CN104323983B - A kind of Policresulen suppository - Google Patents
A kind of Policresulen suppository Download PDFInfo
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- CN104323983B CN104323983B CN201410563316.1A CN201410563316A CN104323983B CN 104323983 B CN104323983 B CN 104323983B CN 201410563316 A CN201410563316 A CN 201410563316A CN 104323983 B CN104323983 B CN 104323983B
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- policresulen
- suppository
- polyoxyethylene
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Abstract
The invention discloses a kind of Policresulen suppository, it is made up of Policresulen, polyoxyethylene and polyoxyethylene stearate fat (40).Compared with prior art, Policresulen suppository prepared by the present invention, solve the degraded of Policresulen, and the Leakage of suppository；And production technology is simple, it is suitable for industrialized production.
Description
Technical field
The invention belongs to pharmaceutical technology field, be specifically related to a kind of Policresulen suppository.
Background technology
Policresulen and preparation thereof the earliest by Germany hectogram pause pharmaceutical factory develop, in 1993 start import, like treasured
Treat and record as national essential drugs.Policresulen is the hemostasis of a kind of local and bactericide, has pathogen the strongest
Killing action, be mainly used in gynaecology, surgery and dept. of dermatology, ear-nose-throat department clinically, have an advantage in that normal tissue is lossless
Wound.
Policresulen is highly acid material, and its mechanism of action is to be killed bacterium by strong acid and protein coagulation effect, dripped
The multiple pathogenic microorganisms such as worm, mould；Can be selectively applied to occur epithelial cell and the columnar epithelium of dystopy of pathology, make
Solidification, sex change, come off, and promote tissue repair, cause vessel retraction and plasma protein solidification to stop blooding, and do not affect normal
Scaly epithelium.In Amino-Cerv, the sour environment of vagina can be recovered, be unfavorable for the excessive multiplication of germ, beneficially physiology bacterium
Group's grows again, and can alleviate the malaise symptoms such as pruritus vulvue, leucorrhea increasing.
From treatment results analysis, the various vaginitis of patients treated with Policresulen, there is wide spectrum, spy efficiently, conveniently, safely
Point, and to the improvement of local symptom and reduce vaginal fluid and have positive effect, be conducive to downright bad or pathological tissues regeneration and on
Again the covering of skin, harmless to health tissues, have no adverse reaction after medication, be the novel of a kind of good treatment gynaecological imflammation
Medicine, clinic is promoted the use of.
The most clinical conventional Policresulen preparation is pessary, 36% solution or gel.But current suppository
Shortcoming be easily to melt and flow out, have greasy feeling, after medicine-feeding, have burning sensation；Concentrate can need to use, dilute after water dilutes
It is difficult to ensure that the accuracy of solution concentration during releasing, and there is the hygienic issues of easy pollution clothes and bed clothes；Gel needs
Vagina surface is coated, although said preparation is good in the tack of vaginal mucosal surfaces, but is difficult to by applicating implement
Ensure that coating uniformly, medication dead angle (such as fornix vaginae portion) easily occurs, is more crucially administered inconvenience.
CN102824358A discloses a kind of Policresulen compound suppository, uses soybean lecithin and mixing-in fat acid glycerol
Ester is suppository base, and fusing point is relatively low, easily from internal outflow, medication inconvenience after thawing.
CN101919807A discloses the suppository composition of a kind of performance improvement, and the polyoxyethylene using HMW is base
Matter, but also need to other oleaginous bases and alcohols with the use of, be used alone the polyoxyethylene of HMW when filling,
Because of matrix more thickness, filling inconvenience.
CN1771989A discloses a kind of compound preparation treating gynaecological imflammation, uses glycerin gelatine, polyethylene glycol, polyoxy
Ethene 40 stearate and cocoa butter etc. are as suppository base, but this compound preparation gives the autopath's medication of some main components
Bring inconvenience, and corresponding side effect also can increase.
CN103181889A and CN103520087A discloses the technology of preparing of Policresulen expansible plug, containing of expansible plug
Medicine matrix is fully contacted with vaginal walls, and active medicine bioavilability improves, but expanding material water suction physical expansion, water suction
Expand slowly and substantial amounts of liquid can be absorbed；Expanding material imbibition, causes vaginal dryness, and discomfort, foreign body sensation strengthen.
Swell value size difficulty control, the also problem of unavoidable liquid outflow.Even if the way using tail end to intercept in CN103520087A, expand
Sliver and other elastomers expand irregular, it is impossible to be close to vagina epithelium and mucous membrane well, solve liquid side leakage effect
Undesirable.Such expansible plug tail end all stay cord, also brings discomfort to patient.
