|Publication number||US3358687 A|
|Publication date||Dec 19, 1967|
|Filing date||Dec 6, 1965|
|Priority date||Dec 6, 1965|
|Publication number||US 3358687 A, US 3358687A, US-A-3358687, US3358687 A, US3358687A|
|Inventors||Robert A Miley, Gwilt John Ruff, Godfrey David|
|Original Assignee||Sterling Drug Inc|
|Export Citation||BiBTeX, EndNote, RefMan|
|Patent Citations (5), Referenced by (6), Classifications (10)|
|External Links: USPTO, USPTO Assignment, Espacenet|
United States Patent 3,358,687 SUPPOSITORIES Robert A. Miley, London, John Rufi Gwilt, Monkseaton,
Northumberland', David Godfrey, Ewell, Surrey, England, assignors to Sterling Drug Inc., New York, N.Y.,
a corporation of Delaware Filed Dec. 6, 1965, Ser. No. 511,802 4 Claims. (Cl. 128-271) ABSTRACT OF THE DISCLOSURE fined to another portion of the suppository, and methods of making said suppository containing the active ingredients.
This invention relates to suppositories and in particular provides a suppository with which one is able to administer, in the same formulation, ingredients which are mutually incompatible.
According to the present invention there is provided a suppository containing at least two active ingredients and in which one or more active ingredients are confined to one portion of the suppository, while one or more other active ingredients are confined to another portion or portions of the suppository.
There are frequently instances where it would be desirable to administer, simultaneously by means of a suppository, active substances which are mutually incompatible and this can now be done using the suppository of the present invention. Examples of groups of substances which it may be desired to formulate together in a suppositoiy but which are mutually incompatible are the following:
Cocaine ichthymo]. Codeine incompatible with tannines. Morphine iodides.
alkali metal carbonates. Chloral hydrate incompatible with iodides.
Suppositories normally have an elongated shape and the active ingredients may be confined to different portions extending longitudinally of the suppository although it is preferred that the suppository is divided transversely into portions abutting end to end and containing the separated ingredients.
Where the suppository is divided transversely, it is advantageously employed as a means for administering different active ingredients to difierent parts of the tract to be treated. For example, in the treatment of internal haemorrhoids it is customary to administer a vasoconstrictor decongestant by means of a suppository to the rectal mucosa, i.e. above the ano-rectal sphincter, since the drug is absorbed through the rectal mucosa, although the pain resulting from haemorrhoids is due to inflammation of and tension in the anal canal and consequently relief of this pain will be effected by the application of local anaesthetic to the anal canal, i.e. below the anorectal sphincter. In order to achieve the greatest eifect from the decongestant and the local anaesthetic, therefore, the decongestant should be concentrated at the rec- 'tory.
By confining the decongestant or other suitable drug to that portion of the suppository which penetrates above the ano-rectal sphincter, it is possible to administer the drug in more accurate doses since the whole of the drug is released at the site of the rectal mucosa from which it is absorbed and loss of the drug arising from release into the anal canal, as occurs in the case with conventional suppositories, is minimised.
Suppositories in accordance with the invention may be prepared by mixing separately the active substances which it is desired should be confined to different portions of the suppository with a conventional suppository base, such as a petroleum jelly, cocoa-butter or a triglyceride, preferably in the presence of a dispersing agent, moulding the separate mixtures into the desired complementary shaped portions and pressing the ends of the shaped portions together, or melting the ends and touching them together, so that they adhere to form the final suppository. Other conventional ingredients may be incorporated into one or more portions of the suppository, such as antiseptics, analgesics and astringents.
In order to identify the particular formulation of the suppository and also to indicate which end of the suppository should be inserted first into the tract to be treated, it is possible to incorporate different colouring materials into the portions of the suppository which contain different active substances.
The following example is given to illustrate the invention and the manner in which it may be carried into efiect:
The following ingredients were mixed together and the resulting mixture shaped to form the upper or leading portion of a suppository for treating haemorrhoids:
MG. Phenylephrine hydrochloride (decongestant) 7.5 Oil soluble colour, q.s.
