Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1996-10-21
2000-03-07
Wortman, Donna C.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424 44, A61F 902
Patent
active
060336838
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the field of pharmacotechnology.
Its subject is more especially a new process for the preparation of suppositories and in particular of suppositories having a laxative action.
Specifically, its subject is a process for the preparation of suppositories having a laxative action which are capable of causing a release of carbon dioxide by chemical reaction of active principles upon contact with the moisture present in the rectal ampul.
A process is known from French patent n.degree. 788.198 (Waldenmeyer J. G) which offers the possibility of releasing carbon dioxide in the nascent state under the action of moisture or other cause and in which the raw materials releasing this add by their mixture are coated one by one in a fatty substance which protects them against a premature decomposition and which does however allow them to be reached at the moment of use by the catalytic action of a hydrophilic agent.
It may be deduced, on reading this patent, that this could be a process for the preparation of suppositories releasing carbon dioxide, but nothing is said on this subject and only the use of a fatty substance such as cocoa butter can suggest such a use.
A medicinal preparation using this process subsequently appeared on the market. It is formed of a suppository containing an effervescent mixture of potassium acid tartrate and sodium bicarbonate capable, in a moist environment, of releasing ca. 50 ml to 100 ml of carbon dioxide in the rectum.
The problem created by the development of this medicinal preparation lies in the difficulty of realizing a product which does not react prematurely during production or shortly after production, while keeping the desired effervescence properties intact.
One thus finds oneself confronted with a double problem. The active principles are in fact separated from one another by a particularly lipophilic, absolutely tight barrier. Because of the latter, the medicinal preparation is capable of keeping perfectly, but on the other hand the active principles will not be able to react with one another, with the result that such a medicinal preparation is practically inactive.
On the other hand, if the active principles are not coated in an impermeable matrix, they are capable of reacting prematurely amongst themselves in the presentation pack and, above all, they are capable of reacting too violently amongst themselves in the rectal ampul and triggering distensions of the rectal ampul which are too great.
It was thus important to find a coating sufficiently insulating to prevent the constituents of the effervescent mixture from reacting with one another too soon, but also capable of leading, upon contact with a more or less moist mucous membrane, such as the rectal ampul, to a regular, constant and progressive release of carbon dioxide.
This object can be considered to be achieved by the process according to the invention.
In this process, the fatty substances are melted separately, the mixture is left to cool to the desired temperature and vegetable lecithin is dispersed in the fluid mass resulting from the melting, then a mineral opacifying agent is incorporated, and this is followed by the pouring in succession of the potassium acid tartrate, accompanied by stirring, and then of the sodium bicarbonate, accompanied by more vigorous stirring, these two constituents having a particular granulometry, and stirring is then continued until perfect homogeneity is achieved before proceeding with the drawing-off of the fluid suspension into the alveoli of suppositories.
After cooling, suppositories of a regular truncated-cone shape are obtained whose composition is homogeneous and whose preservation, attested by the volume of the release of carbon dioxide, is assured for at least two years.
It is thus clearly seen that the technical problem to be solved is markedly different from that considered by the Waldenmeyer process. At that time, the fatty substances constituted a tight coating which protected completely, and even too completely, against the catalytic
REFERENCES:
patent: 3764668 (1973-10-01), Higuchi et al.
patent: 5547976 (1996-08-01), Slater et al.
Ijima et al. "Effects of Aerosil 200 and Soybean Lecithin on Release of Carbon Dioxide from Effervescent Suppositories". Yakuzaigaku, vol. 53, No. 1, pp 55-62, 1993.
Hakata et al. "Effects of Bases and Additives on Release of Carbon Dioxide from Effervescent Suppositories". Chem. Pharm. Bull., vol. 41, No. 2, pp 351-356, 1993.
Note-Simonnard Axelle
Sirito Alain
Techni-Pharma
Wortman Donna C.
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