Scope and Claims Analysis for US Patent 8,512,745: Uncoated Ulipristal Acetate Immediate-Release Tablet with Rapid In Vitro Dissolution

US Patent 8,512,745 is a formulation-focused, single-active, immediate-release tablet patent that narrows to an uncoated oral tablet containing defined weight-percent ranges of ulipristal acetate (5 to 50 mg per tablet) with a specific excipient package (lactose monohydrate or mannitol as diluent; HPMC or povidone as binder; croscarmellose sodium as disintegrant; optional magnesium stearate), plus a functional dissolution requirement under defined European Pharmacopoeia conditions. The independent claim is dominated by the dissolution specification: at least about 90% (w/w) of the ulipristal acetate present must dissolve within about 20 minutes at 37°C ±0.5°C, 50 rpm, pH 1 per European Pharmacopoeia §2.9.3.

What does US 8,512,745 claim cover for ulipristal acetate tablets?

Direct answer: Claim 1 covers an uncoated oral tablet containing 5 to 50 mg ulipristal acetate (present at 3 to 18 wt%), with 60 to 95 wt% of lactose monohydrate and/or mannitol as diluent; 1 to 10 wt% of HPMC or povidone as binder; 1 to 10 wt% croscarmellose sodium; 0 to 5 wt% magnesium stearate; and a functional in vitro dissolution endpoint requiring ≥90% dissolution within ~20 minutes at pH 1 under EP §2.9.3 conditions.

Independent claim 1: element-by-element scope

Claim 1 can be parsed into four enforceable layers:

Dosage form and coating
- “pharmaceutical tablet for oral administration”
- “oral tablet and is uncoated”
- Practical impact: any film-coating (even thin) can be a design-around if a court construes “uncoated” strictly based on the intrinsic meaning and prosecution history. If no coating exists, surface treatment may still create dispute risk (e.g., “purified” surfaces, polishing, or barrier treatments).
Active content limits
- “3 to 18 wt % of ulipristal acetate”
- “ulipristal acetate … amount ranging from 5 mg to 50 mg”
- Practical impact: the patent targets both strengths and supports a broad tablet-mass range consistent with those wt% and mg numbers. Any tablet outside both the wt% and mg limits falls outside Claim 1.
Excipient system constraints
- Diluent: 60 to 95 wt% selected from lactose monohydrate and mannitol
- Binder: 1 to 10 wt% selected from hydroxypropyl methyl cellulose and povidone
- Disintegrant: 1 to 10 wt% croscarmellose sodium
- Lubricant/anti-adherent: 0 to 5 wt% magnesium stearate
  These constraints are not simply ingredient identity; they are quantified wt% windows plus exclusive selection sets (binder is limited to the two listed; diluent is limited to lactose monohydrate and mannitol).
Functional dissolution requirement
- “wherein at least about 90% (w/w) of ulipristal acetate present in the tablet is dissolved within about 20 minutes”
- Test: “in vitro dissolution assay according to the general monograph of the European Pharmacopoeia §2.9.3”
- Conditions: 37°C ±0.5°C, 50 rpm, pH = 1
- Practical impact: even if an accused product fits wt% ranges, the dissolution spec becomes a key infringement and validity battleground. It also gives a credible path for partial design-around by reformulation aimed at missing the “≥90% in ~20 minutes” metric, though dissolution performance is highly dependent on the excipient ratios, particle attributes, and manufacturing controls.

How claim 1 reads for typical strength design

Claim 1 supports multiple strengths because dependent claims enumerate specific mg values (5, 10, 15, 20, 30 mg). The wt% constraint in claim 1 also implies tablet total weight must align so that:

ulipristal acetate wt% lies between 3% and 18%, and
ulipristal acetate mg lies between 5 and 50 mg.

Any generic formulation intending to land outside the dissolution profile or outside the excipient wt% lattice can seek non-infringing compositions. Any formulation that adheres tightly to the ingredient selections plus dissolution metric is within the claim’s functional-literal boundaries.

How do dependent claims narrow US 8,512,745 scope?

Direct answer: Dependent claims lock down specific sub-ranges for excipient wt% and specify concrete strengths (5 to 30 mg) and one preferred composition example.

Dependent claims 2–5: excipient sub-range tightening

Claim 2: diluent 65 to 92 wt%
Claim 3: binder 1.5 to 8.5 wt%
Claim 4: croscarmellose sodium 1.5 to 8.5 wt%
Claim 5: magnesium stearate 0.5 to 4 wt%

These narrow the possible design space for an accused product that otherwise sits on the broader Claim 1 envelope.

Dependent claim 6: specific active content level

Claim 6: “10 wt % ulipristal acetate”
This is a point claim that can overlap with multiple mg strengths depending on total tablet mass, but it creates an additional infringement target for products formulated around that exact wt%.

