CA1214725A - Contraceptive vaginal tablets and process for preparing them - Google Patents
Contraceptive vaginal tablets and process for preparing themInfo
- Publication number
- CA1214725A CA1214725A CA000441915A CA441915A CA1214725A CA 1214725 A CA1214725 A CA 1214725A CA 000441915 A CA000441915 A CA 000441915A CA 441915 A CA441915 A CA 441915A CA 1214725 A CA1214725 A CA 1214725A
- Authority
- CA
- Canada
- Prior art keywords
- weight
- parts
- tablets
- vitamin
- sodium bisulfite
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
ABSTRACT
The invention relates to contraceptive vaginal tablets and to a process for preparing them. The tablets of the invention have the following composition: 0.2 to 3 parts by weight of boric acid, 10 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose and 50 to 65 parts by weight of microcrystalline cellulose. The vaginal tablets contain preferably 5 to 10 mg of vitamin K3-sodium bisulfite adduct and have a total weight of 500 mg. The tablets are prepared preferably in such a way that the boric acid, the tartaric acid and the vitamin K3-sodium bisulfite adduct, as well as the polyvinyl pyrrolidone, the magnesium stearate, the carboxymethyl cellulose, the lactose and the microcrystalline cellulose are homogenized separately to powder mixtures and thereafter the powder mixtures are mixed and pressed to form tablets. The tablets should be wetted and inserted into the back-vaginal fornix 10 minutes before the coitus.
The invention relates to contraceptive vaginal tablets and to a process for preparing them. The tablets of the invention have the following composition: 0.2 to 3 parts by weight of boric acid, 10 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose and 50 to 65 parts by weight of microcrystalline cellulose. The vaginal tablets contain preferably 5 to 10 mg of vitamin K3-sodium bisulfite adduct and have a total weight of 500 mg. The tablets are prepared preferably in such a way that the boric acid, the tartaric acid and the vitamin K3-sodium bisulfite adduct, as well as the polyvinyl pyrrolidone, the magnesium stearate, the carboxymethyl cellulose, the lactose and the microcrystalline cellulose are homogenized separately to powder mixtures and thereafter the powder mixtures are mixed and pressed to form tablets. The tablets should be wetted and inserted into the back-vaginal fornix 10 minutes before the coitus.
Description
The invention relates to contraceptive vaginal table-ts which are free from hormones, and to a process for preparing them.
Apart from steriliza~ion, several methods are known for preventing undesirable pregnancy. These include use of condoms, intrauterine instruments, vaginal pessaries (mechanical instruments), hormonal preparations which prevent the occurrence of the pregnancy and local spermicidal preparations which are free from hormones.
All the known methods have, however, disadvantages which prevent general application. It is known that not every conceptive age-group may use preparations containing hormones. Certain persons, who could take these preparations in view of their age, are prevented from employing them owing to the side effects. From among the mechanical instruments the condom and the vaginal pessary cause in certain cases uncomfortable feeling or require preparation destroying the illusions. The intrauterine instruments are free from these disadvantages, but not all persons may wear them, and members of even the youngest age-group may not use them. A further disadvantage of these instruments is that they may be ~nserted only by the physician. With preparations which are free from hormones there is no contraindication relating to age-group. These are rarely applied, however, per se since they are not reliable enough.
The efficiency of the known contraceptive instruments and methods is characterized by the so-called Pearl-index. This is a number which shows how many from among 100 conceptive women using the instrument or method in question, will become pregnant during a year. The Pearl-index of the contraceptive instruments and methods is stated in the following Table.
~Z~ 5 Table vaginal irrigation 29.3-40.8 coitus interruptus 12-38 Ogino-Knaus rule 12-34.5 foam tablet 11.9-42.8 vaginal pellet 7.7-42.3 diaphragm 6.1-33.6 jelly 6.4-41 vaginal pessary 6.0-29 condom 6-28 intrauterine instrument 0.9-8 hormonal preparation 0-1.7 From the data of this Table it can be seen that only the hormonal preparations possess the safety desired. The efficiency of the preparations containing only chemical substances falls far behind that of the hormonal preparations.
