The manufacture method of troche for eliminating gastrointestinal vesicle and application thereof
The present invention relates to the pharmaceutical technology field, refer in particular to a kind of manufacture method and application thereof of troche for eliminating gastrointestinal vesicle.
The manufacture method of traditional lozenge medicine is with active pharmaceutical ingredients and nonactive pharmaceutical compositions such as excipient etc., and directly mix homogeneously is made ingot again, or when system ingot or whole ingot the mixed active pharmaceutical compositions.When making lozenge, owing to added nonactive composition such as excipient, can overcome the not good enough defective of liquor taste, but because traditional method for making, active pharmaceutical ingredients is mixed among the excipient, it is discharged slowly, not as liquor absorbs easily, drug effect is relatively poor.The gastrointestinal froth breaking medicine that the present invention relates to is poly-disilane (Dimethylpolysiloxane) or dimethylamino silane and silica mixture (Simethicon) or its mixture, has the interfacial activity effect, surface tension is reduced, the effect that gastrointestinal is had froth breaking, be usually used in treating distended tummy or the preceding defoamer of gastrointestinal endoscopy, but because its mouthfeel bitterness, liquid difficulty is used for a mouthful newspaper, it is oral that the inactive excipient of normal adding etc. is made lozenge, but because the lozenge made from conventional method is mixed in active pharmaceutical ingredients among the excipient, its disintegrate and release ratio are slower, so the froth breaking effect is not good enough.
The object of the present invention is to provide a kind of manufacture method of gastrointestinal froth breaking ingot system, comprise earlier inactive excipient etc. is made blank lozenge, again blank lozenge dipping is absorbed the gastrointestinal froth breaking active medicine of fixed amount, improve the disintegrate and the rate of release of gastrointestinal froth breaking medicine, reach the purpose that improves curative effect.
Another object of the present invention is to provide the application technology of this manufacture method, be used to make the manufacture method of other quick-acting lozenge medicines of needs.
The object of the present invention is achieved like this: a kind of manufacture method of troche for eliminating gastrointestinal vesicle, it is characterized in that this manufacture method be earlier nonactive composition comprised absorbent, collapse powder, lubricant, diluent and/or bonding agent be pressed into blank lozenge, should flood the gastrointestinal froth breaking active medicine that absorbs fixed amount by blank lozenge again, make troche for eliminating gastrointestinal vesicle.
This gastrointestinal froth breaking active medicine is the mixture of poly-dimethylamino silane and/or dimethylamino silane and silicon dioxide.
The content of this gastrointestinal froth breaking active medicine is the 1-25 parts by weight.
This absorbent is a silicon dioxide.
This collapses powder and comprises carboxymethyl starch sodium, sodium carboxymethyl cellulose, carboxymethylcellulose calcium.
This lubricant comprises Pulvis Talci, stearic acid, magnesium stearate.
This diluent is monosaccharide or polysaccharide, comprises glucose, galactose, fructose, multitudinous sugar, lactose, mannitol, sorbitol.
This bonding agent comprises the lactose of liquid crystal fiber element or direct compression.
The consisting of of this nonactive composition (parts by weight): absorbent 0.5-5.0, collapse powder 0.5-10.0, lubricant 0.5-5.0, diluent and/or bonding agent 10-80.
The Main Ingredients and Appearance of this troche for eliminating gastrointestinal vesicle and content are (mg): poly-dimethylamino silane 40, silicon dioxide 4, microcrystalline Cellulose 304, carboxymethyl starch sodium 8, Pulvis Talci 4.
The Main Ingredients and Appearance of this troche for eliminating gastrointestinal vesicle and content are (mg): poly-dimethylamino silane 50, silicon dioxide 6, lactose 294, carboxymethyl starch sodium 8, magnesium stearate 4.
The Main Ingredients and Appearance of this troche for eliminating gastrointestinal vesicle and content are (mg): the mixture 60 of dimethylamino silane and silicon dioxide, silicon dioxide 7, microcrystalline Cellulose 244, glucose 244, carboxymethyl starch calcium 16, magnesium stearate 16.
The Main Ingredients and Appearance of this troche for eliminating gastrointestinal vesicle and content are (mg: poly-two silane 80, silicon dioxide 8, microcrystalline Cellulose 391, fructose 97, carboxymethyl starch sodium 12, stearic acid 8.
The Main Ingredients and Appearance of this troche for eliminating gastrointestinal vesicle and content are (mg): mixture 40, silica 12, microcrystalline Cellulose 98, mannitol 390, carboxymethyl starch calcium 26, the magnesium stearate 6 of poly-dimethylamino silane 40, dimethylamino silane and silicon dioxide.
This manufacture method can be used for making quick-acting other lozenge medicines except that troche for eliminating gastrointestinal vesicle of needs.
Need other quick-acting lozenge medicated bags to draw together febrifuge, analgesic, hemorrhage, antibiotic medicine, first aid medicine.
