WO2013115742A1

WO2013115742A1 - Pharmaceutical composition comprising alpha-glucosidase inhibitor

Info

Publication number: WO2013115742A1
Application number: PCT/TR2013/000051
Authority: WO
Inventors: Mahmut Bilgic
Original assignee: Mahmut Bilgic
Priority date: 2012-01-31
Filing date: 2013-01-31
Publication date: 2013-08-08

Abstract

The present invention relates to a pharmaceutical composition comprising voglibose, acarbose or miglitol so as to be used in the prophylaxis and treatment of type 2 diabetes (non-insulin dependent) mellitus cases wherein hyperglycemia cannot be controlled by diet or exercise.

Description

PHARMACEUTICAL COMPOSITION COMPRISING ALPHA-GLUCOSIDASE INHIBITOR

The present invention relates to a pharmaceutical composition comprising an alpha-glucosidase inhibitor derivative active agent so as to be used in the prophylaxis and treatment of type 2 diabetes (non-insulin dependent) mellitus cases wherein hyperglycemia cannot be controlled by diet or exercise. Preventing digestion of carbohydrates, alpha-glucosidase inhibitors hinder formation of monosaccharides absorbed from intestines. They positively influence blood sugar level this way.

Primary active agents known as alpha-glucosidase inhibitors are voglibose, acarbose and miglitol.

During preparation of formulations comprising voglibose, acarbose or miglitol, it is observed that the formulation adheres to machine parts such as inner walls of the die and the punch. This causes some part of the medicament to remain on the punches and in the dies, which brings some problems to manufacturers during preparation phase of the medicament. In addition, since some part of the medicament remains on the punches and in the dies, the dosage form obtained does not have the desired shape and desired smoothness and this brings some problems at quality control phases. Furthermore, it is seen that dispersion is affected negatively by thickness of the tablets produced.

At the same time, in the case that the formulations are compressed in tablet form, machine parts present corrosion and wear in time due to friction between tablet surface and punch or inner wall of the die during ejection of the tablets. Therefore, these problems seen during preparation of the formulations comprising voglibose, acarbose or miglitol pose problems for manufacturers at production and quality control phases and impede to obtain the final product effectively.

As it is seen, there is need for development of new approaches in order to obtain medicaments comprising voglibose, acarbose or miglitol which are produced in the manner that no problem is observed at production and quality control phases so as to prevent problems such as adhesion of the formulation to the machine parts such as the die and the punch during preparation and possible corrosions that can arise from the friction between tablet surface and the inner wall of the die during tablet production.

As a result of the studies they conducted in line with this requirement, the inventors have found that the problems encountered at production and quality control phases during preparation of the medicaments can be solved by the formulations they have developed for preparation of dosage forms comprising voglibose, acarbose or miglitol.

Description of the Invention

The present invention relates to pharmaceutical formulations comprising voglibose, acarbose or miglitol and preparation methods for said formulations. Surprisingly, the inventors have seen that in the case that the formulations comprising voglibose, acarbose or miglitol comprise talc, magnesium stearate, PEG, silicone dioxide, sodium benzoate, potassium benzoate, stearic acid, sodium stearyl fumarate and/or a combination thereof as the lubricant, the formulation does not adhere to the punch or inner walls of the die; wear and corrosion resulting from the possible friction in said machine parts are decreased.

In this respect, the present invention relates to voglibose, acarbose or miglitol formulations wherein talc, magnesium stearate, PEG, silicone dioxide, sodium benzoate, potassium benzoate, stearic acid, sodium stearyl fumarate and/or a combination thereof is used as the lubricant.

In the studies they conducted, the inventors have observed that the most ideal results are gained in the case that more preferably a water soluble polymeric lubricant is used in the formulations comprising voglibose, acarbose, miglitol.

According to this, in a preferred embodiment of the present invention, a water soluble polymeric lubricant is used in the formulations comprising voglibose, acarbose, miglitol.

In another preferred embodiment of the present invention, a lubricant having a pH value in water in the range of 5-7.5, more preferably in the range of 5.5-7 is used in the formulations of the present invention.

