Title of Invention	A METHOD FOR PREPARING A PHARMACEUTICAL PREPARATION COMPRISING FLUCONAZOLE
Abstract	A pharmaceutical preparation suitable for oral administration is disclosed. The composition comprises; a core; and a coating which comprises an effective amount of fluconazole; an emulsifier; a binder; and a solid phase acid; wherein the solid phase acid is selected from atleast one of maleic acid, succininc acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid. The in vitro dissolution, as well as the in vivo absorption of the fluconazole dosage form of the present invention is faster and more consistent.

Title of Invention

A METHOD FOR PREPARING A PHARMACEUTICAL PREPARATION COMPRISING FLUCONAZOLE

Abstract

A pharmaceutical preparation suitable for oral administration is disclosed. The composition comprises; a core; and a coating which comprises an effective amount of fluconazole; an emulsifier; a binder; and a solid phase acid; wherein the solid phase acid is selected from atleast one of maleic acid, succininc acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid. The in vitro dissolution, as well as the in vivo absorption of the fluconazole dosage form of the present invention is faster and more consistent.

Full Text	FORM 2 THE PATENTS ACT, 1970 (39 of 1970) & The Patent Rules, 2003 COMPLETE SPECIFICATION (See section 10 and rule 13) TITLE OF THE INVENTION "IMPROVED FORMULATIONS OF FLUCONAZOLE" We, BA RESEARCH INDIA LIMITED, of BA Research House, Opposite "Pushparaj Towers", Nr. Judges Bungalows, Bodakdev, Ahmedabad- 380054, Gujarat, India. The following specification particularly describes the nature of the invention and the manner in which it is to be performed: 1 BA_FORMUL_00l_compl FIELD OF INVENTION The present invention relates to pharmaceutical dosage forms of Fluconazole. The in vitro dissolution, as well as the in vivo absorption of the fluconazole dosage form of the present invention is faster and more consistent. BACKGROUND OF THE INVENTION Fluconazole is an important representative of the wide spectrum triazole antifungal medicinal active ingredients, which is mainly administered orally. It is described in in U.S. Pat. No. 4,404,216. Chemically Fluconazole is 2,4-difluoro-(a), (o)-bis-(lH-l, 2,4-triazole-l-yl-methyl)- benzylalcohol. Fluconazole is white, crystalline solid, which is poorly soluble in water. Fluconazole is administered in the therapy in form of tablets or capsules in strengths of 50 mg, 100mg,l50 mg or 200 mg. Fluconazole is used extensively to treat a wide range of Candida infections. In particular, it is widely used in connection with therapy for oropharyngeal candidiasis in patients with advanced HIV infection and AIDS. Commercially available fluconazole containing medicinal preparations either contains i) lactose, maize starch, magnesium stearate, silicone dioxide, sodium lauryl sulfate; or ii) microcrystalline cellulose, anhydrous calcium phosphate, povidone, sodium croscarmellose, FD4C Red No. 40 aluminium pigment, magnesium stearate as inactive excipients, depending on the type of formulations. WO 9318757, describes immediate release preparation of fluconazole, the preparation being manufactured by formulating a tablet containing menthol and obtaining a porous tablet structure by having menthol sublimed. Inappropriate dissolution rate of fluconazole preparation results in high variability of peak plasma concentration results during a bioequivalence study, which, in turn, causes inconsistency in study results. FIELD OF THE INVENTION We herein disclose a fluconazole containing medicinal formulation, which provides for the fast and consistent dissolution in vitro as well as fast and consistent absorption in vivo. Such a formulation will have the beneficial effects of short absorption time, low inter-individual difference in the time required for absorption & so on. The formulations of the present invention may be in the form of a tablet, pellets, granules, capsules or granules enclosed in a capsule. In a preferred embodiment, the formulation is in the form of a capsule. 2 BA_FORMUL_00l_compi DETAILED DESCRIPTION The present invention describes improved formulations of fluconazole having improved dissolution and in vivo absorption profile. The pharmaceutical preparations may be preferably in the form of pellets or granules which can be further encapsulated. The pharmaceutical formulation of fluconazole comprises of a core coated with the drug emulsion layer. Optionally, polyethylene glycol (PEG) 20,000 may be coated onto the emulsion layer which acts as a protective coating. The core may be spherical in shape. Suitable cores may be those commercially available. Suitable cores may be selected from, but are not limited to, sucrose, lactose, starch, talc, or microcrystalline cellulose or a combination thereof. Optionally, in another