Gelatin or collagen hydrolysate containing drug formulation that

Details Gelatin or collagen hydrolysate containing drug formulation that Gelatin or collagen hydrolysate containing drug formulation that

1994-10-25

1999-08-03

Bawa, Raj

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Capsules

424456, 424457, 424468, 424489, 424490, 424492, 424464, 514951, 514962, A61K 948, A61K 914

Patent

active

059322454

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to a process for the preparation of a colloidally disperse system of poorly water-soluble pharmaceutical substances or of poorly water-soluble inorganic and/or organic compounds. It furthermore relates to a pharmaceutically administrable nanosol, i.e. a stable colloidally disperse system of poorly water-soluble pharmaceutical substances with gelatin. It furthermore relates to an immediate-effect medicament for the treatment of rheumatic and/or inflammatory diseases, which contains a 3-indolylacetic acid derivative. It finally relates to an immediate-effect medicament for the treatment of diabetes, which contains glibenclamide.
The difficulty of bringing pharmaceutical substances with problematic bioavailability into a satisfactory pharmaceutically administrable form is generally known. About 30% of all active compounds in medicaments are included under this group. A rapid release of the active compound from its preparation after administration, i.e. in general a rapid conversion into the dissolved, absorbable form must be demanded of them in order to achieve an acceptable therapeutic result. If it is assumed that the absorption process in vivo is not the rate-determining step, all technological processes for improving pharmaceutical substance release can be attributed to the influencing of two parameters in the so-called Noyes-Whitney equation: ##EQU1## where dc/dt: amount of solid going into solution per time=rate of solution, (wettable surface area), substances generally (in this case pharmaceutical substances). In this equation the changeable target quantities for the pharmacist are only the saturation concentration (saturation solubility) of the pharmaceutical substance and the substance surface area which can effectively be attacked by the solvent. An increase in these two parameters should also result in an increase in the rate of solution.
Classical processes for increasing the saturation solubility of pharmaceutical substances are e.g.:
These measures, however, have the disadvantage that on the one hand they burden the body with toxicologically suspect substances, on the other hand an increased solubility in vivo can be destroyed by the recrystallization processes. Often the amount to be used is additionally inadequate to bring the necessary dose of pharmaceutical substance into solution.
The solubilization of pharmaceutical substances by surface-active, micelle-forming substances or the formation of cyclodextrin inclusion compounds has therefore recently been described. Both applications, however, have the significant disadvantage that primarily dissolved pharmaceutical substance is actually not present in the body in free form, but must be released from its complex with the auxiliary. That is to say on the whole the release of pharmaceutical substance is worsened rather than improved. Apart from this, side effects due to surface-active substances are not to be excluded.
An increase in the surface area of pharmaceutical substances is possible by means of micronization. This processing, however, is very difficult and laborious and has its limit at a particle size of .gtoreq.1 .mu.m. The smaller the particles of powder, however, the more strongly prone they are to aerophilicity and the degree of wetting in contact with solvents (effective surface area A) becomes low--the rate of solution is rather reduced. The addition of hydrophilic excipients is therefore almost always necessary.
Further known processes for the preparation of small particles are e.g. the following:
Violanto (U.S. Pat. No. A-4,826,689) describes a method for the preparation of colloidally disperse particles of water-insoluble organic compounds. In this method, laborious test experiments are necessary to determine optimum values for the parameters temperature, rate of stirring and rate of addition of the aqueous precipitation liquid to the solution of the solid compound in the organic solvent. Only keeping to these preconditions ensures the formation of the particles described. A subsequent separation o

REFERENCES:
patent: 5080907 (1992-01-01), Iijima et al.
patent: 5118528 (1992-06-01), Fessi et al.
patent: 5133908 (1992-07-01), Stainmesse et al.

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