Dependent claims 7, 12–16: specific mg strengths

Claim 7: 5 to 30 mg ulipristal acetate
Claims 12–16: specify tablets containing 5 mg, 10 mg, 15 mg, 20 mg, 30 mg ulipristal acetate

These claims matter for litigation because they let a patentee argue infringement for a particular marketed strength even if wt% distributions vary slightly, provided the composition still meets Claim 1’s wt% constraint and dissolution metric.

Dependent claim 8: specific diluent/binder pairing

“diluent is lactose monohydrate and binding agent is povidone”

This is a further narrowing to a particular excipient identity combination.

Dependent claims 9–10: explicit “numerical formulation” example

Claim 9: ulipristal acetate 6 to 12 wt%, lactose monohydrate 71 to 87 wt%, povidone 4.5 to 5.5 wt%, croscarmellose sodium 4.5 to 5.5 wt%, magnesium stearate 1 to 4 wt%
Claim 10: ulipristal acetate 10 wt%, lactose monohydrate 79 wt%, povidone 5 wt%, croscarmellose sodium 5 wt%, magnesium stearate 1 wt%

This pair creates a tight infringement “fingerprint” around a likely commercial formulation. Even if a competing generic differs, Claim 9 and 10 give a clear target for claim construction and comparative testing.

Dependent claim 11: manufacturing method

“mixing the ingredients and ulipristal acetate and forming a tablet” This is broad and likely easy for any tablet manufacturer to replicate conceptually. In practice, method claims like this can add leverage in discovery around manufacturing steps, but they are often limited in enforceability if the method is too generic.

What is the likely patent scope boundary: composition ranges vs. dissolution metric?

Direct answer: The hard boundary is the combination of (i) the specified excipient lattice with quantified wt% ranges and (ii) the functional dissolution endpoint at pH 1. A product that matches the ingredients but misses the dissolution metric can argue non-infringement. A product that achieves the dissolution metric but uses binder/diluent/disintegrant outside the listed selections or ranges can also argue non-infringement.

Infringement risk profile by deviation type

Ingredient identity deviation (e.g., using a binder other than HPMC or povidone; or a diluent other than lactose monohydrate and mannitol) is the cleanest design-around because it breaks the “selected from the group consisting of” limitations.
wt% ratio deviation (e.g., croscarmellose outside 1–10 wt%) can avoid literal infringement, but may still create doctrine-of-equivalents exposure depending on jurisdiction and claim construction.
Dissolution deviation is high-impact but technically complex. Achieving a materially different dissolution curve without leaving the wt% lattice is difficult, but feasible with particle engineering, grade selection, granulation vs direct compression, and lubricant choice.

What patents protect ulipristal acetate immediate-release tablets with lactose/povidone/croscarmellose systems?

Direct answer: Based on claim structure alone, US 8,512,745 protects a specific uncoated immediate-release tablet formulation package for ulipristal acetate. The claim is formulation- and dissolution-centric, not method-of-treatment-centric.

Typical adjacent patent categories that often coexist in ulipristal acetate estates

While this is not a list of other numbered patents (not provided here), the claim indicates the estate is likely to include at least one or more of the following:

Additional formulation patents around alternative binder systems (e.g., different polymer grades) or alternative disintegrant systems
Process patents for tablet manufacturing (granulation vs direct compression; compression force and milling)
Coating or gastro-resistant layer patents (because the claim explicitly requires “uncoated,” a coating estate may be separately present)
Strength-specific patents if marketed doses map to the enumerated mg values

US 8,512,745 itself is tightly scoped to uncoated tablets and the dissolution function; it would not read on coated or modified-release products if those are construed as not “uncoated.”

When does US 8,512,745 lose exclusivity? How long is it enforceable in the US?

Direct answer: Enforceability duration is driven by the US patent term measured from the earliest effective non-provisional filing date plus any adjustments, and by any patent term adjustment or disclaimer. The user-provided input does not include the filing date, priority, or any PTA/PTD values for US 8,512,745, so a specific expiration date cannot be stated from the claim text alone.

What generic entry risks exist for ulipristal acetate tablets in light of US 8,512,745?

Direct answer: The biggest risk for a potential generic is that its marketed tablet strength falls within the 5–30 mg (and also 5–50 mg per claim 1) framework and that its composition uses lactose monohydrate/manitol diluents, HPMC or povidone binder, croscarmellose sodium disintegrant, and optionally magnesium stearate, while also achieving ≥90% dissolution in ~20 minutes at pH 1 per EP §2.9.3.

Paragraph IV-style infringement test likely to be run

For any ANDA-type challenge where dissolution drives infringement:

Compare the excipient list and wt% composition to the Claim 1 lattice
Compare dissolution profiles under EP §2.9.3 conditions (pH 1; 37°C; 50 rpm)
Evaluate whether any coating exists or any surface film disqualifies “uncoated”

How strong is the patent claim set for enforcement: is it narrow or broad?

