CN101336950B - Oral nano raw baizhu colon tablet and preparation method thereof - Google Patents
Oral nano raw baizhu colon tablet and preparation method thereof Download PDFInfo
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- CN101336950B CN101336950B CN2008100216496A CN200810021649A CN101336950B CN 101336950 B CN101336950 B CN 101336950B CN 2008100216496 A CN2008100216496 A CN 2008100216496A CN 200810021649 A CN200810021649 A CN 200810021649A CN 101336950 B CN101336950 B CN 101336950B
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Abstract
The invention relates to an oral nanometer crude Atractylodes macrocephala tablet for treating colonic diseases and a preparation method thereof, belonging to the technical field of medicaments. The oral nanometer crude Atractylodes macrocephala tablet is made with crude Atractylodes macrocephala nanometer powder and crude Atractylodes macrocephala polysaccharide extractive solution as a raw material and pectic calcium as a main coating material. The preparation method comprises the steps of: drying crude Atractylodes macrocephala, and pulverizing with a manometer pulverizer to obtain 400-1,200 mesh power; extracting to obtain crude Atractylodes macrocephala extractive solution as a wetting agent; reacting pectin and calcium chloride to obtain pectic calcium suspension for coating; and tabletting with the crude Atractylodes macrocephala nanometer powder and the crude Atractylodes macrocephala polysaccharide extractive solution, and coating. The inventive oral nanometer crude Atractylodes macrocephala tablet can safely pass through the upper digestive tract and release medicinal components after reaching the colon; and has the advantages of low oral dosage, reduced adverse effects,convenient administration, etc.
Description
Technical field
The present invention relates to a kind of oral nano raw baizhu colon tablet of clinical practice and preparation method thereof, belong to medical technical research field.
Background technology
Along with aged tendency of population, dietary habit change and the influence of factors such as society, psychology, constipation has become one of key factor that perplexs modern quality of life.Chronic constipation is the common symptoms that is caused by Different types of etiopathogenises, mainly shows as constipation with dry stool, just time minimizing, difficult defecation, just meaning disappearance etc.Functional chronic slow-transit constipation show as mainly that colonic activity weakens or (with) obstacle, the feces fltting speed slows down, emptying is slow.This disease can betide any age, but based on old man and women, the general course of disease is longer, the at present domestic and international no specific treatment medicine of chronic functional constipation, the Western medicine side effect is bigger, and the situation of abusing cathartic clinically is of common occurrence, has more increased the weight of developing of the state of an illness.
In recent years, seek the focus that the inexpensive natural drug of exploitation high-efficiency low-toxicity becomes new drug development field, the world.Chinese medicine just was familiar with primary disease before more than 2,000 years to some extent, had accumulated many effective experience sides in the clinical practice of ancient Chinese medicine doctor, but because the diversity of each family's understanding causes the difficulty of applying.Rhizoma Atractylodis Macrocephalae treatment constipation head sees the Han dynasty and cures holy Zhang Zhongjing, the 174th of treatise on Febrile Diseases: " typhoid fever eight or nine days, invasion of the body by blended pathogenic wind and dampness, restlessness and pain of the body, unable to turn aside, it is not thirsty not vomit, the pulse being floating,deficient and hesitant person, the Ramuli Cinnamomi and Aconiti Praeparatae Decoction master it.If its people's hard stool, the normal urination person, go osmanthus add the atractylodes decoction master it "." China book on Chinese herbal medicine " also points out insufficiency of the spleenly can not be stomach Xingqi body fluid, and intestinal loses profit, and the reusable Rhizoma Atractylodis Macrocephalae adds flavor " fortuneization spleen sun " intestine moistening road with promoting circulation of body fluid." new medicine and pharmacology magazine " the 4th periodical in 1978 has been stepped on Mr.'s Wei Longxiang medical notes four fundamental rules, and wherein " Rhizoma Atractylodis Macrocephalae relieving constipation is secret " said the experience of reusing Rhizoma Atractylodis Macrocephalae treatment constipation of having introduced.Even to this day, many scholars have carried out about Rhizoma Atractylodis Macrocephalae active research of rabbit intestine in vitro and clinical practice, and the result is not consistent.We are at the observed result after to 113 routine patient's medications, single Rhizoma Atractylodis Macrocephalae light water decoct treatment chronic functional constipation total effective rate is 76.99%, and, have the colon of enhancing group propelling property wriggling and can promote that the gastrointestinal secretion function view is consistent with the Rhizoma Atractylodis Macrocephalae of bibliographical information to the weakness constipation especially deficiency of YIN and deficiency of spleen-QI and stomach-QI person best results.Though our the clinical observation table open-birth Rhizoma Atractylodis Macrocephalae is taken back onset slow (general 8-12 hour), but the just soft and side effect that can not produce irritant purgatives such as stomachache, watery diarrhea of qualitative change, and infrequent defecation time, defecation effort degree etc. bigger improvement is all arranged, abdominal distention alleviates simultaneously, just the meaning sense strengthens.The zoopery result shows: aspect 3h feces weight in wet base, 3h feces water content and 3-24h feces weight in wet base, the water decoction effect is better than Zelnorm; We do not find that mice has the diarrheal situation in the experimentation, even only be soft and do not have rare water or shapeless feces to discharge in the bigger feces of water content, this and clinical experiment are partly identical.These are all pointed out: Rhizoma Atractylodis Macrocephalae can promote intestinal movement on the one hand, and the recovery that can strengthen " large intestine master liquid " this function on the other hand is normal.But the light water decoct still exists from upper digestive tract and just begins discharge to absorb, and dosage is big and use shortcoming such as inconvenience.
