The application of Vc-magnesium phosphorate in medicine
The present invention relates to the new application of Vc-magnesium phosphorate, particularly relate to the application in the preparation laxative.
Vc-magnesium phosphorate, English name are Ascorbyl phosphate magnesium, are called for short AP-Mg.
The molecular formula of AP-Mg: C
6H
6O
9PMg
1.55H
2O
Molecular weight is: 379.61
The AP-Mg purposes is wider, usually as food additive, does not still have the report of using as laxative.
1, present, the cathartic kind of treatment constipation is a lot, is broadly divided into three classes by its mechanism of action: (1) irritant laxative: all belong to this type of as commercially available phenolphthalein tablet, hypocatharsis sheet, Triacephentinum, bisatin, hemp intestine-moistening sheet (ball) etc.; (2) saline cathartic; As magnesium sulfate, sodium sulfate etc.; (3) emollient laxative; As glycone, glycerin etc.But these cathartics equal alleviate constipation patient's in clinical practice misery, but all there are some side effect to some extent, life-time service also can cause the custom dependency, even cause losing of calcium and vitamin, cause avitaminosis, therefore, constipation patient especially in, gerontal patient and pregnant, puerpera constipation person want these cathartics of careful selection.(draw from~" consultant of family " Beijing Publishing House, in February, 1980 front page P335-336.)
The objective of the invention is to the new pharmaceutical usage that utilizes AP-Mg to have, make caccagogue.What both can overcome that existing cathartic exists easily causes patient's vitamin deficiency, even easily causes deficiency such as spastic colon constipation, can take into account the effect that replenishes necessary vitamin C of human body and magnesium ion into human body again.
The object of the present invention is achieved like this:
With AP-Mg as active ingredient, combine with one or more excipient, make tablet, granule, powder or syrup by technological operations such as tablet, granule, powder, syrups, also can directly active ingredient be incapsulated and make capsule, be used for laxative action, wherein the consumption of AP-Mg accounts for the 0.6-100% of accumulated dose.
Can be decomposed into Vc and magnesium ion after the AP-Mg absorption of human body.Vc is the vitamin of human body requirement maximum, can strengthen immune function of human body, prevents and treats the generation of vitamin C deficiency and multiple disease.Magnesium ion also has plurality of health care functions, is the 4th cation of needed by human, with the functional activity of many enzymes important relationship is arranged, but catalysis or activate body 300 plurality of enzymes system, so magnesium ion is the key element of all energy metabolisms in the body.In the zoopery of adopting AP-Mg to carry out, find that it has the promotion gastrointestinal motility, increase Absorption, and then softening Excreta, reach cathartic, prevent the effect of constipation gastrointestinal tract moisture content.AP-Mg to the influence of white mice gastrointestinal motility, to the influence of white mice intestinal absorption moisture and discharge function result thereof see Table 1 respectively, table 2, table 3.
1, AP-Mg is to the influence of mice gastrointestinal motility
(1) method: choose 50 of the Kunming kind white mice of healthy weight 18-23g, female 12, male 38, be divided into 5 groups, 10 every group, blank group is given ordinary water, and the positive drug group gives 80 respectively, 2835Mg.kg
-1Magnesium sulfate, the administration group gives 80 respectively, 2835Mg.kg
-1AP-Mg, all irritate stomach by the 0.6ml/20g volume, all irritate stomach after 15 minutes with 10% charcoal end, after 15 minutes white mice being taken off neck puts to death, taking out gastrointestinal tract, has been point measurement small intestinal total length and charcoal end displacement with pylorus, calculates the percentage rate that charcoal end displacement accounts for the small intestinal total length.Intestinal motility has zero difference between t method of inspection calculating group with contrasting between group.
(2) conclusion; The results are shown in Table 1, AP-Mg2835Mg.kg
-1The dosage group has facilitation to intestinal motility, and its advance distance and propelling rate and blank group comparing difference remarkable (p<0.01) are better than the positive drug group, and this test shows that AP-Mg has facilitation to gastrointestinal motility under doses.
2, AP-Mg is to the effect of white mice intestinal absorption moisture content
(1) method: get 60 of healthy mices, body weight 18-23 gram is divided into 4 groups, and 15 every group, blank group is given ordinary water, and the positive drug group gives 5000Mg.kg
-1MgSO
4, the administration group gives 2500 respectively, 5000Mg.kg
-1AP-Mg, all by the 0.6ml/20g volume irritate stomach give with, white mice was taken off neck in 1 hour behind the medicine and puts to death, the full intestinal weight of weighing respectively, between organizing with the t check relatively.
(2) conclusion: the results are shown in Table 2, AP-Mg has the effect that increases the intestinal moisture absorption, 2500Mg.kg
-1The dosage group increases the effect and the MgSO of intestinal moisture content
45000 Mg.kg
-1Dosage is suitable.
