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    • 2. 发明申请
    • Drug-containing sustained release microparticle, process for producing the same and preparation containing the microparticle
    • 含药缓释微粒,其制造方法和含有微粒的制剂
    • US20060153930A1
    • 2006-07-13
    • US10559512
    • 2004-06-11
    • Yutaka MizushimaYasuaki OgawaJunzo TanakaToshiyuki Ikoma
    • Yutaka MizushimaYasuaki OgawaJunzo TanakaToshiyuki Ikoma
    • A61K33/42
    • A61K31/00A61K9/1611A61K33/30A61K33/42A61K45/06A61K2300/00
    • Sustained release microparticles suitable for various types of drugs, or drug-containing sustained release microparticles capable of sustained release of drugs over a period of three days or more and capable of inhibiting initial burst release; a process for producing the same; and preparations containing the microparticles are disclosed. The drug-containing sustained release microparticles comprise a drug other than human growth hormone and a porous apatite derivative, and optionally include a water-soluble bivalent metal compound. The drug-containing sustained release microparticles can be produced by dispersing under agitation microparticles of a porous apatite derivative in an aqueous solution containing a drug so that the aqueous solution infiltrates into the porous apatite derivative; optionally adding an aqueous solution containing a water-soluble bivalent metal compound that may infiltrate into the porous apatite derivative; further adding additives such as a stabilizer to the mixture; and effecting lyophilization or vacuum drying.
    • 适用于各种类型药物的持续释放微粒,或能够在三天或更长时间内持续释放药物并且能够抑制初始爆发释放的药物持续释放微粒; 其制造方法; 并且公开了含有微粒的制剂。 含药物的缓释微粒包含除人生长激素以外的药物和多孔磷灰石衍生物,任选地包含水溶性二价金属化合物。 含药缓释微粒可以通过将多孔磷灰石衍生物的微粒分散在含有药物的水溶液中分散而制成,使得水溶液渗透到多孔磷灰石衍生物中; 任选地加入含有可渗透到多孔磷灰石衍生物中的水溶性二价金属化合物的水溶液; 进一步向混合物中加入稳定剂等添加剂; 并进行冻干或真空干燥。
    • 8. 发明申请
    • DRUG-CONTAINING SUSTAINED RELEASE MICROPARTICLE, PROCESS FOR PRODUCING THE SAME AND PREPARATION CONTAINING THE MICROPARTICLE
    • 包含持续释放微生物的药物,其生产方法和含有微生物的制剂
    • US20100322902A1
    • 2010-12-23
    • US12837810
    • 2010-09-02
    • Yutaka MizushimaYasuaki OgawaJunzo TanakaToshiyuki Ikoma
    • Yutaka MizushimaYasuaki OgawaJunzo TanakaToshiyuki Ikoma
    • A61K38/21A61K47/02A61K31/573
    • A61K31/00A61K9/1611A61K33/30A61K33/42A61K45/06A61K2300/00
    • Sustained release microparticles suitable for various types of drugs, or drug-containing sustained release microparticles capable of sustained release of drugs over a period of three days or more and capable of inhibiting initial burst release; a process for producing the same; and preparations containing the microparticles are disclosed. The drug-containing sustained release microparticles comprise a drug other than human growth hormone and a porous apatite derivative, and optionally include a water-soluble bivalent metal compound. The drug-containing sustained release microparticles can be produced by dispersing under agitation microparticles of a porous apatite derivative in an aqueous solution containing a drug so that the aqueous solution infiltrates into the porous apatite derivative; optionally adding an aqueous solution containing a water-soluble bivalent metal compound that may infiltrate into the porous apatite derivative; further adding additives such as a stabilizer to the mixture; and effecting lyophilization or vacuum drying.
    • 适用于各种类型药物的持续释放微粒,或能够在三天或更长时间内持续释放药物并且能够抑制初始爆发释放的药物持续释放微粒; 其制造方法; 并且公开了含有微粒的制剂。 含药物的缓释微粒包含除人生长激素以外的药物和多孔磷灰石衍生物,任选地包含水溶性二价金属化合物。 含药缓释微粒可以通过将多孔磷灰石衍生物的微粒分散在含有药物的水溶液中分散而制成,使得水溶液渗透到多孔磷灰石衍生物中; 任选地加入含有可渗透到多孔磷灰石衍生物中的水溶性二价金属化合物的水溶液; 进一步向混合物中加入稳定剂等添加剂; 并进行冻干或真空干燥。
    • 10. 发明授权
    • Sustained-release preparation
    • 缓释制剂
    • US07048947B2
    • 2006-05-23
    • US10127558
    • 2002-04-23
    • Shigeru KameiYasutaka IgariYasuaki Ogawa
    • Shigeru KameiYasutaka IgariYasuaki Ogawa
    • A61K9/14C07K7/23
    • C07K7/23A61K9/1647A61K38/00A61K38/09
    • A sustained-release preparation which comprises a physiologically active peptide of general formula wherein X represents an acyl group; R1, R2 and R4 each represents an aromatic cyclic group; R3 represents a D-amino acid residue or a group of the formula wherein R3′ is a heterocyclic group; R5 represents a group of the formula —(CH2)n—R5′ wherein n is 2 or 3, and R5′ is an amino group which may optionally be substituted, an aromatic cyclic group or an O-glycosyl group; R6 represents a group of the formula —(CH2)n—R6′ wherein n is 2 or 3, and R6′ is an amino group which may optionally be substituted; R7 represents a D-amino acid residue or an azaglycyl residue; and Q represents hydrogen or a lower alkyl group, or a salt thereof and a biodegradable polymer having a terminal carboxyl group. The sustained-release preparation shows a constant release of the peptide over a long time and is substantially free from an initial burst.
    • 一种持续释放制剂,其包含通式的生理活性肽,其中X表示酰基; R 1,R 2和R 4各自表示芳族环状基团; R 3表示D-氨基酸残基或下式的基团其中R 3'是杂环基; R 5表示下式的基团 - (CH 2)n - n -R 5其中n为2 或3,并且R 5'是可任选被取代的氨基,芳族环状基团或O-糖基基团; R 6表示下式的基团 - (CH 2)n - 其中n为2 或3,并且R 6'是可任选被取代的氨基; R 7表示D-氨基酸残基或azaglycyl残基; Q表示氢或低级烷基,或其盐和具有末端羧基的生物降解性聚合物。 持续释放制剂显示长时间的肽的恒定释放并且基本上没有初始爆发。