CN112545983A - 一种复方硫酸新霉素滴眼液及其制备方法和应用 - Google Patents
一种复方硫酸新霉素滴眼液及其制备方法和应用 Download PDFInfo
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Abstract
本发明涉及一种复方硫酸新霉素滴眼液及其制备方法和应用，属于宠物用滴眼液技术领域，按重量计，该复方硫酸新霉素的组分包括：0.1％‑1％硫酸新霉素、0.1％‑1％乙酰唑胺、0％‑2％甘草酸二钾、0.5％‑1.5％透明质酸钠。本发明利用乙酰唑胺代替传统复方硫酸新霉素滴眼液中的地塞米松，不仅可以解决长期使用硫酸新霉素所带来的不良反应，而且克服了地塞米松容易引起宠物眼部眼压升高的技术问题，对宠物的眼睛更加温和无刺激，相比较现有技术，不仅能够有效解决宠物因结膜炎导致的结膜充血、红肿、分泌物增加等症状，还可以降低因滴用不合适的眼药水导致的宠物眼部刺痒、红血丝、眼周干涩等副作用。
Description
技术领域
本发明属于宠物用滴眼液技术领域，具体涉及一种复方硫酸新霉素滴眼液及其制备方法和应用。
背景技术
近年来，宠物饲养逐年增多。宠物在人们家庭中的地位逐渐提高，在人们生活中起着越来越重要的作用。然而，宠物在带给每个家庭诸多幸福快乐的同时，宠物自身细菌导致宠物易发生结膜炎却引起了人们许多烦恼。诸如猫、狗、兔子等宠物，在饲养过程中经常会发生眼睛周围肿大、眼球红血丝、以及眼周干涩眼屎增多的状况。目前，宠物眼部疾病一般使用人类的滴眼液，盲目性较大，并且效果不明显。
复方硫酸新霉素滴眼液的成分主要含有硫酸新霉素、地塞米松磷酸钠、玻璃酸钠等，是氨基糖苷类广谱抗生素，对革兰氏阴性菌和阳性菌，抗酸杆菌和放线杆菌属都有效，对葡萄球菌的作用比链球菌强，有些变形杆菌和假单孢菌属对本品也敏感。地塞米松磷酸钠具有较强的抗炎及抗过敏作用。复方硫酸新霉素滴眼液主要用于急、慢性结膜炎，葡萄膜炎，巩膜炎，角膜炎，急性巩膜炎，角膜移植术后，青光眼，白内障及眼部机械或化学烧伤处理，也可用于外耳炎。
复方硫酸新霉素滴眼液对结膜炎等疾病疗效显著，但是，长期硫酸新霉素可引起青光眼、白内障、真菌性眼睑炎等疾病，而复方硫酸新霉素滴眼液中加入的地塞米松，也会导致病人眼压升高。此外，复方硫酸新霉素滴眼液为一种人用滴眼液，在治疗宠物眼部疾病的报道相对较少，虽然有将其直接用在宠物上的先例，但盲目性较大，还可能引起宠物的眼部不适。因此，需要开发一种专用于宠物的复方硫酸新霉素滴眼液，以规避常规人用复方硫酸新霉素滴眼液治疗宠物眼部疾病时，给宠物身体带来的意料不到的伤害。因此，提出一种复方硫酸新霉素滴眼液及其制备方法和应用。
发明内容
本发明的目的就在于为了解决上述问题，提供一种复方硫酸新霉素滴眼液及其制备方法和应用，以提供一种专门适用于宠物的复方硫酸新霉素滴眼液，解决宠物眼疾无专门药物治疗的技术问题。
本发明通过以下技术方案来实现上述目的：
本发明提供了一种复方硫酸新霉素滴眼液，按重量计，组分包括：0.1％-1％硫酸新霉素、0.1％-1％乙酰唑胺、0％-2％甘草酸二钾、0.5％-1.5％透明质酸钠。
作为本发明的进一步优化方案，所述复方硫酸新霉素滴眼液的组分还包括：0.4％-0.8％氯化钠、0.4％-0.8％硼砂、0.1％-0.5％亚硫酸氢钠、0.01％-0.5％羟丙甲纤维素和0.2％-0.8％冰片。
作为本发明的进一步优化方案，所述复方硫酸新霉素滴眼液的组分包括：1％硫酸新霉素、1％乙酰唑胺、2％甘草酸二钾、1％透明质酸钠，0.6％氯化钠、0.6％硼砂、0.3％亚硫酸氢钠、0.2％羟丙甲纤维素和0.5％冰片。
本发明还提供了一种上述复方硫酸新霉素滴眼液的制备方法，步骤包括：
