CN102688249A - Medicinal composition containing strontium salt - Google Patents
Medicinal composition containing strontium salt Download PDFInfo
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- CN102688249A CN102688249A CN2012101484281A CN201210148428A CN102688249A CN 102688249 A CN102688249 A CN 102688249A CN 2012101484281 A CN2012101484281 A CN 2012101484281A CN 201210148428 A CN201210148428 A CN 201210148428A CN 102688249 A CN102688249 A CN 102688249A
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Abstract
The invention relates to a medicinal composition containing strontium salts and vitamin D derivatives. Mixed with auxiliary materials acceptable on pharmacy, the medicinal composition of the invention can be prepared into oral formulations such as particulate granules, common tablets, chewable tablets, dispersible tablets, orally disintegrating tablets, effervescent tablets, buccal tablets, capsules, softgels, sustained release tablets, sustained release capsules, oral solutions, syrups, etc., and can be used to prevent and treat various primary or secondary osteoporosis.
Description
Technical field
The present invention is a kind of Pharmaceutical composition that contains strontium salt, belongs to medical technical field.
Background technology
Osteoporosis is a kind of, bone micro-structure destruction low with the bone amount, causes bone fragility to increase, be prone to take place fracture and is the general osteopathia of characteristic.The osteoporotic common reason of women is that the postmenopausal estrogen level descends rapidly, and bone metabolism is accelerated, and causes the loss of equilibrium between bone formation and the bone resorption.Major part is used to treat the mechanism that osteoporotic medicine is based on anti-bone resorption, reduces over-drastic bone metabolism, keeps normal bone amount and bone strength, thereby has reduced the fracture incidence rate behind the postmenopausal women.The metabolic medicine to osteoplastic effect greater than bone resorption, thereby increased the bone reconstruction, finally facilitate the bone amount to increase the improvement with bone micro-structure, can be in the incidence rate that reduces fracture to a greater extent.
Vitamin D and derivant thereof can promote absorption and the renal tubules heavy Absorption of Phosphorus of mucous membrane of small intestine brush border to calcium; Increasing blood calcium, serium inorganic phosphorus concentration; Collaborative parathyroid hormone (PTH), calcitonin (CT) promote old bone to discharge calcium phosphate, keep and regulate plasma calcium, phosphorus normal concentration.Vitamin D impels calcific deposit in new bone formation position, and hydroxide phosphate is deposited in bone, promotes bone calcification and function of osteoblast and osteoid tissue ripe, is a kind of clinical bone activator commonly used, but can not suppresses the absorption of bone.
Strontium salt has anti-bone resorption and promotes the bone formation dual function as a kind of new chemical compound, thereby makes it become the osteoporotic active drug of treatment, has represented new important development direction on osteoporosis treatment.Strontium is a kind of trace element that can be used as bone label of in Scottish lead ore, finding in 16th century.The difference of it and radiostrontium is radiostrontium to the toxic effect of osteocyte, and the radioactive strontium of tool can not produce beneficial effect [34] to bone.Have the scholar in animal experiment, to prove, strontium salt under the prerequisite that does not influence BMC, can weaken bone resorption and simultaneously enhance bone form and increase the bone amount, this has just increased the probability that strontium becomes the osteoporosis therapy medicine.
Summary of the invention
The present invention is a kind of Pharmaceutical composition that contains strontium salt, is to combine with following two kinds of active component and proper auxiliary materials;
Active component 1: a kind of strontium salt, be selected from Strontium Ranelate, succinic acid strontium etc.,
Active component 2: a kind of vitamin D-derivatives is selected from alfacalcidol, paricalcitol 19-Nor-1,25-dihydroxyvitamin D2, Maxacalcitol, Chinese mugwort ground ostelin, falecalcitriol, calcitriol etc.;
The unit consumption of active component 1 is: Strontium Ranelate 0.2-8g, preferred 1-2g;
The unit consumption of active component 2 is: alfacalcidol 0.05-2ug, preferred 0.25-0.5ug; Paricalcitol 19-Nor-1,25-dihydroxyvitamin D2 0.2-10ug, preferred 1-2ug, Maxacalcitol 0.5-50ug, preferred 2.5-10ug; Chinese mugwort ground ostelin 0.1-3ug, preferred 0.5-0.75ug; Falecalcitriol 0.03-15ug, preferred 0.15-3ug;
Described compositions is oral formulations, comprises granule, ordinary tablet, chewable tablet, dispersible tablet, oral cavity disintegration tablet, effervescent tablet, buccal tablet, capsule, soft capsule, slow releasing tablet, slow releasing capsule, oral administration solution, syrup etc.;
Can be used for the prevention of osteoporosis and the treatment of various former or secondary.
