CN1778300B - Luotongding oral cavity disintegration tablet and preparation thereof - Google Patents
Luotongding oral cavity disintegration tablet and preparation thereof Download PDFInfo
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- CN1778300B CN1778300B CN 200410036337 CN200410036337A CN1778300B CN 1778300 B CN1778300 B CN 1778300B CN 200410036337 CN200410036337 CN 200410036337 CN 200410036337 A CN200410036337 A CN 200410036337A CN 1778300 B CN1778300 B CN 1778300B
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- rotundine
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- cavity disintegration
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Abstract
An oral disintegrating tablet of rotundine is prepared through pretreating and tabletting. Its advantages are high dissolving speed and less consumption of auxiliaries.
Description
Technical field
The present invention relates to a kind of rotundine oral cavity disintegration tablet and preparation method thereof.
Background technology
Rotundine, chemical name is 2,3,9,10-tetramethoxy-5,8,13,13 α-tetrahydrochysene-6H-dibenzo [α, g] quinolizine, be used for analgesia, calm, hypnosis clinically, be non-addicted analgesics, be applicable to Encelialgia (as the pain of gastric ulcer and duodenal ulcer), general headache, menstrual pain and childbirth back uterine contraction pain that digestive system disease causes.Because it also has calmness and syngignoscism in analgesic activity, therefore alleviated the misery of pain-suffered patient.Because of its curative effect is clear and definite, side effect is little, and Rotundine Tablets has been listed in Class A OTC medicine, but for many old people and children that more weak function of deglutition is arranged, poor to the drug compliance of common oral Pharmaceutical dosage forms such as dosage forms such as tablet, capsule; For the severe-Iy ill patients that can not initiatively take medicine, common oral preparation has more increased patient and medical personnel's burden; Drug administration by injection, medication inconvenience, patient's compliance is relatively poor again, easily delay treatment; Therefore develop a kind of taking convenience, the good and rapid-action oral cavity disintegration tablet of compliance has the important clinical meaning.
The preparation method that oral cavity disintegration tablet is commonly used is direct compression process and granulating tabletting process, these two kinds of methods all need a large amount of water-fast efficient disintegrating agent and filleies of using, because the water-fast adjuvant of a large amount of uses, oral cavity disintegration tablet is understood residual insoluble matter after the disintegrate in mouth, mouthfeel is poor like this, and patient's compliance is also poor.In addition, the bulk density of rotundine raw material is less, mobile relatively poor, adopt direct compression process or granulating tabletting process all to need a large amount of mobile strong adjuvants to dilute, so the slice, thin piece of large volume can make patient's compliance reduce equally.Therefore how to improve the drug loading of oral cavity disintegration tablet adjuvant, improve the mobile of principal agent and reduce the technological difficulties that supplementary product consumption becomes preparation rotundine oral cavity disintegration tablet.In addition because illumination and high temperature can make the rotundine variable color, how therefore the common piebaldism of the tablet of preparation or be yellow prepare the color and luster homogeneous, the good oral cavity disintegration tablet of outward appearance is again a difficult point.The inventor has set up the preparation technology of rotundine oral cavity disintegration tablet by lot of experiments, has prepared that mouthfeel is good, taking convenience, stay-in-grade rotundine oral cavity disintegration tablet.
Summary of the invention
The invention provides a kind of rotundine oral cavity disintegration tablet.
The invention provides a kind of preparation method of rotundine oral cavity disintegration tablet.
Oral cavity disintegration tablet provided by the invention comprises the rotundine of 5.0-40.0%, the lubricant of the filler of 30.0-80.0%, the disintegrating agent of 5.0-25.0% and 0.1-5.0% substantially.
Oral cavity disintegration tablet of the present invention, its filler can be selected from one or more in lactose, sucrose, microcrystalline Cellulose (MCC), pregelatinized Starch, starch, mannitol, sorbitol, the dextrin.
Oral cavity disintegration tablet of the present invention, disintegrating agent can be one or more in low-substituted hydroxypropyl methylcellulose (L-HPC), cross-linking sodium carboxymethyl cellulose (CCNa), carboxymethyl starch sodium (CMS-Na), crosslinked polyethylene pyrrole Lip river alkane ketone (PVPP), crosslinked carboxymethyl fecula sodium (CCMS-Na) or gas-producing disintegrant sodium carbonate, sodium bicarbonate, potassium bicarbonate, potassium carbonate, citric acid, the tartaric acid.