Triglyceride base to 900 The complementary portion of the suppository was formed by mixing the following ingredients and shaping the resultant mixture:
- MG. Amethocaine hydrochloride (local anaesthetic) 10 Bismuth subcarbonate (astringent) Tyloxypol (dispersing agent) 25 Oil-soluble colour, q.s. Triglyceride base to 1900 The ends of the two portions were joined by pressing them together or by melting the ends and touching them together and a final suppository was obtained which weighed 2.8 grams. The colouring materials employed in the two portions were different so that the active ingredient in each portion could be identified.
It will be appreciated that the invention is not limited by the specific Example above set forth and that various modifications are possible; for example, instead of separately shaping the two portions of the suppository and joining them as described, the molten complementary composition may be cast into a mould containing the solidified first portion thus automatically securing a bond between the two portions.
It will also be appreciated that the invention is not limited to formulations in which there are mutually incompatible ingredients which have to be kept separate from one another since it is an entirely separate advantage of this invention that difierent ingredients may be suitably positioned in use to exert their particular etfects to the greatest advantage whether those ingredients are compatible or incompatible.
The accompanying drawings are diagrammatic illustrations of the two essential forms of suppositories in accordance with the present invention.
1. A suppository containing at least two active ingredients and divided transversely into two portions abutting end to end, one or more of the active ingredients being confined to one portion and one or more of the other ac tive ingredients being confined to the other portion, one of the active ingredients being a decongestant agent and another being a local anaesthetic agent, the decongestant agent being in the end portion of the suppository intended for insertion into the patient.
2. A method of manufacturing a suppository as in claim 1 which comprises separately mixing with a suppository base the active ingredients which are to be separated from one another, moulding the first mixture in a mould to form a first complementary portion, casting the second molten mixture into the mould containing the solidified first portion in order to mould the second portion into contact with the first portion.
3. A suppository according to claim 1 wherein the separated ingredients are incompatible with one another.
4. A suppository according to claim 1 wherein colouring material is incorporated into one or more of the portions.
References Cited UNITED STATES PATENTS 2,987,445 6/ 1961 Levesque 16782 3,062,716 11/ 1962 Montandraud 16-7-58 FOREIGN PATENTS 591,138 1/1960 Canada. 917,456 2/ 1963 Great Britain. 936,603 2/ 1948 France.
ADELE M. EAGER, Primary Examiner.
|Cited Patent||Filing date||Publication date||Applicant||Title|
|US2987445 *||Oct 10, 1958||Jun 6, 1961||Rohm & Haas||Drug composition|
|US3062716 *||Feb 8, 1960||Nov 6, 1962||Applic Chimiques D Etudes Et D||Method of treating hemorrhoids|
|CA591138A *||Jan 19, 1960||Ciba Ltd||Shaped medicament carriers and process for their manufacture|
|FR936603A *||Title not available|
|GB917456A *||Title not available|
|Citing Patent||Filing date||Publication date||Applicant||Title|
|US4670256 *||Sep 23, 1985||Jun 2, 1987||V. Valhalla Corp.||Vaginal conditioning for sexual activity|
|US5213738 *||Nov 4, 1991||May 25, 1993||L. Perrigo Company||Method for making a capsule-shaped tablet|
|US6663892||Aug 19, 2002||Dec 16, 2003||L. Perrigo Company||Multiple portion tablet|
|US7332183 *||Dec 22, 2003||Feb 19, 2008||Pozen Inc.||Multilayer dosage forms containing NSAIDs and triptans|
|US8022095||Apr 16, 2003||Sep 20, 2011||Pozen, Inc.||Methods of treating headaches using 5-HT agonists in combination with long-acting NSAIDs|
|US20040180089 *||Dec 22, 2003||Sep 16, 2004||Pozen Inc.||Multilayer dosage forms containing NSAIDs and triptans|
|U.S. Classification||604/288, 514/537, 514/653, 424/436, 514/966, 424/472|
|Cooperative Classification||A61J3/08, Y10S514/966|