Details for Patent: 5,753,265
Summary for Patent: 5,753,265
| Title: | Multiple unit pharmaceutical preparation | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Abstract: | PCT No. PCT/SE95/00678 Sec. 371 Date Jun. 22, 1995 Sec. 102(e) Date Jun. 22, 1995 PCT Filed Jun. 7, 1995 PCT Pub. No. WO96/01624 PCT Pub. Date Jan. 25, 1996A new pharmaceutical multiple unit tableted dosage form containing as active ingredient an acid labile H+K+-ATPase inhibitor or an alkaline salt thereof or one of its single enantiomers or an alkaline salt thereof, a method for the manufacture of such a formulation, and the method of treatment with such a formulation in medicine. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Inventor(s): | Pontus John Arvid Bergstrand, Kurt Ingmar Lovgren | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assignee: | AstraZeneca AB | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Application Number: | US08/464,774 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Patent Claim Types: see list of patent claims | Use; Composition; Process; Dosage form; | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Patent landscape, scope, and claims: | United States Patent 5,753,265: Scope, Claims, Expiration, and Pharmaceutical Patent LandscapeU.S. Patent No. 5,753,265 covers a multiple-unit, enteric-coated tablet containing an acid-labile proton-pump inhibitor, including omeprazole-type compounds and their salts or single enantiomers. Its central limitation is the use of individually enteric-coated core units that retain acid resistance after compression into a tablet. The patent issued in 1998 and its ordinary U.S. patent term expired in 2015. It therefore presents no current blocking right for U.S. pharmaceutical development, although it remains relevant to historical formulation strategy, prior-art analysis, and freedom-to-operate reviews. What does U.S. Patent 5,753,265 protect?The patent protects a pharmaceutical architecture rather than a particular proton-pump inhibitor molecule. Its principal combination is:
The protected dosage form is commonly described as a multiple-unit pellet system, or MUPS. The core units can be active-layered seeds, pellets, granules, or comparable subunits. Those units are coated individually before they are blended with tablet excipients and compressed. The patent's technical objective is to combine the dose flexibility and acid protection of enteric-coated pellets with the handling and administration advantages of a tablet. Compression can fracture or deform enteric coatings. The claims require a coating that remains functionally acid resistant after compression. What is the scope of independent claim 1?Claim 1 is the principal composition claim. It requires each of the following elements:
A conventional enteric-coated tablet with one continuous drug-containing core would generally fall outside claim 1 because the claim requires multiple individually coated units. A capsule containing enteric-coated pellets may also fall outside the literal tablet requirement, depending on the remaining claim language and any applicable doctrine-of-equivalents analysis. What chemical compounds are covered by claim 2?Claim 2 introduces a broad Markush definition for the active ingredient. It covers substituted benzimidazole sulfoxide proton-pump inhibitors and related salts or enantiomers. The substituent definitions include:
The claim expressly excludes three named compounds and their corresponding enantiomers or alkaline salts. Those exclusions narrow the Markush group but do not eliminate the broader formulation requirement in claim 1. The chemical definition is consistent with the substituted benzimidazole proton-pump-inhibitor class that includes omeprazole, lansoprazole, pantoprazole, rabeprazole, and related compounds. Exact inclusion of a particular molecule requires mapping every substituent to the claim's structural formula. The structural images for claim 2 and claim 3 are not reproduced in the supplied text, so a compound-by-compound claim chart cannot be completed from the text alone. What does claim 3 add?Claim 3 narrows claim 1 to specifically illustrated compounds. The supplied claim text omits the chemical structures represented by the image placeholders. As a result, the exact compounds covered by claim 3 cannot be identified from the provided transcription. Claim 3 is narrower than claim 2 because it relies on a closed set of depicted compounds rather than the full Markush definition. Its practical value would have depended on whether the commercial active ingredient was one of the illustrated compounds and whether the product used the claimed salt or enantiomeric form. Which formulation features are protected by U.S. Patent 5,753,265?The dependent claims create a layered formulation estate around the core MUPS concept.
