Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Aftertreated polymer
Patent
1996-09-13
1999-01-12
Kulkosky, Peter F.
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Aftertreated polymer
A61K 31735, A61K 31765, A61K 3119
Patent
active
058583440
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to an oral administration form with an active substance carrier wherein the active substance has at least one free carboxyl group ionically bound to a polymer having tertiary amino groups. The present invention further relates to a process for its production.
Binding ionizable substances to ion exchange resins is not new. It is mentioned in the standard works of pharmaceutical technology as one possibility of obtaining oral administration forms exhibiting a prolonged release. U.S. Pat. No. 2,990,332 describes such an oral system having a prolonged release period. However, the active substance release in such a simple ion-exchange-resin-active-substance complex takes place over an only relatively short period, and not over a minimum time of about 4 hours required for a controlled-release preparation.
Improvements are described in U.S. Pat. Nos. 3,138,525; 3,499,960 and 3,594,470; Belgian Patent No. 729,827, and German Patent No. 2,246,037. According to these patents, the ion exchanger particles may be provided with an additional coating for controlling the active substance release in order to achieve a prolonged release period. U.S. Pat. No. 4,221,778 proposes to impregnate the ion exchanger particles, after having been charged with active substance and prior to coating with the control membrane, with an agent which prevents excessive swelling of the ion exchanger particles on their contact with water or gastro-intestinal juice, and thus prevents a decomposition of the control membrane that would result therefrom.
Another application of ion exchangers is to bind pharmaceutical active substances in order to improve their unpleasant taste (DE-OS 3028082) and their unpleasant odor (CH-PS-3 83 552), respectively.
Uncharged basic ion exchangers have been used as drugs to reduce the blood cholesterol level for a long time. Their action is based on the fact that they bind bile acids in the intestinal tract and cause their excretion. The resorption prevented thereby results in an interruption of the so-called enterohepatic circulation. The organism reacts with an increased transformation of cholesterol into bile acid, directly resulting in a reduction of the blood cholesterol level.
The object of the present invention is to provide an oral administration form having acid active substances and a process for its production. This oral administration form has a high exchange capacity of an ion exchange carrier, allowing the transformation of liquid and low-melting active substances into a free-flowing, temperature-insensitive granulate, without having to use additional solvents. In case of active substances which are slightly soluble in the acid gastric juice, higher concentrations of dissolved active substance may be obtained by this granulate and a rapid or retarded release of the active substance from the administration form may be achieved by means of selective measures.
Most surprisingly, it was found that one ion exchanger used in medicine for a long time, colestipol or colestipol hydrochloride, is excellently suitable as a carrier for acidic active substances and combines the following advantages for the administration form:
a. high exchange capacity,
b. liquid active substances may be transformed into a free-flowing granulate without any additional auxiliary agents and solvents,
c. low-melting active substances may be transformed from the melt into a practically temperature-insensitive granular powder without having to use additional solvents,
d. good flow behavior of the granulate both in uncharged and charged condition,
e. the release from the active substance/carrier complex takes place very rapidly and meets, or even exceeds the requirements with respect to a rapidly disintegrating administration form,
f. higher concentrations of dissolved active substance possibly appear in case of active substances which are slightly soluble in the acid gastric juice,
g. a prolonged release may be achieved by additional measures,
h. owing to many years of experience, established toxicological
REFERENCES:
patent: 4996047 (1991-02-01), Kelleher et al.
Cremer Karsten
Muller Walter
Kulkosky Peter F.
LTS Lohmann Therapie-Systeme GmbH
LandOfFree
Oral administration form having acid active substances and a pro does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Oral administration form having acid active substances and a pro, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Oral administration form having acid active substances and a pro will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1511726