沈阳药科大学《药剂学I》教案《Pharmaceutics I》 teaching plan For students major in Pharmacy (in English)Shirui Mao毛世瑞Shenyang Pharmaceutical UniversityChapter 1 Introduction课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce definition, contents, tasks of pharmaceutics, importance of dosage forms and some other related information.[Basic requirements]Master：The definition, contents, tasks of pharmaceutics; importance of dosage forms; pharmacopoeia; drug standards of China;Familiarize：Pharmaceutics related subjects; classification of dosage forms; application of excipients in pharmaceutics; the development of Chinese Pharmacopoeia; prescription drug and OTC; GMP, GLP and GCP.Understand: pharmaceutics historical perspective.二、Emphases and difficulties (教学重点和难点)Emphases：Definitions and tasks of pharmaceutics, importance of dosage form.Difficulties：Classification of dosage forms based on different criteria.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class.四、Teaching contents(教学内容)Definitions of pharmaceutics; contents of pharmaceutics; tasks of pharmaceutics; pharmaceutics related subjects; importance of dosage from; variation in time of onset of action for different dosage forms; classification of dosage forms; application of excipients in pharmaceutics; examples of pharmaceutical excipients; definition of pharmacopoeia, the development of Chinese pharmacopoeia, other important pharmacopoeia( USP, BP, JP, EP, Ph. Int); Drug standards in China; prescription drug and OTC; GMP, GLP, GCP; pharmaceutics historical perceptive.五、Questions/Homework after class (课后思考题或作业)1. Definitions: pharmaceutics; dosage form; pharmacopoeia; OTC; GMP; GLP; GCP.2. What are the tasks of pharmaceutics?3. Can you describe the importance of dosage forms?4. Based on administration route, how can dosage forms be classified?5. Please describe the important stages during the development of Chinese Pharmacopoeia.Chapter 2 Liquid preparationsPart I Introduction, solvents and excipients 课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce definition, classification, advantages and disadvantages of liquid preparations and commonly used solvents and excipients in liquid formulations.[Basic requirements]Master：the classification of liquid preparations; advantages and disadvantages of liquid formulations; solvents for liquid formulations; excipients in liquid formulations especially the concept of solubilizer, hydrotropy agent, cosolvents and preservatives; properties of surfactants.Familiarize：quality of liquid dosage forms; the mechanism of solubilization; classification of hydrotropy agents; flavors including sweeting agents, flavoring agents and mucilage; colorants.Understand: mechanism of cosolvency and hydrotroy.二、Emphases and difficulties (教学重点和难点)Emphases：the solvents and excipients in pharmaceuticsDifficulties：the mechanism of solubilization, cosolvency and hydrotropy.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class.四、Teaching contents(教学内容)1. Introduction: definition of liquid preparations; classification of liquid preparations; advantages and disadvantages of liquid dosage forms; quality of liquid dosage form.2. Solvents for liquid preparationsz Aqueous solvent: waterz Non-aqueous solvents: alcohol, glycerin, propylene glycol, polyethylene glycol, dimethylsulfoxide, fatty oils…3. Excipients in liquid formulations:z Solubilizer: introduce surfactant related knowledge.z Hydrotropy agents: definition, examples, mechanism and classification of hydrotropy agents. z Cosolvency: definition and mechanismz Preservatives; criteria of selection; commonly used substances and their properties: paraben, benzoic acid and sodium benzoate; sorbic acid and others…z Flavors: sweeting agents, flavoring agents, mucilagez Other excipients.五、Questions/Homework after class (课后思考题或作业)1. Definitions: liquid preparations; solubilization; hydrotropy; cosolvency; surfactant2. What are the advantages and disadvantages of liquid preparations?3. Why can surfactants be used to increase the solubility of poorly water soluble drugs?4. When sodium benzoate is used as a preservative in a formulation, the concentration shouldbe higher than that of benzoic acid, why?Part II Solutions and suspensions 课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce the preparation and characterization of low molecular weight solutions, polymer solutions and suspensions.[Basic requirements]Master：Preparation methods of low molecular weight solutions; syrup and its preparation; tincture; physical stability of suspension and stabilizers in suspension; definition of sedimentation volume and degree of flocculation.Familiarize：definition of aromatic waters and spirits; reasons for suspension preparation; methods of suspension preparation, quality control of suspension.Understand: properties of polymer solution; two processes in the preparation of polymer solutions; the double layer theory; the mechanism of flocculation in suspension.