embodiment, polyvinyl pyrrolidone (PVP K-30) may be used as a plasticizer in combination with the core materials. The preferred weight ratio between the core and the drug is I : 0.2-0.6. The core is prepared as per techniques known. In one such embodiment, the core is prepared by - dissolving PVP in suitable alcohols such as propanol, isopropanol and the like; - mixing the starch and talc together; - sucrose is taken in a suitable fluidized bed; - spraying the PVP solution on the sucrose while simultaneously mixing the it with the starch-talc mixture; - drying the wet core The drug emulsion layer comprises of fluconazole in combination with an emulsifier, a binder, and a solid phase acid. The drug is first dissolved in an organic solvent(s). Examples of the organic solvents include, but are not limited to, methylene chloride, ethanol, and isopropanol. The preferred organic solvents are a combination of methylene chloride and ethanol. Suitable emulsifier include, but are not limited to, Poloxamer 188, polysorbate such as Tween 80, sodium lauryl sulfate, phospholipids and the like or their suitable mixtures; Suitable binders include, but are not limited to, polyvinyl pyrrolidone (PVP), hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), and methylcellulose (MC). Suitable solid phase acid may be selected from, but are not limited to, maleic acid, succininc acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid and the like or their suitable mixtures. The preferred weight percentage of emulsifiers is about 0.005-5%, by weight of the total pharmaceutical preparation. The preferred weight percentage of suitable solid phase acid is about 0.005-6% of the total pharmaceutical preparation. 3 BA_FORMUL_001_compl The manufacturing procedure for making the drug emulsion layer is as follows: (a) mixing the solid phase acid with a suitable alcohol; (b) adding the emulsifier to (a), & dissolving it; (c) adding the binder to (b), to form an emulsion solution; and (d) adding fluconazole to the emulsion solution of (c), stirring till the drug is evenly distributed in the emulsion solution. This is followed by adding methylene chloride to the drug-containing emulsion solution, stirring until the drug is completely dissolved to form the drug emulsion layer. The present pharmaceutical compositions are produced by spraying the drug emulsion layer onto the cores prepared above. Optionally, PEG 2000 dissolved in suitable solvent(s) such as suitable alcohols such as ehtanol, propanol, isopropanol and the like, methylene chloride and the like alone or in combination is spray coated over the emulsion layer. The granules/pellets were in a preferred embodiment filled into capsules after optionally being admixed with suitable auxilliary and/or filling agents and subsequent homogenization. The following working examples describe the formulation of the present invention in greater details. However, the examples are meant for illustrative purpose only and should not be construed to limit the scope of the invention in any way. Example 1 a) Preparation of the core: The core was prepared with the following ingredients: Table 1: Ingredients Amounts PVP K-30 20 g Propanol 150 ml Distilled water 120 ml Sucrose 200 g Starch 400 g Talc 450 g The core was prepared by dissolving PVP K-30 in 150 ml of propanol and water as required till an emulsion is formed. Separately the starch and sucrose are mixed together. Finally sucrose is taken in a fluidized bed granulator and the PVPK emulsion is sprayed onto it while 4 BA_FORMUL_001_compl simultaneously adding the starch-talc mixture to the sucrose, to form the cores. The cores were further dried in air. b) Drug emulsion layer: Table la: Ingredients Amount Fluconazole 273 g Poloxamer 188 2.4 g Maieic acid 2.38 g HPMC 410g Ethanol 7450 ml The drug emulsion solution was prepared by mixing the DL-malic acid with 7900 ml of ethanol until the and stirring to obtain a solution. To it was added vitamin E PEG succinate and stirred till completely dissolved. Then, HPMC was added to the resultant solution, to which 273 g of fluconazole was added. The pharmaceutical composition of Example 1 was prepared by putting 456.2 g of the cores as described in (A) into the fluidized bed granulator. The cores were then spray-coated with the aerosolized drug emulsion solution of (B). After drying, spheres with an outer drug layer were obtained. Example 2 The pharmaceutical composition was prepared by the process described in Example 1 with the following composition: Table 2: Ingredients Amount Core 456 g The Emulsion layer Fluconazole 273 g The Emulsion layer Fluconazole 350 g HPMC 4l0g Ethanol 223 ml Methylene chloride 212ml 5 BAJORMUL_001_compl The core and the emulsion layer was prepared as per the process described in Example 1 above and subsequently the pharmaceutical formulation