CN1810278A - Enteric coated Chinese medicine composition for treating cervical and lumbar spondylopathy - Google Patents

Enteric coated Chinese medicine composition for treating cervical and lumbar spondylopathy Download PDF

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CN1810278A
CN1810278A CN 200510005001 CN200510005001A CN1810278A CN 1810278 A CN1810278 A CN 1810278A CN 200510005001 CN200510005001 CN 200510005001 CN 200510005001 A CN200510005001 A CN 200510005001A CN 1810278 A CN1810278 A CN 1810278A
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enteric
coating compositions
chinese medicine
enteric coating
radix
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CN100398122C (en
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杨晓穗
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Jianchangbang Pharmacy Co ltd
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BEIJING BEIDA PHARMACEUTICAL INDUSTRY Co Ltd
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Abstract

The present invention belongs to the field of coated composition technology, and is especially enteric coated Chinese medicine composition for treating wind-cold-damp arthralgia. The enteric coated composition is either water dispersed preparation comprising enteric soluble release-controlling agent, plasticizer, surfactant and water, or organic solution comprising enteric soluble release-controlling agent and organic solvent. The enteric coated composition has less adverse gastrointestinal tract reaction and obviously raised curative effect.

Description

A kind of enteric coating compositions for the treatment of neck, lumbar spondylosis Chinese medicine
Technical field
The present invention relates to a kind of Chinese medicine coated composition, more particularly, the present invention relates to a kind of Chinese medicine enteric coating compositions that can reduce the gastrointestinal tract pessimal stimulation and increase treatment neck, lumbar spondylosis curative effect.
Background technology
Neck, lumbar spondylosis are orthopaedics commonly encountered diseases, frequently-occurring disease.Neck, lumbar spondylosis pathogenic factor belong to the arthromyodynia category due to motherland's medical science more except that wound." element is asked.The numbness opinion ": " wind, cold, wet three gas are assorted extremely, close and be numbness also.Its migratory BI-syndrome caused mainly by pathogenic wind; BI-syndrome caused mainly by pathogenic cold being called painful BI; The dampness victor is an arthralgia caused mainly by damp." have again: " and numbness is that bone is then heavy, be arteries and veins then blood clotting do not dredge, be that muscle is then bent not stretch, be that meat is then meciless, be Pi Zehan.”
Motherland's medical science think cold being a kind of YIN pathogen, its property spasm, cold go into through and check late, tears are and not all right, so the cold coagulation QI and blood is bitterly even there is the place of deciding.Damp being a kind of YIN pathogen, the deep viscous of its property." to total record of helping " cloud: heavy, numb, unable its characteristics that are are not moved, are stranded to " water-damp from the earth is contained the flesh tendon that then victimizes, and lid wet soil soil nature is slow, and the gas of Rong Wei all stays with wet, so wet contain then work and do not move yet " its clinical sign with the limb pain work.So the above-mentioned disease that causes because of arthralgia due to wind-cold dampness has more existing neck, shoulder, arm, pain in the lumbar region pain clinically, numbness, symptom such as unable.The Chinese medicine of neck, lumbar spondylosis is that method with wind-expelling pain-stopping, nourshing blood and promoting blood circulation reaches and removes or alleviate each symptom in the above-mentioned disease due to the treatment arthralgia due to wind-cold dampness.
Doctor trained in Western medicine expectant treatment curative effect is limited, and the treatment that undergos surgery has a big risk, and sufferer is painful big, and the doctor trained in Western medicine operative therapy only removes compressing, the factor of blocking-up damage, and can not prevent secondary injury and repair damaged portion.Thereby, the domestic Chinese medicines that adopt more.
The Chinese medicine made from Herba Lycopodii, Myrrha, Radix Dipsaci, Radix Puerariae, Olibanum, Rhizoma Cibotii, Radix Achyranthis Bidentatae, Flos Carthami, the Radix Paeoniae Alba, Semen Persicae, Radix Rehmanniae, Radix Glycyrrhizae have invigorate blood circulation, collateral dredging, analgesic effect, can be used for neck due to the wind-cold channel blocking network, lumbar spondylosis, disease and see shoulder neck pain, limitation of activity and numb limbs and tense tendons etc.With the Radix Paeoniae Alba, Radix Puerariae is monarch drug, and Radix Paeoniae Alba acid is cool and soften, the gentle muscle that nourishes blood, the sweet suffering of Radix Puerariae and rising is sent out, deliver loose evil, expelling pathogenic factors from muscles pain relieving etc., one keeps one, one gentle one separates, the collaborative effect of bringing into play the wind-expelling pain-stopping nourshing blood and promoting blood circulation.The drug action of above Chinese medicine preparation has obtained zoopery to be proved: can significantly improve mice to the toleration of hot pain and the reaction times in the minimizing writhing test, and can suppress swelling of rat toes and mice ear degree significantly, compared significant analgesia role and antiinflammatory action with positive control.
