CN112641763A - 一种治疗过敏性疾病的口腔速溶膜及其制备方法 - Google Patents
一种治疗过敏性疾病的口腔速溶膜及其制备方法 Download PDFInfo
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Abstract
本发明公布了一种治疗过敏性疾病的口腔速溶膜及其制备方法,包括以下组分:盐酸西替利嗪、成膜材料、增塑剂、甜味剂和pH调节剂;各组分的重量份为:盐酸西替利嗪2.5‑10份、成膜材料30‑70份、增塑剂2‑10份、甜味剂0.2‑0.5份和pH调节剂0.5‑1.0份。作为本发明进一步优化的技术方案,所述盐酸西替利嗪口腔速溶膜外观良好,柔韧性适中,口感良好,溶化时限短,起效迅速,携带方便,服药顺应性好,并且制备工艺简单,成本低。
Description
技术领域
本发明属于医药技术领域,具体涉及一种盐酸西替利嗪口腔速溶膜及其制备方法。
背景技术
盐酸西替利嗪(cetirizine hydrochloride),化学名:(±)-2-[2-[4-[(4-氯苯基)苯甲基]-1-哌嗪基]乙氧基]乙酸二盐酸盐,分子式:C21H25ClN2O3·2HCl;分子量:461.81;化学结构式如下:
盐酸西替利嗪为白色或类白色结晶性粉末;无臭、味苦。在水中易溶,在甲醇或乙醇中溶解,在氯仿或丙酮中几乎不溶。西替利嗪是人体内羟嗪的代谢产物,动物实验证明盐酸西替利嗪为选择性组胺H1受体拮抗剂,抑制组胺的传递作用,还可抑制参与变态反应的血管活性肽及P物质,减少炎症细胞的移动,有效地抑制皮肤变态反应,对变态反应发作时的嗜酸粒细胞的活化与趋化有抑制作用;对变应原皮肤试验,鼻粘膜及支气管激发试验亦有明显的抑制作用。
盐酸西替利嗪是一种抗过敏药,是新一代H1受体拮抗剂,属第二代H1抗组胺药,无抗胆碱和抗5-羟色胺的作用,极少透过血脑屏障,对中枢性H1受体的亲和性低,临床使用时中枢抑制作用较轻。对不同化学诱导性介质包括血管活性多肽、P物质及神经肽等和嗜酸性粒细胞趋化反应有抑制作用,口服见效快,作用强而持久。副作用轻微,表现为嗜睡、疲劳,表情淡漠、注意力不集中等,一般不必停药。临床上用于治疗季节性或常年性过敏性鼻炎、由过敏原引起的荨麻疹及皮肤瘙痒。
西替利嗪口服后经由胃肠道吸收。健康成人一次口服10mg西替利嗪,血药浓度达峰时间(tmax)为1.0±0.5h,血药峰浓度为300ng/ml。药代动力学参数(例如峰值血浆浓度(Cmax)和曲线下面积(AUC))的分布是单峰的。西替利嗪的吸收程度不会随食物的增加而降低,尽管吸收率会降低。当西替利嗪以溶液,胶囊或片剂形式给药时,生物利用度的程度相似,表观分布体积为0.50L/kg。西替利嗪与血浆蛋白结合率高,可以达到93±0.3%,血浆半衰期约10小时,约70%以原形药物随尿液排泄,少量从粪便排泄。
西替利嗪作为一种强效抗过敏药物,由于其抗组胺作用强,疗效与安全性好,患者服药次数少、用药剂量低、副作用小,对西替利嗪药物的研究与开发众多,目前盐酸西替利嗪主要制剂为片剂、口服液、滴剂、口腔崩解片等类型,由于口崩片、胶囊、普通片为固体制剂,老年人、儿童患者服用存在一定的困难,起效慢,在没有水的情况下难以服用。对于口服液和滴剂,虽然起效快,但服用时需定量杯、药匙或滴管,并且液体制剂稳定性差,携带不方便,对于药品的包装、储存、运输要求极为严格。
口腔速溶膜具有置于口腔内,立即溶解释放药物,无需开水送服,吞咽后在胃肠道立即释放等优点。因此,开发一种盐酸西替利嗪口腔速溶膜,将具有重要的市场价值和社会效益。
发明内容
本发明所要解决的技术问题是提供一种盐酸西替利嗪口腔速溶膜,其溶化时间短,释放药物迅速,且无需用水吞服,口感良好;
