CN104644809A - TGCJ sustained-release tablet and preparation method thereof - Google Patents
TGCJ sustained-release tablet and preparation method thereof Download PDFInfo
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Abstract
Belonging to the field of Chinese medicinal preparations, the invention relates to a TGCJ sustained-release tablet and a preparation method thereof. The TGCJ sustained-release tablet is composed of, by weight, 19.8%-69.3% of TGCJ, 9.9%-59.4% of a sustained-release material and 6.0%-60.4% of a pharmaceutical adjuvant. Ultraviolet spectrophotometry determines that the content of TGCJ, in terms of gardenoside, is not less than 70% (weight), and the weight ratio of genipin-1-beta-gentiobioside to gardenoside in the TGCJ is 1-2:10. The invention also discloses the preparation method of the TGCJ sustained-release tablet. The method includes extraction of TGCJ and preparation of the TGCJ sustained-release tablet. When the TGCJ sustained-release tablet enters the human body, drugs are released slowly, the release time can be prolonged, a stable blood concentration can be maintained, and the effectiveness is high. The TGCJ sustained-release tablet can reduce the irritation of drugs to the stomach and intestine, lower the side effect of drugs, reduce drug-taking times, and improve patient medication compliance.
Description
Technical field
The invention belongs to field of traditional Chinese, be specifically related to slow releasing tablet of a kind of Fructus Gardeniae total glycosides and preparation method thereof.
Background technology
The dry mature fruit that Fructus Gardeniae (Gardenia jasminoides Ellis) is Maguireothamnus speciosus Fructus Gardeniae, cold in nature, bitter in the mouth, be conventional Traditional Chinese Medicine of Qin gre lei, there is pathogenic fire purging relieving restlessness, clearing away heat-damp and promoting diuresis, the effects such as removing pathogenic heat from blood and toxic substance from the body, vexed for calentura, jaundice dark coloured urine, blood strangury and dry pain, heat in blood tells nosebleed, conjunctival congestion and swelling pain, pathogenic fire,toxin and furuncles, bruise pain etc.
The iridoid glycoside constituents that the main component of Fructus Gardeniae is is representative with jasminoidin (Gardenoside), as jasminoidin, Gardenoside, genipin-1-β-D-gentiobioside with cape jasmine, deacetyl asperulosidic acid methyl ester and Fructus Gardeniae glycosides etc.In addition, Fructus Gardeniae is also containing organic acid, flavonoid (as gardenin), tannin, a small amount of pectin, polysaccharide and the composition such as volatile oil and unsaturated fatty acid.Fructus Gardeniae total glycosides is the effective site extracted from Fructus Gardeniae; main component is jasminoidin; there is hepatic cholagogic, antipyretic-antalgic, promotion pancreatic secretion, antimicrobial antiphlogistic, blood pressure lowering, prevent and treat atherosclerosis and antithrombus formation, protection ischemic tissue of brain, dementia and treatment soft tissue injury etc. and cure mainly relevant physiologically active to Fructus Gardeniae function; it is the main pharmacodynamics composition of Fructus Gardeniae; disclosed report display, what in Fructus Gardeniae total iridoid glycosides, active component was the highest is jasminoidin and genipin-1-β-D-gentiobioside with cape jasmine.
