CN107929325A - 一种含美洲大蠊的栓剂及其制备方法 - Google Patents
一种含美洲大蠊的栓剂及其制备方法 Download PDFInfo
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- CN107929325A CN107929325A CN201711235287.6A CN201711235287A CN107929325A CN 107929325 A CN107929325 A CN 107929325A CN 201711235287 A CN201711235287 A CN 201711235287A CN 107929325 A CN107929325 A CN 107929325A
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Abstract
本发明属于药物制剂领域，具体涉及一种美洲大蠊直肠用药制剂，它是由含多种形式的美洲大蠊有效提取物为有效成分的直肠栓剂。本发明提供的美洲大蠊栓剂，具有延长药物释放和作用时间，或迅速释药起效的作用，能够用于治疗溃疡性结肠炎相关的疾病及适应症，显著缓解肠道溃疡及炎症反应，克服口服给药疗效差、起效慢的缺点，提高药物作用效率，为临床患者提高更好的治疗方式，丰富美洲大蠊制剂的临床用药形式。
Description
技术领域：本发明涉及药物制剂领域，具体涉及一种美洲大蠊提取物的栓剂制备及其应用。
背景技术：
溃疡性结肠炎(UC)是一种多发于结直肠黏膜及黏膜下层，病因不明的慢性非特异性炎症性肠病，以黏膜炎症和溃疡形成为病理特点，病灶累及结肠和直肠。在我国尤其是近二十年来，其发病率逐年攀升，国内流行病调查资料显示，UC在南方地区的发病率2.05/10万，北方地区的发病率1.64/10万。UC黏液脓血便和里急后重为主要症状，还伴有腹痛、腹泻，肠道外的表现有关节炎、关节痛、结节性红斑、虹膜炎、皮炎及口腔溃疡等，重度患者可能有发热、贫血、水电解质失调等全身症状。常见的并发症包括直肠炎、肛裂、直肠脓疮、肠穿孔、肠道出血、肠梗阻及结肠癌等。UC病因尚未完全明确，目前还没有针对性很强的特效药，药物治疗主要以抗炎和调节免疫为主。2012年我国“炎性肠病诊断与治疗的共识意见”中提出，UC的治疗目标是缓解临床症状以及促进黏膜愈合，防治并发症，改善患者预后。常用化学药物治疗，如氨基水杨酸类、糖皮质激素类、免疫抑制剂类、抗TNF-α单克隆抗体等，在于尽快控制机体炎症反应，缓解症状。但这类药物普遍存在不良反应，如服用柳氮磺吡啶的患者约有10％-40％出现头疼、恶心、白细胞下降，约有25％的患者不耐受。糖皮质激素类药物易导致机体代谢功能紊乱，水潴留等严重的并发症。硫唑嘌呤等免疫抑制剂肾毒性较大。
中药治疗成为溃疡性结肠炎患者维持缓解和预防复发的更有前景的一种途径，其毒副作用小，且疗效确切。据报道，6859例UC患者中18.6％单独使用西药治疗，20.1％和59.1％患者分别单独使用中药或中西药结合治疗，可见在我国多数UC患者在不同程度上采用中医药治疗。直肠栓剂是一种治疗肠道疾病的有效方式，相比口服给药和保留灌肠有很多优点，例如减少药物对胃肠道的刺激、减少药物对肝脏的损害，不能吞服的小孩和成人也可使用此法给药。药物不被肝脏首过作用破坏，在直肠吸收速度较口服快，可更快速到达患病部位。