An aim of the present invention is to find a vaginal tablet which is free from hormones, which possesses the same efficiency as the hormonal preparations and does not show the disadvantages thereof, so that the tablet may be used without any limitation of the age or the physical condition.
Vitamin K3 and the adduct thereof with sodium bisulfite are widely used in the therapy e.g. for treating icterus occulsion, pre- and post-operative treatment in cholemia, biliary fistula, ulcerative colitis, dysentery, steatorrhea, sprue, celiac disease, hemophilia of the newborn, jaundice, salicylism, purpura, thormbophenia, serum sickness, urticaria, haemoptoe. The contraceptive effect of these compounds has not been previously disclosed.
47:2~
The therapeutic use ot boric acid and tartaric acid is also known. The boric acid is used for rinsing cavities owing -to its weak dlsinfectant effect, the tartaric acid is applied for regulating the pH of the preparations due to its weak acidic reaction.
It was surprisingly found that a preparation, which corresponds to the above requirements, may be obtained when 0.2 to 15 parts by weight of boric acid, 10 to 100 parts by weigh-t of tartaric acid, 1 to 10 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 5 parts by weight of polyvinyl pyrrolidone, 2 to 15 parts by weight of magnesium stearate, 8 to 50 parts by weight of carboxymethyl cellulose~ 8 to 12 parts by weight of lactose, and 50 to 320 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
In a preferred embodiment 0.2 to 3.0 parts by weight of boric acid, 10.0 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose and 50 to 65 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
The tablets contain preferably 5 mg of vitamin K3-sodium bisulfite adduct per tablet. A suitable tablet has a total weight of about 500 mg.
The vaginal tablets of the invention should be wetted before use and thereaEter inserted into the back-vaginal fornix.
Here the tablets disintegrate quickly owing to the moisture and . .
, ~L2~2~
form a suspension. This suspension covers the cervix and paralyzes the spermiums being thereon. The rest oE the preparation may be removed by irrigation. The use oE -the tablets does not cause discomfort; the tablets disintegrated in the vagina do not have any noxious side effect.
Further details of the invention are shown in the following Examples without any limitation thereto.
Example 1 Homogeneous powder mixture is prepared from 2.0 g of powdered boric acid, 100.0 g of powdered tartaric acid and 100.0 g of microcrystalline L4~ S
cellulose. Separately 10.0 g of vitamin K3-sodium bisulfite adduct, lO.0 g of polyvinyl pyrrolidone ~Polyplasdon XL*~, 30.0 g of magnesium stearate and 100.0 g of carboxymethyl cellulose are homogenized. The two powder mixtures are mixed thereafter 648.0 g of microcrystalline cellulose are admixed. lO00.0 g of the powder mixture are obtained~ from which 2000 tablets each weighing 500 mg and having a diameter of 12 mm are pressed without edges.
Some proper~ies of the tablets so obtained are summarized as follows:
abrasion hardness (ERWEKA-TAP):
after 5 minutes after 10 minutes 1.46% 3.02%
1.29% 2.86%
compression strength ~ERWEKA): 14.3 N
average height of the tablets: 4.52 mm disintegration time ~flask method according to PA.Mg.VI):
9 to 10 minutes.