, antiinflammatory antipyretic for Fructus Gardeniae total glycosides, protect the liver, function of gallbladder promoting, analgesia, calmness, the effect such as antibacterial, existing detailed patent and bibliographical information both at home and abroad, such as, Wu Hong etc. are studied the antiinflammatory of Fructus Gardeniae total glycosides (TGCJ), analgesic activity, show that Fructus Gardeniae total glycosides has obvious antiinflammatory action and certain analgesic activity, and to determine Fructus Gardeniae total glycosides be antiinflammatory, analgesic effective site (Wu Hong, Wei Wei, Song Lihua. anti-inflammatory and analgesic effect research [J] of Fructus Gardeniae total glycosides. Chinese Chinese medicine information magazine, 2006,13(7): 31-33.); The oxidation resistance to Fructus Gardeniae total saponins such as Su Wei is studied, result shows that Fructus Gardeniae total glycosides all shows stronger antioxidant activity in each antioxidant system, and the dose-effect relationship (Su Wei be proportionate, Zhao Li, Liu Jiantao, Deng. Fructus Gardeniae total glycosides oxidation resistance research [J]. Food Science, 2009,30 (15): 75-77.); That Sha etc. have studied the impact of Fructus Gardeniae total glycosides on liver-depression and spleen-insufficiency type chronic hepatitis hemorheology of rat, find the improvement blood circulation that has of Fructus Gardeniae total glycosides and dirty effect (that Sha of hepatoprotective, Long Zijiang, Wang Zongdian, Deng. Fructus Gardeniae total glycosides is on the impact [J] of liver-depression and spleen-insufficiency type chronic hepatitis hemorheology of rat. Jiangsu Chinese medicine, 2005,26 (1): 52-54.); Lu Jinfeng etc. have studied the impact of Fructus Gardeniae total iridoid glycosides on cerebral hemorrhage rats endothelial barrier; result proves that Fructus Gardeniae total iridoid glycosides can protect rat brain endothelial barrier; promote endothelium reparation; reduce the permeability of blood brain barrier, reduce cerebral edema (Lu Jinfeng, Xiang Jing; Huang Wei; Deng. Fructus Gardeniae total iridoid glycosides is on the impact [J] of cerebral hemorrhage rats endothelial barrier. Pharmacology and Clinics of Chinese Materia Medica, 2012,28 (3): 48-51.).In addition, Chinese patent CN1660198A discloses Fructus Gardeniae total iridoid glycosides and is used for the treatment of cholecystitis, cholelithiasis; Chinese patent CN1546507A discloses the purposes of Fructus Gardeniae total glycosides in the medicines such as preparation treatment cerebral thrombosis, cerebral ischemia, coronary heart disease and angina pectoris; Chinese patent CN1689581A discloses jasminoidin and is used for the treatment of disease of viral infection, as treated upper respiratory tract infection, viral pneumonia in preparation, simplex keratitis keratitis, dermopathic herpesvirus disease, the application in the medicine of herpes viral encephalitis etc.; Chinese patent CN102961394A also discloses the purposes of jasminoidin in preparation treatment fatty liver medicament.
About the extracting and developing of Fructus Gardeniae total iridoid glycosides constituents, domestic existing detailed patent and bibliographical information, such as, Chinese patent CN101066311B discloses a kind of preparation method of total jasminoidin extract, key step comprises to be extracted with alcoholic solution, macroporous resin column separation, impurity removal; Chinese patent CN1706858A discloses a kind of method that cape jasmine fruit prepares jasminoidin, genipin-1-β-D-gentiobioside with cape jasmine, and obtains high-purity jasminoidin and genipin-1-β-D-gentiobioside with cape jasmine; Chinese patent literature CN1706860 discloses the method with preparing total iridoid glycoside with cape jasmine fruit, the method water (or alcoholic solution) soaks or cape jasmine fruit crude extract is prepared in backflow, by macroporous adsorptive resins on crude extract, respectively with a small amount of water and low-concentration ethanol aqueous solution eluting, after concentrating under reduced pressure Fructus Gardeniae total iridoid glycosides; Yao Gan etc. describe with the method for total iridoid glycoside and jasminoidin in HPD450 purification with macroreticular resin Fructus Gardeniae, and establish total iridoid glycoside in Fructus Gardeniae assay method (Yao Gan etc. the research [J] of total iridoid glycoside and jasminoidin in purification with macroreticular resin Fructus Gardeniae. Chinese herbal medicine, 37th volume the 1st phase, in January, 2006); The technique of Zhao Chengcheng to Fructus Gardeniae total iridoid glycosides extract conducts in-depth research, and drawn best preparation method (Zhao Chengcheng. Fructus Gardeniae total iridoid glycosides extract technology and quality research [J]. Chengdu University of Traditional Chinese Medicine's 2011 Master degree candidate's academic dissertations); The purifying process to Fructus Gardeniae total iridoid glycosides such as Chen Fang is studied, and determine best purifying process, key step comprises the (Chen Fang such as alcohol extraction and crystallization, Dong Zhi, Fu Ya. Fructus Gardeniae total iridoid glycosides purifying process research [J]. laser magazine, 2010,31 (2): 95-96.).
