CN108926523A - 一种含有维他昔布的口服糊剂药物组合物 - Google Patents

一种含有维他昔布的口服糊剂药物组合物 Download PDF

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CN108926523A
CN108926523A CN201710376846.9A CN201710376846A CN108926523A CN 108926523 A CN108926523 A CN 108926523A CN 201710376846 A CN201710376846 A CN 201710376846A CN 108926523 A CN108926523 A CN 108926523A
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former times
pharmaceutical composition
times cloth
oral paste
content
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侯文彬
华洁
周晶
崔海峰
裴玉宁
李靖
周福军
单淇
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Qingdao Oubofang Medical Technology Co Ltd
BEIJING ORBIEPHARM CO Ltd
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Qingdao Oubofang Medical Technology Co Ltd
BEIJING ORBIEPHARM CO Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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Abstract

本发明涉及一种用于递送药学上可接受的活性成分维他昔布到动物或人对象的适合的药物组合物载体，用于治疗人或动物的与消炎止疼相关的疾病。本发明组合物是一种口服糊剂组合物，特别适合于对马、牛、羊等动物相关疾病的治疗。属于医药技术领域。

Description

一种含有维他昔布的口服糊剂药物组合物
技术领域
本发明涉及一种制造药物递送的口服糊剂型的方法，属于医药技术领域。
背景技术
我公司已授权专利ZL201110160496.5中公布的新化合物维他昔布为一类非甾体抗炎药——高选择性环氧化酶-2(COX-2)抑制剂，维他昔布咀嚼片已经获批可用于犬因外伤、临床手术或肿瘤等原因引起的急、慢性疼痛及炎症。
疼痛或炎症是马、牛、羊等动物身上常见的临床表现，特别是在关节疼、急腹症和结症等马匹频发疾病上表现尤为突出。目前临床上马专用的抗炎镇痛药少之又少，主要都是将牛羊或者人用药用于马匹疼痛的管理，这增加了临床使用的风险和不确定性，同时无法保证疗效。这些疼痛药物多数以注射为主，使用不方便；偶有片剂，适口性差强人意，而且马、牛、羊等动物服用片剂也不是很方便。相比而言，口服糊剂的剂型是一种应用于马、牛、羊等动物特别方便的制剂形式，给药方便易于储存。如奥美拉唑口服糊剂是一种国外已上市销售的用于治疗马胃溃疡类疾病的药物。
本发明所述制剂是一种稳定的半固体口服糊剂，包含维他昔布类药物，可以用于治疗不适合给片剂类的动物如马、羊、牛等，甚至是人，特别容易接受的是马、牛、羊。本发明口服糊剂在室温下放置稳定性好，便于临床使用。
发明内容
本发明提供了一种口服糊剂组合物的制备方法，该药物组合物特别容易接受的动物是马、牛、羊。具体的说，本发明组合物包含：活性成分维他昔布、基质载体、粘度调节剂等。
本发明的药物组合物相对于普通咀嚼片而言可以显著性提高维他昔布在马上的生物利用度，而且本发明的药物组合物马内服后起效快，达峰时间仅0.71h。
本发明的药物组合物口服糊剂稳定性好，易于推广和工业化生产。
本发明中使用的活性物质为维他昔布。是本领域中已知的化合物，其制备方法可以参考相关的文献和专利。含量在0.01-40％之间，优选0.5-30％。
基质载体为三乙酸甘油酯、丙二醇二辛酸酯/二葵酸酯、淀粉、二氧化硅、花生油、芝麻油、大豆油中的一种或多种的组合，优选三乙酸甘油酯、淀粉、二氧化硅，含量在50-95％之间，优选75-90％。
粘度调节剂为聚乙二醇类化合物中的一种或多种的组合，优选聚乙二醇300或聚乙二醇400，含量在 0.01-30％之间，优选0.1-20％
本发明的制备方法为：先混合均匀液体辅料，再加入固体辅料混匀，接着加入维他昔布原料药均质混合均匀，整个过程保持温度在50-60度之间；最后将混合物灌封到合适的给药器中。
本发明所制备的口服糊剂在内服后生物利用度好，同时我们发现维他昔布口服糊剂临床马用给药方便、适口性好，且糊剂质量稳定，便于长期保存(详见实施例1)。
具体实施方式
提供下面的实施例以更加全面的详细说明本发明，但实施例不限制于本发明，其通过所附权利要求完整地限制。
实施例1：
处方组成如下：
原辅料 处方1
维他昔布 6g
三乙酸甘油酯 609.6g
淀粉 101.6
聚乙二醇300 83.8g
制成 100支
制备方法：先混合均匀处方量的三乙酸甘油酯和聚乙二醇300，再加入处方量的淀粉充分混合均匀，最后加入处方量原料药维他昔布，充分均质混合均匀，最后将糊剂灌封到合适的给药器中，整个过程温度保持在50-60℃之间。
我们对处方1进行稳定性研究，并在马上进行药代动力学研究，且与维他昔布咀嚼片做比较，结果如下：
1、稳定性研究
将处方1样品放置加速试验，并与0月比较关键检测指标，结果如下，结果显示处方1的糊剂在加速的保存条件下都很稳定，各检测指标与0天无差异：
2、马药代动力学研究
2.1试验方案
12匹蒙古马，体重300-350kg，随机分为2组(每组6匹)，一组给予维他昔布糊剂(处方1)，另一组给予维他昔布咀嚼片，均空腹给药，剂量0.1mg/kg。颈静脉不同时间点采血测定血浆中维他昔布浓度并计算PK/PD参数。
2.2试验结果
试验结果显示处方1的起效快，达峰时间仅0.71h，生物利用度高。具体数据见下表：