Oral cavity disintegration tablet of the present invention, lubricant is made up of in Polyethylene Glycol and magnesium stearate, Stepanol MG, micropowder silica gel, the Pulvis Talci one or more.
Oral cavity disintegration tablet provided by the invention can also contain in adhesive, solubilizing agent or the correctives one or more.Wherein adhesive can be polyethylene pyrrole Lip river alkane ketone (PVP), hydroxypropyl methylcellulose battalion (HPMC) or its combination; Solubilizing agent can be one or more in polyethylene pyrrole Lip river alkane ketone (PVP), poloxamer, tween, the Polyethylene Glycol; Correctives can be aspartame, stevioside or its combination, and it accounts for the 0.01-1.0% of gross weight.
The preparation method of oral cavity disintegration tablet of the present invention is for will carrying out direct compression or pelletizing press sheet more earlier after the medicine pretreatment.
The concrete preparation method of oral cavity disintegration tablet provided by the invention is: the recipe quantity rotundine is mixed with the filler or the disintegrating agent of a small amount of good fluidity in the prescription, add an amount of short chain alcohol as wetting agent moistening said mixture, under moisture state, fully mix principal agent and mobile adjuvant, the amount that adds alcohol is can be made into suitable soft just degree of being, with above-mentioned moistening material intensive drying in air dry oven, sieving for standby.Short chain alcohol is volatile ethanol, isopropyl alcohol or its combination.
Direct compression: standby with crossing 80 mesh sieves after each adjuvant drying, take by weighing recipe quantity adjuvant and above-mentioned pretreated principal agent and adjuvant mixture respectively, fully the laggard interline body burden of mix homogeneously is measured, and with conventional tablet machine tabletting, the hardness of control tablet is 2-5kg/cm
2, get final product with common bubble-cap formula packaging material packing.
Tabletting after granulating: each adjuvant is crossed 80 mesh sieves, take by weighing recipe quantity adjuvant and above-mentioned pretreated principal agent and adjuvant mixture respectively, behind the mix homogeneously, add binding agent and make suitable soft, granulation, cold drying, granulate, carry out the intermediate assay, with conventional tablet machine tabletting, the hardness of control tablet is 2-4kg/cm
2, get final product with common bubble-cap formula packaging material packing.Adopt granulating tabletting process, can only medicine (not comprising adjuvant) be carried out pretreatment, then according to preparation prescription and the preparation of conventional granulating tabletting process.
The oral cavity disintegration tablet of the present invention's preparation can use conventional tablet pharmaceutical equipment to produce, and the tablet of preparation has suitable hardness, can use conventional plastic-aluminum bubble-cap formula packing, is not transported the restriction with condition of storage.
Oral cavity disintegration tablet provided by the invention, dissolution rate is fast, rapid-action, the cumulative leaching rate height, the granule after the disintegrate can pass through 0.425 μ m screen cloth fully, does not need water, need not to chew, medicine can borrow swallowing act to go into the stomach onset in 1-60 disintegrate fully in second after the medicine disintegrate, greatly facilitate the emergency case patient's medication under part dysphagia or the special environment.
The present invention is by taking the medicine preconditioning technique and adjuvant being screened, adjust means such as ratio of adjuvant, reached raising adjuvant drug loading, improve the purpose of principal agent flowability and minimizing supplementary product consumption, it is lubricant that the present invention has simultaneously selected Polyethylene Glycol for use, avoid the normal piebaldism that occurs of rotundine tablet, prepared color and luster homogeneous, the good oral cavity disintegration tablet of outward appearance.
Oral cavity disintegration tablet mouthfeel provided by the invention is good, volume is little, sheet heavy moderate, hardness strong, it is broken to be difficult for, preparation technology is simple, be fit to industrialized great production.
Figure: the comparison of rotundine oral cavity disintegration tablet and ordinary tablet stripping curve.
The specific embodiment
Embodiment 1: the preparation oral cavity disintegration tablet
Preparation: each adjuvant is dry in advance, and 80 mesh sieves are standby excessively.The rotundine that takes by weighing 10g mixes with the microcrystalline Cellulose of 20g, adds an amount of moistening of dehydrated alcohol, fully mixes principal agent and mobile adjuvant under moisture state.With above-mentioned moistening material intensive drying in 30 ℃ of air dry ovens, it is standby to cross 80 mesh sieves.Take by weighing each adjuvant of residue by recipe quantity, rotundine and other adjuvant mix homogeneously after desire is handled.Measure intermediate content, tabletting behind adding magnesium stearate, the PEG4000 mix homogeneously.
