Oral administration form for peptide pharmaceutical substances,

Details Oral administration form for peptide pharmaceutical substances, Oral administration form for peptide pharmaceutical substances,

1994-09-13

1997-03-25

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424464, 424465, 424468, 424469, 424474, 424484, 514774, A61K 924, A61K 926, A61K 928

Patent

active

056142196

DESCRIPTION:

BRIEF SUMMARY
The invention relates to an oral administration form for peptide medicaments, which contains at least one peptide pharmaceutical substance, dispersed in a matrix of gelatin or a gelatin derivative, in addition to pharmaceutically customary excipients and auxiliaries. The invention furthermore relates to a process for the preparation of such an oral administration form.
In the highly industrialized countries, it can be assumed that about 2-3% of the population exhibit the diabetes syndrome. For the effective treatment of this disorder with its very important symptoms hyperglycemia, polyuria, glucosuria, as well as hyperlipidemia, we have to rely today, as before, on the exogenous supply of insulin, in spite of the enormous variety of pharmaceutical developments. Even the oral antidiabetics of the sulfonylurea type, which are only indicated if the endogenous production of insulin is at least still partially maintained, at most offer a limited width of application.
The administration of insulin is carried out to the greatest possible extent by injection (parenteral administration). Other administration routes, e.g. nasal, pulmonary, rectal or, especially, oral administration are presently under test. However, it has still not become public that an appropriate preparation could be ready to be put on the market. On the contrary, we find ourselves still at the stage of informative investigations. As is known, injections are associated with disadvantages. Thus, for example, lipodystrophy or other foreign body reactions can occur at the administration site. Problems with the handling of injection syringes are particularly to be expected with very young and relatively old patients. In these groups of patients, a regularly required injection must often be carried out by a person looking after them. It is therefore obvious that this effort does not particularly promote patient compliance.
The optimum, simplest and safest use of pharmaceutical substances, however, is oral administration, for example of tablets, capsules or beverage solutions. In the case of peptide pharmaceutical substances, such as e.g. insulin, marked difficulties result, however, because these are inactivated to the greatest part by enzymatic degradation after release in the gastro-intestinal tract (GIT; stomach or small intestine) even before absorption. Enzymatic degradation in the stomach or small intestinal fluid or on the mucosa threatens to lower the bioavailability of peptide pharmaceutical substances, particularly insulin, to a minimum. Additionally, the mechanism of absorption by means of passive transport is largely lacking for peptide pharmaceutical substances. This is based, on the one hand, on the molecular size, because the exclusion limit for passive transport is assumed to be about 500 Daltons. On the other hand, substance-specific properties, such as hydrophilicity (low distribution coefficient), self-association to form larger units or binding to constituents of the gastro-intestinal tract make absorption difficult. In addition, absorption is also made difficult if negative charge formed as a result of dissociation of functional active compound groups leads to electrostatic repulsion at the glycocalyx, the negatively charged glycoprotein layer on which the lipid double layer lies. Absorption of peptide pharamaceutical substances, however, is of extraordinary importance despite this if it is wished to manage a parenteral supply successfully.
It has already been proposed to administer insulin encapsulated in liposomes. In these investigations, however, it did not appear possible to determine the amount of insulin absorbed quantitatively. These experiments can therefore probably only offer rough guiding values. The use of liposomes is moreover accompanied, as is known, by difficulties both in the preparation and in the storage of appropriate pharmaceutical forms.
More recently, useful starts were reported in order to be able to administer insulin orally. Of particular interest in this case are pharmaceutical forms which are stomach-

REFERENCES:
patent: 4582719 (1986-04-01), Kaetsu et al.

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