Example 2 Tablets are prepared according to the process described in Example l with the ~ollowing composition:
boric acid 5.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct5.0 mg polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose 50.0 mg lactose 50.0 mg microcrystalline cellulose 320.0 mg * Trade Mark 500.0 mg Example 3 Tablets are prepared according to the process described in Example 1 with the following composition:
boric acid 15.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct 5.0 mg polyvinyl pyrrolidone5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose50.0 mg lactose 50.0 mg microcrystalline cellulose 310.0 mg 500.0 mg Example ~
Tablets are prepared according to the process descri.bed in Example 1 with the following composition:
boric acid 1.0 mg tartaric acid 100.0 mg vitamin K3-sodium bisul~ite adduc~ 5.0 mg polyvinyl pyrrolidone5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose50.0 mg lactose 50.0 mg microcrystalline cellulose 274.0 mg 500.0 mg 72~
Example 5 Tablets are prepared with the following composition:
boric acid 1.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose 50.0 mg lactose 50.0 mg lV microcrystalline cellulose319.0 mg 500.0 mg Example 6 Tablets are prepared with the following composition:
boric acid 5.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg polyvinyl pyrrolidone 5.0 mg magnesium s~earate 15.0 mg carboxymethyl cellulose 50.0 mg lac~ose 50.0 mg microcrystalline cellulose315.0 mg_ 500.0 mg Example 7 Tablets are prepared with the following composition:
boric acid 15.0 mg tartaric acid '0.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg ~2~9~72~i polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose50.0 mg lactose 50.0 mg microcrystalline cellulose305.0 mg 500.0 mg Example 8 Tablets are prepared with the following composition:
boric acid 1.0 mg tartaric acid 100.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg lactose 50.0 mg carboxymethyl cellulose50.0 mg microcrystalline cellulose2~.0 mg 500.0 mg The following in vitro and in vivo tests were performed with the tablets of the invention.
In vitro test Sperm obtained from 32 normo zoospermia persons was examined.
From the sperm 1 ml quantities containing 10 to lO0 millions of spermatozoa were mixed with 1 ml suspension obtained from 1 tablet at +38C on a watch-glass. The motion of the spermatozoa was observed. Partial immobilisation began l minute after the mixing and became complete in 5 to lO minutes depending on the vitality of the spermatozoa. The immobilized spermatozoa became eosin binders, which indicates the cell death. This process is irreversible. The spermatozoa could not be revived either by changing the pH or by adding fresh serum or by other methods.
In vivo model test The following test was carried out with women in their ovulation period. Tablets prepared according to the invention were wetted by water and thereafter inserted into the back-vaginal fornix. After 5 minutes the vagina was exposed and each 2 ml of a sperm having a concentration of 160 to 240 millions spermatozoa/ml were injected onto the women's cervix. The exposing instrument was removed and af~er 5 and 10 minutes repeated exposures were performed thereafter the content of the vagina was examined.
According to the microscopic examinations the immobilization is 50% after 5 minutes, while 100% after 10 minutes.
In vivo application test The tablets were used by women who were proved to be conceptive and till the time of the examination protected themselves only by the Ogino-Knaus rule. Among these women pregnancy occurred only in two cases during a one year period. In view of this fact the tablets of the inventions have the same efficiency as the intrauterine instruments ~the Pearl-index was 2).
The women examined were subjected to gynaecological examination every two or three months so that any side effects on the vagina or damaging effect on the mucous membrane would be determined. No such cases were found.
In view of the above described it can be stated that the vaginal tablets of the invention are suitable for the modern contraception in every respect.
Apart from steriliza~ion, several methods are known for preventing undesirable pregnancy. These include use of condoms, intrauterine instruments, vaginal pessaries (mechanical instruments), hormonal preparations which prevent the occurrence of the pregnancy and local spermicidal preparations which are free from hormones.
All the known methods have, however, disadvantages which prevent general application. It is known that not every conceptive age-group may use preparations containing hormones. Certain persons, who could take these preparations in view of their age, are prevented from employing them owing to the side effects. From among the mechanical instruments the condom and the vaginal pessary cause in certain cases uncomfortable feeling or require preparation destroying the illusions. The intrauterine instruments are free from these disadvantages, but not all persons may wear them, and members of even the youngest age-group may not use them. A further disadvantage of these instruments is that they may be ~nserted only by the physician. With preparations which are free from hormones there is no contraindication relating to age-group. These are rarely applied, however, per se since they are not reliable enough.