Major advantage of the present invention is:
1, manufacture method of the present invention has changed traditional system ingot production method, create and earlier nonactive compositions such as excipient are made blank lozenge, again blank lozenge dipping is absorbed the manufacture method of the active drug of fixed amount, improve the disintegrate and the rate of release of active medicine greatly with the lozenge medicine of method manufacturing of the present invention, significantly improved the curative effect of medicine.
2, manufacture method of the present invention can also be used to make the lozenge of the quick-acting treatment various diseases of needs except being used to make the troche for eliminating gastrointestinal vesicle, and does not need to increase equipment investment and production cost, is a kind of brand-new manufacturing process technology.
3, control the content of active pharmaceutical ingredients in the manufacture method of the present invention easily, the pained medicine of suiting one's taste, desire reduces the content of its active medicine, only needs to adopt centrifugal method just can remove unnecessary active pharmaceutical ingredients, and is very convenient.
The present invention is further described below in conjunction with preferred embodiment:
Embodiment 1
With bonding agent microcrystalline cellulose etc. 3049, collapse powder 8g and absorbent silicon dioxide 4g mix homogeneously, sieve (30 order) removes coarse granule, adds lubricant Pulvis Talci 4g and puts into mixer mixing 5 minutes together, makes blank lozenge with Ingot pressing machine; Above-mentioned blank lozenge be impregnated in the poly-dimethylamino silane 40g of gastrointestinal froth breaking active medicine, make to absorb poly-dimethylamino silane, make troche for eliminating gastrointestinal vesicle.
For preventing blank lozenge dipping absorbing activity overdose, cause the mouthfeel bitterness, can adopt centrifugal method to remove the active medicine of excess, keep specific active medicine content, very convenient.
Embodiment 2
The Main Ingredients and Appearance of troche for eliminating gastrointestinal vesicle and content are (mg) in the present embodiment:
Gastrointestinal froth breaking active medicine is poly-dimethylamino silane 50
Absorbent is a silicon dioxide 6
Bonding agent is a lactose 294
Collapsing powder is carboxymethyl starch sodium 8
Lubricant is a magnesium stearate 4
Its manufacture method is identical with embodiment 1, so do not repeat.
Embodiment 3
The Main Ingredients and Appearance of troche for eliminating gastrointestinal vesicle and content are (mg) in the present embodiment:
Gastrointestinal active defoaming agent medicine is the mixture (Simethicon) 60 of dimethylamino silane and silicon dioxide
Absorbent is a silicon dioxide 7
Bonding agent is a microcrystalline Cellulose 244
Diluent is a glucose 244
Collapsing powder is carboxymethylcellulose calcium 16
Lubricant is a magnesium stearate 16
Its manufacture method is identical with embodiment 1, so do not repeat.
Embodiment 4
The Main Ingredients and Appearance of troche for eliminating gastrointestinal vesicle and content (mg) in the present embodiment:
Gastrointestinal active defoaming agent medicine is poly-dimethylamino silane 80
Absorbent is a silicon dioxide 8
Bonding agent is a microcrystalline Cellulose 391
Diluent is a fructose 97
Collapsing powder is sodium carboxymethyl cellulose 12
Lubricant is a stearic acid 8
Its manufacture method is identical with embodiment 1, so do not repeat.
Embodiment 5
The Main Ingredients and Appearance of troche for eliminating gastrointestinal vesicle and content (mg) in the present embodiment:
Gastrointestinal active defoaming agent medicine is the mixture 40 of poly-dimethylamino silane 40 and dimethylamino silane and silicon dioxide
Absorbent is a silica 12
Bonding agent is a microcrystalline Cellulose 98
Diluent is a mannitol 390
Collapsing powder is carboxymethylcellulose calcium 26
Lubricant is a magnesium stearate 6
Its manufacture method is identical with embodiment 1, so do not repeat.
The performance of product of the present invention and curative effect, the medicament that will have identical proportioning is tested its outward appearance, hardness, collapsibility and defoaming respectively with the lozenge of above-mentioned manufacture method manufacturing and the lozenge of manufacture method manufacturing commonly used, and test result sees Table 1: table 1
Wherein: I is for making ingot again behind nonactive and the active medicine mix homogeneously;
Mixed active pharmaceutical compositions when II is the system ingot;
III is a mixed active pharmaceutical compositions when putting in order ingot; Can clearly see following result from experimental data:
1, product of the present invention has gloss, and the product tarnish that common method is made;
2, product of the present invention collapses the product that the time of loosing makes well below common method, only uses 92 seconds, and the shortest need of common method 424 seconds, the longest is 805 seconds.
3, product foam time of the present invention is 15 seconds, and the product foam time that common method is made is all more than 120 seconds.
Conclusion is disintegrate and the rate of release that product of the present invention improves medicine greatly, reaches the purpose that improves curative effect.
Manufacture method of the present invention, can also be generalized to manufacturing needs other quick-acting lozenge medicines, for example febrifuge analgesic, antibiotic medicine, first aid medicine etc.Thereby the disintegrate and the rate of release that can improve medicine equally greatly improve the effect of curing the disease.