CA1199871A - Drug preparations for glycoside hydrolase inhibitors - Google Patents
Drug preparations for glycoside hydrolase inhibitorsInfo
- Publication number
- CA1199871A CA1199871A CA000410394A CA410394A CA1199871A CA 1199871 A CA1199871 A CA 1199871A CA 000410394 A CA000410394 A CA 000410394A CA 410394 A CA410394 A CA 410394A CA 1199871 A CA1199871 A CA 1199871A
- Authority
- CA
- Canada
- Prior art keywords
- weight
- active ingredient
- amount
- preparation according
- drug preparation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired
Links
- 238000002360 preparation method Methods 0.000 title claims description 30
- 239000003814 drug Substances 0.000 title claims description 16
- 229940079593 drug Drugs 0.000 title claims description 16
- 102000005744 Glycoside Hydrolases Human genes 0.000 title claims description 6
- 108010031186 Glycoside Hydrolases Proteins 0.000 title claims description 6
- 239000004093 hydrolase inhibitor Substances 0.000 title claims description 6
- 239000000654 additive Substances 0.000 claims description 20
- 239000004480 active ingredient Substances 0.000 claims description 17
- 230000000996 additive effect Effects 0.000 claims description 14
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 14
- 229920002472 Starch Polymers 0.000 claims description 11
- 239000000843 powder Substances 0.000 claims description 10
- 239000008107 starch Substances 0.000 claims description 10
- 235000019698 starch Nutrition 0.000 claims description 10
- 235000019359 magnesium stearate Nutrition 0.000 claims description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 7
- 239000001913 cellulose Substances 0.000 claims description 6
- 229920002678 cellulose Polymers 0.000 claims description 6
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 6
- BPQQTUXANYXVAA-UHFFFAOYSA-N Orthosilicate Chemical compound [O-][Si]([O-])([O-])[O-] BPQQTUXANYXVAA-UHFFFAOYSA-N 0.000 claims description 5
- 150000005846 sugar alcohols Chemical class 0.000 claims description 5
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 4
- 229940124036 Hydrolase inhibitor Drugs 0.000 claims description 3
- 235000021355 Stearic acid Nutrition 0.000 claims description 3
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 3
- 235000013539 calcium stearate Nutrition 0.000 claims description 3
- 239000008116 calcium stearate Substances 0.000 claims description 3
- 150000002337 glycosamines Chemical class 0.000 claims description 3
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 3
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 3
- 239000008117 stearic acid Substances 0.000 claims description 3
- 239000000454 talc Substances 0.000 claims description 3
- 235000012222 talc Nutrition 0.000 claims description 3
- 229910052623 talc Inorganic materials 0.000 claims description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 3
- 239000000126 substance Substances 0.000 claims 1
- XUFXOAAUWZOOIT-SXARVLRPSA-N (2R,3R,4R,5S,6R)-5-[[(2R,3R,4R,5S,6R)-5-[[(2R,3R,4S,5S,6R)-3,4-dihydroxy-6-methyl-5-[[(1S,4R,5S,6S)-4,5,6-trihydroxy-3-(hydroxymethyl)-1-cyclohex-2-enyl]amino]-2-oxanyl]oxy]-3,4-dihydroxy-6-(hydroxymethyl)-2-oxanyl]oxy]-6-(hydroxymethyl)oxane-2,3,4-triol Chemical compound O([C@H]1O[C@H](CO)[C@H]([C@@H]([C@H]1O)O)O[C@H]1O[C@@H]([C@H]([C@H](O)[C@H]1O)N[C@@H]1[C@@H]([C@@H](O)[C@H](O)C(CO)=C1)O)C)[C@@H]1[C@@H](CO)O[C@@H](O)[C@H](O)[C@H]1O XUFXOAAUWZOOIT-SXARVLRPSA-N 0.000 description 6
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 6
- 229960002632 acarbose Drugs 0.000 description 6
- XUFXOAAUWZOOIT-UHFFFAOYSA-N acarviostatin I01 Natural products OC1C(O)C(NC2C(C(O)C(O)C(CO)=C2)O)C(C)OC1OC(C(C1O)O)C(CO)OC1OC1C(CO)OC(O)C(O)C1O XUFXOAAUWZOOIT-UHFFFAOYSA-N 0.000 description 6
- 229940057948 magnesium stearate Drugs 0.000 description 6
- 229940016286 microcrystalline cellulose Drugs 0.000 description 6
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 6
- 239000008108 microcrystalline cellulose Substances 0.000 description 6
- 229920002261 Corn starch Polymers 0.000 description 4
- 235000010980 cellulose Nutrition 0.000 description 4
- 239000008120 corn starch Substances 0.000 description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 3
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Chemical class OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical class OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 229930195725 Mannitol Chemical class 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 2
- 238000007908 dry granulation Methods 0.000 description 2