The efficiency of the known contraceptive instruments and methods is characterized by the so-called Pearl-index. This is a number which shows how many from among 100 conceptive women using the instrument or method in question, will become pregnant during a year. The Pearl-index of the contraceptive instruments and methods is stated in the following Table.
~Z~ 5 Table vaginal irrigation 29.3-40.8 coitus interruptus 12-38 Ogino-Knaus rule 12-34.5 foam tablet 11.9-42.8 vaginal pellet 7.7-42.3 diaphragm 6.1-33.6 jelly 6.4-41 vaginal pessary 6.0-29 condom 6-28 intrauterine instrument 0.9-8 hormonal preparation 0-1.7 From the data of this Table it can be seen that only the hormonal preparations possess the safety desired. The efficiency of the preparations containing only chemical substances falls far behind that of the hormonal preparations.
An aim of the present invention is to find a vaginal tablet which is free from hormones, which possesses the same efficiency as the hormonal preparations and does not show the disadvantages thereof, so that the tablet may be used without any limitation of the age or the physical condition.
Vitamin K3 and the adduct thereof with sodium bisulfite are widely used in the therapy e.g. for treating icterus occulsion, pre- and post-operative treatment in cholemia, biliary fistula, ulcerative colitis, dysentery, steatorrhea, sprue, celiac disease, hemophilia of the newborn, jaundice, salicylism, purpura, thormbophenia, serum sickness, urticaria, haemoptoe. The contraceptive effect of these compounds has not been previously disclosed.
47:2~
The therapeutic use ot boric acid and tartaric acid is also known. The boric acid is used for rinsing cavities owing -to its weak dlsinfectant effect, the tartaric acid is applied for regulating the pH of the preparations due to its weak acidic reaction.
It was surprisingly found that a preparation, which corresponds to the above requirements, may be obtained when 0.2 to 15 parts by weight of boric acid, 10 to 100 parts by weigh-t of tartaric acid, 1 to 10 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 5 parts by weight of polyvinyl pyrrolidone, 2 to 15 parts by weight of magnesium stearate, 8 to 50 parts by weight of carboxymethyl cellulose~ 8 to 12 parts by weight of lactose, and 50 to 320 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
In a preferred embodiment 0.2 to 3.0 parts by weight of boric acid, 10.0 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose and 50 to 65 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
The tablets contain preferably 5 mg of vitamin K3-sodium bisulfite adduct per tablet. A suitable tablet has a total weight of about 500 mg.
The vaginal tablets of the invention should be wetted before use and thereaEter inserted into the back-vaginal fornix.
Here the tablets disintegrate quickly owing to the moisture and . .
, ~L2~2~
form a suspension. This suspension covers the cervix and paralyzes the spermiums being thereon. The rest oE the preparation may be removed by irrigation. The use oE -the tablets does not cause discomfort; the tablets disintegrated in the vagina do not have any noxious side effect.
Further details of the invention are shown in the following Examples without any limitation thereto.
Example 1 Homogeneous powder mixture is prepared from 2.0 g of powdered boric acid, 100.0 g of powdered tartaric acid and 100.0 g of microcrystalline L4~ S
cellulose. Separately 10.0 g of vitamin K3-sodium bisulfite adduct, lO.0 g of polyvinyl pyrrolidone ~Polyplasdon XL*~, 30.0 g of magnesium stearate and 100.0 g of carboxymethyl cellulose are homogenized. The two powder mixtures are mixed thereafter 648.0 g of microcrystalline cellulose are admixed. lO00.0 g of the powder mixture are obtained~ from which 2000 tablets each weighing 500 mg and having a diameter of 12 mm are pressed without edges.
Some proper~ies of the tablets so obtained are summarized as follows:
abrasion hardness (ERWEKA-TAP):
after 5 minutes after 10 minutes 1.46% 3.02%
1.29% 2.86%
compression strength ~ERWEKA): 14.3 N
average height of the tablets: 4.52 mm disintegration time ~flask method according to PA.Mg.VI):
9 to 10 minutes.