Visible, Fructus Gardeniae total iridoid glycosides constituents has multiple pharmacological effect effect, there is wide potential applicability in clinical practice, simultaneously, the research report taking jasminoidin as the total iridoid glycoside isolation and purification method of representative is also a lot, but about the research of Fructus Gardeniae total glycosides preparation process, particularly Fructus Gardeniae total glycosides slow releasing preparation is but very few, also little about the preparation of Fructus Gardeniae total glycosides on market, this has limited to the application of Fructus Gardeniae total glycosides at field of medicaments to a certain extent.The moulding process of Chen Fang to Fructus Gardeniae total iridoid glycosides is studied, Fructus Gardeniae total glycosides after separation and purification has been prepared into capsule (Chen Fang. Fructus Gardeniae total iridoid glycosides purification and Study on Forming. Medical University Of Chongqing's 2010 Master degree candidate's academic dissertations), but Fructus Gardeniae total glycosides slow releasing preparation not to be related to; Du Xianhua is studied in the systemic kinetics of rat intestine jasminoidin, result shows that jasminoidin has absorption at whole intestinal segment, there is absorption window widely, be applicable to being prepared into oral sustained release or controlling agent (Du Xianhua, Niu Xin, Feng Qianjin, Deng. jasminoidin rat is in the dynamic (dynamical) research of body intestinal absorption (J). West China pharmaceutical journal, 2008,2(5): 558-560), but it does not disclose the concrete preparation method of slow releasing preparation.
In view of above-mentioned deficiency, be necessary to invent the new preparation of a kind of Fructus Gardeniae total glycosides, make it to expand Fructus Gardeniae total glycosides application clinically, facilitate patient to use, the drug action of Fructus Gardeniae total glycosides can be played again to the full extent, reduce toxic and side effects.After slow releasing preparation refers to administration, medicine can discharge medicine, to maintain effective blood drug concentration, to reach the preparation of long-acting in the time of subscribing with zero level or close to the speed of zero level.Fructus Gardeniae total glycosides is the effective site extracted from Fructus Gardeniae, and main component is jasminoidin, and jasminoidin is eliminated soon in vivo, and the holdup time is short, and in intestinal, tool absorption window widely, is suitable for making slow releasing preparation.
Summary of the invention
The object of this invention is to provide a kind of Fructus Gardeniae total glycosides slow releasing tablet, described Fructus Gardeniae total glycosides slow releasing tablet, with different release mechanisms, can reduce rate of release, extends release time, reduces medicining times, reduces the compliance etc. of side effects of pharmaceutical drugs and raising patient medication.
The present invention relates to a kind of Fructus Gardeniae total glycosides slow releasing tablet, composed of the following components:
A, Fructus Gardeniae total glycosides 19.8% ~ 69.3%(weight)
B, slow-release material 9.9% ~ 59.4%(weight)
C, pharmaceutic adjuvant 6.0% ~ 60.4%(weight)
Preferably, by weight percentage, Fructus Gardeniae total glycosides accounts for 30%-50%, and slow-release material accounts for 20%-40%, and pharmaceutic adjuvant accounts for 10%-50%.
Fructus Gardeniae total glycosides of the present invention measures with ultraviolet visible spectrophotometry (Chinese Pharmacopoeia 2010 editions one annex V A), is no less than 70%(weight in jasminoidin content); In described Fructus Gardeniae total glycosides, the weight ratio of genipin-1-β-D-gentiobioside with cape jasmine and jasminoidin is 1-2:10.Measuring Fructus Gardeniae total glycosides step is: getting need testing solution and suitably dilute, take water as blank, measures absorbance at 237nm wavelength place, in jasminoidin, calculates the content of Fructus Gardeniae total glycosides.
Described slow-release material is one or more in hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, hyprolose, ethyl cellulose, carbomer, stearic acid, hexadecanol, octadecanol, polyacrylic resin cellulose acetate; Preferably, slow-release material is one or more in hydroxypropyl methylcellulose, ethyl cellulose, carbomer.
Wherein, described pharmaceutic adjuvant is one or more in filler, lubricant, binding agent.
Preferably, filler is one or more in microcrystalline Cellulose, pregelatinized Starch, micropowder silica gel, lactose, starch, dextrin, calcium hydrogen phosphate, calcium sulfate.
