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
  • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
  • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
• • 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
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
• • 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
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
  • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P19/00—Drugs for skeletal disorders
  • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
  • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis

Definitions

• composition with a content of calcium or mixture of calcium and vitamin D or mixture of calcium and magnesium in a new formulation
• the invention from the pharmaceutical field relates to a therapeutical preparation with the content of calcium or mixture of calcium and vitamin D or mixture of calcium and magnesium for a long-term peroral use for prevention and treatment of primary and secondary osteoporosis and for correction of hyperphosphataemia in patients in advanced stages of renal insufficiency.
• the formulations with a content of calcium have used as a source of calcium its chemically defined therapeutic acceptable compounds, mainly in the form of effervescent tablets, tablets, solutions, powders and the like, or as a source have served treated animal and mineral raw materials.
• the drawback of the e.g. effervescent tablets is the fact, that after a longer time they are refused by patients, because they can, in addition to others, induce shifts in the acid-base balance to a metabolic alkalosis, the transport of calcium into bloodstream is fast and calcium concentration may exceed the safe level to cause temporary hypercalcaemia, which is dangerous from the point of view of origin and development of atherosclerosis.
• the preparation can at a long-term administration induce metabolic acidosis connected with increasing washing up of calcium from the bony mass.
• the drawback of biopreparations can be the presence of undesirable admixtures and non-standard content of biologically usable cations.
• Another drawback is more time, raw materials and energy consuming manufacture.
• the substance of the pharmaceutical composition according to this invention is the dosaged formulation, containing as the active substance calcium in the amount of from 150 mg to 1500 mg, preferably from 200 mg to 600 mg, or the mixture of calcium with vitamin D, wherein vitamin D is in the amount of from 100 I.U to 1000 I.U, preferably from 400 I.U to 900 I.U, or the mixture of calcium and magnesium, wherein magnesium is in the amount of from 20 mg to 500 mg, preferably from 150 mg to 300 mg. Active substances containing calcium and magnesium are micronized so that at least 80 % of the particles are less than 75 micrometers in size.
• the pharmaceutical composition according to the invention is in the form of instant powder, which after adding a liquid (water, milk, tea and the like), forms after a short mixing a pudding-like gelled suspension, tolerated during use by the patients, who use the preparations with above mentioned active substances for preventive or therapeutic reasons.
• a liquid water, milk, tea and the like
• the advantage is the precise dosage of the active substances.
• a balanced mixture of micronized active substances and adjuvants is prepared either by simple mixing or in the case of need of further machine treatment by granulating by means of water and ethanol mixture consisting of water in the range of 30 to 80 % by weight and ethanol in the range of 20 to 70 % by weight, preferably 60 % by weight of water and 40 % by weight of ethanol and by subsequent drying either in a chamber, in vacuo, by fluidization, or by microwave irradiation at the temperature of 30 to 60 °C, preferably 35 to 45 °C.
• the obtained mixture appropriately adjusted in therapeutic doses into single dosage packages formed by a thermosealed combined foil preventing a passage of vapours and gases, is chemically and physically stable and enables a simple manipulation in the preparation of suspension for therapeutic or preventive use by the patient.
• the formulation according to this invention contains in addition to to the micronized active substances from the group of therapeutically acceptable salts of calcium, magnesium or from another sources such as treated eggshells, calcium shells of animals or inorganic minerals, and vitamins, additional adjuvants which are responsible for possibility of forming a gelled, pudding-like suspension tolerated by the patients.
• starch derivatives preferably distarchphosphate in an amount of from 5 to 40 % by weight, preferably from 15 to 25 % by weight.
• Mono and/or disaccharides preferably saccharoses, in an amount of from 10 to 80 % by weight, preferably from 20 to 40 % by weight.
• Pharmaceutically usable phosphoric acid salts such as sodium hydrogenphosphate in an amount of from 0.05 to 0.45 % by weight, preferably from 0.1 to 0.35 % by weight and sodium phosphate in an amount of from 0.2 to 2.0 % by weight, preferably from 0.7 to 1.4 % by weight.
• Corrigents of taste and odour of the pharmaceutical composition from the group of natural and naturally identical aromas in amounts from 0.1 to 5 % by weight, preferably from 0.5 to 1 % by weight, from the group of artificial sweetening agents in amounts from 0.035 to 0.20 % by weight, preferably from 0.05 to 0.15 % by weight, from the group of pharmaceutically usable organic acids, preferably citric acid in an amount of from 0.1 to 4 % by weight, preferably from 0.8 to 1 ,8 % by weight and salts thereof, preferably trisodiumcitrate in an amount from 0.05 to 2.0 % by weight, preferably from 0.1 to 0.5 % by weight, cocoa powder in an amount of from 1 to 30 % by weight, preferably from 10 to 20 % by weight.
• Substances correcting the appearance from the group of permitted natural and synthetic coloring agents in amounts from 0.001 to 0.005 % by weight, preferably from 0.002 to 0.004 % by weight.