Example 2 Tablets are prepared according to the process described in Example l with the ~ollowing composition:
boric acid 5.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct5.0 mg polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose 50.0 mg lactose 50.0 mg microcrystalline cellulose 320.0 mg * Trade Mark 500.0 mg Example 3 Tablets are prepared according to the process described in Example 1 with the following composition:
boric acid 15.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct 5.0 mg polyvinyl pyrrolidone5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose50.0 mg lactose 50.0 mg microcrystalline cellulose 310.0 mg 500.0 mg Example ~
Tablets are prepared according to the process descri.bed in Example 1 with the following composition:
boric acid 1.0 mg tartaric acid 100.0 mg vitamin K3-sodium bisul~ite adduc~ 5.0 mg polyvinyl pyrrolidone5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose50.0 mg lactose 50.0 mg microcrystalline cellulose 274.0 mg 500.0 mg 72~
Example 5 Tablets are prepared with the following composition:
boric acid 1.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose 50.0 mg lactose 50.0 mg lV microcrystalline cellulose319.0 mg 500.0 mg Example 6 Tablets are prepared with the following composition:
boric acid 5.0 mg tartaric acid 50.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg polyvinyl pyrrolidone 5.0 mg magnesium s~earate 15.0 mg carboxymethyl cellulose 50.0 mg lac~ose 50.0 mg microcrystalline cellulose315.0 mg_ 500.0 mg Example 7 Tablets are prepared with the following composition:
boric acid 15.0 mg tartaric acid '0.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg ~2~9~72~i polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg carboxymethyl cellulose50.0 mg lactose 50.0 mg microcrystalline cellulose305.0 mg 500.0 mg Example 8 Tablets are prepared with the following composition:
boric acid 1.0 mg tartaric acid 100.0 mg vitamin K3-sodium bisulfite adduct 10.0 mg polyvinyl pyrrolidone 5.0 mg magnesium stearate 15.0 mg lactose 50.0 mg carboxymethyl cellulose50.0 mg microcrystalline cellulose2~.0 mg 500.0 mg The following in vitro and in vivo tests were performed with the tablets of the invention.
In vitro test Sperm obtained from 32 normo zoospermia persons was examined.
From the sperm 1 ml quantities containing 10 to lO0 millions of spermatozoa were mixed with 1 ml suspension obtained from 1 tablet at +38C on a watch-glass. The motion of the spermatozoa was observed. Partial immobilisation began l minute after the mixing and became complete in 5 to lO minutes depending on the vitality of the spermatozoa. The immobilized spermatozoa became eosin binders, which indicates the cell death. This process is irreversible. The spermatozoa could not be revived either by changing the pH or by adding fresh serum or by other methods.
In vivo model test The following test was carried out with women in their ovulation period. Tablets prepared according to the invention were wetted by water and thereafter inserted into the back-vaginal fornix. After 5 minutes the vagina was exposed and each 2 ml of a sperm having a concentration of 160 to 240 millions spermatozoa/ml were injected onto the women's cervix. The exposing instrument was removed and af~er 5 and 10 minutes repeated exposures were performed thereafter the content of the vagina was examined.
According to the microscopic examinations the immobilization is 50% after 5 minutes, while 100% after 10 minutes.
In vivo application test The tablets were used by women who were proved to be conceptive and till the time of the examination protected themselves only by the Ogino-Knaus rule. Among these women pregnancy occurred only in two cases during a one year period. In view of this fact the tablets of the inventions have the same efficiency as the intrauterine instruments ~the Pearl-index was 2).
The women examined were subjected to gynaecological examination every two or three months so that any side effects on the vagina or damaging effect on the mucous membrane would be determined. No such cases were found.
