The present disclosure relates generally to pharmaceutical compositions. More specifically, the disclosure is directed to an immediate release effervescent pharmaceutical composition comprising telmisartan, polyethylene glycol, citric acid, tartaric acid, sodium bicarbonate, glycine, sodium citrate and one or more pharmaceutically acceptable adjuvant or excipients.
BACKGROUND OF THE INVENTION
[0002] Background description includes information that may be useful in understanding the present invention. It is not an admission that any of the information provided herein is prior art or relevant to the presently claimed invention, or that any publication specifically or implicitly referenced is prior art. [0003] Telmisartan is an angiotensin II receptor blocker intended to treat hypertension and cardiovascular manifestations associated with diabetes. Crystalline telmisartan (4'-[2-n-propyl-4-methyl-6-(l-methylbenzimidazol-2-yl) benzimidazol-1-ylmethyl] biphenyl-2-carboxylic acid) exists in two polymorphic forms i.e. A and B. Both polymorphic forms have poor aqueous solubility of approximately 0.078 mg/mL and low solubility at the physiological pH range of 1 to 7. Telmisartan belongs to Biopharmaceutical Classification System (BCS) class II drug. This system classifies the drugs in four classes on the basis of their solubility and permeability. BCS class II represents the drugs with low solubility and high permeability. Thus, telmisartan is a drug with low solubility and high permeability.
[0004] It has been reported in patent EP2203158A2 that telmisartan is sparingly soluble in strong acids and soluble in strong bases. The solubility of drug is a critical attribute to determine efficient drug absorption. As a consequence, telmisartan formulations suffer from limited absorption profile and erratic bioavailability. Therefore, there is a requirement to provide compositions comprising the drug that help improve its solubility and therefore its bioavailability in the physiological environment.

[0005] The present disclosure provides an immediate release effervescent pharmaceutical composition of telmisartan that improves its solubility and dissolution profile.
OBJECTS OF THE INVENTION
[0006] An object of the present disclosure provides a pharmaceutical composition
comprising telmisartan that improves its solubility and dissolution profile.
[0007] An object of the present disclosure is to provide a pharmaceutical
composition comprising telmisartan that is an immediate release composition and
has effervescent properties.
[0008] Another object of the present disclosure is to provide a process of
preparation of the pharmaceutical composition.
SUMMARY OF THE INVENTION
[0009] This summary is provided to introduce a selection of concepts in a
simplified form that are further described below in Detailed Description section.
This summary is not intended to identify key features or essential features of the
claimed subject matter, nor is it intended to be used as an aid in determining the
scope of the claimed subject matter.
[0010] Aspects of the present disclosure relate to providing a composition
comprising telmisartan that improves its solubility in the physiological
environment by effervescence.
[0011] In an aspect, the present disclosure provides an effervescent
pharmaceutical composition comprising telmisartan, polyethylene glycol, citric
acid, tartaric acid, sodium citrate, glycine, sodium bicarbonate and one or more
pharmaceutically acceptable excipient(s) or adjuvant(s).
[0012] In an embodiment, the telmisartan may be crystalline or amorphous
telmisartan. In an embodiment, the telmisartan may be present in a range of about
8% to about 24% w/w of the composition.
[0013] In an embodiment, the polyethylene glycol may be selected from
polyethylene glycol 4000, polyethylene glycol 2000, polyethylene glycol 1000 or