In another aspect, the formulations of the present invention relates to use of a lubricant having water content in the range of 0.01% to 1%, preferably in the range of 0.05% to 0.8%, more preferably in the range of 0.08% to 0.5%. In a preferred embodiment of the present invention, a lubricant having

- water content in the range of 0.01% to 1%, preferably in the range of 0.05% to 0.8%, more preferably in the range of 0.08% to 0.5% and

- a pH value in water in the range of 5-7.5, more preferably in the range of 5.5-7 is used. As a result of the studies they conducted, the inventors have concluded that a lubricant possessing these characteristics has positive effects on water solubility and stability of the formulation.

The lubricant used in a preferred embodiment of the invention is polyethylene glycol (PEG).

Molecular weight of PEG used according to the invention is in the range of 4000 to 10000, preferably in the range of 5000 to 8000. More preferably, PEG 6000 is used.

Dioo value of PEG 6000 used according to the invention is in the range of 10-500 μπι, preferably in the range of 30-400 μπι, more preferably in the range of 50-300 μπι. According to this, a characteristic feature of the present invention is that PEG 6000 is used as lubricant in said formulation and dioo value of PEG 6000 is in the range of 10-500 μπι, preferably in the range of 30-400 μπι, more preferably in the range of 50-300 μπι.

In another aspect, amount of the lubricant used for preparation of the formulations comprising voglibose, acarbose or miglitol is a significant parameter for characteristics of the formulation to be obtained. Use of the lubricant less than the required amount results in adhesion of the prepared formulation to machine parts and binding to the punch holes. Particularly, use of the lubricant less than 0.6% in proportion to total weight results negatively in terms of the formulation.

Use of the lubricant more than the required amount, on the other hand, causes increase in dissolution times of the obtained dosage forms.

The inventors have seen that formulations do not adhere to machine parts during preparation and dissolution times of the obtained dosage forms are not long in the case that the amount of lubricant used in the formulations comprising voglibose, acarbose or miglitol is in the range of 1% to 5%, preferably in the range of 0.6% to 5%, more preferably in the range of 0.6% to 3%. Thus, said problems encountered during both production and use of the formulations comprising voglibose, acarbose or miglitol are solved.

In another aspect, the present invention relates to formulations comprising a lubricant in the range of 1% to 5%, preferably in the range of 0.6% to 5%, more preferably in the range of 0.6% to 3% in proportion to total weight of the formulations. In a preferred embodiment of the present invention, the formulations comprising voglibose, acarbose or miglitol are characterized in that PEG 6000 is used in the range of 1% to 5%, preferably in the range of 0.6% to 5%, more preferably in the range of 0.6% to 3%.

During the studies they conducted in order to solve the problem of adhesion of the formulations comprising voglibose, acarbose or miglitol to machine parts, the inventors have surprisingly detected that particle size of the active agent and particle size of the lubricant used in the formulation comprising voglibose, acarbose or miglitol play a role in solving this problem effectively.

Another characteristic feature of the present invention is that the ratio of dioo value of voglibose, acarbose or miglitol to dioo value of the lubricant is in the range of 10: 1 to 1 : 10, preferably in the range of 8: 1 to 1 :8 and more preferably in the range of 5: 1 to 1 :5. According to a preferred embodiment of the present invention, a pharmaceutical composition comprising voglibose, acarbose or miglitol characterized in that

- the lubricant is used in the range of 1% to 5%, preferably in the range of 0.6% to 5%, more preferably in the range of 0.6% to 3% and - the ratio of dioo value of voglibose, acarbose or miglitol to dioo value of the lubricant is in the range of 10: 1 to 1: 10, preferably in the range of 8: 1 to 1 :8 and more preferably in the range of 5: 1 to 1 :5.

According to another embodiment of the invention, a pharmaceutical composition comprising voglibose, acarbose or miglitol characterized in that

- PEG 6000 is used in the range of 1% to 5%, preferably in the range of 0.6% to 5%, more preferably in the range of 0.6% to 3% and

- the ratio of dioo value of voglibose, acarbose or miglitol to dioo value of the lubricant is in the range of 20: 1 to 1 : 1, preferably in the range of 15: 1 to 3: 1 and more preferably in the range of 10: 1 to 5: 1.

% amounts given in scope of the invention are calculated in proportion to unit dosage weight.