The specific embodiment
Come the preparation of strontium salt and vitamin D analog derivative done further specifying through following instance, but be not limited in following instance.
Embodiment 1
Strontium Ranelate, alfacalcidol suspension mix granule formulation
Prescription:
Method for preparing:
Lemon yellow is joined in the PVP-k30 aqueous solution, subsequent use after the stirring and dissolving.
Recipe quantity is crossed 80 mesh sieves respectively to Strontium Ranelate, alfacalcidol, sucrose, L-HPC, strawberry essence, behind the mix homogeneously, add the 2%PVP-k30 aqueous solution and make soft material in right amount, 24 mesh sieves are granulated, drying, granulate, packing.
Embodiment 2
Succinic acid strontium, alfacalcidol suspension mix granule formulation
Prescription:
Method for preparing:
Carmine is joined in the PVP-k30 aqueous solution, subsequent use after the stirring and dissolving.
Recipe quantity is crossed 80 mesh sieves respectively to succinic acid strontium, alfacalcidol, sucrose, L-HPC, strawberry essence, behind the mix homogeneously, add the 2%PVP-k30 aqueous solution and make soft material in right amount, 24 mesh sieves are granulated, drying, granulate, packing.
Embodiment 3
Strontium Ranelate, Maxacalcitol suspension mix granule formulation
Prescription:
Method for preparing:
Carmine is joined in the PVP-k30 aqueous solution, subsequent use after the stirring and dissolving.
Recipe quantity Strontium Ranelate, Maxacalcitol, sucrose, L-HPC, orange flavor are crossed 80 mesh sieves respectively, behind the mix homogeneously, add the 5%PVP-k30 aqueous solution and make soft material in right amount, 24 mesh sieves are granulated, drying, granulate, packing.
Embodiment 4
Succinic acid strontium, Maxacalcitol suspension mix granule formulation
Prescription:
Method for preparing:
Carmine is joined in the PVP-k30 aqueous solution, subsequent use after the stirring and dissolving.
Recipe quantity Strontium Ranelate, Maxacalcitol, sucrose, L-HPC, orange flavor are crossed 80 mesh sieves respectively, behind the mix homogeneously, add the 5%PVP-k30 aqueous solution and make soft material in right amount, 24 mesh sieves are granulated, drying, granulate, packing.
Embodiment 5
Strontium Ranelate, falecalcitriol suspension mix granule formulation
Prescription:
Method for preparing:
Sunset yellow is joined in the PVP-k30 aqueous solution, subsequent use after the stirring and dissolving.
Recipe quantity Strontium Ranelate, falecalcitriol, sucrose, L-HPC, orange flavor are crossed 80 mesh sieves respectively, behind the mix homogeneously, add the 4%PVP-k30 aqueous solution and make soft material in right amount, 24 mesh sieves are granulated, drying, granulate, packing.
Embodiment 6
Succinic acid strontium, falecalcitriol suspension mix granule formulation
Prescription:
Method for preparing:
Sunset yellow is joined in the PVP-k30 aqueous solution, subsequent use after the stirring and dissolving.
Recipe quantity Strontium Ranelate, falecalcitriol, sucrose, L-HPC, orange flavor are crossed 80 mesh sieves respectively, behind the mix homogeneously, add the 4%PVP-k30 aqueous solution and make soft material in right amount, 24 mesh sieves are granulated, drying, granulate, packing.
Embodiment 7
Strontium Ranelate, paricalcitol 19-Nor-1,25-dihydroxyvitamin D2 effervescent tablet
Prescription:
Method for preparing:
Strontium Ranelate, paricalcitol 19-Nor-1,25-dihydroxyvitamin D2, mannitol, lactose, citric acid, sodium bicarbonate are crossed 100 mesh sieves respectively, behind the mix homogeneously, add ethanol solution and make soft material in right amount; 24 mesh sieves are granulated; Drying, 40 mesh sieve granulate add aspartame, protein sugar, PEG6000; Tabletting behind the mix homogeneously promptly gets.