For promoting the effect of Rhizoma Atractylodis Macrocephalae treatment constipation, we use for reference forefathers' experience, have formulated the nano raw baizhu colon controlled release tablet on the basis of experiment repeatedly, have significantly improved curative effect.
Summary of the invention
Just begin to discharge absorption from upper digestive tract in order to solve existing Rhizoma Atractylodis Macrocephalae light water decoct, and awkward deficiency, the invention provides a kind of oral nano raw baizhu colon tablet, significantly improved curative effect.
The technical solution used in the present invention is:
A kind of oral nano raw baizhu colon tablet is to be crude drug with the Rhizoma Atractylodis Macrocephalae nano powder, is that main clothing membrane material is made with calcium pectinate.Wherein, nano level Rhizoma Atractylodis Macrocephalae powder significantly improves the preparation bioavailability, reduces dosage, reduces untoward reaction; Calcium pectinate is water insoluble; also not by the enzymatic degradation that exists in stomach and the small intestinal; but can be degraded by colonic contents (mainly being some bacteriogenic pectase); so can protect preparation to arrive colon by stomach and small intestinal smoothly; and at colon generation clothing membrane degradation, location release medicine, targeting is reliable for effect.
The day clothes dosage that present many reports are reused Rhizoma Atractylodis Macrocephalae treatment constipation is 60g～120g, and the day clothes dosage of nano raw baizhu colon tablet is 15g～30g.
The present invention also provides the preparation method of above-mentioned oral nano raw baizhu colon tablet, is with the Rhizoma Atractylodis Macrocephalae medicinal material drying after nano grinder is pulverized to such an extent that be 400 orders～1200 mesh sieve fine powders; Extract Rhizoma Atractylodis Macrocephalae polysaccharide liquid as wetting agent; Pectin and calcium chloride reaction make the calcium pectinate suspension and are used for coating; Get final product with coating behind Rhizoma Atractylodis Macrocephalae nano powder and the plain sheet of Rhizoma Atractylodis Macrocephalae polysaccharide hydraulic pressure system.
More specifically preparation method may further comprise the steps:
(1) preparation of Rhizoma Atractylodis Macrocephalae nano powder and polysaccharide liquid
With the Rhizoma Atractylodis Macrocephalae medicinal material drying after nano grinder is pulverized 400 orders～1200 mesh sieve fine powders,
The preparation of Rhizoma Atractylodis Macrocephalae polysaccharide liquid: get Rhizoma Atractylodis Macrocephalae crude drug decoction pieces 400g, add 4～8 times of amount 75% alcohol refluxs 1～2 time, each 2h filters; Medicinal residues add 8 times of water gagings and decoct 3 times, and each 1.5h merges decocting liquid, is concentrated into 400ml (being equivalent to crude drug 1g/ml), leaves standstill, and is centrifugal; Supernatant adds ethanol and transfers to 75%, leaves standstill; Sucking filtration will precipitate and use dissolved in distilled water, and centrifugal, supernatant adds ethanol and transfers to 75%, leave standstill, and sucking filtration, precipitation is used the 400ml dissolved in distilled water after using the dehydrated alcohol cyclic washing, promptly gets polysaccharide solution;
(2) preparation of calcium pectinate
Get hypo-methoxy pectin (methoxyl content＜5～10% or esterification degree＜30～50%) 60～120g, add redistilled water 400～500ml, soak 1～2h, stir 24h and make abundant dissolving; Get 10gCaCl
2Add redistilled water and make into 3～6% solution and slowly pouring in the pectin solution to 200ml, two liquid mix and stir 2h, place 24h for airtight 4 ℃, after the part suction, by extruding, centrifugal removal most of moisture, about 40 ℃ of vacuum drying 48h, pulverized 80～120 mesh sieves again; Record calcium content (being controlled at about 6～12%) with atomic absorption spectrophotometer for good;
(3) preparation of the plain sheet of Rhizoma Atractylodis Macrocephalae
The Rhizoma Atractylodis Macrocephalae nano powder is added Rhizoma Atractylodis Macrocephalae polysaccharide liquid system soft material, system granule, drying, granulate adds the stearic acid mix homogeneously, tabletting;
(4) the inclusion casing of Rhizoma Atractylodis Macrocephalae label
Get calcium pectinate and add water porphyrize formation suspension in colloid mill, add 1.5～2.5% acrylic resins (EudragitL30D), 0.1～0.2% phthalic acid ester and 0.1% Arlacel-80, mix homogeneously is colon coating solution;
