CN101422449A - Nonoxinol pellicles film and preparation method and use thereof in preparing contraceptive medicine - Google Patents
Nonoxinol pellicles film and preparation method and use thereof in preparing contraceptive medicine Download PDFInfo
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- CN101422449A CN101422449A CNA2008102431980A CN200810243198A CN101422449A CN 101422449 A CN101422449 A CN 101422449A CN A2008102431980 A CNA2008102431980 A CN A2008102431980A CN 200810243198 A CN200810243198 A CN 200810243198A CN 101422449 A CN101422449 A CN 101422449A
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Abstract
The invention discloses a nonoxynol nonylphenoxy-polyethoxyethanol film agent used for contraception, which is prepared by nonoxynol nonylphenoxy-polyethoxyethanol, film-forming material, a plasticizer, distilled water, an antiseptic and essence according to certain weight ratio; the preparation method is as follows: (1) proper amount of distilled water is added into chitosan hydrochloride, stirred evenly, rested and fully expanded; (2) the plasticizer and the essence are added into the nonoxynol nonylphenoxy-polyethoxyethanol and evenly stirred; (3) the film-forming material in step (1) is heated in water bath and proper amount of the plasticizer and the antiseptic are added and evenly stirred, then added into the main medicament dissolved in the step (2), and then arranged on the water bath, heated and stirred fully; and (4) the medicine slurry is fully paved on a glass board by a board scraping method, blown and dried, thus instantly forming the film. The nonoxynol nonylphenoxy-polyethoxyethanol film agent prepared by the invention takes the chitosan hydrochloride as the film-forming material; the chitosan hydrochloride has excellent biocompatibility and biological degradability; the decomposed product is innoxious, is small in thrill, convenient in use, high in safety and simple in preparation technique; and a pharmacological test result shows that the contraception effect is remarkable.
Description
Technical field
The invention belongs to the chemicals field, be specifically related to a kind of Nonoxinol pellicles film that is used to practise contraception and preparation method thereof.
Background technology
Family planning is the fundamental state policy of China, and contraception relates to each family.Reproduction is the process of a complexity, comprises a plurality of links such as formation, maturation, discharging, fertilization, implantation and fetal development of sperm and ovum, and blocking-up wherein any one link all can reach the contraception or the purpose of termination of pregnancy.Disturb the endocrine effect because oral contraceptive often has, cause nausea, vomit, even the irregular side reaction such as bleed of vagina, thereby limited the scope of application.And external applied contraceptive does not disturb endocrine function, has reversibility, so the research work of external applied contraceptive comes into one's own.External applied contraceptive is fit to each age group, the women of each level, and side reaction is few relatively.Studies show that according to data at home and abroad report and some, the killing sperm in vagina agent nonoxynolum that uses both at home and abroad at present, long-term clinical proving effect reliable contraception medicine be in the present contraceptive device a kind of safe, effectively reach easy to use, comparatively ideal contraceptive device.Nonoxynolum is a nonionic surfactant, 0.2% nonoxynolum solution can kill sperm rapidly, this medicine film is put into the vagina deep can dissolve the smart extremely effect of performance fast, interact with the spermatid lipoprotein membrane in vagina dissolving back, change the permeability of spermatid, kill sperm or sperm is lost vigor, thereby make sperm can not advance people's cervix uteri mouth, can't fertilize an egg reaches contraceptive effect.
Summary of the invention
The object of the present invention is to provide a kind of Nonoxinol pellicles film and preparation method and the application in the preparation contraceptive thereof.The foregoing invention purpose is to realize by following technical scheme.
A kind of Nonoxinol pellicles film that is used to practise contraception is characterized in that it is made by following materials of weight proportions: nonoxynolum, filmogen, plasticizer, distilled water, antiseptic, essence are by weight being 1:2～3:1～2:40～60:0.0002～0.02:0.01～0.2.
Above-mentioned filmogen is a chitosan hydrochlorate.
Above-mentioned plasticizer is organic carboxyl acid esters or multicomponent alcoholics compound.
Above-mentioned antiseptic is an ethyl hydroxybenzoate, a kind of in benzyl alcohol or the benzoic acid.
Above-mentioned essence is jasmine Oleum sesami, a kind of in rose essence or the vanillin.
Above-mentioned multicomponent alcoholics compound is a kind of in glycerol, propylene glycol or the Macrogol 600.
Above-mentioned organic carboxyl acid esters is a triacetyl glycerine, a kind of in phthalic acid ester or the citron acid esters.
