CN100446774C - Clindamycin hydrochloride vaginal effervescent tablet and its preparing method - Google Patents
Clindamycin hydrochloride vaginal effervescent tablet and its preparing method Download PDFInfo
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- CN100446774C CN100446774C CNB2005100100551A CN200510010055A CN100446774C CN 100446774 C CN100446774 C CN 100446774C CN B2005100100551 A CNB2005100100551 A CN B2005100100551A CN 200510010055 A CN200510010055 A CN 200510010055A CN 100446774 C CN100446774 C CN 100446774C
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- clindamycin hydrochloride
- acid
- effervescent tablet
- clindamycin
- vaginal effervescent
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Abstract
The present invention discloses a vaginal effervescent tablet made from clindamycin hydrochloride and a preparation method thereof. The clindamycin hydrochloride is applied to the vaginal effervescent tablet, and the clindamycin hydrochloride is used as a therapeutical agent. The vaginal effervescent tablet is composed of an effervescent disintegrating agent, a lubricating agent, an adhesive and a surfactant. After the vaginal effervescent tablet is locally applied, imperceptible and persistent foam can be generated in an effervescent disintegrating mode, and medicine is uniformly distributed in foam; thereby, the contact area of the medicine and vaginal mucosa is enlarged, and the medicine is fully absorbed. Because the medicine is applied to the vagina, the first pass effect of the liver is avoided, the adverse reaction caused by systemic medication is overcome, the toxicity is lowered, the effective concentration of the medicine on focus positions is enhanced, and the defects of other preparations for treating the bacterial vaginitis is overcome. The present invention has the advantages of scientific, reasonable and feasible formula, obvious treatment effect, no adverse reaction, and good economical and social benefits.
Description
Technical field
The present invention relates to a kind of effervescent tablet for the treatment of bacterial vaginosis, be specifically related to a kind of vagina effervescence by the Clindamycin Hydrochloride preparation.
Background technology
Clindamycin Hydrochloride belongs to lincomycin series antibiotics, antibacterial activity is high 4～8 times than lincomycin, gram positive bacteria such as staphylococcus (comprising the penicillin resistant strain), Streptococcus, diphtheria corynebacterium, anthrax bacillus etc. all there is higher antibacterial activity, the Grain-negative anaerobe is also had good antibacterial activity, and Bacteroides comprises that clinical common pathogenic anaerobe such as bacteroides fragilis, Fusobacterium, dyspepsiacoccus, peptostreptococcus, bacillus perfringens are extremely sensitive to this product mostly.And anaerobe is the main pathogens of pudendum, vaginitis, salpingitis, pelvic inflammatory disease, endometritis, pelvic cavity combined postoperative disease, and clindamycin can be brought into play important therapeutical effect to above-mentioned infection.
In China, the gynaecopathia sickness rate is up to more than 50%, and is higher at some outlying district sickness rate, especially suffers from gynaecopathia in the married woman mostly to some extent.Infectious disease is the most general in the gynaecopathia, and bacterial vaginosis is the modal vaginal infection disease of childbearing age women.Clindamycin is as a clinical line medicine of treatment bacterial vaginosis, and present domestic have only injection and capsule only have externally used paste and suppository abroad.
Summary of the invention
The object of the present invention is to provide a kind of vagina tissue that directly acts on, increase the medicine local concentration, act on lasting, easy to use, short treating period, curative effect soon, the effervescent tablet-clindamycin hydrochloride vaginal effervescent tablet of the treatment bacterial vaginosis that has no side effect.
The invention provides a kind of preparation method of clindamycin hydrochloride vaginal effervescent tablet, before the preparation that raw material and main adjuvant is dry in advance, control moisture content strengthens stability of formulation.
Clindamycin hydrochloride vaginal effervescent tablet of the present invention, its composition comprises:
Clindamycin 30～35%
Acid 22～35%
Basic salt 24～39%
Polyvinylpyrrolidone 2～5%
Tween 80 4～8%
Lubricant 0.1～0.8%
Described acid is organic acid or mineral acid, and organic acid is tartaric acid, fumaric acid, malic acid, and mineral acid is a boric acid.Described basic salt is sodium carbonate, sodium bicarbonate.Described polyvinylpyrrolidone can replace with Polyethylene Glycol.Described lubricant is magnesium stearate, Pulvis Talci.