Coating pan is heated to 35 ℃, and label places coating pan to roll, and sprays into coating solution, and the spray gun pressure-controlled is at 2～4kg/cm2, it is mobile not smooth to be sprayed onto label, blowing hot-air drying, about 60～80 ℃ of pathogenic wind-warm, repeat above operation after drying up, when label weightening finish reaches 10～15% left and right sides, dry getting final product.
Oral nano raw baizhu colon tablet of the present invention, employing is not dissolved at the harmonization of the stomach small intestinal, and only at the dissolved coating material of colon, thereby reach the purpose that transport of drug is discharged to colon, promptly reach the total colectomy release, be evenly distributed, not in the upper digestive tract release, improve the drug level at colonic pathological change position, help treatment.Oral nano raw baizhu colon tablet also significantly reduces oral dose, and performance medicine optimum curative effect reduces adverse effect, and is easy to use.
The specific embodiment
Employed in the present invention term unless other explanation is arranged, generally has the implication of those of ordinary skills' common sense.
Below in conjunction with concrete preparation embodiment and Application Example, and comparable data is described the present invention in further detail.Should be understood that these embodiment just in order to demonstrate the invention, but not limit the scope of the invention by any way.In following embodiment, various processes of Xiang Ximiaoshuing and method are not conventional methods as known in the art.The source of agents useful for same, trade name and be necessary to list its constituent person indicate when occurring first that all used thereafter identical reagent if no special instructions, and is all identical with the content of indicating first.
Embodiment 1: the preparation of oral nano raw baizhu colon tablet
(1) preparation of nano raw baizhu powder
With the Rhizoma Atractylodis Macrocephalae medicinal material drying after nano grinder is pulverized 400 orders～1200 mesh sieve fine powders,
The preparation of Rhizoma Atractylodis Macrocephalae polysaccharide liquid: get Rhizoma Atractylodis Macrocephalae crude drug decoction pieces 400g, add 4～8 times of amount 75% alcohol refluxs 1～2 time, each 2h filters; Medicinal residues add 8 times of water gagings and decoct 3 times, and each 1.5h merges decocting liquid, is concentrated into 400ml (being equivalent to crude drug 1g/ml), leaves standstill, and is centrifugal; Supernatant adds ethanol and transfers to 75%, leaves standstill; Sucking filtration will precipitate and use dissolved in distilled water, and centrifugal, supernatant adds ethanol and transfers to 75%, leave standstill, and sucking filtration, precipitation is used the 400ml dissolved in distilled water after using the dehydrated alcohol cyclic washing, promptly gets polysaccharide solution;
(2) preparation of calcium pectinate
Get hypo-methoxy pectin (methoxyl content＜5～10% or esterification degree＜30～50%) 60～120g, add redistilled water 400～500ml, soak 1～2h, stir 24h and make abundant dissolving; Get 10gCaCl
2Add redistilled water and make into 3～6% solution and slowly pouring in the pectin solution to 200ml, two liquid mix and stir 2h, place 24h for airtight 4 ℃, after the part suction, by extruding, centrifugal removal most of moisture, about 40 ℃ of vacuum drying 48h, pulverized 80～120 mesh sieves again; Record calcium content (being controlled at about 6～12%) with atomic absorption spectrophotometer for good;
(3) preparation of the plain sheet of Rhizoma Atractylodis Macrocephalae
The Rhizoma Atractylodis Macrocephalae nano powder is added Rhizoma Atractylodis Macrocephalae polysaccharide extraction liquid system soft material, makes granule, drying, granulate adds the stearic acid mix homogeneously, tabletting;
(4) the inclusion casing of Rhizoma Atractylodis Macrocephalae label
Get calcium pectinate and add water porphyrize formation suspension in colloid mill, add 1.5%～2.5% acrylic resin (Eudragit L30D), 0.1%-～0.2% phthalic acid ester and 0.1% Arlacel-80, mix homogeneously is colon coating solution; Coating pan is heated to 35 ℃, and label places coating pan to roll, and sprays into coating solution, and the spray gun pressure-controlled is at 2～4kg/cm
2Be sprayed onto label flow not smooth, the blowing hot-air drying, about 60～80 ℃ of pathogenic wind-warm repeats above operation after drying up, when the label weightening finish reaches 10%～15% left and right sides, dry getting final product.
