Ex parte Bilgic

• Decision Date: 21 September 2018
• Docket Number: 138,Application 13/692,Appeal 2017-009804
• Parties: Ex parte MAHMUT BILGIC[1] Technology Center 1600
• Court: United States Patent and Trademark Office. United States Patent and Trademark Office, Patent Trial and Appeal Board

Ex parte MAHMUT BILGIC^[1] Technology Center 1600

Appeal 2017-009804

Application 13/692, 138

United States Patent and Trademark Office, Patent Trial and Appeal Board

September 21, 2018

FILING DATE: 12/03/2012

Before DEMETRA J. MILLS, RICHARD M. LEBOVITZ, and RYAN H. FLAX, Administrative Patent Judges.

DECISION ON APPEAL

MILLS, Administrative Patent Judge.

This is an appeal under 35 U.S.C. § 134. The Examiner has rejected the claims for obviousness. We have jurisdiction under 35 U.S.C. § 6(b).

We affirm.

NATURE OF THE INVENTION

The Specification states that present inventors have "surprisingly found that when cephalosporin antibiotic and clavulanic acid are mixed with the granules comprising effervescent couple and at least one excipient in the presence of high-molecular weight PEG [polyethylene glycol], gelling or agglomeration problem of cefdinir and also [a] stability problem of clavulanic acid are eliminated." Spec. 5.

STATEMENT OF CASE

The following claim is representative.

27. An effervescent formulation comprising the combination of a cephalosporin antibiotic and clavulanic acid or pharmaceutically acceptable derivatives thereof characterized in that said formulation comprises;

10-40% by weight of a cephalosporin antibiotic

5-25% by weight clavulanic acid

20-70% by weight effervescent couple

0.2-5% by weight high molecular weight PEG and

1-20% by weight other pharmaceutically acceptable excipients with respect to the total weight of unit dose

wherein said cephalosporin antibiotic and said clavulanic acid are present in a stable and homogenously soluble form.

Cited References

Crowley	WO 9607408A1	03/14/96
Smith	EP 1034784 A2	Sept. 13, 2000
Gao	CN1850087 (A)	(Oct. 25, 2006) (English Translation).

Grounds of Rejection

1. Claims 27, 40, 41, 45 and 52-56 stand rejected under 35 U.S.C. § 112(b)or35U.S.C.§ 112, second paragraph, as being indefinite for failing to particularly point out and distinctly claim the subject matter.

2. Claims 27, 40, 41, 45 and 52-56 stand rejected under pre-AIA 35 U.S.C. § 103(a) as being unpatentable over Smith in view of Gao and Crowley.

FINDINGS OF FACT

The Examiner's findings of fact are set forth in the Final Action at pages 4-9 and are adopted in this Decision. The following findings of fact highlight certain evidence.

1. Smith teaches a composition using effervescent couple (see ¶ 27), which reads on an effervescent formulation, comprising a cephalosporin (see ¶ 11) such as disclosed (see ¶ 12) including cefixime (see ¶ 12); 10 - 60% by weight of the active materials such as salts of clavulanic acid (see ¶ 32), which reads on pharmaceutically acceptable derivative of clavulanic acid, in unit dosage form (see ¶34). Final Act. 4.

2. Smith discloses that clavulanic acid is used in formulations in combination with P-lactam antibiotics. ¶¶ 2, 11.

3. According to Smith, its antibiotic effervescent

[0035] [F]ormulations may contain 0.1 - 90% by weight, preferably from 10 - 60% by weight of the active materials, depending on the method of administration. [0036] The clavulanate may suitably be administered to the patient at a daily dosage of from 0.3 to 15 mg/kg, preferably from 0.7 to 10 mg/kg, for example from 0.7 to 7 mg/kg, of body weight. For an adult human (of approximately 70 kg body weight), from 25 to 1000 mg, preferably from 50 to 500 mg, of clavulanate expressed as its free acid equivalent may be administered daily, suitably in from 1 to 6, preferably from 2 to 4, separate doses. Higher or lower dosages may, however, be used in accordance with clinical practice. [0037] When the formulations according to the invention are presented in unit dosage form, each unit dose may suitably comprise from 12.5 to 1000 mg, preferably from 12.5 to 250 mg, of clavulanate. Each unit dose may, for example, be 12.5, 25, 50, 75, 100, 125, 150, 200, or 250 mg of clavulanate.

