CN102266284A - Secnidazole pessary and preparation process thereof - Google Patents
Secnidazole pessary and preparation process thereof Download PDFInfo
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- CN102266284A CN102266284A CN 201110164664 CN201110164664A CN102266284A CN 102266284 A CN102266284 A CN 102266284A CN 201110164664 CN201110164664 CN 201110164664 CN 201110164664 A CN201110164664 A CN 201110164664A CN 102266284 A CN102266284 A CN 102266284A
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Abstract
The invention relates to secnidazole pessary, which consists of the following components by weight: 500 grams of secnidazole serving as a major ingredient and 2,300 grams of 36 type mixed fatty glyceride serving as a minor ingredient to prepare 1,000 grains of suppository, wherein each grain is 2.8 grams, the 36 type mixed fatty glyceride is a mixture of triglyceride, diglyceride and monoglyceride, and a melting point of the 36 type mixed fatty glyceride is between 35 and 37 DEG C. The secnidazole pessary is absorbed by vaginae directly, and does not harm hearts, kidneys and livers by detection. The secnidazole pessary has a good curative effect, does not have side effect, has simple components and is convenient to use. The invention also discloses a preparation process for the secnidazole pessary.
Description
Technical field
The present invention relates to a kind of secnidazole vaginal suppository, the invention still further relates to the preparation technology of this secnidazole vaginal suppository.
Background technology
Secnidazole (Secnidazole) belongs to the 5-nitro glyoxaline compound, and the characteristics of 5-nitroimidazoles medicine are that anaerobe is had selection toxicity, and facultative and aerobe are not then had influence.It is 0.70mg/L that the minimum of secnidazole is killed trichomonacide concentration, and metronidazole is 0.60mg/L, and tinidazole is 1.125mg/L.The minimum of secnidazole is killed trichomonacide and is similar to metronidazole, and is lower than tinidazole, and it is 1/10 of metronidazole that secnidazole presses down growth concentration to Giardia lamblia trophozoite external 50%.
Secnidazole toxicity is extremely low, and the safe dose of long term toxicity is 400mg/kg, and 5-nitroimidazoles medicine structure may have potential mutagenic action, but the mutagenicity test of secnidazole is found that secnidazole does not have mutagenic action.
The similar medicine with other of secnidazole is compared, and absolute bioavailability is near 100%.The secnidazole half-life, the secnidazole half-life was the longest between 17-29h.Secnidazole is the metabolite of no physiologically active by oxidative metabolism in hepatic tissue.Secnidazole clearance rate in the body is approximately 1.68L/h (28ml/mg).
Secnidazole is the 5-nitro glyoxaline antibacterials that French Rhone-Poulenc Rorer develops the earliest, 1980 in Switzerland's Initial Public Offering, China's approval in 1998 is advanced product from French Luo Napulang Lean company, and the antibacterial activity of secnidazole, safety, pharmacokinetics skill and effectiveness all are better than similar medicine.
At present, go up existing secnidazole injection, secnidazole tablet and secnidazole vagina effervescence etc. both at home and abroad, but the component of this class preparation is complicated.As Chinese patent 200310109011.5 secnidazole vagina effervescence and production methods thereof, except that the active component secnidazole is arranged, also have multiple adjuvants such as medicinal disintegrating agent, binding agent, lubricant, wetting agent, filler, because adjuvant is more, so this preparation technology is also complicated.
The Chinese patent publication number is that CN1548043A discloses a kind of secnidazole injection and preparation method thereof, it is to be principal agent with the secnidazole, the adjuvant that oozes regulating action such as being had makes, but this injection is to heart, kidney, liver has damage, testing data factually shows: behind injection secnidazole injection, the heartbeat amplitude has bigger decline (0.41g-0.19g), the creatinine of kidney and blood urea nitrogen raise simultaneously, the transaminase of liver can raise, can descend after 7 days in drug withdrawal, but raise during also than medication not, this shows that the secnidazole injection is to heart, kidney, liver function has caused damage to a certain degree.
The Chinese patent publication number is that CN1973838A discloses a kind of secnidazole tablet and preparation method thereof, it is to be principal agent with the secnidazole, make with microcrystalline Cellulose, starch, pregelatinized Starch, lactose, cross-linked carboxymethyl cellulose sodium, crospolyvinylpyrrolidone, polyvinylpyrrolidone or hypromellose, magnesium stearate, Pulvis Talci, micropowder silica gel etc., component and preparation technology are very complicated.Secnidazole tablet will be by bigger with respect to the side effect of injection, at first after the drug oral administration, enter liver, metabolism in liver through portal vein, secnidazole can be destroyed by the first-pass effect of liver, and the while is subject to the effect destruction of pH or enzyme and loses activity in gastrointestinal.
