Details for Patent: 7,393,543

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Summary for Patent: 7,393,543

Title:	Vaginally administratable progesterone-containing tablets and method for preparing same
Abstract:	The present invention provides a method for preparing a tablet for the vaginal administration of progesterone for systemic use. The method comprises first mixing water with micronized progesterone, the total amount of water mixed with said micronized progesterone not exceeding the maximum wetting capacity of the micronized progesterone, drying the wetted, micronized progesterone; mixing the dry micronized progesterone with other pharmaceutically acceptable excipients or diluents; and; forming a tablet by direct compaction of the dry micronized progesterone. Tablets prepared by this method are also provided.
Inventor(s):	Azariah Jossifoff
Assignee:	Ferring BV
Application Number:	US10/832,742
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form;

Scope and Claims of US Patent 7,393,543: Dry Natural (Micronized) Progesterone Vaginal Effervescent Tablets With Tmax 3.05–9.75 Hours

US 7,393,543 is a US utility patent focused on a specific combination of (1) dosage form (vaginal tablet), (2) actives (dry natural progesterone, including micronized natural progesterone), (3) a required effervescent component, (4) defined tablet manufacturing approach (wetting and drying progesterone; then direct compaction), and (5) an in-vagina pharmacokinetic performance window (Tmax from 3.05 hours to 9.75 hours after placement). The claim set is structured as both broad composition claims and narrower dependent claims that lock down active grade (micronized), active loading (about 50 mg and 100 mg), effervescent loading (about 8% or 6–8 wt.%), and an explicit excipient blend.

The patent landscape around this type of product typically turns on whether competitors can avoid one or more required claim elements: effervescent presence, “dry” progesterone obtained by specific wet/dry processing, direct compaction, micronized grade, defined progesterone and effervescent weight ranges, or the Tmax performance window.

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What does US 7,393,543 claim for vaginal effervescent progesterone tablets (and what is the core claim “lock”)?

Core “lock” elements present across the independent claim concepts you provided:

1. Dosage form: a tablet for vaginal administration that dissolves in the vagina.
2. Active: natural progesterone that is dry (including the “micronized” embodiments).
3. Excipients: pharmaceutically acceptable excipients are required.
4. Effervescent: an effervescent is required.
5. PK window: tablet provides a Tmax from 3.05 hours to 9.75 hours after placement in the vagina.
6. At least one independent claim contains a manufacturing process constraint: preparing wetted progesterone by mixing progesterone with water, drying to obtain dry natural progesterone, then mixing with excipients and effervescent, then forming a dry tablet by direct compaction.

Practical enforcement consequence: the strongest infringement position comes from products that match the claimed formulation and meet the claimed Tmax window. If a competitor matches the composition but shifts Tmax outside 3.05–9.75 hours, or eliminates effervescent, or avoids the wetting/drying and direct compaction scheme, it may land outside these claims.

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How broad are the claims: composition-only vs process claims vs “consisting essentially of” excipient-lists?

What types of claim scope appear in the provided claim set?

You provided the following claim categories:

• Composition + performance (Tmax) + effervescent + dry natural progesterone (independent-like structure):
  Claims 1, 4, 21, and 24 reflect a composition and property combination.

• Composition + process steps + performance (Tmax):
  Claims 2 and 3 include manufacturing steps: wetted progesterone from water + drying, then mixing and direct compaction.

• Composition with quantitative loading windows (wt.% of progesterone and effervescent):
  Claim 4 (6–20 wt.% progesterone; 5–12 wt.% effervescent) plus dependent narrowing (claims 5–6).

• Dependent claims locking active grade and dosage levels:
  Claims 7–16 specify micronized progesterone and 50 mg / 100 mg embodiments.

• Excipient-specific “consisting essentially of” composition with explicit excipient proportions:
  Claim 22 and Claim 23 include a specific excipient package including colloidal anhydrous silica, maize 1500 starch, povidone 30, lactose, adipic acid, sodium bicarbonate, magnesium stearate, and sodium lauryl sulfate, with provided weight percentages.

• Numeric performance requirement appears in multiple claims:
  Tmax 3.05–9.75 hours appears repeatedly.

Scope implication

• Claims 1 and 4-like constructs are “wide” in that they do not list every excipient, only “pharmaceutically acceptable excipients” plus an effervescent and performance.
• Claims 2 and 3-like constructs are “narrower” because manufacturing steps are part of the claim.
• Claims 22–23-like constructs are narrowest because the excipient list and weight percentages are pinned (“consisting essentially of” and specific wt.%).
• Tmax is a performance limiter even for composition claims, converting them into potentially testable properties and creating a strong design-around axis.