- 238000005469 granulation Methods 0.000 description 2
- 230000003179 granulation Effects 0.000 description 2
- 239000003112 inhibitor Substances 0.000 description 2
- 239000000594 mannitol Chemical class 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 235000012239 silicon dioxide Nutrition 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- 229960001866 silicon dioxide Drugs 0.000 description 2
- 239000000600 sorbitol Chemical class 0.000 description 2
- 238000005507 spraying Methods 0.000 description 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical class OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 239000004411 aluminium Substances 0.000 description 1
- 229940099112 cornstarch Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000009477 fluid bed granulation Methods 0.000 description 1
- 150000002402 hexoses Chemical class 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 150000002972 pentoses Chemical class 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 229940116317 potato starch Drugs 0.000 description 1
- 229940100486 rice starch Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Abstract
BAYER AKTIENGESELLSCHAFT
New drug preparations for glycoside hydrolase inhibitors ABSTRACT OF THE DISCLOSURE
The invention relates to glycoside hydrolase inhibitor-containing drug preparations comprising (a) at least one glycoside hydrolase inhibitor of the amino sugar type and.
at least one additive selected from magnesium stearate, calcium sterate, stearic acid and talc; the preparations also optionally contain a further additive or additives.
New drug preparations for glycoside hydrolase inhibitors ABSTRACT OF THE DISCLOSURE
The invention relates to glycoside hydrolase inhibitor-containing drug preparations comprising (a) at least one glycoside hydrolase inhibitor of the amino sugar type and.
at least one additive selected from magnesium stearate, calcium sterate, stearic acid and talc; the preparations also optionally contain a further additive or additives.
Description
The present invention relates to new glycoside hydrolase inhibitor - containing drug preparatlons.
According to the present invention we provide a drug preparation comprising at least one glycoside hydrolase inhibitor of the amino sugar type as active ingredient and s-tarch, and at least one additive selected from magnesium stearate, calcium stearate, stearic acid and talc, wherein the additive is present in an amount of 0.1 to 3% b~ weight relative to the weight of active ingredient and the relationship between -the amount by weight of active ingredient and the total amount by weight of the other additive(s) including starch is 1:1 to 1:25, -the moisture content of the preparation not being above 6% by weigh-t of the preparation. The drug preparation according to the present invention also optionally comprises a further additive or additives.
Particularly suitable glycoside hydrolase inhibitors, which can be used within the scope of the present invention, are acarbose and inhibitors related to acarbose. Such inhibitors are described, for example, in sritish patent no. 1,482,543, British patent no. 2,011,397 and in DE~OS (German published specification) 2,903,710.
The preparations according to the invention are particularly suitable for the preparation of tablets (see Examples 1 and 2) and for the preparation of granular powders (see Example 3); the granular powders being, if desired, encapsulated ~see Example 4). The further additives which are optionall~
included depend on the form chosen as suitable for the final L
administration and preferably include at least one su~stance chosen from silicate polyvinylpyrrolidone, sugar alcohol and cellulose.
In the drug preparations according to the invention, the relationship between the amount by weight of active ingredient and the total amount by weight of the other additives including the starch is generally 1:1 to 1:25 preferably 1:2.5 to 1:10.
- la -8~
In addition, the preparations according to the invention contain starch. This starch can be added in the form of potato starch, corn starch, wheat starch or rice starch. This starch, which is preferably dried, is generally added in an amount which is 1 to 10 -times the weight of active ingredient.
The magnesium stearate, calcium stearate, stearic acid and/or talc contained in the preparation is generally employed in an amount of 0~1 to 3O~ preferably 0.5 to 1. 5~o and particularly 1o by weight relative to the weight of active ingredien-t.
