CN110215473A - A kind of medicament reducing anti-infective tetracycline clinical side effects - Google Patents
A kind of medicament reducing anti-infective tetracycline clinical side effects Download PDFInfo
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- CN110215473A CN110215473A CN201910493918.7A CN201910493918A CN110215473A CN 110215473 A CN110215473 A CN 110215473A CN 201910493918 A CN201910493918 A CN 201910493918A CN 110215473 A CN110215473 A CN 110215473A
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- 239000004098 Tetracycline Substances 0.000 title claims abstract description 39
- 235000019364 tetracycline Nutrition 0.000 title claims abstract description 39
- 150000003522 tetracyclines Chemical class 0.000 title claims abstract description 39
- 229960002180 tetracycline Drugs 0.000 title claims abstract description 38
- 229930101283 tetracycline Natural products 0.000 title claims abstract description 38
- 230000000694 effects Effects 0.000 title claims abstract description 25
- 230000002924 anti-infective effect Effects 0.000 title claims abstract description 14
- 241001183967 Isodon Species 0.000 claims abstract description 22
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- 229920000168 Microcrystalline cellulose Polymers 0.000 claims abstract description 13
- 229920002472 Starch Polymers 0.000 claims abstract description 13
- 229920000609 methyl cellulose Polymers 0.000 claims abstract description 13
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- 235000010981 methylcellulose Nutrition 0.000 claims abstract description 13
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- 229940016286 microcrystalline cellulose Drugs 0.000 claims abstract description 13
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims abstract description 13
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- 229960004475 chlortetracycline Drugs 0.000 description 2
- CYDMQBQPVICBEU-XRNKAMNCSA-N chlortetracycline Chemical compound C1=CC(Cl)=C2[C@](O)(C)[C@H]3C[C@H]4[C@H](N(C)C)C(O)=C(C(N)=O)C(=O)[C@@]4(O)C(O)=C3C(=O)C2=C1O CYDMQBQPVICBEU-XRNKAMNCSA-N 0.000 description 2
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- 210000004698 lymphocyte Anatomy 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 229960000282 metronidazole Drugs 0.000 description 1
- VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
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- 231100000195 subchronic toxicity Toxicity 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/65—Tetracyclines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Natural Medicines & Medicinal Plants (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Biotechnology (AREA)
- Communicable Diseases (AREA)
- Microbiology (AREA)
- Medical Informatics (AREA)
- Botany (AREA)
- Alternative & Traditional Medicine (AREA)
- Engineering & Computer Science (AREA)
- Mycology (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention discloses a kind of medicaments for reducing anti-infective tetracycline clinical side effects, belong to technical field of pharmaceuticals, which is made of tetracycline, rabdosia lophanthide extractive, microcrystalline cellulose, starch, magnesium stearate, methylcellulose, atoleine.It is significant that the curative effect of medicine is demonstrated by test, and toxic side effect is small, safely and effectively, quality is stablized, and treatment total effective rate reaches 100%.
Description
Technical field
The present invention relates to technical field of pharmaceuticals more particularly to a kind of medicaments for reducing anti-infective tetracycline clinical side effects.
Background technique
Tetracycline is to find when studying the chemical structure of aureomycin and terramycin nineteen fifty-three.It can be generated from streptomycete
Or it is semi-synthetic by raw material of aureomycin.Tetracycline is easily denaturalized at high temperature, and degradation generates epitetracyclin, or dehydration is formed
Dehydration tetracycline, dehydration tetracycline can also form epimer, claim epianhydrotetracycline.This product is pale yellow crystals powder
End, it is odorless, it is atomic to be dissolved in water, it is slightly soluble in ethyl alcohol, is soluble in diluted acid diluted alkaline.It takes orally after entering in vivo, is distributed widely in each group
It knits, but is not easy through blood-brain barrier.Such antibiotic is widely used in Grain-positive and negative bacteria, intracellular mycoplasma, clothing
Certain filterable virus and protozoon are also had effect by infection caused by substance and rickettsia.The antibacterial action of Tetracyclines
The growth for inhibiting bacterium is essentially consisted in, but also has bactericidal effect in higher concentration, some countries including the U.S., Fourth Ring
Element is also widely used as growth promoter and feeds to animal, but bacterium is more serious to this kind of antibiotics resistance phenomenon, in addition malicious
Side reaction is also more, with clinically a large amount of generations of tetracycline antibiotics drug-fast bacteria and going deep into its adverse reaction
Solution, part tetracycline antibiotics gradually exit from clinical application, therefore, be clinically badly in need of antimicrobial spectrum is wider, antibacterial activity more
Novel tetracyclic element class antibiotic strong and that drug-fast bacteria can be overcome.The applicant is by proposing one kind after theory practice thus
The medicament of tetracycline clinical side effects is reduced, to adapt to present social development needs, widens the application range of tetracycline, is improved suitable
The property used.
