CN108524466A - 一种氟苯尼考微囊制剂及其制备方法 - Google Patents
一种氟苯尼考微囊制剂及其制备方法 Download PDFInfo
- Publication number
- CN108524466A CN108524466A CN201810710233.9A CN201810710233A CN108524466A CN 108524466 A CN108524466 A CN 108524466A CN 201810710233 A CN201810710233 A CN 201810710233A CN 108524466 A CN108524466 A CN 108524466A
- Authority
- CN
- China
- Prior art keywords
- florfenicol
- parts
- cosolvent
- preparation
- auxiliary agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/429—Thiazoles condensed with heterocyclic ring systems
- A61K31/43—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems
- A61K31/431—Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula, e.g. penicillins, penems containing further heterocyclic rings, e.g. ticarcillin, azlocillin, oxacillin
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/35—Caprifoliaceae (Honeysuckle family)
- A61K36/355—Lonicera (honeysuckle)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/39—Convolvulaceae (Morning-glory family), e.g. bindweed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/71—Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/72—Rhamnaceae (Buckthorn family), e.g. buckthorn, chewstick or umbrella-tree
-
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- 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
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/10—Anthelmintics
- A61P33/12—Schistosomicides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/14—Ectoparasiticides, e.g. scabicides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Tropical Medicine & Parasitology (AREA)
- Mycology (AREA)
- Alternative & Traditional Medicine (AREA)
- Biotechnology (AREA)
- Botany (AREA)
- Medical Informatics (AREA)
- Microbiology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Inorganic Chemistry (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明公开了一种氟苯尼考微囊制剂及其制备方法,其制作原料包括氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,且所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:2.5‑3.5,所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/5‑1/3。本发明用特定占比的氟苯尼考制得的微囊制剂,其配合相关助剂,使得药物服用后,有效增强了灭菌和灭寄生虫的效果;并且药物用量少,药物峰浓度降低,药物的毒副作用大大减少,安全性更高。
Description
技术领域
本发明涉及动物药品的制备技术领域,具体涉及一种氟苯尼考微囊制剂及其制备方法。
背景技术
动物寄生虫病是家畜传染性疾病不可忽视的重要组成部分,且病原寄生虫种类繁多,常见的体内寄生虫有蛔虫、鞭毛虫、圆线虫、旋毛虫、结节虫、球虫、绦虫、吸虫等,体外寄生虫有蜱、蚤、蝇、蜱、虱等。它严重影响肉、乳、蛋的产量,皮毛的质量,严重制约畜牧业的健康发展及某些人畜共患寄生虫病还直接危害人类的健康,给畜牧养殖行业造成巨大的经济损失同时也引起严重的公共卫生问题。
氟苯尼考(Florfeniol),抗生素类药物,通过抑制肽酰基转移酶活性而产生广谱抑菌作用,抗菌谱广,包括各种革兰氏阳性、阴性菌和支原体等。敏感菌包括牛、猪的嗜血杆菌、痢疾志贺氏菌、沙门氏菌、大肠杆菌、肺炎球菌、流感杆菌、链球菌、金黄色葡萄球菌、衣原体、钩端螺旋体,立克次氏体等。
发明内容
本发明的目的在于提供一种氟苯尼考微囊制剂及其制备方法,其解决了牲畜服用传统氟苯尼考药物灭菌和灭寄生虫效果差以及毒副作用大,安全性较低的缺陷。