These claims are cumulative. A product does not infringe a dependent claim unless it first meets every limitation of claim 1 and then satisfies the added limitation. How important is the 10% acid-resistance limitation?Claim 5 requires that acid resistance decrease by no more than 10% during compression. This is a quantitative performance limitation, not merely a formulation description. An infringement analysis would require:
The limitation could have made claim 5 more difficult to enforce than claim 1 because the patent owner would need to establish the relevant baseline and testing method. It also creates design-around opportunities through a different coating system or tablet manufacturing process. What do claims 14 through 19 protect?Claims 14 through 19 cover manufacturing processes. Claim 14 requires:
Claims 15, 18, and 19 add an over-coating, alkaline compound, or separating layer. These process claims are directed to the sequence and materials used to make the dosage form. They would not necessarily reach a product made by a materially different process if the process steps could not be proven. Process claims also create evidentiary issues. Manufacturing records, batch instructions, coating parameters, and technical dossiers may be required to determine whether an accused product follows the claimed sequence. What do the blister-package claims cover?Claims 20 and 23 cover press-through blister packages containing the claimed tableted dosage form. These claims are packaging claims linked to the underlying composition. Claim 20 requires multiple press-through blisters, each containing a composition within the specified claim set. Claim 23 requires at least one press-through blister containing the tableted dosage form. The packaging claims do not independently protect the active ingredient. They require the packaged product to contain a tablet that falls within the underlying composition claims. A blister package containing a non-infringing enteric formulation would not satisfy these claims merely because it uses the same packaging format. What method-of-use patents and therapeutic claims are included?Claims 21 and 22 cover administration of the composition for:
These are method claims directed to therapeutic use in mammals and humans. They require administration of a therapeutically effective dose of a composition falling within the referenced composition claims. The claims do not broadly cover all uses of proton-pump inhibitors. They are tied to the claimed multiple-unit tableted composition. A generic manufacturer could face a method-claim issue only if its product and labeling met the composition and therapeutic-use limitations. In practice, inducement analysis would depend heavily on the approved label, promotional conduct, and the scope of any remaining enforceable patent rights. When did U.S. Patent 5,753,265 expire?U.S. Patent 5,753,265 issued on May 19, 1998. The patent derives from an international pharmaceutical formulation filing with a 1995 filing date and an earlier 1994 priority date. Its ordinary U.S. patent term ran approximately 20 years from the relevant nonprovisional or PCT filing date and ended in 2015, subject to any recorded patent-term adjustment or extension.
The patent is therefore expired. An expired patent can remain relevant as prior art, as a technical disclosure, or in historical litigation, but it cannot ordinarily support a new U.S. infringement action. What was the FDA Orange Book status of this patent?The Orange Book lists patents submitted by NDA holders for approved drug products. Listing does not establish validity, enforceability, or infringement. It identifies patents that an ANDA applicant may need to address through a certification under the Hatch-Waxman framework.[2] U.S. Patent 5,753,265 is associated with the historical patent landscape for enteric-coated proton-pump-inhibitor formulations and Astra's multiple-unit tablet technology. Any historical Orange Book listing would have been tied to a specific NDA and dosage form rather than to every proton-pump-inhibitor product. The patent's expiration means it does not create a current Orange Book barrier to an ANDA. A current applicant would instead evaluate still-active patents covering:
Were there Paragraph IV challenges involving this patent?Paragraph IV certification is used when an ANDA applicant asserts that a listed patent is invalid, unenforceable, or not infringed. A Paragraph IV notice can trigger a 30-month stay under the Hatch-Waxman statute if the NDA holder files suit within the statutory period.[2] The long commercial history of omeprazole and other proton-pump inhibitors produced extensive ANDA litigation involving active-ingredient, formulation, and method-of-use patents. U.S. Patent 5,753,265 belongs to the formulation layer of that landscape. Because the patent expired in 2015, it is no longer a live Paragraph IV barrier. The key distinction is between:
The expiration of this patent did not necessarily eliminate all historical patent risks surrounding the relevant proton-pump inhibitor. What patent landscape surrounded omeprazole and related proton-pump inhibitors?The relevant patent estate generally divided into five layers.
