CN113952312A - 经口腔粘膜吸收的赛洛多辛药物 - Google Patents
经口腔粘膜吸收的赛洛多辛药物 Download PDFInfo
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- CN113952312A CN113952312A CN202111291195.6A CN202111291195A CN113952312A CN 113952312 A CN113952312 A CN 113952312A CN 202111291195 A CN202111291195 A CN 202111291195A CN 113952312 A CN113952312 A CN 113952312A
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- Prior art keywords
- silodosin
- medicine
- oral
- tabletting
- oral mucosa
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Abstract
经口腔粘膜吸收的赛洛多辛药物,以赛洛多辛为有效药物成分,与口腔粘膜药物中可以接受的辅助成分共同组成,服用时无需用水,置于舌下或口颊处含化,服用方便,起效快,对口腔无刺激性;由于该药物基本不经过胃肠道吸收,减少胃肠道对药物的降解,可以较低的给药剂量达到与口服制剂相同或更好的治疗效果,提高生物利用度,并可同时降低不良反应风险,使患者具有满意的依从性。
Description
技术领域
本发明涉及一种经口腔粘膜吸收的药物,具体讲是一种可经口腔粘膜吸收的赛洛多辛药物,包括但不限于舌下片/颗粒/丸/膜、口颊含片/颗粒/丸/膜、含片/颗粒/丸/膜、口腔粘附片和口腔贴片等可全部或主要由舌下粘膜和/或口颊粘膜等口腔粘膜吸收的药物制剂。
背景技术
下尿路症状(LUTS)是老年男性常见的主诉,严重影响患者的生活质量,并对个人和社会造成沉重的经济负担。LUTS的发病率随增龄而增加,随着我国人口老龄化,将有更多的老年人受LUTS困扰。LUTS分为储尿期、排尿期和排尿后症状。储尿期症状包括尿频、尿急、尿失禁及夜尿增多等;排尿期症状包括排尿踌躇、排尿困难及间断排尿等;排尿后症状包括排尿不尽、尿后滴沥等。引起LUTS的原因主要与***疾病相关,膀胱过度活动症、***、夜尿症等均可导致LUTS。
良性***增生症(BPH)是导致老年男性LUTS最常见的一种良性疾病。组织学表现为***间质和腺体成分增生;解剖学表现为***体积增大;临床症状以LUTS为主和尿动力学上的膀胱出口梗阻。BPH组织学改变常发生于40岁后,60岁发病率大于50%,80岁达83%。我国年龄60岁及以上的泌尿科门诊患者占就诊疾病的构成比为47.0%。与组织学表现相类似,老年男性随增龄排尿困难等症状亦增加,约50%组织学诊断为BPH的患者有中重度LUTS。
BPH/LUTS的治疗方式包括等待观察、药物治疗和手术治疗。对于轻度或中度以上LUTS但生活质量尚未受到明显影响的患者可采取等待观察。对于中-重度BPH/LUTS但尚未出现相关并发症的患者可进行药物治疗。而中-重度BPH/LUTS已明显影响患者生活质量,尤其是药物治疗效果不佳或拒绝接受药物治疗的患者或出现导致的相关并发症时,建议采用手术治疗。
α肾上腺素受体阻滞剂是国内外指南一致推荐的BPH治疗一线用药,通过阻滞分布在***、膀胱颈部平滑肌的肾上腺素受体,松弛平滑肌,达到缓解膀胱出口动力性梗阻的作用。