二、Emphases and difficulties (教学重点和难点)Emphases：Physical stability of suspension and stabilization strategies.Difficulties：To understand the mechanism of flocculation and deflocculation.三、Teaching methods and means (教学方法与教学手段)1. Teaching methods：Lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class. 3) Experimentation will be provided with demonstration.四、Teaching contents(教学内容)1. Low molecular solutions: definition, preparation of solutions; syrups definition, components and preparation methods; aromatic waters; tinctures; spirits.2. Polymer solutions: definition, properties of polymer solutions, preparation of polymer solutions, some commonly used natural and synthesized polymers.3. Suspensions: definitions, reasons for suspension preparation; features desired in a pharmaceutical suspension; physical stability of suspension ( flocculation and deflocculation; sedimentation, particle size increase and crystal growth); stabilizers in suspensions (suspending agents, wetting agents, flocculating and deflocculating agents…); preparation of suspensions (dispersing method, coagulation methods); apparatus for suspension preparation; quality evaluation of suspension( sedimentation volume, degree of flocculation…).五、Questions/Homework after class (课后思考题或作业)1. Definitions: syrups, single syrups, spirit, aromatic water, tincture, suspension; sedimentationvolume; degree of flocculation.2. What are the properties of polymer solutions?3. Can you describe the physical stability of suspensions?4. Which kinds of stabilizers should be used in order to increase the physical stability ofsuspension?Part III Emulsions 课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce preparation, stability and quality evaluation of emulsions.[Basic requirements]Master：definition of emulsion, its composition, emulsion types; formulation of emulsions ( choice of emulsion type, oil phase and emulsifying agents…); HLB calculation; methods of emulsion preparation; stability of emulsion;Familiarize：emulsion types identification; classification of emulsions; commonly used emulsifying machines; factors influencing emulsification; multiple emulsions; quality evaluation of emulsions.Understand: theory of emulsification.二、Emphases and difficulties (教学重点和难点)Emphases：Preparation and stability of emulsions.Difficulties：Theory of emulsification.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussions.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class. 3) Experimentation will be provided with demonstration.四、Teaching contents(教学内容)1. Introduction: definition of emulsion; composition of emulsion; emulsion types and identification; classification of emulsions; properties of emulsions; basic requirements for emulsifying agents.2. Preparation of emulsions:z Formulation of emulsions: choice of emulsion type, oil phase and emulsifying agents;formulation by the HLB method; HLB calculation.z Drug substance additionz Methods of emulsion preparation: manual methods ( dry gum method, wet gum method and direct mixing method); mechanical method; commonly used emulsifying machines3. Stability of emulsion: creaming, flocculation, phase inversion, and coalescence (breaking,cracking).4. Multiple emulsions: definition, preparation and stability5. Quality evaluation五、Questions/Homework after class (课后思考题或作业)1. Definitions: emulsions, dry gum method, wet gum method; phase inversion; creaming;emulsion flocculation; emulsion coalescence.2. Please describe emulsion preparation process by using dry gum method.3. Can you describe the potential physical stability problem of emulsion?4. In the design of emulsion formulations, which parameters should you consider?Chapter 3 Parenteral and ophthalmic preparationsPart I Solvents and excipients for injections 课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce solvents and vehicles for injections.[Basic requirements]Master：advantages and disadvantages of injections; quality requirement of injections; definition of pyrogen, properties of pyrogen, sources of pyrogen, methods to remove pyrogens; definition of water for injection, sterile water for injection; parenteral added substances such as antibacterial agents, antioxidants, buffers, tonicity contributors.Familiarize：Routes of injection administration.Understand: Properties of different administration routes二、Emphases and difficulties (教学重点和难点)Emphases：definition and properties of pyrogen, sources of pyrogen and methods to remove pyrogen.Difficulties：parenteral formulation additives selection.