Voglibose, acarbose or miglitol comprised in the pharmaceutical formulations of the present invention can be in the form of their pharmaceutically acceptable salts, hydrates, solvates, esters, enantiomers, diastereomers or combinations thereof in terms of chemical structure; in crystalline form, amorphous form or combinations thereof in terms of polymorphic structure.

The pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be prepared in any of the dosage forms such as tablet, effervescent tablet, effervescent granule, effervescent dry powder, film coated tablet, enterically coated tablet, dry powder, granule, capsule, prolonged-release tablet, modified-release tablet, delayed-release tablet. The pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant are preferably in tablet or effervescent tablet, film coated tablet, modified-release tablet form.

In another aspect, the present invention relates to pharmaceutical formulations in tablet form comprising voglibose, acarbose or miglitol and lubricant. The pharmaceutical formulation obtained can be formed into any of the abovementioned dosage forms. In the case that the composition is in tablet form, the tablets obtained can be treated with film coating agents for instance sugar based coating agents, water soluble film coating agents, enteric coating agents, delayed release coating agents or coating compositions comprising a combination thereof. As the sugar based coating agent, saccharose can be used alone or optionally with any of the agents such as talc, calcium carbonate, calcium phosphate, calcium sulphate, gelatine, gum arabic, polyvinylpyrrolidone and pullulan or a combination thereof. The water soluble film coating agent can be selected from cellulose derivatives such as hydroxypropyl cellulose, hydroxypropyl methyl cellulose, hydroxyethyl cellulose, methyl hydroxyethyl cellulose and sodium carboxymethyl cellulose; synthetic polymers such as polyvinyl acetal diethyl aminoacetate, aminoalkyl methacrylate copolymers and polyvinylpyrrolidone and polysaccharides such as pullulan or combinations thereof.

The enteric coating agents can be selected from cellulose derivatives such as hydroxypropyl methyl cellulose phthalate, hydroxypropyl methyl cellulose acetate succinate, carboxymethyl ethyl cellulose, cellulose acetate phthalate; acrylic acid derivatives such as methacrylic acid copolymer L, methacrylic acid copolymer LD and methacrylic acid copolymer S and natural substances such as shellac or combinations thereof.

The delayed release coating agents can be selected from cellulose derivatives such as ethyl cellulose; acrylic acid derivatives such as aminoalkyl methacrylate copolymer RS, ethyl acrylate-methyl methacrylate copolymer emulsion or combinations thereof.

The pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can comprise various excipients in addition to voglibose, acarbose or miglitol as the active agent and lubricant.

The pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant comprise at least one excipient selected from a group comprising disintegrant, diluent, lubricant, glidant, binder, effervescent couple comprising at least one acidic agent and at least one basic agent, coloring agent, pH regulating agent, surfactant, stabilizing agent, sweetener and/or taste regulating agent, flavoring agent in addition to voglibose, acarbose or miglitol and lubricant.

The disintegrant that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising carboxymethyl cellulose, carboxymethyl cellulose calcium, carboxymethyl cellulose sodium, croscarmellose sodium, crospovidone, hydroxypropyl cellulose, microcrystalline cellulose, methyl cellulose, chitosan, starch, sodium starch glycolate.

The diluent that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising calcium carbonate, dibasic calcium phosphate, tribasic calcium phosphate, calcium sulphate, microcrystalline cellulose, dextrose, fructose, lactitol, lactose, magnesium carbonate, magnesium oxide, maltitol, maltodextrin, maltose, mannitol, simethicone, sorbitol, starch, sodium chloride, sucrose, talc, xylitol. The glidant that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising tribasic calcium phosphate, colloidal silicon dioxide, magnesium silicate, magnesium trisilicate, talc.

The binder that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising carboxymethyl cellulose sodium, ethyl cellulose, gelatine, hydroxyethyl cellulose, hydroxymethyl cellulose, hydroxypropyl cellulose, hypromellose, magnesium aluminium silicate, maltodextrin, methyl cellulose, povidone, starch.

The acidic agent composing the effervescent couple comprising at least one acidic agent and at least one basic agent that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising organic acids such as malic acid, citric acid, tartaric acid, fumaric acid; and the basic agent can be selected from a group comprising agents such as sodium carbonate, potassium carbonate, sodium hydrogen carbonate, potassium hydrogen carbonate. The pH regulating agent that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising citrate, phosphate, carbonate, tartrate, fumarate, acetate and amino acid salts.