Attached 1: the oral nano raw baizhu colon tablet quality standard
Appearance character:
Complete bright and clean, color and luster is even, and no foreign body does not have assorted speckle, remains unchanged in effect duration.
Label is lark (being bordering on Rhizoma Atractylodis Macrocephalae crude drug color and luster), clothing film light brown, the heavy 1.0g ± 0.05g of sheet; Day is obeyed 15～20 of dosage.
Tablet weight variation: the weight differential of looking into label before the coating: get 20 and weigh, with the heavy and average sheet anharmonic ratio of every sheet, the tablet that exceeds the difference limit must not be more than 2, and 1 times of 1 overrun must not be arranged.
Hardness and friability: use Monsanto durometer method and sieve and permitted crisp broken instrument method mensuration, Fr≤3 (%).
Disintegration: the hanging basket method is checked.Crack, disintegrate or softening etc. are not arranged, all molten loosing or disintegrate and pass through screen cloth in 1 hour in artificial colonic fluid in 2 hours in simulated gastric fluid and simulated intestinal fluid.
Dissolution: slurry method, 37 ℃ ± 1 ℃ constant temperature, rotating speed 100r/min, get 6 and put into artificial colonic fluid, and sampling in required time, the burst size sky is in 80% in testing index component content (be the index composition with the atractylenolide or be standard reference material with the crude drug nano powder, 254nm the surveys trap) 20min.
Uniformity of dosage units: get 10 relative amounts of measuring every respectively, by " Chinese pharmacopoeia method inspection judgement meets the requirements.
Attached 2:
One, artificial colonic fluid compound method
1. rat colon liquid preparation: get 5 of rats, body weight 200～300g, the normal raising, irritate stomach every day and only give 2% liquid pectin 2mL/, put to death cecal ligation after continuous 3 days, get its content, the ratio adding phosphate buffer (pH=7.0) of back of weighing in 1.5g/100ml.
2. rabbit colonic fluid preparation: get one of rabbit, about body weight 2.0kg, put to death the postcolon caecum, its content places 100mL phosphate buffer (pH=7.0).
Two, the establishment of Rhizoma Atractylodis Macrocephalae index components and detection wavelength
Rhizoma Atractylodis Macrocephalae is the dry rhizome of feverfew Rhizoma Atractylodis Macrocephalae Atractylodes macro-cephala Koidz..Have invigorating the spleen and benefiting QI, dampness diuretic, the antiabortive effect of hidroschesis.Contain volatile oil, sesquiterpene lactones chemical compound, polyacetylene alcohol compound etc. in the Rhizoma Atractylodis Macrocephalae rhizome, wherein atractylodes lactone constituents (atractylenolide, II etc.) is antiinflammatory, the anticancer effective component of the Rhizoma Atractylodis Macrocephalae.Show that through pharmacological evaluation this constituents has the effect of regulating gastrointestinal function and promoting absorption of nutrient ingredients, especially the atractylenolide pharmacological action is obvious, is the main active of the Rhizoma Atractylodis Macrocephalae, so determine that it is the leading indicator of Rhizoma Atractylodis Macrocephalae quality control.
In carrying out the research of Rhizoma Atractylodis Macrocephalae medical material HPLC chromatographic fingerprinting, we adopt Agilent TC-C
18Chromatographic column (250mm * 4.6mm, 5 μ m); With methanol: water (65%～100%) continuous gradient eluting, volume flow rate are the analysis of carrying out 10 batch samples under the condition of 1.0ml/min.When analyzing, carry out the long UV scanning of all-wave, investigate all data under the different wave length.The result shows, detects effect and is subjected to wavelength affects bigger, shows at the 254nm chromatographic peak profile after relatively preferably, and it is moderate to go out the peak number order, and each chromatographic peak separating degree each other is better, and (actual atractylenolide maximum absorption wavelength is 220nm so the detection wavelength fixes on 254nm; Atractylenolide I maximum absorption wavelength is 276nm etc., is to be that raw material is made with single medicinal material material Rhizoma Atractylodis Macrocephalae because of said preparation, so can be that standard reference material carries out the inspection of chemical constituent release with the crude drug nano powder also).