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class.四、Teaching contents (教学内容)1. Introduction: definition of injections; types of injections; advantages and disadvantages ofparenteral administration; parenteral routes of administration; quality requirement of injections.2. Pyrogens: definition of pyrogen; properties of pyrogen (thermostable, filterable, water soluble, non-volatile); sources of pyrogen; methods to remove pyrogens (heating at high temperature, acid-base method, adsorption method, ion-exchange, gel filtration, reverse osmosis).3. Solvents and vehicle for injections:z Aqueous vehicles: water for injection, sterile water for injection…z Nonaqueous vehicles: fixed vegetable oil, alcohol, glycerin, propylene glycol, PEG…4. Parenteral additives: antibacterial agents, antioxidants, buffers, tonicity contributors…五、Questions/Homework after class (课后思考题或作业)1. Definitions: injections, water for injection, sterile water for injection, pyrogen2. What are the advantages and disadvantages of parenteral preparations?3. What are properties of pyrogen? What are the sources?4. How to remove pyrogen during the preparation of injections?Part II Injections and infusions 课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce the preparation and characterization of injections and infusions.[Basic requirements]Master：the preparation process of injections (ampules washing methods, ingredients for preparations, filling volume criteria and sterilization methods); the type of glass and their properties; quality control ( sterility testing, clarity testing and pyrogen testing); infusion and quality control; infusion related problems; fat emulsions for intravenous injection; injectable sterile powder; advantages and disadvantage of freeze drying;Familiarize：environmental control for injections preparation; osmolarity definition and calculation; total parenteral nutrition; problems related to freeze drying; sterile divided products.Understand: plasma substitutes; the phase diagram for water二、Emphases and difficulties (教学重点和难点)Emphases：the preparation and characterization of injections and infusions.Difficulties：To solve the injection, infusion related problems.三、Teaching methods and means (教学方法与教学手段)1. Teaching methods：Lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class. 3) Experimentation will be provided with demonstration.四、Teaching contents(教学内容)1. Preparation of injections: environmental control; choice of containers; type of glass; preparation process (ampule washing, drying and sterilization methods; ingredients for preparations; solution preparation and filtration; recommended filling volume; sterilization).2. Quality control: sterility testing; clarity testing, pyrogen testing.3. Infusion: definition, preparation of infusion, quality control; osmolarity and its calculation; infusion related problems.4. Others: total parenteral nutrition, fat emulsions for intravenous injection, plasma substitute, injectable sterile powder, sterile divided products…五、Questions/Homework after class (课后思考题或作业)1. Definitions: infusion, osmolarity, total parenteral nutrition,2. Please describe the classification of glass for parenterals.3. What are the sterilization requirements for injections?4. Which methods can be used for pyrogen testing?5. Please describe infusion related problems.6. Please describe the composition and quality requirement of fat emulsions for intravenousinjection.7. What are the advantages and disadvantages of freeze drying?Part III R&D of injection and ophthalmic drug delivery课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce the design of injection formulations and ophthalmic drugdelivery system.[Basic requirements]Master：in which cases antibacterial can be added in injections; definition of iso-osmotic solution and isotonic solution; osmotic pressure adjustment methods: freezing point depression method and sodium chloride equivalent method); pharmaceutical requirement of ophthalmic drug delivery system;Familiarize：small volume and large volume parenterals; types of ophthalmic preparations; factors influencing ocular drug absorption.Understand: the physiological structure of eyes.二、Emphases and difficulties (教学重点和难点)Emphases：the methods and calculation for osmolarity adjustmentDifficulties：formulation design of injections.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussions.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class. 3) Experimentation will be provided with demonstration.