If the preparation according to the invention is proces-sed to a granular powder by the dry granulation procedure, the addition of cellulose is recommended as a further additive. This can be added in powder form. Microcry-stalline cellulose is particularly preferred. The amount of cellulose employed is generally 0.2 to 1.5 times the weight of active ingredient contained in the preparation.
In addition, when dry granulation is used, it is advan-tageous to employ a silicate, preferably silicon dioxide as a further additive. In this context, colloidal sili-con dioxide is very particularly preferably used. Theamount of silicate is generally 0.5 to 1.5,O,preferably lio~ by weight relative to the weight oF active ingredient.
On processing the preparation according to the inven-tion to a granular powder by the fluidised bed granulation 30 procedure, it is advantageous to employ polyvinylpyrroli-done, as a further additive. This PVP has, in general, a molecular weight From about 15~000 to about 60,000, PVP with a molecular weight from 20,000 to 30~000 is preferred.
Le A 21 279 7~
If it is desired to prepare a granular powder which dissolves rapidly in water, it is recommended that at leas-t one sugar alcohol of the pentose or hexose type b~ added to the drug preperation according to the in~ention. For this alcohol, mannitol or sorbitol is preferred. Such sugar alcohols are, in general, employed in an amount of 5 to 15 times, prefera-bly about 10 times, the weight of active ingredient.
Since the glycoside hydrolase inhibitors of the amino sugar type are hygroscopic, and the moisture content of the preparation has an effect on the stability~ in particular the storage stability, of the preparation9 care should be taken that the moisture content is not above 6o by weight, preferably not above 5O by weight, of the preparation.
The absolute amount by weight of the active ingredient contained in the preparation according to the invention depends on the desired therapy. In general, this abso-lute amount by weight is 100 mg per sinyle dose.
The Examples which follow illustrate very particularlypreferred drug preparations according to the present invention.
Example 1 100 kg of acarbose were mixed with 108.5 kg of dried starch, 45 kg of microcrystalline cellulose, 0.5 kg of colloidal silicon dioxide and 0.5 kg of magnesium stear-ate and this mixture was dry compressed. After the com-pressed materialhad been broken up and sieved~ the granu-lar powder obtained was mixed with 15 kg of microcrys-talline cellulose and 0.5 kg of magnesium stearate and then compressed to tablets, each of 0.27 9, or filled into capsules.
Le A 21 279 Example 2 100 k~ of acarbose with 94 kg of corn starch and 40 kg of microcrystalline cellulose were granulated in a flui-dised bed granulator by continuous spraying of waterand simultaneous introduction oF hot air. The product temperature was not allowed to fall below about 70C
during this granulation. The granular powder thus obtai-ned was sieved and, after mixing with 15 kg of microcrys-talline cellulose and 1 kg of magnesium stearate, wascompressed to tablets of 0.25 9.
Example 3 10 kg of acarbose were mixed with 70 kg of granulated or spray-dried mannitol, 19.9 kg of sorbitol and 0.1 kg of silicon dioxide and then filled into moisture-tight aluminium sachets each containing 1 9. The content of a sachet could be dissolved in water and taken.
Example 4 100 kg of acarbose with 43.5 kg of corn starch and 82 kg of microcrystalline cellulose were granulated in a fluidised bed granulator by continuously spraying in an aqueous snlution of 8 kg of polyvinylpyrrolidone (content of PVP: about 126 by weight) and s~imultaneous introduc-tion of hot air. The product temperature was not allowed to fall below about 70C during this granulation. The granular powder thus obtained was sieved and mixed with 15 kg of dried corn starch, 0.5 kq of cellulose and 1 kg of magnesium stearate and filled into capsules.
Le A 21 279
According to the present invention we provide a drug preparation comprising at least one glycoside hydrolase inhibitor of the amino sugar type as active ingredient and s-tarch, and at least one additive selected from magnesium stearate, calcium stearate, stearic acid and talc, wherein the additive is present in an amount of 0.1 to 3% b~ weight relative to the weight of active ingredient and the relationship between -the amount by weight of active ingredient and the total amount by weight of the other additive(s) including starch is 1:1 to 1:25, -the moisture content of the preparation not being above 6% by weigh-t of the preparation. The drug preparation according to the present invention also optionally comprises a further additive or additives.
