CN1056059C - Prescription for curing gonorrhea and preparation thereof - Google Patents
Prescription for curing gonorrhea and preparation thereof Download PDFInfo
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- CN1056059C CN1056059C CN96115230A CN96115230A CN1056059C CN 1056059 C CN1056059 C CN 1056059C CN 96115230 A CN96115230 A CN 96115230A CN 96115230 A CN96115230 A CN 96115230A CN 1056059 C CN1056059 C CN 1056059C
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Abstract
The present invention relates to a capsule for treating gonorrhea, which is composed of rifampin, methylbenzylpyrimidine, sodium bicarbonate and gentamycin sulfate. The capsule for treating gonorrhea can be obtained by uniformly mixing the medicine powder and filling the capsule with the medicine powder. The medicine has an obvious treatment effect on a patient who is concurrently infected by chlamydia trachomatis and urine decomposing mycoplasma, and is particularly sensitive to diplococcus infection of gonorrhea. The present invention has better effects on staphylococcus aureus, escherichia coli and diplococcus pneumoniae, is suitable for treating urinary system infection, and price is lower.
Description
The present invention relates to a kind of prescription and processing technology thereof for the treatment of the gonorrhea medicine.
Gonorrhea is the sexually transmitted disease that is caused by gonorrhea diplococcus, it mainly damages the urogenital organ, treat this sick medicine kind though sickness rate accounts for the sexually transmitted disease (STD) first place more, but price is higher, need about 120 yuan a course of treatment, to infecting the patient that chlamydia trachomatis and urine decompose mycoplasma, needs prescribe medicine respectively, and the toxic and side effects of medicine is stronger, and patient is caused very big burden.
The purpose of this invention is to provide a kind ofly has significant curative effect simultaneously to infecting the patient that chlamydia trachomatis and urine decomposes mycoplasma simultaneously, and low-cost sweeping drenched capsular prescription and processing technology thereof.
The object of the present invention is achieved like this:
Sweep and drench capsular prescription, the ratio between its composition and each component following (weight ratio):
Rifampicine: 4
Methyl benzyl Aminometradine: 1-1.5
Sodium bicarbonate: 2-2.5
Gentamycin sulfate: 1-1.5
Described capsular processing technology is that fill promptly with behind the above-mentioned each component medicamental pulverata mixing.
Rifampicine has broad-spectrum antibacterial action, to gram-positive cocci particularly drug-resistant staphylococcus aureus very strong antibacterial action is arranged, also inhibited to gram negative bacteria, some virus and chlamydia trachomatis, oral absorption rapidly and fully, blood drug level reached the peak in 1-2 hour, effective blood drug concentration can be kept 8-12 hour, and penetration power is strong, can enter cell.Methyl benzyl Aminometradine is effective to multiple Gram-positive and negative bacteria, can strengthen multiple antibiotic such as gentamycin, concentration exceeds 100 times of plasma concentration in the urine, and gentamycin is widely used in the treatment sensitive organism and infects particularly gram negative bacteria, and simultaneously urine being decomposed mycoplasma infection has better curative effect.Sodium bicarbonate and gentamycin partner treatment urinary tract infection can strengthen its antibacterial action, can reduce the poison of first piperazine power mycin simultaneously and pay effect.
The present invention infects responsive especially to gonorrhea diplococcus, staphylococcus aureus, escherichia coli and Diplococcus pneumoniae all there is better inhibition effect, particularly infecting chlamydia trachomatis simultaneously and urinating decomposition mycoplasma person has significant curative effect, is particularly useful for urinary system infection.