The preparation method of above-mentioned Nonoxinol pellicles film, it is characterized in that comprising following four steps: the first step: it is an amount of to get the chitosan hydrochlorate adding distil water, and abundant swelling is placed in the back that stirs, and is standby; Second step: with plasticizer, essence joins in the nonoxynolum, and it is standby to stir; The 3rd goes on foot: the filmogen of the first step is put in the water-bath heated, add an amount of plasticizer and antiseptic and stir, and standby; The 4th step: the 3rd film material that obtain of step is added in the principal agent in second step, put in the water-bath heating and stir, above-mentioned medicine slurry evenly is laid on the glass plate dry back film forming with the scraper plate method.
In the 4th step of above-mentioned preparation method with 75 ℃ of forced air drying 5-10min.
Above-mentioned Nonoxinol pellicles film is used for the application of female genital contraceptive in preparation.
The medicine film that relates among the present invention is characterised in that with the chitosan hydrochlorate to be filmogen, and chitosan (Chitosan) also claims chitosan; Chitosan; Soluble chitin; Chitosan; Chitan; Poly-glucosamine, chemistry 2-amino-beta--1 by name, the 4-glucosan, molecular formula is (C
6H
11O
4N)
nIt is a kind of natural cationic polysaccharide that chitin obtains through deacetylation; extensively be present in the cell wall of the duricrust of insecticide, Crustacean and mushroom, have degradability, good film property, excellent biological compatibility and certain excellent properties such as antibiotic and antitumor.Be widely used in industries such as medicine, food, chemical industry, environmental protection, have the good reputation of omnipotent polysaccharide.Pharmaceutically, utilize its film property, absorbability and bactericidal properties, be used to prepare artificial skin, artificial blood vessel, operation suture thread, be used as hemorrhage and Wound-healing agent, antitumor agent, immunopotentiating agent and anti-cholesterol agent, can be used as the adsorpting detoxication agent of artificial kidney again, take off the endotoxin ultrafilter membrane.As pharmaceutic adjuvant, its viscosity, compressibility, flowability and disintegrative are all very outstanding, also can be widely used on slow releasing agent and the intra-gastric floating tablet.
Nonoxinol pellicles film of the present invention be with chitosan as filmogen, have a lot of advantages.Chitosan can be dissolved in the weak acid, and chitosan hydrochlorate can be soluble in water, is filmogen very easily, and this film is edible film, safety non-toxic, so the safety coefficient of external is also than higher.Because the existence of polar group, chitosan has very high affinity and retentiveness to water, and performance of keeping humidity is good.Chitosan also has excellent biological compatibility and biological degradability, helps medicine film absorbing in vaginal mucosa, and catabolite generally has no side effect to human body, do not put aside in vivo, and non-immunogenicity, nonirritant is fit to life-time service; Show that through the animal pharmacological test result membrane contraceptive effect of the present invention is remarkable.
The specific embodiment
Embodiment 1
(1) take by weighing chitosan hydrochlorate 1g, the 25ml distilled water is slowly added in the chitosan hydrochlorate at normal temperatures, the limit edged stirs and prevents its caking, places 30min until the back that stirs and makes its abundant swelling, and is standby;
(2) with the 0.4g Macrogol 600,0.01g jasmine Oleum sesami joins in the 0.5g nonoxynolum and stirs;
(3) chitosan hydrochlorate of step (1) is put into 90 ℃ of water-bath heated and stirred, the ethyl hydroxybenzoate that adds 0.1g Macrogol 600 and 0.005g again continues to stir, and is standby;
(4) the film material that step (3) is made is slowly poured in the nonoxynolum solution of step (2), puts in 80 ℃ the water-bath heating and stirs, and above-mentioned medicine serosity evenly is poured on the glass plate of four smooth 10cm*20cm of cleaning manual system film 800cm
2, film thickness monitoring is put in 70 ℃ the constant temperature blast drier and is taken out behind the 10min about 43um, film is taken off getting final product.
Embodiment 2
(1) take by weighing chitosan hydrochlorate 2g, nonoxynolum 1g is standby; The 45ml distilled water is slowly added in the chitosan hydrochlorate at normal temperatures, and the limit edged stirs and prevents its caking, places 30min until the back that stirs and makes its abundant swelling, and is standby;
(2) with the 1g propylene glycol, the 0.05g rose essence joins in the 1g nonoxynolum and stirs;
(3) chitosan hydrochlorate of step (1) is put into 75 ℃ of water-bath heated and stirred, the benzoic acid that adds 0.5g propylene glycol and 0.005g again continues to stir, and is standby;
(4) the film material that step (3) is made is slowly poured in the nonoxynolum solution of step (2), puts in 85 ℃ the water-bath heating and stirs, and above-mentioned medicine serosity evenly is poured on the glass plate of four smooth 10cm*20cm of cleaning manual system film 800cm
2, film thickness monitoring is put in 70 ℃ the constant temperature blast drier and is taken out behind the 10min about 50um, film is taken off getting final product.
