CA1079637A - Cephalosporine tablets - Google Patents
Cephalosporine tabletsInfo
- Publication number
- CA1079637A CA1079637A CA262,741A CA262741A CA1079637A CA 1079637 A CA1079637 A CA 1079637A CA 262741 A CA262741 A CA 262741A CA 1079637 A CA1079637 A CA 1079637A
- Authority
- CA
- Canada
- Prior art keywords
- weight
- tablet according
- tablet
- orally active
- disintegrant
- 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
Classifications
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
-
- 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
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Medicinal Preparation (AREA)
- Cephalosporin Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
ABSTRACT
A small tablet containing over 90% by weight of an orally active cephalosporin such cephalexin and which utilises as a binder polyvinyl pyrrolidone having a number average molecular weight of from 500,000 to 1,500,000.
A small tablet containing over 90% by weight of an orally active cephalosporin such cephalexin and which utilises as a binder polyvinyl pyrrolidone having a number average molecular weight of from 500,000 to 1,500,000.
Description
107963~
This inventi~n relates to pharmaceu~ical formulations, m~re particularly ~¦to tablets containing an orally active cephalosporin such as cephalexin or cephradine.
Both cephalexin (7-(0--amino-phenylacetamido)-3-methyl-3-cephem_4_ carboxylic acid) and cephradine (7-[~-a-amino-(1,4-cyclohexadienyl)_ acetamido]-3-methyl-3-cephem-4-carboxylic acid) are excellent broad spectrum antibiotics having low toxicity. However, for effective chemotherapy of bacterial infections in humans it has been found that quite high dosages are needed. Conseguentially, heretofore, administration of these cephalospor ms has necessarily taken the form of either rather large tablets or numerous small tablets. Both of these forms of administlation have undesirable face.s so far as patient acceptability, partic~larly in children and the elderly, is concerned. Thus, there has long been a need for smaller tablets containing adequate amounts of active ingredient.
Accordingly, the present invention provides a tablet which comprises :
!j (a) greate~ than 90~/, by weight of an orally active cephalosporin;
(b) less than 107. by weight of excipients which comprise:
(i) from 2 to 5% by weight of a binder which is polyvinyl ¦ pyrrolidone having a number average molecular weight of ¦ from 500,000 to 1,500,000;
l (ii) from 1.5 to 5Z by weight of a disintegrant; and ¦ (iii) from 0.3 to 2% by weight of a lubricant, ¦and which has (c) a diametral crushing strength of from 5.0 to 15.0 Kg.; and ~(d) will disintegrate in distilled water within 15 minutes at 37 C.
¦ Preferably, the excipients will comprise from 2 to 4% by weight of binder, Ifrom 1.5 to 4% by weight of disintegrant and from 0.3 to 2L by weight of lubri-icant.
The tablet will contain approximately from 9~ to 96%, preferably from 92 to 95%, a~d most preferably from 93 to 95%, by weight of the orally active cephalo- i f ' ~ff ~1 '.
10~79637 .` ':' sporin. The pree~red cephalosporin is cephalexin, which is particularly useful in the practice o~ the in~ention when it iS in the ~orm of its monPhydrate. ~ ;~
The use of polyvinyl pyrrolidone having a number average molecular weight of from 500,000 to 1,000,000, and ideally approximately 700,000, as determined by viscosity measurements, as the binder is much preferred.
The disintegrant is preferably a sodium starch glycolate containing from 15 to 35, most preferably about 25, carboxymethyl groups per 100 glucose units, although other disintegrants such as ion exchange resins of the type known by the trade mark "Amberlite IRP 88*", or sodium carboxymethylcellulose may be used.
Similarly, although ~he use of magnesium stearate as the lubricant is preferred, other lubricants such as stearic acid or calcium stearate can Also be used.
Physicians commonly administer orally active cephalosporins in the form of tablets containing approximately 250, 500 or 1000 mg. of the active ingredient. Accordingly, in three further aspects of the invention there are provided:
(A) a tablet which contains approximately 250 mg. of an orally active cepha-losporin, and which has a volume of from 0.20 to 0.23 ml, when determined by displacement of liquid paraffin;
(B~ a tablet which contains approximately 500 mg. of an orally active cepha-losporin, and which has a volume of from 0.40 - 0.47 ml., when tetermined by displacement of liquid paraffin; and (C) a tablet which contains approximately 1000 mg. of an orally active cepha-losporin, and which has a volume of from 0.80 to 0.95 ml., when determined by displacement of liquid paraffin.