本发明通过以下技术方案来实现上述目的:
一种氟苯尼考微囊制剂,其制作原料包括氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,且所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:2.5-3.5,所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/5-1/3。
进一步改进在于,所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:3。
进一步改进在于,所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/4。
进一步改进在于,所述助剂由失水山梨醇脂肪酸酯、阿拉伯胶、β-环糊精、月桂氮卓酮、咖啡酸、苄星青霉素、苯甲酸钠、冰片、三氯叔丁醇、妥曲珠利、白头翁、金银花提取物、牵牛子、多叶勾儿茶和维生素C组成。
进一步改进在于,所述助剂按质量份数由2-4份失水山梨醇脂肪酸酯、1-3份阿拉伯胶、2-4份β-环糊精、1-3份月桂氮卓酮、3-5份咖啡酸、1-4份苄星青霉素、2-4份苯甲酸钠、1-3份冰片、2-4份三氯叔丁醇、1-3份妥曲珠利、3-5份白头翁、1-4份金银花提取物、2-4份牵牛子、3-5份多叶勾儿茶和1-4份维生素C组成。
一种氟苯尼考微囊制剂的制备方法,步骤包括
(1)称量:按质量比分别称量氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,并制备内包衣层材料;
(2)混合:将步骤(1)称量的氟苯尼考、氟苯尼考助溶剂和助剂加热融化并搅拌均匀,冷却至室温后投入无水葡萄糖中,混合搅拌并调节pH值至中性,得到混合制剂;
(3)第一层包被:在步骤(2)制得的混合制剂中加入内包衣层材料进行制粒和滚圆,形成具有第一层包被的颗粒;
(4)第二层包被:在步骤(3)制得的颗粒表面喷涂丙烯酸树脂溶液,制得球形微囊颗粒;
(5)烘干:将步骤(4)制得的球形微囊颗粒烘干,得到氟苯尼考微囊制剂成品。
进一步改进在于,所述内包衣层材料选自碳酸钙或磷酸氢钙。
进一步改进在于,所述加热的温度为75~90℃。
本发明的有益效果在于:用特定占比的氟苯尼考制得的微囊制剂,其配合相关助剂,使得药物服用后,有效增强了灭菌和灭寄生虫的效果;并且药物用量少,药物峰浓度降低,药物的毒副作用大大减少,安全性更高。
附图说明
图1为氟苯尼考微囊制剂的制备流程图;
图2为猪口服两种氟苯尼考制剂后药时曲线比较图。
具体实施方式
下面结合附图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
一种氟苯尼考微囊制剂,其制作原料包括氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,且所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:2.5,所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/5。
其中,所述助剂由2份失水山梨醇脂肪酸酯、1份阿拉伯胶、2份β-环糊精、1份月桂氮卓酮、3份咖啡酸、1份苄星青霉素、2份苯甲酸钠、1份冰片、2份三氯叔丁醇、1份妥曲珠利、3份白头翁、1份金银花提取物、2份牵牛子、3份多叶勾儿茶和1份维生素C组成。
实施例2
一种氟苯尼考微囊制剂,其制作原料包括氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,且所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:3,所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/4。
其中,所述助剂由3份失水山梨醇脂肪酸酯、2份阿拉伯胶、3份β-环糊精、2份月桂氮卓酮、4份咖啡酸、2份苄星青霉素、3份苯甲酸钠、2份冰片、3份三氯叔丁醇、2份妥曲珠利、4份白头翁、2份金银花提取物、3份牵牛子、4份多叶勾儿茶和3份维生素C组成。
实施例3
一种氟苯尼考微囊制剂,其制作原料包括氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,且所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:3.5,所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/3。
其中,所述助剂由4份失水山梨醇脂肪酸酯、3份阿拉伯胶、4份β-环糊精、3份月桂氮卓酮、5份咖啡酸、4份苄星青霉素、4份苯甲酸钠、3份冰片、4份三氯叔丁醇、3份妥曲珠利、5份白头翁、4份金银花提取物、4份牵牛子、5份多叶勾儿茶和4份维生素C组成。
结合图1所示,上述各实施例均采用以下方法制备而成:一种氟苯尼考微囊制剂的制备方法,步骤包括
(1)称量:按质量比分别称量氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,并制备内包衣层材料;
(2)混合:将步骤(1)称量的氟苯尼考、氟苯尼考助溶剂和助剂加热融化并搅拌均匀,冷却至室温后投入无水葡萄糖中,混合搅拌并调节pH值至中性,得到混合制剂;
(3)第一层包被:在步骤(2)制得的混合制剂中加入内包衣层材料进行制粒和滚圆,形成具有第一层包被的颗粒;
(4)第二层包被:在步骤(3)制得的颗粒表面喷涂丙烯酸树脂溶液,制得球形微囊颗粒;
(5)烘干:将步骤(4)制得的球形微囊颗粒烘干,得到氟苯尼考微囊制剂成品。
其中,所述内包衣层材料选自碳酸钙或磷酸氢钙;所述加热的温度为75~90℃。