Smith, p. 4.

4. Smith discloses an effervescent couple such as solid carboxylic acid and an alkali metal carbonate (see ¶ 27).

5. Smith discloses a lubricant such as polyethylene glycol (see ¶ 27), which is PEG.

6. Smith discloses other conventional excipients (see ¶ 27) such as binding agents (see ¶ 27) and disintegrants (see ¶ 27), which read on other pharmaceutically acceptable excipients.

7. Smith discloses tablets formulations (see ¶ 24), which read on tablet form.

8. Smith discloses the ratio of the amount of the clavulanate to the amount of any antibacterial agent (see ¶ 38) such as cefixime (see ¶ 12) is from 1:1 to 1:12 (see ¶ 38) (Note: Providing salts of clavulanate comprise 10 - 60% by weight in unit dosage form, the cephalosporin must comprise at least 10 - 60% by weight in unit dosage form according to a proportionality of the salts of clavulanate to the cephalosporin of 1:1.)

9. According to Smith, suitable unit dosages and maximum daily dosages of any antibacterial agent used in combination with clavulanate may be determined according to the unit dosages and maximum daily dosages of the agent used conventionally (see ¶ 39); and pharmaceutical formulation (see Abstract) using an effervescent couple (see ¶ 27) containing clavulanic acid and an antibacterial agent (see Abstract) such as cefixime (see ¶ 12).

10. Gao discloses an effervescent tablet containing cefixime (Abstract). Final Act. 5.

11. The tablet of Gao wherein contains pharmaceutically-acceptable acid base pair (see Abstract) causing releasing carbon dioxide after chemical reaction (see page 3, second and third paragraphs), which reads on effervescent couple, such as citric acid (see page 3, sixth paragraph), which reads on carboxylic acid, and sodium carbonate (see page 3, ninth paragraph), which is alkali metal carbonate. Final Act. 5.

12. The acidic compound of Gao comprises 15-40% per weight of the tablet (see page 3, eighth paragraph), which reads on unit dose, and basic compound comprises 20-40% per tablet weight (see page 3, eleventh paragraph). (Note: Thus, acid-base pair comprises a total of 35-80% per weight of the tablet.) Final Act. 5.

13. Gao discloses effervescent tablets add lubricant (0.1 to 5 per weight %) (see page 4, sixth to ninth paragraphs) such as PEG 6000 (see page 4, eighth paragraph), which is a high molecular weight PEG (see page 7, second paragraph of instant specification) to ensure the preparation process of cefixime effervescent smooth resistance (see page 4, sixth paragraph); pharmaceutically-acceptable (see Abstract) binder (0.1 to 5% per weight) (see page 4, third to fourth paragraphs), which is binding agent, and disintegrating agent (0-2% weight) (see page 4, fifth to seventh paragraphs), which is disintegrant (Note: Binder and disintegrating agent are other pharmaceutically acceptable excipients which comprise a total of 0.1-7% per weight of the tablet.); use of cefixime effervescent tablets for easy storage, transport, carry, suitable for patients who cannot swallow solid dosage (see page 2, last paragraph); contain disintegrants to further accelerate the rate of disintegration of effervescent tablets (see page 4, fifth paragraph); and add a binder to facilitate the combination of each component in the effervescent tablet (see page 4, third paragraph). Final Act. 5.

14. Crowley teaches pharmaceutically acceptable salts of clavulanic acid, which is a β-lactamase inhibitor, referred as clavulanate (see page 1, second paragraph) coformulated with an antibiotic compound such as cephalosporins (see page 7, last paragraph), which is a lactamase antibiotic (see page 7, last paragraph), e.g., cefixime (see page 8, first paragraph), in a tablet (see page 9, fifth paragraph) to increase their (antibiotics) resistance to the p-lactamase enzymes produced by microorganisms (see page 1, second paragraph), thus preventing bacterial resistance. Final Act. 6.

PRINCIPLES OF LAW

In making our determination, we apply the...