FORM 2
THE PATENT ACT 1970
(39 of 1970)
&
The Patents Rules, 2003
COMPLETE SPECIFICATION
(See section 10 and rule13)
1. TITLE OF THE INVENTION:
SINGLE NEEDLE DEVICE AS A MICRONEEDLE
2. APPLICANT (S)
(a) NAME: WOCKHARDT LTD.
(b) NATIONALITY: INDIAN
(c) ADDRESS: D-4, M.I.D.C. Area, Chikalthana, Aurangabad - 431210
(M.S) India
3. PREAMBLE TO THE DESCRIPTION
The present invention provides a device for the delivery of biological material across the biological tissue with minimal or no pain, damage and irritation to the tissue. The device comprises one microneedle attached to a needle cap.
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The following specification particularly describes the invention and the manner in which it is to be performed.


4. Description
The present invention provides a device for the delivery of biological material across the biological tissue with minimal or no pain, damage and irritation to the tissue. The device comprises one microneedle attached to a needle cap wherein the needle cap is attached to an injection pen device.
Dosed biological material delivery devices, often referred to as "injection pen device" are commonly used for routine injection of biological materials.
Dosed biological material delivery devices are a preferred means of delivery wherever the volume of biological material delivered needs to be variable but accurate, critical, small and needs to be administered very frequently. Hence, "injection pen device" refer generally to any and all free- standing portable device containing a plurality of doses of a biological material liquid which can be operated by a patient for self injection to deliver metered doses of the liquid to the patient's body on a plurality of occasions.
The term "microneedle" refers to a device for transdermal or intradermal delivery or removal of fluids without many of the risks associated with standard syringes. Microneedle is designed to pierce the stratum corneum skin barrier layer in a minimally invasive and pain-free manner to provide transient pathways for the delivery of macromolecules to the underlying skin epidermis. Since the needle is short, it does not reach the nerve-rich regions of the lower parts of the skin. As a consequence, the stimulus caused by microneedle insertion into the skin is weak and cause less pain.
EP Patent No. 1 880 741 Al discloses a method for directly delivering whereby a substance is introduced into an intradermal space within mammalian skin which involves administering the substance through at least one small gauge hollow needle having an outlet with an exposed height between 0 and 1 mm.
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The present inventors while working for suitable micro needle device design have found that it could be possible to effect modification of conventional hypodermic needle to function as a microne6dle device. The present invention provides a device wherein the length of the conventional hypodermic needle attached to a cap can be reduced to function as a microneedle.
The conventional hypodermic needle attached to a cap will have varying lengths. The projected needle length of the hypodermic needle from the cap outlet can be anywhere between 6mm to 9mm. The 30 gauge or 31 gauge conventional needles have outer diameters of 305 urn and 254 um and inner diameter of around 200 jam.
The various studies on pain perception reveal the following facts.
Upto 150 urn length (pain is almost insignificant)
From 150 µm to 200 µm (weak to very mild perception)
From 500 µm- 750 µm and a width of 50 µm ( 5 - 10% of the sensation produced by a
26 gage hypodermic needle) i.e. upper end for pain perception commencement can be
considered as 500 µm.
This device manufacture requires modification to be effected in the manufacturing process so as to produce needle whose projected out lengths could be less than 1000 µm or of desired length.
One of the aspects of present invention provides device for transport of biological materials across biological barrier wherein the device comprises one hollow needle attached to a needle cap to function as microneedle.
As used herein, the term "hollow" means having one annular bore or channel through the interior of the microneedle, having a diameter sufficiently large to permit passage of fluid and/or solid materials through the microneedle.
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"Biological Material Storage" may mean a syringe or cartridge containing suitable pharmaceutical substance.
As used herein, the term " biological material " refers to an agent which possesses therapeutic, prophylactic, or diagnostic properties in vivo, for example when administered to an animal, including mammals, such as humans. The biological material is selected from the group comprising of peptides, proteins, carbohydrates, nucleic acid molecules, lipids and other pharmaceutically active ingredients or combinations thereof.
The pharmaceutically active ingredients may be one or more of anesthetics, analgesics, anti bacterials, anti virals, antiadrenergics, antiamebics, antianginals, antiarrhythmics, antibiotics, anticoagulants, anticonvulsants, antidepressants, antidiabetics, antidiuretics, antidyskinetics, antiemetics, antifungals, antihistaminics, antihyperparathyroids, antihypertensives, antiinflammatories, antimigraines, antineoplastics, antineoplastics, antiprotozoals, antipsychotics, antispasmodics, antithrombotics, antiulceratives, anxiolytics, astringents, bone resorption inhibitors, bronchodilators, cardiotonics, cholinergics, diaprostic agents, diuretics, hormones, steriods, hydrochloride as anineoplastic, hypnotics, immunomodulators, immunosuppresants, mucolytics, muscle relaxants, neuromuscular blocking agents, oxytocics, vasodilator and the like.
The pharmaceutically active ingredients may further include one or more ketamine, chloroprocaine hydrochloride, alfentanil, amikacin, abacavir, bretylium tosylate, metronidazole, diltiazem hydrochloride, ciprofloxacin, dextran sulfate sodium, fosphenytoin sodium, rubidium chloride, insulin, desmopressin acetate, haloperidol lactate, dimenhydrinate, abelcet, diphenhydramine hydrochloride, paricalcitol, diltiazem hydrochloride, ketorolac, dihydroergotamine mesylate, mitoxantrone hydrochloride, leuprolide acetate, metronidazole, aripiprazole, dicyclomine hydrochloride, dipyridamole, cimetidine hydrochloride, diazepam, zinc chloride, zoledronic acid, aminophyllin, digoxin, pyridostigmine bromide, diatrizoate sodium, furosemide, estrogen, androgen and the like, steriods such as glucocorticoid and the like, mechlorethamine hydrochloride,
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etomidate, mitoxantrone hydrochloride, tacrolimus, acetylcysteine, baclofen, vecuronium bromide, oxytocin nitroglyceine and the like.
In another embodiment of the invention, wherein the outer diameter of microneedle varies from about 200 µm to 350 µm and length of the microneedle is in the range of 100 µm to 999 µm.
The length of the microneedle typically is between about 10 µm and 1 mm, preferably between 100 µm and 500 µm, and more preferably between 150 µm and 350 µm. The length is selected for the particular application, accounting for both an inserted and un inserted portion. In transdermal applications, the "insertion depth" of the microneedle is preferably less than about 500 µm, so that insertion of the microneedles into the skin does not penetrate into the dermis, thereby avoiding contacting nerves which may cause pain. In such applications, the actual length of the microneedle typically is longer, since the portion of the microneedle distal the tip may not be inserted into the skin; the uninserted length depends on the particular device design and configuration. The actual (overall) height or length of microneedle should be equal to the insertion depth plus the un inserted length.
Suitable materials for manufacturing microneedle include one or more metals. The metals can be selected from the group comprising of pharmaceutical grade stainless steel, gold, titanium, nickel, iron, tin, chromium, copper, palladium, platinum, alloys, silicon, silicon dioxide, and combinations thereof.
In another embodiment of the present invention, the biological material is selected from the group comprising of peptides, proteins, carbohydrates, nucleic acid molecules, lipids and other pharmaceutically active ingredients and combinations thereof.
A pen device that would be used for the administration of set dose of the biological material is detailed below. The pen device can be used for dose titration if a