combinations thereof. In an embodiment, the polyethylene glycol may be present
in a range of about 20% to about 40% w/w of the composition.
[0014] In an embodiment, the citric acid may be present in a range of about 2% to
about 10%) w/w of the composition.
[0015] In an embodiment, the tartaric acid may be present in a range of about 3%
to about 10%o w/w of the composition.
[0016] In an embodiment, the sodium citrate may be present in a range of about
2%o to about 8%o w/w of the composition.
[0017] In an embodiment, the sodium bicarbonate may be present in a range of
about 15%) to about 25% w/w of the composition.
[0018] In an embodiment, the glycine may be present in a range of about 10%> to
about 24%o w/w of the composition.
[0019] In an embodiment, the excipient or adjuvant may be present in a range of
about 0.1%o to about 1.0% w/w of the composition.
[0020] In an embodiment, the pharmaceutically acceptable excipient(s) or
adjuvant(s) may be selected from those well known in the art, including
lubricants, preservatives, diluents, sweetening agent, coloring agent, fillers,
glidants, or combinations thereof.
[0021] In an aspect, the present disclosure provides an effervescent
pharmaceutical formulation comprising telmisartan, polyethylene glycol, citric
acid, tartaric acid, sodium citrate, sodium bicarbonate, glycine and one or more
pharmaceutically acceptable excipient or adjuvant.
[0022] In an aspect, the present disclosure provides a process of preparing an
effervescent pharmaceutical formulation comprising telmisartan, wherein the
process comprises the steps of: (a)mixing telmisartan, polyethylene glycol, citric
acid, tartaric acid, sodium citrate, glycine and sodium bicarbonate; (b) granulating
the mixture by heating at a temperature in the range of 40-50°C; (c) cooling and
sieving to get uniform sized granules; and (d) adding and mixing one or more
pharmaceutically acceptable excipient(s) or adjuvant(s) to give the formulation;
wherein the formulation is an effervescent granules pharmaceutical formulation.

[0023] Other aspects of the invention will be set forth in the description which follows, and in part will be apparent from the description, or may be learnt by the practice of the invention.
BRIEF DESCRIPTION OF THE DRAWINGS
[0024] The following drawings form part of the present specification and are included to further illustrate aspects of the present disclosure. The disclosure may be better understood by reference to the drawings in combination with the detailed description of the specific embodiments presented herein.
[0025] Figure 1 provides the percentage drug release of telmisartan with respect to time from a composition as per an embodiment of the present disclosure and a commercially available composition.
DETAILED DESCRIPTION OF THE INVENTION
[0026] The following is a detailed description of embodiments of the disclosure. The embodiments are in such detail as to clearly communicate the disclosure. However, the amount of detail offered is not intended to limit the anticipated variations of embodiments; on the contrary, the intention is to cover all modifications, equivalents, and alternatives falling within the spirit and scope of the present disclosure as defined by the appended claims.
[0027] All publications herein are incorporated by reference to the same extent as if each individual publication or patent application were specifically and individually indicated to be incorporated by reference. Where a definition or use of a term in an incorporated reference is inconsistent or contrary to the definition of that term provided herein, the definition of that term provided herein applies and the definition of that term in the reference does not apply. [0028] Reference throughout this specification to "one embodiment" or "an embodiment" means that a particular feature, structure or characteristic described in connection with the embodiment is included in at least one embodiment. Thus, the appearances of the phrases "in one embodiment" or "in an embodiment" in various places throughout this specification are not necessarily all referring to the

same embodiment. Furthermore, the particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments.
[0029] In some embodiments, numbers have been used for quantifying weights, percentages, ratios, and so forth, to describe and claim certain embodiments of the invention and are to be understood as being modified in some instances by the term "about." Accordingly, in some embodiments, the numerical parameters set forth in the written description and attached claims are approximations that can vary depending upon the desired properties sought to be obtained by a particular embodiment. In some embodiments, the numerical parameters should be construed in light of the number of reported significant digits and by applying ordinary rounding techniques. Notwithstanding that the numerical ranges and parameters setting forth the broad scope of some embodiments of the invention are approximations, the numerical values set forth in the specific examples are reported as precisely as practicable. The numerical values presented in some embodiments of the invention may contain certain errors necessarily resulting from the standard deviation found in their respective testing measurements. [0030] Various terms as used herein are shown below. To the extent a term used in a claim is not defined below, it should be given the broadest definition persons in the pertinent art have given that term as reflected in printed publications and issued patents at the time of filing.
[0031] As used in the description herein and throughout the claims that follow, the meaning of "a," "an," and "the" includes plural reference unless the context clearly dictates otherwise. Also, as used in the description herein, the meaning of "in" includes "in" and "on" unless the context clearly dictates otherwise. [0032] Unless the context requires otherwise, throughout the specification which follow, the word "comprise" and variations thereof, such as, "comprises" and "comprising" are to be construed in an open, inclusive sense that is as "including, but not limited to."
[0033] The recitation of ranges of values herein is merely intended to serve as a shorthand method of referring individually to each separate value falling within