Preferably, lubricant is one or more in Pulvis Talci, magnesium stearate, micropowder silica gel.
Preferably, binding agent is one or more in 95% ethanol, polyvinylpyrrolidone, ethyl cellulose.
Another object of the present invention is to provide a kind of preparation method of Fructus Gardeniae total glycosides slow releasing tablet, specifically comprises the following steps:
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 60% ~ 80% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 30% ~ 50% ethanol elutions again, collect total iridoid glycoside, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
By Fructus Gardeniae total glycosides, slow-release material, filler mixing, cross 80 mesh sieves, add binding agent moistening and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add lubricant, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
Preferably, described in step 1), the concentration of reflux, extract, ethanol is 70%, and the concentration of eluting ethanol is 40%.
Preferably, the model of macroporous resin described in step 1) is HPD100, LS-303 or XDA-8, and optimum is XDA-8.
Vitro release test shows, Fructus Gardeniae total glycosides slow releasing preparation of the present invention discharged 20%-40% in 2 hours, in 4 hours, discharge 40%-60%, and in 10 hours, release is greater than 75%, reach the effect of 12 hours slow releasing, comparatively ordinary preparation drug release is slowly lasting.For checking the effect of Fructus Gardeniae total glycosides slow releasing tablet of the present invention, the release of inventor to Fructus Gardeniae total glycosides slow releasing tablet measures, the Fructus Gardeniae total glycosides slow releasing tablet obtained by most preferred embodiment is selected to measure by " test of Fructus Gardeniae total glycosides slow releasing tablet In Vitro Dissolution " method described in embodiment 15, record 3 batches of Fructus Gardeniae total glycosides slow releasing tablet Duplicate Samples release curves, refer to Fig. 1.
Compared with the prior art, Fructus Gardeniae total glycosides slow releasing tablet of the present invention has following significant progress:
Fructus Gardeniae total glycosides slow releasing preparation of the present invention enters sustained release after human body, can extend release time, and can reduce the undulatory property of blood drug level, avoid peak valley phenomenon, the blood drug level of held stationary, effectiveness is high simultaneously; The zest of medicine to gastrointestinal can be reduced, reduce side effects of pharmaceutical drugs and untoward reaction, reduce medicining times, improve the compliance of patient medication; Can fully meet clinical needs thus, for extensive patients clinical application provides strong guarantee.Further, Sustained Release Preparations of Chinese Medicinal has become forward position and the focus of Chinese medicine preparation research, represents the development development trend of following Chinese medicine preparation technology.
Accompanying drawing explanation
Fig. 1 is Fructus Gardeniae total glycosides dissolution of sustained-release tablets correlation curve figure;
In accompanying drawing, curve 1 is embodiment 2 parallel sample 1, and curve 2 is embodiment 2 parallel sample 2, and curve 3 is embodiment 2 parallel sample 3.
Detailed description of the invention
The preparation of embodiment 1 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 60% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, HPD100 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 50% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 200g
Carbomer 500g
Lactose 100g
Micropowder silica gel 200g
95% appropriate amount of ethanol
Magnesium stearate 10g
By Fructus Gardeniae total glycosides, carbomer, lactose, micropowder silica gel mixing, cross 80 mesh sieves, add 95% ethanol wet and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 2 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 70% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, XDA-8 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 40% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 500g
Hydroxypropyl methylcellulose 400g
Microcrystalline Cellulose 100g
95% appropriate amount of ethanol
Magnesium stearate 10g
By Fructus Gardeniae total glycosides, hydroxypropyl methylcellulose, microcrystalline Cellulose mixing, cross 80 mesh sieves, add 95% ethanol wet and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 3 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 70% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, XDA-8 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 40% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 200g
Ethyl cellulose 150g
Calcium hydrogen phosphate 50g
Polyethylene Glycol 100g
Starch 400g
Magnesium stearate 50g
Micropowder silica gel 50g
By Fructus Gardeniae total glycosides, ethyl cellulose, calcium hydrogen phosphate, starch mixing, cross 80 mesh sieves, add Polyethylene Glycol moistening and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add micropowder silica gel, magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 4 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 80% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, XDA-8 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 40% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 400g