The preparation method of clindamycin hydrochloride vaginal effervescent tablet agent of the present invention may further comprise the steps:
(1) Clindamycin Hydrochloride, acid, basic salt are sieved drying respectively;
(2) polyvinylpyrrolidone, tween 80 are added dehydrated alcohol and make binding agent;
(3) Clindamycin Hydrochloride, acid, basic salt are mixed, add binding agent, make soft material;
(4) 12 mesh sieves are granulated, oven dry, 16 mesh sieve granulate;
(5) add lubricant, be mixed;
(6) measure granule content, it is heavy to calculate sheet, is pressed into special-shaped sheet.
Main feature of the present invention is first clindamycin to be applied to the vagina effervescence agent, can the effervescent disintegrate produce a large amount of trickle and persistent foams after the use, medicine is evenly distributed in the foam, has enlarged the contact area of medicine and vaginal mucosa, absorb fully, evident in efficacy, avoid the liver first-pass effect of oral formulations, overcome the untoward reaction that systemic administration causes, reduced toxicity, improve the lesions position concentration medicine, thereby improved curative effect.Simultaneously also overcome external preparation such as unguentum, suppository and need use skewness, the defective of pollution clothes by utensil.
Another characteristics of the present invention are to adopt reasonably combination and technology in Recipe.In prescription, add the tween 80 of about 4-8%, can make foam duration longer, improve curative effect as surfactant; It can make polyvinylpyrrolidone be dissolved in fast in the dehydrated alcohol as binding agent, has shortened preparation time.On technology, the hydrophilic supplementary material is carried out drying earlier, thereby realize that soda acid mixes one-step palletizing simultaneously, promptly guaranteed the blended uniformity of supplementary material, avoid occurring phenomenons such as piebaldism, simultaneously stability of drug products and the production efficiency that improves again.
The mechanism of action of Clindamycin Hydrochloride is to combine with bacterial ribosome 50S subunit, stops peptide elongation, thereby suppresses the protein synthesis of bacterial cell, belong to bacteriostatic, also have bactericidal action when higher concentration, every of the present invention contains clindamycin 0.2g, dosage is relatively large, and action effect is remarkable.
The present invention reasonably is applied to the vagina effervescence agent with Clindamycin Hydrochloride, and its prescription is reasonable, technology is reliable, easy operating.Remarkable through clinical practice treatment bacterial vaginosis effect, untoward reaction is few, and advantage is obvious, overcome the defective of existing clindamycin dosage form, be a kind of vagina local application for the treatment of bacterial vaginosis safely and effectively, can promote, will produce remarkable economic efficiency and social benefit.
The specific embodiment
Embodiment 1
Clindamycin Hydrochloride 200g
Tartaric acid 150g
Sodium bicarbonate 170g
Boric acid 50g
Polyvinylpyrrolidone 15g
Tween 80 35g
Dehydrated alcohol 150ml
Magnesium stearate 2g
Pulvis Talci 2g
Clindamycin Hydrochloride, tartaric acid, sodium bicarbonate, boric acid are sieved dry control moisture＜2% respectively; Polyvinylpyrrolidone, tween 80 are added dehydrated alcohol make binding agent; Clindamycin Hydrochloride, tartaric acid, sodium bicarbonate, boric acid are mixed, add binding agent and make soft material; 12 mesh sieves are granulated, oven dry, 16 mesh sieve granulate; Add magnesium stearate and Pulvis Talci, be mixed; Pressing cost invention clindamycin hydrochloride vaginal effervescent tablet abnormity sheet is 1000 behind the mensuration granule content.
Embodiment 2
Clindamycin Hydrochloride 200g
Tartaric acid 170g
Sodium bicarbonate 192g
Polyvinylpyrrolidone 20g
Tween 80 40g
Dehydrated alcohol 150ml
Magnesium stearate 2g
With Clindamycin Hydrochloride, tartaric acid, sodium bicarbonate sieve respectively, drying, control moisture content＜2%;
Polyvinylpyrrolidone, tween 80, dehydrated alcohol are mixed with binding agent; With Clindamycin Hydrochloride, tartaric acid, sodium bicarbonate mixing, add binding agent, the system soft material; Granulate oven dry, 16 mesh sieve granulate with 12 mesh sieves.Add magnesium stearate, be mixed, pressing cost invention Clindamycin Hydrochloride effervescent tablet abnormity sheet is 1000 behind the mensuration granule content.
