CN104523728A - Pharmaceutical composition for treating phthisis - Google Patents
Pharmaceutical composition for treating phthisis Download PDFInfo
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- CN104523728A CN104523728A CN201410629165.5A CN201410629165A CN104523728A CN 104523728 A CN104523728 A CN 104523728A CN 201410629165 A CN201410629165 A CN 201410629165A CN 104523728 A CN104523728 A CN 104523728A
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Abstract
The invention discloses a pharmaceutical composition for treating phthisis. The pharmaceutical composition is prepared with amentoflavone, dihydrogen morin, hemiphroside B and syringopicroside in proportion as crude medicines. Various dosage forms can be prepared according to a conventional preparation technology. The pharmaceutical composition overcomes the defects in the prior art and is obvious in phthisis treating curative effect and safe. A medicine preparing method is simple; cost is low; and clinical tests prove that the pharmaceutical composition has the obvious clinical effects on the phthisis.
Description
Technical field
The invention belongs to biomedicine field, particularly relate to one and treat phthisical pharmaceutical composition.
Background technology
Pulmonary tuberculosis is the chronic infectious disease causing morbidity after invading body by mycobacterium tuberculosis under certain condition.The situation is tense for current global tuberculosis prevention and treatment, and newly-increased 9,200,000 the tuberculosis cases in the whole world in 2006, have 1,700,000 people to die from tuberculosis for 2006.Phthisical treatment is based on chemotherapy, and tuberculosis immunological investigation is striden along in recent years, people has been had morbidity lungy, clinical process, prognosis and recurrence and is more fully familiar with.Due to the renewal of tuberculosis Immunology, the therapy that chemotherapy and immunization therapy combine becomes the effective Therapeutic mode of some patients.A large amount of in recent years Chinese medicine basic research display, treatment by Chinese herbs have sterilization, antibacterial, reduce toxicity, reduce drug resistance incidence rate and improve the advantages such as patient immune function.
In recent years, Drug-fast case bacterial strain and high resistant rate tubercule bacillus make refractory pulmonary tuberculosis increase rapidly.The liver toxicity deadly defect of Western medicine " omnidistance associating " chemotherapeutic modalities, western medicine pulmonary tuberculosis is limited to, Chinese medicine tuberculosis becomes the focus of concern, advantage comprises: one is differentiation of tcm, symptomatic treatment, first can mitigation symptoms, promotes the recovery of patient's resistance against diseases, alleviate complication, for patient establishes its good confidence.Two is that Chinese medicine compound not easily causes pathogenic bacteria drug resistance, has very large potentiality at treatment drug tolerance pulmonary tuberculosis with slowing down in tubercule bacillus speed of mutation.
Pulmonary tuberculosis, from the beginning of at lung, is then involved spleen kidney for a long time, is very then spread all over the five internal organs, shows as the weakened body resistance syndromes such as gas cloudy loss, hyperactivity of fire caused by deficiency of YIN, deficiency of both YIN and YANG in whole lysis.Pulmonary tuberculosis rule for the treatment of invigorating deficiency and tonifying vital QI, righting parasite killing.In treatment, should focus on adjusting tonifying the lung spleen kidney three dirty, as " reason empty unit mirror ": " control void and have three, lung spleen kidney is also, and lung is the sky of the five internal organs, and spleen is the mother of bones of the body collectively, and kidney is the source of all things on earth, and control lung and control spleen and control kidney, Zhi Laozhi road is finished ".
Amentoflavone (amentoflavone): CAS 1617-53-4, molecular formula C
30h
18o
10, molecular weight 538.46, antifungal (Aspergillus fumigatus, Botrytis cinerea and powder green trichoderma bacterium), Nucleoside-diphosphatase inhibitor.
Dihydromorin. (dihydromorin): CAS 18422-83-8, molecular formula C
15h
12o
7, molecular weight 304.3.
