Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Reexamination Certificate
2000-01-19
2001-08-07
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
C424S430000, C424S436000, C424S422000, C514S966000, C514S967000, C514S968000
Reexamination Certificate
active
06270789
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to a base for a suppository to be applied to rectum, urethra, vagina or the like and a suppository containing that. In particular, the present invention relates to the suppository having superior heat resistance which should not cause quality deterioration such as deformation and cracks during the storage even in a relatively high temperature, and also shows the same release, internal absorbability, safety, effect and the like as those of the suppositories used thus far at the applied region, and the base therefor.
BACKGROUND OF THE INVENTION
The suppository is a solid preparation at normal temperature, and when applied to rectum, urethra, vagina or the like, is softened or melted at the body temperature, or dissolved in local mucus to make the drug absorbed into the body through the mucous membrane.
In the suppository such as a drug for treating hemorrhoids, the oily or fatty base for the suppository acts as the lubricant upon evacuation and prevent becoming more serious condition.
Many suppositories being commercially available contain oily or fatty bases such as hard fat, cacao butter and the like and their melting point is adjusted to not higher than the body temperature in order to be softened or melted at around body temperature.
For the above reasons, as to the condition for storing the suppositories, it is required to keep the suppositories in cool storage at usually not higher than 15° C. or at most 30° C., or to preserve them in the upside position of the suppository down, therefore there are many limitations in storage compared with other formulations.
It is difficult to maintain good conditions for the suppository in the case where the suppository stands at high temperature for a long time, for example, in the summer or in the car during transportation. Therefore, after the suppository has been handed to the patient, it is particularly difficult to keep it in the good condition.
On the other hand, the suppository comprising macrogol and the like has a higher melting point so as to be dissolved in the local mucus and to exhibit the effect of the drug. Therefore, it hardly causes the problems described above in the suppository comprising an oily or fatty base, however, the patient may suffer from congestion, erythema or the like on mucous membrane caused by the physical stimulation of the suppository brought about by the absorption of mucus at the local area.
The suppository containing a higher alcohol, surfactant, absorption controlling agent and the like sometimes causes poor absorption or the sustained release of the drug. Further, it may have a side effect such as strong stimulation of the local mucous membrane.
These suppositories having a high melting point may not spread by the reasons, for example, that suppository administered in the rectum is not adequately melted or softened and may not play a role of the lubricant upon evacuation which is a characteristic of the suppository. Under the circumstances, one of the objects of the present invention is to provide a suppository which does not exhibit the quality deterioration such as the deformation and crack and shows the same drug release, internal absorbability, effect and safety as those of the conventional suppositories at the applied region.
SUMMARY OF THE INVENTION
As a result of the efforts of the present inventors, it was found that a base for a suppository comprising oily or fatty base and polyethylene, if necessary further polyglycerin fatty acid ester, is capable of achieving the above objects. Namely, the present invention relates to,
(1) A base for a suppository comprising oily or fatty base and polyethylene,
(2) The base for the suppository according to (1) further comprising polyglycerin fatty acid ester,
(3) The base for the suppository according to (1) or (2), wherein the weight ratio of the oily or fatty base or the total amount of oily or fatty base and polyglycerin fatty acid ester to polyethylene is 1:0.01-0.5,
(4) The base for the suppository according to one of (1) to (3), wherein the content of polyethylene in the total weight of the base for suppository is 1 to 20 weight %,
(5) The base for the suppository according to one of (1) to (4), wherein the average molecular weight of polyethylene is 500 to 30,000,
(6) The base for the suppository according to (2) or (3), wherein the content of polyglycerin fatty acid ester in the total weight of the base for the suppository is 0.5 to 10 weight %,
(7) The base for the suppository according to (1) or (2), wherein the oily or fatty base is at least one member selected from the group consisting cacao butter, lauric oil, beef tallow and hard fat, or the above base to which at least one member selected from the group consisting of coconut oil, palm kernel oil, tsubaki oil, olive oil, soybean oil, sesame oil, corn oil, middle chain fatty acid triglyceride, liquid petrolatum or isopropyl myristate being liquid at the normal temperature is added,
(8) A suppository comprising a drug and the base for suppository according to (1) or (2), and
(9) The suppository according to (8), wherein the drug is at least one member selected from the group consisting adrenocortical hormone, local anesthetic, antipyretic-analgesic-antiphlogistic, antiphlogistic-antipruritus-wound healing agent, vitamin, sulfa drug, antibiotic, fungicide, bactericide, vasoconstrictor, antihistamine, narcotic, hypnotic sedative, antianxiety drug, antiepileptic, stimulant-analeptic, antiparkinsonism drug, central nervous system acting drug, skeletal muscle relaxant, autonomic drug, spasmolytic, antivertigos, cardiotonic, antiarrythmic drug, diuretic, antihypertensive agent, coronary vasodilator, peripheral vasodilator, antihyperlipemia agent, respiratory accelerator, antidiarrheic-intestinal function controlling agent, peputic ulcer treating agent, bronchodilator, antiallergic drug, cathartic, clyster, cholagogue and various hormones except for adrenocortical hormone.
REFERENCES:
patent: 4765978 (1988-08-01), Abidi et al.
patent: 4871777 (1989-10-01), Breitzke
patent: 5783555 (1998-07-01), Suzuki et al.
patent: 55081812 (1980-06-01), None
patent: 63179820 (1988-07-01), None
Fukuda Izumi
Omachi Kengo
Sameshima Teruyuki
Amato Pharmaceutical Products, Ltd.
Fubara Blessing
Page Thurman K.
Wenderoth , Lind & Ponack, L.L.P.
LandOfFree
Base for suppository does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Base for suppository, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Base for suppository will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2492442