Stearic acid 200g
Starch 200g
Ethyl cellulose 200g
95% appropriate amount of ethanol
Micropowder silica gel 5g
Pulvis Talci 5g
By Fructus Gardeniae total glycosides, stearic acid, starch mixing, cross 80 mesh sieves, add 95% ethanol, soft material is made in ethyl cellulose moistening, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add micropowder silica gel, Pulvis Talci, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 5 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 60% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, XDA-8 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 30% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 500g
Hydroxypropyl methylcellulose 300g
Microcrystalline Cellulose 200g
95% appropriate amount of ethanol
Magnesium stearate 10g
By Fructus Gardeniae Fructus Gardeniae total glycosides, hydroxypropyl methylcellulose, microcrystalline Cellulose mixing, cross 80 mesh sieves, add 95% ethanol wet and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 6 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 80% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, LS-303 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 50% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 300g
Hexadecylic acid 100g
Carbomer 100g
Calcium sulfate 100g
Calcium hydrogen phosphate 300g
Polyethylene Glycol 50g
Polyvinylpyrrolidone 50g
Magnesium stearate 10g
By Fructus Gardeniae total glycosides, hexadecylic acid, carbomer, calcium sulfate, calcium hydrogen phosphate mixing, cross 80 mesh sieves, add Polyethylene Glycol, soft material is made in polyvinylpyrrolidone moistening, cross 20 mesh sieves and granulate, drying, crosses 18 order granulate, adds magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 7 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 80% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, HPD100 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 50% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 500g
Ethyl cellulose 200g
Calcium hydrogen phosphate 300g
95% appropriate amount of ethanol
Magnesium stearate 10g
By Fructus Gardeniae total glycosides, ethyl cellulose, calcium hydrogen phosphate mixing, cross 80 mesh sieves, add that 95% ethanol is wet makes soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 8 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 70% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, HPD100 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 30% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 700g
Octadecanol 100g
Pregelatinized Starch 200g
95% appropriate amount of ethanol
Magnesium stearate 10g
By Fructus Gardeniae total glycosides, octadecanol, pregelatinized Starch mixing, cross 80 mesh sieves, add 95% ethanol wet and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 9 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 70% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, LS-303 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 30% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 400g
Hydroxypropyl methylcellulose 300g
Microcrystalline Cellulose 250g
Polyethylene Glycol 50g
Magnesium stearate 10g
By Fructus Gardeniae total glycosides, hydroxypropyl methylcellulose, ethyl cellulose, microcrystalline Cellulose mixing, cross 80 mesh sieves, add Polyethylene Glycol moistening and make soft material, cross 20 mesh sieves and granulate, drying, crosses 18 order granulate, adds micropowder silica gel, magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 10 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 60% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, XDA-8 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 40% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 400g
Polyacrylic resin 100g
Ethyl cellulose 150g
Octadecanol 50g
Starch 100g
Dextrin 100g
Microcrystalline Cellulose 50g
Polyethylene Glycol 50g
Micropowder silica gel 10g
By Fructus Gardeniae total glycosides, polyacrylic resin, ethyl cellulose, octadecanol, starch, dextrin, microcrystalline Cellulose mixing, cross 80 mesh sieves, add Polyethylene Glycol moistening and make soft material, cross 20 mesh sieves to granulate, dry, cross 18 order granulate, add micropowder silica gel, magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 11 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 60% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, LS-303 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 40% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 400g
Hydroxypropyl methylcellulose 300g
Ethyl cellulose 150g
95% appropriate amount of ethanol
Micropowder silica gel 150g
Magnesium stearate 15g