3, the discharge function of AP-Mg
(1) method: 72 of healthy mices are divided equally 6 groups, and 12 every group, blank group is given ordinary water, all the other each groups are given 50% sucralfate, all give by 1ml//day, and hunger is spent the night two days later continuously, with above-mentioned half amount filling stomach once blank group was given ordinary water after half an hour in the 3rd day, and the positive drug group is given 5000Mg.kg
-1MgSO
4, model group gives that 50% sucralfate, administration group give 2500,5000 respectively, 7500Mg.kg
-1AP-Mg all irritates stomach by the 0.6mL/20g volume.Began to write down respectively in 1 hour behind the medicine and respectively organize mice accumulative total defecation grain number in 30,60,120,180,360 minutes each time periods, with between group relatively the t method of inspection calculate group difference.
(2) conclusion: the results are shown in Table 3, positive drug and AP-Mg5000Mg.kg
-1Dosage group and model group comparing difference are remarkable, (between P<0.05-0.001), AP-Mg2500Mg.kg
-1Discharge function is promptly arranged, AP-Mg5000Mg.kg
-1With MgSO
45000Mg.kg
-1Discharge function approaching, show AP-Mg5000Mg.kg
-1Dosage have and MgSO
4Identical discharge function.
Invention advantage: be not difficult to find out that from above-mentioned zoopery result the fast and strong positive drug magnesium sulfate effect of AP-Mg discharge function and discharge function is suitable.Use AP-Mg to have as cathartic that a medicine is used, the characteristics of safety non-toxic more in addition, both can avoid the side effect of existing cathartic, can be human body again increases necessary nutrition, has also widened the range of application of AP-Mg simultaneously.Its major advantage is; (1) the AP-Mg free of toxic effects is safe in utilization.(2) AP-Mg do not have smell, tasteless, the stimulating gastrointestinal road is not easy to be accepted.(3) the AP-Mg discharge function relaxes.(4) the AP-Mg stable in properties is difficult for oxidation, is not afraid of alkali, not influenced by the ferrum plasma, easily stores.(5) high temperature resistant, be not destroyed in 25 minutes 218 ℃ of bakings.(6) low price, easy to manufacture, do not produce environmental pollution.
Carry out on the zooperal basis at AP-Mg, use with the animal experiment dose,equivalent and take for numerical example custom constipation patient, each 200Mg (AP-Mg) (capsule) was administered three times on the 1st, had also obtained satisfied cathartic effect.
Excipient generally includes starch, lactose, sucrose, essence etc. among the present invention.Further specify the preparation method of preparation of the present invention by the following examples.
Embodiment 1
Patrol following prescription and make AP-Mg tablet (used content is weight percentage)
AP-Mg 50%
Lactose 25%
Starch 24%
Stearic acid 1%
(1) with AP-Mg, lactose pulverize separately, cross 100 mesh sieves, direct mistake 100 mesh sieves of starch are standby;
(2) get appropriate amount of starch and be mixed with 10% gelatinized corn starch, make adhesive fully;
(3) with AP-Mg, lactose and surplus starch mixing, add the soft ability of adhesive system, cross 16 mesh sieve system granules;
(4) wet granular is placed in about 50 ℃ of drying baker about 3 hours of forced air drying;
(5) dried granule adds magnesium stearate, mix homogeneously behind 16 mesh sieve granulate;
(6) with the flat stamping of diameter 90mm, promptly.
Embodiment 2
Make AP-Mg capsule (used content is weight percentage) by following prescription
AP-Mg?48%
Starch 52%
(1) AP-Mg, starch are passed through 100 mesh sieves respectively, carry out pretreatment;
(2) the abundant mix homogeneously of AP-Mg, starch that will be treated;
(3) medicated powder with mixing is filled into No. 2 capsulae vacuuses promptly.
Get and pulverize, and cross the AP-Mg100g of 100 mesh sieves, be filled into respectively in No. 2 capsulae vacuuses, promptly get pure AP-Mg capsule.
Embodiment 3
Make AP-Mg powder (used content is weight percentage) by following prescription
AP-Mg 10%
Icing Sugar 90%
With AP-Mg and Icing Sugar pulverize separately, cross 100 mesh sieves, the method that employing equivalent is progressively increased is with the two mix homogeneously, and subpackage is promptly.
Embodiment 4
Make AP-Mg granule (used content is weight percentage) by following prescription
AP-Mg 6%
Cane sugar powder 94%
After AP-Mg pulverized, cross 100 mesh sieves, with an amount of Icing Sugar mix homogeneously, other gets sucrose and is configured to 50% syrup in right amount, joins in the material of above-mentioned mixing, and the system soft material is granulated by 12 mesh sieves, oven dry, and after 12 mesh sieve granulate, pack gets final product.
Embodiment 5
Make AP-Mg dry syrup (used content is weight percentage) by following prescription
AP-Mg 5%
Cane sugar powder 93%
Citric acid 1.745%
Fructus Citri tangerinae flavor essence 0.125%
Orange flavor essence 0.125%
(1), cross 100 mesh sieves with AP-Mg, sucrose, citric acid pulverize separately:
(2) get AP-Mg, citric acid and an amount of Icing Sugar mixing;
(3) get in addition that an amount of sucrose is made into 50% syrup and pigment incorporated wherein make adhesive fully;
(4) adhesive that step (3) is made joins in the material of step (2) mixing, and the system soft material is crossed 12 mesh sieves and granulated, drying, behind the granulate promptly.