CN102784120B - Metronidazole composition freeze-dried disintegrating tablets for vaginas and preparation method thereof - Google Patents
Metronidazole composition freeze-dried disintegrating tablets for vaginas and preparation method thereof Download PDFInfo
- Publication number
- CN102784120B CN102784120B CN201210300817.1A CN201210300817A CN102784120B CN 102784120 B CN102784120 B CN 102784120B CN 201210300817 A CN201210300817 A CN 201210300817A CN 102784120 B CN102784120 B CN 102784120B
- Authority
- CN
- China
- Prior art keywords
- metronidazole
- vagina
- lyophilizing
- disintegrating tablet
- preparation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Abstract
The invention provides metronidazole composition freeze-dried disintegrating tablets for vaginas and a preparation method of the freeze-dried disintegrating tablets, relates to the field of a medicine and a medicine preparation method technology and mainly solves the technical problems that the metronidazole suppositories and effervescent tablets are inconvenient to transport and store, the application is limited; and the inflamed mucosas are frequently stimulated by the metronidazole suppositories and effervescent tablets when metronidazole suppositories and effervescent tablets are utilized, and the clinical application is influenced. The metronidazole composition freeze-dried disintegrating tablets are prepared from the following components by weight: 10-24% of metronidazole, 24-50% of mannitol, 2-4% of gelatin, 32-74% of hydroxypropyl-beta-cyclodextrin with medium substitution degree and 50% of purified water. The metronidazole composition freeze-dried disintegrating tablets for vaginas prepared by the above components are easy in preparation process, and simple in components, moreover, the metronidazole composition freeze-dried disintegrating tablets for vaginas have the advantages of being fast to disintegrate, convenient to take, and good in compliance, and the tablets take effect quickly and are fully absorbed; and the disintegrating tablets can be completely disintegrated in the vaginas while meeting water, so that foreign body sensation does not exist in the vaginas.
Description
Technical field:
The present invention relates to the preparation method technical field of medicine and medicine, relate in particular to a kind of metronidazole compositions vagina lyophilizing disintegrating tablet and preparation method thereof.
Background technology:
Metronidazole is nitro imidazole derivatives.Its mechanism of action is: (1) may anti-bacteria DNA (deoxyribonucleic acid) synthetic, thereby disturb growth, the breeding of antibacterial, finally cause antibacterial dead.Metronidazole has killing action to the cell of growing under anaerobic condition and anaerobe, and its metabolite of generating while reducing in human body, also has anaerobe resistant effect, a little higher than Mlc of its bacteriocidal concentration; (2) can suppress ameba redox reaction, protozoon nitrogen chain is ruptured; (3) in addition, metronidazole also has the powerful effect of killing infusorian.Metronidazole has powerful antibacterial action to most of anaerobe, but to aerobe and facultative anaerobe without effect.In addition, metronidazole also has powerful effect to microorganisms such as infusorian, ameba, guinea worms.Metronidazole antimicrobial spectrum comprises bacteroides fragilis and other Bacteroidess, fusiform bacilarmature, aerogenesis clostruidium, Eubacterium, Wei Rong coccus, dyspepsiacoccus and peptostreptococcus etc.Actinomyces, Lactobacillus, propionibacterium are to this medicine drug resistance, and metronidazole belongs to antiprotozoan agent and antibacterial.
Metronidazole claims again metronidazole, and late 1950s begins for clinical with treatment trichomonal vaginitis.Disease of female genital organs's kind has a lot, and due to female sex organ, some is exposed to outside, and the symptoms such as some prurituss, pain also easily appear in the skin at these positions, and patient is ashamed to mention, and are a great inconvenience.As pruritus genitalium, vulval eczema, leukoplakia vulvae, ulcus vulvae acutum, pelvic infection etc.The Protostat that is used for the treatment of now disease of female genital organs is suppository and effervescent tablet.It is substrate that but suppository be take polyoxyethylene monoesters acid and glycerol, and transportation and storage inconvenience, require, 30 ℃ of following preservations, in some high temperature, severe cold areas use, to be restricted.Soda acid effervescent is contained in effervescent tablet the inside, uses often inflammation mucosa is produced to zest, affects clinical practice.
