约50重量% 的至少一种药学上可接受的赋形剂。 另外公开了一种制备固体剂型的方法,其包含(i)非依依夫韦恩和(ii)聚乙烯吡咯烷酮(PVP),第一聚合物; (iii)水溶性第二聚合物; 和(iv)任选的至少一种药物赋形剂。
    • 9. 发明申请
    • Colorimetric detection of cyanide with a chromogenic oxazine
    • 用显色恶嗪比色检测氰化物
    • US20090258429A1
    • 2009-10-15
    • US11991355
    • 2006-09-01
    • Francisco M. RaymoMassimiliano Tomasulo
    • Francisco M. RaymoMassimiliano Tomasulo
    • C07D265/14G01N21/78
    • G01N33/1826C07D498/04C09B19/00G01N31/22Y10T436/172307
    • A chromogenic oxazine compound for the colorimetric detection of cyanide was designed. Indeed, the [1,3]oxazine ring of our compound opens to form a phenolate chromophore in response to cyanide. The heterocyclic com-pound may be comprised of fused benzooxazine and indoline rings: wherein R1 is an alkyl (e.g., methyl, ethyl, propyl, isopropyl, butyl, isobutyl), a substituted alkyl, a cycloalkyl (e.g., cyclopentyl, cyclohexyl), a substituted cycloalkyl, an aryl (e.g., phenyl), or a substituted aryl and R2 is a chromophore (e.g., nitroso, nitro, azo dyes). This quantitative chromogenic transformation permits the detection of micromolar concentrations of cyanide in water. Furthermore, our chromogenic oxazine is insensitive to the presence of large concentrations of fluoride, chloride, bromide or iodide anions, which are generally the principal interferents in the colorimetric detection of cyanide.
    • 设计了用于氰化物比色检测的显色恶嗪化合物。 事实上,我们化合物的[1,3]恶嗪环打开以形成响应于氰化物的酚盐发色团。 杂环化合物可以由稠合的苯并恶嗪和二氢吲哚环组成:其中R1是烷基(例如甲基,乙基,丙基,异丙基,丁基,异丁基),取代的烷基,环烷基(例如环戊基,环己基) 取代的环烷基,芳基(例如苯基)或取代的芳基,R2是发色团(例如亚硝基,硝基,偶氮染料)。 这种定量显色转化允许在水中检测微摩尔浓度的氰化物。 此外,我们的显色恶嗪对大量氟化物,氯化物,溴化物或碘化物阴离子的存在不敏感,这些阴离子通常是氰化物比色检测中的主要干扰物。