赛洛多辛是一种新型高选择性α1A受体阻滞剂,与α1A受体的亲和力远远高于α1D受体和α1B受体。体外研究结果显示,赛洛多辛对***α1A受体选择性是α1B的162倍,约为同属高选择性α1A受体阻滞剂的坦索罗辛(α1A/α1B=9.55)的17倍。这就意味着,赛洛多辛拥有明显舒张下尿路平滑肌的作用,在有效改善***增生患者症状的同时,心血管不良反应发生率低,心血管耐受性良好。
赛洛多辛是一种白色至淡黄白色粉末,在约105℃至109℃熔化。它极易溶于乙酸,易溶于醇,极微溶于水。
已上市的赛洛多辛剂型仅有口服片剂和胶囊,规格为2mg、4mg,给药后由赛洛多辛的全身(血液)清除率约为人肝血流量的20%,在肝脏中的利用度估计约为80%,但生物利用度为32.2%。其原因被认为是CYP3A4和P-糖蛋白参与了赛洛多辛的代谢,表明胃肠道中的首过效应有显著影响。
发明内容
针对上述情况,本发明拟提供一种经口腔粘膜吸收的赛洛多辛药物,包括但不限于舌下片/颗粒/丸/膜、口颊含片/颗粒/丸/膜、含片/颗粒/丸/膜、口腔粘附片和口腔贴片等可全部或主要由舌下粘膜和/或口颊粘膜等口腔粘膜吸收的药物制剂。
与其他非口服给药途径相比,口腔黏膜给药具有以下特点:①口腔黏膜中的颊黏膜和舌下黏膜部位的血流丰富,血流速度快;②口腔黏膜对外界刺激具有较强的耐受性,当黏膜组织受到制剂中的一些成分刺激和损伤,停止用药后能够较快地恢复;③剂型易定位,用药方便,可以随时撤去药物。赛洛多辛口腔黏膜给药,药物经舌下粘膜和/或口颊粘膜,通过舌静脉和面静脉等汇至颈内静脉而直接进入血液循环,迅速起效;由于避开肠胃首过效应,减少胃肠道对药物的降解,提高生物利用度,可以较低给药剂量达到相同或更好的治疗效果,并减少不良反应;且给药方便,患者依从性好。
综上所述,本发明提供一种经口腔粘膜吸收的赛洛多辛药物,服用时无需用水,置于舌下或口颊处含化,服用方便,起效快,对口腔无刺激性;由于该药物基本不经过胃肠道吸收,减少胃肠道对药物的降解,可以较低的给药剂量达到与口服制剂相同或更好的治疗效果,提高生物利用度,并可同时降低不良反应风险,使患者具有满意的依从性。
本发明经口腔粘膜吸收的赛洛多辛药物,同样以赛洛多辛为有效药物成分,与口腔粘膜药物中可以接受的辅助成分共同组成。其中,所说的口腔粘膜药物中可以接受的辅助成分,可以选择目前在口腔粘膜药物制剂中通常需要和/或使用的多种辅料成分,包括:
稀释剂:如微晶纤维素、乳糖、乳糖复合物Ludipress(由乳糖、Kollidon 30和Kollidon CL组成)、Ludipress LCE(由乳糖和Kollidon 30组成)、Ludiflash(由90%Mannitol、5%CL-SF和5%SR 30D组成)、Cellactose 80、Tablettose80、MicroceLac 100、StarLac、Prosolv HD 90、淀粉、预胶化淀粉、糖粉、葡萄糖、硫酸钙、糊精、甘露醇、赤藓糖醇、麦芽糖、麦芽糖醇、麦芽糖糊精、山梨醇、木糖醇中的一种或几种。
粘合剂:如常用的聚维酮类成分(如Kollidon VA 64、Kollidon VA 64Fine、Plasdone S-630)、淀粉浆、羟丙基甲基纤维素、甲基纤维素、角叉菜胶、卡波姆、瓜尔胶、明胶、***胶、黄原胶、海藻酸或如海藻酸钠、海藻酸钾、海藻酸钙等其盐类成分、海藻酸丙二醇酯等各种成分中的一种或几种、磷酸淀粉钠、壳聚糖、糊精和糖浆中的一种或几种。
润湿剂:如常用的水、乙醇、无水乙醇及不同浓度的乙醇溶液中的一种或几种。
