上海交通大学：《药剂学》教学资源（课件讲义）Tablets 3

国生 国生一 Quality control of tablets ·Appearance 圈Appearance ·Crushing strength ·Size ·Disintegration ·Friability .Shape ·Dissolution ·Color ·Weight variation Marking Drug content uniformity 国生一 国话生一 图Crushing strength 加压 ④Disintegration ·Fracture force 画日日：日 Monsanto hardness tester ·Tensile strength抗张强度 弹簧 标尺 T=2F/π·DL 一片剂 Tablet disintegration testing apparatus 国生一 国秋生 圈Friability ©Dissolution ·Roche fibrilator refers to the rate and extent of drug dissolving from solid dosage forms in certain solution. Dissolution methods are developed to evaluate the potential in vivo performance of a solid oral dosage form as quality control tests demonstrating the appropriate performance of drug products. 1

1 Shanghai Jiao Tong University Quality control of tablets • Appearance • Crushing strength • Disintegration • Friability • Dissolution • Weight variation • Drug content uniformity Shanghai Jiao Tong University Appearance • Size • Shape • Color • Marking Shanghai Jiao Tong University Crushing strength • Fracture force • Monsanto hardness tester • Tensile strength抗张强度 Shanghai Jiao Tong University Tablet disintegration testing apparatus Disintegration Shanghai Jiao Tong University Friability • Roche fibrilator Shanghai Jiao Tong University Dissolution • refers to the rate and extent of drug dissolving from solid dosage forms in certain solution. Dissolution methods are developed • to evaluate the potential in vivo performance of a solid oral dosage form • as quality control tests demonstrating the appropriate performance of drug products

圈生一 Dissolution Apparatuses 国生 Dissolution test Chinese pharmacopoeia specifies that three Medium selection apparatuses could be used for determining Sink conditions:the capacity for the selected dissolution rate medium to solubilize the dose is at least three ·1-basket 一学 times the amount necessary. ·2-paddle An aqueous medium,typical pH range for ·3-small cup dissolution testing from pH I to pH 7.5,is recommended. .For poorly soluble drugs,the addition of surfactant may be required to increase the solubility. 国丛生 国生 ④Weight variation Drug content uniformity The weight of tablet is routinely measured to help ensure that a tablet contains a proper amount of drug. For low-dose drugs,even though tablets weight variation looks acceptable,it Average weight (g) Variation(%) could mask a wide variation in content. <0.30 ±7.5 So it is necessary for the tablets ≥0.30 ±5.0 containing such a drug to determine content uniformity 国生一 国秋生 ©Tablets coating Requirements of tablet core Protect the medicinal agent ·Mask the taste ·Smooth surface Separate reactive substances ·Physical shape Provide esthetics or distinction ·Mechanical strength Provide special release characteristics 2

2 Shanghai Jiao Tong University Dissolution Apparatuses Chinese pharmacopoeia specifies that three apparatuses could be used for determining dissolution rates. • 1 - basket • 2 - paddle • 3 - small cup Shanghai Jiao Tong University Dissolution test Medium selection • Sink conditions : the capacity for the selected medium to solubilize the dose is at least three times the amount necessary. • An aqueous medium, typical pH range for dissolution testing from pH 1 to pH 7.5, is recommended. • For poorly soluble drugs, the addition of surfactant may be required to increase the solubility. Shanghai Jiao Tong University Weight variation • The weight of tablet is routinely measured to help ensure that a tablet contains a proper amount of drug. Average weight(g) Variation(%) < 0.30 ±7.5 ≥ 0.30 ±5.0 Shanghai Jiao Tong University Drug content uniformity • For low-dose drugs, even though tablets weight variation looks acceptable, it could mask a wide variation in content. So it is necessary for the tablets containing such a drug to determine content uniformity. Shanghai Jiao Tong University Tablets coating • Protect the medicinal agent • Mask the taste • Separate reactive substances • Provide esthetics or distinction • Provide special release characteristics Shanghai Jiao Tong University Requirements of tablet core • Smooth surface • Physical shape • Mechanical strength

国生一 国生 Sugar-coated tablets Coating methods Sealing coat:prevent coating solution penetration into the core ·Sugar coating Subcoat:round off the sharp comers of the tablet to produce a smooth surface Film coating Smoothing c provides the tablet withasmooth finish. ·Compression coating Coloring:lakes often being preferred because a uniform colour is easier to achieve with them Polishng:transferred topolishing pan and coed with to provide a glossy finish to the surface 国生一 国生一 Film-coating places a thin skin-tight coating of a Ingredients of Film-forming solutions plastic-like material over the compressed tablet. Film-forming polymer easier to automate ·Plasticizer ·more rapid ·Pore material ·Less weight gains ·Better dissolution ·Antiadherent moisture involvement can be avoided Colorant and opacifier Suitable for tablets with marking on surface ·Solvents 国生一 国秋生 ©Aqueous film coating Compression- Aqueous polymeric dispersions are water- coated tablets insoluble polymers dispersed in aqueous systems 云 ·Nontoxic ·Low viscosity e ·High polymer content ·Productive 3

3 Shanghai Jiao Tong University Coating methods • Sugar coating • Film coating •Compression coating Shanghai Jiao Tong University Sugar-coated tablets • Sealing coat: prevent coating solution penetration into the core • Subcoat: round off the sharp corners of the tablet to produce a smooth surface • Smoothing coat: provides the tablet with a smooth finish. • Coloring: lakes often being preferred because a uniform colour is easier to achieve with them • Polishing: transferred to a polishing pan and coated with to provide a glossy finish to the surface Shanghai Jiao Tong University Film-coating places a thin skin-tight coating of a plastic-like material over the compressed tablet. • easier to automate • more rapid • Less weight gains • Better dissolution • moisture involvement can be avoided • Suitable for tablets with marking on surface Shanghai Jiao Tong University Ingredients of Film-forming solutions • Film-forming polymer • Plasticizer • Pore material • Antiadherent • Colorant and opacifier • Solvents Shanghai Jiao Tong University Aqueous film coating • Aqueous polymeric dispersions are water￾insoluble polymers dispersed in aqueous systems • Nontoxic • Low viscosity • High polymer content • Productive Shanghai Jiao Tong University Compression￾coated tablets

国生 圈生Learning Objectives of Tablets True density,Granule density,Bulk density, Coating equipment Angle of repose Conventional coating pan Tablet excipients:diluents(fillers),binders, disintegrants,lubricants ·Side-vented pan Mechanisms of disintegrants ·Fluid bed Methods of preparation:wet granulation,dry granulation,direct compression, characteristics and procedure 国f线Learning Objectives of Tablets Advantages and disadvantages of direct compression Evaluation:Appearance,Crushing strength, Disintegration,Friability,Dissolution,Weight variation,Drug content uniformit Coating:Sugar coating,film coating, compression coating 4

4 Shanghai Jiao Tong University Coating equipment • Conventional coating pan • Side-vented pan • Fluid bed Shanghai Jiao Tong University Learning Objectives of Tablets True density, Granule density, Bulk density, Angle of repose Tablet excipients: diluents (fillers), binders, disintegrants, lubricants Mechanisms of disintegrants Methods of preparation: wet granulation, dry granulation, direct compression, characteristics and procedure Shanghai Jiao Tong University Learning Objectives of Tablets Advantages and disadvantages of direct compression Evaluation: Appearance, Crushing strength, Disintegration, Friability, Dissolution, Weight variation, Drug content uniformit Coating: Sugar coating, film coating, compression coating