US Patent 5,972,383: What Is Claimed, How Broad the Scope Is, and Where It Sits in the Raloxifene Formulation Landscape

US Drug Patent 5,972,383 claims method-of-use coverage for oral solid formulations of raloxifene hydrochloride that are defined by a specific excipients framework (surfactant + polyvinylpyrrolidone + water-soluble diluent), with multiple dependent claim fallbacks that narrow to polysorbate 80 + lactose and optionally lubricant/disintegrant and film coating.

The core scope is not “a new drug” but a formulation-defined dosing method: administering a solid oral raloxifene-HCl product where the excipient selections match the claims.

What is the claim nucleus and what does it cover?

Independent claim structure (claims 1 and 13)

Claim 1 covers a method of treating:

mammary tumors, prostatic tumors, or osteoporosis

by administering to a human a solid orally administerable pharmaceutical formulation that comprises:

raloxifene hydrochloride
surfactant
polyvinylpyrrolidone (PVP)
water soluble diluent

with the additional excipient definitions:

the surfactant is either (i) sorbitan fatty acid ester or (ii) polyoxyethylene sorbitan fatty acid ester
the water soluble diluent is a polyol or sugar

Claim 13 is a narrower composition-basis variant that uses “consisting essentially of” rather than “comprising,” while keeping the same excipient-type constraints (surfactant category + diluent category).

Condition expansion beyond the three headline diseases

The patent’s claim set then layers additional disease descriptors that remain tied to the same formulation architecture:

Mammary or prostatic fibrocystic disease (claims 34 and 46)
Alleviation / treatment framing for mammary cancer (claims 67, 79, etc.)
Benign prostatic hypertrophy (BPH) (claims 100, 112, 115, etc.)

These are drafted as method claims that still require the same formulation excipient selection.

Practical bottom line on coverage

If a competitor’s oral solid raloxifene product uses the claimed surfactant class (sorbitan fatty acid esters or polyoxyethylene sorbitan fatty acid esters) plus PVP plus a polyol/sugar diluent, it falls within the broadest independent scope (subject to other claim elements like “solid,” “orally administerable,” and any dependent limitations if asserted).

How broad is the excipient language: does it read on multiple products?

Surfactant scope: medium breadth

The claims define surfactant at the category level:

Sorbitan fatty acid ester (examples not specified in your text, but claim language captures the class)
Polyoxyethylene sorbitan fatty acid ester (this is the key route to specific embodiments)
Dependent claims then select:
- polysorbate 80 (claims 3, 7, 36, 40, 69, 73, 82, 102, 106, 115, etc.)

Impact: A large set of related excipients is captured at the category level, but litigation risk increases if the competitor uses a surfactant outside those categories (for example, different emulsifiers, non-sorbitan based surfactants, or surfactants not falling into those chemical classes).

Water-soluble diluent scope: medium breadth

The diluent is defined as:

polyol or sugar

Dependent claims then narrow:

sugar = lactose (claims 6, 39, 72, 116/117-style dependents not shown in your list but explicitly present in key dependent claims like 6, 39, 72, 115)

Impact: Many typical tablet/capsule diluents will be “polyol or sugar,” so this element is not extremely narrow unless lactose-only is needed for a particular dependent claim.

PVP scope: narrow to one polymer identity

The claims specify polyvinylpyrrolidone (including in dependent claim as cross-linked PVP for disintegrant).

This is an important gate. If the formulation uses a different polymer/disintegrant system and PVP is absent or replaced, it will avoid the literal claim language.

“Consisting essentially of” vs “comprising”

The claims split into:

comprising formulations (more permissive; additional excipients typically allowed)
consisting essentially of formulations (less permissive; additional materials cannot materially affect the basic and novel characteristics)

From the text provided, “consisting essentially of” is used in the independent claim set (claim 13) and in corresponding fibrocystic/cancer/BPH “consisting essentially of” variants (claims 46, 79, 112, etc.).

Impact for landscape: The presence of optional extras like lubricant, disintegrant, and film coating is handled through dependent claim add-ons. Competitors can still sell “comprising” scope formulations with additional excipients and still land outside “consisting essentially of” if they are challenged.

What are the biggest dependent claim narrowing points?

The dependent claims create a ladder of specificity that matters for claim mapping and enforcement leverage.

