Tablet or capsule having a content of stable ranitidine hydrochl

Details Tablet or capsule having a content of stable ranitidine hydrochl Tablet or capsule having a content of stable ranitidine hydrochl

1996-08-19

1999-06-08

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424464, 514970, A61K 920

Patent

active

059103205

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION



BACKGROUND ART

From GB-B-1 565 966 ranitidine hydrochloride is known in a crystalline form that according to DE-C-3 139 134 is to be referred to an Form 1. It was not yet possible according to DE-C-3 139 134, however, to produce tablets with pure and highly crystalline ranitidine hydrochloride. That prior art provides for that purpose a new form of ranitidine hydrochloride that is said to be pure and highly crystalline and is referred to as Form 2. Form 2 can be obtained by recrystallisation of Form 1, it being possible to accelerate the recrystallisation process by adding seed crystals of Form 2.
According to DE-C-3 139 134, the X-ray diffraction spectrum of Form a is characterised inter alia by a strong band .theta.=10.degree. (4.40.ANG.) which Form 1 lacks according to Hohnjec et al. in Flory, Analytical Profiles of Drug Substances, Vol. 15, 1986, pages 549 to 550. The two forms can therefore be distinguished well from each other by means of radiography.
According to the prior art mentioned, therefore, at room temperature ranitidine hydrochloride exists as Form 2, whereas Form 1 is unstable, with the result that it changes into Form 2 in the presence of seed crystals of Form 2. It is therefore to be considered surprising that, according to the invention, tablets or capsules can be provided that are characterised by a powder mixture having a content of stable ranitidine hydrochloride Form 1 together with a carrier and/or diluent.


SUMMARY OF THE INVENTION

In the tablets or capsules according to the invention, ranitidine hydrochloride Form 1 is preferably in crystal-line form.
Preferred tablets or capsules according to the invention are those in which ranitidine hydrochloride Form 2 still cannot be detected by X-ray diffractometry at least 2 years after manufacture of the tablets or capsules.
With regard to-the availability of ranitidine hydrochloride Form 1, attention in drawn to GB-B-1 565 966 and to commercial products.


DESCRIPTION OF THE PREFERRED EMBODIMENTS

The invention is explained in detail below by means of Example.


EXAMPLE 1



______________________________________ ranitidine hydrochloride Form 1 336 mg Aerosil 5 mg Promojel 15 mg Emcocel 80 mg Emcanpress 31 mg corn starch 25 mg talc 5 mg magnesium stearate 3 mg Total 500 mg ______________________________________ 336 mg* of ranitidine hydrochloride Form 1 correspond to 300 mg of ranitidine base. *Translator's note: There is no unit of quantity in the German text.
The above recipe was used for direct tableting wherein, according to the size of charge chosen, multiples of the given amounts of all the constituents were thoroughly mixed in the dry state and compressed in a conventional tableting press. By X-ray diffractometry it could clearly be shown that the tablets produced did not contain any ranitidine hydrochloride Form 2.


EXAMPLES 2 TO 3



______________________________________ Components Example 2 Example 3 ______________________________________ 1 ranitidine hydrochloride Form 1 336.00 mg 336.00 mg 2 Avicel 101 64.00 mg 3 corn starch 4.60 mg 86.80 mg 4 Kollidon 25 13.00 mg 3.20 mg 5 drinking water for granulation 6 soluble starch 8.40 mg 7 Emcocel 40.00 mg 30.20 mg 8 Promojel 20.00 mg 20.00 mg 9 Kollidon Cl 9.80 mg 10 sodium dodecyl sulfate 1.00 mg 1.00 mg 11 magnesium stearate 3.00 mg 3.00 mg total 490.00 mg 490.00 mg ______________________________________
According to the size of charge chosen, a multiple of components 1 to 3 was mixed in the dry state. Components 4 and 6 were dissolved in 5, followed by granulation in a WS granulator or a Lodige granulator, drying and sieving. The resulting granules were thoroughly mixed with components 7 to 11 and compressed in a tablet press to form tablets weighing 490 mg. Once again, no ranitidine hydrochloride Form 2 could be detected by X-ray diffractometry in the tablets obtained.


EXAMPLE 4



______________________________________ ranitidine hydrochloride Form 1 336 mg Avicel 101 68 mg corn starch 14 mg Kollidon 2

REFERENCES:
patent: 5338871 (1994-08-01), Ngooi et al.

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