was prepared according to the process described therein. Example 3 The pharmaceutical composition was prepared by the process described in Example 1 with the following composition Table 3: Ingredients Amount Core 1050 g The Emulsion layer Fluconazole 350 g Poloxamer 188 96 g Malic acid 78.80 g HPMC 176 g g Ethanol 5900 ml Methylene chloride 3900 ml The pharmaceutical composition was prepared according to the general process described in Example 1. Dissolution test: In order to demonstrate the improved efficacy of the present formulation, in vitro dissolution profile and in vivo absorption of fluconazole capsules of 200 mg strength prepared according to Example 1 are compared with commercially available flucanozole (Diflucan) capsules prepared by originator Pfizer. The test was performed in paddle apparatus according to Ph.Eur. at 50 rpm. The dissolving medium was 500 ml 0.1 M HC1. Samples were analyzed by HPLC. Results of in vitro dissolution tests show that the capsules exhibit signiflcanty higher dissolution rate in the initial 30 minutes of dissolution compared to the original preparation (- 93% for the capsules of the present invention compared to -86% for Diflucan). Pharmacokinetic study: In vivo dissolution differences between said between the aforesaid two preparations were also demonstrated in a single dose, crossover, randomized comparative pharmacokinetic study performed in 27 healthy volunteers. 6 BA_FORMUL_001_compl It was found that - 77.8% subjects achieved Tmax earlier in test product compare to reference product; - Max. Plasma con. of 40.7% subjects are less in test product compare to ref product; - 60% of subjects have higher Cmax compare to ref product Thus, it was found that among the test population, 55.6% of subjects had earlier Tmax and higher Cmax in test product compare to reference product thereby demonstrating that the absorption rate of the present formulation has significantly improved over the test product. While the invention has been described by way of examples and in terms of the preferred embodiments, it is to be understood that the invention is not limited to the disclosed embodiments. On the contrary, it is intended to cover various modifications as would be apparent to those skilled in the art. Therefore, the scope of the appended claims should be accorded the broadest interpretation so as to encompass all such modifications. 7 B A_FORM U L_001 _compl We claim 1. A pharmaceutical preparation suitable for oral administration, comprising: - a core; and - a coating which comprises an effective amount of fluconazole; an emulsifier; a binder; and a solid phase acid; wherein the solid phase acid is selected from atleast one of maleic acid, succininc acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid. 2. The pharmaceutical preparation according to claim 1, wherein said emulsifier is selected from the group comprising Poloxamer 188, polysorbate such as Tween 80, sodium lauryl sulfate, phospholipids or their suitable combinations. 3. The pharmaceutical preparation according to claim 1 or 2, wherein said binder is atleast one selected from the group comprising of polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxypropyl methylcellulose and methylcellulose. 4. The pharmaceutical preparation according to claims 1-3, further comprising a protective layer. 5. The pharmaceutical preparation according to claims 1-4, wherein said protective layer comprises polyethylene glycol. 6. The pharmaceutical preparation according to claims 1-5, wherein said core comprises at least one selected from the group consisting of sucrose, lactose, starch, talc, and microcrystalline cellulose. 7. The pharmaceutical preparation according to claims 1-6, further comprising polyvinyl pyrrolidone (PVP K-30) as a plasticizer. 8. A method for making the pharmaceutical preparation according to claim 1, comprising: i) obtaining said core; ii) mixing the solid phase acid with a suitable alcohol; iii) mixing into the above the said emulsifier with said binder to form an emulsion; iv) mixing fluconazole and an organic solvent with said emulsion to form a drug emulsion; and v) spraying said drug emulsion onto said core. 9. The method according to claim 8, further comprising of coating a protective layer onto said drug emulsion. 8 BA_FORMUL_00l_compl ABSTRACT A pharmaceutical preparation suitable for oral administration is disclosed. The composition comprises: a core; and a coating which comprises an effective amount of fluconazole; an emulsifier; a binder; and a solid phase acid; wherein the solid phase acid is selected from atleast one of maleic acid, succininc acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid. The in vitro dissolution, as well as the in vivo absorption of the fluconazole dosage form of the present invention is faster and more consistent. 9