the range. Unless otherwise indicated herein, each individual value is incorporated into the specification as if it were individually recited herein. [0034] All methods described herein can be performed in any suitable order unless otherwise indicated herein or otherwise clearly contradicted by context. The use of any and all examples, or exemplary language (e.g. "such as") provided with respect to certain embodiments herein is intended merely to better illuminate the invention and does not pose a limitation on the scope of the invention otherwise claimed. No language in the specification should be construed as indicating any non-claimed element essential to the practice of the invention. [0035] Groupings of alternative elements or embodiments of the invention disclosed herein are not to be construed as limitations. Each group member can be referred to and claimed individually or in any combination with other members of the group or other elements found herein. One or more members of a group can be included in, or deleted from, a group for reasons of convenience and/or patentability. When any such inclusion or deletion occurs, the specification is herein deemed to contain the group as modified.
[0036] The description that follows, and the embodiments described therein, is provided by way of illustration of an example, or examples, of particular embodiments of the principles and aspects of the present disclosure. These examples are provided for the purposes of explanation, and not of limitation, of those principles and of the disclosure.
[0037] It should also be appreciated that the present disclosure can be implemented in numerous ways, including as a system, a method or a device. In this specification, these implementations, or any other form that the invention may take, may be referred to as processes. In general, the order of the steps of the disclosed processes may be altered within the scope of the invention. [0038] The headings and abstract of the invention provided herein are for convenience only and do not interpret the scope or meaning of the embodiments. [0039] The following discussion provides many example embodiments of the inventive subject matter. Although each embodiment represents a single combination of inventive elements, the inventive subject matter is considered to

include all possible combinations of the disclosed elements. Thus if one
embodiment comprises elements A, B, and C, and a second embodiment
comprises elements B and D, then the inventive subject matter is also considered
to include other remaining combinations of A, B, C, or D, even if not explicitly
disclosed.
[0040] Among the various approaches to improve the solubility of poorly soluble
drugs effervescence is one of the promising approaches. The inventors of the
present disclosure overcome the low solubility of BCS Class II drug - telmisartan,
which suffers from limited absorption profile and erratic bioavailability, by
providing an effervescent pharmaceutical composition.
[0041] The term 'therapeutically effective amount' used throughout the present
disclosure denotes an amount sufficient to produce the desired effects without
causing any side-effects.
[0042] The term, "subject" used throughout the present disclosure denotes an
animal, preferably a mammal, and most preferably a human. The term "mammal"
used herein refers to warm-blooded vertebrate animals of the class 'mammalia',
including humans, characterized by a covering of hair on the skin and in the
female, milk-producing mammary glands for nourishing the young. The term
mammal includes animals such as cat, dog, rabbit, bear, fox, wolf, monkey, deer,
mouse, pig and human.
[0043] The term, 'management', or 'treatment' as used herein refers to alleviate,
slow the progression, attenuation, prophylaxis or as such treat the existing disease
or condition. Treatment also includes treating, preventing development of, or
alleviating to some extent, one or more of the symptoms of the diseases or
condition.
[0044] As used herein, the term 'effervescent composition' refers to compositions
essentially comprising acid and base components which undergo reaction in the
presence of water and yield carbon dioxide. This effervescence aids in dissolution
of the drug.
[0045] In an embodiment, the present disclosure provides an effervescent
pharmaceutical composition comprising telmisartan, polyethylene glycol, citric