The tablets of the invention may also comprise small amounts of other commonly used excipients, for instance they may be coloured by the use of suitable dyes or lakes.
* Trademark of Rohm and Haas Company for a weakly acidic, fine particle size, synthetic cation exchange resin, formed of a methacrylic acid-divlnylbenzene copolymer.
¦ In addition, if desired, the tablets of the invention may be coated ~lusing a polymer coating agent which is, for example, a cellulose derivative ¦Isuch as hydroxypropyl cellulose, hydroxypropylmethyl cellulose or methyl ¦ cellulose.
The tablets of the invention can be prepared by dissolving or dispersing the binder in water or a suitable organic sol~ent and using this solution ~ r or dispersion to mass and subsequently granulate the cephalosporin. The granules are then passed through a sieve of suitable mesh size and dried.
After resieving to break up any agglomerates the dried granules are combined with the lubricant and disintegrant and compressed into tablets using a conventional tabletting machine. If it is desired to produce coloured ; tablets, a dye may be added to the solution or dispersion of binder, or a lake to the dried powder blend prior to compression. Coating of the tablets may be carried out subsequent to compression using appropriate coating ~equipment.
. I ~ .
! To further illustrate the invention and to show how the same may be ¦ carried into effect, reference will now be made to the following non- ! :
¦l~limitative examples. I ;~
Il l O
¦1 -4- !
1,, 1 i1' ~
10~79637 E~l'L~ 1 This is an example of a conventional tablet containing ceph~lexin, 1'1 ingredients were : ~~
Cephalexin monohydrate~: 1000 ~ -~Primiel t -Pregelatinised Starch 70 Flowable Starch 55,7 Magnesium Stearate 14.8 Stearic Acid 29.6 Starch dried q.s. 1480 ~ ~as determined by iodometric assay : t trademask 'PrimDjel' is the trade mark for a sodium starch glycolate containing approximately 25 carboxymethyl units per 100 glucose units.
The above in~redients were formulated into a tablet using conventional procedure.
¦ Although the tablet prepared from the above ingredients was satisfactory, ¦its volume was 1.15 ml. (as measured by displacement of liquid paraffin~.
This is an example of a tablet of the in~ention.
m~.
Cephalexin monohydrate~- 1000 -'Kollidon go' t 24 'Primojel' t 20 Magnesium Stearate 6 Total 1050 ~as determined by lodometric assay t trademar~
_5_ ll l ' I 1079637 i The 'Kollidon 90', which is a polyvinyl pyrrolidone having a number averag~
molecular weight of approximately 700,000, as determined by viscosity measure- .
ments,was dissolved in water and then massed with the cephalexin monohydrate so as to form a granular material. After sieving, this material was dried and 1 then resieved. The resieved mixture was then combined and intimately admixed ¦ with the 'Primojel' and magnesium s~earate and compressed into a tablet.
The volume of the tablet, when measured by displacement of liquid paraffin, ~ was 0.87 ml. It will be immediately appreciated that this is significantly less than the volume of the conventional tablet of Example 1.
The diametral crushing strength of this tablet, which is of course a ~measure of the hardness of the tablet, was measured using an Erweka tester ¦type TBT (E~weka Apparatebau Gmbh., Frankfurt am Main, W. Germany) and was -¦found to be 12 Kg., a quite satisfactory hardness. In addition, the disinte-Igration time of this tablet was determined using the method described in the l ~1 IBritish Pharmacopoeia 1973 Appendix XIX A, pages A 131/', i.e. in distilled ~Iwater at 37 C. + 2 C. and was found to be 4 minutes, a good disintegration time.
.~ . .- .
l~ XAMPLES 3 AND 4 l~ Using the procedure of Example 2, there were prepared tablets containing 0 ~ the ingredients listed below.
mg.
¦ Cephalexin monohydrate~: 500 'Primojel' t 14 l 'Kollidon 90' t 15 5 j, Magnesium Stearate 6 I Total 5__ ¦
. I
Volume 0.43 ml.
IDiametral Crushing Strength 11 Kg.