Medicine of the present invention is through acute toxicity test in mice, and process and result are as follows:
Get the white mice that weight is 20 ± 2g, male and female half and half, provide by Institute of Basic Medical Sciences, Liaoning Province, after white mice is got by animal housing, normally raise and observed no abnormally in 2 days, be divided into 11 groups at random, wherein 1 group is the blank group, every group of 10 animals, male and female half and half, divide into groups, dye pharmaceutical quantities and dosage sees Table 1:
Pharmaceutical quantities and dosage minute ml/g medicine mg of tested material dosage logarithm administration concentration gavage amount number of animals dosage group mg/kg dosage mg/ml distilled water ml1 630 2.7243 26.50 0.02 10 530 202 695 2.8420 34.75 0.02 10 695 203 911 2.9597 45.55 0.02 10 911 204 1,195 3.0774 69.75 0.02 10 1,195 205 1,567 3.1951 78.35 0.02 10 1,567 206. 2,054 3.3128 102.70 0.02 10 2,054 207 2,694 3.4305 134.70 0.02 10 2,694 208 3,533 3.5428 176.65 0.02 10 3,533 209 4,633 3.6659 231.65 0.02 10 4,633 2,010 6,075 3.7836 303.75 0.02 10 6,075 2011 0.00-0.00 0.02 10 0.00 20 are dyed in table 1 grouping
Through gastric infusion, irritating the stomach amount is 0.02ml/g, and water is can't help in administration fasting in preceding 12 hours, irritates fasting in 3 hours behind the stomach, observes seven days, and whether record animal dead situation, and dissect dead animal is checked deadly for other reason.
Calculate LD50 and 95% credibility interval with karber method (Guan Shi method), the results are shown in Table 2: table 2 result and karber method ask a LD50 computational chart minute tested material dosage log10 dose number of animals dead animal to count death rate pi+pi+1 group mg/kg x n ri pi1 530 2.7243 10 0 0.00 0.202 695 2.8420 10 2 0.20 0.503 911 2.9597 10 3 0.30 0.804 1,195 3.0774 10 5 0.50 1.105 1,567 3.1951 10 6 0.60 1.306 2,054 3.3128 10 7 0.70 1.407 2,694 3.4305 10 7 0.70 1.608 3,533 3.5482 10 9 0.90 1.809 4,633 3.6659 10 9 0.90 1.9010 6,075 3.7836 10 10 1.00 ∑s 58 5.8 10.6
Carrying out acute toxicity test in mice with medicine of the present invention is 1444mg/kg with Guan Shi method calculating LD50, and 95% credibility interval is 1166.53mg/kg-1789.38mg/kg.
As follows with dish dilution method to sensitivity testing process of the present invention and result:
Gonococcus provides (No. 92402) by Nat'l Pharmaceutical ﹠ Biological Products Control Institute, the MH culture medium is provided by the health and epidemic prevention check of the military region, Zhejiang Province rear-service department, lot number 950509, the quick GC medium in osmanthus is provided by sexually transmitted disease (STD) research department, skin disease prevention and treatment institute, Guangxi, lot number 950600.
Experimental technique
1. bacterium liquid preparation, the gonococcus recovery, after double going down to posterity on the quick plating medium in osmanthus, with inoculating loop picking colonies typical 4-5, be inoculated on the quick plating medium in osmanthus, after cultivating in 12 hours, choose a small amount of culture suspendible in MH meat soup, its turbidity is adjusted to Chinese bacterial concentration standard 93-1 standard pipe, be equivalent to 8 * 10
8/ ml is standby.
2. the preparation of stock solution of the present invention: accurately take by weighing to sweep and drench capsule powder 400mg, add a little 0.1N NaOH and make its dissolving, adding distil water is to 100ml again.This moment, concentration was 4000ug/ml, by the degerming of bacteriological filtration film (0.22um) filter, was mixed with the medicinal liquid of 10 times of the required final concentrations of agar culture medium with the sterile working with distilled water, quantitatively was sub-packed in the bottle standby.The concentration of this advance copy invention stock solution is 4000,2000,1000,500,250, unit: ug/ml.
3. fine jade refers to dilute the preparation of plate: get 1 part of each dilution medicinal liquid, be added in the culture medium of 9 parts of volumes (culture medium is through being cooled to 50-55 ℃ in water-bath behind the high pressure), stir mixing.Each sterilization is poured into 20ml in plate, treat that agar solidifies after, plate is stored in standby in 4 ℃ of refrigerators (placing a period of time with preceding in 36 ℃ of incubators).
