片剂的制备工业药剂

,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,2020/11/4,*,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,2020/11/4,*,单击此处编辑母版标题样式,单击此处编辑母版文本样式,第二级,第三级,第四级,第五级,2020/11/4,*,Purpose,Introduction,Equipments and Materials,Procedures,Experimental Instructions,Questions,Test report,2020/11/4,1,Purpose,1. To master the basic technological course of tablets through the preparation of aspirin tablets.,2. To be familiar with the q,uality control of tablets,.,3. To be familiar with the basic structure and operation method of single-punch.,2020/11/4,2,Introduction,Tablets are solid preparations of various shapes, usually round, and obtained by compressing uniform volumes of particles containing one or more active ingredients with suitable excipients,.,2020/11/4,3,Introduction -,tablet types,Some of the pharmaceutical tablet types based on the way of administration or presentation to the patient are listed on the right:,1.,Simple uncoated tablets,2. Coated tablets,3. Effervescent tablets,4. Buccal and sublingual tablets,5. Chewable tablets,6. Multilayered tablets,7. Sugarcoated tablets,8. Fast-disintegrating tablets,9. Vaginal tablets,10. Osmotic tablets,11. Controlled-release tablets,12. Multicomponent tablets,2020/11/4,4,Introduction -,tablet design,Tablet formulation design starts with a predetermined value, which is,the dose size,.,Tablet design is based on the experience and knowledge of,excipients, which are materials serving the purpose of making a good tablet when combined with a drug.,2020/11/4,5,Introduction -,tablet design,Tablet excipients can be classified on the basis of their functionality as listed below:,1. Fillers/diluents,2. Binders,3. Disintegrants,4. Lubricants,5. Glidants,6. Buffering,agents,7. Sweeteners,8. Wetting agents,9. Coating agents,10. Matrix formers,2020/11/4,6,Introduction -,manufacturing processes,Deciding on a manufacturing method is a complex task that requires time, equipment, and formulation optimization, as well as a close collaboration between formulation scientists and process engineers.,In general terms, there are three manufacturing processes for tablets:,wet granulation,dry granulation, and,direct compression,.,2020/11/4,7,Introduction -,manufacturing processes,The purpose of,wet granulation,is to convert the drug and excipient mixture into granules that flow well into dies, and which are compressible into mechanically strong and acceptable tablets.,1. flowability 2. compressibility,Wet granulation compression method has been widely used in tablets production, especially for drugs resistant to wet and heat.,2020/11/4,8,Introduction -,manufacturing processes,The steps of wet granulation,Premixing drug with other ingredients using a mixer.,Transferring the mixture into a traditional low shear granulator where a binder solution is added under a mechanical shear until a certain damp mass and a certain granule size are obtained.,Wet sieving of granules through a desired screen size.,Drying of granules in a tray-oven dryer.,Dry sieving/milling of granules to a certain particle size distribution.,Adding a lubricant to the dry granules.,Compressing the granules into tablets.,2020/11/4,9,Introduction -,manufacturing processes,The steps of wet granulation,2020/11/4,10,混,合,压,片,填充剂,黏合剂,崩解剂,API,辅料,粉,碎,和,过,筛,制,软,材,干,燥,整,粒,混,合,制,湿粒,润滑剂,崩解剂,湿法制粒压片工艺流程,Introduction -,manufacturing processes,2020/11/4,11,Equipments and Materials,Equipments:,electronic balance, single-punch press, nylon sieve (16 and 18 mesh), punch (9.5mm shallow concave punch), etc,.,Materials :,aspirin (in granule crystal), tartaric acid, talcum powder, starch, concentrated hydrochloric acid, sodium hydroxide, distilled water, etc.,2020/11/4,12,Procedure,1. Preparation of aspirin tablets,(1) Formulation (weight in 100 tablets),Aspirin30 g,Starch 2 g,Tartaric acid 0.2 g,10% starch paste qs,Starch 1 g,Talcum powder 1.5 