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Which elements are most likely required for infringement: effervescent, micronization, direct compaction, or Tmax?

Effervescent

• Your independent/composition language explicitly includes an effervescent in claims 1, 2, 4, 21, 22, and 24.
• Removing effervescence is a primary design-around lever, unless another claimed feature implicitly recreates effervescence (not present in your text).

Dry natural progesterone

• Claims require “dry natural progesterone” (or “wetted … and drying … to obtain dry natural progesterone” in process claims).
• A competitor using a different form (e.g., granulated wet mix or a different drying paradigm) may argue non-reads on “dry” obtained via the claimed steps.

Tmax 3.05–9.75 hours

• This is a performance constraint that can be dispositive in claim construction and proof.
• It can also be used as a boundary in litigation through bioequivalence-style or PK bridging studies.

Micronized progesterone

• Dependent claims 7–16 tie infringement to micronized progesterone and specific mg levels.
• If a competitor uses non-micronized progesterone, it may still infringe broader claims that only require natural progesterone (depending on how “dry natural progesterone” is construed versus “micronized” being optional).

Direct compaction

• Claims 2 and 3 include “forming a dry tablet by direct compaction.”
• A competitor using wet granulation then drying, or another tableting method, could argue non-infringement if the manufacturing steps are interpreted as limiting.

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What are the numerical formulation boundaries in US 7,393,543 (wt.% and mg windows)?

Progesterone wt.% and effervescent wt.% (tablet composition)

• Claim 4: 6 to 20 wt.% dry natural progesterone
• Claim 4: 5 to 12 wt.% effervescent

Dependent narrowing:

• Claim 5: progesterone 8 to 12 wt.%
• Claim 6: effervescent 6 to 8 wt.%

Additional dependent numeric examples:

• Claim 10: micronized progesterone at ~50 mg or ~100 mg (and claim 9/15/16 mirror these in different dependent positions)

Effervescent specific examples:

• Claim 17: effervescent 5% to 12% by weight
• Claim 18: effervescent about 8% by weight
• Claim 19: effervescent 5% to 12% by weight
• Claim 20: effervescent about 8% by weight

Micronized progesterone amount

• Claim 11: at least 50 mg
• Claim 12: about 50 mg
• Claim 13: about 100 mg
• Claims 14–16 mirror these but depend from a different parent claim (claim 10).

Explicit excipient composition with wt.% (tightest formulation lock)

Claim 23 provides a specific blend (as stated):

• Dry micronized natural progesterone: 8.0 wt.%
• Colloidal anhydrous silica: 0.2 wt.%
• Maize 1500 starch: 16.8 wt.%
• Povidone 30: 3.9 wt.%
• Lactose: 60.8 wt.%
• Adipic acid: 4.6 wt.%
• Sodium bicarbonate: 3.4 wt.%
• Magnesium stearate: 1.8 wt.%
• Sodium lauryl sulfate: 60.4 wt.% (as written)

Scope note: the last line as written conflicts with the other wt.% totals (9 components sum exceeds 100% if sodium lauryl sulfate is 60.4 wt.% while lactose is 60.8 wt.%). For patent landscape purposes, claim 22–23 should be treated as having an excipient-locked embodiment where the narrative intent is clear: a particular excipient package including an acid (adipic acid), a base (sodium bicarbonate), a binder/filler system (maize starch, povidone 30, lactose), and surfactant (sodium lauryl sulfate), with lubricants (magnesium stearate) and glidant (colloidal silica).

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How is the tablet made: what do claims 2 and 3 require about wetting, drying, and compaction?

Process steps in claim 2

Claim 2 requires:

1. Preparing a mixture of water and natural progesterone to obtain wetted natural progesterone
2. Drying wetted natural progesterone to obtain dry natural progesterone
3. Mixing dry progesterone with at least one pharmaceutically acceptable excipient and an effervescent to form a second mixture
4. Forming a dry tablet by direct compaction
5. Tablet dissolves in vagina and gives Tmax 3.05–9.75 hours

Process steps in claim 3

Claim 3 tightens the first step:

1. Mix water with the natural progesterone in the absence of pharmaceutically acceptable excipients to obtain wetted progesterone
2. Dry to form dry natural progesterone
3. Mix dry progesterone with (a) pharmaceutically acceptable excipients and (b) effervescent
4. Form tablet by direct compaction
5. Tablet dissolves in vagina and gives Tmax 3.05–9.75 hours

Design-around implications

• Manufacturing changes that eliminate “direct compaction” or insert excipients during the initial wetting/drying step may be used to argue non-infringement against the process-including claims.

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What is the Orange Book status of US 7,393,543 and which products map to it?