4. inoculation plate, each plating bacteria suspension 0.05ml, and evenly with the coating of " L " type Glass rod, inoculation does not simultaneously contain in the culture medium of the present invention in contrast.
5. cultivate: after treating the inoculum drying, the 3-10%CO that contains that plate is turned in humidity
2(candle jar method) cultivates 20 hours observed results in 35 ℃ in the environment.
6. criterion
MIC is meant the least concentration of the present invention that antibacterial does not grow, and MIC uses ug/ml and represents.
Drug dose grouping and result packet original liquid concentration of the present invention are cultivated wherein drug level result
(ug/ml) (ug/ml) 1 4,000 400 no bacterial growth 2 2,000 200 no bacterial growth 3 1,000 100 no bacterial growths 4 500 50 have a small amount of bacterial growth 5 250 25 that many bacterial growth 6 0.00 0.00 full ware bacterial growths are arranged
According to criterion, gonococcus is to sensitivity testing result of the present invention, and MIC is 100ug/ml.
The used medicine of the present invention of Shenyang City's mother and child care
Treatment gonorrhea 9 routine clinical observation oral 5 capsules of the present invention every morning, serveing on three is a course of treatment.Efficacy determination:
(1) cure: no frequent micturition, the dysurea sense, the local scorching hyperemia that becomes, swelling disappears, no purulent secretion.
The no gonococcus of the sick inspection of secretions smear.
(2) take a turn for the better: frequent micturition, the dysurea symptom obviously alleviates, and the congested swelling of local scorching change alleviates, and secretions obviously reduces.
The no gonococcus of the sick inspection of secretions smear.
(3) invalid: local scorching the change do not have change.
In 9 examples, male 3 examples, women 6 examples.The oldest 46 years old, minimum 25 years old.The 9 routine patients that go to a doctor all have tangible frequent micturition, dysurea symptom, and obvious edema of clinical examination glans penis and urethra or cervical secretions, urethral secretions increase and be pus sample or milky, and the sick inspection of secretions smear is all looked into and seen gram-negative diplococci.
Cure rate 100% is all cured in 9 routine gonorrhea patient's medications (the present invention) course of treatment.Evident in efficacy, have no side effect, dosage form is simple, taking convenience, cost is lower, and need about 30 yuan a course of treatment.
TCM Specialist Clinic portion of Liaoning academy of traditional Chinese medicine
Treat the gonorrhea clinical observation with the present invention
Man's 11 examples, women 4 examples.Male's year makes: in 22-45 year, the women makes 20-28 year year.
Most for promptly going to a doctor about one week of morbidity, indivedual cases are in half a year to one year, and outbreak repeatedly.
The male is mainly the red pain of itching of glans penis, and the burning pain of urinating, and most of companion's yellow-white purulent secretion overflows, and undesired different in nature contact history is arranged.In male's 11 examples, 6 example microscopies are made a definite diagnosis, and 5 examples of surplusing are refused microscopies.In women's 4 examples, 3 examples are married women, and suffer from altogether for the people woman, and 1 routine unmarried has different in nature contact history.4 examples mainly show as leucorrhea, fulminant leucorrhagia with yellowish discharge, abnormal flavour are arranged, companion's urethral stimulant disease.4 routine women refuse microscopy.
In 15 examples, 8 examples are first visit, and 7 examples are further consultation.Further consultation person all at first washes treatment through the penicillium sp preparation, DeGrain, and use the present invention instead.
Above-mentioned patient uses the present invention, and each 5, oral once a day, three days is a course of treatment.Press curative effect determinate standard, person's 6 examples that heal full a course of treatment, person's 4 examples that heal entirely 2 courses of treatment, effective 2 examples, invalid 1 example, not clear 1 example.Total effective rate 99%.
In 6 examples that heal entirely, 3 days prescription on individual diagnosis person's 4 examples of falling ill, 1 all prescription on individual diagnosis person's 2 examples of falling ill, 4 examples are in healing the person entirely 2 courses of treatment, and 3 examples were fallen ill for 2 weeks, 1 example 1 week of morbidity.2 routine responders, 1 routine nonresponder is repeated infection, and course of treatment of medication only.