Summary of the invention
For the deficiencies in the prior art, inventor considers to prepare a kind of poly-first with water-soluble medium polyethylene glycol as matrix
Phenol sulphur aldehyde suppository, because polyethylene glycol fusing point is high, can slowly melt in vivo, it is to avoid fat-soluble matrix is low and rapid because of fusing point
The problem melted and slip or flow out liquid (hereinafter referred to as: leakage of oil).But, because Policresulen is highly acid material, with
After polyethylene glycol contact, degraded rapidly, has related substance to increase, the best solution.
For solving to contact the problem of degraded with polyethylene glycol, inventor has carried out a large amount of creative work, has been found surprisingly that,
When the solution of Policresulen adds s6 (40), and the stability of preparation significantly improves.Reason is probably tristearin
Poly-hydrocarbon oxygen ester (40) of acid is a kind of nonionic surface active agent, has a preferable stabilization to Policresulen, but merely
Use s6 (40), it is impossible to avoiding oil leakage phenomenon, double suppository is prepared in inventor's consideration further, first will be poly-
It is filled in suppository bubble-cap after ethylene glycol is melted, cooling shaping, then by Policresulen and s6 (40)
Fused solution pours into, and well avoids contacting of medicine and polyethylene glycol, forms double suppository, thus can improve stability,
The problem that turn avoid the easy leakage of oil of fat-soluble matrix.But spillage test finds, only makes moderate progress for Leakage, still can not
Avoid Leakage completely.
For preventing leakage of oil further, inventor has carried out serial experiment, when replacing polyethylene glycol with polyoxyethylene, because of poly-
Oxygen ethene has preferable booster action, and suppository medicated layer release is faster；When suppository uses, medicated layer is first pushed, polyoxy second
Alkene layer is at tail end, and this layer expands, and hinders leaking outside of policresulen solution.Because polyoxyethylene is to have relatively low water suction
Property and the swellability (swelling about 2-8 times) of appropriateness and have mucous membrane attach property and the preferable macromolecule resin of biocompatibility.
Therefore, it is an object of the invention to provide a kind of stay-in-grade Policresulen double suppository, poly-first can be solved
The stability of phenol sulphur aldehyde, can preferably solve again Leakage.
Specifically, the present invention is achieved through the following technical solutions:
The invention provides a kind of Policresulen suppository, it is by Policresulen, polyoxyethylene and polyoxyethylene stearate
Ester (40) forms.
Described Policresulen suppository, its proportioning is:
Policresulen 60-120mg
Polyoxyethylene 1-2g
S6 (40) 0.3-1.4g.
Described Policresulen suppository, its proportioning is:
Policresulen 90mg
Polyoxyethylene 1-2g
S6 (40) 0.3-1.4g.
Above-described Policresulen suppository, its polyoxyethylene is 1 with the weight ratio of s6 (40):
0.3-0.7.Preferably, weight ratio is 1: 0.5.
Described Policresulen suppository, its polyoxyethylated molecular weight is 10000-30000.
It is a further object of the present invention to provide the preparation method of a kind of Policresulen suppository.
Above-described Policresulen suppository, prepares by the following method:
A. polyoxyethylene adds heat fusing, is filled in suppository bubble-cap, cooling shaping；
B. s6 (40) adds heat fusing, adds Policresulen, stirs, be filled into step a and prepare
Containing in polyoxyethylene blank suppository bubble-cap, cooling, shaping.
Compared with prior art, Policresulen suppository prepared by the present invention, solve liquid during suppository uses
Leaking outside and easily skid off problem, constant product quality, accelerating investigation has related substance to be basically unchanged；And its with after be comfortable on, nothing
Foreign body sensation, excitant is little, easy cleaning.
Detailed description of the invention
Following example further describe preparation process and the beneficial effect of the present invention, and embodiment is only used for the mesh of illustration
, do not limit the scope of the invention, simultaneously those of ordinary skill in the art according to the present invention made obvious change and
Within modification is also contained in the scope of the invention.
Embodiment 1
Policresulen 60mg
Polyoxyethylene 10000 2g
S6 (40) 1.4g
Preparation technology:
Polyoxyethylene 10000 is heated to 65 DEG C and melts, and is filled in suppository bubble-cap, 10 DEG C of cooling shapings；
S6 (40) is heated to 40 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 8 DEG C of coolings, shaping.