氟苯尼考是时间依赖性药物,必须维持长时间有效血药浓度才能发挥最佳效果,但氟苯尼考内服吸收迅速,达峰时间快(1.82±0.61h),峰浓度高(22.61±1.03μg·mL-1),有效血药浓度维持时间不足12h,临床上为保证疗效,常加量1~3倍使用。由于氟苯尼考有较强的免疫抑制和胚胎毒性,超量使用极易造成猪场的疫苗接种失败和母猪流产,严重制约了氟苯尼考在猪场的使用。
图2给出了猪口服两种氟苯尼考制剂后药时曲线比较结果,从图中可以看出,猪分别口服传统氟苯尼考药物以及本发明制得的氟苯尼考微囊制剂,药时曲线存在较大差异。本发明通过助剂的使用以及小肠溶蚀工艺让药物在小肠段缓慢释放,血中达峰浓度降低(20μg·mL-1→12μg·mL-1),达峰时间延迟(1.8h→5.6h),体内有效血药浓度维持时间延长(15.2h→23.6h),临床用量大大减少,每吨饲料只需10%微囊氟苯尼考500克就可以有效地防治猪病,药物的毒副作用大大减少,安全性更高。
本发明制得的氟苯尼考微囊制剂适用于多种牲畜的病症预防和治疗。在喂养过程中需要参照不同的牲畜(种类、体型、育龄、病症情况等),使用合理的喂养方案。以不同类型的家养猪为例介绍,其应用方案以及保健目标见表1。
表1:微囊氟苯尼考临床使用方案
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 (8)
1.一种氟苯尼考微囊制剂,其特征在于:其制作原料包括氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,且所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:2.5-3.5,所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/5-1/3。
2.根据权利要求1所述的一种氟苯尼考微囊制剂,其特征在于:所述氟苯尼考、氟苯尼考助溶剂与无水葡萄糖之间的质量比为1:1:3。
3.根据权利要求1所述的一种氟苯尼考微囊制剂,其特征在于:所述助剂的质量占氟苯尼考、氟苯尼考助溶剂与无水葡萄糖总量的1/4。
4.根据权利要求1-3任一项所述的一种氟苯尼考微囊制剂,其特征在于:所述助剂由失水山梨醇脂肪酸酯、阿拉伯胶、β-环糊精、月桂氮卓酮、咖啡酸、苄星青霉素、苯甲酸钠、冰片、三氯叔丁醇、妥曲珠利、白头翁、金银花提取物、牵牛子、多叶勾儿茶和维生素C组成。
5.根据权利要求4所述的一种氟苯尼考微囊制剂,其特征在于:所述助剂按质量份数由2-4份失水山梨醇脂肪酸酯、1-3份阿拉伯胶、2-4份β-环糊精、1-3份月桂氮卓酮、3-5份咖啡酸、1-4份苄星青霉素、2-4份苯甲酸钠、1-3份冰片、2-4份三氯叔丁醇、1-3份妥曲珠利、3-5份白头翁、1-4份金银花提取物、2-4份牵牛子、3-5份多叶勾儿茶和1-4份维生素C组成。
6.一种氟苯尼考微囊制剂的制备方法,其特征在于:步骤包括
(1)称量:按质量比分别称量氟苯尼考、氟苯尼考助溶剂、无水葡萄糖和助剂,并制备内包衣层材料;
(2)混合:将步骤(1)称量的氟苯尼考、氟苯尼考助溶剂和助剂加热融化并搅拌均匀,冷却至室温后投入无水葡萄糖中,混合搅拌并调节pH值至中性,得到混合制剂;
(3)第一层包被:在步骤(2)制得的混合制剂中加入内包衣层材料进行制粒和滚圆,形成具有第一层包被的颗粒;
(4)第二层包被:在步骤(3)制得的颗粒表面喷涂丙烯酸树脂溶液,制得球形微囊颗粒;
(5)烘干:将步骤(4)制得的球形微囊颗粒烘干,得到氟苯尼考微囊制剂成品。
7.根据权利要求6所述的一种氟苯尼考微囊制剂的制备方法,其特征在于:所述内包衣层材料选自碳酸钙或磷酸氢钙。
8.根据权利要求6所述的一种氟苯尼考微囊制剂的制备方法,其特征在于:所述加热的温度为75~90℃。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201810710233.9A CN108524466A (zh) | 2018-07-02 | 2018-07-02 | 一种氟苯尼考微囊制剂及其制备方法 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201810710233.9A CN108524466A (zh) | 2018-07-02 | 2018-07-02 | 一种氟苯尼考微囊制剂及其制备方法 |
Publications (1)
Publication Number | Publication Date |
---|---|
CN108524466A true CN108524466A (zh) | 2018-09-14 |
Family
ID=63487679
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201810710233.9A Pending CN108524466A (zh) | 2018-07-02 | 2018-07-02 | 一种氟苯尼考微囊制剂及其制备方法 |
Country Status (1)
Country | Link |
---|---|
CN (1) | CN108524466A (zh) |
Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102429918A (zh) * | 2011-11-02 | 2012-05-02 | 南京威泰珐玛兽药研究所有限公司 | 一种含有氟苯尼考和茶皂素的药物组合物及其制备方法 |
CN102688220A (zh) * | 2012-06-07 | 2012-09-26 | 湖州爱宝莱动物药业有限公司 | 一种替米考星微囊制剂及其制备方法 |
CN103054833A (zh) * | 2012-12-28 | 2013-04-24 | 湖南农业大学 | 一种兽用抗菌药物油乳剂微囊包被剂及制备方法 |
CN105287433A (zh) * | 2015-11-26 | 2016-02-03 | 广东温氏大华农生物科技有限公司 | 一种微囊化动物药品及其制备方法 |