四、Teaching contents(教学内容)1. Research and development of injections: formulation design; when antibacterials can be added;safety of injections; definition of iso-osmotic solutions, isotonic solutions and their relationship; osmotic pressure adjustment by using freezing point depression method or sodium chloride equivalent method and the calculation method; formulation analysis.2. Ophthalmic drug delivery: definition and classification; types of ophthalmic preparations;pharmaceutical requirements (pH, osmolarity, sterility…);五、Questions/Homework after class (课后思考题或作业)1. Definitions: iso-osmotic solution, isotonic solution; freezing point depression method;sodium chloride equivalent.2. When antibacterials can be added in injections?3. What is the relationship between iso-osmotic solution and isotonic solution?4. What are the quality requirement of ophthalmic formulations?Chapter 4 Solid dosage formsPart I Powders 课时安排：3学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce the preparations of powders and how to evaluate its properties.[Basic requirements]Master：the definition and classification of powders, properties of powders, preparation of powders; characteristics of fluid energy mill; sieve specifications in CP; the definition of geometric dilution, critical relative humidity (CRH), elder hypothesis; quality control of powder Familiarize：methods of comminution; comminution instruments such as ball mill, impact mill and fluid energy mill; blending methods; factors influencing the mixing process; dosing methods二、Emphases and difficulties (教学重点和难点)Emphases：The mechanism and characteristics of fluid energy mill; the concept of CRH and elder hypothesis.Difficulties：Analyze factors influencing the mixing process.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class.四、Teaching contents(教学内容)Introduction: definition of powders and classification; properties of powders; preparation of powders; methods of communication; communication instruments including ball mill, impact mill, fluid energy mill and their properties; sieve specifications in CP; sifting process; blending methods including spatulation, trituration, sifting and tumbling; factors influencing the mixing process; the definition of geometric dilution, critical relative humidity (CRH), elder hypothesis; dosing methods; quality of powders五、Questions/Homework after class (课后思考题或作业)1. Definitions: geometric dilution, critical relative humidity (CRH), elder hypothesis2. Please describe the mechanism and characteristics of fluid energy mill.3. Can you describe the factors influencing the mixing process?4. Please describe the preparation process of powders.Part II Tablets preparation 课时安排：4学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce the commonly used tablets excipients and tablets preparation methods.[Basic requirements]Master：commonly used tablets excipients especially fillers, binders, disintegrants and lubricants, their abbreviations and properties; prerequisite for tablet preparation; tablet preparation methods including wet granulation, dry granulation and direct compressionFamiliarize：Advantages and disadvantages of tablets; tape of tablets; granulation purpose; factors influencing the compressibility of tablets; processing problemsUnderstand: the mechanism of disintegration; tablet compression machinery二、Emphases and difficulties (教学重点和难点)Emphases：Commonly used tablets excipients, especially for direct compression; methods of tablet preparationDifficulties：Analyze processing problems during tablet preparation三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class. 3) Experimentation will be provided with demonstration四、Teaching contents(教学内容)1. Introduction: the definition of tablets, tablet forms, advantages and disadvantages of tablets; types of tablets; quality of tablets.2. Tablet excipients: including commonly used fillers (diluents), binders (adhesives), disintegrants,lubricants, introduce the properties of each excipients, their full name and abbreviations; a brief introduction about absorbents, wetting agents, and some other excipients; mention the new development in the area of excipients, the co-processed excipients.3. Tablets preparation: prerequisite for tablet preparation; granulation purpose; wet granulation process will be explained in detail; dry granulation method; direct compression method and commonly used diluents; advantages and disadvantages of direct compression; tablet machinery4. Processing problems: capping and lamination, loose, adhere to the punch, high weigh variance, slow disintegration, poor dissolution, and so on.