Summary of the invention
The object of the present invention is to provide a kind of medicaments for reducing anti-infective tetracycline clinical side effects.
The purpose of the present invention is what is be achieved through the following technical solutions, the medicine of the anti-infective tetracycline clinical side effects of the reduction
Agent is made of effective component and auxiliary element, and the effective component is made of tetracycline and rabdosia lophanthide extractive, it is described auxiliary at
Divide includes microcrystalline cellulose, starch, magnesium stearate, methylcellulose, atoleine.
Preferably, tetracycline 3-7 parts in effective component, 17-22 parts of rabdosia lophanthide extractive.
Preferably, microcrystalline cellulose 30-40 parts in auxiliary element, 20-30 parts of starch, 2-3 parts of magnesium stearate, Methyl cellulose
It is 11-16 parts plain, 2-6 parts of atoleine.
It is preferred: 5 parts of tetracycline, 20 parts of rabdosia lophanthide extractive, 35 parts of microcrystalline cellulose, 25 parts of starch, magnesium stearate 2.5
Part, 14 parts of methylcellulose, 4 parts of atoleine be made.
The preparation method for preparing liquid: taking the rabdosia lophanthide completely crushed, crosses 80 meshes, dries in the air after first impregnating 2h with warm water
It is dry, it immerses in appropriate 60% ethyl alcohol, 5d is extracted at 50 DEG C, then mechanical shaking extraction (60 DEG C, 300r/rain) 12h is filtered, filtrate
The rotary evaporation at 50 DEG C, steaming no longer change to volume, drying and grinding into powder in 60 DEG C of baking ovens, according to the weight of gained powder
Amount, is added pharmaceutically acceptable lysate, the solution of 0.2g/ml is made up to rabdosia lophanthide extractive.
The preparation method of medicament of the present invention: tetracycline, methylcellulose, microcrystalline cellulose and starch are accurately weighed up, and are mixed
It closes uniformly, then plus softwood is made in rabdosia lophanthide extractive, is pelletized with nylon wire, in 20-40 DEG C of aeration-drying, dry granular stiffened resin acid
Magnesium, atoleine select grain to be uniformly mixed tabletting after chemical examination qualification.
The rabdosia lophanthide is one kind under Labiatae Rabdosia, 5~October of florescence.It is born in small stream side, ditch side or mountain
The wet place of paddy, 60~80 centimetres high, stem is upright, square, branch, slightly coat.What its leaf was rubbed has yellow juice, and summer and autumn harvest,
It dries, fresh goods can adopt at any time.Rabdosia lophanthide has effects that clearing heat and promoting diuresis, removing jaundice clearing damp, cool blood dissipates the stasis of blood.
Beneficial effects of the present invention: it yet there are no the report for sharing rabdosia lophanthide extractive and tetracycline, more have no use
The report of rabdosia lophanthide extractive reduction tetracycline clinical side effects.It is proved by clinical test, rabdosia lophanthide extractive and tetracycline
Sharing not only has the function of reducing tetracycline clinical side effects, but also has obvious synergistic function.
