CN1051454C - High-performance non-toxic vagina contraceptive - Google Patents
High-performance non-toxic vagina contraceptive Download PDFInfo
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- CN1051454C CN1051454C CN94112674A CN94112674A CN1051454C CN 1051454 C CN1051454 C CN 1051454C CN 94112674 A CN94112674 A CN 94112674A CN 94112674 A CN94112674 A CN 94112674A CN 1051454 C CN1051454 C CN 1051454C
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- Prior art keywords
- lactone
- gluconic acid
- acid delta
- water
- vagina
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Abstract
The present invention relates to a high-efficiency non-toxic vaginal contraceptive which contains the following components in 100 ml of water: 10 to 40g of glucanic acid delta-lactone, 0.1 to 0.5g of surface active agent, 2.5 to 20g of neutralization agent and 10 to 40g of carrier. The preparation method for the vaginal contraceptive comprises the steps that after the glucanic acid delta-lactone is dissolved in water, the neutralization agents are added, and the pH value is regulated to a range of 4.5 to 5.5; the surface active agents are added and uniformly mixed at a temperature of 60 to 80 DEG C, the carries are melted or dissolved by adding water at a temperature of 60 to 80 DEG C, the two liquids are mixed at a temperature of 60 to 80 DEG C, water is added until the total volume is 100 ml, and then the solution is uniformly mixed so as to obtain the vaginal contraceptive of the present invention. The vaginal contraceptive of the present invention has no toxic or side effect, and the effective rate of sperm killing is 100%.
Description
The present invention relates to a kind of vagina contraceptive.
The contraceptive kind is a lot of at present, its medial vagina spermicide thing also can be divided into following a few class: 1. 2. 3. progestogens such as norethindrone, methylnorethindron, 4. other spermicide such as hydroxyquinoline potassium sulfate, Propranolol etc. of nonionic surfactant spermicide such as menthylphenoxypolyethoxy ethanol, nonoxynolum (NP-9), the poly-ethoxy ethanol (NP-10) of nonyl benzene oxygen, the poly-ethoxy ethanol (TS--88) of terpenyl benzene oxygen of mercurial spermicide such as phenylmercuric acetate, phenylmercuric nitrate.Above medicine or mercurous or contain the noxious substances such as derivant of benzene, though major part can excrete with vaginal secretions and seminal fluid after the medication, but still have on a small quantity by local absorption, anaphylaxis and the burn feeling of vagina penis may appear in user, and progestogens also may cause break-through bleeding and irregular menstruation.
The object of the present invention is to provide a kind of easy to use, vagina contraceptive that has no side effect of containing the gluconic acid delta-lactone.
Purpose of the present invention can realize by following measure: a kind of vagina contraceptive that contains the gluconic acid delta-lactone is characterized in that: contain following component in 100ml water:
Gluconic acid delta-lactone 10～40 grams
Surfactant 0.1～0.5 gram
Nertralizer 2.5～20 grams
Carrier 10～40 gram surfactants are sucrose fatty acid ester or sodium alkyl sulfate.Nertralizer is sodium carbonate or sodium bicarbonate or sodium hydrogen phosphate.Carrier is Oleum Linderae or 35～38 ℃ of semi-synthetic Oleum Cocois or partial hydrogenation Oleum Gossypii semen, gelatin and glycerol.Preferably nertralizer is a sodium hydrogen phosphate.Carrier is gelatin and glycerol.A kind of preparation method that contains the vagina contraceptive of gluconic acid delta-lactone, it is characterized in that: 1. 10～40 gram gluconic acid delta-lactones are added nertralizer after with water dissolution, pH value is transferred between 4.5～5.5, under 60～80 ℃ condition, add the surfactant mixing again, 2. under 60～80 ℃ condition, make the carrier fusion or be dissolved in water, 3. above-mentioned two kinds of liquid are mixed and add water to 100ml stirring and to obtain product of the present invention under 60～80 ℃ condition.