In view of the above described it can be stated that the vaginal tablets of the invention are suitable for the modern contraception in every respect.
Claims (11)
PROPERTY OR PRIVILEGE IS CLAIMED ARE DEFINED AS FOLLOWS:
1. Contraceptive vaginal tablets characterized in that they contain:
0.2 to 15 parts by weight of boric acid, 10 to 100 parts by weight of tartaric acid, 1 to 10 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 5 parts by weight of polyvinyl pyrrolidone, 2 to 15 parts by weight of magnesium stearate, 8 to 50 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose, and 50 to 320 parts by weight of microcrystalline cellulose.
0.2 to 15 parts by weight of boric acid, 10 to 100 parts by weight of tartaric acid, 1 to 10 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 5 parts by weight of polyvinyl pyrrolidone, 2 to 15 parts by weight of magnesium stearate, 8 to 50 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose, and 50 to 320 parts by weight of microcrystalline cellulose.
2. Contraceptive vaginal tablets characterized in that they contain:
0.2 to 3 parts by weight of boric acid, 10 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose, and 50 to 65 parts by weight of microcrystalline cellulose.
0.2 to 3 parts by weight of boric acid, 10 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose, and 50 to 65 parts by weight of microcrystalline cellulose.
3. A contraceptive vaginal tablet according to claim 1 which has the following composition:
boric acid about 5 parts by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 5 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 320 parts by weight.
boric acid about 5 parts by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 5 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 320 parts by weight.
4. A contraceptive vaginal tablet according to claim 1 which has the following composition:
boric acid about 15 parts by weight, tartaric acid about 50 parts by weight.
vitamin K3-sodium bisulfite adduct about 5 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 310 parts by weight.
boric acid about 15 parts by weight, tartaric acid about 50 parts by weight.
vitamin K3-sodium bisulfite adduct about 5 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 310 parts by weight.
5. A contraceptive vaginal tablet according to claim 1 which has the following composition:
boric acid 1 part by weight, tartaric acid about 100 parts by weight, vitamin K3-sodium bisulfite adduct about 5 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 274 parts by weight.
boric acid 1 part by weight, tartaric acid about 100 parts by weight, vitamin K3-sodium bisulfite adduct about 5 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 274 parts by weight.
6. A contraceptive vaginal tablet according to claim 1 which has the following composition:
boric acid about 1 part by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 319 parts by weight.
boric acid about 1 part by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 319 parts by weight.
7. A contraceptive vaginal tablet according to claim 1 which has the following composition:
boric acid about 5 parts by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 315 parts by weight.
boric acid about 5 parts by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 315 parts by weight.
8. A contraceptive vaginal tablet according to claim 1 which has the following composition:
boric acid about 15 parts by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 305 parts by weight.
boric acid about 15 parts by weight, tartaric acid about 50 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 305 parts by weight.
9. A contraceptive vaginal tablet according to claim 1 which has the following composition:
boric acid about 1 part by weight, tartaric acid about 100 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 269 parts by weight.
boric acid about 1 part by weight, tartaric acid about 100 parts by weight, vitamin K3-sodium bisulfite adduct about 10 parts by weight, polyvinyl pyrrolidone about 5 parts by weight, magnesium stearate about 15 parts by weight, carboxymethyl cellulose about 50 parts by weight, lactose about 50 parts by weight, microcrystalline cellulose about 269 parts by weight.