Existing granule of the preparation of above on the market Chinese prescription preparation and tablet are sold.But because this medicine has stimulation to stomach, prepared tablet is in the stomach disintegrate, and granule disperses at stomach become suspension in water after, all can stimulate patient's gastrointestinal tract to produce untoward reaction.After some patients take commercially available tablet and granule, have a stomachache, feel sick, gastrointestinal side effect such as nausea, vomiting, influenced compliance of patients and treatment of diseases; Because the untoward reaction of this Chinese medicine has also limited the patient who suffers from gastric ulcer, acute gastritis, gastrorrhagia simultaneously and has taken the crowd that having reduced takes medicine just controls.
Summary of the invention
The present invention stimulates the problem of stomach in order to solve above-mentioned Chinese medicine, has developed the enteric coating compositions of suitable this medicine, uses said composition that this Chinese medicine is carried out coating, has solved problems such as gastrointestinal side effect.
The enteric coating compositions of treatment neck of the present invention, lumbar spondylosis Chinese medicine is made by the component of following weight percentage ratio: enteric controlled-release agent 0.5-45%, lubricant 0-10%, plasticizer 0-10%, surfactant 0-1%, solvent 50-95%;
Described enteric controlled-release agent is Lac, methacrylic acid copolymer, cellulose acetate benzene three esters, hypromellose phthalate ester, cellulose acetate phthalate ester or polyvinyl alcohol phthalate ester, described lubricant is Pulvis Talci, magnesium stearate, calcium stearate, stearic acid sucrose ester or silicon dioxide, described plasticizer is triethyl citrate, Polyethylene Glycol, glycerol, propylene glycol or Oleum Ricini, described surfactant is tween, span or sodium lauryl sulphate, and described solvent is ammonia, ethanol, acetone or the ether of water, 30wt%.
The molecular weight of described methacrylic acid copolymer is 50000-500000.
Described solution is made by methacrylic resin copolymer 30wt%, Tween 80 1wt%, triethyl citrate 10wt%, Pulvis Talci 5.5wt% and water 53.5wt%.
Described solution is made by hypromellose phthalate ester 6wt%, acetone 75.2wt%, ethanol 18.8wt%.
Described solution is made by 95% ethanol of Lac 18.7wt%, Tween 80 1wt%, triethyl citrate 1wt%, Oleum Ricini 1wt%, surplus.
Described solution is made by cellulose acetate phthalate ester 30wt%, water 63.3wt%, triethyl citrate 2.3wt%, 30wt% ammonia 4.4wt%.
The Chinese medicine of described treatment arthralgia due to wind-cold dampness is preferably made by the Chinese crude drug of following weight parts: Herba Lycopodii 70-85, Myrrha 40-60, Radix Dipsaci 70-85, Radix Puerariae 45-60, Olibanum 40-60, Rhizoma Cibotii 70-90, Radix Achyranthis Bidentatae 45-60, Flos Carthami 45-60, Radix Paeoniae Alba 190-220, Semen Persicae 45-60, Radix Rehmanniae 45-60, Radix Glycyrrhizae 20-30.
The consumption of enteric coating compositions of the present invention is 2-24mg/cm 2If enteric coating compositions of the present invention contains methacrylic acid copolymer, contain the methacrylic acid copolymer of 1-15mg in the enteric-coated composition on unit square centimetre surface.
The inventor investigates coatings to acidproof effect in the simulated gastric fluid and the stripping situation in simulated intestinal fluid by external acid-resistant strength test and dissolution in vitro test; And by the curative effect after the zoopery checking coating.As expected, enteric-coated composition of the present invention discharges less than 10 in simulated gastric fluid, and in the release in simulated intestinal fluid 60 minutes greater than more than 80 percent.
The function of this medicine is for " to invigorate blood circulation collateral dredging, pain relieving."; be that method with nourshing blood and promoting blood circulation reaches collateral dredging and separates the symptom that neck, lumbar spondylosis were removed or alleviated to the stasis of blood, wind-expelling pain-stopping; cervical spondylosis and blood stasis are closely related; the blood stasis of the traditional Chinese medical science; with aspects such as the character of blood, resistance of blood flow, blood flow, blood capillary blood flows confidential relation is arranged in general; therefore, study with dog vertebral artery blood flow detection method, enteric-coated composition more of the present invention and commercially available pain are put down particulate effect.
The animal pharmacodynamics experiment showed, that the present invention passes through prepared Chinese medicine preparation not only directly to have reduced the bad gastrointestinal reaction of medicine, and can significantly improve the curative effect of product with enteric coatings.May be because: enteric coatings has prevented the destruction of some destructive factor of the strong acidic condition of stomach or stomach to a kind of or some active ingredient of this Chinese medicine.Yet the analysis of mechanism and reason also needs the further checking of test.