崩解剂:如交联聚维酮、羧甲基淀粉钠、交联羧甲基纤维素钠、低取代羟丙基纤维素、微晶纤维素、微晶纤维素-微粉硅胶、预胶化淀粉、干淀粉、淀粉、海藻酸钠、海藻酸、羟丙基淀粉、羧甲基纤维素钙中的一种或几种,用量一般可为片剂总重量的0.1%~50%。
掩味(矫味)剂:如常用的甘草甜素、阿斯巴甜、晶状麦芽糖、处理琼脂(TAG)、甜菊苷、三氯蔗糖、黄原胶、糖精、维生素C、果糖、葡聚糖、甜蜜素、索马甜、糖精、薄荷醇等允许使用的甜味剂和/或食用香精成分中的一种或几种。
润滑剂:如常用的硬脂酸镁、硬脂酸、硬脂富马酸钠、十二烷基硫酸钠、聚乙二醇4000(或聚乙二醇6000)、微粉硅胶、滑石粉等成分中的一种或几种。
吸收促进剂:聚山梨酸酯;聚氧乙烯与烷基形成的醚类;聚氧乙烯与脂肪酸形成的酯类;脂肪酸;脂肪醇;胆酸及其与制药学上可接受的阳离子形成的盐类;C1-C6脂肪醇与脂肪酸形成的酯类;多元醇与脂肪酸形成的酯类,所述的多元醇含有2-6个羟基功能基团;聚乙二醇化的甘油酯;十二烷基硫酸钠等成分中的一种或几种。
遮光剂:二氧化钛、氧化铁、四氧化三铁、氧化锌等允许使用的遮光剂成分中的一种或几种。
滴丸基质:聚乙二醇6000、聚乙二醇4000、聚乙二醇300、硬脂酸钠、甘油明胶中的一种或几种。
成膜材料:聚乙烯醇、乙烯-醋酸乙烯共聚物、羟丙基甲基纤维素、聚维酮、羟丙基纤维素;成膜增塑剂:甘油、山梨醇;表面活性剂:聚山梨酯80、十二烷基硫酸钠;填充剂:碳酸钙、二氧化硅、淀粉;着色剂:色素、二氧化钛和脱膜剂液状石蜡中的一种或几种。
本发明上述经口腔粘膜吸收药物中的赛洛多辛,是在口腔的舌下、口颊或口腔的其它部位含化,全部或基本上是由包括舌下粘膜和口颊粘膜等口腔内的粘膜组织吸收起效,其具体制剂形式,可以包括目前已有使用的舌下片/颗粒/丸/膜、口颊含片/颗粒/丸/膜、含片/颗粒/丸/膜、口腔粘附片和口腔贴片等。
本发明上述药物中,所说有效药物成分赛洛多辛在药物制剂中的含量,一般可以为药物总重量的0.1%~100%,上述辅助成分的用量则可分别按目前各相应制剂的常规方式使用。
本发明上述经口腔粘膜吸收药物的制备,可以采用目前同类药物制剂的常规方式制备得到。以片剂为例,其典型的制备方式可以有:
a.干法制粒压片方式:将有效药物成分赛洛多辛与所选择的辅助成分混合均匀,直接压成块,再破碎成颗粒,压片,制得成品。
b.湿法制粒压片方式:将有效药物成分赛洛多辛与内加的辅助成分混合均匀,加入粘合剂和/或润湿剂制粒并干燥后,再加入(或不加入)外加辅料(润滑剂和/或崩解剂),充分混匀,压片,制得成品。
c.粉末直接压片方式:将有效药物成分赛洛多辛与所选择的辅助成分混合均匀,直接压片,制得成品。
d.半干法制粒压片方式:将所选择的辅助成分混合均匀,加入粘合剂和/或润湿剂制粒并干燥后,再加入有效药物成分(也可以与外加润滑剂和/或崩解剂等辅料一并加入)充分混匀,压片,制得成品。
e.冷冻干燥法制片方式:将有效药物成分赛洛多辛、赋形剂和其他辅料与溶剂进行混合,配制成药液,将配制好的药液灌装到泡罩内,置冷冻干燥机中进行冷冻干燥,制得成品。
上述片剂典型的制备方式中,有效药物成分赛洛多辛可经单独预处理或与全部或部分辅助成分共同预处理或不经预处理,可以晶体、粉末、微粉、固体分散体和/或包合物等形式,与所选择的辅助成分进行混合,制粒,干燥,整粒后压片;或与所选择的辅助成分(预先制备成空白颗粒)进行混合后压片;或与所选择的辅助成分混匀后直接压片。