• Substances facilitating technological process which prevent undesirable agglomeration of particles and antistatic affecting substances from the group of silicon oxides in amounts from 0.1 to 7.0 % by weight, lubricating agents from the group of magnesium, calcium and aluminium salts of higher fatty acids, preferably calcium stearate, or magnesium stearate in amounts of from 0.1 to 0.7 % by weight, preferably from 0.2 to 0.4 % by weight, or substances from the group of silicon organic compounds, preferably dimethylpolysiloxane in an amount of from 0.07 to 0.9 % by weight, preferably from 0.1 to 0.5 %.by weight.
• Preserving agents such as sorbic acid in an amount of from 0.01 to 0.04 % by weight, its salts, preferably sodium and potassium salt in amounts of from 0.01 to 0.05 % by weight, benzoic acid in an amount of from 0.006 to 0.02 % by weight, its salts, preferably sodium salt in an amount of from 0.01 to 0.03 % by weight, p-hydroxybenzoic acid esters in amounts of from 0.001 to 0.08 % by weight, preferably from 0.01 to 0.06 % by weight and salts thereof, preferably sodium and potassium salt in amounts of from 0.001 to 0.08 % by weight.
• sorbic acid in an amount of from 0.01 to 0.04 % by weight
• its salts preferably sodium and potassium salt in amounts of from 0.01 to 0.05 % by weight
• benzoic acid in an amount of from 0.006 to 0.02 % by weight
• its salts preferably sodium salt in an amount of from 0.01 to 0.03 % by weight
• Example 1 a) pharmaceutical composition, containing in 1 dose:
• Citric acid 0.0300 g 1.00 %
• Micronized calcium carbonate is agitated in a suitable apparatus along with saccharose and starch derivative, carageenan is added and agitation continued.
• sodium hydrogenphosphate, sodium phosphate, citric acid and sodium citrate which are adjusted by sieving through a screen of the mesh size of 1.0 mm, are admixed. After homogeneity is reached, this mixture is added into the first mixture. Both mixtures are agitated, along at least for 20 minutes and after homogenization is completed, dimethylpolysiloxane in the mixture with maltodextrin and powdered orange aroma are finally added.
• the obtained mixture is adjusted into one-dose sachets from combined foil, preferably PP/AI/PE, with one dose in the amount of 3.000 g.
• This way prepared 1 dose contains 500 mg of biologically usable calcium.
• Example 2 a) pharmaceutical composition, containing in 1 dose:
• Cocoa powder 0.5000 g 16.66 %
• Micronized calcium carbonate is agitated in a suitable apparatus along with the starch derivative, saccharose, carageenan, sodium hydrogenphosphate, sodium phosphate and cocoa powder pre-sieved through a screen of the mesh side of 1.25 mm, until homogeneous.
• the obtained mixture is moistened with a necessary amount of water and ethanol mixture until a desirable graininess is reached.
• the granulate is dried to moisture not exceeding 2,5 % by weight, its particles are adjusted to a size suitable for an adjustment and filled into one-dose sachets from combined foil PP/AI/PE with one dose in the amount of 3.000 g. This way prepared 1 dose contains 500 mg of biologically usable calcium.
• composition containing in 1 dose:
• Micronized calcium carbonate is agitated in a suitable pharmaceutical apparatus along with starch derivative, saccharose, carageenan, sodium hydrogenphosphate and sodium phosphate pre-sieved through a screen of the mesh side of 1.25 mm, until homogeneity is reached.
• This mixture is under agitation gradually moistened with the necessary amount of water and ethanol mixture and granulated.
• the granulate is dried by fluidization at the temperature of fed air 50 °C until residual moisture not exceeding 2.0 % by weight is reached.
• the dry mixture is transferred into a mixing device, desirable amounts of powdered vanilla aroma and colorant are added and the mixture is agitated until homogeneity is reached.
• This process is the mixture prepared for adjustment into one-dose sachets from combined foil, with one ' dose in the amount of 3.000 g. This way prepared 1 dose contains 500 mg of biologically usable calcium.
• composition containing in 1 dose:
• Citric acid 0.0300 g 1.00 %
• Powdered peach aroma 0.0250 g 0.83 %
• Micronized calcium carbonate is agitated in a suitable pharmaceutical apparatus along with saccharose and starch derivative, carageenan is added and agitation continued. After the accomplished homogenization sodium hydrogenphosphate, sodium phosphate, citric acid and sodium citrate pre-adjusted through a screen having the mesh side of 1.25 mm are stepwise added.
• colecalciferol is diluted with the mixture prepared before in the ratio of 1 : 50. Diluted colecalciferol is transferred into the mixture prepared before and admixed by intensive agitation until homogeneous. Yellow synthetic colorant, powdered peach aroma, maltodextrin and dimethylpolysiloxane are then stepwise added to the mixture. After homogenization is completed, the mixture is prepared to be adjusted into a combined three-layer foil PP/AI/PE in the doses of 3.000 g, what is one dose and this contains 500 mg of biologically usable calcium and 800 I.U. of vitamin D3.
• composition containing in 1 dose:
• Powdered coconut aroma 0.0250 g 0.83 %
• composition containing in 1 dose:
• Citric acid 0.0300 g 1.00 %
• Powdered citric aroma 0.0250 g 0.83 %
• Micronized magnesium hydroxidecarbonate and calcium carbonate are admixed in a suitable apparatus with a half amounts of saccharose and starch derivative. Carageenan is added, the mixture is perfectly commixed and the rests of saccharose and starch derivative are added. After accomplished homogenization previously homogenized mixture of sodium hydrogenphosphate, sodium phosphate, citric acid and sodium citrate with the adjusted size of particles through a screen of the mesh side of 1.0 mm is added to this mixture. When homogenization of these mixtures is completed, dimethylpolysiloxane, maltodextrin and powdered citric aroma are stepwise added.
• prepared 1 dose contains 200 mg of biologically usable magnesium and 250 mg of biologically usable calcium
• the invention is useful in the pharmaceutical industry in the manufacture of therapeutic preparations for treatment and prevention of osteoporosis.