Use clindamycin hydrochloride vaginal effervescent tablet treatment bacterial vaginosis clinical effectiveness of the present invention and observe, and compare with the metronidazole effervescent tablet.
Physical data: non-anemia of pregnant woman woman 120 examples more than 18 years old, test group 60 examples, matched group 60 examples
Diagnostic criteria: vaginal secretions increases or distinguishes the flavor of for sparing the matter shape or having to smell as of rotten fish; The linear element cell accounts for more than 20% in wet sheet of vagina or the staining section; And meet in following 3 indexs at least 2: the vagina discharge opeing of (1) uniformity, (2) vagina PH＞4.7, (3) amine test positive.
Therapeutic Method: use clindamycin hydrochloride vaginal effervescent tablet of the present invention, behind the pudendum cleaning, with finger tablet is pushed the vagina deep before sleeping, 1 slice/day, 7 days is a course of treatment.The same test group of matched group Metronidazole Tablet usage and dosage.
Curative effect determinate standard: (1) cures: the symptom complete obiteration, and the leucorrhea outward appearance is normal, the stench flavor of no fish; Clues cell is less than 20%; Vagina PH＜4.7; Amine test is turned out cloudy.(2) produce effects: symptom and Signs alleviate; Clues cell is less than 20%; Binomial index vagina PH＜4.7, amine test is turned out cloudy and is met one.(3) invalid: symptom does not have improvement; Clues cell is more than more than 20%; Binomial index vagina PH＜4.7, amine test is turned out cloudy and is not all met.
Therapeutic outcome:
7 days effects relatively after test group and the treatment of control group
Group recovery from illness produce effects is invalid
Test group (N=60) 54 33
Matched group (N=60) 45 4 11
The test group cure rate is 90%, and effective percentage reaches 95%, and the matched group cure rate is 75%, and effective percentage reaches 82%.Clindamycin Hydrochloride effervescent tablet relapse rate of the present invention is extremely low, and untoward reaction is rare, has no side effect.
Claims (7)
1, a kind of clindamycin hydrochloride vaginal effervescent tablet is characterized in that composition comprises:
Clindamycin 30～35%
Acid 22～35%
Basic salt 24～39%
Polyvinylpyrrolidone 2～5%
Tween 80 4～8%
Lubricant 0.1～0.8%;
Its preparation method is:
(1) Clindamycin Hydrochloride, acid, basic salt are sieved drying respectively;
(2) polyvinylpyrrolidone, tween 80 are added dehydrated alcohol and make binding agent;
(3) Clindamycin Hydrochloride, acid, basic salt are mixed, add binding agent, make soft material;
(4) 12 mesh sieves are granulated, oven dry, 16 mesh sieve granulate;
(5) add lubricant, be mixed;
(6) measure granule content, it is heavy to calculate sheet, is pressed into special-shaped sheet.
2, clindamycin hydrochloride vaginal effervescent tablet according to claim 1 is characterized in that: described acid is organic acid or mineral acid, and organic acid is tartaric acid, fumaric acid or malic acid, and mineral acid is a boric acid.
3, clindamycin hydrochloride vaginal effervescent tablet according to claim 1 is characterized in that: described basic salt is sodium carbonate or sodium bicarbonate.
4, clindamycin hydrochloride vaginal effervescent tablet according to claim 1 is characterized in that: described lubricant is magnesium stearate or Pulvis Talci.
5, clindamycin hydrochloride vaginal effervescent tablet according to claim 1 is characterized in that: the weight of making 1000 each crude drug of effervescent tablet is:
Clindamycin Hydrochloride 200g
Tartaric acid 150g
Sodium bicarbonate 170g
Boric acid 50g
Polyvinylpyrrolidone 15g
Tween 80 35g
Dehydrated alcohol 150ml
Magnesium stearate 2g
Pulvis Talci 2g.
6, clindamycin hydrochloride vaginal effervescent tablet according to claim 1 is characterized in that: the weight of making 1000 each crude drug of effervescent tablet is:
Clindamycin Hydrochloride 200g
Tartaric acid 170g
Sodium bicarbonate 192g
Polyvinylpyrrolidone 20g
Tween 80 40g
Dehydrated alcohol 150ml
Magnesium stearate 2g.
