WO2013043142A1 - Procédé de production pour formulations pharmaceutiques comprenant une isoflavone - Google Patents

Procédé de production pour formulations pharmaceutiques comprenant une isoflavone Download PDF

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Publication number
WO2013043142A1
WO2013043142A1 PCT/TR2012/000120 TR2012000120W WO2013043142A1 WO 2013043142 A1 WO2013043142 A1 WO 2013043142A1 TR 2012000120 W TR2012000120 W TR 2012000120W WO 2013043142 A1 WO2013043142 A1 WO 2013043142A1
Authority
WO
WIPO (PCT)
Prior art keywords
effervescent
production method
formulations
comprised
granulation solution
Prior art date
Application number
PCT/TR2012/000120
Other languages
English (en)
Inventor
Mahmut Bilgic
Original Assignee
Mahmut Bilgic
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Mahmut Bilgic filed Critical Mahmut Bilgic
Publication of WO2013043142A1 publication Critical patent/WO2013043142A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
    • A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates

Definitions

  • the present invention discloses a production method for effervescent formulations comprising at least one component belonging to the group of isoflavones.
  • Plant originated estrogens or phenolic compounds having estrogenic effect are called phytoestrogens.
  • Phytoestrogens which have estrogenic effect in variable degrees and which are similar to natural estrogens in terms of both structure and shape exert their effects directly through binding to receptors by competing with natural estrogens in the organism.
  • phytoestrogens can change the efficiency of some enzymes having a role in estrogen metabolism.
  • Phytoestrogens are divided into different subclasses according to different resources. These can be listed under four different classes in total: isoflavones, lignans, coumestans and stilbenes. Each class is composed of different compounds in itself and resources of these compounds are different from each other in the diet.
  • Daidzein and genistein are the compounds belonging to the class of isoflavones of flavonoids in plants. Furthermore, since isoflavones are plant originated compounds having an estrogenlike biological activity, they are also called phytoestrogens. Isoflavones are comprised particularly in soybean and soy products. Soybean comprises 84 mg daidzein and 1 1 1 mg genistein per 100 g of soybean.
  • Isoflavone formulations existing in the prior art are generally in tablet form and these formulations are not usually preferred since they cause difficulty of use for patients.
  • the inventors have prepared the water soluble isoflavone formulations disclosed in the patent application numbered TR2011/07832.
  • the formulations disclosed in said patent application can be obtained by a method existing in the prior art, though the preferred method is dry method.
  • agglomeration which is seen as a result of the gathering of the components of the formulation due to physicochemical interactions is one of the important factors which has a negative effect on flow and homogeneity of the formulation.
  • the present invention relates to a production method especially for water soluble effervescent formulations comprising genistein and optionally at least one other active agent.
  • the formulations can be produced effectively without encountering any agglomeration problem by the production method developed in the scope of the present invention.
  • Another advantage of the production method of the present invention is that it enables to produce the formulations easily.
  • the characteristic feature of the production method of the present invention is that said method is wet granulation method and wet granulation is performed twice successively.
  • the present invention provides a production method for the effervescent formulations comprising genistein and optionally at least one other active agent, characterized in that said production method is wet granulation method and the process of wet granulation is performed twice successively.
  • the effervescent formulations of the present invention are produced by a production method which is basically composed of the following steps:
  • the effervescent formulations produced by the production method of the present invention characterized in that the granulation solution comprises at least one pharmaceutically acceptable binder and deionised water.
  • the binder comprised in the granulation solution is selected from a group comprising potato, wheat or corn starch; microcrystalline cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropyl methyl cellulose and polyvinylpyrrolidone or combinations thereof.
  • the type of the binder comprised in the content of the granulation solution affects the flow characteristics of the formulations significantly.
  • the binder comprised in the granulation solution is polyvinylpyrrolidone.
  • Polyvinylpyrrolidone is a water soluble synthetic polymer which is generally known as "Povidone” in short and obtained by polymerizing N-vinylpyrrolidone monomer. PVP is generally comprised in pharmaceutical tablet formulations as binder.
  • K-value is a value expressing molecular weight of polymers in industry and it is found by using the viscosity of polymer solution. As a general rule, a polymer having high K-value has high molecular weight; on the other hand, a polymer having low K-value has low molecular weight.
  • molecular weight of said binder affects flow of the formulation especially in the formulations obtained by wet granulation method.
  • molecular weight of polyvinylpyrrolidone in the content of the granulation solution in the first step of the production method of the present invention should be in the range of 20.000 gr/mol to 50.000 gr/mol, preferably in the range of 25.000 to 45.000 gr/mol, more preferably in the range of 28.000 gr/mol to 40.000 gr/ mol.