A representative historical family is Astra's omeprazole compound and formulation portfolio, including earlier U.S. patents directed to omeprazole and pharmaceutical preparations. Esomeprazole created a separate enantiomer-focused estate, including U.S. Patent No. 5,714,504. Those patents should not be treated as interchangeable with U.S. Patent 5,753,265 because each has different claim language, priority dates, expiration dates, and product coverage. How strong was the patent estate for the claimed formulation?The patent was technically meaningful but legally narrow in its central combination. Its strongest features were:
Its limitations were equally important:
For historical enforcement, an accused product would need to be compared against the entire claim combination. A product using a single enteric-coated matrix, a capsule rather than a tablet, or a formulation whose pellets were not compressed into the claimed dosage form could present non-infringement positions. What generic launch risks exist today?For this patent specifically, the generic launch risk is zero from an active U.S. patent-term perspective. The patent cannot presently block an ANDA, 505(b)(2) application, or commercial launch. The relevant current risk would come from later patents or regulatory exclusivities associated with the particular proton-pump inhibitor and dosage form. A generic or follow-on developer should distinguish:
These products do not share one unified patent estate. Each requires an NDA-, active-ingredient-, strength-, and formulation-specific review using the FDA Orange Book and relevant USPTO records.[1] Does biosimilar risk apply?No. Proton-pump inhibitors are chemically synthesized small molecules, not biologics. The applicable regulatory pathway is generally an ANDA under section 505(j) of the Federal Food, Drug, and Cosmetic Act, or in some cases a 505(b)(2) application. The FDA Purple Book biosimilar framework does not apply.[3] The commercial threat is generic substitution, not biosimilar substitution. Bioequivalence, delayed-release performance, dissolution, labeling, and patent certifications are the central regulatory issues. What licensing or ownership issues affect the patent?The patent was issued to Astra-related ownership and formed part of the originator's broader proton-pump-inhibitor formulation portfolio. Ownership and enforcement rights may have moved through corporate restructuring, including AstraZeneca's successor interests. The patent document itself does not establish the full commercial licensing history for omeprazole, co-promotion, or manufacturing rights. Commercial agreements should be distinguished from patent assignments and recorded ownership. For current diligence, the decisive issue is not historical licensing but whether any enforceable successor patent, regulatory exclusivity, or contractual restriction remains applicable to the target product. Key Takeaways
FAQs About U.S. Patent 5,753,265Is U.S. Patent 5,753,265 still enforceable?No. Its ordinary U.S. patent term expired in 2015, absent an unusual recorded adjustment or extension. Does the patent cover omeprazole MUPS tablets?Its claim structure is directed to the MUPS architecture used for acid-labile proton-pump inhibitors, including omeprazole-type compounds. Product-specific coverage requires mapping the active ingredient, coating, compression behavior, and all other claim limitations. Does the patent cover enteric-coated capsules?Not necessarily. Claim 1 requires an oral multiple-unit tablet. A capsule containing enteric-coated pellets may not satisfy the literal tablet limitation. Can an expired patent still affect an ANDA filing?It can remain relevant as prior art and may explain formulation technology, but it ordinarily cannot support a current infringement block. An ANDA applicant must still assess other unexpired patents listed for the relevant reference product. Is a 505(b)(2) application required for a product using this formulation?Not solely because this patent exists. The appropriate pathway depends on the proposed active ingredient, reference product, formulation differences, clinical bridging requirements, and FDA determination. The expired patent does not itself mandate a 505(b)(2) pathway. References
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Drugs Protected by US Patent 5,753,265
| Applicant | Tradename | Generic Name | Dosage | NDA | Approval Date | TE | Type | RLD | RS | Patent No. | Patent Expiration | Product | Substance | Delist Req. | Patented / Exclusive Use | Submissiondate |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| >Applicant | >Tradename | >Generic Name | >Dosage | >NDA | >Approval Date | >TE | >Type | >RLD | >RS | >Patent No. | >Patent Expiration | >Product | >Substance | >Delist Req. | >Patented / Exclusive Use | >Submissiondate |
Foreign Priority and PCT Information for Patent: 5,753,265
| Foriegn Application Priority Data | ||
| Foreign Country | Foreign Patent Number | Foreign Patent Date |
| Sweden | 9402431-2 | Jul 08, 1994 |
| PCT Information | |||
| PCT Filed | June 07, 1995 | PCT Application Number: | PCT/SE95/00678 |
| PCT Publication Date: | January 25, 1996 | PCT Publication Number: | WO96/01624 |
International Family Members for US Patent 5,753,265
| Country | Patent Number | Estimated Expiration | Supplementary Protection Certificate | SPC Country | SPC Expiration |
|---|---|---|---|---|---|
| Austria | 275396 | ⤷ Start Trial | |||
| Australia | 2993695 | ⤷ Start Trial | |||
| Australia | 2993895 | ⤷ Start Trial | |||
| Australia | 695971 | ⤷ Start Trial | |||
| >Country | >Patent Number | >Estimated Expiration | >Supplementary Protection Certificate | >SPC Country | >SPC Expiration |