Specific embodiment
Embodiment one: the medicament of the anti-infective tetracycline clinical side effects of the reduction is by 3 grams of tetracycline, rabdosia lophanthide extractive 17
Gram, 30 grams of microcrystalline cellulose, 20 grams of starch, 2 grams of magnesium stearate, 11 grams of methylcellulose, atoleine 2 restrain at.
Embodiment two: the medicament of the anti-infective tetracycline clinical side effects of the reduction is by 5 grams of tetracycline, rabdosia lophanthide extractive 20
Gram, 35 grams of microcrystalline cellulose, 25 grams of starch, 2.5 grams of magnesium stearate, 14 grams of methylcellulose, atoleine 4 restrain at.
Embodiment three: the medicament of the reduction tetracycline clinical side effects is by 7 grams of tetracycline, 22 grams of rabdosia lophanthide extractive, micro-
40 grams of crystalline cellulose, 30 grams of starch, 3 grams of magnesium stearate, 16 grams of methylcellulose, atoleine 6 restrain at.
Inspection to medicament of the invention: precision weighs the standard items, sample fine powder and right amount of auxiliary materials of medicament of the present invention, point
(adding 1mL by every 5mg) is not dissolved with 0.05mol/L hydrochloric acid solution, precision is added water and is made into 800u/mL, shakes up filtration, precision is inhaled
It takes subsequent filtrate 1mL to set in 50mL measuring bottle, adds 0.01mol/L hydrochloric acid solution to be diluted to scale and shake up.With 0.01mol/L hydrochloric acid solution
Make blank, scanned between 220~400nm of wavelength, records absorption spectrum.
The result shows that: there is absorption maximum at wavelength 245nm and 397nm, has minimal absorption at 229nm and 359 nm.
Wherein peak shape is preferable at 257nm, therefore selects 257nm for assay wavelength.
Assay: selecting 257nm for measurement wavelength, and above-mentioned 800u/mL standard solution is molten with 0.01mol/L HC
Liquid is diluted to 80u/mL solution, precision draws 1,2,3,4,5mL set in 25mL measuring bottle respectively, add 0.01mol/L hydrochloric acid solution dilute
It releases to scale and shakes up, using solvent as blank, trap is measured at 257nm wavelength, the results showed that, within the scope of 3~22u/mL
With good linear relationship.Its regression equation A=0.03791 ρ -0.0005.
Stability test: taking above-mentioned standard product solution, trap measured after 5,20,30,48h, as a result almost without
Change (RSD=0.34%), shows that solution is stablized in 48h.
Recovery test: conventionally, it is that 100.21%, RSD is that average recovery rate is measured at 257nm wavelength
0.93%。
Toxicity test
The measurement of acute toxicity test: taking weight is the small white mouse of 20-22g, sets 3 groups altogether, every group 10, half male and half female is distinguished
By 1000mg/kg, 1500mg/kg, 2000mg/kg gastric infusion, if gavaging distilled water is blank control group.Prohibit before mouse administration
10h is eaten, water is can't help, ends a hunger strike within 5 one 6 days after administration, administration is observed continuously 10 days after stopping, the spirit of whole small white mouses, appetite, drink
Situations such as water and control group are more without exception.It determines therefrom that after small white mouse gavages medicament 2000mg/kg of the invention without poisoning
The phenomena of mortality.By toxicological evaluation standard, it may not be necessary to measure median lethal dose (LD50), i.e. LD50 > 1500mg/kg, as a result table
Bright medicament of the invention belongs to nontoxic grade.
Cumulative toxicity test: the applicant was tested using 20 days accumulation test methods, and taking weight is the little Bai of 21-26g
Mouse sets 4 groups altogether, and every group 20, half male and half female presses the agent of 300mg/kg, 400mg/kg, 500mg/kg, 600mg/kg respectively
Amount carries out gastric infusion, continuously gavages medicament of the present invention 20 days, and mouse fasting 6h, can't help water, 6-8h ends a hunger strike after administration before being administered.
Spirit, appetite, drinking-water and the death condition that small white mouse is observed during administration are no different paradoxical reaction, and administration is observed interior small after stopping
The death condition of white mouse, weight, feed intake amount and the measurement heart, liver, spleen, lung, the internal organs of kidney are without exception.
