Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1997-03-24
2000-01-04
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424489, 424465, A61K 920
Patent
active
060107170
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/NL95/00321, filed Sep. 25, 1995.
This invention relates to specific starch products which are suitable as tabletting excipient, in particular as filler and/or binder. Tablets usually contain--in addition to the active ingredient such as a drug, vitamin, cleansing agent, color, insecticide or herbicide--particular inert components, often designated by the term of tabletting excipients. These tabletting excipients are classified according to their functional properties, such as binders, fillers, disintegrants, lubricants, flavors and colors. Suitable starch products can also fulfil several functions, such as the combination of binder and filler (often designated as filler/binder).
The starch products according to the invention are suitable in particular as filler/binder in tablets, pellets, pills, capsules and granules. For the manufacture of the tablets, the conventional production techniques can be used, viz. dry granulation, wet granulation and direct compression. The starch products according to the invention are suitable in particular in the manufacture of tablets by direct compression, whereby the powder mixture to be tabletted is introduced into the molds of a tabletting press and then compressed into tablets with a stamp.
Most kinds of starch consist of granules in which two types of glucose polymers occur, viz. amylose (15-35% by weight based on the dry substance) and amylopectin (65-85% by weight based on the dry substance). Amylose consists of substantially linear molecules with an average degree of polymerization (DP) of 1000-5000 (depending on the kind of starch). Amylopectin consists of very large, highly branched molecules with an average degree of polymerization of about 2,000,000. The commercially most important types of starch, viz. maize starch, potato starch, wheat starch and tapioca starch, contain 15-30% by weight of amylose. Of some types of cereal (barley, maize, millet, milo, rice and sorghum) and of potato starch, there exist varieties that consist substantially completely of amylopectin. These types of starch contain less than 5% by weight of amylose and are designated by the term amylopectin starches.
By debranching amylopectin molecules with so-called debranching enzymes, such as pullulanase and isoamylase, short-chain linear glucose polymers are obtained with a degree of polymerization which is substantially between 10 and 75. These products are designated as short-chain amylose, linear dextrin or amylodextrin, as opposed to long-chain amylose with a degree of polymerization of more than 100, which occurs naturally in starch granules or has been obtained by limited partial depolymerization of this amylose.
The use of various starch products as tabletting excipient is known. European patent specification 499 648 and International patent publication WO 94/01092 describe the use of low-molecular and/or high-molecular amylose products as tabletting excipient. The preparation and use of low-molecular or high-molecular amylose as tabletting excipient is also described in the following two journal articles: Preparation, Characterization, and Pharmaceutical Application of Linear Dextrins: I. Preparation and Characterization of Amylodextrin, Metastable Amylodextrins, and Metastable Amylose. Pharmaceutical Research, Vol. 10, No. 9, 1993, pp. 1274-1279. Characterization and Pharmaceutical Application of Linear Dextrins: IV. Drug release from capsules and tablets containing amylodextrin. International Journal of Pharmaceutics 98 (1993) 219-224.
The starch products described in the above-mentioned publications have as disadvantages that they do not possess optimum tabletting properties, that the method of preparation is laborious and expensive and/or that relatively expensive and scarce amylopectin starches have to be used as starting material in the preparation. The starch products according to the invention possess excellent tabletting properties and are produced from amylose-containing types of starch.
The starch products that are used as tabletting excipi
REFERENCES:
patent: 5468286 (1995-11-01), Wai-Chiu et al.
Gerrit H.P. Te Wierik, Jacoba Van der Veen, Anko C. Eisens and Coenraad F. Lerk, Preparation, characterization and application of linear dextrins. Part VI. General applicability and mechanism of programmed release from amylodextrin tablets, Journal of Controlled Release, 27 (1993) 9-17.
Gerrit H.P. Te Wierik, Anko C. Eissens, Arie C. Besemer, and Conrad F. Lerk, Preparation, Characterization, and Pharmaceutical Application of Linear Dextrins. I. Preparation and Characterization of Amylodextrin, Metastable Amylodextrins, and Metastable Amylose, Pharmaceutical Research, vol. 10, No. 9, 1993.
Arends-Scholte Anna Willemina
Bergsma Jacob
Eissens Anko Cornelus
Gottlieb Kornelis Fester
Lerk Coenraad Ferdinand
Benston, Jr. William E.
Page Thurman K.
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