本发明所要解决的另一个技术问题是提供一种所述盐酸西替利嗪口腔速溶膜的制备方法,该方法工艺简易,所制得的口腔速溶膜具有较高的机械强度及耐磨性。
为解决上述技术问题,本发明所采取的技术方案是:
本发明首先公开了一种盐酸西替利嗪口腔速溶膜,包括以下各组分:盐酸西替利嗪、成膜材料、增塑剂、甜味剂和pH调节剂。
各组分的重量份为:盐酸西替利嗪2.5-10份、成膜材料30-70份、增塑剂2-10份、甜味剂0.2-0.5份和pH调节剂0.5-1.0份;
优选的,盐酸西替利嗪5-10份、成膜材料30-90份、增塑剂3-7份、甜味剂0.2-0.3份和pH调节剂0.5-0.6份;
进一步优选的,盐酸西替利嗪5份、成膜材料50-80份、增塑剂4份、甜味剂0.3份和pH调节剂0.6份;
最优选的,盐酸西替利嗪5份、成膜材料60份、增塑剂4份、甜味剂0.3份和pH调节剂0.6份。
本发明所述盐酸西替利嗪口腔速溶膜,还包括:水,优选为纯化水;所述水的重量份为500-1500份,优选为700-1200份,最优选为1000份。
其中,所述成膜材料选自聚乙烯醇-聚乙二醇共聚物、聚乙烯醇、西黄芪胶、海藻酸钠、明胶、羟丙甲琥珀酸酯、虫胶、阿拉伯胶、琼脂、甲基纤维素、乙基纤维素、羟丙纤维素或羟丙甲纤维素中的任意一种或任意两种按照任意比例组成的混合物;优选为羟丙甲纤维素或海藻酸钠;最优选为羟丙甲纤维素;
所述增塑剂选自聚乙二醇、甘油、1,2-丙二醇、硅油、甘露糖醇、山梨醇、聚丙二醇或己二醇中的任意一种或任意两种按照任意比例组成的混合物;优选为甘油、1,2-丙二醇或山梨醇;最优选为甘油和1,2-丙二醇的混合物;
所述甜味剂选自三氯蔗糖、阿斯巴甜、甜菊苷、甘草甜素、糖精、糖精钠、果糖或蔗糖中的任意一种或任意两种按照任意比例组成的混合物;优选为糖精钠或三氯蔗糖;
所述pH调节剂选自冰醋酸、醋酸钠、枸橼酸或酒石酸中的任意一种或两种按照任意比例组成的混合物;优选为冰醋酸和醋酸钠的混合物。
本发明进一步公开了一种所述盐酸西替利嗪口腔速溶膜的制备方法,包括以下步骤:
(1)按照所述配比称取各组分,将所述成膜材料溶于纯化水中,充分搅拌成均匀,得到A液,备用;
(2)将所述盐酸西替利嗪溶于纯化水中,充分搅拌后再添加所述甜味剂和增塑剂,搅拌均匀后加入pH调节剂调节pH值,之后继续充分搅拌,混合均匀,得到B液;
(3)将B液在搅拌状态下加入到A液中,搅拌至均匀后,静置以排出气泡;
(4)排除气泡后,得到刮涂用凝胶;将所述刮涂用凝胶刮涂至玻璃板上,烘干,冷却后从玻璃板上剥离膜剂,剪切分装,即得。
其中,步骤(1)中所述成膜材料:纯化水=6g:60~80ml,优选为成膜材料:纯化水=6g:70ml,搅拌的时间为2-16h,优选为4h;步骤(2)所述中盐酸西替利嗪:纯化水=0.5g:20~40ml,优选为盐酸西替利嗪:纯化水=0.5g:30ml;步骤(4)中所述烘干的温度为40-60℃;优选为40℃。
本发明方法能够使所制得的口腔速溶膜具有较高的机械强度及耐磨性,可以保证药膜在包装、运输、取用时不破裂,并保持良好的外观。
本发明盐酸西替利嗪口腔速溶膜的组成中,成膜材料、增塑剂的种类和用量对盐酸西替利嗪口腔速溶膜的外观、口感和溶化时间具有明显的影响。在其他组分及用量一定的条件下:当成膜材料种类为羟丙甲纤维素,所制备的盐酸西替利嗪口腔速溶膜溶化时限明显短于成膜材料为聚乙烯醇,或者由羟丙甲纤维素和聚乙烯醇按照质量比1:2组成的混合物,粘度15cP的羟丙基甲基纤维素相比其它粘度的羟丙基甲基纤维素,具有更好的成膜性能;增塑剂至少包括1,2-丙二醇、甘油中的一种,以甘油为增塑剂,膜剂的外观较差,有白色颗粒析出。无论是甘油还是1,2-丙二醇,随着膜剂增塑剂增多,耐折有较明显的改善,以甘油为增塑剂有较好的耐折,但是膜剂的崩解时间较长;以1,2-丙二醇为增塑剂膜剂的耐折较差,崩解性能较好,当增塑剂为1,2-丙二醇和甘油的混合物时,将1,2-丙二醇和甘油的重量比设置为0.5:1~2:1能够同时满足膜剂的耐折性好和崩解性能好,优选地,1,2-丙二醇和甘油的重量比为1:1。