g,2020/11/4,13,(2) Preparing processes,Preparing 10% starch paste: H,eating the aqueous dispersion of starch,( 2 g starch and 0.2g tartaric acid in 20mL water),at 80,for 15 min,.,G,rinding,aspirin to pass the sieve of 80 meshes.,Mixing aspirin powder with starch.,Adding 10% starch paste to prepare a damp mass.,Screening the damp mass through a nylon sieve of 18 meshes into granules.,Drying of the wet granules at 60,for 15 min.,Dry sieving of granules through 16 meshes.,Adding starch and talcum powder to dry granules with blending uniformly.,Compressing the granules into tablets.,制软材,制湿粒,研磨,混合,干燥,整粒,压片,混合,制淀粉浆,2020/11/4,14,single-punch press,rotary tablet press,2020/11/4,15,2. Single-punch press,manual driving wheel,hopper,feed shoe,cam gearing,core components,die,(,模圈,),lower punch,(,下冲,),upper punch,(,上冲,),2020/11/4,16,2020/11/4,17,2020/11/4,18,2020/11/4,19,3. Installing of single-punch press,Installing of core components,Installing of the lower punch,安装下冲： 旋松下冲固定螺钉，转动大皮带轮使下冲芯杆升到最高位置，将下冲插入下冲芯杆的孔中（注意使下冲杆的,缺口斜面,对准下冲紧固螺钉，并要插到底）最后旋紧下冲固定螺钉。,2020/11/4,20,Installing of the lower punch,安装上冲：旋松上冲紧固螺母，将上冲插入上冲芯杆的孔中，要插到底，旋紧上冲紧固螺母。,Installing of the mould,安装中模：旋松中模固定螺钉，将中模拿平放入中模台板的孔中，旋紧中模固定螺钉。缓缓转动大皮带轮，调整中模台板的位置，使上冲进入中模孔中，旋紧中模台板固定螺钉。,2020/11/4,21,(2) Adjustment of out-of-tablets,出片调整,转动大皮带轮使下冲升到最高位置，观察下冲口面是否与中模平面相齐（或高或低都将影响出片），若不齐则旋松蝶形螺丝，松开齿轮压板转动上调节齿轮，使下冲口面与中模平面相齐，然后将压板按上，旋紧蝶形螺丝。,用手转动大皮带轮，空车运转若正常，则可加料试压，进行下一步调整。,2020/11/4,22,(3) Adjustment of tablet weight,片重调节,旋松蝶形螺丝，松开齿轮压板。转动下调节齿轮向左转使下冲芯杆上升，则充填深度减少（药片重量减轻）。调节好后将轮齿压板按上，旋紧蝶形螺丝。,(4) Adjustment of tablet hardness,硬度调节,旋松连杆锁紧螺母、转动上冲芯杆，向左转使上冲芯杆向下移动，则压力加大，压出的药片硬度增加；反之，硬度降低。调节好后用扳手卡住上冲芯杆下部的六方，将连杆锁紧螺母锁紧。,2020/11/4,23,4. Tablet compression,压片,冲模的安装、调试完成后，即可启动电机试压，检查片重、硬度和表面光洁度等，质量如合格，即可投料批量生产。,在生产过程中仍须随时检查药片质量，及时调整。,2020/11/4,24,5. Q,uality control of tablets,After manufacturing tablets, a series of tests are carried out to assure that they meet the specifications of pharmacopoeia or industry standards. These tests are as listed on the right:,Weight,Weight variation,Disintegration,Hardness,Friability,Dissolution,Drug content uniformity,Thickness,2020/11/4,25,(1) Tablet weight and weight variation,The quantity of fill placed in the die cavity of a tablet press determines the weight of the resulting tablet.,Weight variation,: sample amount,20 tablets,.,Tablets should comply with the following requirements stated in the table below.,Average weight,Weight variation limit,Less than 0.3 g, 7.5%,0.3 g or more, 5%,2020/11/4,26,(2) Tablet hardness,In general, tablets should be sufficiently hard to resist breaking during normal handling, packaging and shipping, and yet soft enough to disintegrate properly after swallowing.,Hardness of the tablet is controlled by (or is affected by) the degree of the pressure applied during the compression stage.,2020/11/4,27,(2) Tablet hardness,Sample amount,4 tablets,.,2020/11/4,28,(3) Tablet disintegration test,Tablets must be tested to ensure disintegration.,The CP, BP, USP and EP have official standards, including descriptions of the apparatus type dimensions and test conditions.,2020/11/4,29,(3) Tablet disintegration test,Sample amount,6 tablets,.,2020/11/4,30,(4) Tablet friability,This test shows the strength of tablets against mechanical attrition.,Method: allowing the tablets to roll and fall within the rotating apparatus (friabilator); determine the loss in weight;,Requirement: weight loss 1%,2020/11/4,31,(4) Tablet friability,2020/11/4,32,Experimental Instructions,1. Aspirin acid should be milled and forced through screen (80 mesh), then mix with excipients, usually we use the method that mass increased as others increased, screen and mix several times to insure uniformly mixed.,2. The dosage of adhesives should be aptitude to make the soft material be conglomeration in hand and when fingers press it slightly, it should disperse but does not turn into powders.,2020/11/4,33,