Embodiment 8
Succinic acid strontium, Chinese mugwort ground ostelin slow releasing capsule
Prescription:
Method for preparing:
Get the II acrylic resin earlier and add the solution that dehydrated alcohol is prepared into 3 %, subsequent use; Other gets EC and adds dehydrated alcohol and be prepared into 3% solution, and is subsequent use.
Succinic acid strontium, Chinese mugwort ground ostelin, HPMC (K100M), microcrystalline Cellulose, CMC-Na are crossed 80 mesh sieves respectively, behind the mix homogeneously, with the dehydrated alcohol mixed liquor system soft material of II acrylic resin, EC; Cross 18 mesh sieves, system wet granular, 50 ℃ of aeration-dryings; Granulate, packing.
Embodiment 9 compounds are to the influence of rat bone density, bone calcium phosphorus, blood calcium phosphorus
Experimental technique:
The foundation of osteoporosis model and medication: the Wistar rat is divided into 5 groups at random, and 6 every group, each component cage is fed.All animals are with 10% chloral hydrate intraperitoneal injection of anesthesia, dosage 3ml/kg.The 1st group of matched group carries out sham-operation, exposes bilateral ovaries in external at the aseptic condition median incision of lower abdomen, also receives behind the 1min.The 2nd～4 group of aseptic condition median incision of lower abdomen, complete excision bilateral ovaries, thoroughly hemostasis back layer-by-layer suture.After the operation, each is organized rat and divides cage to feed.Anti-infective therapy (wound disinfection, intramuscular injection gentamycin, 3d continuously).Rat ovary excision back the 3rd week beginning gastric infusion 2ml/100g, continuous 8 weeks.Matched group (equal-volume normal saline), model group (equal-volume normal saline), Strontium Ranelate group, alfacalcidol group, compound recipe Strontium Ranelate+alfacalcidol group.Each is organized rat and all feeds with standard feed, free diet.
Correlated samples is gathered with index and is detected: behind last 1 administration 24h, with chloral hydrate anesthesia, with the bone density (BMD) of dual intensity X line borne densitometers mensuration femur, spinal column and whole body bone, weigh; Get the serum that the blood centrifugalize obtains, measure TALP (ALP) activity, serium inorganic phosphorus, blood calcium; Get the right side tibia, reject meat, muscle, put in the exsiccator, dry to constant weight in 105 ℃, record weight, ashing is weighed then, with diluted hydrochloric acid dissolution, standardize solution, is used for bone Ca, P measures, and the calculating bone ash accounts for the proportion of bone.
Experimental result:
Model group and matched group relatively, the BMD of femur, spinal column and whole body bone obviously descends (P < 0.05), shows that oophorectomize can make rat BMD obviously reduce the generation osteoporosis.Experiment finishes the back and observes the Strontium Ranelate group; The BMD of alfacalcidol group, compound recipe Strontium Ranelate+alfacalcidol group is significantly higher than model group (P < 0.05); Show that the experiment medicine can significantly improve the BMD of removal ovary rat; And the effect of compound recipe Strontium Ranelate+alfacalcidol group is particularly remarkable, and prompting compound recipe Strontium Ranelate+alfacalcidol is having certain synergism aspect the raising BMD.
The influence of table 1 couple rat BMD (
± S, n=10)
After the ovariectomized rats in the serum ALP, Ca, P content significantly raise, bone ash heavily reaches bone Ca, bone P content and but obviously descends, when having pointed out climacteric in the bone Ca, P deposition slow down, osteoporotic process.Compound recipe Strontium Ranelate+alfacalcidol is this process of antagonism significantly.
Table 2 is respectively organized ALP in the rat blood serum, Ca, P content relatively (
± S)
Table 3 respectively organize the rat bone ash heavy and, Ca, P content relatively (
± S)
Claims (5)
1. a Pharmaceutical composition that contains strontium salt is characterized in that, is to combine with following two kinds of active component and proper auxiliary materials:
Active component 1: a kind of strontium salt is selected from Strontium Ranelate, succinic acid strontium etc.;
Active component 2: a kind of vitamin D-derivatives is selected from alfacalcidol, paricalcitol 19-Nor-1,25-dihydroxyvitamin D2, Maxacalcitol, Chinese mugwort ground ostelin, falecalcitriol, calcitriol etc.