The surfactant that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from sodium lauryl sulphate, polysorbate, polyoxyethylene, polyoxypropylene glycol and similar agents.

The stabilizing agent that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising tocopherol, tetrasodium edetate, nicotinamide, cyclodextrin.

The sweetener and/or taste regulating agent that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from a group comprising acesulfame, aspartame, dextrose, fructose, maltitol, maltose, mannitol, saccharine, saccharine sodium, sodium cyclamate, sorbitol, sucralose, sucrose, xylitol, sodium chloride.

The flavoring agent that can be used in the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can be selected from menthol, lemon, orange, vanilla, strawberry, raspberry, caramel and similar flavors.

According to a preferred embodiment of the present invention, a pharmaceutical composition comprising voglibose, acarbose or miglitol characterized in that; - a lubricant is used in the range of 1% to 5%, preferably in the range of 0.6% to 5%, more preferably in the range of 0.6% to 3% in said formulation and

- the ratio of dioo value of voglibose, acarbose or miglitol to di₀o value of the lubricant is in the range of 10: 1 to 1 : 10, preferably in the range of 8: 1 to 1 :8 and more preferably in the range of 5: 1 to 1 :5,

- said formulation comprises at least one excipient selected from a group comprising disintegrant, diluent, lubricant, glidant, binder, effervescent couple comprising at least one acidic agent and at least one basic agent, coloring agent, pH regulating agent, surfactant, stabilizing agent, sweetener and/or taste regulating agent, flavoring agent in addition to voglibose, acarbose or miglitol and lubricant.

According to another preferred embodiment of the present invention, a pharmaceutical composition comprising voglibose, acarbose or miglitol characterized in that;

- PEG 6000 is used in the range of 1% to 5%, preferably in the range of 0.6% to 5%, more preferably in the range of 0.6% to 3% in said formulation and

- the ratio of dioo value of voglibose, acarbose or miglitol to dioo value of the lubricant is in the range of 20: 1 to 1 : 1, preferably in the range of 15: 1 to 3: 1 and more preferably in the range of 10: 1 to 5: 1,

The pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant can comprise voglibose, acarbose or miglitol in the range of 0.003% to50% by weight, preferably in the range of 0.005% to 40% by weight, more preferably in the range of 0.01% to 30% by weight.

In the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant, a second active agent can optionally be used in addition to voglibose, acarbose or miglitol. The second active agent can be selected from a group comprising antacid, anticholinergic, antispasmodic, antiemetic, antidiabetic, antipropulsive, antiallergic, antidiarrheal, antiobesity, antithrombotic, antifibrinolytic, antianemic, antihypertensive, antifungal, antipruritic, antipsoriatic, antibiotic, antiseptic, antiacne, antibacterial, antimycotic, antiviral, antineoplastic, antiarrhythmic, antiadrenergic, antiepileptic, anti-parkinson, antiprotozoal, anthelmintic, anti-inflammatory, diuretic, laxative, sulphonamide, imidazole, corticosteroid, thiazolidinedione, biguanide, immunostimulant, immunosuppressant, myorelaxant, analgesic, psycholeptic, psychoanaleptic peripheral vasodilator, beta blocker, calcium channel blocker and lipid modifying agents; alpha-glucosidase inhibitors, aldose reductase inhibitors, ACE inhibitors; multivitamin and minerals, vitamin A, vitamin D and its analogues, vitamin vitamin C, vitamin E, vitamin B_6> vitamin B_2, vitamin K, calcium, potassium, sodium, zinc, magnesium, fluoride, selenium. In another aspect, the second active agent can be selected from a group comprising repaglinide belonging to the group of meglitinides; acetohexamide, glindeclamide, glibornuride, gliclazide, gliquidone, glimepiride, glipizide, chlorpropamide, tolbutamide belonging to the group of sulfonylureas; pioglitazone, rosiglitazone, rivoglitazone, rosiglitazone maleate, pioglitazone hydrochloride, troglitazone belonging to the group of thiazolidinediones; phenformin, metformin, metformin hydrochloride belonging to the group of biguanides; dipeptidyl peptidase-4 inhibitors sitagliptin, vildagliptin, saxagliptin, saxagliptin hydrochloride, sitagliptin phosphate, sitagliptin phosphate monohydrate.