Claims (4)

1.一种口服糊剂的药物组合物，其组成包含活性成分维他昔布、基质载体、粘度调节剂，其活性成分为维他昔布，含量在0.01-40％之间，优选0.5-30％。
2.如权利要求1所述的药物组合物，其基质载体为三乙酸甘油酯、丙二醇二辛酸酯/二葵酸酯、淀粉、二氧化硅、花生油、芝麻油、大豆油中的一种或多种的组合，优选三乙酸甘油酯、淀粉、二氧化硅，含量在50-95％之间，优选75-90％。
3.如权利要求1所述的药物组合物，其粘度调节剂为聚乙二醇类化合物中的一种或多种的组合，优选聚乙二醇300或聚乙二醇400，含量在0.01-30％之间，优选0.1-20％。
4.如权利要求1-3所述的药物组合物，其制备方法为，先混合均匀液体辅料，再向混合物中加入固体辅料，接着加入维他昔布原料药均质混合均匀，整个过程保持温度在50-60度之间；最后将混合物灌封到合适的给药器中。
CN201710376846.9A 2017-05-25 2017-05-25 一种含有维他昔布的口服糊剂药物组合物 Pending CN108926523A (zh)

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112472667A (zh) * 2019-08-23 2021-03-12 青岛欧博方医药科技有限公司 一种维他昔布长效注射液及其制备方法和应用
CN112972481A (zh) * 2021-03-18 2021-06-18 华农（肇庆）生物产业技术研究院有限公司 药物组合物及其制备方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080027011A1 (en) * 2005-12-20 2008-01-31 Hassan Nached Homogeneous paste and gel formulations
CN102464652A (zh) * 2010-11-02 2012-05-23 北京欧博方医药科技有限公司 咪唑衍生物、制备方法及用途

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080027011A1 (en) * 2005-12-20 2008-01-31 Hassan Nached Homogeneous paste and gel formulations
CN102464652A (zh) * 2010-11-02 2012-05-23 北京欧博方医药科技有限公司 咪唑衍生物、制备方法及用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JIANZHONG WANG ET AL.: "Pharmacokinetics of three formulations of vitacoxib in horses", 《JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS》 *

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112472667A (zh) * 2019-08-23 2021-03-12 青岛欧博方医药科技有限公司 一种维他昔布长效注射液及其制备方法和应用
CN112472667B (zh) * 2019-08-23 2022-11-15 北京欧博方医药科技有限公司 一种维他昔布长效注射液及其制备方法和应用
CN112972481A (zh) * 2021-03-18 2021-06-18 华农（肇庆）生物产业技术研究院有限公司 药物组合物及其制备方法和应用

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