Therefore, invent a kind of secnidazole vaginal suppository, it directly absorbs by vagina, and stomach, liver, the undamaged newtype drug of kidney are become an important and urgent job.
Summary of the invention
The objective of the invention is to overcome the weak point of above-mentioned existing various preparations, and a kind of secnidazole vaginal suppository is provided, another object of the present invention is to provide a kind of technology for preparing above-mentioned secnidazole vaginal suppository.
The objective of the invention is to reach: the secnidazole vaginal suppository by following measure, it is characterized in that it is made up of following component: major ingredient secnidazole 500g, adjuvant 36 type mixed fatty glycerides 2300g, make 1000 suppositorys, every heavy 2.8 grams, described 36 type mixed fatty glycerides are the mixture of triglyceride, diacylglycerol and monoglyceride, and the fusing point of 36 type mixed fatty glycerides is 35-37 ℃.
The technology of preparation secnidazole vaginal suppository is characterized in that it comprises the steps:
(1), secnidazole is pulverized, it is standby to cross the 100-150 mesh sieve,
(2), take by weighing main materials and auxiliary materials, earlier adjuvant is added in the colloid mill, in 50-55 ℃ of water-bath, heat melting, slowly add secnidazole and constantly stir and make mix homogeneously, inject the suppository perfusion unit, the melting again of form, flash, injection molding by recipe quantity;
(3), with the material transfer of molding, put in storage after being packaged as finished product.
In technique scheme, described flash melting again is meant the material melting after the strickling of the material after solidifying, the demoulding.
In technique scheme, described secnidazole is pulverized, and it is standby to cross 120 mesh sieves.
Usage and consumption: vagina administration, one time 1,1 time on the one, logotype 7 days was a course of treatment.
Use classes: anaerobe resistant, ameba worm, infusorian, giardia lamblia stiles infect medicine.
Storage: shading, airtight, preserve at shady and cool dry place below 30 ℃.
Attention: the early stage careful usefulness of gestation.
Secnidazole vaginal suppository of the present invention has following advantage: it not only can local action, and the effect of whole body is still arranged after absorbing by vagina.Prescription and production technology are all simpler, practical, are convenient to management and control.
Secnidazole suppository and secnidazole tablet relatively have following advantage: 1. medicine is not destroyed by the effect of gastrointestinal pH value or enzyme and loses activity.2. medicine can not have zest to gastric mucosa, and can avoid stimulates.3. the medicine vagina absorbs, and does not resemble oral drugs and destroyed by the liver first-pass effect.4. the oral interference factor of vagina absorptance is few.5. for or the sheet of being reluctant to swallow, ball and capsular patient, especially baby or child can be with this method administration.6. be an effective way to treatment with the patient who vomits.
Secnidazole suppository and secnidazole injection relatively have following advantage: the medicine vagina absorbs, and can not cause the damage of heart, kidney, liver after testing.
The experiment proved that good effect of the present invention, have no side effect substantially that proportioning is simple, easy to use.
The specific embodiment
Describe performance of the present invention in detail below by embodiment, but they do not constitute limitation of the invention, only do for example, simultaneously by illustrating that advantage of the present invention will become clear more and easy and understand.
Secnidazole vaginal suppository of the present invention, it is made up of following component: major ingredient secnidazole 500g, adjuvant 36 type mixed fatty glycerides 2300g make 1000 suppositorys, every heavy 2.8 grams,
Mixed fatty glycerides is the mixture of triglyceride, diacylglycerol and monoglyceride.Difference according to its fusing point can be divided into 34 types, 36 types, 38 types, four kinds of models of 40 types.Wherein 34 type fusing points are 33-35 ℃, and 36 type fusing points are 35-37 ℃, and 38 type fusing points are 37-39 ℃, and 40 type fusing points are 39-41 ℃.
The molecular formula of triglyceride, diacylglycerol and monoglyceride is respectively:
The preparation technology of secnidazole vaginal suppository of the present invention, it comprises the steps:
(1), secnidazole is pulverized, it is standby to cross the 100-150 mesh sieve,
(2), take by weighing main materials and auxiliary materials, earlier adjuvant is added in the colloid mill, in 50-55 ℃ of water-bath, heat melting, slowly add secnidazole and constantly stir and make mix homogeneously, inject the suppository perfusion unit, the melting again of form, flash, injection molding by recipe quantity;
(3), with the material transfer of molding, put in storage after being packaged as finished product.
Described flash melting again is meant the material melting after the strickling of the material after solidifying, the demoulding.Described secnidazole is pulverized, and it is standby to cross 120 mesh sieves.
One, the selection of adjuvant:
The inventor proves that by experiment adjuvant selects for use mixed fatty glycerides better than other adjuvant.