(1)按组分配比，称取氯化钠、硼砂、亚硫酸氢钠、羟丙甲纤维素和冰片，加入处方量85％的蒸馏水，加热煮沸灭菌，冷却，获得A组分；
(2)分别将透明质酸钠和甘草酸二钾用蒸馏水溶解，混合，获得B组分；
(3)将步骤(1)的A组分与步骤(2)的B组分混合，搅拌，超声溶解至无肉眼观测固形物，获得C组分；
(4)将硫酸新霉素和乙酰唑胺混合，加入步骤(3)的C组分中，利用蒸馏水定容至处方量，过滤去除杂质，灭菌后，得到复方硫酸新霉素滴眼液。
作为本发明的进一步优化方案，所述步骤(1)或步骤(4)的灭菌的条件为：121℃下高压蒸汽灭菌20-30min。
本发明还提供了上述复方硫酸新霉素滴眼液在作为治疗宠物结膜炎药物中的应用。
作为本发明的进一步优化方案，所述宠物为猫或狗。
本发明的有益效果在于：利用乙酰唑胺代替地塞米松，不仅可以解决长期使用硫酸新霉素所带来的不良反应，而且克服了地塞米松容易引起宠物眼部眼压升高的技术问题，对宠物的眼睛更加温和无刺激。此外，本发明的复方硫酸新霉素滴眼液中还加入了甘草酸二钾成分，甘草酸二钾与主药硫酸新霉素和乙酰唑胺具有协同增效作用，可有效解决宠物因结膜炎导致的结膜充血、红肿、分泌物增加等症状，以及因滴用不合适的眼药水导致的眼部刺痒、红血丝、眼周干涩等副作用。
具体实施方式
下面对本申请作进一步详细描述，有必要在此指出的是，以下具体实施方式只用于对本申请进行进一步的说明，不能理解为对本申请保护范围的限制，该领域的技术人员可以根据上述申请内容对本申请作出一些非本质的改进和调整。
实施例1
本实施例提供了8种复方硫酸新霉素滴眼液，按重量计，组分及其质量百分比如下表1所示：
表1：
| 组分 | 1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 |
| 硫酸新霉素 | 0.1％ | 0.5％ | 1.0％ | 0.5％ | 1.0％ | 0.6％ | 0.4％ | 0.1％ |
| 乙酰唑胺 | 0.1％ | 0.5％ | 1.0％ | 0.5％ | 0.1％ | 0.4％ | 0.6％ | 1.0％ |
| 甘草酸二钾 | 2.0％ | 2.0％ | 2.0％ | 0％ | 0.5％ | 1.0％ | 1.5％ | 2.0％ |
| 透明质酸钠 | 1.0％ | 1.0％ | 1.0％ | 1.0％ | 0.5％ | 0.8％ | 1.5％ | 1.2％ |
| 氯化钠 | 0.6％ | 0.6％ | 0.6％ | 0.6％ | 0.4％ | 0.5％ | 0.7％ | 0.8％ |
| 硼砂 | 0.6％ | 0.6％ | 0.6％ | 0.6％ | 0.8％ | 0.5％ | 0.7％ | 0.4％ |
| 亚硫酸氢钠 | 0.3％ | 0.3％ | 0.3％ | 0.3％ | 0.2％ | 0.4％ | 0.5％ | 0.1％ |
| 羟丙甲纤维素 | 0.2％ | 0.2％ | 0.2％ | 0.2％ | 0.4％ | 0.0％1％ | 0.2％ | 0.5％ |
| 冰片 | 0.5％ | 0.5％ | 0.5％ | 0.5％ | 0.3％ | 0.2％ | 0.8％ | 0.5％ |
上述复方硫酸新霉素滴眼液的制备方法，包括以下步骤：
(1)按组分配比，称取氯化钠、硼砂、亚硫酸氢钠、羟丙甲纤维素和冰片，加入处方量85％的蒸馏水，加热煮沸，121℃下高压蒸汽灭菌20-30min，冷却，获得A组分；
(2)分别将透明质酸钠和甘草酸二钾用蒸馏水溶解，混合，获得B组分；
(3)将步骤(1)的A组分与步骤(2)的B组分混合，搅拌，超声溶解至无肉眼观测固形物，获得C组分；