¦Disintegration Time 5 minutes.
i '., 1, 1 ¦ m~.
Cephalexin monohydrate~: 250 'Primojel' t 8 I 'Kollidon 90' t 8 Magnesium Stearate 4 ., I =_=
. ` :~
~ras determined by iodometric assay f trademark Volume 0.23 ml.
Diametral Crushing Strength 10 Kg.
Disintegration Time 6 minutes.
Similarly, using the method described in Example 2, the following ~5 further tablets were prepared.
:' 1 Cephalexin monohydrate~r 1000 'Kollidon 90' t 20 ll ~Primojel~ t 15 Magnesium Stearate 3 10=38 , ~:as determined by iodometric assay I t trademark ¦Volume 0.856 ml.
¦Diametral Crushing Strength 10.5 Kg.
IDisintegration Time 3 minutes, .
, _7_ l l ~, 1 1079637 m~.
l ! Cephalexin monohydrate~ 1000 ,~ ¦ 'Kollidon 90 t 20 ::
~:5 'Amberlite IRP 88' t 15 Magnesium Stearate 3 ~ 1=3=
- _ ~ as determined by iodometric assay ::
t trademark ~:
- L0 Volume 0.849 ml.
Diametral Crushing Strength 14.2 Kg. :-Disintegration Time 5 minutes.
mg. ~ :
Cephalexin monohydrate~- 1000 ::
'Kollidon 90' t 25 'Primojel' t 20 Stearic Acid 7 j 105=2 f ~as determined by iodometric assay ¦ t trademark Volume 0.872 ml. -Diametral Crushing Strength 14 Kg.
Disinteg l~ion Time 13 =inutes.
f:
I
!
. ! -8-l! , ' L ~ EXAMPLE 8 ',¦ mg. ¦
Cephalexin mon~hydrate~.: 1000 l¦ 'Kollidon 90' t 20 5 ~ 'Primojel' t 15 , Stearic acid 7 ¦~
F.D. & C. Yellow No. 6 Aluminium Lake 10 _ 1052 ~' ~as determined by iodometric assay ~ trademark '' ¦Volume 0.910 ml. ~,' Diametral Crushing Strength 10 Kg.
I Disintegration Time 2 minutes ¦ The F.D. & C. Yellow No. 6 hluminium Lake used in Example 8 was ~I combined with the 'Primoiel' and the stearic acid and then mixed with Il ce'phalexin granules formed as in Example 2. The mixture thus formed was then compressed Into ~ tatlet.
_9_ 1 1, 1`
This inventi~n relates to pharmaceu~ical formulations, m~re particularly ~¦to tablets containing an orally active cephalosporin such as cephalexin or cephradine.
Both cephalexin (7-(0--amino-phenylacetamido)-3-methyl-3-cephem_4_ carboxylic acid) and cephradine (7-[~-a-amino-(1,4-cyclohexadienyl)_ acetamido]-3-methyl-3-cephem-4-carboxylic acid) are excellent broad spectrum antibiotics having low toxicity. However, for effective chemotherapy of bacterial infections in humans it has been found that quite high dosages are needed. Conseguentially, heretofore, administration of these cephalospor ms has necessarily taken the form of either rather large tablets or numerous small tablets. Both of these forms of administlation have undesirable face.s so far as patient acceptability, partic~larly in children and the elderly, is concerned. Thus, there has long been a need for smaller tablets containing adequate amounts of active ingredient.
Accordingly, the present invention provides a tablet which comprises :
!j (a) greate~ than 90~/, by weight of an orally active cephalosporin;
(b) less than 107. by weight of excipients which comprise:
(i) from 2 to 5% by weight of a binder which is polyvinyl ¦ pyrrolidone having a number average molecular weight of ¦ from 500,000 to 1,500,000;
l (ii) from 1.5 to 5Z by weight of a disintegrant; and ¦ (iii) from 0.3 to 2% by weight of a lubricant, ¦and which has (c) a diametral crushing strength of from 5.0 to 15.0 Kg.; and ~(d) will disintegrate in distilled water within 15 minutes at 37 C.
¦ Preferably, the excipients will comprise from 2 to 4% by weight of binder, Ifrom 1.5 to 4% by weight of disintegrant and from 0.3 to 2L by weight of lubri-icant.