Herba hemipharagmatis heterophylli glycosides B(hemiphroside B), CAS 165338-28-3, molecular formula C
31h
38o
17, molecular weight 682.6.
Syringopicroside (syringopicroside): CAS 29118-80-7, molecular formula C
24h
30o
11, molecular weight 494.4884.There is antivirus action.
4 kinds of medicines structures of pharmaceutical composition of the present invention are as follows:
Amentoflavone (amentoflavone) Dihydromorin. (dihydromorin)
Herba hemipharagmatis heterophylli glycosides B(hemiphroside B)
Syringopicroside (syringopicroside).
Summary of the invention
The object of the invention is the deficiency overcoming background technology, provide one to treat phthisical pharmaceutical composition.
The present invention is achieved through the following technical solutions:
Of the present invention a kind of treat the crude drug of phthisical pharmaceutical composition composition and weight portion be:
Amentoflavone 1-10 weight portion Dihydromorin. 1-10 weight portion Herba hemipharagmatis heterophylli glycosides B1-10 weight portion syringopicroside 1-10 weight portion.
Of the present inventionly a kind ofly treat phthisical pharmaceutical composition the conventional method of galenic pharmacy can be adopted to be prepared into tablet, capsule, drop pill.
One of the present invention treats phthisical pharmaceutical composition, it is characterized in that being used for the treatment of pulmonary tuberculosis.
Compositions provided by the invention, is shown by tuberculosis Effect study in body, all has certain suppression or killing action to the tulase of Mycobacterium bovis, resistance to INH bacterium, resistance to RFP bacterium, resistance to SM bacterium and resistance to INH+RFP+SM.In Vitro Anti tuberculosis Effect study shows, has significant tuberculosis effect.
Detailed description of the invention
Treat phthisical pharmaceutical composition below by specific experiment example and embodiment to one to be described further, but be not limited to the present invention.
Embodiment 1: treat phthisical pharmaceutical composition
Composition and the weight portion for the treatment of the crude drug of phthisical pharmaceutical composition are:
Amentoflavone 1 weight portion Dihydromorin. 1 weight portion Herba hemipharagmatis heterophylli glycosides B5 weight portion syringopicroside 8 weight portion.
Embodiment 2: treat phthisical pharmaceutical composition
Composition and the weight portion for the treatment of the crude drug of phthisical pharmaceutical composition are:
Amentoflavone 10 weight portion Dihydromorin. 10 weight portion Herba hemipharagmatis heterophylli glycosides B1 weight portion syringopicroside 10 weight portion.
Embodiment 3: treat phthisical pharmaceutical composition
Composition and the weight portion for the treatment of the crude drug of phthisical pharmaceutical composition are:
Amentoflavone 4 weight portion Dihydromorin. 5 weight portion Herba hemipharagmatis heterophylli glycosides B10 weight portion syringopicroside 1 weight portion.
Embodiment 4: treat phthisical pharmaceutical composition
Composition and the weight portion for the treatment of the crude drug of phthisical pharmaceutical composition are:
Amentoflavone 6 weight portion Dihydromorin. 7 weight portion Herba hemipharagmatis heterophylli glycosides B8 weight portion syringopicroside 4 weight portion.
Embodiment 5: the preparation of tablet
Example 1 compositions 150g, adds starch 75g, mixing, granulates, dry, adds microcrystalline Cellulose 20g, magnesium stearate 2.5g, and mixing, is pressed into 1000, obtains present composition tablet.
Embodiment 6: the preparation of capsule
Example 2 compositions 165g, adds starch 65g, mixing, granulates, and dry, granulate, adds appropriate magnesium stearate, and mixing, obtains present composition capsule by encapsulated 1000.
