AP747A - Pharmaceutical compositions in the form of a tablet containing famciclovir. - Google Patents

Pharmaceutical compositions in the form of a tablet containing famciclovir. Download PDF

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Publication number
AP747A
AP747A APAP/P/1997/000911A AP9700911A AP747A AP 747 A AP747 A AP 747A AP 9700911 A AP9700911 A AP 9700911A AP 747 A AP747 A AP 747A
Authority
AP
ARIPO
Prior art keywords
famciclovir
tablet
percentage
lactose
pharmaceutical
Prior art date
Application number
APAP/P/1997/000911A
Other versions
AP9700911A0 (en
Inventor
Michael John Greenway
Jennifer Mary Slater
Original Assignee
Novartis Int Pharmaceutical Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Novartis Int Pharmaceutical Ltd filed Critical Novartis Int Pharmaceutical Ltd
Publication of AP9700911A0 publication Critical patent/AP9700911A0/en
Application granted granted Critical
Publication of AP747A publication Critical patent/AP747A/en

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses

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)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

A pharmaceutical tablet wherein famciclovir is the active ingredient and wherein the percentage of famciclovir by weight in the tablet is 85% or greater.

Description

PHARMACEUTICAL COMPOSITIONS IN THE FORM OF A
TABLET CONTAINING FAMCICLOVIR
This invention relates to a novel formulation of a pharmaceutical 5 product.
EP-A-182024 (Beecham Group p.I.c.), Example 2 describes a method of the preparation of famciclovir, a compound which is useful as the oral form of the . compound, penciclovir which has antiviral activity against infections caused by herpesviruses, such as herpes simplex type 1, herpes simplex type 2 and varicella zoster virus, and also against Hepatitis B virus. Penciclovir and its antiviral activity is disclosed in Abstract Ρ.VI1-5 ρ. 193 of ’Abstracts of 14th Int. Congress of Microbiology’, Manchester, England 7-13 September 1986 (Boyd et. al.).
Famciclovir is preferably administered in the form of tablets containing 125 mg, 250 mg, 500 mg or 750 mg of active ingredient. As is conventional in tablet compositions, the tablets contain excipients such as lactose, sodium starch glycollate and magnesium stearate such that the total excipient content is at least 15%. Anhydrous lactose is conventionally included as a major excipient to compensate for any potential inconsistencies in the compression properties of the active ingredient.
The higher the percentage excipient content, the greater the tablet size for a tablet of any given dosage. Particularly in the case of tablets containing 500 mg and 750 mg of active ingredient, the large tablet size can affect patient compliance as the oval face of the tablet would measure 18mm x 8.5mm and 21mm x 10mm respectively when the tablet contains about 76% famciclovir.
It has been discovered that it is possible to formulate famciclovir into a tablet containing less than 15% excipients as the compression properties of famciclovir have proved to be sufficiently consistent to permit this.
Accordingly, the present invention provides a pharmaceutical tablet wherein famciclovir is the active ingredient and wherein the percentage of famciclovir by weight in the tablet is 85% or greater.
All values for percentage weight given herein unless otherwise stated are defined in terms of the core of any tablet which may be coated, for example, film coated.
AP/P/ 9 7 / 0 0 9 1 1
AP.00747
-2A suitable tablet contains less than 15%, less than 10%, less than 5% and preferably 0% of anhydrous lactose or other similar excipient such as microcrystalline cellulose.
A suitable tablet contains famciclovir at a percentage weight of greater than 5 85%, 86%, 87%, 88%, 89%, 90% or 91%. The highest possible percentage of famciclovir is preferred. Famciclovir may be in any suitable pharmaceutically acceptable form, such as in the form of a salt, solvate or polymorph. Famciclovir is preferably in an anhydrous, free base form.
Conventional excipients included in the composition of the tablet include 10 hydroxypropyl cellulose, for example up to 5% or up to 3%, sodium starch glycollate, for example up to 15%, 10%, 7% or 5% and magnesium stearate, for example up to 2% or 1%.
The tablets may be coated with any suitable coating used for pharmaceutical tablets.
The tablets may be prepared by conventional compression methods known in the art. In a preferred method, famciclovir is granulated with an excipient such as hydroxypropyl cellulose, in order to minimise the effect of any variations in physical form of the active ingredient. The granules are screened and dried and then blended with any further excipients to form a compression mix. Tablets are compressed to the size and weight appropriate to the required dosage and then optionally coated as desired.
The following Example illustrates the invention.
AP/P/ 9 7 / 0 0 9 1 1
AP . Ο Ο 7 4 7
- 3 EXAMPLE
The percentage values in brackets indicate the percentage values in the famciclovir tablets currently registered by the regulatory authorities for pharmaceuticals, in the
United Kingdom of Great Britain and Northern Ireland, the U.S.A and other countries of the world.
Constituent %w/w %w/w
Famciclovir 91.42 (75.66)
Hydroxypropyl cellulose 2.83 (2.34)
sodium starch glycollate 5.00 (5.00)
magnesium stearate 0.75 (0.75)
anhydrous lactose 0 (16.25)
Approximate Core Weight is 547mg for 500mg dosage and 820mg for 750mg dosage.
For coated tablets, 2.5% of core weight is added by the coating and the coated tablet weighs 560mg for the 500mg dosage and 840mg for the 750mg dosage,.
The tablets are prepared by dry mixing famciclovir with hydroxypropyl 20 cellulose and then granulating the mixture with water in a high shear granulator. The wet mass is screened, dried and milled. The milled granules are blended with sodium starch glycollate and magnesium stearate to produce the compression mix. Tablets are compressed at the size and weight appropriate to the required strength of tablet and then aqueous film coated.
The resulting size of an oval face of a 750mg tablet is 19mm x 9mm and of a 500mg tablet is 17mm x 8mm.

