Process for preparing solid pharmaceutical dosage forms of hydro

Details Process for preparing solid pharmaceutical dosage forms of hydro Process for preparing solid pharmaceutical dosage forms of hydro

1996-07-18

1998-10-27

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424464, 424480, 424494, A61K 914

Patent

active

058275410

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/GB95/02485 filed Oct. 20, 1995 published as WO96/13251 May 9, 1996.
The present invention relates to a process for preparing solid pharmaceutical dosage forms and, in particular, to a process for preparing an oral solid rapidly disintegrating dosage form of a pharmaceutically active substance.
Many pharmaceutically active substances are presented for oral administration in the form of tablets, pills or capsules. The tablet, pill or capsule generally has to be swallowed with water so that the pharmaceutically active substance can be absorbed via the gastro-intestinal tract. For some patients swallowing the tablet, pill or capsule is difficult or impossible and this is particularly the case for paediatric patients and geriatic patients. A similar difficulty is often encountered when trying to administer tablets to non-human animals which may be uncooperative in taking tablets, pills or capsules.
Oral solid pharmaceutical dosage forms which rapidly disintegrate in the mouth and methods for their preparation have been proposed in GB-A-1548022 and GB-A-2111423. The solid dosage forms as disclosed comprise an open matrix network carrying the pharmaceutically active substance, the open matrix comprising a water-soluble or water-dispersible carrier material which is inert towards the pharmaceutically active substance. The solid dosage forms are prepared by the sublimation or removal of solvent from a solution or suspension comprising the pharmaceutically active substance and the carrier material. Sublimation or removal of solvent is preferably carried out by freeze drying.
Other methods for the preparation of oral solid pharmaceutical dosage forms which rapidly disintegrate in the mouth are disclosed in U.S. Pat. No. 5,039,540, U.S. Pat. No. 5,120,549, U.S. Pat. No. 5,330,763, PCT/JP93/01631 and PCT/US93/12566.
The solid dosage forms which are produced by these various methods rapidly disintegrate on being placed in the mouth of the patient, thereby delivering the desired dose of the pharmaceutically active substance.
The preparation of oral solid rapidly dispersing dosage forms generally involves the formation of a suspension of the drug in water, optionally together with a co-solvent such as alcohol, together with the matrix forming components. For many drugs a homogeneous suspension cannot be prepared due to the hydrophobicity of the drug which causes a stable foam to form during the mixing process which results in a lack of uniformity of content of the drug in the final product. This problem is exacerbated for very fine particles where air entrapment during mixing becomes greater.
We have now developed a process for the preparation of oral solid rapidly disintegrating dosage forms of hydrophobic drugs in which the foregoing problem is overcome.
Accordingly, the present invention provides a process for the preparation of an oral rapidly disintegrating dosage form of a hydrophobic pharmaceutically active substance which process comprises forming a suspension of the hydrophobic pharmaceutically active substance in a solvent containing a pharmaceutically acceptable surfactant together with a water-soluble or water-dispersible carrier material, forming discrete units of the suspension and removing solvent from the discrete units under conditions whereby a network of the carrier material carrying a dosage of the hydrophobic pharmaceutically active substance is formed.
By the term "rapidly disintegrating" as used herein is meant that the solid dosage form will disintegrate in water at 37.degree. C. in 60 seconds or less, preferably 5 to 10 seconds or less when tested by the following procedure which is analogous to the Disintegration Test for Tablets, B.P. 1973 and which is described in British Patent No. 1548022:
Apparatus
A glass or suitable plastic tube 80 to 100 mm long, with an internal diameter of about 28 mm and an external diameter of 30 to 31 mm, and fitted at the lower end, so as to form a basket, with a disc of rustproof wire gauze complying with the requirements for a No.

REFERENCES:
patent: 5456920 (1995-10-01), Matoba et al.
patent: 5587179 (1996-12-01), Gergely et al.
Derwent Abstract of WO 93 JP1631.

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