本发明技术方案与现有技术相比,具有以下有益效果:
本发明盐酸西替利嗪口腔速溶膜携带方便,可在口腔内快速溶解,并释放药物,无需用水吞服;服药顺应性好,特别适宜老人及吞咽困难的患者服用,质量稳定,起效迅速;解决了盐酸西替利嗪片剂和胶囊起效慢,服用不方便,口服液携带不方便,不利于定量服用,在低温条件下容易冻结;口腔崩解片制备工艺复杂,需要特殊设备等缺点。本发明盐酸西替利嗪口腔速溶膜中辅料用量小,制备工艺简单,成本较低,具有可观的经济和社会效益。
具体实施方式
下面结合具体实施例来进一步描述本发明,本发明的优点和特点将会随着描述而更为清楚。但是应理解所述实施例仅是范例性的,不对本发明的范围构成任何限制。本领域技术人员应该理解的是,在不偏离本发明的精神和范围下可以对本发明技术方案的细节和形式进行修改或替换,但这些修改或替换均落入本发明的保护范围。
实施例1
每片含盐酸西替利嗪5mg,1000片盐酸西替利嗪口腔速溶膜的组成为:
制备方法如下:
(1)将羟丙甲纤维素溶于700ml纯化水中,搅拌均匀,作为A液。
(2)将盐酸西替利嗪溶于300ml水中,搅拌至完全溶解后加入糖精钠和甘油,再加入醋酸缓冲液调节pH值,加完后搅拌均匀,作为B液。
(3)在搅拌状态下将B液加入到A液中,混合均匀。静置过夜,以排除气泡。
(4)排除气泡后,即得刮涂用凝胶。将此胶液刮涂至玻璃板上,在40℃烘干,冷却后将膜剂从玻璃板上剥离,剪切分装,即可。
该膜剂外观不均匀,有部分白色颗粒析出,柔韧性较好,不易折断,有沙粒感,入口溶解慢,粘度小,溶化时限55s。
实施例2
每片含盐酸西替利嗪5mg,1000片盐酸西替利嗪口腔速溶膜的组成为:
制备方法如下:
(1)将羟丙甲纤维素溶于700ml纯化水中,搅拌均匀,作为A液。
(2)将盐酸西替利嗪溶于300ml水中,搅拌至完全溶解后加入糖精钠和甘油,再加入醋酸缓冲液调节pH值,加完后搅拌均匀,作为B液。
(3)在搅拌状态下将B液加入到A液中,混合均匀。静置过夜,以排除气泡。
(4)排除气泡后,即得刮涂用凝胶。将此胶液刮涂至玻璃板上,在40℃烘干,冷却后将膜剂从玻璃板上剥离,剪切分装,即可。
该膜剂外观均匀,柔韧性较差,易折断,入口溶解迅速,粘度小,溶化时限21s。
实施例3
每片含盐酸西替利嗪5mg,1000片盐酸西替利嗪口腔速溶膜的组成为:
制备方法如下:
(1)将羟丙甲纤维素溶于700ml纯化水中,搅拌均匀,作为A液。
(2)将盐酸西替利嗪溶于300ml水中,搅拌至完全溶解后加入糖精钠和甘油,再加入醋酸缓冲液调节pH值,加完后搅拌均匀,作为B液。
(3)在搅拌状态下将B液加入到A液中,混合均匀。静置过夜,以排除气泡。
(4)排除气泡后,即得刮涂用凝胶。将此胶液刮涂至玻璃板上,在40℃烘干,冷却后将膜剂从玻璃板上剥离,剪切分装,即可。
该膜剂外观有花斑,柔韧性一般,可折断,入口溶解迅速,粘度小,溶化时限39s。
实施例4
每片含盐酸西替利嗪5mg,1000片盐酸西替利嗪口腔速溶膜的组成为:
制备方法如下:
(1)将羟丙甲纤维素溶于700ml纯化水中,搅拌均匀,作为A液。
(2)将盐酸西替利嗪溶于300ml水中,搅拌至完全溶解后加入糖精钠和甘油,再加入醋酸缓冲液调节pH值,加完后搅拌均匀,作为B液。
(3)在搅拌状态下将B液加入到A液中,混合均匀。静置过夜,以排除气泡。
(4)排除气泡后,即得刮涂用凝胶。将此胶液刮涂至玻璃板上,在40℃烘干,冷却后将膜剂从玻璃板上剥离,剪切分装,即可。
该膜剂外观均匀,柔韧性较好,不易折断,入口溶解迅速,粘度适中,溶化时限28s。