Embodiment 7: the preparation of drop pill
Taking polyethylene glycol 6000 200g water-bath (80 DEG C) heating boils molten, add embodiment 3 compositions 50g, stirring, is coolant with liquid paraffin, puts in glass tubing (4*80cm), chilling temperature is 10 DEG C, drip internal-and external diameter is 7.0/2.0 (mm/mm), and drip is 2cm apart from liquid level, drips speed with per minute 50 for optimum condition, blot the condensing agent on drop pill surface with cotton, obtain present composition drop pill.
Experimental example 1: inside and outside tuberculosis effect
1. materials and methods
Test drug: embodiment 1 compositions prepared by the embodiment of the present invention 1, embodiment 2, embodiment 3, embodiment 4 method, embodiment 2 compositions, embodiment 3 compositions, embodiment 4 compositions, lot number is respectively: 20111012,20111013,20111014,20111015.Be made into the suspension of desired concn with distilled water before use for subsequent use, this test dose is pressed g compositions/kg and is calculated.Rifampicin (RPP) capsule: 0.15 g × 100, Chengdu Jin Hua pharmaceutcal corporation, Ltd produces, and lot number is 110912, valid until 2013-08, is made into the suspension of desired concn before use for subsequent use with 0.5%CMC.
Test strain H37RV standard bacteria (ATCC27294): cattle type mycobacterium; Single resistance to RFP bacterium; Single resistance to INH bacterium; Single resistance to SM bacterium; Resistance to INH+SM+RFP bacterium; Control branch center by CDC tuberculosis prophylaxis to provide.
Cavia porcellus: primary animal; Male and female half and half, body weight: 300 ~ 320 g.Production licence number: No. 15, is provided by institute of lab animals of Shandong Province.
2. method and result
2.1 impacts on bacterial growth
2.1.1 the external mensuration affecting minimal inhibitory concentration (MIC) on tulase growth: adopt test tube method, medicine is added respectively after in the logical culture medium of Soviet Union, add the bacterium liquid (1mg/ml of timing, often prop up inoculation 0.1 m1), after cultivating 2 weeks through 37 DEG C, often prop up suction 0.1 ml transferred species and establish blank pipe in 2 improvement Roche (L-J) medium slant simultaneously.Cultivate in the logical culture medium of pastille Soviet Union and within 2 weeks, see that the Cmin of bacterial growth is minimal inhibitory concentration.The mensuration of minimal bactericidal concentration (MBC): the culture of bacterial growth will be had no in the logical culture medium of Soviet Union, draw 0.05 ml respectively and be inoculated in improvement Roche (L-J) inclined-plane, cultivate after 4 weeks through 37 DEG C, the minimum dilution drug level that the clump count sum in 2 medium slant inoculated is less than 5 is the minimal bactericidal concentration of this medicine.
The external impact on tulase growth of table 1
As seen from Table 1, the tulase of the present composition to Mycobacterium bovis, resistance to INH bacterium, resistance to RFP bacterium, resistance to SM bacterium and resistance to INH+RFP+SM all has certain suppression or killing action.
2.1.2 the effect to tuberculosis infection Cavia porcellus in body: Cavia porcellus is tested after feminine gender through PPD, random packet, gavage embodiment 1 compositions, embodiment 2 compositions, embodiment 3 compositions, embodiment 4 compositions, be 50mg/kg respectively; Rifampicin 50mg/kg and equivalent distilled water, 1 time/d, continuous 45D.2 weeks upon administration, except matched group, make zoogenetic infection tubercule bacillus each globefish groin subcutaneous injection bacteria suspension 0.5mL/ (bacteria suspension of 1mg/ml is diluted 100 times).After last administration, 24 h put to death animal, dissect the tubercle that naked eyes count each internal organs, get lungs, liver and spleen claim weight in wet base and calculate its organ index, then take a certain amount of tissue and do homogenate to do tulase cultivation, each tissue is placed in 10% formalin simultaneously and fixes and cut into slices to do HE dyeing and z-N dyeing coloured silk.The results are shown in Table 2,3,4.
