国生 Coated tablets 国4生Effervescent tablets 国生 Tablets used in the oral cavity ©Sugar Coated Tablets糖农片 ·Sublingual tablets话下片 ,Troches合片 ©Film Coated Tablets薄膜衣片 ·B证e:比口腔贴片 ©Enteric coaed tablets肠溶农片 国生 国2生Excipients Excipients Perform a varicty of functions Tablets administered by other routes Providingesse mamacturing techology Any component other than the active functioes ·Soutic可溶片 pharmaceutical ingredient(s)intentionallyaded ,Vaginal tahle别道片 to the formulation of a dosage form. Optimizing o modifying drug release ·Enhancingstabiliy Excipients 国生 Excipients 国生Diluents(fillers)) Physically and chemically stable 多Dilues稀释剂(les填充利 Designed to make up the required bulk f taets when Moistening thedugto puduce of ®Nontoxic ●Disinteg态喇解剂 Physiologically inert ©Lubricants润滑剂 Oxchers: ,&g于rminda ·010g Cheap variable. 6
6 Shanghai Jiao Tong University Coated tablets Sugar Coated Tablets糖衣片 Film Coated Tablets薄膜衣片 Enteric coated tablets肠溶衣片 Shanghai Jiao Tong University Effervescent tablets Shanghai Jiao Tong University Tablets used in the oral cavity • Sublingual tablets舌下片 • Troches含片 • Buccal tablets口腔贴片 Shanghai Jiao Tong University Tablets administered by other routes • Solution tablets可溶片 • Vaginal tablet 阴道片 Shanghai Jiao Tong University Excipients Any component other than the active pharmaceutical ingredient(s) intentionally added to the formulation of a dosage form. Shanghai Jiao Tong University Excipients Perform a variety of functions • Providing essential manufacturing technology functions • Enhancing patient acceptance • Providing aid in product identification • Optimizing or modifying drug release • Enhancing stability Shanghai Jiao Tong University Excipients Physically and chemically stable Nontoxic Physiologically inert Commercially available Cheap Shanghai Jiao Tong University Excipients Diluents稀释剂 (fillers填充剂) Moistening agents润湿剂 and adhesives黏合剂 Disintegrants崩解剂 Lubricants润滑剂 Others: • Absorbents吸收剂, • Coloring agents着色剂, • Flavoring agents矫味剂, • …… Shanghai Jiao Tong University Diluents (fillers) Designed to make up the required bulk of tablets when the drug dosage amount is inadequate to produce of adequate weight and size. • 6 or 7 mm diameter • 80 to 100 mg They also improve compressibility and reduce dose variable
国生 Types of diluents 国生 Moistening agents 国生一Adhesives(Binders) 争Starch淀粉 角Sucro蓝额 Moistening agents are used to moisten the Be added either liquid or in dry form during 国Lactos乳糖 wet granulation to form granules or to promote ·Wad @Microcrystalline cellulose(MCC)微品纤雏素 tablets. Inorganic salts Mannitol and s0 rbitol甘露醇和山梨醇 Adhesives 国生三 Disintegrants 国生一Mechanism ofs Capillay action nd Added to tablet formulstions to 308. faclae disintegration Sweling 。CC-吸甲5纤重素销 落 ”5 ewhwat. ,C乙新杆m素 of the tablet when Hest of wetting 用PV伊豪淮围 contacts water. 一 Gas release PEG聚Z 多S正糖 都 t生Types of disintegrants ©生Disintergrants adding method 生Lubricants ●D叮rh干淀粉 Inragbe added during granultion 多CM心N甲淀粉钠 争Gida助液剂peomtof the tabletg2 nulation added after granulation ⊕L-HC低取代是丙基纤米素 Mixed mode07%ntragraeular ●CCNa文联投甲纤鉴素销 PVPP交联聚 die and poch. Effervescem disimegr2nt泡爵解剂 舍Die wall达ricant润清剂educes friction betwen the 多Surfctae表面话性剂 7
7 Shanghai Jiao Tong University Types of diluents Starch淀粉 Sucrose 蔗糖 Dextrin糊精 Lactose乳糖 Pregelatinized starch预胶化淀粉 Microcrystalline cellulose (MCC)微晶纤维素 Inorganic salts Mannitol and sorbitol甘露醇和山梨醇 Shanghai Jiao Tong University Moistening agents Moistening agents are used to moisten the power and induce its stickiness. • Water • Alcohol Shanghai Jiao Tong University Adhesives (Binders) Be added either liquid or in dry form during wet granulation to form granules or to promote cohesive compact for directly compressed tablets. Shanghai Jiao Tong University Adhesives Starch paste 淀粉浆 Cellulose and its derivatives • MC甲基纤维素 • HPC羟丙基纤维素 • HPMC羟丙甲纤维素 • CMC-Na羧甲基纤维素钠 • EC乙基纤维素 PVP 聚维酮 Gelatin明胶 PEG聚乙二醇 Sucrose蔗糖 Shanghai Jiao Tong University Disintegrants Added to tablet formulations to facilitate disintegration of the tablet when it contacts water. Shanghai Jiao Tong University Mechanism of disintegrants Capillary action • Enhance the action of capillary forces in producing a rapid uptake of aqueous. Swelling • Swell on contact with water. Heat of wetting • The heat of wetting makes the entrapped air swell. Gas release • Effervescent salts are added to tablet to release gases to disrupt the tablet structure Shanghai Jiao Tong University Types of disintegrants Dry starch干淀粉 CMS-Na羧甲淀粉钠 L-HPC低取代羟丙基纤维素 CCNa交联羧甲纤维素钠 PVPP交联聚维酮 Effervescent disintegrants泡腾崩解剂 Surfactants表面活性剂 Shanghai Jiao Tong University Disintergrants adding method Intragranular: be added during granulation Extragranular: be added after granulation Mixed mode: 50~75% intragranular 25~50% extragranular Shanghai Jiao Tong University Lubricants Glidant助流剂 promotes flow of the tablet granulation by reducing friction between them. Antiadherent抗黏剂 reduces sticking of the tablet to the die and punch. Die wall lubricant润滑剂reduces friction between the tablet and the walls of the die cavity