  • one characteristic feature of the production method of the present invention is that molecular weight of polyvinylpyrrolidone in the content of the granulation solution in the first step of the production method is in the range of 20.000 to 50.000 gr/mol, preferably in the range of 25.000 to 45.000 gr/mol, more preferably in the range of 28.000 gr/mol to 40.000 gr/ mol.
  • K- value of polyvinylpyrrolidone which is comprised in the first step of the method as the binder is in the range of 20 to 30, preferably in the range of 22 to 28, more preferably in the range of 23 to 28.
  • another characteristic feature of the production method of the present invention is that the effervescent formulations of the present invention comprising genistein and optionally at least one other active agent are obtained by wet granulating them initially with a granulation solution comprising the mixture of deionised water and povidone having a molecular weight in the range of 20.000 gr/mol to 50.000 gr/mol and then with deionised water.
  • effervescent formulations of the present invention comprising genistein and optionally at least one other active agent are produced by the production method given below:
  • the pharmaceutically acceptable excipients that can be comprised in effervescent genistein formulations that shall be produced by the production method of the present invention can be selected from disintegrants, binders, sweeteners, colouring agents, lubricants, flavouring agents, colourants, effervescent acids, effervescent bases, pH regulators, basic substances or combinations thereof.
  • the effervescent acids comprised in the effervescent genistein formulations that shall be produced by the production method of the present invention are selected from a group comprising citric acid, tartaric acid, malic acid, fumaric acid, monosodium citrate and/or pharmaceutically acceptable salts, hydrates, anhydrates or a combination thereof.
  • the effervescent bases comprised in the effervescent genistein formulations that shall be produced by the production method of the present invention are selected from a group comprising sodium, potassium and calcium carbonates, bicarbonates and/or sodium glycine carbonate or a combination thereof.
  • the disintegrants that can be used in the formulations of the present invention can be selected from a group comprising highly dispersive polymers, for instance cross linked hydroxypropyl cellulose, polyvinylpyrrolidone, high molecular weight polymers, microcrystalline cellulose, sodium starch glycolate, povidone, alginic acid, sodium alginate or combinations thereof.
  • highly dispersive polymers for instance cross linked hydroxypropyl cellulose, polyvinylpyrrolidone, high molecular weight polymers, microcrystalline cellulose, sodium starch glycolate, povidone, alginic acid, sodium alginate or combinations thereof.
  • flavouring agents that can be used in the formulations of the present invention can have banana, strawberry, lemon, orange, peach, vanilla flavours or a similar natural fruit flavour or an aromatic plant flavour.
  • the lubricants that can be used in the formulations of the present invention are selected from a group comprising talc, magnesium stearate, PEG 6000, silicone dioxide, sodium benzoate, potassium benzoate, stearic acid, sodium stearyl fumarate and/or combinations thereof.
  • the formulations of the present invention can optionally be used with other active agent or agents in combined form.
  • other active agent refers to various vitamins and/or minerals required for human body.
  • Dosage forms can be taken separately, together or sequentially; though they can also be taken by combining genistein with the other active agent or agents in a single dosage form for combined therapy.
  • the other active agent or agents that can be used together with genistein in combined therapy can be minerals such as calcium, potassium, magnesium, iron, sodium, zinc; vitamins such as vitamin A, B vitamins such as Bl , B12, B6 and/or folic acid, vitamin C, vitamin D, vitamin E.
  • vitamins such as vitamin A, B vitamins such as Bl , B12, B6 and/or folic acid, vitamin C, vitamin D, vitamin E.
  • One or two of the other active agents listed above can be combined with genistein in combined therapy.
  • the present invention comprises binary and ternary combinations of genistein with the other active agents explained above.
  • the other active agent or agents that can be used in combined therapy can be produced together with genistein and by the same production method, though they can also be prepared by producing the active agent formulations separately and then combining them.
  • Effervescent formulation comprising genistein
  • the effervescent genistein formulation that shall be prepared according to the formulation given above is prepared by the production method below:
  • Effervescent couple is wet granulated with the granulation solution which is composed of mixture of deionised water and PVP,
  • the granules are dried, sieved and genistein and the other excipients are added into the granules and they are mixed until a homogeneous mixture is obtained,
  • Effervescent formulation comprising Genistein, Calcium and Vitamin D
  • the effervescent genistein, calcium and vitamin D formulation that shall be prepared according to the formulation given above is produced by the production method below:
  • the effervescent acid, effervescent base and calcium carbonate are wet granulated with the granulation solution which is composed of mixture of deionised water and PVP,
  • the granules are dried, sieved and genistein, Vitamin D and other excipients are added into the granules and they are mixed until a homogeneous mixture is obtained,