Table 2 is on the impact of tuberculosis Organs of Guinea Pigs index
| Group | Dosage (mg/kg) | Number of animals (only) | Liver index (g/100g) | Index and spleen index (g/100g) | Lungs index (g/100g) |
| Matched group | 10 | 3.57±0.42 ** | 0.18±0.03 ** | 0.94±0.15 ** | |
| Model group | 10 | 6.23±1.02 | 0.64±0.43 | 1.63±0.63 | |
| Rifampicin | 50mg/kg | 10 | 4.23±1.01 ** | 0.17±0.01 ** | 0.92±0.13 ** |
| Embodiment 1 compositions | 50 | 10 | 4.43±0.81 ** | 0.32±0.22 ** | 0.93±0.44 ** |
| Embodiment 2 compositions | 50 | 10 | 5.51±1.00 | 0.56±0.27 | 1.27±0.42 |
| Embodiment 3 compositions | 50 | 10 | 4.96±0.85 * | 0.25±0.32 * | 1.34±0.37 * |
| Embodiment 4 compositions | 50 | 10 | 5.50±1.03 | 0.57±0.28 | 1.28±0.45 |
Note: compare with model group:
*p<0.05,
*p<0.0l.
As seen from Table 2, Cavia porcellus is after infection tulase, and its liver index, index and spleen index and lungs index all significantly increase, and the present composition can reduce tuberculosis Guinea Pig Liver index, compares have significant difference with model group; The present composition has the trend reducing tuberculosis Guinea Pig Liver index and lungs index, compares have significant difference with model group; The present composition significantly can reduce tuberculosis Cavia porcellus index and spleen index, compares have significant difference with model group.
Table 3 is on the impact of tuberculosis Cavia porcellus body weight and pulmonary tuberculosis tuberosity quantity
| Group | Dosage (mg/kg) | Number of animals (only) | Body weight (g) | Pulmonary tuberculosis tuberosity number of animals (only) under naked eyes |
| Matched group | 10 | 306.2±23.17 ** | 0 ** | |
| Model group | 10 | 234.8±35.33 | 9 | |
| Rifampicin | 50mg/kg | 10 | 316.4±33.22 ** | 0 ** |
| Embodiment 1 compositions | 50 | 10 | 255.8±45.87 | 1 ** |
| Embodiment 2 compositions | 50 | 10 | 242.6±38.67 | 3 ** |
| Embodiment 3 compositions | 50 | 10 | 261.9±39.32 | 1 ** |
| Embodiment 4 compositions | 50 | 10 | 253.8±35.45 | 2 ** |
Note: compare with model group:
*p<0.05,
*p<0.0l.
As seen from Table 3, Cavia porcellus is after infection tulase, and its body weight significantly reduces, and pulmonary forms a large amount of macroscopic tubercle simultaneously; The present composition all has no significant effect tuberculosis Cavia porcellus body weight, compares no difference of science of statistics with model group, but the present composition can reduce the macroscopic tubercle of Cavia porcellus pulmonary, compares have significant difference with model group.
Table 4 is on the impact of tuberculosis Cavia porcellus spleen, lung tissue cultivation tulase quantity
| Group | Dosage (mg/kg) | Number of animals (only) | Pulmonary tuberculosis bacterium (10*/g tissue) | Splenic tuberculosis bacterium (10*/g tissue) |
| Matched group | 10 | 0 ** | 0 ** | |
| Model group | 10 | 32.7±13.33 | 33.4±14.23 | |
| Rifampicin | 50mg/kg | 10 | 0.0003±0.0002 ** | 0.0004±0.0003 ** |
| Embodiment 1 compositions | 50 | 10 | 0.09±0.01 ** | 0.11±0.04 ** |
| Embodiment 2 compositions | 50 | 10 | 0.39±0.18 ** | 0.42±0.15 ** |
| Embodiment 3 compositions | 50 | 10 | 0.07±0.02 ** | 0.09±0.04 ** |
| Embodiment 4 compositions | 50 | 10 | 0.13±0.05 ** | 0.15±0.06 ** |
Note: compare with model group:
*p<0.05,
*p<0.0l.