(4)将硫酸新霉素和乙酰唑胺混合，加入步骤(3)的C组分中，利用蒸馏水定容至处方量，过滤去除杂质，121℃下高压蒸汽灭菌20-30min，无菌封装，得到复方硫酸新霉素滴眼液。
对比例1：
本对比例提供了一种复方硫酸新霉素滴眼液，按重量计，其组分及其质量百分比包括：0.5％硫酸新霉素、0.5％地塞米松磷酸钠、2％甘草酸二钾、1％透明质酸钠，0.6％氯化钠、0.6％硼砂、0.3％亚硫酸氢钠、0.2％羟丙甲纤维素和0.5％冰片。该复方硫酸新霉素滴眼液的制备方法同实施例1。
试验例1：家兔细菌性结膜炎实验
实验方法：参照中国专利文献《一种治疗细菌感染引起的眼结膜炎和角膜炎的石斛滴眼液》(申请号CN201710487091.X)中家兔细菌性结膜炎试验，取患有细菌性结膜炎的家兔60只，雌雄各半，平均分成10组，每组6只(记为A-F)，分别采用实施例组1-8、对比例1的滴眼液和生理盐水(空白对照)(编号依次为1-10)进行治疗，治疗方法为，每日三次，每次0.1ml，连续给药5天。
每天进行观察评分，评分标准如下表2所示：
表2：
将各项评分累加，0-2为无结膜炎症状，3-4为轻度结膜炎症状，5-6为中度结膜炎症状，7-9为重度结膜炎症状。
结果如下表3所示：
表3：
注：疗效率＝(1-治疗后得分/治疗前评分)×100％
实验结果表明，家兔结膜炎自然痊愈疗效在42％，组1至3、4至8，对家兔结膜炎的疗效均达90％上，平均疗效达96％以上，治疗效果显著；组4中无甘草酸二钾，治疗虽有效果但效果不及组1至3和4至8；组9采用地塞米松磷酸钠，且组9中含有甘草酸二钾，治疗效果不及组1至3和4至8，说明甘草酸二钾与主药硫酸新霉素和乙酰唑胺具有协同增效作用，可有效解决宠物因结膜炎导致的结膜充血、红肿、分泌物增加等症状，以及因滴用不合适的眼药水导致的眼部刺痒、红血丝、眼周干涩等副作用。
试验例2：动物眼压影响实验
选取患有青光眼的家兔、小猎兔犬、家猫各12只，每个品种分4组(每组3只)，分别用实施例1的组2、4，对比例1滴眼液进行治疗，以生理盐水作为空白对照，与给药后0、2、4、8、12、24小时对试验动物的眼压进行测量，取各组3只动物的眼压平均值作为最终测试值，眼压单位：mmHg。
结果如下表3-5所示：
表4：家兔眼压测定结果
| 组别 | 0 | 2 | 4 | 8 | 12 | 24 |
| 组2 | 38.6±4.2 | 27.6±3.3 | 25.1±3.4 | 23.2±3.1 | 20.7±3.4 | 18.2±3.4 |
| 组4 | 37.9±4.5 | 26.8±4.2 | 23.1±4.2 | 22.1±4.3 | 21.1±4.3 | 20.9±3.8 |
| 对比例1 | 38.2±3.9 | 27.5±4.1 | 25.2±4.1 | 21.7±4.5 | 22.2±4.0 | 21.2±4.3 |
| 空白组 | 37.8±4.6 | 36.6±5.1 | 37.7±4.7 | 36.8±4.5 | 36.8±4.3 | 37.8±3.8 |
表5：小猎兔犬眼压测定结果
| 组别 | 0 | 2 | 4 | 8 | 12 | 24 |
| 组2 | 25.2±4.2 | 21.5±3.7 | 20.2±3.9 | 16.9±4.1 | 14.8±4.3 | 14.6±3.4 |
| 组4 | 25.4±4.1 | 22.6±3.6 | 21.3±4.0 | 17.8±4.0 | 15.9±4.4 | 15.5±3.6 |
| 对比例1 | 25.9±4.5 | 20.6±4.2 | 20.5±4.4 | 22.3±4.2 | 22.0±4.3 | 21.6±4.1 |
| 空白组 | 25.1±3.9 | 24.7±4.1 | 24.3±4.3 | 24.1±3.8 | 24.3±4.0 | 24.6±4.1 |