五、Questions/Homework after class (课后思考题或作业)1. Definitions: diluents, disintegrants, lubricants, direct compression2. Please describe the commonly used tablets excipients, list at least two examples in eachtype.3. Can you describe the purpose of granulation?4. Please describe the preparation process of tablets by wet granulation5. What is the prerequisite for tablet preparation?6. For tablets preparation, what are the advantages of direct compression compared to wetgranulation methods?Part III Tablets coating 课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce tablets coating methods and tablet quality control parameters.[Basic requirements]Master：Types of tablet coating; sugar coating processes; properties of film coating; tablet quality parameters; preparation of granulesFamiliarize：Purpose of tablet coating; types of different coating equipments.Understand: Properties of different coating equipments.二、Emphases and difficulties (教学重点和难点)Emphases：Tablets coating methods; tablet quality controlDifficulties：Film evaluation三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussions.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class. 3) Experimentation will be provided with demonstration.四、Teaching contents(教学内容)1. Introduction: reasons for tablet coating, types of tablet coating2. Sugar coating: steps in sugarcoating, including waterproofing and sealing if needed, subcoating, smoothing and final rounding, finishing and coloring if desired and polishing; disadvantages of sugar coating3. Film coating: advantages of film coating; basic components of the coating formulation; aqueous film coating formulation; coating equipments.4. Tablet quality control: tablet weight variation, tablet hardness, tablet friability, tablet disintegration, tablet dissolution…5. Granules: definition, classification, preparation of granules and quality control五、Questions/Homework after class (课后思考题或作业)1. What are the reasons for tablet coating?2. Please describe sugar coating process and the purpose for each step.3. What are the advantages of tablet film coating compared to sugar coating?4. How to control the quality of tablets?5. In which case tablet dissolution should be tested?Part IV Capsules and pills 课时安排：3学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce hard gelatin capsules and soft gelatin capsules, their preparation methods and quality control.[Basic requirements]Master：type of capsules; properties of capsules; limitation of gelatin capsules; manufactureof hard gelatin capsules; hard capsule sizes; composition of soft capsule shell composition, limitation of liquid contents; preparation of soft gelatin capsules; quality control of capsules.Familiarize：Capsule filling machine; drop pills and quality control.Understand: mechanically interlocking caps and bodies.二、Emphases and difficulties (教学重点和难点)Emphases：Hard gelatin and soft gelatin capsules properties, composition and preparation Difficulties：Comparison of hard and soft gelatin capsules and their limitations in liquid content.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussions.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class.四、Teaching contents(教学内容)1. Introduction: definition of capsules; types of capsules; properties of capsules; limitation of gelatin capsules.2. Hard gelatin capsules: composition of hard gelatin shells; advantages and disadvantages of hard gelatin capsules; manufacture of hard gelatin capsule shells; hard capsule sizes; preparation process of filled hard gelatin capsules; capsule filling machines.3. Soft gelatin capsules: soft capsule shell components; limitation of liquid contents; advantages and disadvantages of soft gelatin capsules; preparation methods of soft gelatin capsules (dripping method and rotary die process); comparison of soft gelatin and hard gelatin capsules.4. Quality control of capsules, package and storing capsules; drop pills and quality control.五、Questions/Homework after class (课后思考题或作业)1. Can you describe the classification of capsules?2. What are the properties of capsules?3. What are the limitations of gelatin capsules?4. How many hard capsule sizes are available?5. Please describe the advantages and disadvantages of soft gelatin capsules.Chapter 5 Semisolid formulationsPart I Ointments 课时安排：4学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce the commonly used ointment bases and methods of ointment preparation.