acid, tartaric acid, sodium citrate, sodium bicarbonate, glycine and one or more
pharmaceutical^ acceptable excipient(s) or adjuvant(s).
[0046] In an embodiment, the telmisartan may be crystalline or amorphous
telmisartan. In an embodiment, the telmisartan may be present in a range of about
8% to about 24% w/w of the composition.
[0047] Polyethylene glycol is a hydrophilic carrier which enhances the wettability
of the drug and also acts as a binder. In an embodiment, the polyethylene glycol
may have an average molecular weight in the range of about 950g/mol to about
4000g/mol. In a preferred embodiment, the polyethylene glycol may be selected
from polyethylene glycol 4000, polyethylene glycol 2000, polyethylene glycol
1000 or combinations thereof.
[0048] In an embodiment, the polyethylene glycol may be present in a range of
about 20% to about 40% w/w of the composition.
[0049] In an embodiment, the citric acid may be present in a range of about 2% to
about 10%) w/w of the composition.
[0050] In an embodiment, the tartaric acid may be present in a range of about 3%
to about 10%) w/w of the composition.
[0051] In an embodiment, the sodium citrate may be present in a range of about
2%> to about 8%> w/w of the composition.
[0052] In an embodiment, the sodium bicarbonate may be present in a range of
about 15%o to about 25% w/w of the composition.
[0053] In an embodiment, the glycine may be present in a range of about 10% to
about 24%) w/w of the composition.
[0054] In an embodiment, the excipient or adjuvant may be present in a range of
about 0.1%) to about 1.0% w/w of the composition.
[0055] In an embodiment, the pharmaceutically acceptable excipient(s) or
adjuvant(s) may be selected from those well known in the art, including
lubricants, diluents, preservatives, sweetening agent, flavoring agent, coloring
agent, fillers, glidants, bulking agent, humectant, or combinations thereof.
However, a person of skill in the art would understand that any other excipient(s)
or adjuvant(s) well-known in the art may be employed in the composition.

[0056] In an embodiment, bulking agent(s) includes but is not limited to, lactose USP, Starch 1500, mannitol, sorbitol, maltodextrin, malitol or other non-reducing sugars; microcrystalline cellulose (e.g., Avicel), dibasic calcium phosphate (anhydrous or dihydrate), sucrose, etc. and mixtures thereof. However, a person skilled in the art would appreciate that any other bulking agent(s) can be utilized to serve the intended purpose without departing from the scope and spirit of the invention.
[0057] In an embodiment, glidant(s) includes but not limited to, colloidal silicon dioxide, precipitated silicon dioxide, fumed silica (CAB-O-SIL M-5P, trademark of Cabot Corporation), stearowet and sterotex, silicas (such as SILOID and SILOX silicas—trademarks of Grace Davison Products, Aerosil—trademark of Degussa Pharma), higher fatty acids, the metal salts thereof, or hydrogenated vegetable oils. However, a person skilled in the art would appreciate that any other glidant(s) can be utilized to serve the intended purpose without departing from the scope and spirit of the invention.
[0058] In an embodiment, flavoring agent(s) includes but not limited to, fruit aromas such as orange, banana, strawberry, cherry, wild cherry, lemon; cardamom, anis, mint, menthol, vanillin, and ethyl vanillin, and other similar aromas such as coffee, or the mixtures thereof. However, a person skilled in the art would appreciate that any other flavoring agent(s) can be utilized to serve the intended purpose without departing from the scope and spirit of the invention. [0059] In an embodiment, sweetening agent(s) includes but not limited to, sucralose, acesulfame-K, aspartame, saccharine or saccharine sodium and calcium salts, sodium cyclamate, sucrose, fructose, glucose, sorbitol, or the mixtures thereof. However, a person skilled in the art would appreciate that any other sweetening agent(s) can be utilized to serve the intended purpose without departing from the scope and spirit of the invention.
[0060] In an embodiment, diluent(s) includes but is not limited to, microfine cellulose, lactose, starch, pregelatinized starch, calcium carbonate, calcium sulfate, sugar, dextrates, dextrin, dextrose, dibasic calcium phosphate dihydrate, tribasic calcium phosphate, kaolin, magnesium carbonate, magnesium oxide,