Used the dependent enteric material of some pH among the present invention, can realize suitability for industrialized production by ordinary coating pot and fluidized bed coating equipment.The enteric controlled-release agent is mixed with the composition that comprises lubricant, plasticizer and surfactant, be mixed into aqueous dispersion with water then, perhaps the enteric controlled-release agent is dissolved in the organic solvent that comprises ethanol or acetone, obtain organic solution.Use conventional method that the aqueous dispersion that obtains or organic solution coating is promptly passable to the Chinese medicine preparation then, concrete grammar can be referring to the embodiment part.
The specific embodiment
The present invention will be described below in conjunction with embodiment, but be not limited to following examples.
Embodiment 1
1. the preparation of methacrylic acid copolymer enteric coatel tablets
(1) preparation of treatment neck, lumbar spondylosis Chinese medicine
Prepare following Chinese crude drug: Herba Lycopodii 80g, Myrrha 53g, Radix Dipsaci 80g, Radix Puerariae 53g, Olibanum 53g, Rhizoma Cibotii 80g, Radix Achyranthis Bidentatae 53g, Flos Carthami 53g, Radix Paeoniae Alba 213g, Semen Persicae 53g, Radix Rehmanniae 53g, Radix Glycyrrhizae 26.5g;
In above-mentioned 12 flavor medical materials, get Radix Paeoniae Alba 168g, grind and be fine powder, the residue Radix Paeoniae Alba and all the other ten decoct with water twice simply, 1.5 hours for the first time, 1 hour for the second time, merging filtrate, filter, filtrate decompression is concentrated into the extractum that relative density is 1.1-1.2 (50 ℃), with above-mentioned fine powder mixing, is dried to dried cream, pulverize, obtain the Chinese medicine that tabletting is used.
(2) preparation of the Chinese medicine tablet heart
Use Chinese medicine 300g, the lactose 80g, microcrystalline Cellulose 55g, polyvinylpolypyrrolidone 10g, polyvidone 5g, magnesium stearate 2g and the suitable quantity of water that obtain in the step (1) to make 1000 the Chinese medicine tablet heart.
The preparation method of the sheet heart:
The Chinese medicine that obtains in the step (1) and other sheet heart compositions that remove magnesium stearate are fully mixed; Add entry and make soft material, be stirred to gently the group of being pressed into while preparing and touch that promptly to open be degree; Crossing 18 mesh sieves granulates; Granule is 60 ℃ drying in oven; Dried granule is with 20 mesh sieve granulate; Weigh calculated yield; Add magnesium stearate, mix homogeneously in the prescription ratio; The stamping of 12mm scrobicula.
(3) preparation of coating solution
Methacrylic resin copolymer Eudragit L100,10g Tween 80,100g triethyl citrate, 55g Pulvis Talci and the 535g water that uses 300g Germany Degussa company to produce is made the coating solution of 1000g.
The preparation method of coating solution: Eudragit L 100 is pulverized, cross 100 mesh sieves; Add Tween 80 to triethyl citrate, mix homogeneously gets mixture 1; After Eudragit L 100 and mixture 1 mixing, add entry and mix, obtain required coating solution.
(4) coating
Label is put into coating pan rotate, blowing hot-air, preheating label; Start air pump, regulate the spraying stream pressure; With spray gun roll unilateral spray coating solution; The control coating weightening finish while spraying; After having sprayed, 50 ℃ of dryings 6 hours.
2. external acid-resistant strength and dissolution experiment
Investigate the coating weightening finish respectively and be 1.10mg/cm 2, 8.44mg/cm 2, 14.22mg/cm 2The acid-resistant strength and the dissolution of coated tablet.According to Chinese Pharmacopoeia second method, rotating speed 50rpm, dissolution medium is the hydrochloric acid of pH1.2, is determined at the dissolution in this medium, the results are shown in Table 1.
The investigation (%) of table 1 acid-resistant strength in the hydrochloric acid of pH1.2
time(min) pH 1.10mg/cm 2 8.44mg/cm 2 15.22mg/cm 2
5 1.2 0.21 0.15 0.16
15 1.2 0.26 0.44 0.26
30 1.2 0.71 1.04 0.38
60 1.2 4.43 1.55 0.84
90 1.2 8.78 2.75 1.7
120 1.2 9.13 6.45 4.03
As can be seen from Table 1: 120 minutes drug releases increase with coatings thickness less than 10, and release is slowed down.