Particularly suitable glycoside hydrolase inhibitors, which can be used within the scope of the present invention, are acarbose and inhibitors related to acarbose. Such inhibitors are described, for example, in sritish patent no. 1,482,543, British patent no. 2,011,397 and in DE~OS (German published specification) 2,903,710.
The preparations according to the invention are particularly suitable for the preparation of tablets (see Examples 1 and 2) and for the preparation of granular powders (see Example 3); the granular powders being, if desired, encapsulated ~see Example 4). The further additives which are optionall~
included depend on the form chosen as suitable for the final L
administration and preferably include at least one su~stance chosen from silicate polyvinylpyrrolidone, sugar alcohol and cellulose.
In the drug preparations according to the invention, the relationship between the amount by weight of active ingredient and the total amount by weight of the other additives including the starch is generally 1:1 to 1:25 preferably 1:2.5 to 1:10.
- la -8~
In addition, the preparations according to the invention contain starch. This starch can be added in the form of potato starch, corn starch, wheat starch or rice starch. This starch, which is preferably dried, is generally added in an amount which is 1 to 10 -times the weight of active ingredient.
The magnesium stearate, calcium stearate, stearic acid and/or talc contained in the preparation is generally employed in an amount of 0~1 to 3O~ preferably 0.5 to 1. 5~o and particularly 1o by weight relative to the weight of active ingredien-t.
If the preparation according to the invention is proces-sed to a granular powder by the dry granulation procedure, the addition of cellulose is recommended as a further additive. This can be added in powder form. Microcry-stalline cellulose is particularly preferred. The amount of cellulose employed is generally 0.2 to 1.5 times the weight of active ingredient contained in the preparation.
In addition, when dry granulation is used, it is advan-tageous to employ a silicate, preferably silicon dioxide as a further additive. In this context, colloidal sili-con dioxide is very particularly preferably used. Theamount of silicate is generally 0.5 to 1.5,O,preferably lio~ by weight relative to the weight oF active ingredient.
On processing the preparation according to the inven-tion to a granular powder by the fluidised bed granulation 30 procedure, it is advantageous to employ polyvinylpyrroli-done, as a further additive. This PVP has, in general, a molecular weight From about 15~000 to about 60,000, PVP with a molecular weight from 20,000 to 30~000 is preferred.
Le A 21 279 7~
If it is desired to prepare a granular powder which dissolves rapidly in water, it is recommended that at leas-t one sugar alcohol of the pentose or hexose type b~ added to the drug preperation according to the in~ention. For this alcohol, mannitol or sorbitol is preferred. Such sugar alcohols are, in general, employed in an amount of 5 to 15 times, prefera-bly about 10 times, the weight of active ingredient.
Since the glycoside hydrolase inhibitors of the amino sugar type are hygroscopic, and the moisture content of the preparation has an effect on the stability~ in particular the storage stability, of the preparation9 care should be taken that the moisture content is not above 6o by weight, preferably not above 5O by weight, of the preparation.
The absolute amount by weight of the active ingredient contained in the preparation according to the invention depends on the desired therapy. In general, this abso-lute amount by weight is 100 mg per sinyle dose.
The Examples which follow illustrate very particularlypreferred drug preparations according to the present invention.
Example 1 100 kg of acarbose were mixed with 108.5 kg of dried starch, 45 kg of microcrystalline cellulose, 0.5 kg of colloidal silicon dioxide and 0.5 kg of magnesium stear-ate and this mixture was dry compressed. After the com-pressed materialhad been broken up and sieved~ the granu-lar powder obtained was mixed with 15 kg of microcrys-talline cellulose and 0.5 kg of magnesium stearate and then compressed to tablets, each of 0.27 9, or filled into capsules.
Le A 21 279 Example 2 100 k~ of acarbose with 94 kg of corn starch and 40 kg of microcrystalline cellulose were granulated in a flui-dised bed granulator by continuous spraying of waterand simultaneous introduction oF hot air. The product temperature was not allowed to fall below about 70C
during this granulation. The granular powder thus obtai-ned was sieved and, after mixing with 15 kg of microcrys-talline cellulose and 1 kg of magnesium stearate, wascompressed to tablets of 0.25 9.