Medicine of the present invention mainly is to adopt gluconic acid delta-lactone, surfactant, nertralizer and carrier formulated.Wherein (Glucono δ-lactone) can make the various enzyme inactivations in the refining to the gluconic acid delta-lactone under the prerequisite without any side effects to health, reduce the pH value of refining, disturb sperm surface to nutraceutical absorbing on every side and can not capacitation, make sperm in the several seconds, promptly lose mobility fully.It is slow that this gluconic acid delta-lactone consumption kills feelings speed very little, but the slow cost increase of the too many dissolution velocity of consumption is general, and it contains 10～40 grams in 100ml water more suitable.Also has surfactant such as the sucrose fatty acid ester S of (or claiming the Suges sucrose ester) in the present invention's prescription
1～S
16Number or sodium alkyl sulfate, their foaming effect can make other component among the present invention be uniformly distributed in intravaginal each position, medicine is mixed with seminal fluid and vaginal secretions rapidly and then be distributed in spermatid film surface fast, the while is also strengthened the resistance of sperm motility.This dosage of surfactant reduces the surface tension weak effect very little, and consumption also is waste too much, and it is more suitable that generally it contains 0.1～0.5 gram in 100ml water.Also has nertralizer in the prescription of the present invention, as sodium carbonate, sodium bicarbonate, sodium hydrogen phosphate and erythromycin.Relatively commonly used is that first three is planted, and they can adjust the pH value of gluconic acid delta-lactone, makes it be lower than acrosome reaction can not take place sperm numerical value promptly 6.5, and preferably PH is between 4.5～5.5.When nertralizer proportion in prescription then can not transfer to faintly acid with it very little, but that consumption then makes it to be alkalescence too much is also improper, can reach above-mentioned effect when generally containing 2.5～20 grams in 100ml water.Best in these nertralizers is sodium hydrogen phosphate, and its decapacitation rises outside the neutralization, can also with the Ca in the seminal fluid
2+Reaction generates water-fast material, makes the Ca in the seminal fluid
2+Reduce rapidly, so sperm Ca for want of
2+Absorption can not bring out acrosome reaction, also just lost and the bonded ability of ovum, its in 100ml water, contain 5～20 the gram more satisfactory.Also have carrier such as cocoa butter, oleum sapii, Oleum Linderae, partial hydrogenation Oleum Gossypii semen, 35～38 ℃ of semi-synthetic Oleum Cocois, gelatin, glycerol and Polyethylene Glycol in the prescription of the present invention.They all can increase the viscosity of seminal fluid and vaginal secretions, reduce their partial pressure of oxygen.Because mobility strengthens behind the capacitation, aerobic metabolism also strengthens, if dissolved oxygen reduces the breathing that has then suppressed sperm in refining and the vaginal secretions, limits its effectively activity.It can also increase the viscosity of cervix uteri liquid simultaneously, is unfavorable for that sperm enters the uterus.Cervix uteri liquid has two kinds of compositions under the normal physiological situation, and a kind of is the macromole micelle that ultimate fibre is arranged, the serosity that another kind is made up of protein, inorganic salt and water.The preovulatory phase and the onset of ovulation women's body inner estrogen preponderate, that macromole micelle fiber is the serosity amount that is arranged in parallel is many and the thin sperm that helps passes through, although but in prescription, utilize viscosity that carrier increases cervix uteri liquid between the micelle fiber that the serosity retrogradation is attached to be arranged in parallel the onset of ovulation, to replenish the room, stop sperm to pass through.Carrier commonly used has gelatin, glycerol, Oleum Linderae, 35～38 ℃ of semi-synthetic Oleum Cocois and partial hydrogenation Oleum Gossypii semen, their shared ratios in prescription are too low, and to kill smart effect undesirable, but consumption dissolving influence diffusion and infiltration slowly in human body too much, generally to contain 10～40 grams in 100ml water more suitable.Preferably adopt the blended carrier of gelatin and glycerol, it respectively is 10～20 grams in 100ml water.