Full Text

FORM 2
THE PATENTS ACT, 1970 (39 of 1970)
&
The Patent Rules, 2003
COMPLETE SPECIFICATION
(See section 10 and rule 13)
TITLE OF THE INVENTION
"IMPROVED FORMULATIONS OF FLUCONAZOLE"
We, BA RESEARCH INDIA LIMITED, of BA Research House, Opposite "Pushparaj Towers", Nr. Judges Bungalows, Bodakdev, Ahmedabad- 380054, Gujarat, India.
The following specification particularly describes the nature of the invention and the manner in which it is to be performed:
1

BA_FORMUL_00l_compl
FIELD OF INVENTION
The present invention relates to pharmaceutical dosage forms of Fluconazole. The in vitro dissolution, as well as the in vivo absorption of the fluconazole dosage form of the present invention is faster and more consistent.
BACKGROUND OF THE INVENTION
Fluconazole is an important representative of the wide spectrum triazole antifungal medicinal active ingredients, which is mainly administered orally. It is described in in U.S. Pat. No. 4,404,216.
Chemically Fluconazole is 2,4-difluoro-(a), (o)-bis-(lH-l, 2,4-triazole-l-yl-methyl)-
benzylalcohol. Fluconazole is white, crystalline solid, which is poorly soluble in water.
Fluconazole is administered in the therapy in form of tablets or capsules in strengths of 50
mg, 100mg,l50 mg or 200 mg. Fluconazole is used extensively to treat a wide range of
Candida infections. In particular, it is widely used in connection with therapy for
oropharyngeal candidiasis in patients with advanced HIV infection and AIDS.
Commercially available fluconazole containing medicinal preparations either contains
i) lactose, maize starch, magnesium stearate, silicone dioxide, sodium lauryl sulfate; or
ii) microcrystalline cellulose, anhydrous calcium phosphate, povidone, sodium
croscarmellose, FD4C Red No. 40 aluminium pigment, magnesium stearate as inactive excipients, depending on the type of formulations.
WO 9318757, describes immediate release preparation of fluconazole, the preparation being manufactured by formulating a tablet containing menthol and obtaining a porous tablet structure by having menthol sublimed.
Inappropriate dissolution rate of fluconazole preparation results in high variability of peak plasma concentration results during a bioequivalence study, which, in turn, causes inconsistency in study results.
FIELD OF THE INVENTION
We herein disclose a fluconazole containing medicinal formulation, which provides for the fast and consistent dissolution in vitro as well as fast and consistent absorption in vivo. Such a formulation will have the beneficial effects of short absorption time, low inter-individual difference in the time required for absorption & so on.
The formulations of the present invention may be in the form of a tablet, pellets, granules, capsules or granules enclosed in a capsule. In a preferred embodiment, the formulation is in the form of a capsule.
2

BA_FORMUL_00l_compi
DETAILED DESCRIPTION
The present invention describes improved formulations of fluconazole having improved
dissolution and in vivo absorption profile.
The pharmaceutical preparations may be preferably in the form of pellets or granules which
can be further encapsulated.
The pharmaceutical formulation of fluconazole comprises of a core coated with the drug
emulsion layer. Optionally, polyethylene glycol (PEG) 20,000 may be coated onto the
emulsion layer which acts as a protective coating. The core may be spherical in shape.
Suitable cores may be those commercially available. Suitable cores may be selected from, but
are not limited to, sucrose, lactose, starch, talc, or microcrystalline cellulose or a combination
thereof. Optionally, in another embodiment, polyvinyl pyrrolidone (PVP K-30) may be used
as a plasticizer in combination with the core materials. The preferred weight ratio between the
core and the drug is I : 0.2-0.6.
The core is prepared as per techniques known. In one such embodiment, the core is prepared
by
- dissolving PVP in suitable alcohols such as propanol, isopropanol and the like;
- mixing the starch and talc together;
- sucrose is taken in a suitable fluidized bed;
- spraying the PVP solution on the sucrose while simultaneously mixing the it with the starch-talc mixture;
- drying the wet core
The drug emulsion layer comprises of fluconazole in combination with an emulsifier, a
binder, and a solid phase acid.
The drug is first dissolved in an organic solvent(s). Examples of the organic solvents include,
but are not limited to, methylene chloride, ethanol, and isopropanol. The preferred organic
solvents are a combination of methylene chloride and ethanol.
Suitable emulsifier include, but are not limited to, Poloxamer 188, polysorbate such as Tween
80, sodium lauryl sulfate, phospholipids and the like or their suitable mixtures;
Suitable binders include, but are not limited to, polyvinyl pyrrolidone (PVP), hydroxypropyl
cellulose (HPC), hydroxypropyl methylcellulose (HPMC), and methylcellulose (MC).
Suitable solid phase acid may be selected from, but are not limited to, maleic acid, succininc
acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid and the like or their
suitable mixtures. The preferred weight percentage of emulsifiers is about 0.005-5%, by
weight of the total pharmaceutical preparation. The preferred weight percentage of suitable
solid phase acid is about 0.005-6% of the total pharmaceutical preparation.
3