Embodiment 2
Policresulen 120mg
Polyoxyethylene 30000 2g
S6 (40) 0.6g
Preparation technology:
Polyoxyethylene 30000 is heated to 70 DEG C and melts, and is filled in suppository bubble-cap, 8 DEG C of cooling shapings；
S6 (40) is heated to 42 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 6 DEG C of coolings, shaping.
Embodiment 3
Policresulen 120mg
Polyoxyethylene 30000 2g
S6 (40) 0.3g
Preparation technology:
Polyoxyethylene 30000 is heated to 70 DEG C and melts, and is filled in suppository bubble-cap, 8 DEG C of cooling shapings；
S6 (40) is heated to 42 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 6 DEG C of coolings, shaping.
Embodiment 4
Policresulen 90mg
Polyoxyethylene 20000 2g
S6 (40) 1g
Preparation technology:
Polyoxyethylene 20000 is heated to 65 DEG C and melts, and is filled in suppository bubble-cap, 6 DEG C of cooling shapings；
S6 (40) is heated to 45 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 5 DEG C of coolings, shaping.
Embodiment 5
Policresulen 90mg
Polyoxyethylene 20000 1g
S6 (40) 2g
Preparation technology:
Polyoxyethylene 20000 is heated to 65 DEG C and melts, and is filled in suppository bubble-cap, 6 DEG C of cooling shapings；
S6 (40) is heated to 45 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 5 DEG C of coolings, shaping.
Embodiment 6
Policresulen 90mg
Polyoxyethylene 20000 3g
S6 (40) 0.2g
Preparation technology:
Polyoxyethylene 20000 is heated to 65 DEG C and melts, and is filled in suppository bubble-cap, 6 DEG C of cooling shapings；
S6 (40) is heated to 45 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 5 DEG C of coolings, shaping.
Comparative example 1
Policresulen 90mg
Polyoxyethylene 20000 3g
Preparation technology:
Polyoxyethylene 20000 is heated to 65 DEG C and melts, and adds Policresulen, stirs, be filled into containing polyoxy second
In the suppository bubble-cap of alkene, 5 DEG C of coolings, shaping.
Comparative example 2
Policresulen 90mg
S6 (40) 3g
Preparation technology:
S6 (40) is heated to 45 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 5 DEG C of coolings, shaping.
Comparative example 3
Policresulen 90mg
Macrogol 4000 2g
S6 (40) 1g
Preparation technology:
Macrogol 4000 is heated to 65 DEG C and melts, and is filled in suppository bubble-cap, 6 DEG C of cooling shapings；
S6 (40) is heated to 45 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 5 DEG C of coolings, shaping.
Comparative example 4
Policresulen 90mg
Macrogol 4000 2g
S6 (40) 1g
Preparation technology:
Macrogol 4000 and s6 (40) mixture are heated to 65 DEG C and melt, and add Policresulen,
Stir, be filled in suppository bubble-cap, 5 DEG C of coolings, shaping.
Comparative example 5
Policresulen 90mg
Polyoxyethylene 20000 2g
S6 (40) 1g
Preparation technology:
Polyoxyethylene 20000 and s6 (40) mixture are heated to 65 DEG C and melt, and add Policresulen,
Stir, be filled in suppository bubble-cap, 5 DEG C of coolings, shaping.
Comparative example 6
Policresulen 90mg
Polyoxyethylene 700000 2g
S6 (40) 1g
Preparation technology:
Polyoxyethylene 700000 is heated to 85 DEG C and melts, and is filled in suppository bubble-cap, 6 DEG C of cooling shapings；
S6 (40) is heated to 45 DEG C and melts, and adds Policresulen, stirs, and is filled into containing poly-
In the suppository bubble-cap of oxygen ethene, 5 DEG C of coolings, shaping.
Checking embodiment
1. leak check:
Taking suppository 1, polyoxyethylene layer, in bottom, joins in the special funnel (temperature 37 DEG C) of aperture 1cm, simulates chamber
When road uses, whether Policresulen bolt exists Leakage.
2. have related substance to detect:
Chromatographic condition: chromatographic column: octadecylsilane chemically bonded silica chromatographic column；Flowing phase: with 1% ammonium acetate solution for stream
Dynamic phase A, with methyl alcohol as Mobile phase B；Using gradient elution, program is as follows:
| Time/minute | Mobile phase A/% | Mobile phase B/% |
| 0 | 90 | 10 |
| 3 | 75 | 25 |
| 22 | 57 | 43 |
| 38 | 57 | 43 |
| 40 | 90 | 10 |
Flow velocity: 0.8m1 min-1；Detection wavelength: 280nm；Sample size: 10 μ l；Column temperature: 30 DEG C.