2. the described compositions of claim 1 is characterized in that, the unit consumption of active component 1 is: Strontium Ranelate 0.2-8g, preferred 1-2g.
3. the described compositions of claim l is characterized in that, the unit consumption of active component 2 is: alfacalcidol 0.05-2ug, preferred 0.25-0.5ug; Paricalcitol 19-Nor-1,25-dihydroxyvitamin D2 0.2-10ug, preferred 1-2ug, Maxacalcitol 0.5-50ug, preferred 2.5-10ug; Chinese mugwort ground ostelin 0.1-3ug, preferred 0.5-0.75ug; Falecalcitriol 0.03-15ug, preferred 0.15-3ug.
4. the described compositions of claim l; It is characterized in that; This Pharmaceutical composition is an oral formulations, comprises granule, ordinary tablet, chewable tablet, dispersible tablet, oral cavity disintegration tablet, effervescent tablet, buccal tablet, capsule, soft capsule, slow releasing tablet, slow releasing capsule, oral administration solution, syrup etc.
5. the described compositions of claim l can be used for the prevention of osteoporosis and the treatment of various former or secondary.
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| CN2012101484281A CN102688249A (en) | 2012-05-14 | 2012-05-14 | Medicinal composition containing strontium salt |
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|---|---|---|---|
| CN2012101484281A CN102688249A (en) | 2012-05-14 | 2012-05-14 | Medicinal composition containing strontium salt |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142623A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Calcitriol and strontium ranelate suspension granule and preparation method thereof |
| CN104711313A (en) * | 2015-03-18 | 2015-06-17 | 上海皓元生物医药科技有限公司 | Preparation method for eldecalcitol intermediate |
| JP2018080168A (en) * | 2016-11-10 | 2018-05-24 | 日産化学工業株式会社 | Preparation of vitamin d3 derivative |
| CN110121348A (en) * | 2016-12-28 | 2019-08-13 | 中外制药株式会社 | The pharmaceutical composition of solid dispersions and oil dispersion comprising ED-71 |
| KR20210024566A (en) | 2018-06-27 | 2021-03-05 | 추가이 세이야쿠 가부시키가이샤 | Pharmaceutical composition comprising oil dispersion containing ED-71 and its epoxy body in oil and fat |
-
2012
- 2012-05-14 CN CN2012101484281A patent/CN102688249A/en active Pending
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103142623A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Calcitriol and strontium ranelate suspension granule and preparation method thereof |
| CN103142623B (en) * | 2013-03-21 | 2014-04-16 | 青岛正大海尔制药有限公司 | Calcitriol and strontium ranelate suspension granule and preparation method thereof |
| CN104711313A (en) * | 2015-03-18 | 2015-06-17 | 上海皓元生物医药科技有限公司 | Preparation method for eldecalcitol intermediate |
| CN104711313B (en) * | 2015-03-18 | 2018-01-30 | 上海皓元生物医药科技有限公司 | A kind of preparation method of the ossified alcohol intermediates of Ai Er |
| JP2018080168A (en) * | 2016-11-10 | 2018-05-24 | 日産化学工業株式会社 | Preparation of vitamin d3 derivative |
| JP7085105B2 (en) | 2016-11-10 | 2022-06-16 | 日産化学株式会社 | Vitamin D3 derivative formulation |
| CN110121348A (en) * | 2016-12-28 | 2019-08-13 | 中外制药株式会社 | The pharmaceutical composition of solid dispersions and oil dispersion comprising ED-71 |
| KR20190101981A (en) | 2016-12-28 | 2019-09-02 | 추가이 세이야쿠 가부시키가이샤 | Pharmaceutical composition comprising solid dispersion and oily dispersion of ED-71 |
| KR20220025177A (en) | 2016-12-28 | 2022-03-03 | 추가이 세이야쿠 가부시키가이샤 | Medicinal composition comprising ed-71 solid dispersion and oil dispersion |
| KR20210024566A (en) | 2018-06-27 | 2021-03-05 | 추가이 세이야쿠 가부시키가이샤 | Pharmaceutical composition comprising oil dispersion containing ED-71 and its epoxy body in oil and fat |
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Application publication date: 20120926 |