CN100367935C - Oral drop pills in use for treating diseases of bacterial infection and preparation method - Google Patents
Oral drop pills in use for treating diseases of bacterial infection and preparation method Download PDFInfo
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- CN100367935C CN100367935C CNB2005100049536A CN200510004953A CN100367935C CN 100367935 C CN100367935 C CN 100367935C CN B2005100049536 A CNB2005100049536 A CN B2005100049536A CN 200510004953 A CN200510004953 A CN 200510004953A CN 100367935 C CN100367935 C CN 100367935C
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Abstract
The present invention relates to a medicinal composition having the functions of clearing heat, removing toxicity, relieving inflammation and relieving dysentery and used for treating bacterium infectious diseases such as acute bacterial dysentery, enteritis, upper respiratory tract infection, swelling and pain in the throat, acute and chronic tonsillitis, etc., particularly a medicinal composition oral drop pill preparation prepared by using folium syringae as the traditional Chinese medicinal raw material. The present invention aims to overcome the defects of the existing oral medicine preparation for treating bacterium infectious diseases such as acute bacterial dysentery, enteritis, upper respiratory tract infection, swelling and pain in the throat, acute and chronic tonsillitis, etc. and provide a medicinal composition oral preparation, namely an inflammation relieving drop pill, which has the advantages of high bioavailability, quick medicine release, high effectual speed, low price and no pollution during production. The inflammation relieving drop pill of the present invention is prepared by using the traditional Chinese medicine of folium syringae as the raw material and a medicinal vector used as a matrix.
Description
Technical field
The present invention relates to a kind of heat-clearing and toxic substances removing that has, the anti-inflammtory anti-dysentery effect, be used for the treatment of acute bacillary dysentery, enteritis and upper respiratory tract infection, laryngopharynx swelling and pain, the pharmaceutical composition of bacterial infection diseases such as acute and chronic tonsillitis particularly is a kind of drug composition oral dropping pill formulation that raw material of Chinese medicine is prepared from the Folium Caryophylli.
Background technology
According to drug standard WS promulgated by the ministries or commissions of the Central Government
3The anti-inflammation medicine sheet that the preparation method that provides among-the B-1760-94 is prepared from, it is a kind of heat-clearing and toxic substances removing that has, the anti-inflammtory anti-dysentery effect, be used for the treatment of acute bacillary dysentery, enteritis and upper respiratory tract infection, laryngopharynx swelling and pain, the oral tablet of bacterial infection diseases such as acute and chronic tonsillitis, through clinical verification, determined curative effect is the common drug that clinical and family is used for the treatment of this type of disease.
Below be drug standard WS
3Prescription that provides among-the B-1760-94 and technology and brief description:
Method for making: get Folium Caryophylli 100g, decoct with water secondary, 1.5h for the first time, 1h for the second time, collecting decoction, filter, it is 1.25 (80) clear paste that filtrate decompression is concentrated into relative density, adds Flos Caryophylli fine powder 10g, and mixing is in the 60-80 drying, be ground into fine powder, granulate, compacting is in blocks, promptly.
Function cures mainly: heat-clearing and toxic substances removing, anti-inflammtory anti-dysentery.Be used for acute bacillary dysentery, enteritis and upper respiratory tract infection, laryngopharynx swelling and pain, bacterial infection diseases such as acute and chronic tonsillitis.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially the oral formulations of Chinese medicine, exist all after taking that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.
In addition, conventional peroral dosage form as tablet, capsule etc., because the technology of granulation is arranged, therefore can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.Moreover, the complex manufacturing of conventional oral formulations, production cost is higher, thereby patient's drug cost is also improved thereupon, is unfavorable for improving the ability of seeking medical advice of extensive patients, also is unfavorable for improving the general health level of society.