Table 2 coating thickness 1.10mg/cm 2Coated tablet pH6.8's
Dissolution in the hydrochloric acid medium (in white peony root's total glycoside)
∑ Q(％) 1 2 3 4 5 6 Meansigma methods SD(％)
0 0.0 0.0 0.0 0.0 0.0 0.0 0.0 0.0
5 81.7 87.6 81.8 83.7 85.6 87.3 84.6 2.6
10 86.8 88.1 89.3 86.5 89.3 90.6 88.4 1.6
20 87.5 87.9 91.0 87.6 90.4 90.6 89.2 1.6
30 86.2 87.4 91.7 88.0 89.7 89.8 88.8 2.0
45 87.0 87.4 91.4 87.5 89.7 89.9 88.8 1.8
60 87.5 88.9 92.0 86.4 90.4 91.0 89.4 2.2
Table 3 coating thickness 8.44mg/cm 2Coated tablet pH6.8's
Dissolution in the hydrochloric acid medium (in white peony root's total glycoside)
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0.0 0.0 0.0 0.0 0.0 0.0 0.0 0.0
5 75.8 72.3 77.5 71.6 74.4 72.9 74.1 2.2
10 89.5 88.8 93.2 88.3 91.2 89.1 90.0 1.8
20 93.6 94.9 96.6 93.5 95.8 95.3 95.0 1.2
30 93.3 95.0 96.3 93.9 96.9 95.4 95.1 1.4
45 93.0 94.2 96.8 93.2 96.8 94.1 94.7 1.7
60.0 92.2 93.8 96.2 92.0 96.9 94.7 94.3 2.0
Table 4 coating thickness 14.22mg/cm 2Coated tablet pH6.8's
Dissolution in the hydrochloric acid medium (in white peony root's total glycoside)
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 68.4 70.0 71.2 71.1 68.8 70.4 70.0 1.2
10 88.5 89.6 92.0 88.0 88.7 91.5 89.7 1.7
20 94.4 94.7 99.7 94.2 96.1 98.6 96.3 2.3
30 95.4 95.1 99.0 94.1 97.1 100.7 96.9 2.5
45 94.5 94.4 100.5 95.3 96.1 100.3 96.9 2.8
60 94.9 94.6 99.2 94.7 95.8 100.1 96.6 2.4
Conclusion: above methacrylic resin material X enteric coatel tablets are from the increase along with coating thickness, and the 30min dissolution reduces but still is higher than 80%.
Embodiment 2
1. the preparation of hypromellose phthalate ester enteric coated particles
(1) preparation of treatment neck, lumbar spondylosis Chinese medicine
Prepare following Chinese crude drug: Herba Lycopodii 75g, Myrrha 50g, Radix Dipsaci 75g, Radix Puerariae 50g, Olibanum 50g, Rhizoma Cibotii 75g, Radix Achyranthis Bidentatae 50g, Flos Carthami 50g, Radix Paeoniae Alba 200g, Semen Persicae 50g, Radix Rehmanniae 50g, Radix Glycyrrhizae 25g;
To decoct with water three times in the above-mentioned 12 flavor raw materials, 1.5 hours for the first time, second, third time each hour filtered, merging filtrate, and being evaporated to relative density is the clear paste of 1.30-1.45 (50 ℃ of surveys), obtains Chinese medicine.
(2) particulate preparation
Chinese medicine 300g, lactose 500g, sucrose 550g, Fructus Citri sinensis powdered flavor 10g, hypromellose RT-15100g, the suitable quantity of water of using step (1) to obtain are made 1000 bags
Particulate preparation method:
Chinese medicine and other adjunct ingredients that step (1) is obtained fully mix with quick mixer granulator; Add entry system soft material, the limit adds the waterside and is stirred in right amount; Crossing 24 mesh sieves granulates; Granule is 60 ℃ of oven dry; Dried granule is with 20 mesh sieve granulate; Weigh calculated yield.
(3) preparation of coating solution
Use hypromellose phthalate ester 60g, acetone 752g, ethanol 188g to make the 1000g coating solution.
The compound method of coating solution:
Ethanol and acetone are miscible in the prescription ratio; Adding hypromellose phthalate ester is mixed with 6% coating solution in ethanol and acetone soln.
(4) coating
Granule is put into top spray fluid bed, control whiff pressure, air blast frequency, outlet temperature; Start constant flow pump, regulate constant flow pump speed; Fluidized bed coating; The weightening finish of control coating.
2. external acid-resistant strength and dissolution test
Be 2.20mg/cm to coating thickness respectively 2, 13.25mg/cm 2, 24.45mg/cm 2Granule investigate its acid-resistant strength and dissolution.