Direct answer: Strength is mixed: it is broad in the sense that it covers multiple strengths and two diluent options and two binder options, but it is narrow because it locks ingredient identity to enumerated groups and requires a strict functional dissolution outcome under defined test conditions.

Claim construction leverage

The term “uncoated” can be a gating issue. If the competitor uses any film coating or enteric coating, they may fall outside literal scope.
The dissolution standard is objective. In litigation, dissolution test results can become determinative, but they also become a battleground for protocol, variability, and repeatability.
“at least about 90% … dissolved within about 20 minutes” includes “about,” which adds some flexibility, but it still sets a high-performance threshold that generic products may be engineered to meet.

What formulation design-arounds are most credible against this claim?

Direct answer: The highest-probability design-arounds, based strictly on claim language, are:

Use a binder not selected from HPMC or povidone, or use a croscarmellose level outside 1–10 wt%.
Use a diluent outside lactose monohydrate/manittol.
Maintain ingredients but tune dissolution so it is not ≥90% in ~20 minutes at pH 1 EP conditions.
Add a coating so the tablet is not “uncoated.”

These map directly to claim element boundaries rather than speculative equivalence arguments.

Key claim map for US 8,512,745 (for infringement analysis)

Claim element	Scope in US 8,512,745	Design-around angle
Dosage form	Oral tablet; uncoated	Use film coat or barrier layer; change classification
Ulipristal acetate amount	5 mg to 50 mg; also 3–18 wt%	Use strength outside mg limits or wt% window
Diluent	60–95 wt% of lactose monohydrate and/or mannitol	Use other diluent(s) or move out of wt%
Binder	1–10 wt% of HPMC or povidone	Use other binder or out of wt%
Disintegrant	1–10 wt% croscarmellose sodium	Exclude or out of wt%
Lubricant	0–5 wt% magnesium stearate	Exclude or out of wt%
Dissolution performance	≥90% dissolved within ~20 min at pH 1, EP §2.9.3, 37°C ±0.5°C, 50 rpm	Miss dissolution threshold by reformulation and process

Key Takeaways

US 8,512,745 is a dissolution-anchored formulation patent for an uncoated ulipristal acetate tablet.
Claim 1 sets a strict combination: enumerated excipients (lactose monohydrate/mannitol diluent; HPMC/povidone binder; croscarmellose sodium disintegrant; optional magnesium stearate) with defined wt% windows plus a functional dissolution requirement: ≥90% dissolved in ~20 minutes at pH 1 under EP §2.9.3.
Dependent claims tighten excipient sub-ranges and add explicit strength targets (5–30 mg) and an explicit numerical formulation (Claim 10).
Litigation leverage likely centers on whether an accused product’s composition falls inside the wt%/identity lattice and whether it satisfies the objective pH 1 dissolution test.
The clearest design-arounds are moving outside the enumerated excipient groups or wt% windows, failing the dissolution target, or using a coated tablet that does not meet “uncoated.”

FAQs

1) Does US 8,512,745 cover film-coated ulipristal acetate tablets?

No. Claim 1 requires the tablet to be “uncoated,” which excludes film-coated products under a straightforward reading of claim language.

2) If a generic matches the excipient wt% ranges, can it avoid infringement by failing the dissolution metric?

Yes. Claim 1 is both structural (ingredients and wt% windows) and functional (≥90% dissolution within ~20 minutes at pH 1). Missing the dissolution endpoint can be a basis for non-infringement.

3) Which excipient deviations are most effective against Claim 1?

Switching to a binder outside HPMC/povidone, changing the diluent outside lactose monohydrate/mannitol, or adjusting croscarmellose sodium outside 1–10 wt% are direct element-level deviations.

4) Which claim best targets a specific marketed formulation?

Claim 10 is the most specific because it provides a fully enumerated composition: ulipristal acetate 10 wt%, lactose monohydrate 79 wt%, povidone 5 wt%, croscarmellose sodium 5 wt%, magnesium stearate 1 wt%.

5) Do method claims in US 8,512,745 meaningfully constrain competitors?

Claim 11 is very general (mix ingredients and form a tablet). It is less likely to provide a unique manufacturing barrier compared with the formulation and dissolution limitations in Claim 1.

References

No external sources were provided in the prompt.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Lab Hra Pharma	ELLA	ulipristal acetate	TABLET;ORAL	022474-001	Aug 13, 2010	AB	RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial	Y				⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2009326084	⤷ Start Trial
Brazil	PI0922796	⤷ Start Trial
Canada	2745084	⤷ Start Trial
China	102245173	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 8,512,745

Which drugs does patent 8,512,745 protect, and when does it expire?

Summary for Patent: 8,512,745