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne un procédé de production de formulations effervescentes comprenant au moins un composant appartenant au groupe des isoflavones.
PCT/TR2012/000120 2011-08-08 2012-08-07 Procédé de production pour formulations pharmaceutiques comprenant une isoflavone WO2013043142A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
TR201107832 2011-08-08
TR2011/07832 2011-08-08

Publications (1)

Publication Number Publication Date
WO2013043142A1 true WO2013043142A1 (fr) 2013-03-28

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/TR2012/000119 WO2013074046A1 (fr) 2011-08-08 2012-08-07 Formulations pharmaceutiques comprenant de l'isoflavone
PCT/TR2012/000120 WO2013043142A1 (fr) 2011-08-08 2012-08-07 Procédé de production pour formulations pharmaceutiques comprenant une isoflavone

Family Applications Before (1)

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PCT/TR2012/000119 WO2013074046A1 (fr) 2011-08-08 2012-08-07 Formulations pharmaceutiques comprenant de l'isoflavone

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WO (2) WO2013074046A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013089654A1 (fr) * 2011-12-16 2013-06-20 Mahmut Bilgic Formulations effervescentes comprenant de la génistéine
CN105853376A (zh) * 2016-05-27 2016-08-17 常州市新鸿医药化工技术有限公司 一种制备叶酸颗粒的方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0670160A1 (fr) * 1994-03-01 1995-09-06 Gerhard Dr. Gergely Produit granulaire ou comprimé contenant un système effervescent et un agent actif pharmaceutique, et son procédé de préparation
CN1589786A (zh) * 2003-09-01 2005-03-09 郑州博凯医药保健品有限公司 一种含大豆异黄酮的复合泡腾制剂
WO2011093825A2 (fr) * 2010-01-29 2011-08-04 Mahmut Bilgic Formes posologiques effervescentes comprenant un antibiotique du groupe des céphalosporines
WO2012002918A1 (fr) * 2010-06-03 2012-01-05 Mahmut Bilgic Formulation pour l'ostéoporose

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2001227030A1 (en) * 2000-11-22 2002-06-03 Lupin Laboratories Limited Pharmaceutical composition for controlled release of an active ingredient
DE10127897B4 (de) 2001-06-08 2006-04-20 Bionorica Ag Manteltablette mit Pflanzentrockenextrakten
WO2010097643A1 (fr) * 2009-02-24 2010-09-02 Novatech Istrazivanje D.O.O. Formulation à base de zéolithe micronisée, d'extrait de thé vert et de génistéine en tant qu'agent thérapeutique pour réduire le poids corporel et la cellulite

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0670160A1 (fr) * 1994-03-01 1995-09-06 Gerhard Dr. Gergely Produit granulaire ou comprimé contenant un système effervescent et un agent actif pharmaceutique, et son procédé de préparation
CN1589786A (zh) * 2003-09-01 2005-03-09 郑州博凯医药保健品有限公司 一种含大豆异黄酮的复合泡腾制剂
WO2011093825A2 (fr) * 2010-01-29 2011-08-04 Mahmut Bilgic Formes posologiques effervescentes comprenant un antibiotique du groupe des céphalosporines
WO2012002918A1 (fr) * 2010-06-03 2012-01-05 Mahmut Bilgic Formulation pour l'ostéoporose

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE WPI Week 200545, Derwent World Patents Index; AN 2005-436088, XP002691627 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013089654A1 (fr) * 2011-12-16 2013-06-20 Mahmut Bilgic Formulations effervescentes comprenant de la génistéine
CN105853376A (zh) * 2016-05-27 2016-08-17 常州市新鸿医药化工技术有限公司 一种制备叶酸颗粒的方法

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