With the diameter is the scrobicula stamping of 6mm, the heavily about 100mg of sheet, and the control tablet hardness is at 2-5kg/cm
2Not adding jolting by two disintegration time mensuration methods of pharmacopeia, to measure disintegration be 42 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Embodiment 2: the preparation oral cavity disintegration tablet
Preparation: it is standby that each composition is crossed 80 mesh sieves in advance.Take by weighing each composition by recipe quantity, with rotundine and other adjuvant mix homogeneously.Add the soft ability of an amount of system of 3.0% polyethylene pyrrole Lip river alkane ketone K30 alcoholic solution, 20 mesh sieves are granulated, 40 degree air dry oven oven dry, 18 mesh sieve granulate.Measure intermediate content, tabletting promptly behind the adding magnesium stearate mix homogeneously.
The control tablet hardness is at 2-4kg/cm
2, realize that by disintegrate shown in two appendix of pharmacopeia it is 55 seconds that algoscopy is measured disintegration, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Embodiment 3: the preparation oral cavity disintegration tablet
Preparation: the rotundine that takes by weighing 30g mixes with the microcrystalline Cellulose of 34g, adds an amount of moistening of dehydrated alcohol, fully mixes principal agent and mobile adjuvant under moisture state.With above-mentioned moistening material intensive drying in 30 ℃ of air dry ovens, it is standby to cross 80 mesh sieves.
Each adjuvant is dry in advance, and 80 mesh sieves are standby excessively.Take by weighing sucrose 19g, sodium bicarbonate 2.3g, citric acid 3g, aspartame 0.2g, rotundine and above-mentioned adjuvant mix homogeneously after desire is handled.Measure intermediate content, tabletting behind adding 0.5g Pulvis Talci and the 1.0gPEG400 mix homogeneously.
With the diameter is the scrobicula stamping of 6mm, the heavily about 100mg of sheet, and the control tablet hardness is at 2-5kg/cm
2, not adding jolting by disintegration time mensuration method shown in two appendix of pharmacopeia, to measure disintegration be 25 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Embodiment 4: the preparation oral cavity disintegration tablet
Preparation: the rotundine that takes by weighing 5g mixes with the carboxymethyl starch sodium of 14.5g, joins in the said mixture with an amount of dehydrated alcohol, fully mixes principal agent and mobile adjuvant under moisture state.With above-mentioned moistening material intensive drying in 30 ℃ of air dry ovens, it is standby to cross 80 mesh sieves.
Each adjuvant is dry in advance, and 80 mesh sieves are standby excessively.Take by weighing each adjuvant of residue by prescription, rotundine and other adjuvant mix homogeneously after desire is handled.Measure intermediate content, add evenly back tabletting of mix lubricant.
With the diameter is the scrobicula stamping of 6mm, the heavily about 100mg of sheet, and the control tablet hardness is at 2-5kg/cm
2, not adding jolting by disintegration time mensuration method shown in two appendix of pharmacopeia, to measure disintegration be 37 seconds, the granule after the disintegrate can be all by the screen cloth in 0.425mm aperture.
Claims (3)
1. rotundine oral cavity disintegration tablet, 1000 component is rotundine 10g, microcrystalline Cellulose 45g, direct compression lactose 33.8g, low-substituted hydroxypropyl methylcellulose 10.2g, magnesium stearate 0.5g and 0.5g PEG 4000; It adopts following method preparation: each adjuvant is dry in advance, and 80 mesh sieves are standby excessively, the rotundine that takes by weighing 10g mixes with the microcrystalline Cellulose of 20g, add an amount of moistening of dehydrated alcohol, under moisture state, fully mix principal agent and mobile adjuvant, with above-mentioned moistening material intensive drying in 30 ℃ of air dry ovens, it is standby to cross 80 mesh sieves, take by weighing each adjuvant of residue by recipe quantity, with pretreated rotundine and other adjuvant mix homogeneously, measure intermediate content, adding behind magnesium stearate, the PEG4000 mix homogeneously with the diameter is the stamping of 6mm scrobicula.