本发明上述形式的赛洛多辛药物,可以较低的给药剂量达到与口服制剂相同或更好的治疗效果,提高生物利用度;起效速度较口服片剂更快;服用时无需用水,更为方便。可以较为满意地解决口服片剂所存在的胃肠道首过效应较大、生物利用度较低的不足,提高疗效,降低不良反应,具有更理想的患者依从性,能让BPH患者更快地得到安全有效的治疗,迅速减轻患者痛苦。
以下通过实施例的具体实施方式再对本发明的上述内容作进一步的详细说明。但不应将此理解为本发明上述主题的范围仅限于以下的实例。在不脱离本发明上述技术思想情况下,根据本领域普通技术知识和惯用手段做出的各种替换或变更,均应包括在本发明的范围内。
具体实施方式
实施例1(含片,0.1~8mg/片)
组成:
制备方法:将赛洛多辛进行微粉化预处理至D90=0.1μm~15μm,原料与淀粉、预胶化淀粉等辅助成分混合均匀后,加入5%聚维酮水溶液制粒,流化床干燥,整粒,加入硬脂酸镁,混合均匀,压片,包装,即得。溶化性符合相关要求。服用时,置于口颊处含化。
实施例2(含片,2.5mg/片)
组成:
制备方法:将赛洛多辛进行微粉化预处理至D90=10μm~20μm,与乳糖、预胶化淀粉和赤藓糖醇等辅助成分混合均匀后,直接压片,包装,即得。溶化性符合相关要求。服用时,置于口颊处含化。
实施例3(含片,3.5mg/片)
组成:
制备方法:将赛洛多辛进行微粉化预处理至D90=5μm~25μm,与Ludipress LCE、微晶纤维素等辅助成分混合均匀后,加入硬脂富马酸钠,混合均匀,直接压片,包装,即得。溶化性符合相关要求。服用时,置于口颊处含化。
实施例4(舌下片,1.2mg/片)
组成:
制备方法:将赛洛多辛进行微粉化预处理至D90=10μm~20μm,与玉米淀粉等辅助成分混合均匀后,压片,包装,即得。崩解时限符合相关要求。服用时,置于舌下含化。
实施例5(口腔贴片或口腔粘附片,4mg/片)
组成:
制备方法:将赛洛多辛进行微粉化预处理至D90=15μm~30μm,与麦芽糖、山梨醇、卡波姆和羟丙基甲基纤维素等辅助成分混合均匀,压片即得口腔粘附片,或按贴片工艺进行制备,包装。释放度符合要求。服用时,贴于或粘附于口颊处或口腔内其他部位逐渐溶化。
实施例6(舌下片,2mg/片)
组成:
制备方法:将赛洛多辛进行微粉化预处理至D90=10μm~20μm,与甘露醇和淀粉等辅助成分混合均匀,置流化床中,用纯化水制粒,干燥,整粒,加入微粉硅胶,压片,包装。崩解时限符合相关要求。服用时,置于舌下含化。
实施例7(舌下片,3.2mg/片)
组成:
制备方法:将赛洛多辛进行微粉化预处理至D90=10μm~30μm,与麦芽糖糊精、微晶纤维素和羧甲基淀粉钠等辅助成分过100目筛,混合均匀,加入8%淀粉浆适量,制粒,干燥,整粒,加入外加羧甲基淀粉钠和硬脂富马酸钠,压片,包装。崩解时限符合相关要求。服用时,置于舌下含化。
实施例8(舌下片,2.6mg/片)
组成:
制备方法:将赛洛多辛与木糖醇、预胶化淀粉等辅助成分过100目筛,混合均匀,加入干法制粒机制粒,整粒,加入硬脂酸和交联聚维酮,混合均匀,压片,包装。崩解时限符合相关要求。服用时,置于舌下含化。
实施例9(舌下片,1.6mg/片)
组成:
制备方法:将甘露醇和玉米淀粉等辅助成分过100目筛,加入赛洛多辛,混合均匀,压片,包装。崩解时限符合相关要求。服用时,置于舌下含化。
实施例10(舌下片,0.8mg/片)
组成:
制备方法:将赛洛多辛与聚维酮K30,以溶剂法(如以乙醇为溶剂)制备成赛洛多辛-聚维酮K30固体分散体,干燥,检测固体分散体中赛洛多辛含量,将固体分散体粉碎,过筛,与乳糖、微晶纤维素、葡聚糖等辅助成分过100目筛,混匀,压片,包装,即得。崩解时限符合相关要求。服用时,置于舌下含化。