Summary of the invention
Purpose of the present invention, be to replenish existing be used for the treatment of acute bacillary dysentery, enteritis and upper respiratory tract infection, laryngopharynx swelling and pain, the deficiency of the oral drug preparation of bacterial infection diseases such as acute and chronic tonsillitis, a kind of bioavailability height is provided, and has a quick release, produce effects is cheap fast, and free of contamination aborning drug composition oral preparation oral administration dripping pill.Oral administration dripping pill involved in the present invention is a raw material with the Chinese medicine Folium Caryophylli, is prepared from the pharmaceutically suitable carrier as substrate.Be prepared by the following technical solutions, can obtain oral administration dripping pill involved in the present invention:
[preparation method]
1. the preparation of drug extract: it is an amount of to get Folium Caryophylli, decocts with water secondary, 1.5h for the first time, and 1h for the second time, collecting decoction filters, and filtrate decompression is concentrated into the clear paste that relative density is 1.25 (80 ℃), in 60 ℃～80 ℃ dryings, is ground into fine powder, promptly;
2. substrate: Polyethylene Glycol
(2000～20000), one or more the mixture in pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9;
4. according to the given ratio of prescription, accurately take by weighing drug extract and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing drug extract and substrate and/or emulsion and/or suspension;
5. adopt homemade or general drop pill machine (as the TZDW-1 type drop pill machine of Changzheng Tianmin High Science ﹠ Technology Co., Ltd., Beijing's production), and the temperature control system of adjustment drop pill machine, make the water dropper temperature heating of drop pill machine and remain on (50～90) ℃, the temperature cooling of condensing agent also remains on (40～-5) ℃;
6. when treating that the temperature of condensing agent in dropping-pill machine head and the condensation column is stable respectively and reaching desired state of temperature, fused solution and/or the emulsion and/or the suspension that will contain drug extract and substrate, place in the water dropper jar of drop pill machine, splash in the condensing agent, condensing agent can be any one in liquid paraffin, methyl-silicone oil, the vegetable oil;
7. will shrink the drop pill taking-up of molding by the outlet of drop pill machine, remove the surface condensation agent, be drying to obtain.
Beneficial effect
According to drug standard WS promulgated by the ministries or commissions of the Central Government
3The anti-inflammation medicine sheet that the preparation method that provides among-the B-1760-94 is prepared from, it is a kind of heat-clearing and toxic substances removing that has, the anti-inflammtory anti-dysentery effect, be used for the treatment of acute bacillary dysentery, enteritis and upper respiratory tract infection, laryngopharynx swelling and pain, the oral tablet of bacterial infection diseases such as acute and chronic tonsillitis, through clinical verification, determined curative effect is the common drug that clinical and family is used for the treatment of this type of disease.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially the oral formulations of Chinese medicine, exist all after taking that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.
In addition, conventional peroral dosage form as tablet, capsule etc., because the technology of granulation is arranged, therefore can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.Moreover, the complex manufacturing of conventional oral formulations, production cost is higher, thereby patient's drug cost is also improved thereupon, is unfavorable for improving the ability of seeking medical advice of extensive patients, also is unfavorable for improving the general health level of society.
Oral administration dripping pill involved in the present invention is compared with the Rhizoma Bistortae sheet has following beneficial effect:
1. oral administration dripping pill involved in the present invention; utilize surfactant to be substrate; the extract of pharmaceutically active ingredient is made solid dispersion in containing Folium Caryophylli, makes medicine be molecule, colloid or microcrystalline state and is scattered in the substrate, and the total surface area of medicine increases; and substrate is hydrophilic; medicine is had wetting action, can make that medicine is rapidly molten to loose into microgranule or solution, thereby make the dissolving of medicine and absorb and accelerate; thereby improved bioavailability, brought into play efficient, quick-acting effects etc.
2. oral administration dripping pill involved in the present invention, contact promptly with saliva and to dissolve rapidly, and absorb by oral mucosa, not only rapid-action, and the influence of not taken food, promptly all can containing take after meal ante cibum, can not produce any residual harmful substance at gastric yet, thereby make that patient's medication is safer, also have medication convenience, characteristic of accurate simultaneously.
3. oral administration dripping pill involved in the present invention mixes the extract that contains active constituents of medicine mutually with molten matrix, splashes in the not miscible condensed fluid and makes.Therefore, the stability of drug height, not facile hydrolysis, oxidation, and the operation be under liquid state, to carry out, no dust pollution is not subject to the influence of crystal formation, thereby has guaranteed the quality of medicine, has increased stability.