BA_FORMUL_001_compl
The manufacturing procedure for making the drug emulsion layer is as follows:
(a) mixing the solid phase acid with a suitable alcohol;
(b) adding the emulsifier to (a), & dissolving it;
(c) adding the binder to (b), to form an emulsion solution; and
(d) adding fluconazole to the emulsion solution of (c), stirring till the drug is evenly distributed in the emulsion solution. This is followed by adding methylene chloride to the drug-containing emulsion solution, stirring until the drug is completely dissolved to form the drug emulsion layer.
The present pharmaceutical compositions are produced by spraying the drug emulsion layer
onto the cores prepared above.
Optionally, PEG 2000 dissolved in suitable solvent(s) such as suitable alcohols such as
ehtanol, propanol, isopropanol and the like, methylene chloride and the like alone or in
combination is spray coated over the emulsion layer.
The granules/pellets were in a preferred embodiment filled into capsules after optionally
being admixed with suitable auxilliary and/or filling agents and subsequent homogenization.
The following working examples describe the formulation of the present invention in greater
details. However, the examples are meant for illustrative purpose only and should not be
construed to limit the scope of the invention in any way.
Example 1
a) Preparation of the core:
The core was prepared with the following ingredients:
Table 1:

Ingredients Amounts
PVP K-30 20 g
Propanol 150 ml
Distilled water 120 ml
Sucrose 200 g
Starch 400 g
Talc 450 g
The core was prepared by dissolving PVP K-30 in 150 ml of propanol and water as required till an emulsion is formed. Separately the starch and sucrose are mixed together. Finally sucrose is taken in a fluidized bed granulator and the PVPK emulsion is sprayed onto it while
4

BA_FORMUL_001_compl
simultaneously adding the starch-talc mixture to the sucrose, to form the cores. The cores were further dried in air.
b) Drug emulsion layer: Table la:

Ingredients Amount
Fluconazole 273 g
Poloxamer 188 2.4 g
Maieic acid 2.38 g
HPMC 410g
Ethanol 7450 ml
The drug emulsion solution was prepared by mixing the DL-malic acid with 7900 ml of ethanol until the and stirring to obtain a solution. To it was added vitamin E PEG succinate and stirred till completely dissolved. Then, HPMC was added to the resultant solution, to which 273 g of fluconazole was added.
The pharmaceutical composition of Example 1 was prepared by putting 456.2 g of the cores as described in (A) into the fluidized bed granulator. The cores were then spray-coated with the aerosolized drug emulsion solution of (B). After drying, spheres with an outer drug layer were obtained.
Example 2
The pharmaceutical composition was prepared by the process described in Example 1 with the following composition:
Table 2:

Ingredients Amount
Core 456 g
The Emulsion layer
Fluconazole 273 g
The Emulsion layer
Fluconazole 350 g
HPMC 4l0g
Ethanol 223 ml
Methylene chloride 212ml
5

BAJORMUL_001_compl
The core and the emulsion layer was prepared as per the process described in Example 1 above and subsequently the pharmaceutical formulation was prepared according to the process described therein.
Example 3
The pharmaceutical composition was prepared by the process described in Example 1 with the following composition
Table 3:

Ingredients Amount
Core 1050 g
The Emulsion layer
Fluconazole 350 g
Poloxamer 188 96 g
Malic acid 78.80 g
HPMC 176 g g
Ethanol 5900 ml
Methylene chloride 3900 ml
The pharmaceutical composition was prepared according to the general process described in Example 1.
Dissolution test:
In order to demonstrate the improved efficacy of the present formulation, in vitro dissolution
profile and in vivo absorption of fluconazole capsules of 200 mg strength prepared according
to Example 1 are compared with commercially available flucanozole (Diflucan) capsules
prepared by originator Pfizer. The test was performed in paddle apparatus according to
Ph.Eur. at 50 rpm. The dissolving medium was 500 ml 0.1 M HC1. Samples were analyzed by
HPLC.
Results of in vitro dissolution tests show that the capsules exhibit signiflcanty higher
dissolution rate in the initial 30 minutes of dissolution compared to the original preparation (-
93% for the capsules of the present invention compared to -86% for Diflucan).
Pharmacokinetic study:
In vivo dissolution differences between said between the aforesaid two preparations were also
demonstrated in a single dose, crossover, randomized comparative pharmacokinetic study
performed in 27 healthy volunteers.
6