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• Health & Medical Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Veterinary Medicine (AREA)
• Pharmacology & Pharmacy (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• Chemical & Material Sciences (AREA)
• Epidemiology (AREA)
• Physical Education & Sports Medicine (AREA)
• Orthopedic Medicine & Surgery (AREA)
• Rheumatology (AREA)
• Nutrition Science (AREA)
• Physiology (AREA)
• Zoology (AREA)
• Inorganic Chemistry (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Medicinal Preparation (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

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• 2000
  • 2000-04-06 SK SK498-2000A patent/SK284948B6/sk not_active IP Right Cessation
• 2001
  • 2001-03-15 WO PCT/SK2001/000004 patent/WO2001076610A1/en not_active Application Discontinuation
  • 2001-03-15 RU RU2002130196/15A patent/RU2002130196A/ru unknown
  • 2001-03-15 EP EP01914325A patent/EP1274447A1/en not_active Withdrawn
  • 2001-03-15 CZ CZ20023292A patent/CZ303069B6/cs not_active IP Right Cessation
  • 2001-03-15 AU AU2001239668A patent/AU2001239668A1/en not_active Abandoned
  • 2001-03-15 MD MDA20020265A patent/MD2722B2/ro unknown
  • 2001-03-15 EE EEP200200584A patent/EE200200584A/xx unknown
  • 2001-03-15 PL PL01357777A patent/PL357777A1/pl not_active Application Discontinuation
• 2002
  • 2002-10-29 BG BG107227A patent/BG107227A/xx unknown

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