Low price of the present invention, easy to use and instant effect, Shenyang City's the 7th the People's Hospital's Urology Surgery was used the present invention in 94 years 7-11 months, and its curative effect is as follows:
Observe 52 examples altogether and make a definite diagnosis according to contact history clinical symptoms, lab testing, male's 46 examples wherein, women's 6 examples, in age 20-47 year, all patients all carry out microscopy.The all inactive various antibacterials of all patients before the treatment, obey 6 of capsules of the present invention every day during the treatment, and dose is 600mg, and a week is a course of treatment, further consultation in two days after the drug withdrawal.
Criterion of therapeutical effect is judged
Recovery from illness: clinical symptoms Signs continuous 2 secretions that disappear are cultivated and are negative.
Produce effects: clinical Signs disappears substantially, and routine urinalysis is normal or approaching normal, urine bacterium feminine gender.
Effectively: clinical symptoms, sign alleviate, and routine urinalysis significantly improves.
Invalid: clinical symptoms sign no change, result of laboratory test is positive.
Observe altogether 52 examples except that 2 invalid, effective 50, total effective rate is 96%.
52 examples do not have 1 example and toxic and side effects occurs.
Grandson patient * * man, 39 years old, find G (-) diplococcus when coming institute inside and outside the microscopy cell, routine urinalysis is not found G (-) diplococcus after taking medicine;
The king * * man 26 years old, come the institute microscopy to find inside and outside the cell G (-) diplococcus is arranged all, through take one the course of treatment medicine microscopy do not find G (-) diplococcus;
Yellow * * male 34 years old, come to find G (-) diplococcus inside and outside institute's microscopy cell, normal through two course of therapy routine urinalysis, microscopy is not found G (-) diplococcus.
Be described in detail technical solution of the present invention below.
Embodiment 1: sweep and drench capsular prescription, the ratio between its composition and each component following (weight ratio):
Rifampicine: 4
Methyl benzyl Aminometradine: 1
Sodium bicarbonate: 2
Gentamycin sulfate: 1
2: sweep and drench capsular prescription, the ratio between its composition and each component following (weight ratio):
Rifampicine: 4
Methyl benzyl Aminometradine: 1.5
Sodium bicarbonate: 2.5
Gentamycin sulfate: 1.5
3: sweep and drench capsular prescription, the ratio between its composition and each component following (weight ratio):
Rifampicine: 4
Methyl benzyl Aminometradine: 1.25
Sodium bicarbonate: 2.25
Gentamycin sulfate: 1.25
The all available following technology of above-mentioned three embodiment makes: behind above-mentioned each component medicamental pulverata mixing, fill promptly.
Claims (2)
1. sweep the capsular prescription of pouring for one kind, it is characterized in that the ratio between its composition and each component is as follows:
Rifampicine: 4
Methyl benzyl Aminometradine: 1-1.5
Sodium bicarbonate: 2-2.5
Gentamycin sulfate: 1-1.5
2. make the described capsular processing technology of claim 1 for one kind, it is characterized in that fill promptly with behind the above-mentioned each component medicamental pulverata mixing.
Priority Applications (1)
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CN96115230A CN1056059C (en) | 1996-04-16 | 1996-04-16 | Prescription for curing gonorrhea and preparation thereof |
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CN96115230A CN1056059C (en) | 1996-04-16 | 1996-04-16 | Prescription for curing gonorrhea and preparation thereof |
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CN1162448A CN1162448A (en) | 1997-10-22 |
CN1056059C true CN1056059C (en) | 2000-09-06 |
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CN96115230A Expired - Fee Related CN1056059C (en) | 1996-04-16 | 1996-04-16 | Prescription for curing gonorrhea and preparation thereof |
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Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1075257A (en) * | 1992-09-12 | 1993-08-18 | 海口市制药厂 | The compound method of minocycline hydrochloride capsule |
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1996
- 1996-04-16 CN CN96115230A patent/CN1056059C/en not_active Expired - Fee Related
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1075257A (en) * | 1992-09-12 | 1993-08-18 | 海口市制药厂 | The compound method of minocycline hydrochloride capsule |
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