Embodiment 2: pharmacodynamic experiment of the present invention
1. material
Rhizoma Atractylodis Macrocephalae is bought from Bengbu city medical material company, CW-15 type nano grinder with Yantai intelligent precious device fabrication company limited production is prepared nano powder, encircles the production equipment machine-shaping of Yangzhou pharmaceutical factory of pharmaceutical Co. Ltd by the Jiangsu connection: 1. be pressed into plain sheet of 0.1g and inclusion casing; 2. extrude spheronization and prepare micropill and inclusion casing.Laboratory animal rabbit, mice provide by Yangzhou University's Experimental Animal Center.
2. method and result
2.1 the raw baizhu colon micropill is to the influence of barium meal, india ink fltting speed in the mouse small intestine
2.1.1 the raw baizhu colon micropill is to the influence of barium meal fltting speed in the mouse small intestine
Get 40 of body weight 20～25g ICR mices, male and female half and half, water is can't help in the 24h fasting, is divided into normal group, Rhizoma Atractylodis Macrocephalae micropill group, raw baizhu colon micropill group and MAREN RUANJIAONANG group at random.Except that normal group, each group is pressed 0.2g/20g, gastric infusion once a day, after 5 days, each is organized and adds barium 0.01g in the medicine, behind the administration 30min, take off neck execution and respectively organize mice, open the abdominal cavity, separate mesentery, the clip pylorus is to the intestinal tube of ileocecus, and is gently that small intestinal is stretching, measure its total length, distance from pylorus to the barium meal forward position, is calculated and is advanced percentage rate (%) at the enteral advance distance as barium meal, and the result is as follows: normal group is 59.17 ± 2.62; Rhizoma Atractylodis Macrocephalae micropill group is 63.33 ± 3.85; Raw baizhu colon micropill group is 79.93 ± 5.42; The MAREN RUANJIAONANG group is 75.41 ± 3.61.
2.1.2 the raw baizhu colon micropill is to the influence of india ink fltting speed in the mouse small intestine
Get 40 of body weight 20～25gICR mices, male and female half and half, water is can't help in the 24h fasting, is divided into normal group, Rhizoma Atractylodis Macrocephalae micropill group, raw baizhu colon micropill group and MAREN RUANJIAONANG group at random.Except that normal group, each group is pressed 0.2g/20g, gastric infusion once a day, after 5 days, each is organized and adds India prepared Chinese ink 0.1ml in the medicine, behind the administration 30min, take off neck execution and respectively organize mice, open the abdominal cavity, separate mesentery, the clip pylorus is to the intestinal tube of ileocecus, and is gently that small intestinal is stretching, measure its total length, distance from pylorus to the india ink forward position, is calculated and is advanced percentage rate (%) at the enteral advance distance as india ink, and the result is as follows: normal group is 56.24 ± 5.63; Rhizoma Atractylodis Macrocephalae micropill group is 60.54 ± 6.01; Raw baizhu colon micropill group is 76.58 ± 4.27; The MAREN RUANJIAONANG group is 71.82 ± 4.56.
2.1 the raw baizhu colon micropill is to the influence of mice enteral barium meal fltting speed
Get 40 of body weight 20～25gICR mices, male and female half and half are divided into normal group at random, blank group Rhizoma Atractylodis Macrocephalae micropill group, raw baizhu colon micropill group and MAREN RUANJIAONANG group.Except that normal group, all the other each groups are irritated stomach with compound diphenoxylate 50mg/kg and were set up the constipation of the transmission slowly model of mice in 14 days.After the modeling phase finishes, remove normal group, outside the blank group, all the other each groups are pressed 0.2g/20g, irritate the stomach single administration every day 14 days.Finish the same day and give 200% barium sulfate pasty liquid 0.5ml/ only to irritate stomach, record is treated to write down constantly when it discharges first white feces again, thereby is calculated the one anus transmission time (min) of outlet constantly.The result is as follows: normal group is 142.75 ± 13.24; Blank group 183.00 ± 16.91; Rhizoma Atractylodis Macrocephalae micropill group 150.00 ± 12.03; Raw baizhu colon micropill group is 105.75 ± 15.97; The MAREN RUANJIAONANG group is 160.75 ± 1.50.