The tablet will contain approximately from 9~ to 96%, preferably from 92 to 95%, a~d most preferably from 93 to 95%, by weight of the orally active cephalo- i f ' ~ff ~1 '.
10~79637 .` ':' sporin. The pree~red cephalosporin is cephalexin, which is particularly useful in the practice o~ the in~ention when it iS in the ~orm of its monPhydrate. ~ ;~
The use of polyvinyl pyrrolidone having a number average molecular weight of from 500,000 to 1,000,000, and ideally approximately 700,000, as determined by viscosity measurements, as the binder is much preferred.
The disintegrant is preferably a sodium starch glycolate containing from 15 to 35, most preferably about 25, carboxymethyl groups per 100 glucose units, although other disintegrants such as ion exchange resins of the type known by the trade mark "Amberlite IRP 88*", or sodium carboxymethylcellulose may be used.
Similarly, although ~he use of magnesium stearate as the lubricant is preferred, other lubricants such as stearic acid or calcium stearate can Also be used.
Physicians commonly administer orally active cephalosporins in the form of tablets containing approximately 250, 500 or 1000 mg. of the active ingredient. Accordingly, in three further aspects of the invention there are provided:
(A) a tablet which contains approximately 250 mg. of an orally active cepha-losporin, and which has a volume of from 0.20 to 0.23 ml, when determined by displacement of liquid paraffin;
(B~ a tablet which contains approximately 500 mg. of an orally active cepha-losporin, and which has a volume of from 0.40 - 0.47 ml., when tetermined by displacement of liquid paraffin; and (C) a tablet which contains approximately 1000 mg. of an orally active cepha-losporin, and which has a volume of from 0.80 to 0.95 ml., when determined by displacement of liquid paraffin.
The tablets of the invention may also comprise small amounts of other commonly used excipients, for instance they may be coloured by the use of suitable dyes or lakes.
* Trademark of Rohm and Haas Company for a weakly acidic, fine particle size, synthetic cation exchange resin, formed of a methacrylic acid-divlnylbenzene copolymer.
¦ In addition, if desired, the tablets of the invention may be coated ~lusing a polymer coating agent which is, for example, a cellulose derivative ¦Isuch as hydroxypropyl cellulose, hydroxypropylmethyl cellulose or methyl ¦ cellulose.
The tablets of the invention can be prepared by dissolving or dispersing the binder in water or a suitable organic sol~ent and using this solution ~ r or dispersion to mass and subsequently granulate the cephalosporin. The granules are then passed through a sieve of suitable mesh size and dried.
After resieving to break up any agglomerates the dried granules are combined with the lubricant and disintegrant and compressed into tablets using a conventional tabletting machine. If it is desired to produce coloured ; tablets, a dye may be added to the solution or dispersion of binder, or a lake to the dried powder blend prior to compression. Coating of the tablets may be carried out subsequent to compression using appropriate coating ~equipment.
. I ~ .
! To further illustrate the invention and to show how the same may be ¦ carried into effect, reference will now be made to the following non- ! :
¦l~limitative examples. I ;~
Il l O
¦1 -4- !
1,, 1 i1' ~
10~79637 E~l'L~ 1 This is an example of a conventional tablet containing ceph~lexin, 1'1 ingredients were : ~~
Cephalexin monohydrate~: 1000 ~ -~Primiel t -Pregelatinised Starch 70 Flowable Starch 55,7 Magnesium Stearate 14.8 Stearic Acid 29.6 Starch dried q.s. 1480 ~ ~as determined by iodometric assay : t trademask 'PrimDjel' is the trade mark for a sodium starch glycolate containing approximately 25 carboxymethyl units per 100 glucose units.
The above in~redients were formulated into a tablet using conventional procedure.
¦ Although the tablet prepared from the above ingredients was satisfactory, ¦its volume was 1.15 ml. (as measured by displacement of liquid paraffin~.
This is an example of a tablet of the in~ention.
m~.