By Fructus Gardeniae total glycosides, hydroxypropyl methylcellulose, ethyl cellulose, micropowder silica gel mixing, cross 80 mesh sieves, add 95% ethanol wet and make soft material, cross 20 mesh sieves and granulate, drying, crosses 18 order granulate, adds micropowder silica gel, magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 12 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 80% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, HPD100 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 40% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 400g
Hydroxypropyl methylcellulose 200g
Lactose 100g
Ethyl cellulose 200g
Micropowder silica gel 100g
By Fructus Gardeniae total glycosides, hydroxypropyl methylcellulose, ethyl cellulose, lactose, hexadecanol mixing, cross 80 mesh sieves, add ethyl cellulose moistening and make soft material, cross 20 mesh sieves and granulate, drying, crosses 18 order granulate, adds micropowder silica gel, magnesium stearate, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 13 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 70% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, LS-303 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 50% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 600g
Cellulose acetate 100g
Starch 100g
Lactose 50g
Ethyl cellulose 100g
Micropowder silica gel 50g
By Fructus Gardeniae total glycosides, cellulose acetate, starch, lactose mixing, cross 80 mesh sieves, add ethyl cellulose moistening and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add micropowder silica gel, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
The preparation of embodiment 14 Fructus Gardeniae total glycosides slow releasing tablet
1) Fructus Gardeniae total glycosides extraction and purification process:
Fructus Gardeniae is selected, broken shell, with 7 times amount 70% alcohol reflux 2 times, each 1.5 hours, obtain alcohol extract, reclaim ethanol extremely without alcohol taste, XDA-8 macroporous resin adsorption, with 4 times amount washing removing impurity, use 4 times amount 50% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) Fructus Gardeniae total glycosides sustained-release tablet preparation technique:
Fructus Gardeniae total glycosides 400g
Sodium carboxymethyl cellulose 100g
Hyprolose 200g
Micropowder silica gel 100g
Starch 50g
95% appropriate amount of ethanol
Polyethylene Glycol 50g
Pulvis Talci 15g
By Fructus Gardeniae total glycosides, sodium carboxymethyl cellulose, hydroxy propyl cellulose, micropowder silica gel, starch mixing, cross 80 mesh sieves, add 95% ethanol, soft material is made in Polyethylene Glycol moistening, cross 20 mesh sieves and granulate, drying, crosses 18 order granulate, adds Pulvis Talci, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
Embodiment 15 Fructus Gardeniae total glycosides slow releasing tablet In Vitro Dissolution is tested
Adopt " Chinese Pharmacopoeia " version in 2010 two drug release determination methods (annex XD first method) Rotating shaker, rotating speed 100rmin
-1, dissolution medium is degassed water 900mL, leaching temperature 37.0 DEG C ± 0.5 DEG C.Get Fructus Gardeniae total glycosides slow releasing tablet 7, throw respectively and turn in basket in 7, turn timing basket enters stripping rotor from what be equipped with tablet, 1,2,4,6,8,10,12h gets solution 5mL respectively, supplement the water of identical temperature volume, institute's solution of getting 0.45 μm of filtering with microporous membrane, gets the mass concentration that subsequent filtrate measures Fructus Gardeniae total glycosides simultaneously, according to standard curve and Accumulation dissolution computing formula, try to achieve the preparation of each time point.
Cn is the mass concentration of the n-th time point dissolution medium Chinese medicine, and Ci is the mass concentration of (n-1)th time point dissolution medium Chinese medicine, and Vi is sample volume, and V is the cumulative volume of dissolution medium, and W is the quality of slow releasing tablet, and D is the mass fraction of slow releasing tablet Chinese medicine.
Fructus Gardeniae total glycosides slow releasing tablet different time vitro cumulative stripping value prepared by embodiment 2,5,7,9,11,12 is in table 1:
Table 1 different embodiment gained Fructus Gardeniae total glycosides Dissolution of Sustained Release Tablet degree measurement result (different time vitro cumulative stripping value, %)
。
Claims (10)
1. a Fructus Gardeniae total glycosides slow releasing tablet, is characterized in that, it is composed of the following components:
A, Fructus Gardeniae total glycosides 19.8% ~ 69.3%(weight)
B, slow-release material 9.9% ~ 59.4%(weight)
C, pharmaceutic adjuvant 6.0% ~ 60.4%(weight)
Wherein, described slow-release material is one or more in hydroxypropyl methylcellulose, sodium carboxymethyl cellulose, hyprolose, ethyl cellulose, carbomer, stearic acid, hexadecanol, octadecanol, polyacrylic resin, cellulose acetate, and pharmaceutic adjuvant comprises one or more in filler, lubricant, binding agent.
2. Fructus Gardeniae total glycosides slow releasing tablet as claimed in claim 1, it is characterized in that, by weight percentage, Fructus Gardeniae total glycosides accounts for 30%-50%, and slow-release material accounts for 20%-40%, and pharmaceutic adjuvant accounts for 10%-50%.
