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Pharmaceutical compositions comprising bisphosphonate derivatives and high-dose cholecalciferol

A technology for cholecalciferol and composition, which is applied in the field of pharmaceutical compositions containing bisphosphonate derivatives and high-dose cholecalciferol, can solve the problems of difficulty in preparing calcitriol, inability to increase vitamin D, and the like, and achieves the Increase drug compliance, resolve unstable effects

Inactive Publication Date: 2013-07-10
HANLIM PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, when designing a formulation for monthly administration, there is a problem of not being able to increase the amount of vitamin D in order to obtain the desired blood vitamin D level
Moreover, the half-life of vitamin D in the body is approximately two months, and the half-life of calcitriol, known as an active vitamin D derivative, is only 15 hours, making it difficult to formulate calcitriol for monthly administration

Method used

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  • Pharmaceutical compositions comprising bisphosphonate derivatives and high-dose cholecalciferol
  • Pharmaceutical compositions comprising bisphosphonate derivatives and high-dose cholecalciferol
  • Pharmaceutical compositions comprising bisphosphonate derivatives and high-dose cholecalciferol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-6 and comparative example 1-3

[0050] Examples 1-6 and Comparative Examples 1-3. Film-coated tablets containing risedronate sodium and cholecalciferol

[0051] Each film-coated tablet containing risedronate sodium and cholecalciferol was prepared according to the components and amounts shown in Tables 1 and 2 below. The amounts shown in Tables 1 and 2 are per tablet.

[0052] Mix cholecalciferol powder (40,000 IU / mg), first stabilizer (butylated hydroxytoluene, butylated hydroxyanisole and / or DL-α-tocopheryl acetate) and hydroxypropyl cellulose under stirring Dissolved in ethanol. The resulting solution was mixed with microcrystalline cellulose in a high speed mixer for about 30 seconds to obtain a slurry. The resulting slurry was evenly spread on a dry flat plate, then dried at a temperature of about 40° C., followed by grinding with a grinder (Fitz mill), thereby obtaining granules. Pass the granules through a 40-mesh sieve to obtain granules with cholecalciferol adsorbed on the surface of the microcry...

Embodiment 7-9

[0061] Examples 7-9. Film-coated tablets containing ibandronate sodium and cholecalciferol

[0062] Each film-coated tablet containing ibandronate sodium and cholecalciferol was prepared according to the components and amounts shown in Table 3 below. The amounts shown in Table 3 are per tablet.

[0063] Mix cholecalciferol powder (40,000 IU / mg), first stabilizer (butylated hydroxytoluene, butylated hydroxyanisole and / or DL-α-tocopheryl acetate) and hydroxypropyl cellulose under stirring Dissolved in ethanol. The resulting solution was mixed with microcrystalline cellulose in a high speed mixer for about 30 seconds to obtain a slurry. The resulting slurry was evenly spread on a dry flat plate, then dried at a temperature of about 40° C., followed by grinding with a grinder (Fitz mill), thereby obtaining granules. Pass the granules through a 40-mesh sieve to obtain granules with cholecalciferol adsorbed on the surface of the microcrystalline cellulose.

[0064] The granules ...

experiment example 1

[0069] Experimental Example 1: Stability Test

[0070] Stability tests were performed on the film-coated tablets prepared in Examples 1-9 and Comparative Examples 1-3. All the tablets were exposed at 50° C. for 2 weeks, and on the 7th and 14th days, the amount of active ingredients in the tablets, ie the amount of risedronate sodium or ibandronate sodium and cholecalciferol, was determined.

[0071] (1) The amount of risedronate sodium or ibandronate sodium

[0072] According to the stability test, the amount of risedronate sodium or ibandronate sodium determined on the 7th day and the 14th day is shown in Table 4.

[0073] Table 4

[0074]

[0075] Example 9

[0076] From the results shown in Table 4, it can be confirmed that risedronate sodium and ibandronate sodium maintained stability in the preparation of the present invention and in the preparation of the comparative example.

[0077] (2) The amount of cholecalciferol

[0078] According to the s...

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Abstract

The present invention relates to pharmaceutical compositions for preventing or treating osteoporosis, which comprise bisphosphonate-based compounds such as risedronic acids or the salts thereof, ibandronic acids or the salts thereof, or the like, and high-dose cholecalciferol, and which are to be administered once a month. The present invention also relates to pharmaceutical compositions for preventing or treating osteoporosis to be administered once a month, comprising: (a) cholecalciferol-containing granules obtained by adsorbing, to microcrystalline cellulose, the solution obtained by dissolving, into ethanol or an aqueous ethanol solution: (i) 24,000 to 50,000 IUs of cholecalciferol; (ii) one or more first stabilizers selected from among tocopheryl acetate, butylated hydroxytoluene and butylated hydroxyanisole; and iii) a binder; (b) mannitol as a second stabilizer; and (c) risedronic acids or the salts thereof or ibandronic acids or the salts thereof.

Description

[0001] This application is a divisional application with an application date of June 17, 2010 and an application number of 201080041701.X. Claim the priority of the earlier Korean application KR10-2009-0088480 with a priority date of September 18, 2009. technical field [0002] The present invention relates to a pharmaceutical composition for preventing or treating osteoporosis administered once a month, the pharmaceutical composition comprising bisphosphonate derivatives, such as risedronic acid (or its salt) or ibandronic acid ( or its salts), and high doses of cholecalciferol equivalent to 24,000-50,000 IU. Background technique [0003] Osteoporosis is a metabolic disease that causes osteopenia and changes in bone microarchitecture, thus predisposing to bone damage, which ultimately leads to fracture risk. Osteoporosis is prevalent in the elderly population and poses a high societal burden due to fracture-related complications and increased costs of their treatment. For...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675A61K31/663A61P19/10A61K31/593
CPCA61K9/2077A61K31/59A61K31/675A61K9/1623A61K9/1652A61K9/1694A61K9/2027A61P19/10A61K2300/00A61K9/20
Inventor 金真善李槿赫崔柄善金载臣朴辰夏吴美真金银美
Owner HANLIM PHARMA CO LTD
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