The investigation of table 5 acid-resistant strength in the simulated gastric fluid of pH1.2
time(min) pH 2.20mg/cm 2 13.25mg/cm 2 24.45mg/cm 2
5 1.2 0.17 0.16 0.21
15 1.2 0.25 0.25 0.5
30 1.2 0.71 0.31 0.6
60 1.2 4.83 0.86 0.77
90 1.2 8.38 1.49 0.87
120 1.2 8.63 3.17 1.15
Table 6 coating thickness 2.20mg/cm 2Coated granule dissolution in the hydrochloric acid medium of pH6.8
∑ Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 88.7 83.4 86.5 87.9 81.8 88.3 86.1 2.9
10 89.4 90.3 93.2 94.9 92.1 92.1 92.0 2.0
20 91.0 91.6 94.3 94.0 92.7 92.6 92.7 1.3
30 89.7 93.1 93.6 94.3 92.7 92.4 92.6 1.6
45 90.3 92.1 93.9 94.8 94.5 93.0 93.1 1.7
60 89.7 92.1 93.6 93.9 94.1 91.6 92.5 1.7
Table 7 coating thickness 13.25mg/cm 2Coated granule dissolution in the hydrochloric acid medium of pH6.8
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 78.0 78.8 81.6 83.2 78.4 80.5 80.1 2.0
10 91.0 91.4 91.6 93.9 95.2 92.3 92.6 1.6
20 93.1 93.1 93.8 94.3 98.8 95.0 94.7 2.2
30 94.7 93.6 93.7 94.8 99.9 95.4 95.3 2.3
45 94.0 93.8 93.2 94.6 99.7 95.4 95.1 2.4
60.0 93.9 92.9 93.3 95.6 98.7 94.7 94.9 2.1
Table 8 coating thickness 13.25mg/cm 2Coated granule dissolution in the hydrochloric acid medium of pH6.8
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 68.7 73.1 71.0 68.6 73.6 76.0 71.8 2.9
10 90.7 91.4 89.7 88.1 93.2 92.9 91.0 1.9
20 98.9 96.2 98.1 95.5 99.9 96.7 97.6 1.7
30 100.0 95.9 97.6 97.2 100.1 97.2 98.0 1.7
45 98.9 96.1 97.8 97.6 100.3 96.8 97.9 1.5
60 100.7 96.3 98.6 96.3 100.5 95.8 98.0 2.2
Embodiment 3
1. the preparation of Lac coating Chinese medicine enteric-coated pellet capsule
(1) preparation of treatment neck, lumbar spondylosis Chinese medicine
Identical with embodiment 1.
(2) preparation of the ball heart
Use Chinese medicine 300g, microcrystalline Cellulose 150g, lactose 50g to make 1000 capsules.
Adopt medicine to mix, add water and make soft material in right amount, be extruded into the suitable strip of diameter through extruding sieve plate (1mm) with adjuvant.Advance spheronizator and make granule round as a ball fully,, get 18～24 purpose micropills and carry out coating in 60 degrees centigrade of oven dry.
(3) preparation of coating solution
Use Lac 375g, Tween 80 20g, triethyl citrate 20g, Oleum Ricini 20ml, 95% an amount of ethanol to make the 2000ml coating solution.
(4) coating
Adopt the fluidized-bed coating machine coating.It is an amount of to take by weighing pill, puts in the air-flow coating device, has the agent solvent solution enteric coated with Lac, 40 ℃ of dry 2h.Coating thickness is to contain the pill core weightening finish.Art for coating condition: blower frequency: 27.5HZ; Whiff pressure: 0.2MPa, hydrojet flow velocity: 1mL/min, stream temperature: 33 ℃.
(5) encapsulated
Encapsulated by specification, every 0.5g.
2. external acid-resistant strength and dissolution test
Investigate the coating weightening finish respectively and be 0.55mg/cm 2, 4.44mg/cm 2, 7.89mg/cm 2Enteric-coated pellet capsule in the hydrochloric acid of pH1.2 acid-resistant strength and in the simulated intestinal fluid medium dissolution.
The acid-resistant strength examination of table 9 in the hydrochloric acid of pH1.2
time(min) pH 0.55mg/cm 2 4.44mg/cm 2 7.89mg/cm 2
5 1.2 0.11 0.03 0.4
15 1.2 0.23 0.27 0.49
30 1.2 0.77 0.39 0.62
60 1.2 4.36 0.88 0.7
90 1.2 8.15 1.72 0.81
120 1.2 9.62 4.01 0.99
Table 10 coating thickness 0.55mg/cm 2Capsule dissolution in the simulated intestinal fluid medium
∑ Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 77.7 81.2 76.9 77.6 76.5 82.8 78.8 2.6
10 88.3 85.2 84.6 88.4 89.6 86.2 87.0 2.0
20 89.4 85.2 85.2 89.3 92.1 85.4 87.8 2.9
30 89.6 86.8 85.6 90.2 92.0 86.4 88.5 2.5
45 89.4 86.2 85.5 90.5 90.2 86.7 88.1 2.2
60 89.3 86.9 85.2 89.9 91.3 85.2 87.9 2.6
Table 11 coating thickness 4.44mg/cm 2Capsule dissolution in the simulated intestinal fluid medium
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 77.2 76.1 74.3 78.2 75.7 77.6 76.5 1.4
10 92.9 91.9 89.1 92.4 90.0 90.9 91.2 1.5
20 96.3 94.1 90.4 96.3 92.0 92.4 93.6 2.4
30 95.2 93.7 90.3 93.9 90.9 91.5 92.6 2.0
45 94.8 92.2 89.7 93.7 89.3 89.7 91.6 2.3
60 92.8 91.5 88.8 92.7 88.1 88.8 90.4 2.1
Table 12 coating thickness 7.89mg/cm 2Capsule dissolution in the hydrochloric acid medium of pH6.8
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 67.1 64.3 67.3 62.8 63.3 68.0 65.5 2.3
10 89.2 84.8 87.0 84.6 84.7 88.7 86.5 2.1
20 99.5 94.0 94.3 95.7 95.5 97.7 96.1 2.1
30 99.4 95.5 95.2 95.5 95.3 98.6 96.6 1.9
45 100.5 96.1 94.4 96.0 96.0 97.8 96.8 2.1
60 100.3 95.2 95.8 95.9 96.9 98.5 97.1 2.0
Embodiment 4
1. the preparation of cellulose acetate phthalate ester X multiple-unit enteric coatel tablets
The multiple-unit enteric coatel tablets are a kind of novel enteric coated preparation, and are different with the casing sheet of routine, and the coatings of multiple-unit enteric coatel tablets obtains enteric coatel tablets being wrapped in the tabletting particle surface behind the granule tabletting.Its advantage is, slice, thin piece is broken into two with one's hands to take still has the enteric effect, therefore, and more stable quality.