美洲大蠊(Periplaneta americana L.)为蜚蠊目蜚蠊科(Blattidae)大蠊属(Periplaneta)昆虫，其药用可追溯到《神农本草经》，“主血淤，癥坚，寒热，破积聚，喉咽痹，内寒，无子，生川泽”。历代重要本草典籍《新修本草》、《本草纲目》、《名医别录》也均有记载。《本草纲目》以“蜚蠊”名将其列为中品，主瘀血癥坚寒热、通利血脉。湖南省中药材标准(2009版)记载美洲大蠊具有健脾消疳、活血通脉、利水消肿、敛疮生肌的功效。现代研究表明，美洲大蠊提取物具有抗肿瘤、抗衰老、保肝、强心、修复溃疡等功效。目前以美洲大蠊为原料已成功研制出肝龙胶囊、消症益肝片、康复新液、心脉隆注射液等药物制剂，其中康复新液在临床上广泛用于治疗外伤、烧烫伤、口腔溃疡、宫颈糜烂、溃疡性结肠炎以及各种消化道溃疡等。临床已有将康复新液单用或与美沙拉嗪、利多卡因等药物通过保留灌肠的方法治疗溃疡性结肠炎，但临床使用较不方便。本发明提供一种美洲大蠊直肠用栓剂，能够有效减轻结肠部位炎症及溃疡症状，缩短治疗周期。
发明内容：
本发明提供了一种增强美洲大蠊提取物缓解溃疡性结肠炎的腔道给药制剂，该制剂使用较灌肠方便、刺激性小，且起效较口服迅速，与常规的美洲大蠊口服制剂相比，可以更快更好的发挥其抗溃疡性结肠炎的作用。
本发明的另一个目的是提供一种美洲大蠊提取物直肠用栓剂的制备方法。
①将美洲大蠊干燥成虫体粉碎至80～100目，加入药材重量6～20倍浓度为50％～90％的乙醇溶液，提取0.5h～2h，提取1～3次，合并提取滤液，45℃～65℃减压浓缩至相对密度1.10～1.30的浸膏，加入3～6倍水萃取，取水萃取液干燥成为稠膏或干膏粉，其中含总氨基酸不少于5％。
②先按所用栓模的量计算出所需主药及基质的量，将处方量的基质在水浴上加热溶化。
③加入步骤1所得提取物粉末及促吸收剂、抗氧化剂、润滑剂、抗菌剂等，充分搅匀，用胶体磨均质乳化，浇模，冷却后取出，晾干，即得。
本发明制备栓剂的工艺简单，可重复，操作可行，并且能产业化生产。根据动物实验，表明本发明所制得的美洲大蠊栓剂比康复新液口服和灌服效果更好。
本发明与国内现有抗溃疡性结肠炎药物相比，具有几个方面的优势：
①操作简单，无需使用灌肠器具，病人乐意接受，增加患者顺应性；对不能吞服的病员更适合此法给药；直肠给药距离结肠病变部位近，药物在直肠吸收较口服更快。
②避免化疗药物疗效差、副作用大的确定。
③使用脂溶性与水溶性基质，可根据需要达到不同药物释放度，适宜于不同临床需求。
具体实施方法：
实施例1
采用美洲大蠊为原料，将美洲大蠊干燥并粉碎至80目，加入10倍重量的80％乙醇溶液，回流提取2次，每次0.5h，过滤，合并滤液，浓缩成相对密度1.10的清膏，加入8倍量水萃取，将水层萃取液喷雾干燥制成干粉。另取混合脂肪甘油酯，置40℃水浴溶化，加入所得提取物粉末、聚乙二醇甘油酯、蓖麻油、甘油、胆酸、尼泊金酯等充分搅匀，重量比为80：5：2：2:3:1:1，趁热倾入冷却并涂有液体石蜡的栓模中至稍有溢出模口为度，待冷却凝固后，用刀削出溢出部分，推出栓剂，晾干，即得脂溶性含药栓剂。
实施例2