CN106822033A (zh) * | 2015-12-07 | 2017-06-13 | 王玉万 | 以玉米芯粉为囊心材料制备含药物的囊心物及其微囊 |
CN107823186A (zh) * | 2017-11-20 | 2018-03-23 | 四川兴华药业有限责任公司 | 一种恩诺沙星肠溶粉配方及制备方法 |
-
2018
- 2018-07-02 CN CN201810710233.9A patent/CN108524466A/zh active Pending
Patent Citations (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102429918A (zh) * | 2011-11-02 | 2012-05-02 | 南京威泰珐玛兽药研究所有限公司 | 一种含有氟苯尼考和茶皂素的药物组合物及其制备方法 |
CN102688220A (zh) * | 2012-06-07 | 2012-09-26 | 湖州爱宝莱动物药业有限公司 | 一种替米考星微囊制剂及其制备方法 |
CN103054833A (zh) * | 2012-12-28 | 2013-04-24 | 湖南农业大学 | 一种兽用抗菌药物油乳剂微囊包被剂及制备方法 |
CN105287433A (zh) * | 2015-11-26 | 2016-02-03 | 广东温氏大华农生物科技有限公司 | 一种微囊化动物药品及其制备方法 |
CN106822033A (zh) * | 2015-12-07 | 2017-06-13 | 王玉万 | 以玉米芯粉为囊心材料制备含药物的囊心物及其微囊 |
CN107823186A (zh) * | 2017-11-20 | 2018-03-23 | 四川兴华药业有限责任公司 | 一种恩诺沙星肠溶粉配方及制备方法 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CN102578387B (zh) | 一种用于畜禽饲料的缓释复合酸化剂及其制备方法与饲料 | |
CN102716168B (zh) | 一种含有利福昔明的用于预防和治疗奶牛干奶期乳房炎制剂及其制备方法 | |
CN107184427A (zh) | 一种含聚谷氨酸和透明质酸的协同组合物及应用 | |
CN106860451A (zh) | 一种利福霉素‑硝基咪唑偶联分子的新应用 | |
CN106508810A (zh) | 安格斯肉牛育肥牛饲养管理方法 | |
CN110507672A (zh) | 一种高效微生态调整剂及其应用 | |
CN106578529A (zh) | 一种改善仔猪生产性能、肠道健康和抗氧化性能的组合物及其制备方法 | |
Lin et al. | Effects of coated sodium butyrate on performance, diarrhea, intestinal microflora and barrier function of pigs during the first 2-week post-weaning | |
US20030215506A1 (en) | Methods and compositions for enhancement of creatine transport | |
CN108719599A (zh) | 一种饲料添加用组合物、饲料添加颗粒及饲料添加微丸 | |
CN113273646B (zh) | 一种母猪分娩接生用粉剂及其制备方法和应用 | |
ES2769893T3 (es) | Formulaciones de compuestos orgánicos volátiles que tienen actividad antimicrobiana | |
CN110089639A (zh) | 一种提高保育猪生长性能的饲料添加剂及其制备和应用 | |
CN108524466A (zh) | 一种氟苯尼考微囊制剂及其制备方法 | |
CN101897758A (zh) | 一种治疗动物子宫炎症及其他产后疾病的中药组合物 | |
CN102283842A (zh) | 一种复方乙酰甲喹氟苯尼考纳米乳抗菌药物及其制备方法 | |
CN107184807A (zh) | 一种祛痘消肿面膜粉 | |
CN108272756A (zh) | 一种阿莫西林可溶性粉及其制备方法 | |
CN107550867B (zh) | 一种抗静电酒石酸泰万菌素预混剂及其制备方法 | |
CN105030665A (zh) | 一种兽用长效盐酸林可霉素注射液及其制备方法 | |
CN109276602A (zh) | 余甘子的用途及其组合物和组合物用途 | |
CN108524467A (zh) | 一种复方磺胺间甲氧嘧啶钠微囊制剂及其制备方法 | |
CN104906132B (zh) | 一种防治羔羊口炎的膏药制剂 | |
CN103251552B (zh) | 一种恩诺沙星糊剂及其制备方法 | |
CN103784948B (zh) | 一种用于治疗哺乳动物阴道炎的泡腾栓剂 |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
PB01 | Publication | ||
PB01 | Publication | ||
SE01 | Entry into force of request for substantive examination | ||
SE01 | Entry into force of request for substantive examination | ||
RJ01 | Rejection of invention patent application after publication | ||
RJ01 | Rejection of invention patent application after publication |
Application publication date: 20180914 |