1) Polysorbate 80 + lactose + PVP + magnesium stearate (or stearic acid) + cross-linked PVP

A repeated “tight embodiment” appears in dependent claim patterns culminating in a specific excipient package.

Example tight package appears in your text:

polysorbate 80
lactose
polyvinylpyrrolidone
magnesium stearate
(See claim 16: “consisting essentially of ... polysorbate 80, lactose, polyvinylpyrrolidone, and magnesium stearate.”)

Then dependent claims specify further:

lubricant: magnesium stearate or stearic acid
disintegrant: cross-linked polyvinylpyrrolidone
(see claim 10 and claim 43 and claim 109 patterns)

Why it matters: This is the cleanest literal-match path for generic/formulation design-around decisions: use a different lubricant, avoid lactose, or substitute the PVP system.

2) Film coating is a frequent optional narrowing element

The text includes multiple “further comprising a film coating” dependents (e.g., claims 17, 18, 19, 20, 50, 51, 52, etc.).

Impact: Film-coating presence will not usually be a strong differentiator unless the asserted claim is a dependent one.

3) Dosage form limitation: tablet or capsule

The later dependents repeatedly add:

“wherein said formulation is in the form of a tablet or capsule” (claims 21, 22, 31, 35-like, 54-58, 87-97, 120-123, etc.)

Impact: If an accused product is a different solid oral form (for example, granules in sachets), the “tablet or capsule” dependents won’t read, but the broader independent claims without that limitation might still read.

How does the claim set handle disease scope: is it strong or mostly “labeling”?

The diseases listed vary by claim family while staying formulation-defined.

Treatment vs prophylaxis vs alleviation

Across the list you provided, the claims cover:

treating (mammary tumors, prostatic tumors, osteoporosis)
treatment or prophylaxis (mammary or prostatic fibrocystic disease)
alleviating (mammary cancer, benign prostatic hypertrophy, etc.)

Impact: Disease wording broadens potential infringement theories through different clinical indication framings, but enforcement still requires the formulation excipient match.

What is the likely patent landscape role: is this a “blocking” formulation patent or narrow utility?

Based strictly on the claim text you provided, the patent’s enforcement leverage rests on formulation elements rather than:

a unique therapeutic mechanism,
a unique raloxifene dose schedule,
or a unique manufacturing method.

That places it in the formulation-use niche: it can block or burden generics that copy the excipient architecture for oral solid raloxifene-HCl while keeping PVP + the claimed surfactant category + polyol/sugar diluent.

Expected collision zones in the landscape

Within the raloxifene oral solid ecosystem, the most plausible collision occurs for:

raloxifene HCl tablets/capsules that use PVP (including cross-linked PVP)
a sorbitan / polysorbate surfactant class
sugar or polyol diluent, especially lactose
magnesium stearate lubrication (or stearic acid in some dependents)
and optionally film coating

If a competitor’s product uses a different disintegrant system (for example, starch or croscarmellose) without cross-linked PVP, they can potentially avoid the dependent claims that require cross-linked PVP.

Claim scope matrix: which elements are gating vs optional?

Claim element category	Where it appears	Literal “gate”?	Notes from claim text
Active: raloxifene hydrochloride	All independent/most dependent	Yes	Central to every claim you listed
Form: solid orally administerable	All independent/most dependent	Yes	Tablet/capsule dependents narrow further
Surfactant class	Claim 1, 13 and many dependents	Yes	sorbitan fatty acid ester or polyoxyethylene sorbitan fatty acid ester
Specific surfactant (polysorbate 80)	Many dependents	Yes (for those dependents)	Helps distinguish tighter embodiments
Polyvinylpyrrolidone	All independent/most dependent	Yes	Cross-linked PVP only in certain dependents
Diluent class	Claim 1, 13 and many dependents	Yes	polyol or sugar
Specific diluent (lactose)	Multiple dependents	Yes (for those dependents)	“sugar is lactose” appears multiple times
Lubricant and disintegrant	Added in dependents	Optional (unless asserted)	Mg stearate or stearic acid; disintegrant can be cross-linked PVP
Film coating	Added in dependents	Optional	Multiple dependent claim recurrences
Disease wording	All	Yes (if asserted)	but formulation still governs capture

Actionable “freedom-to-operate” logic derived from the claims (landscape-ready)

A formulation designer trying to avoid literal infringement would focus on changing at least one of the gating claim elements that are hardest to argue as “equivalent” at the claim-construction stage (since the claims are specific about excipient identity categories and in some cases specific excipients).