3. Fructus Gardeniae total glycosides slow releasing tablet as claimed in claim 1, it is characterized in that, described Fructus Gardeniae total glycosides with determined by ultraviolet spectrophotometry, and is no less than 70%(weight in jasminoidin content), in Fructus Gardeniae total glycosides, the weight ratio of genipin-1-β-D-gentiobioside with cape jasmine and jasminoidin is 1 ~ 2:10.
4. Fructus Gardeniae total glycosides slow releasing tablet as claimed in claim 1, it is characterized in that, described slow-release material is one or more in hydroxypropyl methylcellulose, ethyl cellulose, carbomer.
5. the Fructus Gardeniae total glycosides slow releasing tablet according to any one of Claims 1-4, is characterized in that, described filler is one or more in microcrystalline Cellulose, pregelatinized Starch, micropowder silica gel, lactose, starch, dextrin, calcium hydrogen phosphate, calcium sulfate.
6. the Fructus Gardeniae total glycosides slow releasing tablet according to any one of Claims 1-4, is characterized in that, described lubricant is one or more in Pulvis Talci, magnesium stearate and micropowder silica gel.
7. the Fructus Gardeniae total glycosides slow releasing tablet any one of claim according to any one of 1 to 4, is characterized in that, described binding agent is one or more in 95% ethanol, Polyethylene Glycol, polyvinylpyrrolidone, ethyl cellulose.
8. the preparation method of the Fructus Gardeniae total glycosides slow releasing tablet according to any one of claim 1 ~ 7, is characterized in that comprising the following steps:
1) extraction process:
Fructus Gardeniae is selected, and broken shell, with 7 times amount 60% ~ 80% alcohol reflux 2 times, each 1.5 hours, obtains alcohol extract, reclaim ethanol extremely without alcohol taste, macroporous resin adsorption, with 4 times amount washings, removing impurity, use 4 times amount 30% ~ 50% ethanol elutions again, collect Fructus Gardeniae total glycosides, concentrated, dry;
2) preparation process:
By Fructus Gardeniae total glycosides, slow-release material, filler mixing, cross 80 mesh sieves, add binding agent moistening and make soft material, cross 20 mesh sieves and granulate, dry, cross 18 order granulate, add lubricant, mixing, tabletted, obtains Fructus Gardeniae total glycosides slow releasing tablet.
9. method according to claim 8, is characterized in that, described in step 1), the concentration of reflux, extract, ethanol is 70%, and the concentration of eluting ethanol is 40%.
10. method according to claim 8, is characterized in that, the model of macroporous resin described in step 1) is HPD100, LS-303 or XDA-8.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113181202A (en) * | 2021-03-24 | 2021-07-30 | 上海中医药大学附属曙光医院 | Application of iridoid glycoside compound in preparing medicine for treating diseases related to DUSP9 abnormal expression |
| CN113293379A (en) * | 2021-05-10 | 2021-08-24 | 重庆大学 | Yellow gardenia fruit extract corrosion inhibitor and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101066311A (en) * | 2007-06-07 | 2007-11-07 | 北京本草天源药物研究院 | Total jasminoidin extract and its prepn process |
| CN101756924A (en) * | 2008-12-24 | 2010-06-30 | 鲁南制药集团股份有限公司 | Sustained-release tablets of faropenem sodium |
-
2013
- 2013-11-25 CN CN201310597311.6A patent/CN104644809A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101066311A (en) * | 2007-06-07 | 2007-11-07 | 北京本草天源药物研究院 | Total jasminoidin extract and its prepn process |
| CN101756924A (en) * | 2008-12-24 | 2010-06-30 | 鲁南制药集团股份有限公司 | Sustained-release tablets of faropenem sodium |
Non-Patent Citations (1)
| Title |
|---|
| 胡志方等: "《药剂学》", 30 July 2007, 西北工业大学出版社 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113181202A (en) * | 2021-03-24 | 2021-07-30 | 上海中医药大学附属曙光医院 | Application of iridoid glycoside compound in preparing medicine for treating diseases related to DUSP9 abnormal expression |
| CN113293379A (en) * | 2021-05-10 | 2021-08-24 | 重庆大学 | Yellow gardenia fruit extract corrosion inhibitor and application thereof |
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