maltodextrin, mannitol, potassium chloride, powdered cellulose, sodium chloride,
sorbitol, talc and mixture thereof. However, a person skilled in the art would
appreciate that any other diluent(s) can be utilized to serve the intended purpose
without departing from the scope and spirit of the invention.
[0061] In an embodiment, lubricant(s) includes but is not limited to, zinc stearate,
magnesium stearate, stearic acid, calcium stearate, Vegetable stearin and mixture
thereof. However, a person skilled in the art would appreciate that any other
lubricant(s) can be utilized to serve the intended purpose without departing from
the scope and spirit of the invention
[0062] The compositions of the present disclosure have appreciable acceptance
due to their industrial viability, low manufacturing costs and high patient
compliance. Effervescent compositions have comparatively faster dissolution than
other solid dosage forms leading to improved solubility and consequently
increased bioavailability.
[0063] In an embodiment, the composition of the present disclosure is synergistic
and possesses improved solubility. In an embodiment, the composition shows
immediate drug release and improved dissolution profile.
[0064] In an embodiment, the composition provides efficient dispersion in water
for the poorly aqueous soluble telmisartan.
[0065] In an embodiment, the present disclosure provides an effervescent
pharmaceutical formulation comprising telmisartan, polyethylene glycol, citric
acid, tartaric acid, sodium citrate, glycine, sodium bicarbonate and one or more
pharmaceutically acceptable excipient(s) or adjuvant(s).
[0066] In an embodiment, the formulation may be a solid or a semi-solid
formulation. In an embodiment, the formulation may be a solid formulation
selected from powder, tablet, granules, nanoparticles, microparticles, or lozenges.
[0067] In a preferred embodiment, the formulation is an effervescent granules
pharmaceutical formulation.
[0068] In an embodiment, the present disclosure provides an effervescent granules
pharmaceutical formulation comprising telmisartan, polyethylene glycol, citric

acid, tartaric acid, sodium citrate, sodium bicarbonate, glycine, and one or more pharmaceutical^ acceptable excipient(s) or adjuvant(s).
[0069] In an embodiment, the present disclosure provides an effervescent granules pharmaceutical formulation comprising telmisartan, polyethylene glycol, citric acid, tartaric acid, sodium citrate, sodium bicarbonate, glycine, talc and magnesium stearate.
[0070] In an embodiment, the present disclosure provides an effervescent granules pharmaceutical formulation comprising telmisartan in an amount of about 24% w/w of the formulation, polyethylene glycol in an amount of about 24% w/w of the formulation, citric acid in an amount of about 6% w/w of the formulation, tartaric acid in an amount of about 6% w/w of the formulation, sodium citrate in an amount of about 4% w/w of the formulation, sodium bicarbonate in an amount of about 20%) w/w of the formulation, glycine in an amount of about 16%> w/w of the formulation, talc in an amount of about 0.4% w/w of the formulation and magnesium stearate in an amount of about 0.4% w/w of the formulation. [0071] In an embodiment, the present disclosure provides an effervescent granules pharmaceutical formulation comprising telmisartan in an amount of about 16% w/w of the formulation, polyethylene glycol in an amount of about 32% w/w of the formulation, citric acid in an amount of about 6% w/w of the formulation, tartaric acid in an amount of about 6% w/w of the formulation, sodium citrate in an amount of about 4% w/w of the formulation, sodium bicarbonate in an amount of about 20%) w/w of the formulation, glycine in an amount of about 16% w/w of the formulation, talc in an amount of about 0.4% w/w of the formulation and magnesium stearate in an amount of about 0.4% w/w of the formulation. [0072] In an embodiment, the present disclosure provides an effervescent granules pharmaceutical formulation comprising telmisartan in an amount of about 16% w/w of the composition, polyethylene glycol in an amount of about 32% w/w of the composition, citric acid in an amount of about 2% w/w of the composition, tartaric acid in an amount of about 6% w/w of the composition, sodium citrate in an amount of about 8% w/w of the composition, sodium bicarbonate in an amount of about 20%) w/w of the composition, glycine in an amount of about 16% w/w of