7, the preparation method of the described clindamycin hydrochloride vaginal effervescent tablet agent of claim 1 is characterized in that may further comprise the steps:
(1) Clindamycin Hydrochloride, acid, basic salt are sieved drying respectively;
(2) polyvinylpyrrolidone, tween 80 are added dehydrated alcohol and make binding agent;
(3) Clindamycin Hydrochloride, acid, basic salt are mixed, add binding agent, make soft material;
(4) 12 mesh sieves are granulated, oven dry, 16 mesh sieve granulate;
(5) add lubricant, be mixed;
(6) measure granule content, it is heavy to calculate sheet, is pressed into special-shaped sheet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100100551A CN100446774C (en) | 2005-05-31 | 2005-05-31 | Clindamycin hydrochloride vaginal effervescent tablet and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100100551A CN100446774C (en) | 2005-05-31 | 2005-05-31 | Clindamycin hydrochloride vaginal effervescent tablet and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1748708A CN1748708A (en) | 2006-03-22 |
| CN100446774C true CN100446774C (en) | 2008-12-31 |
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| CNB2005100100551A Expired - Fee Related CN100446774C (en) | 2005-05-31 | 2005-05-31 | Clindamycin hydrochloride vaginal effervescent tablet and its preparing method |
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Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101744833B (en) * | 2008-12-02 | 2012-05-23 | 济南宏瑞创博医药科技开发有限公司 | Medicinal composition for treating bacterial vaginitis |
| CN102335151B (en) * | 2010-07-20 | 2015-07-08 | 杭州赛利药物研究所有限公司 | Clindamycin phosphate vaginal mucosa tablet and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002003896A1 (en) * | 2000-07-11 | 2002-01-17 | Umd, Inc. | Device and method for intravaginal or transvaginal treatment of fungal, bacterial, viral or parasitic infections |
| CN1360495A (en) * | 1999-08-06 | 2002-07-24 | 法玛西雅厄普约翰美国公司 | Intravaginal clindamycin ovule composition |
| WO2003020736A1 (en) * | 2001-08-28 | 2003-03-13 | Pharmacia Corporation | Crystaline clindamycin free base |
| CN1586497A (en) * | 2004-08-02 | 2005-03-02 | 程月发 | Clindamycin metronidazole vagina effervescent tablet and its preparing method and use |
-
2005
- 2005-05-31 CN CNB2005100100551A patent/CN100446774C/en not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1360495A (en) * | 1999-08-06 | 2002-07-24 | 法玛西雅厄普约翰美国公司 | Intravaginal clindamycin ovule composition |
| WO2002003896A1 (en) * | 2000-07-11 | 2002-01-17 | Umd, Inc. | Device and method for intravaginal or transvaginal treatment of fungal, bacterial, viral or parasitic infections |
| WO2003020736A1 (en) * | 2001-08-28 | 2003-03-13 | Pharmacia Corporation | Crystaline clindamycin free base |
| CN1586497A (en) * | 2004-08-02 | 2005-03-02 | 程月发 | Clindamycin metronidazole vagina effervescent tablet and its preparing method and use |
Non-Patent Citations (2)
| Title |
|---|
| 克林霉素阴道泡腾片的临床疗效观察. 王美村等.哈尔滨医科大学学报，第30卷第6期. 1996 |
| 克林霉素阴道泡腾片的临床疗效观察. 王美村等.哈尔滨医科大学学报，第30卷第6期. 1996 * |
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| CN1748708A (en) | 2006-03-22 |
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Inventor after: Shao Fangxiao Inventor after: Zhao Dawei Inventor after: Du Lirong Inventor after: Li Jianping Inventor after: Cui Xiaobiao Inventor after: Cui Yingbin Inventor after: Tian Xiaokun Inventor before: Shao Fangxiao Inventor before: Li Jianping Inventor before: Cui Xiaobiao Inventor before: Cui Yingbin Inventor before: Tian Xiaokun |
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Free format text: CORRECT: INVENTOR; FROM: SHAO FANGXIAO LI JIANPING CUI XIAOBIAO CUI YINGBIN TIAN XIAOKUN TO: SHAO FANGXIAO ZHAO DAWEI DU LIRONG LI JIANPING CUI XIAOBIAO CUI YINGBIN TIAN XIAOKUN |
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Granted publication date: 20081231 Termination date: 20170531 |
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| CF01 | Termination of patent right due to non-payment of annual fee |