So still lack at present and in the urgent need to a kind of like this Protostat, its preparation technology is simple, component is simple.And this Protostat convenient drug administration, bioavailability are high, good stability, content accurately, good looking appearance, good effect, nonirritant, compliance be high.
Summary of the invention:
The object of the invention is to overcome the defect of prior art, utilizes cyclodextrin inclusion technique, increases the water solublity of metronidazole, the stability of improving metronidazole, reduction vaginal irritation.Utilize computer molecular simulateo, best complex ratio and the inventory of Theoretical Calculation metronidazole and cyclodextrin.
The invention provides a kind of in vagina fast metronidazole compositions vagina lyophilizing disintegrating tablet of disintegration rate and preparation method thereof, the method preparation condition is gentle, is easy to control, and is applicable to industrialized great production.Said composition composition is simple: principal agent is metronidazole, also includes skeleton agent (mannitol), forming agent (gelatin), solubilizing agent (medium substitution value hydroxypropyl-β-cyclodextrin).
For realizing the object of the invention, technical scheme realizes in the following way:
A metronidazole compositions, is characterized in that: said composition comprises following component and component quantity ratio:
The preferred ingredient quantity ratio of described each component of metronidazole compositions is:
A metronidazole compositions vagina lyophilizing disintegrating tablet that contains metronidazole compositions, is characterized in that, by following component and component quantity ratio, is prepared from:
The preferred ingredient quantity ratio of preparing each component of metronidazole compositions vagina lyophilizing disintegrating tablet is:
A preparation method for metronidazole compositions vagina lyophilizing disintegrating tablet, is characterized in that, the concrete steps of this preparation method are:
A) the medium substitution value hydroxypropyl-β-cyclodextrin of group component is dissolved in 70%-80% purified water of component water total amount, under stirring, be heated to 55 ℃, the metronidazole that slowly adds group component, continue to stir 10 hours, treat that medium substitution value hydroxypropyl-β-cyclodextrin, by after metronidazole enclose, adds the mannitol of group component;
B) gelatin of group component is dissolved in the purified water of component water consumption 20%-30%, is heated to dissolve completely;
C) two kinds of solution that merging above-mentioned steps a, step b obtain also stir;
D) with sodium bicarbonate, regulate pH value to 5.5-6.5;
E) according to metronidazole compositions vagina lyophilizing disintegrating tablet specification, determine after loading amount, medicinal liquid after merging is moved in drug-containing dish by loading amount, and put into freeze drying box, medicinal liquid is carried out to freezing (cryogenic temperature is-20 ℃--50 ℃), and evacuation is dried (cryogenic temperature is-20 ℃--50 ℃), and evacuation is dry, and (baking temperature is at 0 ℃-+5 ℃, vacuum is 0.1 handkerchief-20 handkerchief), control moisture and be no more than 1.0%;
F) after metronidazole compositions vagina lyophilizing disintegrating tablet is dry, in freeze drying box, seal;
G) will after the medicament taking-up freeze drying box freezing, cut drug-containing dish, and carry out finished product packing.
Described medium substitution value hydroxypropyl-β-cyclodextrin consumption is 200%-600% of metronidazole quality in prescription.
Described metronidazole compositions vagina lyophilizing disintegrating tablet specification is 100mg/ sheet or 200mg/ sheet.
For the disintegration rate of metronidazole compositions vagina lyophilizing disintegrating tablet, we have formulated relevant detection method:
Disintegration
According to inspection technique disintegration (two appendix X A of Chinese Pharmacopoeia version in 2010), stainless steel shaft by hanging basket by upper end hangs on metal rack, immerse in 1000ml beaker, and while regulating hanging basket position that it is declined screen cloth apart from beaker bottom 25mm, in beaker, fill temperature and be the water of 37 ℃ ± 1 ℃, while regulating height of water level to make hanging basket increase, screen cloth is at 15mm place, underwater.