Sample determination: it is appropriate (being approximately equivalent to Policresulen 90mg) that precision weighs sample, adds water and is surely dissolved in 100ml measuring bottle
In, as need testing solution；Another precision weighs metacresol-4, and 6-disulfonic acid is appropriate, adds and dissolves and dilute constant volume, takes 10 respectively
μ l enters liquid chromatograph, must not cross 0.5%.
The impact on Policresulen suppository of table 1. accelerated test
As seen from the table, embodiment of the present invention 1-4, after accelerating to investigate, there is related substance to be basically unchanged, without oil leakage phenomenon；Real
Execute example 5, with substantial amounts of s6 (40), constant despite related substance, but in spillage test, a large amount of matrix are stearic
Poly-hydrocarbon oxygen ester (40) thawing of acid can dissolve part polyoxyethylene, has slight oil leakage phenomenon；Embodiment 6, matrix polyoxyethylene stearate
Ester (40) consumption is very few, it is impossible to fully packaging medicine, can contact with polyoxyethylene, have related substance to increase；And in the process of use
Chinese traditional medicine rate of release is fast, and excitant is strong, does not plays the due effect of s6 (40) matrix.Polyoxyethylene is used
Measure excessive, not only increase preparation cost, and suppository can be caused to expand volume and increase, cause patient medication uncomfortable；Contrast is real
Executing example 1, matrix is all with polyoxyethylene, although oil-proof, but has related substance to increase substantially；Comparative example 2, and matrix is whole
Use s6 (40), be basically unchanged despite related substance, but leakage of oil is serious；Comparative example 3, use polyethylene glycol
4000 replace polyoxyethylene, have slight leakage of oil, and have related substance to increase substantially；Comparative example 4, the suppository obtained by this technique
Having related substance to increase, oil leakage phenomenon is obvious；Comparative example 5, and the suppository obtained by this technique has related substance to increase, and have slight
Oil leakage phenomenon；Comparative example 6, use the polyoxyethylene of HMW instead, when filling polyoxyethylene layer, because of feed liquid thickness, nothing
Method is the most filling.
Claims (4)
1. a Policresulen suppository, it is characterised in that it is by Policresulen, polyoxyethylene and s6
(40) composition, described polyoxyethylated molecular weight is 10000-30000；Described polyoxyethylene and s6 (40)
Weight ratio is 1: 0.3-0.7；Described Policresulen suppository is prepared by the following method:
A. polyoxyethylene adds heat fusing, is filled in suppository bubble-cap, cooling shaping；
B. s6 (40) adds heat fusing, adds Policresulen, stirs, and be filled into prepared by step a contains
Have in polyoxyethylene blank suppository bubble-cap, cooling, shaping.
Policresulen suppository the most according to claim 1, it is characterised in that
Policresulen 60-120mg
Polyoxyethylene 1-2g
S6 (40) 0.3-1.4g.
Policresulen suppository the most according to claim 1, it is characterised in that
Policresulen 90mg
Polyoxyethylene 1-2g
S6 (40) 0.3-1.4g.
Policresulen suppository the most according to claim 1, it is characterised in that polyoxyethylene and s6
(40) weight ratio is 1: 0.5.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410563316.1A CN104323983B (en) | 2014-10-21 | 2014-10-21 | A kind of Policresulen suppository |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410563316.1A CN104323983B (en) | 2014-10-21 | 2014-10-21 | A kind of Policresulen suppository |
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| CN104323983A CN104323983A (en) | 2015-02-04 |
| CN104323983B true CN104323983B (en) | 2016-09-07 |
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Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104688671A (en) * | 2015-02-09 | 2015-06-10 | 孙巧玲 | Compound suppository containing policresulen and preparation technology of compound suppository |
| CN112526032B (en) * | 2020-12-28 | 2022-05-17 | 北京金城泰尔制药有限公司 | Method for detecting policresulen |
| CN115400086B (en) * | 2022-10-08 | 2023-08-22 | 山东新时代药业有限公司 | Policresulen liposome, preparation and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1771989A (en) * | 2005-11-04 | 2006-05-17 | 山东恒瑞医药科技发展有限公司 | Compound prepn for treating women's inflammation |
| CN101919807A (en) * | 2010-07-16 | 2010-12-22 | 钟术光 | Suppository composition |
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2014
- 2014-10-21 CN CN201410563316.1A patent/CN104323983B/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1771989A (en) * | 2005-11-04 | 2006-05-17 | 山东恒瑞医药科技发展有限公司 | Compound prepn for treating women's inflammation |
| CN101919807A (en) * | 2010-07-16 | 2010-12-22 | 钟术光 | Suppository composition |
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