The adjuvant that suppository is commonly used has: glycerin gelatine, Polyethylene Glycol.Because secnidazole is to wet, thermally labile, the variable color of easily degrading is not so consider that glycerin gelatine, Polyethylene Glycol are as adjuvant.
According to 2000 editions appendix of Chinese Pharmacopoeia to the requirement of vaginal suppository and the physicochemical property of secnidazole, the key issue of development secnidazole vaginal suppository is that melting of suppository becomes time limit and dispersing uniformity and the stability of drug of medicine in substrate, so will melt change time limit and the dispersing uniformity of medicine in substrate investigation index, and be that the heating-up temperature that guarantees the stability of drug substrate in the preparation process should be lower than 60 ℃ as formulation and technology.According to the above, designed four typical prescriptions, technology is as follows:
Investigation project and result
Prescription screening is the result show:
1, the secnidazole powder diameter influences its dispersing uniformity in substrate, and crossing 120 mesh sieve ends can be uniformly dispersed in melting substrate, places not free settling layering.
2, use 36 type mixed fatty glycerides as substrate (adjuvant) separately, suppository melts and becomes the time limit and meet the pharmacopeia requirement, use separately 38 type mixed fatty glycerides and 36 types, 38 types to mix and use as substrate (adjuvant), suppository melts and becomes the time limit and do not meet the pharmacopeia requirement.
According to above result of the test, select prescription 3 as optimal scheme.
38 type mixed fatty glycerides are for to be that the mixture of triglyceride, diacylglycerol and monoglyceride, the fusing point of 38 type mixed fatty glycerides are 37-39 ℃.
Be the treatment contrast experiment of oral of secnidazole vaginal suppository and secnidazole below:
Choose patient's 52 examples, be the women, age 18-45 year, adopt the treatment of secnidazole vaginal suppository.Choose matched group 40 examples, be the women, age 18-43 year, adopt oral of secnidazole to treat.
The content of observing is treatment time, and human body is to the reaction of medicine etc.Each patient all adopts identical dose every day.
Statistical result:
Use secnidazole vaginal suppository (with healing person's counting)
Obvious rising does not appear in the creatinine of the kidney of human body and blood urea nitrogen during medication, and obvious rising does not appear in the transaminase of liver.
Use oral of secnidazole (with healing person's counting)
Obviously raising appears in the creatinine of the kidney of human body and blood urea nitrogen during medication, and obvious rising also appears in the transaminase of liver, and the number that occurs stomach discomfort simultaneously has 5 people.
Through above correlation data as can be known: use the secnidazole vaginal suppository obviously to shorten with using oral treatment time of secnidazole, the healing number increases in the identical time, invalid number reduces, and little to the human body side effect, analyzes by statistics to have significant difference.
Analyze former because behind the oral administration, enter liver through portal vein, metabolism in liver, secnidazole can be destroyed by the first-pass effect of liver, and the effect destruction and the part that are subject to pH or enzyme simultaneously in gastrointestinal lose activity, and have also increased the weight of the drainage burden of kidney simultaneously.
Be the treatment contrast experiment of secnidazole vaginal suppository and secnidazole injection below:
Choose patient's 48 examples, be the women, age 22-50 year, adopt the treatment of secnidazole vaginal suppository.Choose matched group 36 examples, be the women, age 21-48 year, adopt the secnidazole injection to treat.
The content of observing is treatment time, and human body is to the reaction of medicine etc.Each patient all uses identical dose every day.
Statistical result:
Use secnidazole vaginal suppository (with healing person's counting)
Obvious rising does not appear in the creatinine of the kidney of human body and blood urea nitrogen during medication, and obvious rising does not appear in the transaminase of liver.
Use secnidazole injection (with healing person's counting)
Obviously raising appears in the creatinine of the kidney of human body and blood urea nitrogen during medication, and obvious rising also appears in the transaminase of liver, and the number that occurs discomforts such as having palpitation simultaneously has 3 people.
Through above correlation data as can be known: use the secnidazole vaginal suppository and use secnidazole injection for treating time, healing number, invalid number is suitable substantially, analyzes no significant difference by statistics; But the secnidazole vaginal suppository is littler to the human body side effect.
Claims (4)
1. secnidazole vaginal suppository, it is characterized in that it is made up of following component: major ingredient secnidazole 500g, adjuvant 36 type mixed fatty glycerides 2300g, make 1000 suppositorys, every heavy 2.8 grams, described 36 type mixed fatty glycerides are the mixture of triglyceride, diacylglycerol and monoglyceride, and the fusing point of 36 type mixed fatty glycerides is 35-37 ℃.