4. production technology, the equipment of preparation drop pill are simple, easy to operate, the automaticity height, and labor intensity is low, the production efficiency height.Workshop does not have dust simultaneously, helps labor protection and environmental protection yet.
5. the production cost of preparation drop pill is usually with about 50% of other oral formulations of kind, and compares with oral liquid, and the dosage of drop pill is accurate, thereby makes the patient take metering control easily.
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of oral administration dripping pill of the present invention.
First group: the test of single-matrix
1. the preparation of drug extract: it is an amount of to get Folium Caryophylli, decocts with water secondary, 1.5h for the first time, and 1h for the second time, collecting decoction filters, and filtrate decompression is concentrated into the clear paste that relative density is 1.25 (80 ℃), in 60 ℃～80 ℃ dryings, is ground into fine powder, promptly;
2. substrate: Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), one or more the mixture in pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the oral administration dripping pill of different size.
[result of the test]
Test 1: for observe drug extract and different substrates when 1: 1 the proportioning prepared oral administration dripping pill in qualitative difference, according to 1: 1 ratio, with drug extract respectively with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 15 groups of different experimental results and see Table 1.
Test 2: for observe drug extract and different substrates when 1: 3 the proportioning prepared oral administration dripping pill in qualitative difference, according to 1: 3 ratio, with drug extract respectively with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 15 groups of different experimental results and see Table 2.
Test 3: for observe drug extract and different substrates when 1: 9 the proportioning prepared oral administration dripping pill in qualitative difference, according to 1: 9 ratio, with drug extract respectively with Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 15 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. the preparation of drug extract: it is an amount of to get Folium Caryophylli, decocts with water secondary, 1.5h for the first time, and 1h for the second time, collecting decoction filters, and filtrate decompression is concentrated into the clear paste that relative density is 1.25 (80 ℃), in 60 ℃～80 ℃ dryings, is ground into fine powder, promptly;
2. substrate:
2.1 Polyethylene Glycol---English name Macrogol,
2.2 polyoxyethylene stearate 40 esters---English name Polyoxyl (40) Stearate,
Molecular formula is with C
17H
35COO (CH
2CH
2O)
aH represents that n is about 40,
2.3 poloxamer---English name Poloxamer, polyoxyethylene poly-oxygen propylene aether,
Molecular formula HO (C
2H
4O)
a(C
3H
6O)
b(C
2H
4O)
cH,
The sodium salt of the starch carboxymethyl ester that 2.4 carboxymethyl starch sodium---English name Carboxymethylstach Sodium, starch generates with the monoxone effect under alkali condition,
2.5 betacyclodextrin---English name Betacyclodextrin, molecular formula C
6H
10O
5, this product is that ring dextrin glucosyl transferase acts on 7 glucoses that starch generates with α-1, the bonded cyclic oligosaccharide of 4-glycosidic bond;
3. proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the oral administration dripping pill of different size.
[result of the test]
Test 4: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared oral administration dripping pill when 1: 1 the proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, according to 1: 1 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 4.
Test 5: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared oral administration dripping pill when 1: 3 the proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, according to 1: 3 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 5.
Test 6: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared oral administration dripping pill when 1: 9 the proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, according to 1: 9 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 6.
Test 7: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared oral administration dripping pill when 1: 1 the proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, according to 1: 1 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 7.
Test 8: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared oral administration dripping pill when 1: 3 the proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, according to 1: 3 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 8.
Test 9: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared oral administration dripping pill when 1: 9 the proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, according to 1: 9 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 9.
Test 10: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained oral administration dripping pill when 1: 1 proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, according to 1: 1 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 10.
Test 11: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained oral administration dripping pill when 1: 3 proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, according to 1: 3 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 11.
Test 12: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained oral administration dripping pill when 1: 9 proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, according to 1: 9 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 12.