(1) preparation of treatment neck, lumbar spondylosis Chinese medicine
Identical with embodiment 2.
(2) particulate preparation
Use 300g Chinese medicine, 40g lactose, 55g microcrystalline Cellulose, 10g polyvinylpolypyrrolidone XL-10,5g polyvidone, 2g magnesium stearate, suitable quantity of water to make 1000 granules.
Particulate preparation: Chinese medicine ingredients and other the label composition that removes magnesium stearate are fully mixed; Dry method is pressed large stretch of, Hardness Control 40N-60N; Crossing 24 mesh sieves granulates; Weigh calculated yield.
(3) preparation of coating solution
Use 300g cellulose acetate phthalate ester, 800g water, 23g triethyl citrate, 44g 30% ammonia to make the 1000g coating solution.
The preparation of coating solution: the cellulose acetate phthalate ester is pulverized, crossed 100 mesh sieves; Add the Tween 80 of recipe quantity to the triethyl citrate of recipe quantity, mix homogeneously, mixture 1; After cellulose acetate phthalate ester and mixture 1 mixing, add the prescription water gaging and mix, obtain required coating solution.
(4) granule coating
Granule is put into coating pan rotate, blowing hot-air, preheating label; Start air pump, regulate the spraying stream pressure; With spray gun roll unilateral spray coating solution; The control coating weightening finish while spraying; After having sprayed, 50 ℃ of dryings 6 hours.
(5) granule tabletting
Prepare, clean tablet machine; Adjustment sheet weight sheet hardness; Electronic tabletting.
2. external acid-resistant strength and dissolution test
Respectively the coating weightening finish is 2.35mg/cm 2, 10.67mg/cm 2, 19.97mg/cm 2Label investigate its acid-resistant strength and dissolution.
The investigation of table 13 acid-resistant strength in the hydrochloric acid of pH1.2
time(min) pH 2.35mg/cm 2 10.67mg/cm 2 19.97mg/cm 2
5 1.2 0.26 0.18 0.42
15 1.2 0.24 0.26 0.47
30 1.2 0.69 0.32 0.64
60 1.2 3.41 0.89 0.72
90 1.2 7.73 1.67 0.81
120 1.2 8.48 4.96 1.01
Table 14 coating thickness 2.35mg/cm 2Granule dissolution in the hydrochloric acid medium of pH6.8
∑ Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 81.5 79.2 78.5 83.2 78.2 82.5 80.5 2.2
10 92.2 92.1 88.7 89.9 90.4 94.6 91.3 2.1
20 94.2 93.8 91.2 92.0 93.6 95.8 93.4 1.6
30 94.7 93.0 91.1 91.2 93.0 95.4 93.1 1.8
45 94.7 93.6 90.9 90.6 93.2 95.5 93.1 2.0
60 94.2 94.0 90.5 91.1 93.4 95.7 93.2 2.0
Table 15 coating thickness 10.67mg/cm 2Granule dissolution in the hydrochloric acid medium of pH6.8
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD (％)
0 0 0 0 0 0 0 0 0
5 73.9 75.3 76.1 74.2 72.9 75.0 74.6 1.1
10 90.7 90.6 91.1 90.2 92.1 88.5 90.5 1.2
20 95.6 95.2 92.8 94.4 98.4 92.4 94.8 2.2
30 96.3 95.3 94.3 93.7 98.2 93.0 95.1 1.9
45 95.9 95.1 93.5 94.0 98.0 91.3 94.6 2.3
60 96.6 96.1 92.6 94.4 98.2 91.7 94.9 2.5
Table 16 coating thickness 19.97mg/cm 2Granule dissolution in the hydrochloric acid medium of pH6.8
∑Q(％) 1 2 3 4 5 6 Meansigma methods SD(％)
0 0 0 0 0 0 0 0 0
5 62.8 66.8 67.9 66.5 64.5 65.7 65.7 1.8
10 85.7 87.7 91.2 86.8 87.8 86.2 87.6 2.0
20 96.2 96.2 100.5 97.2 98.4 94.5 97.2 2.1
30 98.4 97.5 100.2 97.2 98.8 96.3 98.1 1.4
45 97.2 97.1 100.2 97.3 99.2 94.7 97.6 1.9
60 97.7 97.2 102.2 96.4 99.2 94.9 97.9 2.5
Embodiment 5
Present embodiment carries out the enteric coated preparation pharmacodynamics by the different dosing group to the effect of dog vertebral artery blood flow and investigates.