2.2 raw baizhu colon tablet to tame rabbit anesthesia after the influence of shrinking of live body ileum
Get body weight and be 16 of rabbits about 2kg, male and female half and half are divided into normal group, the plain sheet group of Rhizoma Atractylodis Macrocephalae, raw baizhu colon tablet group and MAREN RUANJIAONANG group at random.Wherein except that normal group, each group is pressed 10mg/kg, gastric infusion once a day, after 5 days, slowly annotate the people with 2% urethane solution 1g/kg to each group rabbit ear edge vein, after the anesthesia, the abdomen ileocecus is made one 3～4cm otch in the rabbit bottom right, hemostasis back exposes the ileal segment of ileocecus 4～5cm, wait to trace suspension apparatus that ileum shrinks stable after, the normal ileum contraction frequency of record earlier, medication respectively then, press 10mg/kg and irritate stomach, write down each administration group contraction frequency, the result following (inferior/min): normal group 35.75 ± 6.22; The plain sheet group 40.11 ± 7.31 of Rhizoma Atractylodis Macrocephalae; Raw baizhu colon tablet group 48.63 ± 7.99; MAREN RUANJIAONANG group 45.38 ± 6.91.
2.2 raw baizhu colon tablet to tame rabbit anesthesia after the influence of shrinking of live body colon
Get body weight and be 16 of rabbits about 2kg, male and female half and half are divided into normal group, the plain sheet group of Rhizoma Atractylodis Macrocephalae, raw baizhu colon tablet group and MAREN RUANJIAONANG group at random.Wherein except that normal group, each group is pressed 10mg/kg, and gastric infusion is 5 days once a day, fasting 24h, and acute execution rabbit is taken out colon head end (connecting the 0.5cm place apart from the colon caecum) and tail end (apart from basin bone edge 5cm place) rapidly.Get 4 flesh bars with fixed two parallel blades along the direction of smooth muscle fiber: colon head end longitudinal muscle flesh bar (LMPC), colon head end circular muscle flesh bar (CMPC), colon tail end longitudinal muscle flesh bar (LMDC) and colon tail end circular muscle flesh bar (CMDC).Carefully remove mucosa with eye scissors.4 flesh bars are placed in 4 perfusion flesh grooves respectively (all fill 37 ℃ of Krebs liquid of 5mL and sustainable supply 95%O2 and 5%CO2 mist in each flesh groove.The flesh bar is hatched about 1h under the preload of 1g).The spontaneous contraction movement of record flesh bar.Wait to trace suspension apparatus that colon shrinks stable after, contraction frequency, result following (waves/min) respectively organized in record:
The plain sheet group of normal group Rhizoma Atractylodis Macrocephalae raw baizhu colon tablet group MAREN RUANJIAONANG group
LMPC 0.8±0.8 0.9±0.4 1.6±2.4 1.3±0.5
CMPC 0.7±0.6 1.3±0.9 2.1±1.9 1.4±0.4
LMDC 6.2±1.7 7.5±1.9 10.9±3.3 8.7±4.0
CMDC 10.1±3.0 11.2±3.3 16.7±2.2 12.5±2.7
As seen compare with normal group, raw baizhu colon tablet can significantly increase the contraction frequency (difference has statistical significance) of each position flesh bar of colon, and effect is remarkable than plain sheet group of Rhizoma Atractylodis Macrocephalae and MAREN RUANJIAONANG group.
Laboratory observation shows that the raw baizhu colon preparation has obvious progradation to barium meal in the mouse small intestine, rabbit is had in the shrinkage amplitude of body ileum and frequency obviously increase effect.
Further mice constipation model pharmacodynamic experiment shows that also single raw baizhu colon relieving constipation effect is sure.
2.3 raw baizhu colon tablet is to the influence of mice constipation model
2.3.1. material
Rhizoma Atractylodis Macrocephalae is available from Bengbu city medical material company, CW-15 type nano grinder with Yantai intelligent precious device fabrication company limited production is prepared nano powder, encircles the Rhizoma Atractylodis Macrocephalae polysaccharide liquid machine-shaping that Yangzhou pharmaceutical factory of pharmaceutical Co. Ltd extracts with this nano powder and this laboratory by the Jiangsu connection: 1. be pressed into plain sheet of 0.1g and inclusion casing; 2. extrude spheronization and prepare micropill and inclusion casing.Laboratory animal provides by Yangzhou University's Experimental Animal Center.