Unless otherwise specified, get 6 groups of test samples (every group of dosage is 200mg), be set up respectively in the glass tubing of stating hanging basket, add baffle plate, start disintegration tester and check, each sheet all should all disintegrates in 1.1 seconds.Result is as following table:
Dosage equates, disintegration time and the medicine of different Metric 21s reach peak concentration
The disintegration rate that can find out metronidazole compositions vagina lyophilizing disintegrating tablet of the present invention from above experimental result is faster than metronidazole ordinary tablet.
Advantage of the present invention:
The first, tablet disintegrate is rapid, and drug effect is fast.Metronidazole compositions vagina lyophilizing disintegrating tablet of the present invention is disintegrate rapidly in 2 seconds in vagina, is beneficial to the rapid stripping of medicine, shortens dissolution time, accelerates to absorb, and brings into play fast curative effect, and vaginal irritation is little.
The second, drug absorption is abundant.Metronidazole compositions vagina lyophilizing disintegrating tablet of the present invention is disintegrate completely in vagina, makes the absorption of medicine more abundant, is conducive to like this improve the bioavailability of medicine.
Three, convenient drug administration, compliance is good.Metronidazole compositions vagina lyophilizing disintegrating tablet of the present invention is met water in vagina can make its complete disintegrate, the sense of intravaginal foreign, and compliance is good.
The selected adjuvant of metronidazole compositions vagina lyophilizing disintegrating tablet is all the adjuvants that are suitable for this tablet of preparation.Insoluble in water according to research metronidazole, for improving its dissolubility, so add medium substitution value hydroxypropyl-β-cyclodextrin in prescription, consumption is 200%-600% of metronidazole quality in prescription.In this prescription, use medium substitution value hydroxypropyl-β-cyclodextrin, be that to have haemolysis little because of it, stimulate slightly, the advantages such as metabolism occur hardly in human body, and be conducive to improve dissolubility, stability and the bioavailability of medicine, and can improve the quality of medicament.
The preparation technology of metronidazole compositions vagina lyophilizing disintegrating tablet of the present invention is simple, component is simple.And this Protostat disintegration time in vagina was no more than for 2 seconds, convenient drug administration, bioavailability are high, good stability, content accurately, good looking appearance, good effect, nonirritant, compliance be high.
The specific embodiment:
For the present invention is described in detail, below in conjunction with specific embodiment, be described further,
Embodiment 1
Prescription: 1000 amounts
Medium substitution value hydroxypropyl-β-the cyclodextrin of recipe quantity is dissolved in 80% purified water of prescription water total amount, under stirring, be heated to 55 ℃, the metronidazole that slowly adds recipe quantity, continue to stir 10 hours, treat that medium substitution value hydroxypropyl-β-cyclodextrin will be to after metronidazole enclose, the mannitol that adds recipe quantity, sucralose, the gelatin of recipe quantity is dissolved in the purified water of prescription water consumption 20%, be heated to dissolve completely, merge above-mentioned two kinds of solution and stir, with sodium bicarbonate, regulate pH value to 5.5-6.5, according to metronidazole compositions vagina lyophilizing disintegrating tablet specification, determine after loading amount, medicinal liquid after merging is pressed in loading amount subpackage drug-containing dish, and put into freeze drying box, to medicinal liquid, carry out freezing, after metronidazole compositions vagina lyophilizing disintegrating tablet is dry, in freeze drying box, seal, cutting after taking out, packing.
Embodiment 2
Prescription: 1000 amounts
Medium substitution value hydroxypropyl-β-the cyclodextrin of recipe quantity is dissolved in 80% purified water of prescription water total amount, under stirring, be heated to 55 ℃, the metronidazole that slowly adds recipe quantity, continue to stir 10 hours, treat that medium substitution value hydroxypropyl-β-cyclodextrin is by after metronidazole enclose, the mannitol that adds recipe quantity, sucralose, the gelatin of recipe quantity is dissolved in the purified water of prescription water consumption 20%, be heated to dissolve completely, merge above-mentioned two kinds of solution and stir, with sodium bicarbonate, regulate pH value to 5.5-6.5, according to metronidazole compositions vagina lyophilizing disintegrating tablet specification, determine after loading amount, medicinal liquid after merging is pressed in loading amount subpackage drug-containing dish, and put into freeze drying box, to medicinal liquid, carry out freezing, after metronidazole compositions vagina lyophilizing disintegrating tablet is dry, in freeze drying box, seal, cutting after taking out, packing.