Get 30 of dogs, male and female have concurrently, and body weight 10～15kg is divided into 6 groups, 5 every group, give normal saline, the root flat granule of pain and four kinds of self-controls respectively and treat neck, lumbar spondylosis Chinese medicine enteric coated preparation.After Animal Anesthesia, operation separates the outer branch of common carotid artery cranium, and ligation, only keeps internal carotid artery, is connected in the MFV-1200 effusion meter, stablizes 30 minutes, measures blood flow respectively before administration He after the administration.
The normal saline experimental group is taken normal saline 6ml, and the enteric coated preparation experimental group of root flat granule experimental group of pain and invention is respectively taken 0.21g crude drug amount by every kg dog and calculated administration, the results are shown in Table 17.
Table 17 normal saline, the root flat granule of pain and enteric coated preparation are to increasing the comparison of dog blood flow
N=5, (x on average ± s)
Blood flow recruitment ml/min0 after the administration
Time (min) Normal saline The flat granule of root pain Methacrylic resin coating enteric coatel tablets Hypromellose phthalate ester coating enteric coated particles Lac coating enteric-coated pellet capsule Cellulose acetate phthalate ester coating multiple-unit enteric coatel tablets
Before the administration 23.6±7.1 36.1±14.3 25.3±5.5 24.1±5.6 32.1±14.8 26.2±12.5
5min 1.3±2.4 2.7±9.0 / / / /
10min 1.0±1.2 14.1±5.7 / / / /
15min / / 1.6±5.7 1.1±7.0 2.6±9.6 1.7±5.4
20min 4.3±2.8 18.7±8.3 / / / /
30min 2.8±2.3 17.0±6.1 2.9±4.4 2.8±6.3 4.8±8.8 3.7±8.3
60min 3.6±2.7 10.0±7.7 16.7±10.8 15.9±8.5 13.1±8.1 16.1±10.8
90min / / 26.0±6.2 26.7±9.7 21.6±8.3 24.6±5.3
120min / / 25.2±5.1 24.8±9.8 31.2±9.1 27.1±7.3
180min / / 23.4±7.8 27.5±7.7 28.3±5.9 22.1±5.2
240min / / 13.1±6.8 14.6±7.3 12.2±4.9 14.7±8.4
Can obtain to draw a conclusion from table 17:
1 methacrylic resin coating enteric coatel tablets begin blood flow increasing after 1 hour for the dog administration; And the flat granule of root pain just began onset after after the administration 10 minutes.
2 enteric-coated composition effective tives from 60min to 240min, about altogether 3h.And the flat granule of root pain is approximately from 10min to 60min, about altogether 50min.
The maximum blood flow recruitment of 3 methacrylic resin coating enteric coatel tablets groups is 26.0 ± 6.2, is significantly higher than the maximum blood flow recruitment 18.7 ± 8.3 of the flat groups of grains of root pain, P＜0.01.
The maximum blood flow of 4 hypromellose phthalate ester coating enteric coated particles groups is 27.5 ± 7.7, is significantly higher than the maximum blood flow 18.7 ± 8.3 of the flat groups of grains of root pain, P＜0.01.
The maximum blood flow of 5 Lac coating enteric-coated pellet capsule groups is 31.2 ± 9.1, is significantly higher than the maximum blood flow 18.7 ± 8.3 of the flat groups of grains of root pain, P＜0.01.
The maximum blood flow of 6 Lac coating enteric-coated pellet capsule groups is 27.1 ± 7.3, is significantly higher than the maximum blood flow 27.1 ± 7.3 of the flat groups of grains of root pain, P＜0.01.