High-impact design changes (to exit the literal claim language)

Replace PVP with a different polymer/disintegrant system so the formulation does not “comprise polyvinylpyrrolidone” (especially if cross-linked PVP is required in the asserted dependent claim).
Use a surfactant outside the sorbitan fatty acid ester and polyoxyethylene sorbitan fatty acid ester classes.
Use a diluent that is not a polyol or sugar (or keep within “sugar/polyol” but change composition so the accused product cannot be mapped to the exact formulations in dependent claims such as lactose).

Mid-impact changes (mainly protect against dependent-claim assertions)

Switch polysorbate 80 to a different member of (or outside) the surfactant class.
Switch lactose to a different sugar or polyol.
Swap magnesium stearate for stearic acid (or vice versa) to attack the specific package in dependents like claim 16 and related lubricant/disintegrant claim ladders.
Use a different lubrication/disintegrant approach to avoid cross-linked PVP where that is explicitly claimed.

What is the claim set telling you about the “basic and novel characteristics” (for “consisting essentially of” claims)?

Where consisting essentially of is used (notably claim 13 and the corresponding dependent independent claim families), the patent emphasizes a closed excipient package anchored on:

raloxifene hydrochloride
a surfactant limited to the defined sorbitan/polyoxyethylene sorbitan class (or specifically polysorbate 80 in tighter dependents)
PVP
polyol/sugar diluent (or lactose in tighter dependents)
and then in tighter dependents: magnesium stearate and disintegrant specifics

That drafting suggests the “basic and novel characteristics” are the formulation excipient selection, not the therapeutic protocol.

For landscape mapping, that means competitors should treat “consisting essentially of” claims as more sensitive to added excipients that could be argued to materially affect the excipient system, beyond just adding a standard lubricant or coating.

Key Takeaways

US 5,972,383 is a formulation-defined method patent for oral solid raloxifene HCl, where infringement is driven by excipient selection, not by a unique clinical protocol.
Claim 1 is the broadest entry point: it covers treatment of mammary tumors, prostatic tumors, or osteoporosis using an oral solid formulation comprising raloxifene HCl + PVP + surfactant (sorbitan fatty acid ester or polyoxyethylene sorbitan fatty acid ester) + polyol or sugar diluent.
Dependent claims narrow to polysorbate 80 and lactose and then further to specific lubricant/disintegrant and film coating.
The most credible “avoidance” strategies in the landscape are excipient-level: remove/replace PVP, use a surfactant outside the sorbitan/polyoxyethylene sorbitan classes, or change the diluent beyond polyol/sugar or beyond lactose for the tight embodiments.
Disease wording expands the attack surface, but it does not replace excipient matching. Formulation mapping is the dominant determinant of infringement exposure.

FAQs

1) Does this patent claim raloxifene itself or a new therapeutic?

It claims methods of treating or alleviating conditions using oral solid formulations of raloxifene hydrochloride. The novelty asserted is in the formulation excipient combination, not the drug molecule.

2) What excipients are central to independent claim 1?

Independent claim 1 requires raloxifene hydrochloride, a surfactant limited to sorbitan fatty acid ester or polyoxyethylene sorbitan fatty acid ester, polyvinylpyrrolidone, and a water-soluble diluent that is polyol or sugar.

3) Are polysorbate 80 and lactose required to infringe?

Not for the broadest claim 1. Polysorbate 80 and lactose appear in dependent claims that narrow scope. They are required only if an asserted claim depends on those limitations.

4) If a competitor uses a film coating, is that automatically infringing?

Film coating is typically introduced through dependent claims (“further comprising a film coating”). Film coating alone does not determine infringement unless the asserted claim includes that limitation.

5) Which element is most likely to be the easiest design-around?

From a claim-mapping perspective, changing or removing polyvinylpyrrolidone from the formulation is a direct way to avoid the literal “comprising polyvinylpyrrolidone” language, especially where dependent claims require cross-linked PVP.

References

[1] United States Patent and Trademark Office (USPTO). US 5,972,383 (Raloxifene hydrochloride oral solid formulation methods; claim set as provided).

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Details for Patent: 5,972,383

Summary for Patent: 5,972,383