Subchronic toxicity test: feeding test for 90 days, taking weight is small white mouse 20 of 19-22g, wherein male 10,
Female 10, if 4 test groups and a control group, test group add medicament of the present invention in feed respectively, additive capacity is
1%, 2%, 3%, 4%, successive administration, control group fed conventional nutrient feed.Isolation is for experiment after feeding 2 weeks after animal is bought,
Experimental animal free choice feeding, free water.Groups of animals ingests, drinks water, excrement is normal, does not occur Poisoning clinical symptoms,
Red blood cell count(RBC) between each test group and control group, white blood cell count(WBC), hemoglobin and lymphocyte number content difference are not shown
It writes, difference is not also significant between each test group, and urea nitrogen difference is not significant between each test group and control group, weight, feeding
Amount amount and the measurement heart, liver, spleen, lung, the internal organs of kidney are without exception.
Clinical test
1, general information treats 120 Stomatology Clinic patients from the observation of our hospital, is diagnosed as periodontitis, male 49, female
61；Age 36-66 years old；Shortest course of disease 6 months, the longest 8 years.On the basis of patient knows and is voluntary, we will suffer from
Person is divided into 4 groups, and each group is more not statistically significant (P > 0.05) in general information such as age, genders, is comparable.
Preparation method according to the present invention, the applicant accurately weigh up methylcellulose, microcrystalline cellulose and starch, mix
It closes uniformly, then plus softwood is made in rabdosia lophanthide extractive, is pelletized with nylon wire, in 20-40 DEG C of aeration-drying, dry granular stiffened resin acid
Magnesium, atoleine select grain to be uniformly mixed after chemical examination qualification and are set as A medicine through medicament made from tabletting.
Preparation method according to the present invention, the applicant are accurate by tetracycline, methylcellulose, microcrystalline cellulose and starch
It weighs up, is uniformly mixed, then plus softwood is made in pharmaceutically acceptable solution, is pelletized with nylon wire, dry in 20-40 DEG C of ventilation
Dry, dry granular stiffened fatty acid magnesium, atoleine select grain to be uniformly mixed after chemical examination qualification and are set as B medicine through medicament made from tabletting.
On the basis of patient is voluntary, takes the present invention and by pharmaceutical treatment made from embodiment two be treatment group, adopt
It is control group with Routine Treatment Therapy For Instability, taking the treatment of A medicine is A medicine group, and taking the treatment of B medicine is B medicine group.
2, diagnostic criteria: different degrees of chronic inflammation is presented in gum, and color is dark red or scarlet, and quality is soft, and stippling disappears
Lose, edge round blunt and not with facing attach；Periodontal bag formation, attachment loss, pyorrhea in bag；Loosening in various degree occurs in tooth；X
Line shows that alveolar bone has different degrees of absorption.
3, treatment method treatment group takes is treated by medicament made from embodiment of the present invention two, is taken orally, adult normal
0.25~0.5g of dosage, three times a day, 8 years old or more children's usual amounts are every time 15~30mg/kg, three times a day.The course for the treatment of one
As be 4~7 days；Control group conventionally treated by Effect of Oral Metronidazole piece；A medicine group and B medicine group suggested use and dosage with control
Treatment group is identical.
4. criterion of therapeutical effect is cured: symptom completely disappears, and depth of pocket shoals or restores normal, and tooth non-loosening can be just
Often chewing.Improve: gum mild hyperaemia, bleeding, pain, oedema mitigate.Invalid: variation is unobvious.