Cephalexin monohydrate~- 1000 -'Kollidon go' t 24 'Primojel' t 20 Magnesium Stearate 6 Total 1050 ~as determined by lodometric assay t trademar~
_5_ ll l ' I 1079637 i The 'Kollidon 90', which is a polyvinyl pyrrolidone having a number averag~
molecular weight of approximately 700,000, as determined by viscosity measure- .
ments,was dissolved in water and then massed with the cephalexin monohydrate so as to form a granular material. After sieving, this material was dried and 1 then resieved. The resieved mixture was then combined and intimately admixed ¦ with the 'Primojel' and magnesium s~earate and compressed into a tablet.
The volume of the tablet, when measured by displacement of liquid paraffin, ~ was 0.87 ml. It will be immediately appreciated that this is significantly less than the volume of the conventional tablet of Example 1.
The diametral crushing strength of this tablet, which is of course a ~measure of the hardness of the tablet, was measured using an Erweka tester ¦type TBT (E~weka Apparatebau Gmbh., Frankfurt am Main, W. Germany) and was -¦found to be 12 Kg., a quite satisfactory hardness. In addition, the disinte-Igration time of this tablet was determined using the method described in the l ~1 IBritish Pharmacopoeia 1973 Appendix XIX A, pages A 131/', i.e. in distilled ~Iwater at 37 C. + 2 C. and was found to be 4 minutes, a good disintegration time.
.~ . .- .
l~ XAMPLES 3 AND 4 l~ Using the procedure of Example 2, there were prepared tablets containing 0 ~ the ingredients listed below.
mg.
¦ Cephalexin monohydrate~: 500 'Primojel' t 14 l 'Kollidon 90' t 15 5 j, Magnesium Stearate 6 I Total 5__ ¦
. I
Volume 0.43 ml.
IDiametral Crushing Strength 11 Kg.
¦Disintegration Time 5 minutes.
i '., 1, 1 ¦ m~.
Cephalexin monohydrate~: 250 'Primojel' t 8 I 'Kollidon 90' t 8 Magnesium Stearate 4 ., I =_=
. ` :~
~ras determined by iodometric assay f trademark Volume 0.23 ml.
Diametral Crushing Strength 10 Kg.
Disintegration Time 6 minutes.
Similarly, using the method described in Example 2, the following ~5 further tablets were prepared.
:' 1 Cephalexin monohydrate~r 1000 'Kollidon 90' t 20 ll ~Primojel~ t 15 Magnesium Stearate 3 10=38 , ~:as determined by iodometric assay I t trademark ¦Volume 0.856 ml.
¦Diametral Crushing Strength 10.5 Kg.
IDisintegration Time 3 minutes, .
, _7_ l l ~, 1 1079637 m~.
l ! Cephalexin monohydrate~ 1000 ,~ ¦ 'Kollidon 90 t 20 ::
~:5 'Amberlite IRP 88' t 15 Magnesium Stearate 3 ~ 1=3=
- _ ~ as determined by iodometric assay ::
t trademark ~:
- L0 Volume 0.849 ml.
Diametral Crushing Strength 14.2 Kg. :-Disintegration Time 5 minutes.
mg. ~ :
Cephalexin monohydrate~- 1000 ::
'Kollidon 90' t 25 'Primojel' t 20 Stearic Acid 7 j 105=2 f ~as determined by iodometric assay ¦ t trademark Volume 0.872 ml. -Diametral Crushing Strength 14 Kg.
Disinteg l~ion Time 13 =inutes.
f:
I
!
. ! -8-l! , ' L ~ EXAMPLE 8 ',¦ mg. ¦
Cephalexin mon~hydrate~.: 1000 l¦ 'Kollidon 90' t 20 5 ~ 'Primojel' t 15 , Stearic acid 7 ¦~
F.D. & C. Yellow No. 6 Aluminium Lake 10 _ 1052 ~' ~as determined by iodometric assay ~ trademark '' ¦Volume 0.910 ml. ~,' Diametral Crushing Strength 10 Kg.
I Disintegration Time 2 minutes ¦ The F.D. & C. Yellow No. 6 hluminium Lake used in Example 8 was ~I combined with the 'Primoiel' and the stearic acid and then mixed with Il ce'phalexin granules formed as in Example 2. The mixture thus formed was then compressed Into ~ tatlet.