采用美洲大蠊为原料，将美洲大蠊干燥并粉碎至80目，加入8倍重量的70％乙醇溶液，回流提取1h，过滤，将滤液浓缩成相对密度1.10的清膏，加入10倍量水萃取，将水层萃取液喷雾干燥制成干粉。另取聚乙二醇400、明胶，置40℃水浴溶化，加入所得提取物粉末、甘油、胆酸、尼泊金酯等充分搅匀，重量比为60：25：5：2:2:1，趁热倾入冷却并涂有液体石蜡的栓模中至稍有溢出模口为度，待冷却凝固后，用刀削出溢出部分，推出栓剂，晾干，即得水溶性含药栓剂。
实施例3
采用美洲大蠊为原料，将美洲大蠊干燥并粉碎至100目，加入12倍重量的75％乙醇溶液，60℃温浸提取1.5h，过滤，将滤液浓缩成相对密度1.15的清膏，加入6倍量水萃取，将水层萃取液喷雾干燥制成干粉。另取聚乙二醇4000、聚乙二醇400，置40℃水浴溶化，加入所得提取物粉末并混合，使药物均匀分散在基质中，重量比为40：50：5，趁热倾入冷却并涂有聚氧乙烯蓖麻油、亚油酸、脂肪酸甘油酯以及植物油的栓模中至稍有溢出模口为度，待冷却凝固后，用刀削出溢出部分，推出栓剂，晾干，即得水溶性含药栓剂。
实施例4
采用美洲大蠊为原料，将美洲大蠊干燥并粉碎至100目，加入15倍重量的70％乙醇溶液，索式提取2次，每次1h，过滤，将滤液浓缩成相对密度1.20的清膏，加入10倍量水萃取，将水层萃取液冷冻干燥制成干粉。另取聚乙二醇2000、硬脂酸聚烃氢(40)酯、甘油，置45℃水浴溶化，加入所得提取物粉末及吐温-80并混合，使药物均匀分散在基质中，重量比为20：55：10：10:2，趁热倾入冷却并涂有液体石蜡的栓模中，待温度降至室温，置于-20℃中冷却30min，至稍有溢出模口为度，待冷却凝固后，用刀削出溢出部分，推出栓剂，晾干，即得。
实施例5
将实施例1-4中所得含药栓剂进行融变时限、溶出度、含量的检测，结果美洲大蠊栓剂表面光滑，在室温25℃成型性较好，有一定的硬度，其重量差异小于百分之5，符合重量差异限度要求；水溶性基质栓剂融变时限＜30min，脂溶性基质栓剂融变时限＜60min，因此本栓剂符合融变时限要求。
实施例6
按照实施例制备出溃疡性结肠炎大鼠模型，将大鼠高脂饮食喂养，颈背部脱毛后，每天以20g/L二硝基氯苯丙酮液滴背1次，每次0.3ml，连续14天。第15天采用尼龙导管经肛门插入结肠，注入0.1％二硝基氯苯乙醇液，第16天同样插管注入8％乙酸溶液2ml，15s后用生理盐水冲洗，制备得溃疡性结肠炎大鼠模型。将溃疡性结肠炎大鼠分为4组：模型组(生理盐水灌肠)、康复新液灌胃组、康复新液灌肠组、美洲大蠊栓剂组，另取一组空白未造模大鼠作为对照。大鼠分笼饲养，给予高脂饲料和正常饮水，共给药治疗4周，4周后对各组大鼠大便情况进行疾病活动指数(DAI)评分，随后处死动物，取各组动物结肠，匀浆后取匀浆液测定炎症因子TNF-α和IL-1β含量。
表1 DAI评分细则
| 评分 | 大便性状 | 隐血或血便 |
| 0 | 正常 | 阴性 |
| 1 | 软便 | 阴性 |
| 2 | 软便 | 隐血阳性 |
| 3 | 腹泻 | 隐血阳性 |
| 4 | 腹泻 | 血便 |
表2各组药物抗溃疡性结肠炎结果
| 组别 | DAI评分 | TNF-α(ng/ml) | IL-1β(ng/ml) |
| 空白组 | 0.6±0.21 | 41.6±8.21 | 58.3±6.58 |
| 模型组 | 10.5±2.13 | 328.6±13.82 | 291.4±9.75 |