Example 3 10 kg of acarbose were mixed with 70 kg of granulated or spray-dried mannitol, 19.9 kg of sorbitol and 0.1 kg of silicon dioxide and then filled into moisture-tight aluminium sachets each containing 1 9. The content of a sachet could be dissolved in water and taken.
Example 4 100 kg of acarbose with 43.5 kg of corn starch and 82 kg of microcrystalline cellulose were granulated in a fluidised bed granulator by continuously spraying in an aqueous snlution of 8 kg of polyvinylpyrrolidone (content of PVP: about 126 by weight) and s~imultaneous introduc-tion of hot air. The product temperature was not allowed to fall below about 70C during this granulation. The granular powder thus obtained was sieved and mixed with 15 kg of dried corn starch, 0.5 kq of cellulose and 1 kg of magnesium stearate and filled into capsules.
Le A 21 279
Claims (9)
PROPERTY OR PRIVILEGE IS CLAIMED ARE DEFINED AS FOLLOWS:
1. A drug preparation comprising at least one glycoside hydrolase inhibitor of the amino sugar type as active ingredient and starch, and at least one additive selected from magnesium stearate, calcium stearate, stearic acid or talc where the additive(s) is present in an amount of 0.1 to 3% by weight relative to the weight of active ingredient, the relationship between the amount by weight of active ingredient and the total amount by weight of the other additive(s) including starch is 1:1 to 1:25, the moisture content of the preparation not being above 6% by weight of the preparation.
2. A drug preparation according to claim 1, additionally comprising as a further additive or additives at least one substance selected from silicate, polyvinylpyrrolidone, sugar alcohol and cellulose.
3. A drug preparation according to claim 2, in which the relationship between the amount by weight of active ingredient and the total amount by weight of the other additives including starch is 1:1 to 1:25.
4. A drug preparation according to claim 1 or 2, in which the relationship between the amount by weight of active ingredient and the total amount by weight of the other additives including starch is 1:2.5 to 1:10.
5. A drug preparation according to claim 2 or 3, in which cellulose is present as a further additive, in an amount of 0.2 to 1.5 times the weight of active ingredient.
6. A drug preparation according to claim 2 or 3, in which silicate is present as a further additive, in an amount of 0.5 to 1.5% by weight relative to the weight of active ingredient.
7. A drug preparation according to claim 2 or 3 in which sugar alcohol is present as a further additive, in an amount of 5 to 15 times the weight of active ingredient.
8. A drug preparation according to claim 1 or 2 in which the content of water is not greater than 5% by weight of the preparation.
9. A drug preparation according to claim 1 or 2 in the form of tablets or of a granular powder.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19813134591 DE3134591A1 (en) | 1981-09-01 | 1981-09-01 | NEW MEDICINE PREPARATIONS FOR GLYCOSIDE HYDROLASE INHIBITORS |
| DEP3134591.3 | 1981-09-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1199871A true CA1199871A (en) | 1986-01-28 |
Family
ID=6140604
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA000410394A Expired CA1199871A (en) | 1981-09-01 | 1982-08-30 | Drug preparations for glycoside hydrolase inhibitors |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP0073428B1 (en) |
| JP (1) | JPH0739340B2 (en) |
| AT (1) | ATE23438T1 (en) |
| CA (1) | CA1199871A (en) |
| DE (2) | DE3134591A1 (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5851550A (en) * | 1991-05-08 | 1998-12-22 | Smithkline Beecham P.L.C. | Pharmaceutical formulations of compacted granulates of β-Lactam antibiotics |
