片劑的制備工業(yè)藥劑

1、PurposeIntroductionEquipments and MaterialsProceduresExperimental InstructionsQuestionsTest report Purpose 1. To master the basic technological course of tablets through the preparation of aspirin tablets.2. To be familiar with the quality control of tablets.3. To be familiar with the basic structur

2、e and operation method of single-punch.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.Introduction - tablet typesSome of the pharmaceutical table

3、t types based on the way of administration or presentation to the patient are listed on the right:1. Simple uncoated tablets2. Coated tablets3. Effervescent tablets4. Buccal and sublingual tablets5. Chewable tablets6. Multilayered tablets7. Sugarcoated tablets8. Fast-disintegrating tablets9. Vaginal

4、 tablets10. Osmotic tablets11. Controlled-release tablets12. Multicomponent tabletsIntroduction - tablet designTablet 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 pu

5、rpose of making a good tablet when combined with a drug.Introduction - tablet designTablet excipients can be classified on the basis of their functionality as listed below:1. Fillers/diluents2. Binders3. Disintegrants4. Lubricants5. Glidants6. Buffering agents7. Sweeteners8. Wetting agents9. Coating

6、 agents10. Matrix formersIntroduction - manufacturing processesDeciding 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 ma

7、nufacturing processes for tablets: wet granulation, dry granulation, and direct compression.Introduction - manufacturing processesThe 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 an

8、d acceptable tablets. 1. flowability 2. compressibilityWet granulation compression method has been widely used in tablets production, especially for drugs resistant to wet and heat. Introduction - manufacturing processesThe steps of wet granulation1 Premixing drug with other ingredients using a mixe

9、r. 2 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.3 Wet sieving of granules through a desired screen size.4 Drying of granules in a tray-oven dryer.5 Dry si

10、eving/milling of granules to a certain particle size distribution.6 Adding a lubricant to the dry granules.7 Compressing the granules into tablets.Introduction - manufacturing processesThe steps of wet granulation 混合壓片填充劑黏合劑崩解劑API輔料粉碎和過篩制軟材干燥整粒混合制濕粒潤滑劑崩解劑濕法制粒壓片工藝流程Introduction - manufacturing proces

11、sesEquipments 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,

12、etc.Procedure1. 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(2) Preparing processesPreparing 10% starch paste: Heating the aqueous dispersion of starch ( 2 g starch and 0.2g tartari

13、c acid in 20mL water) at 80 for 15 min. Grinding 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

14、 of granules through 16 meshes.Adding starch and talcum powder to dry granules with blending uniformly.Compressing the granules into tablets.制軟材制濕粒研磨混合干燥整粒壓片混合制淀粉漿single-punch pressrotary tablet press2. Single-punch pressmanual driving wheel hopper feed shoe cam gearing core components die (模圈) lowe

15、r punch (下沖) upper punch (上沖) 3. Installing of single-punch press(1)Installing of core components Installing of the lower punch安裝下沖： 旋松下沖固定螺釘，轉(zhuǎn)動大皮帶輪使下沖芯桿升到最高位置，將下沖插入下沖芯桿的孔中（注意使下沖桿的缺口斜面對準(zhǔn)下沖緊固螺釘，并要插到底）最后旋緊下沖固定螺釘。 Installing of the lower punch安裝上沖：旋松上沖緊固螺母，將上沖插入上沖芯桿的孔中，要插到底，旋緊上沖緊固螺母。 Installing of the

16、mould安裝中模：旋松中模固定螺釘，將中模拿平放入中模臺板的孔中，旋緊中模固定螺釘。緩緩轉(zhuǎn)動大皮帶輪，調(diào)整中模臺板的位置，使上沖進(jìn)入中?？字校o中模臺板固定螺釘。(2) Adjustment of out-of-tablets 出片調(diào)整 轉(zhuǎn)動大皮帶輪使下沖升到最高位置，觀察下沖口面是否與中模平面相齊（或高或低都將影響出片），若不齊則旋松蝶形螺絲，松開齒輪壓板轉(zhuǎn)動上調(diào)節(jié)齒輪，使下沖口面與中模平面相齊，然后將壓板按上，旋緊蝶形螺絲。 用手轉(zhuǎn)動大皮帶輪，空車運(yùn)轉(zhuǎn)若正常，則可加料試壓，進(jìn)行下一步調(diào)整。(3) Adjustment of tablet weight片重調(diào)節(jié) 旋松蝶形螺絲，松開齒輪壓板

17、。轉(zhuǎn)動下調(diào)節(jié)齒輪向左轉(zhuǎn)使下沖芯桿上升，則充填深度減少（藥片重量減輕）。調(diào)節(jié)好后將輪齒壓板按上，旋緊蝶形螺絲。(4) Adjustment of tablet hardness硬度調(diào)節(jié) 旋松連桿鎖緊螺母、轉(zhuǎn)動上沖芯桿，向左轉(zhuǎn)使上沖芯桿向下移動，則壓力加大，壓出的藥片硬度增加；反之，硬度降低。調(diào)節(jié)好后用扳手卡住上沖芯桿下部的六方，將連桿鎖緊螺母鎖緊。4. Tablet compression壓片 沖模的安裝、調(diào)試完成后，即可啟動電機(jī)試壓，檢查片重、硬度和表面光潔度等，質(zhì)量如合格，即可投料批量生產(chǎn)。 在生產(chǎn)過程中仍須隨時檢查藥片質(zhì)量，及時調(diào)整。5. Quality control of tablet

18、s 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:WeightWeight variationDisintegrationHardnessFriabilityDissolutionDrug content uniformityThickness(1) Tablet weig

19、ht 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 weightWeight variation limitLess

20、than 0.3 g 7.5%0.3 g or more 5%(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

21、of the pressure applied during the compression stage. (2) Tablet hardness Sample amount 4 tablets.(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 condition

22、s.(3) Tablet disintegration test Sample amount 6 tablets.(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%(4)

23、 Tablet friabilityExperimental Instructions1. 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 a

24、ptitude to make the soft material be conglomeration in hand and when fingers press it slightly, it should disperse but does not turn into powders. Purpose 1. To master the basic technological course of tablets through the preparation of aspirin tablets.2. To be familiar with the quality control of tablets.3. To be familiar with the basic structure and operation method of single-punch.Introduction - tablet designTablet excipients can be classified on the basis of their functionality as listed below:1. Fillers/diluents2. Binders3. Dis