Claims (7)

1. A pharmaceutical tablet wherein famciclovir is the active ingredient and wherein the percentage of famciclovir by weight in the tablet is 85% or greater.
2. A pharmaceutical tablet according to claim 1, containing less than 15% lactose.
3. A pharmaceutical tablet according to claim 1 or 2, containing less than 5% 10 lactose.
4. A pharmaceutical tablet according to claim 1, 2, or 3, containing 0% lactose.
5. A pharmaceutical tablet according to claim 1, 2, 3, or 4, wherein the 15 percentage of famciclovir by weight in the tablet is 90% or greater.
6. A pharmaceutical tablet according to any one of claims 1 to 5, having the
following composition: Constituent %w/w Famciclovir 91.42 Hydroxypropyl cellulose 2.83 sodium starch glycollate 5.00 magnesium stearate 0.75 anhydrous lactose 0
V V 6 0 0 / Z 6 /d/dV
7. A process for the preparation of a tablet according to any one of claims 1 to 6, wherein the famciclovir and excipients are granulated and then compressed to form a tablet.
APAP/P/1997/000911A 1996-01-16 1997-01-02 Pharmaceutical compositions in the form of a tablet containing famciclovir. AP747A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB9600847.9A GB9600847D0 (en) 1996-01-16 1996-01-16 Pharmaceuticals

Publications (2)

Publication Number Publication Date
AP9700911A0 AP9700911A0 (en) 1997-01-31
AP747A true AP747A (en) 1999-05-03

Family

ID=10787105

Family Applications (2)

Application Number Title Priority Date Filing Date
APAP/P/1997/000911A AP747A (en) 1996-01-16 1997-01-02 Pharmaceutical compositions in the form of a tablet containing famciclovir.
APAP/P/1998/001298A AP1114A (en) 1996-01-16 1997-01-13 Indole compounda as anti-inflammatory/analgesic agents.

Family Applications After (1)

Application Number Title Priority Date Filing Date
APAP/P/1998/001298A AP1114A (en) 1996-01-16 1997-01-13 Indole compounda as anti-inflammatory/analgesic agents.

Country Status (37)

Country Link
US (1) US6765007B1 (en)
EP (1) EP0874632B1 (en)
JP (2) JP4711360B2 (en)
KR (1) KR100338829B1 (en)
CN (1) CN1132582C (en)
AP (2) AP747A (en)
AR (1) AR005456A1 (en)
AT (1) ATE220910T1 (en)
AU (1) AU713090B2 (en)
BG (1) BG63488B1 (en)
BR (1) BR9706982A (en)
CY (1) CY2390B1 (en)
CZ (1) CZ287205B6 (en)
DE (1) DE69714215T2 (en)
DK (1) DK0874632T3 (en)
DZ (1) DZ2159A1 (en)
EA (1) EA001946B1 (en)
EG (1) EG23684A (en)
ES (1) ES2180922T3 (en)
GB (1) GB9600847D0 (en)
HU (1) HU225472B1 (en)
IL (1) IL124913A0 (en)
MX (1) MX9805713A (en)
MY (1) MY127527A (en)
NO (1) NO315689B1 (en)
NZ (1) NZ326769A (en)
OA (1) OA10812A (en)
PE (1) PE35498A1 (en)
PL (1) PL187291B1 (en)
PT (1) PT874632E (en)
SK (1) SK282132B6 (en)
TR (1) TR199800954T2 (en)
TW (1) TW434016B (en)
UA (1) UA63897C2 (en)
UY (2) UY24437A1 (en)
WO (1) WO1997025990A1 (en)
ZA (1) ZA97310B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007037790A2 (en) * 2005-06-08 2007-04-05 Elan Corporation, Plc Modified release famciclovir compositions
AU2010265866B2 (en) 2009-06-26 2012-07-12 Taris Biomedical Llc Solid drug tablets for implantable drug delivery devices
JP2015063521A (en) * 2013-09-02 2015-04-09 科研製薬株式会社 Tablet having high drug content and method for producing the same
CN104434852B (en) * 2013-09-18 2018-11-20 北京韩美药品有限公司 Famciclovir vertical compression piece and preparation method thereof
CN112587491B (en) * 2021-01-03 2022-08-23 迪沙药业集团有限公司 Famciclovir tablet composition