the composition, talc in an amount of about 0.4% w/w of the composition and
magnesium stearate in an amount of about 0.4% w/w of the composition.
[0073] In an embodiment, the present disclosure provides an effervescent granules
pharmaceutical formulation comprising telmisartan in an amount of about 24%
w/w of the composition, polyethylene glycol in an amount of about 16%> w/w of
the composition, citric acid in an amount of about 2% w/w of the composition,
tartaric acid in an amount of about 6% w/w of the composition, sodium citrate in
an amount of about 8% w/w of the composition, sodium bicarbonate in an amount
of about 20%) w/w of the composition, glycine in an amount of about 24% w/w of
the composition, talc in an amount of about 0.4% w/w of the composition and
magnesium stearate in an amount of about 0.4% w/w of the composition.
[0074] In an embodiment, the disclosure provides use of an effervescent
pharmaceutical composition or formulation comprising telmisartan in the
management of hypertension and cardiovascular conditions associated with
diabetes.
[0075] In an embodiment, the present disclosure provides a method of treatment,
amelioration or prevention of hypertension and cardiovascular conditions
associated with diabetes in a subject by administering a therapeutically effective
amount of the effervescent pharmaceutical composition or formulation comprising
telmisartan.
[0076] In an embodiment, the cardiovascular conditions associated with diabetes
include heart failure, stroke, renal failure, myocardial infarction or combinations
thereof.
[0077] In an embodiment, the effervescent pharmaceutical composition or
formulation may be prepared via melt-fusion technique.
[0078] In a preferred embodiment, the effervescent pharmaceutical formulation is
an effervescent granules pharmaceutical formulation. The present disclosure
provides a process of preparing the effervescent pharmaceutical formulation
comprising telmisartan, wherein the process comprises the steps of: (a)mixing
telmisartan, polyethylene glycol, citric acid, tartaric acid, sodium citrate, glycine
and sodium bicarbonate; (b) granulating the mixture by heating at a temperature in

the range of 40-50°C; (c) cooling and sieving to get uniform sized granules; and (d) adding and mixing one or more pharmaceutically acceptable excipient(s) or adjuvant(s) to give the formulation; and wherein the formulation is an effervescent granules pharmaceutical formulation.
[0079] While the foregoing describes various embodiments of the disclosure, other and further embodiments of the disclosure may be devised without departing from the basic scope thereof. The scope of the invention is determined by the claims that follow. The invention is not limited to the described embodiments, versions or examples, which are included to enable a person having ordinary skill in the art to make and use the invention when combined with information and knowledge available to the person having ordinary skill in the art. EXAMPLES
[0080] The disclosure will now be illustrated with working examples, which is intended to illustrate the working of disclosure and not intended to take restrictively to imply any limitations on the scope of the present disclosure. Unless defined otherwise, all technical and scientific terms used herein have the same meaning as commonly understood to one of ordinary skill in the art to which this disclosure belongs. Although methods and materials similar or equivalent to those described herein can be used in the practice of the disclosed methods and compositions, the exemplary methods, devices and materials are described herein. [0081] EXAMPLE 1: Preparation of granules formulation [0082] An effervescent granules Formulation A (500mg) was prepared as per the present disclosure and with composition as disclosed in Table 1. Telmisartan, PEG 4000, citric acid, tartaric acid, sodium citrate, sodium bicarbonate and glycine were mixed and granulated by heating at temperature around 40-50°C. The prepared granules were then allowed to cool and sieved to get uniform size distribution. After sieving, talc and magnesium stearate were added in appropriate concentrations to prepare granules with improved flow property.

Table 1: Effervescent granules Formulation A

Ingredients Quantity (%w/w) (500 mg)
Telmi saltan 24%
PEG 4000 24%
Citric acid 6%
Tartaric acid 6%
Sodium citrate 4%
Sodium bicarbonate 20%
Glycine 16%
Talc 0.4%
Magnesium stearate 0.4%
[0083] Based on similar process as disclosed above, 500 mg of Formulations B-D were prepared using the compositions of Table 2.
Table 2: Effervescent granules Formulations B-D

Ingredients Formulation B
Quantity (500
mg) Formulation C
Quantity (500
mg) Formulation D
Quantity (500
mg)
Telmi saltan 16% 16% 24%
PEG 4000 32% 32% 16%
Citric acid 6% 2% 2%
Tartaric acid 6% 6% 6%
Sodium citrate 4% 8% 8%
Sodium bicarbonate 20% 20% 20%
Glycine 16% 16% 24%
Talc 0.4% 0.4% 0.4%
Magnesium stearate 0.4% 0.4% 0.4%