Embodiment 3
(1) take by weighing chitosan hydrochlorate 1g, nonoxynolum 0.5g is standby; The 25ml distilled water is slowly added in the chitosan hydrochlorate at normal temperatures, and the limit edged stirs and prevents its caking, places 30min until the back that stirs and makes its abundant swelling, and is standby;
(2) with the 0.6g triacetyl glycerine, the 0.1g vanillin joins in the 0.5g nonoxynolum and stirs;
(3) chitosan hydrochlorate of step (1) is put into 85 ℃ of water-bath heated and stirred, the benzyl alcohol that adds 0.2g triacetyl glycerine and 0.005g again continues to stir, and is standby;
(4) the film material that step (3) is made is slowly poured in the nonoxynolum solution of step (2), puts in 90 ℃ the water-bath heating and stirs, and above-mentioned medicine serosity evenly is poured on the glass plate of four smooth 10cm*20cm of cleaning manual system film 800cm
2, film thickness monitoring is put in 75 ℃ the constant temperature blast drier and is taken out behind the 10min about 45um, film is taken off getting final product.
Embodiment 4
(1) take by weighing chitosan hydrochlorate 1g, nonoxynolum 0.5g is standby; The 25ml distilled water is slowly added in the chitosan hydrochlorate at normal temperatures, and the limit edged stirs and prevents its caking, places 30min until the back that stirs and makes its abundant swelling, and is standby;
(2) with the 0.5g phthalic acid ester, the 0.2g vanillin joins in the 0.5g nonoxynolum and stirs;
(3) chitosan hydrochlorate of step (1) is put into 85 ℃ of water-bath heated and stirred, the benzoic acid and the 0.3g phthalic acid ester that add 0.005g again continue to stir, and be standby;
(4) the film material that step (3) is made is slowly poured in the nonoxynolum solution of step (2), puts in 85 ℃ the water-bath heating and stirs, and above-mentioned medicine serosity evenly is poured on the glass plate of four smooth 10cm*20cm of cleaning manual system film 800cm
2, film thickness monitoring is put in 75 ℃ the constant temperature blast drier and is taken out behind the 10min about 48um, film is taken off getting final product.
Embodiment 5
(1) take by weighing chitosan hydrochlorate 1g, nonoxynolum 0.5g is standby; The 20ml distilled water is slowly added in the chitosan hydrochlorate at normal temperatures, and the limit edged stirs and prevents its caking, and the back that stirs is standby;
(2) with 0.5g citron acid esters, the 0.1g rose essence joins in the 0.5g nonoxynolum and stirs;
(3) chitosan hydrochlorate of step (1) is put into 85 ℃ of water-bath heated and stirred, the ethyl hydroxybenzoate that adds 0.2g citron acid esters and 0.005g again stirs, and is standby;
(4) the film material that step (3) is made is slowly poured in the nonoxynolum solution of step (2), puts in 85 ℃ the water-bath heating and stirs, and above-mentioned medicine serosity evenly is poured on the glass plate of four smooth 10cm*20cm of cleaning manual system film 800cm
2, film thickness monitoring is put in 75 ℃ the constant temperature blast drier and is taken out behind the 10min about 45um, film is taken off getting final product.
Embodiment 6
(1) take by weighing chitosan hydrochlorate 1g, nonoxynolum 0.5g is standby; The 20ml distilled water is slowly added in the chitosan hydrochlorate at normal temperatures, and the limit edged stirs and prevents its caking, and the back that stirs is standby;
(2) with the 0.4g glycerol, 0.1g jasmine Oleum sesami joins in the 0.5g nonoxynolum and stirs;
(3) chitosan hydrochlorate of step (1) is put into 85 ℃ of water-bath heated and stirred, the ethyl hydroxybenzoate that adds 0.2g glycerol and 0.005g again stirs, and is standby;
(4) the film material that step (3) is made is slowly poured in the nonoxynolum solution of step (2), puts in 85 ℃ the water-bath heating and stirs, and above-mentioned medicine serosity evenly is poured on the glass plate of four smooth 10cm*20cm of cleaning manual system film 800cm
2, film thickness monitoring is put in 75 ℃ the constant temperature blast drier and is taken out behind the 10min about 45um, film is taken off getting final product.
Embodiment 7 pharmacology tests
1, laboratory animal: health adult female white big ear rabbit and male large ear rabbit, body weight 2.5-3.0kg derive from Nanjing University of Traditional Chinese Medicine zoopery center
2, experiment medicine: preparation of the present invention (Nanjing University of Traditional Chinese Medicine pharmacological experiment chamber provides)
3, experimental technique: conformed for 1 week after 20 of does of experiment are bought, be divided into 4 groups at random by body weight, 5 every group, promptly blank group, nonoxynol-9 filler 1.5,3.0,6.0mg group.Doe administration copulation precontract 16h, the 100 μ g estrus inductions of intramuscular injection diethylstilbestrol.Each group kneads film and slowly pushes the rabbit vagina depths, and clinostatism 10min in case membrane dissolving back drug wastage, carries out double cross with the male rabbit of tool fertility then and joins.All doe vagina scraping blades have a large amount of propulsion sperm persons in field of microscope, be considered as the copulation success.The meticulous breeding observing of rabbit 20 days is put to death rabbit in post-coitum the 21st day and to be dissected with the air tap inserting method, write down ovulation point, the uterus implantation point of its ovary, live tire and stillborn fetus number, corpus luteum number, calculates and respectively organizes contraceptive prevalence rate.