实施例11(舌下片,0.5mg/片)
组成:
制备方法:将赛洛多辛与羟丙基β-环糊精,以喷雾干燥法制备成包合物,检测包合物中赛洛多辛含量,将赛洛多辛-羟丙基β-环糊精包合物粉碎,过筛,将微晶纤维素、甜菊苷等辅助成分过100目筛,混合均匀,压片,包装。崩解时限符合相关要求。服用时,置于舌下含化。
实施例12(舌下片,3.2mg/片)
组成:
制备方法:将赛洛多辛和淀粉、赤藓糖醇等辅助成分过100目筛,加入挤出滚圆机,用纯化水挤出,滚圆,整粒,加入硬脂酸总混,压片,包装,即得。崩解时限符合相关要求。服用时,置于舌下含化。
实施例13(舌下片,2.5mg/片)
组成:
制备方法:按照处方量称取赛洛多辛和甘露醇等溶于水中,然后放入冻干机内低温迅速冻结成型,将冻结后的药物在高真空低温条件下升华,除去水分并适当干燥除去残余水分,制片,包装。崩解时限符合相关要求。服用时,置于舌下含化。
实施例14(滴丸,1mg/丸)
组成:
制备方法:按滴制法,将赛洛多辛加入熔融的聚乙二醇4000中,不断搅拌使全部熔融,趁热过滤,置贮液瓶中保温,用滴管滴至液状石蜡冷凝液中冷凝成丸,包装,即得。溶散时限符合要求。服用时,置于舌下或口颊处含化。
实施例15(微丸,1mg/粒)
组成:
制备方法:将空白丸芯(糖丸)加入流化床,底喷加入赛洛多辛的水溶液,制成微丸,包装。溶散时限符合要求。服用时,置于舌下或口颊处含化。
实施例16(舌下含服颗粒,3mg)
组成:
制备方法:将赛洛多辛与乳糖、甘露醇等辅料过80目筛,混合均匀,加入10%淀粉浆制粒后,干燥,整粒,装袋即得。崩解时限符合相关要求。服用时,置于舌下含化。
实施例17(膜剂,0.3%)
组成:
制备方法:称取赛洛多辛加入纯化水中,搅拌分散均匀,再称取二氧化钛、甘油加入纯化水中,搅拌分散均匀,再将聚乙烯醇加入分散均匀的溶液中,充分搅拌溶解形成胶液,胶液通过抽真空离心脱泡。将胶液注入涂布机,涂膜。按规格剪裁,包装。崩解溶化时间符合要求。服用时,置于舌下或口颊处含化。
以上虽然以实施例描述了本发明的精神,但是只用于说明目的而不是限制本发明,实施例的变化对于本领域一般的技术人员,在阅读本发明的技术路线后或者实施例后变得显而易见。因此,在不背离本发明范围和精神的情况下,可以对本发明的实施例进行调整和改变,这些调整和改变都属于本发明的等同替换。
Claims (6)
1.经口腔粘膜吸收的药物,以赛洛多辛为有效药物成分,与口腔粘膜药物中可以接受的辅助成分共同组成,其特征是每单位剂量中所含赛洛多辛为0.1mg-8.0mg。
2.如权利要求1所述的经口腔粘膜吸收的赛洛多辛药物,其特征是剂型为片剂、颗粒剂、丸剂、膜剂、口腔粘附片和口腔贴片等剂型。
3.如权利要求1、2所述的经口腔粘膜吸收的赛洛多辛药物,其特征是采用干法制粒、湿法制粒工艺制备的颗粒,以及干法制粒压片、湿法制粒压片、半干法制粒压片、粉末直接压片和冷冻干燥法制片工艺制备的片剂。
4.如权利要求1、2所述的经口腔粘膜吸收的赛洛多辛药物,其特征是采用丸剂制备方法,进行丸剂制备。
5.如权利要求1、2所述的经口腔粘膜吸收的赛洛多辛药物,其特征是采用膜剂制备方法,进行膜剂制备。
6.如权利要求3、4、5所述的经口腔粘膜吸收的赛洛多辛药物,其有效药物成分赛洛多辛可经单独预处理或与全部或部分辅助成分共同预处理或不经预处理,可以晶体、粉末、微粉、固体分散体和/或包合物等形式,与所选择的辅助成分进行片剂、颗粒剂、丸剂、膜剂、口腔粘附片和口腔贴片等剂型的制备。
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