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US4250166A Expired / Lapsed US ⏱️ 0.0 years remaining

Long acting preparation of cefalexin for effective treatments of bacterial infection sensitive to cefalexin

Assignee: Shionogi and Co Ltd
•
Filing: 1977-05-27
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Granted: 1981-02-10
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Expires: 1997-05-27
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Abstract

Abstract A cefalexin preparation coated with a coating layer the solubility of which layer is pH-dependent and dissolves in the upper intestine is preferably administered concurrently with a normal (plain, quick-releasing) cefalexin. The coated preparation is preferably coated, in the particle form and when administered orally, exists in the particle form in the stomach. Preferably, the coating layer is made from a coating material having a dissolution pH of from 5.5 to 6.5, and the ratio in terms of potency of the coated cefalexin to the normal cefalexin is between 15:85 and 60:40. The coated cefalexin and the normal cefalexin can be formulated in a pharmaceutical preparation preferably in a unit-dosage form, e.g., capsules, tablets or particles or in strip-packages.

Inventors

  • 👤 Hideyuki Maekawa
  • 👤 Yasushi Takagishi
  • 👤 Hiroshi Kato

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 10:10
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/48; A61K9/50; A61K9/5084; A61K31/00; A61K31/33; A61K31/395; A61K31/54; A61K31/542; A61K31/545

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 75 words
A long-acting cefalexin preparation which comprises normal cefalexin which dissolves rapidly in the stomach, and coated particulate cefalexin which does not dissolve in the stomach but dissolves rapidly in the upper intestine, wherein the said coated portion is coated with a copolymer of methylmethacrylate and methacrylic acid which has a dissolution pH of from 5.5 to 6.5, and wherein the potency ratio of the normal cefalexin to the coated portion is between 40:60 and 25:75.
Claim 2
Dependent Claim 75 words
A long-acting cefalexin preparation which comprises normal cefalexin which dissolves rapidly in the stomach, and coated particulate cefalexin which does not dissolve in the stomach but dissolves rapidly in the upper intestine, wherein the said coated portion is coated with a copolymer of methylmethacrylate and methacrylic acid which has a dissolution pH of from 5.5 to 6.5, and wherein the potency ratio of the normal cefalexin to the coated portion is between 40:60 and 25:75.
Claim 3
Dependent Claim 14 words
A preparation as claimed in claim 1 wherein the potency ratio is approximately 30:70.
Claim 4
Dependent Claim 14 words
A preparation as claimed in claim 1 wherein the dissolution pH is approximately 6.0.
Claim 5
Dependent Claim 21 words
A preparation as claimed in claim 1 wherein the particulate cefalexin is in the form of powder, beads, granules or microcapsules.
Claim 6
Dependent Claim 12 words
A preparation as claimed in claim 1 in a unit dosage form.
Claim 7
Dependent Claim 12 words
A preparation as claimed in claim 5 in the form of capsules.
Claim 8
Dependent Claim 12 words
A preparation as claimed in claim 5 in the form of tablets.
Claim 9
Dependent Claim 18 words
A preparation as claimed in claim 5 in the form of beads, granules or microcapsules contained in strip-packages.
Claim 10
Dependent Claim 23 words
A preparation as claimed in claim 5 wherein the unit dosage form contains 50 to 2000 mg of cefalexin in terms of potency.
Claim 11
Dependent Claim 23 words
A preparation as claimed in claim 9 wherein the unit dosage form contains 500 to 1000 mg of cefalexin in terms of potency.
Claim 12
Dependent Claim 39 words
A method for treating a human infection caused by bacteria sensitive to cefalexin which comprises administering to a human suffering from said infection immediately following a meal a bactericidally effective amount of a preparation as claimed in claim 1.
Claim 13
Dependent Claim 13 words
A method according to claim 11 wherein the potency ratio is about 30:70.
Claim 14
Dependent Claim 13 words
A method according to claim 11 wherein the dissolution pH is about 6.0.
Claim 15
Independent Claim 38 words
A method for treating a human infection caused by bacteria sensitive to cefalexin which comprises administering to a human suffering from said infection immediately following a meal a pharmaceutical composition in compressed tablet form according to claim .

References Cited (Backward Citations)

DE644754C Cited
DE1767320U Cited
US3078216A Cited
DE2259646A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-02-10 1984-08-11 1985-02-10 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-02-10 1988-08-11 1989-02-10 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-02-10 1992-08-11 1993-02-10 $7700.00 Window Closed / Lapsed

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