4, experimental result:
The Nonoxinol pellicles film various dose is to the antifertility action of doe
Nonoxinol pellicles film various dose group doe ovary ovulation point and blank group relatively do not have group difference (P〉0.05), show that respectively to organize doe ovary ovulation function normal; Nonoxinol pellicles film various dose group is compared with blank group uterus implantation point, and highly significant meaning (P＜0.001) is arranged; The tire of living is counted the various dose group and has been compared highly significant meaning (P＜0.001) with the blank group.
The Nonoxinol pellicles film various dose is to the influence of doe contraceptive effect
Contraceptive prevalence rate is compared with the blank group with the unpregnancy number, the no significance meaning of 1.5mg group (P〉0.05), the 3.0mg group has significance meaning (P＜0.05), and the 6.0mg group has highly significant meaning (P＜0.001).Rabbit antifertility experimental result shows that the contraceptive prevalence rate of high, medium and low dosage experiments medicine group is respectively 100%, 80% and 60%.
Conclusion: prove that by above effect experiment preparation of the present invention has certain contraceptive effect to rabbit.
Claims (10)
1, a kind of Nonoxinol pellicles film that is used for the contraception of female genital is characterized in that it is made by following materials of weight proportions:
Nonoxynolum, filmogen, plasticizer, distilled water, antiseptic, essence are 1:2～3:1～2:40～60:0.0002～0.02:0.01～0.2 by weight.
2, membrane according to claim 1 is characterized in that described filmogen is a chitosan hydrochlorate.
3, membrane according to claim 1 is characterized in that described plasticizer is organic carboxyl acid esters or multicomponent alcoholics compound.
4, membrane according to claim 1 is characterized in that described antiseptic is a kind of in ethyl hydroxybenzoate, benzyl alcohol or the benzoic acid.
5, membrane according to claim 1 is characterized in that described essence is a kind of in jasmine Oleum sesami, rose essence or the vanillin.
6, membrane according to claim 3 is characterized in that described multicomponent alcoholics compound is a kind of in glycerol, propylene glycol or the Macrogol 600.
7, membrane according to claim 3 is characterized in that described organic carboxyl acid esters is a triacetyl glycerine, phthalic acid ester, a kind of in the citron acid esters.
8, a kind of method for preparing the described Nonoxinol pellicles film of claim 1 is characterized in that preparation process is as follows:
The first step: it is an amount of to get the filmogen adding distil water, and the back that stirs is standby;
Second step: with plasticizer, essence joins in the nonoxynolum, and it is standby to stir;
The 3rd goes on foot: first step filmogen is put in the water-bath heated, add an amount of plasticizer and antiseptic and stir, and standby;
The 4th step: the 3rd film material that obtain of step is added in the principal agent in second step, put in the water-bath heating and stir, above-mentioned medicine slurry evenly is laid on the glass plate dry back film forming with the scraper plate method.
9, preparation method according to claim 7 is characterized in that in the 4th step with 75 ℃ of forced air drying 10-15min.
10, Nonoxinol pellicles film as claimed in claim 1 is used for the application of female genital contraceptive in preparation.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008102431980A CN101422449A (en) | 2008-12-10 | 2008-12-10 | Nonoxinol pellicles film and preparation method and use thereof in preparing contraceptive medicine |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008102431980A CN101422449A (en) | 2008-12-10 | 2008-12-10 | Nonoxinol pellicles film and preparation method and use thereof in preparing contraceptive medicine |
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| Publication Number | Publication Date |
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| CN101422449A true CN101422449A (en) | 2009-05-06 |
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| CNA2008102431980A Pending CN101422449A (en) | 2008-12-10 | 2008-12-10 | Nonoxinol pellicles film and preparation method and use thereof in preparing contraceptive medicine |
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Owner name: NANJING TRADITIONAL CHINESE MEDICINE UNIV. Free format text: FORMER OWNER: LI HAITAO Effective date: 20090626 |
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Effective date of registration: 20090626 Address after: 282, Hanzhoung Road, Jiangsu, Nanjing Province, China: 210029 Applicant after: Nanjing University of Chinese Medicine Address before: Room 03, building 904, man Cheng District, Fenghuang street, 55, Jiangsu, Nanjing Province, China: 210029 Applicant before: Li Haitao |
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Open date: 20090506 |