2. the technology of the described secnidazole vaginal suppository of preparation claim 1 is characterized in that it comprises the steps:
(1), secnidazole is pulverized, it is standby to cross the 100-150 mesh sieve,
(2), take by weighing main materials and auxiliary materials, earlier adjuvant is added in the colloid mill, in 50-55 ℃ of water-bath, heat melting, slowly add secnidazole and constantly stir and make mix homogeneously, inject the suppository perfusion unit, the melting again of form, flash, injection molding by recipe quantity;
(3), with the material transfer of molding, put in storage after being packaged as finished product.
3. according to the preparation technology of the described secnidazole vaginal suppository of claim 2, it is characterized in that described flash again melting be meant with the material after solidifying wipe off, material melting after the demoulding.
4. according to the preparation technology of the described secnidazole vaginal suppository of claim 2, it is characterized in that described secnidazole pulverizing, it is standby to cross 120 mesh sieves.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
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| CN 201110164664 CN102266284A (en) | 2011-06-20 | 2011-06-20 | Secnidazole pessary and preparation process thereof |
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| CN 201110164664 CN102266284A (en) | 2011-06-20 | 2011-06-20 | Secnidazole pessary and preparation process thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103784390A (en) * | 2013-12-31 | 2014-05-14 | 哈尔滨欧替药业有限公司 | Secnidazole vagina expansive suppository and preparation method and detection method thereof |
| US10335390B2 (en) | 2014-09-05 | 2019-07-02 | Symbiomix Therapeutics, Llc | Secnidazole for use in the treatment of bacterial vaginosis |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1546020A (en) * | 2003-12-02 | 2004-11-17 | 浙江巨都集团股份有限公司 | Vaginal effervescence tablet of secnidazole and its preparation |
| CN1973838A (en) * | 2006-11-28 | 2007-06-06 | 湖北科益药业股份有限公司 | Secnidazole tablet and its prepn process |
| CN101698101A (en) * | 2008-12-02 | 2010-04-28 | 济南宏瑞创博医药科技开发有限公司 | Medicine composite for treating vaginitis |
-
2011
- 2011-06-20 CN CN 201110164664 patent/CN102266284A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1546020A (en) * | 2003-12-02 | 2004-11-17 | 浙江巨都集团股份有限公司 | Vaginal effervescence tablet of secnidazole and its preparation |
| CN1973838A (en) * | 2006-11-28 | 2007-06-06 | 湖北科益药业股份有限公司 | Secnidazole tablet and its prepn process |
| CN101698101A (en) * | 2008-12-02 | 2010-04-28 | 济南宏瑞创博医药科技开发有限公司 | Medicine composite for treating vaginitis |
Non-Patent Citations (1)
| Title |
|---|
| 《中国现代应用药学杂志》 20080430 陈文钦 《塞克硝唑栓的研制和质量控制》 1-4 第25卷, 第2期 * |
Cited By (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103784390A (en) * | 2013-12-31 | 2014-05-14 | 哈尔滨欧替药业有限公司 | Secnidazole vagina expansive suppository and preparation method and detection method thereof |
| CN103784390B (en) * | 2013-12-31 | 2016-10-05 | 哈尔滨欧替药业有限公司 | Secnidazole vaginal expansion plug and preparation method thereof and detection method |
| US10335390B2 (en) | 2014-09-05 | 2019-07-02 | Symbiomix Therapeutics, Llc | Secnidazole for use in the treatment of bacterial vaginosis |
| US10682338B2 (en) | 2014-09-05 | 2020-06-16 | Lupin Inc. | Secnidazole for use in the treatment of bacterial vaginosis |
| US10849884B2 (en) | 2014-09-05 | 2020-12-01 | Lupin Inc. | Secnidazole for use in the treatment of bacterial vaginosis |
| US10857133B2 (en) | 2014-09-05 | 2020-12-08 | Lupin Inc. | Secnidazole for use in the treatment of bacterial vaginosis |
| US11000507B2 (en) | 2014-09-05 | 2021-05-11 | Lupin Inc. | Secnidazole for use in the treatment of bacterial vaginosis |
| US11000508B2 (en) | 2014-09-05 | 2021-05-11 | Lupin Inc. | Secnidazole for use in the treatment of trichomoniasis |
| US11020377B2 (en) | 2014-09-05 | 2021-06-01 | Lupin Inc. | Secnidazole for use in the treatment of bacterial vaginosis |
| US11324721B2 (en) | 2014-09-05 | 2022-05-10 | Lupin Inc. | Secnidazole for use in the treatment of trichomoniasis |
| US11602522B2 (en) | 2014-09-05 | 2023-03-14 | Lupin Inc. | Secnidazole for use in the treatment of sexually transmitted infection |
| US11684607B2 (en) | 2014-09-05 | 2023-06-27 | Lupin, Inc. | Secnidazole for use in the treatment of bacterial vaginosis |
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Application publication date: 20111207 |