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2671970A1 (en) * 1991-01-30 1992-07-31 Wellcome Found DISPERSABLE TABLETS IN WATER.

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3421800C1 (en) * 1984-06-12 1986-04-17 Maschinen und Werkzeugbau Michael Brümmer GmbH, 8804 Dinkelsbühl Elastic roller for treating a thermoplastic film
EP0182024B1 (en) * 1984-09-20 1991-04-03 Beecham Group Plc Purine derivatives and their pharmaceutical use
CA2103050A1 (en) 1991-05-15 1992-11-16 Yung-Chi Cheng Determination of prodrugs metabolizable by the liver and therapeutic use thereof
GB9303157D0 (en) * 1993-02-17 1993-03-31 Scotia Holdings Plc Treatment of a group of related disorders
IL111138A (en) 1993-10-05 1997-04-15 Smithkline Beecham Plc Pharmaceutical compositions comprising penciclovir and/or its bioprecursor and/or its derivatives for the treatment and prophylaxis of post-herpetic neuralgia
JP3702594B2 (en) * 1997-08-07 2005-10-05 株式会社明電舎 Parameter adjustment method and apparatus

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2671970A1 (en) * 1991-01-30 1992-07-31 Wellcome Found DISPERSABLE TABLETS IN WATER.

Also Published As

Publication number Publication date
HUP9901021A3 (en) 2000-08-28
HK1016473A1 (en) 1999-11-05
GB9600847D0 (en) 1996-03-20
EP0874632B1 (en) 2002-07-24
SK95698A3 (en) 1999-01-11
BG63488B1 (en) 2002-03-29
JP2009091362A (en) 2009-04-30
NO315689B1 (en) 2003-10-13
DE69714215D1 (en) 2002-08-29
BG102638A (en) 1999-07-30
KR19990077229A (en) 1999-10-25
CZ287205B6 (en) 2000-10-11
UY24556A1 (en) 2001-08-27
UA63897C2 (en) 2004-02-16
PL187291B1 (en) 2004-06-30
ATE220910T1 (en) 2002-08-15
EA199800573A1 (en) 1999-02-25
UY24437A1 (en) 1997-06-06
PE35498A1 (en) 1998-08-07
HU225472B1 (en) 2006-12-28
JP4711360B2 (en) 2011-06-29
BR9706982A (en) 1999-07-20
TR199800954T2 (en) 1998-10-21
US6765007B1 (en) 2004-07-20
CN1132582C (en) 2003-12-31
DE69714215T2 (en) 2003-01-23
EP0874632A1 (en) 1998-11-04
IL124913A0 (en) 1999-01-26
MX9805713A (en) 1998-10-31
ZA97310B (en) 1997-10-23
AP9801298A0 (en) 1998-09-30
CN1208350A (en) 1999-02-17
PL327922A1 (en) 1999-01-04
AP9700911A0 (en) 1997-01-31
PT874632E (en) 2002-10-31
AP1114A (en) 2002-10-18
TW434016B (en) 2001-05-16
EA001946B1 (en) 2001-10-22
DZ2159A1 (en) 2002-12-01
NO983259L (en) 1998-07-15
AU1541897A (en) 1997-08-11
CZ225498A3 (en) 1998-12-16
ES2180922T3 (en) 2003-02-16
AU713090B2 (en) 1999-11-25
CY2390B1 (en) 2004-09-10
SK282132B6 (en) 2001-11-06
NZ326769A (en) 2000-05-26
AR005456A1 (en) 1999-06-23
NO983259D0 (en) 1998-07-15
DK0874632T3 (en) 2002-11-11
HUP9901021A2 (en) 1999-08-30
OA10812A (en) 2003-01-29
WO1997025990A1 (en) 1997-07-24
MY127527A (en) 2006-12-29
EG23684A (en) 2007-05-09
JP2000503311A (en) 2000-03-21
KR100338829B1 (en) 2002-07-18

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