The group practices of table 1 drug extract and single-matrix
(drug extract: substrate=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 2000 | 50.0 | 62 | ＜30 | ＞10 | + |
| Polyethylene Glycol 4000 | 50.0 | 73 | ＜30 | ＞10 | + |
| Polyethylene Glycol 6000 | 50.0 | 75 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 8000 | 50.0 | 74 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 10000 | 50.0 | 77 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 20000 | 50.0 | 79 | ＜30 | ＞10 | ++ |
| Polyoxyethylene stearate 40 esters | 50.0 | 76 | ＜30 | ＞10 | ++ |
| Betacyclodextrin | 50.0 | 69 | ＜30 | ＞10 | + |
| Poloxamer | 50.0 | 78 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium | 50.0 | 70 | ＜30 | ＞10 | + |
| Sodium lauryl sulphate | 50.0 | 73 | ＞30 | ＞10 | + |
| Stearic acid | 50.0 | 62 | ＞30 | ＞10 | ++ |
| Sodium stearate | 50.0 | 60 | ＞30 | ＞10 | ++ |
| Glycerin gelatine | 50.0 | 61 | ＞30 | ＞10 | + |
| Lac | 50.0 | 61 | ＞30 | ＞10 | + |
The group practices of table 2 drug extract and single-matrix
(drug extract: substrate=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 2000 | 25.0 | 80 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 25.0 | 87 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 25.0 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 25.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 25.0 | 90 | ＜30 | ＜10 | ++ |
| Betacyclodextrin | 25.0 | 82 | ＜30 | ＞10 | ++ |
| Poloxamer | 25.0 | 88 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 25.0 | 83 | ＜30 | ＞10 | +++ |
| Sodium lauryl sulphate | 25.0 | 76 | ＜30 | ＞10 | ++ |
| Stearic acid | 25.0 | 74 | ＞30 | ＞10 | +++ |
| Sodium stearate | 25.0 | 71 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 25.0 | 71 | ＞30 | ＞10 | +++ |
| Lac | 25.0 | 71 | ＞30 | ＞10 | +++ |
The group practices of table 3 drug extract and single-matrix
(drug extract: substrate=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 2000 | 10.0 | 81 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 10.0 | 88 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 10.0 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 10.0 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 10.0 | 91 | ＜30 | ＜10 | ++ |
| Betacyclodextrin | 10.0 | 84 | ＜30 | ＞10 | ++ |
| Poloxamer | 10.0 | 87 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 10.0 | 84 | ＜30 | ＞10 | +++ |
| Sodium lauryl sulphate | 10.0 | 78 | ＜30 | ＞10 | +++ |
| Stearic acid | 10.0 | 75 | ＞30 | ＞10 | +++ |
| Sodium stearate | 10.0 | 73 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 10.0 | 73 | ＞30 | ＞10 | +++ |
| Lac | 10.0 | 72 | ＞30 | ＞10 | +++ |
The group practices of table 4 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | 50 | 83 | ＜30 | ＞10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 50 | 83 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 50 | 80 | ＜30 | ＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 50 | 74 | ＜30 | ＞10 | + |
The group practices of table 5 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | 25 | 89 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 25 | 88 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 25 | 84 | ＜30 | ＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 25 | 80 | ＜30 | ＞10 | ++ |
The group practices of table 6 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | 10 | 90 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 10 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 10 | 88 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 10 | 83 | ＜30 | ＞10 | +++ |
The group practices of table 7 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | 50 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 50 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 50 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 50 | 87 | ＜30 | ＜10 | ++ |
The group practices of table 8 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | 25 | 93 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 25 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 25 | 91 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 25 | 88 | ＜30 | ＜10 | +++ |
The group practices of table 9 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | 10 | 93 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 10 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 10 | 92 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 10 | 89 | ＜30 | ＜10 | +++ |
The group practices of table 10 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | 50 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 50 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 50 | 87 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 50 | 84 | ＜30 | ＞10 | +++ |
The group practices of table 11 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | 25 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 25 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 25 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 25 | 87 | ＜30 | ＜10 | +++ |
The group practices of table 12 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | 10 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 10 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 10 | 91 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 10 | 91 | ＜30 | ＜10 | +++ |
1. can be seen by the result in the table: when the ratio of drug extract and substrate was 1: 1, its rounding rate, the ball method of double differences was different and index such as hardness is all undesirable, and dissolve scattered time limit influenced not obvious.