| US6110497A (en) * | 1991-05-08 | 2000-08-29 | Laboratorios Beecham Sa | Pharmaceutical formulations |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0281200B1 (en) * | 1987-03-02 | 1994-01-19 | Yamanouchi Europe B.V. | Pharmaceutical composition, pharmaceutical granulate and process for their preparation |
| US5211958A (en) * | 1987-11-30 | 1993-05-18 | Gist-Brocades, N.V. | Pharmaceutical composition and process for its preparation |
| JPH10182687A (en) * | 1996-10-21 | 1998-07-07 | Bayer Yakuhin Kk | Stabilization of storage of acarbose |
| JP2001523704A (en) * | 1997-11-25 | 2001-11-27 | バイエル・アクチエンゲゼルシヤフト | Sustained release formulation comprising an α-glucosidase inhibitor |
| MX348865B (en) * | 2010-04-27 | 2017-07-03 | Bayer Ip Gmbh | Orally disintegrating tablet containing acarbose. |
| TR201100148A2 (en) * | 2011-01-06 | 2012-07-23 | Bi̇lgi̇ç Mahmut | Stable acarbose formulations. |
| CN108904462A (en) | 2013-03-15 | 2018-11-30 | 布伦特里实验室公司 | Dual purpose sulfate combination of oral medication tablet and its application method |
| CN116650430A (en) * | 2023-07-18 | 2023-08-29 | 浙江乐普制药有限公司 | Acarbose tablet and preparation method thereof |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3995026A (en) * | 1972-03-01 | 1976-11-30 | Bayer Aktiengesellschaft | Amylase inhibitor |
| DE2347782C3 (en) * | 1973-09-22 | 1979-10-11 | Bayer Ag, 5090 Leverkusen | Amino sugar derivatives, processes for their preparation and medicaments containing these compounds |
| DE2413720C3 (en) * | 1974-03-21 | 1980-03-27 | Bayer Ag, 5090 Leverkusen | Animal feed |
| FR2338707A1 (en) * | 1976-01-22 | 1977-08-19 | Rhone Poulenc Ind | NEW GLYCO-HYDROLASE INHIBITOR AND ITS PREPARATION BY CULTURE OF A STREPTOMYCES |
| JPS5953920B2 (en) * | 1977-12-28 | 1984-12-27 | 東洋醸造株式会社 | Novel amino sugar compound and its production method |
| GB2016497A (en) * | 1978-02-10 | 1979-09-26 | Taisho Pharmaceutical Co Ltd | Microbiological production of amylase inhibitor |
| JPS54106403A (en) * | 1978-02-10 | 1979-08-21 | Taisho Pharmaceut Co Ltd | Amylase inhibitor tai-b |
| JPS54106402A (en) * | 1978-02-10 | 1979-08-21 | Taisho Pharmaceut Co Ltd | Amylase inhibitor tai-a |
-
1981
- 1981-09-01 DE DE19813134591 patent/DE3134591A1/en not_active Withdrawn
-
1982
- 1982-08-20 AT AT82107609T patent/ATE23438T1/en not_active IP Right Cessation
- 1982-08-20 DE DE8282107609T patent/DE3274185D1/en not_active Expired
- 1982-08-20 EP EP82107609A patent/EP0073428B1/en not_active Expired
- 1982-08-30 CA CA000410394A patent/CA1199871A/en not_active Expired
- 1982-09-01 JP JP57150818A patent/JPH0739340B2/en not_active Expired - Lifetime
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5851550A (en) * | 1991-05-08 | 1998-12-22 | Smithkline Beecham P.L.C. | Pharmaceutical formulations of compacted granulates of β-Lactam antibiotics |
| US5861172A (en) * | 1991-05-08 | 1999-01-19 | Laboratorios Beecham Sa | Pharmaceutical formulations of compacted granulates of β-lactam antibiotics |
| US6110497A (en) * | 1991-05-08 | 2000-08-29 | Laboratorios Beecham Sa | Pharmaceutical formulations |
| US6352720B1 (en) | 1991-05-08 | 2002-03-05 | Laboratorios Beecham Sa | Pharmaceutical formulations comprised of compacted amoxicillin granulates |
Also Published As
| Publication number | Publication date |
|---|---|
| JPS5846013A (en) | 1983-03-17 |
| EP0073428A2 (en) | 1983-03-09 |
| ATE23438T1 (en) | 1986-11-15 |
| DE3134591A1 (en) | 1983-03-10 |
| EP0073428B1 (en) | 1986-11-12 |
| DE3274185D1 (en) | 1987-01-02 |
| EP0073428A3 (en) | 1983-08-24 |
| JPH0739340B2 (en) | 1995-05-01 |
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