[0084] EXAMPLE 2: Determination of Effervescent Granule Dissolution Rate
[0085] The end point of dissolution rate of effervescent granules of Formulation A comprising telmisartan was determined visually. Around 0.5 gram of effervescent granules were added in 500 mL of water and mixed with continuous stirring of 100 rpm at 37 ± 0.5 °C. The end point was determined by visual inspection and cessation of effervescence of powdered granules was taken as endpoint. The cessation of effervescence of powdered granules for effervescent granules of Formulation A was around 60 seconds. The dissolution rate was also determined for a commercial tablet of telmisartan comprising 120mg of telmisartan.
[0086] A comparison of the dissolution rates of telmisartan in the present composition and commercial composition has been provided in Figure 1. It shows that about 100% dissolution of telmisartan was noted within 30 minutes from the presently claimed composition as opposed to about 120 minutes in the commercial composition.
[0087] The foregoing examples are merely illustrative and are not to be taken as limitations upon the scope of the invention. Various changes and modifications to the disclosed embodiments will be apparent to those skilled in the art. Such changes and modifications may be made without departing from the scope of the invention.
ADVANTAGES OF THE PRESENT INVENTION
[0088] The present disclosure provides a composition that improves the solubility
of telmisartan.
[0089] The present disclosure provides a composition that is immediate release
composition, is industrially viable and has low manufacturing costs.
[0090] The present disclosure provides a composition that has improved
dissolution profile and higher patient compliance.

We Claim:

1. An effervescent pharmaceutical composition comprising telmisartan,
polyethylene glycol, citric acid, tartaric acid, sodium citrate, sodium bicarbonate,
glycine and one or more pharmaceutically acceptable excipient(s) or adjuvant(s).
2. The composition as claimed in claim 1, wherein the telmisartan is present in a range of 8% to 24% w/w of the composition.
3. The composition as claimed in claim 1, wherein the polyethylene glycol has an average molecular weight in the range of 950g/mol to 4000g/mol.
4. The composition as claimed in claim 1, wherein the polyethylene glycol is present in a range of 20% to 40% w/w of the composition.
5. The composition as claimed in claim 1, wherein the citric acid is present in a range of 2% to 10% w/w of the composition.
6. The composition as claimed in claim 1, wherein the tartaric acid is present in a range of 3% to 10% w/w of the composition.
7. The composition as claimed in claim 1, wherein the sodium citrate is present in a range of 2% to 8% w/w of the composition.
8. The composition as claimed in claim 1, wherein the sodium bicarbonate is present in a range of 15% to 25% w/w of the composition.
9. The composition as claimed in claim 1, wherein the glycine is present in a range of 10% to 24% w/w of the composition.
10. The composition as claimed in claim 1, wherein the excipient or adjuvant is
present in a range of 0.1% to 1.0% w/w of the composition.
11. An effervescent pharmaceutical formulation comprising telmisartan,
polyethylene glycol, citric acid, tartaric acid, sodium citrate, glycine, sodium
bicarbonate and one or more pharmaceutically acceptable excipient(s) or
adjuvant(s).
12. The formulation as claimed in claim 11, wherein the formulation is a solid
formulation selected from powder, tablet, granules, nanoparticles, microparticles,
or lozenges.

13. The formulation as claimed in claim 11, wherein the formulation is an effervescent granules pharmaceutical formulation.
14. The formulation as claimed in claim 11, wherein the formulation is an effervescent granules pharmaceutical formulation comprising telmisartan, polyethylene glycol, citric acid, tartaric acid, sodium citrate, sodium bicarbonate, glycine, talc and magnesium stearate.
15. A process of preparing an effervescent pharmaceutical formulation comprising
telmisartan, wherein the process comprises the steps of: (a) mixing telmisartan,
polyethylene glycol, citric acid, tartaric acid, sodium citrate, glycine and sodium
bicarbonate; (b) granulating the mixture by heating at a temperature in the range
of 40-50°C; (c) cooling and sieving to get uniform sized granules; and (d) adding
and mixing one or more pharmaceutically acceptable excipient(s) or adjuvant(s) to
give the formulation; and wherein the formulation is an effervescent granules
pharmaceutical formulation.