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predetermined dose adjustment may be attached. The pen used for precise administration of dose is described in detail with references to the drawing.
Figure 1 shows mechanism for discharge of biological material through micro needle attached to a pen device - Existing attachment of needle and needle cap
Figure 2 shows mechanism for discharge of biological material through micro needle attached to a pen device - Proposed microneedle attachment to needle cap
Figure 1 shows the pen device (1) where in present needle and a cap (5) that would be associated with a pen. Needle cap (5) has an internal thread (6) that mates with the cartridge or syringe (2) and needle (9) extends on both sides of the needle cap (5). On attachment of needle cap (5) to the cartridge or syringe (2) by screw mechanism, needle (9) which extends on to the internal of the cap pierces the rubber seal 93) of the cartridge or syringe (2) and establishes contact with the biological material in the cartridge or syringe (2). Needle cap (5) is removed and set dosage of the biological material is administered to a patient.
Figure 2 shows the proposed system wherein instead of needle (9) which protrudes out of the cap is replaced by a shortened needle which acts as a microneedle.
While the present invention has been described in terms of its specific embodiments, certain modifications and equivalents will be apparent to those skilled in the art and are intended to be included within the scope of the present invention.
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WE CLAIM:
1. A device for transport of biological materials across biological barrier wherein the device comprises one hollow microneedle attached to a needle cap.
2. The device as claimed in claim 1, wherein the outer diameter of microneedle varies from about 200 microns to 350 microns and length of the microneedle is at least 100 microns.
3. The device as claimed in claim 1, wherein the suitable material for manufacturing microneedle include one or more metals.
4. The device of claim 1, wherein the biological material is selected from the group comprising one or more of peptides, proteins, carbohydrates, nucleic acid molecules, lipids and other pharmaceutically active ingredients.
Dated this 05TH day of June 2008
For Wockhardt Limited

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(Mandar Kodgule) Authorized Signatory