10. Process for preparing contraceptive vaginal tablets characterized in that:
0.2 to 15 parts by weight of boric acid, 10 to 100 parts by weight of tartaric acid, 1 to 10 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 5 parts by weight of polyvinyl pyrrolidone, 2 to 15 parts by weight of magnesium stearate, 8 to 50 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose, and 50 to 320 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
0.2 to 15 parts by weight of boric acid, 10 to 100 parts by weight of tartaric acid, 1 to 10 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 5 parts by weight of polyvinyl pyrrolidone, 2 to 15 parts by weight of magnesium stearate, 8 to 50 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose, and 50 to 320 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
11. Process for preparing contraceptive vaginal tablets characterized in that:
0.2 to 3 parts by weight of boric acid, 10 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose and 50 to 65 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
0.2 to 3 parts by weight of boric acid, 10 to 20 parts by weight of tartaric acid, 1 to 2 parts by weight of vitamin K3-sodium bisulfite adduct, 0.8 to 1.2 parts by weight of polyvinyl pyrrolidone, 2 to 5 parts by weight of magnesium stearate, 8 to 12 parts by weight of carboxymethyl cellulose, 8 to 12 parts by weight of lactose and 50 to 65 parts by weight of microcrystalline cellulose are homogenized and formed into tablets.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000441915A CA1214725A (en) | 1983-11-24 | 1983-11-24 | Contraceptive vaginal tablets and process for preparing them |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA000441915A CA1214725A (en) | 1983-11-24 | 1983-11-24 | Contraceptive vaginal tablets and process for preparing them |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1214725A true CA1214725A (en) | 1986-12-02 |
Family
ID=4126595
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000441915A Expired CA1214725A (en) | 1983-11-24 | 1983-11-24 | Contraceptive vaginal tablets and process for preparing them |
Country Status (1)
| Country | Link |
|---|---|
| CA (1) | CA1214725A (en) |
-
1983
- 1983-11-24 CA CA000441915A patent/CA1214725A/en not_active Expired
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| El-Beheiry et al. | Methotrexate and fertility in men | |
| US4202880A (en) | Delivery means for biologically active agents comprising hydrophilic polyurethane | |
| Lindsay et al. | Prospective double-blind trial of synthetic steroid (Org OD 14) for preventing postmenopausal osteoporosis. | |
| Scheinhorn et al. | Antituberculous therapy in pregnancy: risks to the fetus | |
| US4565694A (en) | Contraceptive vaginal tablets | |
| EP0472791A1 (en) | Composition containing neem oil for fertility control and prevention of pregnancy | |
| CA1214725A (en) | Contraceptive vaginal tablets and process for preparing them | |
| Croxatto et al. | Clinical assessment of subdermal implants of megestrol acetate, d-norgestrel, and norethindrone as a longterm contraceptive in women | |
| Tietze | History of contraceptive methods | |
| Abrutyn et al. | Teratology study of intravaginally administered nonoxynol-9-containing contraceptive cream in rats | |
| Cicero et al. | Acute alcohol exposure markedly influences male fertility and fetal outcome in the male rat | |
| Paz et al. | A direct effect of α‐chlorohydrin on rat epididymal spermatozoa | |
| Zaneveld et al. | Acrosin inhibitors as vaginal contraceptives in the primate and their acute toxicity | |
| NZ206039A (en) | Contraceptive vaginal tablets containing boric acid and vitamin k3 | |
| Wilk | Production of fetal rat malformations by norchlorcyclizine and chlorcyclizine after intrauterine application | |
| Normington et al. | Hypertension and oedema complicating pregnancy in Addison's disease. | |
| Dipaolo et al. | Malformations induced in the mouse by thalidomide | |
| Zahid et al. | Effect of chloroquine on liver weight of developing albino rats | |
| Tauber et al. | Reduced menstrual blood loss by release of an antifibrinolytic agent from intrauterine contraceptive devices | |
| Prema et al. | Serum copper in long-term users of copper intrauterine devices | |
| Swan et al. | Thyroid Autograft: A 12-Year Follow-Up | |
| Bernstein | Physiological aspects of vaginal contraception a review | |
| GB2121289A (en) | Intrauterine contraceptive device and method of its production | |
| Barlow et al. | Teratogenic effects of Silastic intrauterine devices in the rat with or without added medroxyprogesterone acetate | |
| Juneja et al. | Mouse sperm-egg interaction in vitro in the presence of neem oil |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MKEX | Expiry |