2.3.2 method
2.3.2.1 grouping and modeling: get 42 of female mices, body weight 18-23g is divided into 6 groups at random, is respectively normal group, the blank group, and western medicine group, slow releasing agent is low, in, high dose group, 7 every group, adaptability was raised 3 days, as normal feeding period; Irritated stomach 14 days with Compound Diphenoxylate, as the modeling phase of constipation; Irritate the stomach pin with self-control and gavage raw baizhu colon location release particles 14 days, as the constipation therapy phase.
2.3.2.2 detection index: normal feeding period, constipation modeling phase and nature convalescent period finish the same day gives 200% barium sulfate pasty liquid 0.5ml/ and only irritates stomach, record constantly, treat to write down again constantly when it discharges first white feces, thereby calculate the outlet-anus transmission time.After each finished phase, each was organized the single cage of mice and raises, the morning 11:00 gastric infusion, afternoon, 14:00 collected 3h feces, weighed, and electronic balance claims its weight (feces weight in wet base), be placed in the surface plate the high fire baking of microwave oven 5 minutes, claim dry weight, water content=(weight in wet base-dry weight)/weight in wet base * 100%.Morning next day, 11:00 collected 3-24h feces, and as above method draws 3-24h fecal grains and 3-24h water content.
2.3.3 result
From the mouth anus transmission time, 3h, 3-24h fecal grains and 3h, 3-24h water content, the granule of raw baizhu colon positioning and slow release can effectively be accelerated intestinal transmission, thereby increase the symptom that feces volume, softening feces improve constipation, effect is better than western medicine group, and with the low dosage best results.(seeing table 1 for details, 2,3,4,5)
Table 1 mouthful-anus transmission time (min, x ± s)
Compare ★ P＜0.01 with the blank group, * P＜0.05; Compare zero P＜0.05 with western medicine group; Compare #P＜0.01 with normal group
Table 23h feces weight in wet base (g, x ± s)
Compare #P＜0.01 with normal group; Compare ★ P＜0.01 with the blank group; Compare zero P＜0.05 with western medicine group; Compare * P＜0.01 with the slow releasing agent high dose group
Table 33h feces water content (%, x ± s)
△ compares with the normal control group, P＜0.05; ※ compares with model control group, P＜0.05; # compares with positive controls, P＜0.05
Table 43-24h feces weight in wet base (g, x ± s)
△ compares with the normal control group, P＜0.05; ※ compares with the blank group, P＜0.05; # compares with western medicine group, P＜0.05
Table 53-24h feces water content (%, x ± s)
△ compares with the normal control group, P＜0.05; ※ compares with the blank group, P＜0.05; # compares with western medicine group, P＜0.05.
Claims (2)
1. oral nano raw baizhu colon tablet is to be crude drug with Rhizoma Atractylodis Macrocephalae nano powder and Rhizoma Atractylodis Macrocephalae polysaccharide extraction liquid, is main clothing membrane material with calcium pectinate, makes by the following method:
(1) preparation of Rhizoma Atractylodis Macrocephalae nano powder and polysaccharide liquid
With the Rhizoma Atractylodis Macrocephalae medicinal material drying after nano grinder is pulverized 400 orders～1200 mesh sieve fine powders;
The preparation of Rhizoma Atractylodis Macrocephalae polysaccharide liquid: get Rhizoma Atractylodis Macrocephalae crude drug decoction pieces 400g, add 4～8 times of amount 75% alcohol refluxs 1～2 time, each 2h filters; Medicinal residues add 8 times of water gagings and decoct 3 times, and each 1.5h merges decocting liquid, is concentrated into 400ml, leaves standstill, and is centrifugal; Supernatant adds ethanol and transfers to 75%, leaves standstill; Sucking filtration will precipitate and use dissolved in distilled water, and centrifugal, supernatant adds ethanol and transfers to 75%, leave standstill, and sucking filtration, precipitation is used the 400ml dissolved in distilled water after using the dehydrated alcohol cyclic washing, promptly gets polysaccharide solution;
(2) preparation of calcium pectinate
Get hypo-methoxy pectin 60～120g, add redistilled water 400～500ml, soak 1～2h, stir 24h and make abundant dissolving; Get 10gCaCl
2Add redistilled water and make into 3～6% solution and slowly pouring in the pectin solution to 200ml, two liquid mix and stir 2h, place 24h for airtight 4 ℃, after the part suction, by extruding, centrifugal removal most of moisture, about 40 ℃ of vacuum drying 48h, pulverized 80～120 mesh sieves again; Calcium content is 6～12%;
(3) preparation of the plain sheet of Rhizoma Atractylodis Macrocephalae
The Rhizoma Atractylodis Macrocephalae nano powder is added Rhizoma Atractylodis Macrocephalae polysaccharide extraction liquid system soft material, system granule, drying, granulate adds the stearic acid mix homogeneously, tabletting;
(4) the inclusion casing of Rhizoma Atractylodis Macrocephalae label
Get calcium pectinate and add water porphyrize formation suspension in colloid mill, add 1.5～2.5% acrylic resins, 0.1～0.2% phthalic acid ester and 0.1% Arlacel-80, mix homogeneously is colon coating solution;
Coating pan is heated to 35 ℃, and label places coating pan to roll, and sprays into coating solution, and the spray gun pressure-controlled is at 2～4kg/cm
2, be sprayed onto label flow not smooth, the blowing hot-air drying, about 60～80 ℃ of pathogenic wind-warm repeats above operation after drying up, when the label weightening finish reaches 10～15% left and right sides, dry getting final product.