Embodiment 3
Prescription: 1000 amounts
Medium substitution value hydroxypropyl-β-the cyclodextrin of recipe quantity is dissolved in 80% purified water of prescription water total amount, under stirring, be heated to 55 ℃, the metronidazole that slowly adds recipe quantity, continue to stir 10 hours, treat that medium substitution value hydroxypropyl-β-cyclodextrin is by after metronidazole enclose, the mannitol that adds recipe quantity, sucralose, the gelatin of recipe quantity is dissolved in the purified water of prescription water consumption 20%, be heated to dissolve completely, merge above-mentioned two kinds of solution and stir, with sodium bicarbonate, regulate pH value to 5.5-6.5, according to metronidazole compositions vagina lyophilizing disintegrating tablet specification, determine after loading amount, medicinal liquid after merging is pressed in loading amount subpackage drug-containing dish, and put into freeze drying box, to medicinal liquid, carry out freezing, after metronidazole compositions vagina lyophilizing disintegrating tablet is dry, in freeze drying box, seal, cutting after taking out, packing.
More than show and described ultimate principle of the present invention, principal character and advantage of the present invention.The technical staff of the industry should understand; the present invention is not restricted to the described embodiments; what in above-described embodiment and description, describe is only preference of the present invention; be not used for limiting the present invention; without departing from the spirit and scope of the present invention; the present invention also has various changes and modifications, and these changes and improvements all fall in the claimed scope of the invention.The claimed scope of the present invention is defined by appending claims and equivalent thereof.
Claims (5)
1. a metronidazole compositions vagina lyophilizing disintegrating tablet, is characterized in that, by following component and component quantity ratio, is prepared from:
。
2. metronidazole compositions vagina lyophilizing disintegrating tablet according to claim 1, is characterized in that, the preferred ingredient quantity ratio of preparing each component of metronidazole compositions vagina lyophilizing disintegrating tablet is:
。
3. a preparation method for metronidazole compositions vagina lyophilizing disintegrating tablet described in claim 1, is characterized in that, the concrete steps of this preparation method are:
A) the medium substitution value hydroxypropyl-β-cyclodextrin of group component is dissolved in 70%-80% purified water of component water total amount, under stirring, be heated to 55 ℃, the metronidazole that slowly adds group component, continue to stir 10 hours, treat that medium substitution value hydroxypropyl-β-cyclodextrin, by after metronidazole enclose, adds the mannitol of group component;
B) gelatin of group component is dissolved in the purified water of component water consumption 20%-30%, is heated to dissolve completely;
C) two kinds of solution that merging above-mentioned steps a, step b obtain also stir;
D) with sodium bicarbonate, regulate pH value to 5.5-6.5;
E) according to metronidazole compositions vagina lyophilizing disintegrating tablet specification, determine after loading amount, the medicinal liquid after merging moved in drug-containing dish by loading amount, and put into freeze drying box, to medicinal liquid carry out freezing, evacuation dry, control moisture and be no more than 1.0%;
F) after metronidazole compositions vagina lyophilizing disintegrating tablet is dry, in freeze drying box, seal;
G) will after the medicament taking-up freeze drying box freezing, cut drug-containing dish, and carry out finished product packing.
4. the preparation method of metronidazole compositions vagina lyophilizing disintegrating tablet according to claim 3, is characterized in that: described medium substitution value hydroxypropyl-β-cyclodextrin consumption is 200%-600% of metronidazole quality in prescription.