[Basic requirements]Master：Properties of ointment bases, including oleaginous bases, emulsion bases, water-soluble bases and gels, and the commonly used bases; additives in ointments; preparation method selection based on the properties of the ointment bases; gels; ophthalmic ointment; ointment formulation analysis.Familiarize：Absorption of ointments; selection of appropriate bases; paste二、Emphases and difficulties (教学重点和难点)Emphases：ointment bases and ointment preparation methods.Difficulties：Ointment formulation analysis三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class; 3) Experimentation will be provided with demonstration四、Teaching contents(教学内容)1. Introduction: definition of ointments, absorption of ointments.2. Ointment bases and their properties:z Oleaginous bases: hydrocarbon bases, fat and fixed oil bases, silicones, absorption bases z Emulsion bases: hydrophilic ointment and cold creamz Gel bases: cellulose derivatives, carbopol 934…3. Preparation of ointments:z Oleaginous based ointments: trituration, levigation, fusion…z emulsion based ointments: melting and emulsification4. Others: pastes, ophthalmic ointment, formulation analysis, quality control…五、Questions/Homework after class (课后思考题或作业)1. Definitions: ointment, cream, gel, paste2. Please describe the classification of ointment bases.3. What is the composition of ophthalmic ointment?4. How to select the preparation method based on the properties of ointment bases?Part II Suppository 课时安排：2学时（药学（英语））一、Aim (教学目的)In this lecture we will introduce the commonly used suppository bases and suppository preparation methods.[Basic requirements]Master：Classification of suppository; commonly used suppository bases; preparation of suppository; displacement value and its calculation;Familiarize：Pharmaceutical additives in suppositories; the advantages and disadvantages of suppository for systemic action; factors influencing absorption from rectal suppositories.Understand: the physiological structure in the rectal.二、Emphases and difficulties (教学重点和难点)Emphases：Commonly used suppository bases; suppository preparation methods; displacement value.Difficulties：Using displacement value as the parameter for bases amount calculation in the formulation design of suppository.三、Teaching methods and means (教学方法与教学手段)1.Teaching methods：Lectures with questions and discussion.2. Teaching means：1）the slides are in English and the lectures are given in English；2）questions will be asked at random during the class. 3) Experimentation will be provided with demonstration四、Teaching contents(教学内容)1. Introduction: the definition of suppository; classification of suppository; composition of suppositories.。
星点设计-响应面法优化米拉贝隆缓释片处方徐斌;浦雨伟;周卫;丁逸梅;卢定强【期刊名称】《中国药房》【年(卷),期】2017(28)1【摘要】OBJECTIVE:To optimize the formulation of Mirabegron sustained-release tablets. METHODS:Using polyethylene oxide(PEO)and hydroxypropylmethyl cellulose(HPMC K4M)as the sustained release matrix,Mirabegron sustained-release tab-lets were prepared by powder direct compression technology. Using 1,3,5,7 h accumulative release rate as indexes,the amounts of PEO,HPMC K4M and OPADRY? were optimized by composite design-response surface method,and then validated. Accumula-tive release rates of sustained-release tablet and original tablet (MyrbetriqTM) were compared in different pH mediums (water,pH 1.0 simulated gastric fluid,pH 4.5 acetate buffer solution,pH 6.8 phosphate buffer solution) at different rotation rates (100,50 r/min),and similiar factor f2 was calculated to fit drug release model of sustained-release tablet. RESULTS:In the optimized firmu-lation each Mirabegron sustained-release tablet contained mirabegron 25 mg,PEO 108.02 mg,HPMC K4M 21.69 mg,OPADRY? 2.27%. Relative error of accumulative release rates at 1,3,5,7 h to predicted value were 4.78%,3.48%,0.69% and -1.41%, respectively. f2 of release curves of sustained-release tablet and original tablet were higher than 65 in different pH medium at differ-ent rotation rates. Thedrug release of sustained-release tablet was fitted to zero-order release equation. CONCLUSIONS:Mirabe-gron sustained-release tablet by optimized technology is similar to original tablet in drug release behavior.%目的:优化米拉贝隆缓释片处方.方法:采用聚氧乙烯(PEO)和羟丙甲基纤维素(HPMC K4M)为缓释骨架材料,以粉末直压法制备米拉贝隆缓释片.以1、3、5、7 h的累积释放度为指标,采用星点设计-响应面法优化处方中PEO、HPMC K4M和包衣液(OPADRY?)的用量,并进行验证.比较所制缓释片与原研片(MyrbetriqTM)在不同pH介质(水、pH 1.0的人工胃液、pH 4.5醋酸盐缓冲液、pH 6.8磷酸盐缓冲液)中不同转速(100、50 r/min)下的累积释放度,计算相似因子f2,拟合缓释片的释药模型.结果:优化处方中每片米拉贝隆缓释片含米拉贝隆25 mg、PEO 108.02 mg、HPMC K4M 21.69 mg、OPADRY?2.27%;其1、3、5、7 h的累积释放度与预测值的相对误差分别为4.78%、3.48%、0.69%、-1.41%.所制缓释片与原研片在不同pH介质中和不同转速下释放曲线的f2均大于65;缓释片释药符合零级释药特征.结论:优化处方制备的米拉贝隆缓释片与原研片的释放行为相似.【总页数】5页(P110-114)【作者】徐斌;浦雨伟;周卫;丁逸梅;卢定强【作者单位】南京工业大学药学院,南京 210009;江苏省药物研究所有限公司,南京210009;南京工业大学药学院,南京 210009;中国药科大学药学院,南京 210009;南京工业大学药学院,南京 210009;江苏省药物研究所有限公司,南京 210009;南京工业大学药学院,南京 210009;江苏省药物研究所有限公司,南京 210009【正文语种】中文【中图分类】R943【相关文献】1.星点设计-响应面法优化盐酸安非他酮缓释片 [J], 岳莉;王江涛;吴海妹;龙连清2.星点设计-响应面法优化盐酸罗沙替丁醋酸酯缓释片的处方 [J], 段颐珊;杜娟;孙璐;李雪怡;林宁3.星点设计-响应面法优化布地奈德缓释片处方 [J], 任远志;张涛;黄华;刘秀洁;周劲松4.九味镇心颗粒联合米拉贝隆缓释片治疗普通抗感染无效的女性更年期尿路刺激症状患者的疗效观察 [J], 邱实; 何龙; 陈鹏; 李健; 郭时英; 杨宏伟5.米拉贝隆联合托特罗定缓释片治疗膀胱过度活动症患者的初步临床研究 [J], 朱蜀侠;王明松因版权原因，仅展示原文概要，查看原文内容请购买。