Being prepared as follows of medicine of the present invention: add gluconic acid delta-lactone and water in container, add nertralizer after the dissolving again pH value is transferred between 4.5～5.5, adding the surfactant mixing again under 60～80 ℃ condition is A liquid.Adding its temperature of thermal control under the adding carrier normal pressure in another container makes it fusion or is dissolved in water to be B liquid at 60～80 ℃.A, B two liquid are mixed under 60～80 ℃ condition, and add water to 100ml and stir and to obtain medicine of the present invention.Because different its outward appearances of the ratio of contained various components are also different in the medicine, or are in a liquid state or are solid-state.So can be made into three kinds of convenient dosage forms of using: a semifluid: the translucent drug packaging of flowable yellow in squeezable container, is measured the injection vagina in accordance with regulations and got final product during use; B suppository: adjust each components contents, inject the vaginal suppository mould when hot, then become suppository after the cooling with definite shape and hardness; C sponge plug:, put into vagina during use and get final product with the liquid medicinal liquid of inertia hydrophilic support such as flexible polyurethane foam absorption ormal weight.No matter which kind of dosage form, the each consumption of medicine of the present invention are 4～6 grams.
The present invention has following advantage compared to existing technology:
1, kill smart evidence through pharmacodynamics one is external, medicine of the present invention kills smart effect 100%, and more rapid-action than nonoxynolum, places to wait for that the some time comes into force at once behind the vagina.
2, the used raw material of the present invention is the nutritional labeling of food substantially, and is without any side effects, through the no any untoward reaction of skin mucosa local excitation test, so needn't worry the problem that intravaginal retains after the sexual life.
3, medicine of the present invention has good lubricity and coating, can increase the lubricated of vagina, and the protection vaginal mucosa prevents that sexual intercourse is anti-outward.Particularly middle-aged and elderly people also had good lubricating effect except that contraception is, with the real skin parent's of assurance sexual love joyful sense.
4, cost of drugs of the present invention is low, only is 1/3 of nonoxynolum (NP-9), and it can alleviate the financial burden of user and the spending of national implementation plan fertility.
Example 1
In container, add 20 gram gluconic acid delta-lactones and 6 gram water, add 20 gram sodium bicarbonate after the dissolving again pH value is transferred to 5.5.Adding 0.5 gram sucrose fatty acid ester mixing again under 60～80 ℃ condition is A liquid.Add 40 gram Oleum Linderaies in another container, it is B liquid that heating and control temperature make it fusion at 60～80 ℃.A, B two liquid are mixed and add water to 100ml stirring under 60～80 ℃ condition, can get faint yellow glossiness solid suppository after injecting the cooling of vaginal suppository mould while hot.Each bolt weighs 4～6 grams.
Example 2
Repeat the operation of example 1, wherein gluconic acid delta-lactone 20 grams, sodium alkyl sulfate 0.1 gram, sodium carbonate 2.5 grams, 36 ℃ of Oleum Gossypii semen 40 restrain, and the product that obtains is that PH is 5 faint yellow glossiness solid suppository.
Example 3
Repeat the operation of example 1, wherein gluconic acid delta-lactone 30 grams, sodium alkyl sulfate 0.1 gram, sodium carbonate 10 grams, Oleum Cocois 10 restrain, the product that obtains is that pH value is 4.5 faint yellow semifluid, and the reuse plastic sheeting encapsulated after its flexible polyurethane foam with the band wire rope adsorbed about 5ml.
Example 4
Add 40 gram gluconic acid delta-lactones and 8 gram water to container, add 20 gram sodium hydrogen phosphates after the dissolving again pH value is transferred to 5, adding 0.1 gram sucrose fatty acid ester mixing again under 60～80 ℃ condition is A liquid.Add 10 gram water and 10 gram gelatin to another container, be B liquid adding 10 gram glycerol mixings at 60～80 ℃ again after treating the gelatin off-bottom with heating in water bath control temperature under normal pressure and the stirring condition.A, B two liquid are mixed and add water to 100ml stirring and to obtain yellow semifluid shape product under 60～80 ℃ condition, it is encapsulated in the soft plastic bottle so that use.