5. the preparation method of metronidazole compositions vagina lyophilizing disintegrating tablet according to claim 3, is characterized in that: described metronidazole compositions vagina lyophilizing disintegrating tablet specification is 100mg/ sheet or 200mg/ sheet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210300817.1A CN102784120B (en) | 2012-08-23 | 2012-08-23 | Metronidazole composition freeze-dried disintegrating tablets for vaginas and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210300817.1A CN102784120B (en) | 2012-08-23 | 2012-08-23 | Metronidazole composition freeze-dried disintegrating tablets for vaginas and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102784120A CN102784120A (en) | 2012-11-21 |
| CN102784120B true CN102784120B (en) | 2014-03-26 |
Family
ID=47149842
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201210300817.1A Active CN102784120B (en) | 2012-08-23 | 2012-08-23 | Metronidazole composition freeze-dried disintegrating tablets for vaginas and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN102784120B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107536816A (en) * | 2016-06-29 | 2018-01-05 | 康普药业股份有限公司 | A kind of Protostat |
| CN110267652A (en) * | 2016-10-13 | 2019-09-20 | 康特伦英国斯温顿捷迪斯有限公司 | Freeze-drying medicinal composition for vaginal delivery |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1214784C (en) * | 2003-06-27 | 2005-08-17 | 刘辉 | Quick-releasing talbet in vagina and its preparing method |
| CN100366294C (en) * | 2004-04-30 | 2008-02-06 | 量子高科（北京）研究院有限公司 | Oral cavity quick dissolving preparation and production method thereof |
| CN102614138A (en) * | 2011-01-26 | 2012-08-01 | 量子高科（北京）研究院有限公司 | Oral disintegrating tablet and preparation method thereof |
| CN102631336B (en) * | 2012-02-07 | 2013-09-18 | 海南卫康制药(潜山)有限公司 | Freeze-drying orally disintegrating tablet with vitamin K1 composition for infants and preparation method for freeze-drying orally disintegrating tablet |
-
2012
- 2012-08-23 CN CN201210300817.1A patent/CN102784120B/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| CN102784120A (en) | 2012-11-21 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101698101B (en) | Medicine composite for treating vaginitis | |
| CN101744833B (en) | Medicinal composition for treating bacterial vaginitis | |
| CN105250231B (en) | Pharmaceutical composition containing etoricoxib and preparation method thereof | |
| CN102973528B (en) | Calcitriol solid lipidic dispersion and preparation method thereof | |
| CN102784120B (en) | Metronidazole composition freeze-dried disintegrating tablets for vaginas and preparation method thereof | |
| CN101053565A (en) | Vaginal tablets containing coltrimazole | |
| CN102038679B (en) | Metronidazole, clotrimazole and chlorhexidine acetate vagina gel and preparation method thereof | |
| CN102579655A (en) | Externally applied traditional Chinese medicine preparation for treating oral ulcer | |
| CN1739580A (en) | Recipe and prepn process of Chinese medicine gel prepn | |
| CN104138350A (en) | Baicalein temperature-sensitive gel, preparing method thereof and applications of the gel | |
| CN106798867B (en) | A kind of Smilax china L ball and its preparation technology | |
| CN101912376B (en) | Matrine vaginal effervescent tablets with bilayer structure and preparation method | |
| CN101623252A (en) | Sertraline hydrochloride oral liquid and preparation method thereof | |
| CN102283800B (en) | Sertaconazole nitrate suppository for treating vaginitis and preparation method thereof | |
| CN103893131B (en) | A kind of solid composite medicament containing Febustat | |
| CN104780907A (en) | Medicinal lozenge based on ibuprofen sodium dihydrate | |
| CN102380020A (en) | Garlic enteric-coated tablets and production method thereof | |
| CN102525979B (en) | Infant ibuprofen composition | |
| CN111116350A (en) | Preparation method of potassium sodium hydrogen citrate | |
| CN103690500A (en) | Phloroglucinol lyophilized oral preparation and preparation method thereof | |
| CN1709354A (en) | Injection agent of cordate houttuynia and honeysuckle and its preparing method | |
| CN103784948A (en) | Effervescent suppository for treating mammal vaginitis | |
| CN102018796A (en) | Rinse-free concentrated clear traditional Chinese medicinal itching-relieving lotion | |
| CN1771989A (en) | Compound prepn for treating women's inflammation | |
| CN102266305B (en) | Bifonazole vagina effervescent tablet and preparation method thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| GR01 | Patent grant | ||
| GR01 | Patent grant |