Oral pharmaceutical preparation containing ibandronat

Details Oral pharmaceutical preparation containing ibandronat Oral pharmaceutical preparation containing ibandronat

1998-11-25

2000-11-07

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424480, A61K 936

Patent

active

061433268

DESCRIPTION:

BRIEF SUMMARY
The invention relates to pharmaceutical formulations of ibandronate or its physiologically tolerable salts for oral application, and to processes for producing same.
The active substance ibandronaic acid (1-hydroxy-3-(N-methyl-N-pentyl)aminopropyl-1,1-diphosphonic acid) and its salts (ibandronates), respectively, are among the class of diphosphonic acids which, in particular, are of interest in the treatment of bone diseases and particular disorders in the calcium metabolism such as hypercalcaemia, osteoporosis, tumor osteolysis or Paget's disease. In the treatment of the diseases mentioned, these active substances must be administered frequently and over a long period of time and therefore, the aim should be especially oral application in addition to intravenous application since it is the former which is more accepted by many patients.
Fundamentally, however, oral treatment is generally complicated by the well-known problems with oral tolerability of diphosphonic acids. Diphosphonic acids or their physiologically safe salts, and particularly aminodiphosphonic acids are known to give rise to irritations of the upper gastrointestinal tract (Fleisch H., Bisphosphonates in Bone Disease, Herbert Fleisch, Bern 1993, pp. 126-131). The same applies for diphosphonates which are also ingested at relatively low dosages of, e.g., less than 50 mg per single administration form. WO 93/09785 points out that the active substance risedronate ([1-Hydroxy-2-(3-pyridinyl)ethylidene]bisphosphonate), for example, may give rise to erosions and ulcerations in the upper sections of the digestive tract. Various references allude to the gastrointestinal intolerability of the active substances pamidronate (Dodwell D. et al., Biochemical Effects, Antitumor Activity and Pharmacokinetics of Oral and Intravenous Pamidronate (APD) in the Treatment of Skeletal Breast Cancer, Br. J. Cancer 62, 496 (1990)) and tiludronate (Reginster J. Y., Efficacy and Tolerability of a New Formulation of Oral Tiludronate (Tablet) in the Treatment of Paget's Disease of Bone, J. Bone Miner. Res. 9, 615-619 (1994)). In addition, it is also well-known that motility disorders may occur when swallowing the tablets and/or the tablets to be ingested get stuck due to the particular anatomic situation in the oesophagus. This may give rise to odynophagia or oesophageal strictures as well. Frequently, this is the case with elderly patients or with patients who, due to their disease, are forced to take the required tablets predominantly in a lying position.
Accordingly, in order to solve these problems, the art demanded that fundamentally, orally available administration forms be coated with a gastric juice-resistant film so that the active substance is released only subsequent to the passage through the stomach and thus, irritations of the stomach and the oesophagus would be avoided. For example, WO 95/08331 describes administration forms by which it is possible to reduce the irritating potential of alendronate and other diphosphonates in oral application.
Due to the above-described oral intolerability of diphosphonates, there has been a search for more tolerable administration forms for a number of these active substances. In particular, oral administration forms coated with gastric juice-resistant coatings have been developed in this context. Such coatings are the choice in protecting the upper sections of the gastrointestinal tract, particularly the oesophagus or the stomach, from intolerable active substances. These gastric juice-resistant coatings on solid oral administration forms dissolve only at higher pH values of about 5.5 on, so that in the acidic gastric medium, being at a pH value far below 5.5, no active substance will be released from the administration form and thus, the stomach is protected from irritations caused by the active substance. As no active substance is released in the stomach, it is possible at the same time to prevent oesophagitis or other irritations of the oesophagus caused by the refluxing gastric contents containing active substance.

REFERENCES:
patent: 5296475 (1994-03-01), Flesch et al.
patent: 5358941 (1994-10-01), Bechard et al.
patent: 5431920 (1995-07-01), Bechard

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