Example 5
Repeat the operation of example 4, wherein gluconic acid delta-lactone 25 grams, sodium alkyl sulfate 0.1 gram, sodium bicarbonate 5 restrain, gelatin 10 restrains, glycerol 10 grams, and the faint yellow semi-fluid product pH value that obtains is 4.5.
Example 6
Repeat the operation of example 4, wherein gluconic acid delta-lactone 10 grams, sodium alkyl sulfate 0.5 gram, sodium hydrogen phosphate 5 grams, gelatin 20 grams, glycerol 20 restrain, the product that obtains is injected the vaginal suppository mould while hot, obtain pH value after the cooling and be 4.5 faint yellow glossiness solid suppository.
Claims (7)
1, a kind of vagina contraceptive that contains the gluconic acid delta-lactone is characterized in that: contain following component in 100ml water:
Gluconic acid delta-lactone 10～40 grams
Surfactant 0.1～0.5 gram
Nertralizer 2.5～20 grams
Carrier 10～40 grams
2, the vagina contraceptive that contains the gluconic acid delta-lactone according to claim 1 is characterized in that: surfactant is sucrose fatty acid ester or sodium alkyl sulfate.
3, the vagina contraceptive that contains the gluconic acid delta-lactone according to claim 1 is characterized in that: nertralizer is sodium carbonate or sodium bicarbonate or sodium hydrogen phosphate.
4, the vagina contraceptive that contains the gluconic acid delta-lactone according to claim 1 is characterized in that: carrier is Oleum Linderae or 35～38 ℃ of semi-synthetic Oleum Cocois or partial hydrogenation Oleum Gossypii semen, gelatin and glycerol.
5, according to claim 1 or the 3 described vagina contraceptives that contain the gluconic acid delta-lactone, it is characterized in that: nertralizer is a sodium hydrogen phosphate.
6, according to claim 1 or the 4 described vagina contraceptives that contain the gluconic acid delta-lactone, it is characterized in that: carrier is gelatin and glycerol.
7, a kind of preparation method that contains the vagina contraceptive of gluconic acid delta-lactone, it is characterized in that: 1. 10～40 gram gluconic acid delta-lactones are added nertralizer after with water dissolution, pH value is transferred between 4.5～5.5, under 60～80 ℃ condition, add the surfactant mixing again, 2. under 60～80 ℃ condition, make the carrier fusion or be dissolved in water, 3. above-mentioned two kinds of liquid are mixed and add water to 100ml stirring and to obtain product of the present invention under 60～80 ℃ condition.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN94112674A CN1051454C (en) | 1994-12-13 | 1994-12-13 | High-performance non-toxic vagina contraceptive |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN94112674A CN1051454C (en) | 1994-12-13 | 1994-12-13 | High-performance non-toxic vagina contraceptive |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1124622A CN1124622A (en) | 1996-06-19 |
| CN1051454C true CN1051454C (en) | 2000-04-19 |
Family
ID=5036346
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN94112674A Expired - Fee Related CN1051454C (en) | 1994-12-13 | 1994-12-13 | High-performance non-toxic vagina contraceptive |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1051454C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3439633T3 (en) * | 2016-04-06 | 2022-01-10 | Gedea Biotech Ab | Glucono delta-lactone for treatment of vaginal fungal infections |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4105783A (en) * | 1975-07-23 | 1978-08-08 | Yu Ruey J | Therapeutic treatment of dry skin |
| US4197316A (en) * | 1975-07-23 | 1980-04-08 | Scott Eugene J Van | Treatment of dry skin |
-
1994
- 1994-12-13 CN CN94112674A patent/CN1051454C/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4105783A (en) * | 1975-07-23 | 1978-08-08 | Yu Ruey J | Therapeutic treatment of dry skin |
| US4197316A (en) * | 1975-07-23 | 1980-04-08 | Scott Eugene J Van | Treatment of dry skin |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1124622A (en) | 1996-06-19 |
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