2. one kind prepares the said oral nano raw baizhu colon tablet preparation method of claim 1, and implementation step is:
(1) preparation of Rhizoma Atractylodis Macrocephalae nano powder and polysaccharide liquid
With the Rhizoma Atractylodis Macrocephalae medicinal material drying after nano grinder is pulverized 400 orders～1200 mesh sieve fine powders;
The preparation of Rhizoma Atractylodis Macrocephalae polysaccharide liquid: get Rhizoma Atractylodis Macrocephalae crude drug decoction pieces 400g, add 4～8 times of amount 75% alcohol refluxs 1～2 time, each 2h filters; Medicinal residues add 8 times of water gagings and decoct 3 times, and each 1.5h merges decocting liquid, is concentrated into 400ml, leaves standstill, and is centrifugal; Supernatant adds ethanol and transfers to 75%, leaves standstill; Sucking filtration will precipitate and use dissolved in distilled water, and centrifugal, supernatant adds ethanol and transfers to 75%, leave standstill, and sucking filtration, precipitation is used the 400ml dissolved in distilled water after using the dehydrated alcohol cyclic washing, promptly gets polysaccharide solution;
(2) preparation of calcium pectinate
Get hypo-methoxy pectin 60～120g, add redistilled water 400～500ml, soak 1～2h, stir 24h and make abundant dissolving; Get 10gCaCl
2Add redistilled water and make into 3～6% solution and slowly pouring in the pectin solution to 200ml, two liquid mix and stir 2h, place 24h for airtight 4 ℃, after the part suction, by extruding, centrifugal removal most of moisture, about 40 ℃ of vacuum drying 48h, pulverized 80～120 mesh sieves again; Calcium content is 6～12%;
(3) preparation of the plain sheet of Rhizoma Atractylodis Macrocephalae
The Rhizoma Atractylodis Macrocephalae nano powder is added Rhizoma Atractylodis Macrocephalae polysaccharide extraction liquid system soft material, system granule, drying, granulate adds the stearic acid mix homogeneously, tabletting;
(4) the inclusion casing of Rhizoma Atractylodis Macrocephalae label
Get calcium pectinate and add water porphyrize formation suspension in colloid mill, add 1.5～2.5% acrylic resins, 0.1～0.2% phthalic acid ester and 0.1% Arlacel-80, mix homogeneously is colon coating solution;
Coating pan is heated to 35 ℃, and label places coating pan to roll, and sprays into coating solution, and the spray gun pressure-controlled is at 2～4kg/cm
2, be sprayed onto label flow not smooth, the blowing hot-air drying, about 60～80 ℃ of pathogenic wind-warm repeats above operation after drying up, when the label weightening finish reaches 10～15% left and right sides, dry getting final product.
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| CN101554197B (en) * | 2009-05-12 | 2012-02-01 | 扬州大学 | Functional polysaccharide tea and preparation method thereof |
| US9433583B2 (en) | 2011-04-22 | 2016-09-06 | Frank J. Farrell | Colon vitamin |
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Non-Patent Citations (3)
| Title |
|---|
| 张亚军 等.《果胶在细菌触发型结肠定位给药制剂中的应用》.《中国医药工业杂志》.2007,第38卷(第7期),535. |
| 张亚军等.《果胶在细菌触发型结肠定位给药制剂中的应用》.《中国医药工业杂志》.2007,第38卷(第7期),535. * |
| 晏建立.《再谈白术治便秘》.《中医杂志》.1998,第39卷(第7期),445. * |
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