2. rotundine oral cavity disintegration tablet, 1000 component is rotundine 20g, microcrystalline Cellulose 35g, mannitol 29.4g, pregelatinized Starch 2.5g, cross-linking sodium carboxymethyl cellulose 12g, 3.0% polyethylene pyrrole Lip river alkane ketone K30 alcoholic solution is an amount of, aspartame 0.1g, magnesium stearate 0.5g and 0.5g PEG 4000; It adopts following method preparation: it is standby that each composition is crossed 80 mesh sieves in advance, take by weighing each composition by recipe quantity, with rotundine and other adjuvant mix homogeneously, add the soft ability of an amount of system of 3.0% polyethylene pyrrole Lip river alkane ketone K30 alcoholic solution, 20 mesh sieves are granulated, 40 degree air dry oven oven dry, 18 mesh sieve granulate, measure intermediate content, tabletting promptly behind the adding magnesium stearate mix homogeneously.
3. rotundine oral cavity disintegration tablet, 1000 component is rotundine 30g, microcrystalline Cellulose 34g, sucrose 19.0g, crosslinked polyethylene pyrrole Lip river alkane ketone 10g, sodium bicarbonate 2.3g, citric acid 3g, aspartame 0.2g, Pulvis Talci 0.5g, 1.0g PEG6000; It adopts following method preparation: the rotundine that takes by weighing 30g mixes with the microcrystalline Cellulose of 34g, add an amount of moistening of dehydrated alcohol, under moisture state, fully mix principal agent and mobile adjuvant, with above-mentioned moistening material intensive drying in 30 ℃ of air dry ovens, it is standby to cross 80 mesh sieves, each adjuvant is dry in advance, and 80 mesh sieves are standby excessively, get sucrose 19g, sodium bicarbonate 2.3g, citric acid 3g, aspartame 0.2g, with pretreated rotundine and above-mentioned adjuvant mix homogeneously, decide intermediate content, adding behind 0.5g Pulvis Talci and the 1.0g PEG6000 mix homogeneously with the diameter is the scrobicula stamping of 6mm.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410036337 CN1778300B (en) | 2004-11-18 | 2004-11-18 | Luotongding oral cavity disintegration tablet and preparation thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410036337 CN1778300B (en) | 2004-11-18 | 2004-11-18 | Luotongding oral cavity disintegration tablet and preparation thereof |
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| CN1778300A CN1778300A (en) | 2006-05-31 |
| CN1778300B true CN1778300B (en) | 2010-09-08 |
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| CN 200410036337 Expired - Fee Related CN1778300B (en) | 2004-11-18 | 2004-11-18 | Luotongding oral cavity disintegration tablet and preparation thereof |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2218443B1 (en) * | 2007-11-21 | 2014-03-26 | Dainippon Sumitomo Pharma Co., Ltd. | Orally disintegrating tablet |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1125572A (en) * | 1994-12-28 | 1996-07-03 | 顺德市广容制药厂 | Manufacture method of "Luotongding"pain-killing tablet |
| CN1483407A (en) * | 2002-09-18 | 2004-03-24 | 中国人民解放军军事医学科学院毒物药 | Medicinal composition containing rotundine for anayesia and giving up drug-taking |
-
2004
- 2004-11-18 CN CN 200410036337 patent/CN1778300B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1125572A (en) * | 1994-12-28 | 1996-07-03 | 顺德市广容制药厂 | Manufacture method of "Luotongding"pain-killing tablet |
| CN1483407A (en) * | 2002-09-18 | 2004-03-24 | 中国人民解放军军事医学科学院毒物药 | Medicinal composition containing rotundine for anayesia and giving up drug-taking |
Non-Patent Citations (2)
| Title |
|---|
| 张辉等.口腔崩解片的研制.海南医学14 9.2003,14(9),88-90. * |
| 马萍等.口腔速崩片的研究进展.中国药师7 3.2004,7(3),173-175. * |
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| CN1778300A (en) | 2006-05-31 |
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Effective date of registration: 20170613 Address after: 264670, No. 15, pioneering Road, hi tech Zone, Shandong, Yantai Patentee after: Shandong Luye Pharma Co., Ltd. Address before: 264003 Laishan, Shandong Province Bao Road, No. 9 District, No. Patentee before: Luye Natural Medicinal Research Developing Co., Ltd., Shandong Prov. |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
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Granted publication date: 20100908 Termination date: 20181118 |