表6：家猫眼压测定
| 组别 | 0 | 2 | 4 | 8 | 12 | 24 |
| 组2 | 24.7±3.7 | 22.0±3.2 | 19.7±3.8 | 17.3±4.0 | 14.2±4.1 | 14.3±3.7 |
| 组4 | 24.8±4.1 | 22.8±3.8 | 22.2±4.2 | 20.8±4.2 | 18.8±3.8 | 16.6±3.9 |
| 对比例1 | 24.2±4.0 | 23.2±4.2 | 22.2±3.9 | 20.3±4.1 | 19.7±3.8 | 19.3±4.2 |
| 空白组 | 24.3±3.6 | 24.3±4.1 | 24.7±4.3 | 24.3±3.8 | 24.1±4.0 | 24.5±4.1 |
实验结果表明，组2和组4对家兔、小猎兔犬、家猫均有降低眼压的作用，但组4的效果略差，说明甘草酸二钾与乙酰唑胺配合，对眼压的降低也有促进作用，对比例1中均出现了家兔、小猎兔犬、家猫眼压先降低后上升的情况，说明地塞米松磷酸钠滴眼液具有不良反应，长期使用可使家兔、小猎兔犬、家猫眼压升高，对小猎兔犬、家猫尤其严重，因此本发明方案尤其适合狗和猫。
以上所述实施例仅表达了本发明的几种实施方式，其描述较为具体和详细，但并不能因此而理解为对本发明专利范围的限制。应当指出的是，对于本领域的普通技术人员来说，在不脱离本发明构思的前提下，还可以做出若干变形和改进，这些都属于本发明的保护范围。
Claims (7)
1.一种复方硫酸新霉素滴眼液，其特征在于，按重量计，组分包括：0.1％-1％硫酸新霉素、0.1％-1％乙酰唑胺、0％-2％甘草酸二钾、0.5％-1.5％透明质酸钠。
2.根据权利要求1所述的一种复方硫酸新霉素滴眼液，其特征在于，所述复方硫酸新霉素滴眼液的组分还包括：0.4％-0.8％氯化钠、0.4％-0.8％硼砂、0.1％-0.5％亚硫酸氢钠、0.01％-0.5％羟丙甲纤维素和0.2％-0.8％冰片。
3.根据权利要求2所述的一种复方硫酸新霉素滴眼液，其特征在于，所述复方硫酸新霉素滴眼液的组分包括：1％硫酸新霉素、1％乙酰唑胺、2％甘草酸二钾、1％透明质酸钠，0.6％氯化钠、0.6％硼砂、0.3％亚硫酸氢钠、0.2％羟丙甲纤维素和0.5％冰片。
4.一种如权利要求1-3任一所述的复方硫酸新霉素滴眼液的制备方法，其特征在于，步骤包括：
(1)按组分配比，称取氯化钠、硼砂、亚硫酸氢钠、羟丙甲纤维素和冰片，加入处方量85％的蒸馏水，加热煮沸灭菌，冷却，获得A组分；
(2)分别将透明质酸钠和甘草酸二钾用蒸馏水溶解，混合获得B组分；
(3)将步骤(1)的A组分与步骤(2)的B组分混合，搅拌，超声溶解至无肉眼观测固形物，获得C组分；
(4)将硫酸新霉素和乙酰唑胺混合，加入步骤(3)的C组分中，利用蒸馏水定容至处方量，过滤去除杂质，灭菌后，得到复方硫酸新霉素滴眼液。
5.根据权利要求4所述的一种复方硫酸新霉素滴眼液的制备方法，其特征在于，所述步骤(1)或步骤(4)的灭菌的条件为：121℃下高压蒸汽灭菌20-30min。
6.一种如权利要求1-3任一所述的复方硫酸新霉素滴眼液在作为治疗宠物结膜炎药物中的应用。
7.根据权利要求6所述的一种复方硫酸新霉素滴眼液在作为治疗宠物结膜炎药物中的应用，其特征在于，所述宠物为猫或狗。
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Application publication date: 20210326 |
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