BA_FORMUL_001_compl
It was found that
- 77.8% subjects achieved Tmax earlier in test product compare to reference product;
- Max. Plasma con. of 40.7% subjects are less in test product compare to ref product;
- 60% of subjects have higher Cmax compare to ref product
Thus, it was found that among the test population, 55.6% of subjects had earlier Tmax and higher Cmax in test product compare to reference product thereby demonstrating that the absorption rate of the present formulation has significantly improved over the test product. While the invention has been described by way of examples and in terms of the preferred embodiments, it is to be understood that the invention is not limited to the disclosed embodiments. On the contrary, it is intended to cover various modifications as would be apparent to those skilled in the art. Therefore, the scope of the appended claims should be accorded the broadest interpretation so as to encompass all such modifications.
7

B A_FORM U L_001 _compl
We claim
1. A pharmaceutical preparation suitable for oral administration, comprising:
- a core; and
- a coating which comprises an effective amount of fluconazole; an emulsifier; a binder; and a solid phase acid; wherein the solid phase acid is selected from atleast one of maleic acid, succininc acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid.
2. The pharmaceutical preparation according to claim 1, wherein said emulsifier is selected from the group comprising Poloxamer 188, polysorbate such as Tween 80, sodium lauryl sulfate, phospholipids or their suitable combinations.
3. The pharmaceutical preparation according to claim 1 or 2, wherein said binder is atleast one selected from the group comprising of polyvinyl pyrrolidone, hydroxypropyl cellulose, hydroxypropyl methylcellulose and methylcellulose.
4. The pharmaceutical preparation according to claims 1-3, further comprising a protective layer.
5. The pharmaceutical preparation according to claims 1-4, wherein said protective layer comprises polyethylene glycol.
6. The pharmaceutical preparation according to claims 1-5, wherein said core comprises at least one selected from the group consisting of sucrose, lactose, starch, talc, and microcrystalline cellulose.
7. The pharmaceutical preparation according to claims 1-6, further comprising polyvinyl pyrrolidone (PVP K-30) as a plasticizer.
8. A method for making the pharmaceutical preparation according to claim 1, comprising:
i) obtaining said core;
ii) mixing the solid phase acid with a suitable alcohol;
iii) mixing into the above the said emulsifier with said binder to form an emulsion;
iv) mixing fluconazole and an organic solvent with said emulsion to form a drug
emulsion; and
v) spraying said drug emulsion onto said core.
9. The method according to claim 8, further comprising of coating a protective layer onto
said drug emulsion.

8

BA_FORMUL_00l_compl
ABSTRACT
A pharmaceutical preparation suitable for oral administration is disclosed. The composition comprises: a core; and a coating which comprises an effective amount of fluconazole; an emulsifier; a binder; and a solid phase acid; wherein the solid phase acid is selected from atleast one of maleic acid, succininc acid, malic acid, citric acid, ascorbic acid, and alginic acid, tartaric acid. The in vitro dissolution, as well as the in vivo absorption of the fluconazole dosage form of the present invention is faster and more consistent.
9

Documents:

http://ipindiaonline.gov.in/patentsearch/GrantedSearch/viewdoc.aspx?id=Q44rINCYJ2b7lUByezehUg==&loc=vsnutRQWHdTHa1EUofPtPQ==

« Previous Patent

Next Patent »

Patent Number

272779

Indian Patent Application Number

523/MUM/2007

PG Journal Number

18/2016

Publication Date

29-Apr-2016

Grant Date

26-Apr-2016

Date of Filing

22-Mar-2007

Name of Patentee

CLIANTHA RESEARCH LIMITED

Applicant Address

BA RESEARCH HOUSE, OPPOSITE "PUSHPARAJ TOWERS" NR.JUDGES BUNGALOWS, BODAKDEV, AHMEDABAD-380 054, GUJARAT, INDIA.

Inventors:

#	Inventor's Name	Inventor's Address
1	SHARMA, NAVEEN	BA RESEARCH INDIA LIMITED, BA RESEARCH HOUSE, OPPOSITE "PUSHPARAJ TOWERS" NR.JUDGES BUNGALOWS, BODAKDEV, AHMEDABAD 380 054

PCT International Classification Number

A61K31/4196

PCT International Application Number

N/A

PCT International Filing date

PCT Conventions:

#	PCT Application Number	Date of Convention	Priority Country
1			NA