| 康复新口服 | 9.3±1.43 | 289.1±12.31 | 236.3±11.28 |
| 康复新灌肠 | 7.7±2.29 | 203.4±14.16 | 198.2±9.35 |
| 美洲大蠊栓剂 | 3.6±0.50 | 101.2±7.84 | 118.2±5.86 |
结果显示，美洲大蠊栓剂与模型组比较有显著差异，说明美洲大蠊栓剂均能有效治疗结肠炎症，且栓剂作用强于康复新液口服或灌肠，说明美洲大蠊栓剂较康复液能明显降低大鼠结肠炎症。
Claims (6)
1.一种含美洲大蠊提取物的栓剂，包括有效量的美洲大蠊提取物游离形式、微粉化、纳米化以及药学上可接受的载体组成，其特征在于：美洲大蠊提取物所占重量比1％～10％，基质所占重量比为50％～80％，吸收促进剂所占重量比为0.5％～3％，增塑剂重量比1％～5％，润滑剂1％～5％，抗氧化剂所占重量比为0.5％～3％，防腐剂所占重量比为0.5％～3％。
2.根据权利要求1所述的栓剂，其特征在于：美洲大蠊提取物为经提取分离纯化后的减压干燥药物、冻干药物、微粉化药物、纳米化药物等一种或多种形式；
所述栓剂基质为聚乙二醇400，聚乙二醇4000，甘油，明胶，聚氧乙烯40，泊洛沙姆，可可豆脂、半合成或全合成脂肪酸甘油酯、半合成椰油酯、半合成苍子油脂和硬脂酸丙二醇酯等的一种或多种；
所述的吸收促进剂为聚乙二醇甘油酯、EDTA及其盐、柠檬酸及其盐、胆酸及其盐、亚油酸及其盐、油酸及其盐、薄荷脑、冰片、尿素、羧甲基纤维素钠、氮酮、环糊精类衍生物等一种或多种；
所述的增塑剂为吐温-80、脂肪酸甘油酯、蓖麻油、甘油、丙二醇中的一种或多种；
所述的润滑剂为油脂性基质的软肥皂、甘油和90％乙醇制成的醇溶液，或亲水性基质栓剂的液体石蜡、植物油等的一种或多种；
所述的抗氧化剂为叔丁基羟基茴香醚、叔丁基对甲酚、没食子酸酯类等的一种或多种；
所述的防腐剂为尼泊金类、苯甲酸与苯甲酸钠、山梨酸等的一种或多种。
3.根据权利要求1中的美洲大蠊提取物的制备方法，其特征在于：将美洲大蠊Peripleneta americana干燥虫体粉碎至80～100目，加入药材重量6～20倍浓度为50％～90％的乙醇溶液，回流提取0.5h～2h，提取1～3次，合并提取滤液，45℃～65℃减压浓缩至相对密度1.10～1.30的浸膏，加入3～6倍水萃取，取水萃取液干燥成为稠膏或干膏粉，其中含总氨基酸不少于5％。
4.权利要求3所述的美洲大蠊提取物可采用机械研磨、超临界流体微粉化制备技术、低温冷冻喷淋技术和水溶液蒸发沉积技术中的一种，制得美洲大蠊提取物微粉。
5.根据权利要求1～4中的栓剂的制备方法，其特征在于：按所用栓膜的量计算出所需主药及基质的量，将处方量的基质在水浴上加热溶化，将美洲大蠊提取物过100目筛，其余固体辅料均过80目筛，将处方量的美洲大蠊提取物加入溶化的基质中并混合，使药物均匀分散在基质中，趁热倾入冷却并涂有增溶剂、吸收促进剂、增塑剂以及润滑剂的栓模中，至稍有溢出模口为度，待冷凝后，用刀削去溢出部分，推出栓剂，晾干，即得。
6.根据权利要求1～5中的栓剂，可以为圆锥形、圆柱形、鱼雷形等形状，每颗重量约2g，长3～4cm，用于直肠给药。
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