实施例5
每片含盐酸西替利嗪5mg,1000片盐酸西替利嗪口腔速溶膜的组成为:
制备方法如下:
(1)将羟丙甲纤维素溶于700ml纯化水中,搅拌均匀,作为A液。
(2)将盐酸西替利嗪溶于300ml水中,搅拌至完全溶解后加入糖精钠和甘油,再加入醋酸缓冲液调节pH值,加完后搅拌均匀,作为B液。
(3)在搅拌状态下将B液加入到A液中,混合均匀。静置过夜,以排除气泡。
(4)排除气泡后,即得刮涂用凝胶。将此胶液刮涂至玻璃板上,在60℃烘干,冷却后将膜剂从玻璃板上剥离,剪切分装,即可。
该膜剂外观一般,膜剂周边有卷边,柔韧性较差,柔韧性较好,易折断,入口溶解迅速,吸水快,粘度一般,溶化时限35s。
Claims (8)
1.一种治疗过敏性疾病的口腔速溶膜,其特征在于,包括以下各组分:盐酸西替利嗪、成膜材料、增塑剂、甜味剂和pH调节剂。
2.按照权利要求1所述的治疗过敏性疾病的口腔速溶膜,其特征在于,各组分的重量份为:盐酸西替利嗪2.5-10份、成膜材料30-70份、增塑剂2-10份、甜味剂0.2-0.5份和pH调节剂0.5-1.0份。
3.按照权利要求2所述的治疗过敏性疾病的口腔速溶膜,其特征在于:盐酸西替利嗪5份、成膜材料60份、增塑剂4份、甜味剂0.3份和pH调节剂0.6份。
4.按照权利要求1、2或3中任一项所述的治疗过敏性疾病的口腔速溶膜,其特征在于,还包括:水;所述的水的重量份为500-1500份,优选为700-1200份,最优选为1000份。
5.按照权利要求3所述的治疗过敏性疾病的口腔速溶膜,其特征在于,所述的成膜材料选自聚乙烯醇-聚乙二醇共聚物、聚乙烯醇、西黄芪胶、海藻酸钠、明胶、羟丙甲琥珀酸酯、虫胶、阿拉伯胶、琼脂、甲基纤维素、乙基纤维素、羟丙纤维素或羟丙甲纤维素中的任意一种或任意两种按照任意比例组成的混合物;优选为羟丙甲纤维素或海藻酸钠;最优选为羟丙甲纤维素。
6.按照权利要求4所述的治疗过敏性疾病的口腔速溶膜,其特征在于,所述增塑剂为聚乙二醇、甘油、1,2-丙二醇、硅油、甘露糖醇、山梨醇、聚丙二醇或己二醇中的任意一种或任意两种按照任意比例组成的混合物中的一种;
所述pH调节剂为冰醋酸、醋酸钠、枸橼酸或酒石酸中的任意一种或两种按照任意比例组成的混合物中的一种;
所述甜味剂选自三氯蔗糖、阿斯巴甜、甜菊苷、甘草甜素、糖精、糖精钠、果糖或蔗糖中的任意一种或任意两种按照任意比例组成的混合物的一种。
7.根据权利要求5所述的治疗过敏性疾病的口腔速溶膜,其特征在于,所述增塑剂为甘油、1,2-丙二醇或山梨醇;最优选为甘油和1,2-丙二醇的混合物;所述pH调节剂为冰醋酸和醋酸钠的混合物;所述甜味剂为糖精钠或三氯蔗糖。
8.一种权利要求6任何一项所述治疗过敏性疾病的口腔速溶膜的制备方法,其特征在于,包括以下步骤:
1)按照所述配比称取各组分,将所述成膜材料溶于纯化水中,充分搅拌成均匀,得到A液,备用;
2)将所述盐酸西替利嗪溶于纯化水中,充分搅拌后再添加所述甜味剂和增塑剂,搅拌均匀后加入pH调节剂调节pH值,之后继续充分搅拌,混合均匀,得到B液;
3)将B液在搅拌状态下加入到A液中,搅拌至均匀后,静置以排出气泡;
4)排除气泡后,得到刮涂用凝胶;将所述刮涂用凝胶刮涂至玻璃板上,烘干,冷却后从玻璃板上剥离膜剂,剪切分装,即得;
其中,步骤1)中所述成膜材料:纯化水=6g:60~80ml,优选为成膜材料:纯化水=6g:70ml,搅拌的时间为2-16h,优选为4h;步骤2)所述中盐酸西替利嗪:纯化水=0.5g:20~40ml,优选为盐酸西替利嗪:纯化水=0.5g:30ml;步骤4)中所述烘干的温度为40-60℃;优选为40℃。
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