As the second active agent in addition to voglibose, acarbose or miglitol, the pharmaceutical formulations of the present invention comprising voglibose, acarbose or miglitol and lubricant optionally comprise active agents preferably from biguanide group, more preferably metformin or a pharmaceutically acceptable salt thereof, for example metformin hydrochloride.

In another aspect, the present invention is for use of said pharmaceutical formulation in the combination of voglibose, acarbose or miglitol with metformin or a pharmaceutically acceptable salt thereof. Said formulations are preferably in modified-release tablet, tablet, film-coated tablet or effervescent tablet form.

The pharmaceutical formulation of the present invention can be obtained by a method comprising the steps of:

• mixing the active agent voglibose, acarbose or miglitol and the second active agent, if available, homogeneously and adding at least one of the abovementioned excipients if required and the lubricant or

• granulating the active agent voglibose, acarbose or miglitol and the second active agent, if available, with at least one of the abovementioned excipients and mixing them homogeneously and then adding the lubricant or

• mixing the active agent voglibose, acarbose or miglitol and the second active agent if available with at least one of the excipients and optionally granulating the mixture with the granulation solution comprising excipient and mixing the obtained granules with the lubricant and optionally with at least one excipient or

• using any of the abovementioned methods separately for active agent compositions and combining the formulations obtained afterwards in the case that two active agents are used. The pharmaceutical formulation of the present invention can be used in the prophylaxis and treatment of type 2 diabetes (non-insulin dependent) mellitus cases wherein hyperglycemia cannot be controlled by diet or exercise.

There are examples relating to the formulations of the invention given below. Said examples are given in order to explain the invention, yet the present invention should not be limited to these.

EXAMPLE 1: Formulation and process for preparation of tablets comprising voglibose and metformin combination

The mixture comprising at least one other excipient, effervescent acid and effervescent base is mixed with the granulation solution and granulated. The obtained granules are dried. The granules dried are mixed with voglibose, metformin and PEG 6000 having a particle size of 200 μπι. The obtained formulation is compressed in tablet compression machine.

EXAMPLE 2: Formulation and process for preparation of formulation comprising acarbose and metformin combination

A granulation solution is prepared with at least one excipient. Acarbose and metformin hydrochloride are granulated with this granulation solution. The obtained granules are mixed with the lubricant and the other excipients. The formulation prepared can be packed in powder or granule form as well as compressed in tablet form.

Claims

1. A pharmaceutical formulation comprising voglibose, acarbose or miglitol, characterized in that said formulation comprises talc, magnesium stearate, PEG, silicon dioxide, sodium benzoate, potassium benzoate, stearic acid, sodium stearyl fumarate and/or a combination thereof as lubricant.

2. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claim 1, characterized in that the lubricant used is more preferably a water soluble polymeric lubricant.

3. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1 and 2, characterized in that said formulation is for use of a lubricant having a pH value in water in the range of 5% to 7.5%.

4. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-3, characterized in that said formulation is for use of a lubricant having a pH value in water in the range of 5.5% to 7%.

5. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-4, characterized in that water content of the lubricant used in said formulation is in the range of 0.01% to 1%.

6. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-5, characterized in that water content of the lubricant used in said formulation is in the range of 0.05% to 0.8%.

7. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-6, characterized in that water content of the lubricant used in said formulation is in the range of 0.08% to 0.5%.

8. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-7, characterized in that amount of the lubricant is in the range of 1% to 5% in proportion to total amount of the formulation.

9. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-8, characterized in that amount of the lubricant is in the range of 0.6% to 5% in proportion to total amount of the formulation.

10. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-9, characterized in that amount of the lubricant is in the range of 0.6% to 3% in proportion to total amount of the formulation.

1 1. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that d₁₀o value of the lubricant is in the range of 10-500 μπι.

12. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that dioo value of the lubricant is in the range of 30-400 μηι.

13. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that dioo value of the lubricant is in the range of 50-300 μηι.

14. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that the ratio of dioo value of voglibose, acarbose or miglitol to dioo value of the lubricant is in the range of 10:1 to 1 : 10.

15. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that the ratio of dioo value of voglibose, acarbose or miglitol to dioo value of the lubricant is in the range of 8: 1 to 1 :8.

16. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that the ratio of dioo value of voglibose, acarbose or miglitol to dioo value of the lubricant is in the range of 5: 1 to 1 : 5.

17. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that the lubricant used is PEG.

18. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that the molecular weight of PEG used as the lubricant is in the range of 4000 to 10000.

19. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that the molecular weight of PEG used as the lubricant is in the range of 5000 to 8000.

20. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that the molecular weight of PEG used as the lubricant is 6000.

21. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that said formulation is in any of the dosage forms of tablet, effervescent tablet, effervescent granule, effervescent dry powder, film coated tablet, enterically coated tablet, dry powder, granule, capsule, prolonged-release tablet, modified- release tablet, delayed-release tablet.

22. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that said formulation is in the form of tablet, modified- release tablet, film tablet, effervescent tablet.

23. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that said formulation is in effervescent tablet form.

24. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that voglibose, acarbose or miglitol are in the form of their pharmaceutically acceptable derivatives, salts, hydrates, solvates, esters, enantiomers, diastereomers or combinations thereof in terms of chemical structure.

25. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that voglibose, acarbose or miglitol are in amorphous or crystalline form or a combination of these in terms of polymorphic structure.

26. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that said formulation comprises pharmaceutically acceptable excipients in addition to voglibose, acarbose or miglitol and the lubricant.

27. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claim 26, characterized in that said formulation comprises at least one excipient selected from a group comprising disintegrant, diluent, lubricant, glidant, binder, effervescent couple comprising at least one effervescent acid and at least one effervescent base, coloring agent, pH regulating agent, surfactant, stabilizing agent, sweetener and/or taste regulating agent, flavoring agent in addition to voglibose, acarbose or miglitol and the lubricant.

28. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, characterized in that said formulation comprises voglibose, acarbose or miglitol as active agent in the range of 0.003% to 50% by weight.

29. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-28, characterized in that said formulation comprises voglibose, acarbose or miglitol as active agent in the range of 0.005% to 40% by weight.

30. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to claims 1-29, characterized in that said formulation comprises voglibose, acarbose or miglitol as active agent in the range of 0.01% to 30% by weight.

31. The pharmaceutical composition comprising voglibose, acarbose or miglitol according to any preceding claims, wherein said composition comprises at least a second active agent selected from a group comprising antacid, anticholinergic, antispasmodic, antiemetic, antidiabetic, antipropulsive, antiallergic, antidiarrheal, antiobesity, antithrombotic, antifibrinolytic, antianemic, antihypertensive, antifungal, antipruritic, antipsoriatic, antibiotic, antiseptic, antiacne, antibacterial, antimycotic, antiviral, antineoplastic, antiarrhythmic, antiadrenergic, antiepileptic, anti-parkinson, antiprotozoal, anthelmintic, anti-inflammatory, diuretic, laxative, sulphonamide, imidazole, corticosteroid, thiazolidinedione, biguanide, immunostimulant, immunosuppressant, myorelaxant, analgesic, psycholeptic, psychoanaleptic peripheral vasodilator, beta blocker, calcium channel blocker and lipid modifying agents; alpha- glucosidase inhibitors, aldose reductase inhibitors, ACE inhibitors; multivitamin and minerals, vitamin A, vitamin D and its analogues, vitamin B] vitamin C, vitamin E, vitamin Ββ_, vitamin B_2i vitamin K, calcium, potassium, sodium, zinc, magnesium, fluoride, selenium in addition to voglibose, acarbose or miglitol.

32. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, wherein the second active agent that can be comprised in the formulation in addition to voglibose, acarbose or miglitol is selected from biguanides.

33. The pharmaceutical formulation comprising voglibose, acarbose or miglitol according to any preceding claims, wherein the second active agent that can be comprised in the formulation in addition to voglibose, acarbose or miglitol is metformin hydrochloride.

34. A pharmaceutical formulation comprising the combination of voglibose, acarbose or miglitol with metformin or a pharmaceutically acceptable salt thereof, characterized in that said formulation comprises talc, magnesium stearate, PEG, silicon dioxide, sodium benzoate, potassium benzoate, stearic acid, sodium stearyl fumarate and/or a combination thereof as lubricant.