5, treatment results such as following table
| Group | Number of cases | Dose (g) | Recovery from illness | It is effective | In vain | Side effect | Total effective rate (%) |
| A group | 30 | 1.5g/ it | 0 | 3 | 27 | 6 | 10. |
| B group | 30 | 1.5g/ it | 1 | 6 | 23 | 3 | 30.43 |
| Treatment group | 30 | 0.75g/ days | 28 | 2 | 0 | 0 | 100 |
| Control group | 30 | Convention amount | 7 | 14 | 9 | 2 | 70 |
By clinical data it is found that the dose taken for the treatment of group is less, total effective rate is but significantly larger than other each groups, also obvious good
In control group, it is often more important that toxicity reduces, and have no toxic side effect appearance, and wherein A group has 2 nausea occur, and 3 are vomitted
Spit symptom, epigastric discomfort, abdominal distension, 1 there is symptom of diarrhea；B group has 1 nausea occur, and 1 symptoms of emesis occurs, and 1
There is heating paresthesia.It follows that each medicine for the treatment of group has synergistic function after proportion, it is worth clinical application.
Claims (6)
1. a kind of medicament for reducing anti-infective tetracycline clinical side effects, it is characterised in that the medicament by effective component and auxiliary at
It is grouped as, the effective component is made of tetracycline and rabdosia lophanthide extractive, and the auxiliary element includes microcrystalline cellulose, forms sediment
Powder, magnesium stearate, methylcellulose, atoleine.
2. a kind of medicament for reducing anti-infective tetracycline clinical side effects according to claim 1, it is characterised in that the medicine
3-7 parts of effective component tetracycline, 17-22 parts of rabdosia lophanthide extractive in agent.
3. a kind of medicament for reducing anti-infective tetracycline clinical side effects according to claim 1, it is characterised in that the medicine
30-40 parts of auxiliary element microcrystalline cellulose, 20-30 parts of starch, 2-3 parts of magnesium stearate, 11-16 parts of methylcellulose, liquid in agent
2-6 parts of body paraffin.
4. a kind of medicament for reducing anti-infective tetracycline clinical side effects according to claim 2-3, it is characterised in that should
Medicament is fine by 5 parts of tetracycline, 20 parts of rabdosia lophanthide extractive, 35 parts of microcrystalline cellulose, 25 parts of starch, 2.5 parts of magnesium stearate, methyl
14 parts, 4 parts of atoleine of dimension element is made.
5. a kind of medicament for reducing anti-infective tetracycline clinical side effects according to claim 1, it is characterised in that small stream is yellow
Careless method for preparing extractive is as follows: taking the rabdosia lophanthide completely crushed to cross 80 meshes, dries after first impregnating 2h with warm water, immerses appropriate
In 60% ethyl alcohol, 5d is extracted at 50 DEG C, then mechanical shaking extraction (60 DEG C, 300r/rain) 12h is filtered, and filtrate is in 50 DEG C of backspins
Turn evaporation, steaming no longer changes to volume, drying and grinding into powder in 60 DEG C of baking ovens, and according to the weight of gained powder, pharmacy is added
Upper acceptable lysate, is made the solution of 0.2g/ml to obtain the final product.
6. a kind of medicament for reducing anti-infective tetracycline clinical side effects according to claim 1, it is characterised in that medicament
The preparation method is as follows: tetracycline, methylcellulose, microcrystalline cellulose and starch are accurately weighed up, be uniformly mixed, be then added
Softwood is made in rabdosia lophanthide extractive, is pelletized with nylon wire, in 20-40 DEG C of aeration-drying, dry granular stiffened fatty acid magnesium, atoleine,
Grain is selected to be uniformly mixed tabletting after chemical examination qualification.
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1405177A (en) * | 2002-11-01 | 2003-03-26 | 广州中医药大学 | Rabdosia lophanthide extractive, natural medicine for treating hepatitis |
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2019
- 2019-06-08 CN CN201910493918.7A patent/CN110215473A/en not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1405177A (en) * | 2002-11-01 | 2003-03-26 | 广州中医药大学 | Rabdosia lophanthide extractive, natural medicine for treating hepatitis |
Non-Patent Citations (2)
| Title |
|---|
| 肖忠革: "四环素类药物治疗牙周炎的作用机制及临床应用进展", 《现代中西医结合杂志》 * |
| 范葶莉: "溪黄草水提物与抗菌药联用对大肠杆菌的体外抑制效果", 《中兽医医药杂志》 * |
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Application publication date: 20190910 |