As seen from Table 4, the Cavia porcellus lungs of tubercle bacillus affection and spleen all have a large amount of tulases; And the present composition significantly can reduce the tulase quantity of tuberculosis Cavia porcellus lungs and spleen, compare with model group and have significant difference.
Claims (7)
1. treat a phthisical pharmaceutical composition, it is characterized in that the composition of the crude drug making this pharmaceutical composition and weight portion are:
Amentoflavone 1-10 weight portion Dihydromorin. 1-10 weight portion Herba hemipharagmatis heterophylli glycosides B1-10 weight portion syringopicroside 1-10 weight portion.
2. according to claim 1: one treats phthisical pharmaceutical composition, it is characterized in that composition and the weight portion of the crude drug making this pharmaceutical composition are:
Amentoflavone 1 weight portion Dihydromorin. 1 weight portion Herba hemipharagmatis heterophylli glycosides B5 weight portion syringopicroside 8 weight portion.
3. according to claim 1: one treats phthisical pharmaceutical composition, it is characterized in that composition and the weight portion of the crude drug making this pharmaceutical composition are:
Amentoflavone 10 weight portion Dihydromorin. 10 weight portion Herba hemipharagmatis heterophylli glycosides B1 weight portion syringopicroside 10 weight portion.
4. according to claim 1: one treats phthisical pharmaceutical composition, it is characterized in that composition and the weight portion of the crude drug making this pharmaceutical composition are:
Amentoflavone 4 weight portion Dihydromorin. 5 weight portion Herba hemipharagmatis heterophylli glycosides B10 weight portion syringopicroside 1 weight portion.
5. according to claim 1: one treats phthisical pharmaceutical composition, it is characterized in that composition and the weight portion of the crude drug making this pharmaceutical composition are:
Amentoflavone 6 weight portion Dihydromorin. 7 weight portion Herba hemipharagmatis heterophylli glycosides B8 weight portion syringopicroside 4 weight portion.
6. one according to claim 1 treats phthisical pharmaceutical composition, and the conventional method of galenic pharmacy can be adopted to be prepared into tablet, capsule, drop pill.
7. one as claimed in claim 1 treats phthisical pharmaceutical composition, it is characterized in that being used for the treatment of pulmonary tuberculosis.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410629165.5A CN104523728A (en) | 2014-11-11 | 2014-11-11 | Pharmaceutical composition for treating phthisis |
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| CN201410629165.5A CN104523728A (en) | 2014-11-11 | 2014-11-11 | Pharmaceutical composition for treating phthisis |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101214256A (en) * | 2008-01-14 | 2008-07-09 | 李永吉 | Syringopicroside tablet and preparation technique thereof |
| CN101744805A (en) * | 2009-12-21 | 2010-06-23 | 沈阳药科大学 | Novel use of natural amentoflavone in curing viral diseases |
| CN103211732A (en) * | 2013-04-28 | 2013-07-24 | 江南大学 | Preparation method and application of mixture with tyrosinase inhibitory activity |
-
2014
- 2014-11-11 CN CN201410629165.5A patent/CN104523728A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101214256A (en) * | 2008-01-14 | 2008-07-09 | 李永吉 | Syringopicroside tablet and preparation technique thereof |
| CN101744805A (en) * | 2009-12-21 | 2010-06-23 | 沈阳药科大学 | Novel use of natural amentoflavone in curing viral diseases |
| CN103211732A (en) * | 2013-04-28 | 2013-07-24 | 江南大学 | Preparation method and application of mixture with tyrosinase inhibitory activity |
Non-Patent Citations (1)
| Title |
|---|
| 刘婕等: "苯丙素苷类化合物防治神经退行性疾病的研究进展", 《药物评价研究》 * |
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Application publication date: 20150422 |