No actionable Orange Book mapping can be produced from the information provided. Determining Orange Book status requires matching the patent number to FDA listed drug product records and specific NDA/ANDA/BLA entries, which is not included in your input.

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When does exclusivity end: patent expiration and potential regulatory exclusivity timelines?

No expiration date, filing date, or listed maintenance status is included in your input. Without the patent’s priority and USPTO data, exclusivity and patent-term end cannot be calculated from the claim text alone.

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What Paragraph IV or biosimilar risk exists around this patent?

A Paragraph IV or biosimilar risk assessment requires:

• the FDA-listed reference product,
• whether any ANDAs exist, and
• whether any generic candidates have asserted non-infringement or invalidity, or have been involved in Hatch-Waxman litigation.

No such FDA litigation dataset is included in your input, so no definitive risk mapping can be stated.

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How strong is the patent estate for this kind of product: are these claims a standalone “Tmax effervescent” shield or part of a broader family?

No priority/family information is provided. Without related continuation/divisional/patent family members, cannot assess whether this is the principal claim set or one member within a multi-layer estate covering polymorphs, particle size distributions, excipient matrices, coating strategies, or PK targets.

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Which claim elements create the largest design-around space for competitors?

High-yield design-around levers

1. Tmax shift outside 3.05–9.75 hours:
   Even a similar excipient composition may be non-infringing if Tmax falls outside the window.
2. Eliminate effervescent:
   Removes a required element from multiple claims.
3. Avoid direct compaction or avoid the specific wetting/drying scheme:
   Targets claims 2 and 3.
4. Use non-micronized natural progesterone:
   Primarily reduces risk against micronized-dependent claims (7–16), but not necessarily against broader natural progesterone claims.
5. Avoid the explicit excipient package and/or wt.% ranges:
   Particularly against claim 22–23.

Low-yield levers

• Minor excipient substitutions that still preserve effervescence, dry progesterone, and the PK window may not provide a clean exit if broader claims apply.

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What litigation proof is likely required given Tmax performance claims?

Because the claims require a Tmax window, enforcement typically depends on:

• a clinical PK study design consistent with the patent’s measurement approach,
• demonstration that the accused product’s Tmax after vaginal placement falls within 3.05–9.75 hours.

For competitors, the corresponding defensive posture is typically:

• test a comparable protocol and demonstrate Tmax is outside the claimed range, or
• argue that the formulation does not meet other limiting elements like effervescent content, micronization, or manufacturing process features.

(Underlying procedural posture still depends on the patent’s prosecution history and claim construction record, which is not in your input.)

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How does US 7,393,543 compare with adjacent progesterone vaginal product IP themes (formulation vs PK targets)?

Based on the claim structure, the patent aligns with a broader class of formulation patents that use:

• a known active (progesterone),
• a known dosage form (vaginal tablet),
• a formulation enhancement (effervescence),
• and a measurable PK endpoint (Tmax window).

That combination shifts the patent from “composition only” into “composition plus performance,” which is generally more difficult to fully design around than composition-only claims but also more dependent on measurable endpoints during litigation.

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Key Takeaways

• US 7,393,543 claims dry natural progesterone vaginal effervescent tablets with a defined Tmax 3.05–9.75 hours performance window.
• Scope divides into:
  • broader composition claims requiring effervescence, dry progesterone, and Tmax,
  • narrower process claims requiring water-wetting, drying, and direct compaction, and
  • narrowest excipient-locked embodiments with specific excipient ingredients and (at least in the narrative intent) specific wt.% targets.
• The highest design-around levers are removing effervescence, shifting Tmax outside the window, and changing manufacturing method (for the process-including claims).
• Micronized progesterone and specific mg levels are captured via dependent claims, which reduces risk for formulations using different particle grade or dose, but does not automatically remove risk for broader non-micronized claims.

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FAQs

1. Can a vaginal progesterone tablet avoid US 7,393,543 by using non-effervescent excipients?
2. How does changing progesterone particle size (micronized vs non-micronized) affect infringement risk for dependent claims?
3. If a competitor’s product hits the same excipient blend but has a different Tmax, does that avoid infringement?
4. Do manufacturing changes like wet granulation versus direct compaction avoid claims that include process steps?
5. Which excipients in claim 22–23 most likely correspond to the effervescent system and dissolution performance?

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References

No sources were provided in the prompt for US 7,393,543 bibliographic data, Orange Book listings, prosecution history, or litigation records, so no numbered reference list can be generated from cited materials.

Drugs Protected by US Patent 7,393,543

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: 7,393,543

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Israel	127129	Nov 18, 1998

International Family Members for US Patent 7,393,543

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	1176200
Canada	2568823
Denmark	1131052