_9_ 1 1, 1`
Claims (7)
- CLAIM:
l. A tablet which comprises :
(a) greater than 90% by weight of an orally active cephalosporin;
(b) less than 10% by weight of excipients which comprise:
(i) from 2 to 5% by weight of a binder which is polyvinyl pyrrolidone having a number average molecular weight of from 500,000 to 1,500,000;
(ii) from 1.5 to 5% by weight of a disintegrant; and (iii) from 0.3 to 2% by weight of a lubricant, and which has (c) a diametral crushing strength of from 5.0 to 15.0 Kg; and (d) will disintegrate in distilled water within 15 minutes at 37°C. - 2. A tablet according to claim 1 wherein the orally active cephalosporin is 7-(D-.alpha.-amino-phenylacetamido)-3-methyl-3-cephem-4-carboxylic acid, monohydrate.
- 3. A tablet according to claim 1 wherein the polyvinyl pyrrolidone has a number average molecular weight of from 500,000 to 1,000,000.
- 4. A tablet according to any one of claims 1-3, wherein the disintegrant is a sodium starch glycolate containing from 15 to 35, carboxymethyl groups per 100 glucose units.
- 5. A tablet according to any one of claims 1-3, which contains approximately 1000 mg. of an orally active cephalosporin and which has a volume of from 0.80 to 0.95 ml., when determined by displacement of liquid paraffin.
- 6. A tablet according to any one of claims 1-3, wherein the lubricant is magnesium stearate.
- 7. A tablet according to any one of claims 1-3, and containing from 92% to 95% by weight of the orally active cephalosporin, from 2% to 4% by weight of said polyvinyl pyrrolidone binder, and from 1.5% to 4% by weight of the disintegrant.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB41744/75A GB1560475A (en) | 1975-10-11 | 1975-10-11 | Pharmaceutical formulation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA1079637A true CA1079637A (en) | 1980-06-17 |
Family
ID=10421183
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA262,741A Expired CA1079637A (en) | 1975-10-11 | 1976-10-05 | Cephalosporine tablets |
Country Status (6)
| Country | Link |
|---|---|
| JP (1) | JPS5247914A (en) |
| AT (1) | AT348670B (en) |
| AU (1) | AU514174B2 (en) |
| CA (1) | CA1079637A (en) |
| DD (1) | DD126926A5 (en) |
| GB (1) | GB1560475A (en) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE13486T1 (en) * | 1980-11-12 | 1985-06-15 | Ciba Geigy Ag | RAPIDLY DISPERSING MEDICATION PRESSES. |
| JPS59155310A (en) * | 1983-02-21 | 1984-09-04 | Daicel Chem Ind Ltd | Production of solid medicinal preparation with improved disintegration |
| JPS59167522A (en) * | 1983-03-14 | 1984-09-21 | Daicel Chem Ind Ltd | Production of solid drug |
| JPS59176217A (en) * | 1983-03-28 | 1984-10-05 | Daicel Chem Ind Ltd | Powder composition for solid pharmaceutical preparation |
| JPS59193815A (en) * | 1983-04-15 | 1984-11-02 | Daicel Chem Ind Ltd | Preparation of tablet |
| JPS62173183A (en) * | 1986-01-25 | 1987-07-30 | マツダ株式会社 | Article mounting method to built-up carrying jig |
| US5837292A (en) * | 1996-07-03 | 1998-11-17 | Yamanouchi Europe B.V. | Granulate for the preparation of fast-disintegrating and fast-dissolving compositions containing a high amount of drug |
-
1975
- 1975-10-11 GB GB41744/75A patent/GB1560475A/en not_active Expired
-
1976
- 1976-09-30 AU AU18292/76A patent/AU514174B2/en not_active Expired
- 1976-10-05 CA CA262,741A patent/CA1079637A/en not_active Expired
- 1976-10-06 DD DD195197A patent/DD126926A5/xx unknown
- 1976-10-08 AT AT749476A patent/AT348670B/en not_active IP Right Cessation
- 1976-10-08 JP JP51121193A patent/JPS5247914A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| AU1829276A (en) | 1978-04-06 |
| AT348670B (en) | 1979-02-26 |
| JPS5247914A (en) | 1977-04-16 |
| ATA749476A (en) | 1978-07-15 |
| DD126926A5 (en) | 1977-08-24 |
| AU514174B2 (en) | 1981-01-29 |
| JPS619283B2 (en) | 1986-03-22 |
| GB1560475A (en) | 1980-02-06 |
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