Claims (8)

1. enteric coating compositions for the treatment of neck, lumbar spondylosis Chinese medicine, it is characterized in that this Chinese medicine enteric coating compositions is made by the component of following weight percentage ratio: enteric controlled-release agent 0.5-45%, lubricant 0-10%, plasticizer 0-10%, surfactant 0-1%, solvent 50-95%;
2. enteric coating compositions according to claim 1, it is characterized in that, described enteric controlled-release agent is a Lac, methacrylic acid copolymer, cellulose acetate benzene three esters, the hypromellose phthalate ester, cellulose acetate phthalate ester or polyvinyl alcohol phthalate ester, described lubricant is a Pulvis Talci, magnesium stearate, calcium stearate, stearic acid sucrose ester or silicon dioxide, described plasticizer is a triethyl citrate, Polyethylene Glycol, glycerol, propylene glycol or Oleum Ricini, described surfactant is a tween, span or sodium lauryl sulphate, described solvent are water, the ammonia of 30wt%, ethanol, acetone or ether.
3. enteric coating compositions according to claim 2 is characterized in that, the molecular weight of described methacrylic acid copolymer is 50000-500000.
4. enteric coating compositions according to claim 1 is characterized in that, described solution is made by methacrylic resin copolymer 30wt%, Tween 80 1wt%, triethyl citrate 10wt%, Pulvis Talci 5.5wt% and water 53.5wt%.
5. enteric coating compositions according to claim 1 is characterized in that, described solution is made by hypromellose phthalate ester 6wt%, acetone 75.2wt%, ethanol 18.8wt%.
6. enteric coating compositions according to claim 1 is characterized in that, 95% ethanol of described solution mountain Lac 18.7wt%, Tween 80 1wt%, triethyl citrate 1wt%, Oleum Ricini 1wt%, surplus is made.
7. enteric coating compositions according to claim 1 is characterized in that, described solution is made by cellulose acetate phthalate ester 30wt%, water 63.3wt%, triethyl citrate 2.3wt%, 30wt% ammonia 4.4wt%.
8. enteric coating compositions according to claim 1, it is characterized in that the Chinese medicine of described treatment neck, lumbar spondylosis is made by the Chinese crude drug of following weight parts: Herba Lycopodii 70-85, Myrrha 40-60, Radix Dipsaci 70-85, Radix Puerariae 45-60, Olibanum 40-60, Rhizoma Cibotii 70-90, Radix Achyranthis Bidentatae 45-60, Flos Carthami 45-60, Radix Paeoniae Alba 190-220, Semen Persicae 45-60, Radix Rehmanniae 45-60, Radix Glycyrrhizae 20-30.
CNB2005100050016A 2005-01-28 2005-01-28 Enteric coated Chinese medicine composition for treating cervical and lumbar spondylopathy Expired - Fee Related CN100398122C (en)

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Cited By (3)

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CN104825503A (en) * 2015-04-24 2015-08-12 成都汇智远景科技有限公司 Tongkat ali extract enteric coated tablet
CN105968385A (en) * 2016-05-31 2016-09-28 上海浦力膜制剂辅料有限公司 Preparation method of lac aqueous dispersion and application of lac aqueous dispersion in coating
CN110251478A (en) * 2019-05-15 2019-09-20 浙江维康药业股份有限公司 A kind of high temperature resistant enteric coating technique for droplet ball

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CN87104143A (en) * 1987-06-06 1988-12-28 连云港制药厂 Coloured enteric film coat coating tablets solution prescription
ES2077023T3 (en) * 1989-03-10 1995-11-16 Yamanouchi Pharma Co Ltd COATING MATERIAL THAT CONTROLS THE RELEASE OF A MEDICINAL PRODUCT FOR FORMULATIONS OF PROLONGED ACTIVITY.
CN1042696C (en) * 1993-05-13 1999-03-31 江西南昌桑海制药厂 Film coating technique for strong VC Yinqiao tablets
CN1090483C (en) * 1997-07-31 2002-09-11 谢理峰 Potassium and magnesium controlled-release tablet and producing method thereof
UA73092C2 (en) * 1998-07-17 2005-06-15 Брістол-Майерс Сквібб Компані Tablets with enteric coating and method for their manufacture
CN1353983A (en) * 2000-11-18 2002-06-19 唐修文 Enteric tablet coating liquor and its preparation method
CN1296046C (en) * 2003-12-23 2007-01-24 广州市医药工业研究所 Diltiazem hydrochloride control release capsule and its preparing method

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104825503A (en) * 2015-04-24 2015-08-12 成都汇智远景科技有限公司 Tongkat ali extract enteric coated tablet
CN105968385A (en) * 2016-05-31 2016-09-28 上海浦力膜制剂辅料有限公司 Preparation method of lac aqueous dispersion and application of lac aqueous dispersion in coating
CN110251478A (en) * 2019-05-15 2019-09-20 浙江维康药业股份有限公司 A kind of high temperature resistant enteric coating technique for droplet ball
CN110251478B (en) * 2019-05-15 2021-06-18 浙江维康药业股份有限公司 High-temperature-resistant enteric coating process for micro-dropping pills

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