2. when the ratio of drug extract and substrate is 1: 3, the rounding rate, the ball method of double differences is different and index such as hardness slightly all begins to enter preferable state.
3. when the ratio of drug extract and substrate is 1: 9, the rounding rate, the ball method of double differences is different and index such as hardness improves not obvious.
4. the general effect of composite interstitial substance is better than single-matrix.
5. the hardness method for expressing in the subordinate list adopts drop pill is placed on the glass plate, press...withes one's finger it, observes its metamorphosis."+" expression flicking promptly is out of shape, " ++ " expression distortion of firmly pressing, and " +++" expression is indeformable by it.
Claims (2)
1. an oral administration dripping pill for the treatment of bacterial infection disease is a raw material with the Chinese medicine Folium Caryophylli, is prepared from the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1) it is an amount of to get Folium Caryophylli, decocts with water secondary, and 1.5 hours for the first time, 1 hour for the second time, collecting decoction filters, and it is 1.25 clear paste that filtrate is evaporated to relative density in 80 ℃, in 60 ℃～80 ℃ dryings, be ground into fine powder, promptly get the extract that contains the Folium Caryophylli effective ingredient, standby;
(2) described substrate is Macrogol 2000 or Macrogol 4000 or polyethylene glycol 6000 or Polyethylene Glycol 8000 or cetomacrogol 1000 0 or Macrogol 2000 0 and polyoxyethylene stearate 40 esters, and the mixture of Macrogol 2000 or Macrogol 4000 or polyethylene glycol 6000 or Polyethylene Glycol 8000 or cetomacrogol 1000 0 or Macrogol 2000 0 and carboxymethyl starch sodium; By weight, the ratio of polyoxyethylene stearate 40 esters or carboxymethyl starch sodium and described Polyethylene Glycol is 1: 1～1: 10, describedly contains the extract of Folium Caryophylli effective ingredient and the ratio of substrate is 1: 1～1: 3;
(3) take by weighing described extract and substrate according to aforementioned proportion, be placed on heating while stirring in the heating container, until the fused solution or emulsion or the suspension that obtain containing described extract and substrate, standby;
(4) temperature control system of adjustment drop pill machine makes the water dropper heating of drop pill machine and maintains the temperature at 50 ℃～90 ℃, and the condensing agent cooling also maintains the temperature at 40 ℃～-5 ℃;
When (5) treating that dropping-pill machine head and condensing agent reach described state of temperature respectively, will contain fused solution or the emulsion or the suspension of described extract and substrate, place in the water dropper jar of drop pill machine, splash in the condensing agent, shrink molding promptly.
2. oral administration dripping pill as claimed in claim 1 is characterized in that: described condensing agent be methyl-silicone oil or/and liquid paraffin or/and vegetable oil.
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| CNB2005100049536A CN100367935C (en) | 2005-01-31 | 2005-01-31 | Oral drop pills in use for treating diseases of bacterial infection and preparation method |
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| CN100367935C true CN100367935C (en) | 2008-02-13 |
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| CN108714163A (en) * | 2018-08-24 | 2018-10-30 | 绥化学院 | A kind of clove leaf syrup and preparation method thereof for treating abscess of throat |
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Non-Patent Citations (1)
| Title |
|---|
| 中华人民共和国卫生部药品标准中药成方制剂第9册. 100，中华人民共和国药典委员会. 1994 * |
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Assignee: Jiangsu Zhengda Fenghai Pharmaceutical Co., Ltd. Assignor: Beijing Zhengda Oasis Medicine Technology Co., Ltd. Contract record no.: 2011320000177 Denomination of invention: Oral drop pills in use for treating diseases of bacterial infection and preparation method Granted publication date: 20080213 License type: Exclusive License Open date: 20050831 Record date: 20110308 |
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