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Stable paricalcitol pharmaceutical composition and preparation method thereof

A technology for paricalcitol and a composition is applied in the field of paricalcitol pharmaceutical composition and preparation thereof, and can solve the problems of unstable hygroscopicity of paricalcitol, inability to prepare oral preparations and the like

Active Publication Date: 2014-11-26
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the extremely unstable nature of paricalcitol itself and its hygroscopicity, oral preparations cannot be prepared by conventional methods

Method used

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  • Stable paricalcitol pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Prescription Composition of Paricalcitol Tablets

[0036] Paricalcitol 0.002g

[0037] Hydroxypropyl-α-CD inclusion complex 0.168g

[0038]Trehalose 2.5g

[0039] Starch slurry 7.00g

[0040] Povidone 4.50g

[0041] Lactose 70.23g

[0042] Talc powder 0.60g

[0043] Made into tablets 85mg / tablet, made into 1000 pieces

[0044] Specific preparation method:

[0045] a. Weigh 0.168g hydroxypropyl-α-CD cyclodextrin and dissolve it in pure water, weigh 0.002g paricalcitol and add it to the cyclodextrin solution, stir until the solution is clear and transparent, forming a paricalcitol ring Dextrin inclusion compound;

[0046] b. Weigh 2.5g of trehalose and dissolve in the above clathrate, freeze-dry, pre-freeze at -40°C, vacuumize at 85 Pa, -20°C, dry at 100 Pa, 20°C to obtain freeze-dried mixture Ⅰ ;

[0047] c. Crush the freeze-dried mixture I, pass through a 100-mesh sieve, add 7.00g of starch slurry, 4.50g of povidone, and 70.23g of lactose according to the pres...

Embodiment 2

[0059] Prescription Composition of Paricalcitol Tablets

[0060] Paricalcitol 0.002g

[0061] Hydroxypropyl-γ-CD inclusion complex 0.004g

[0062] Dextran 1.40g

[0063] Pectin 4.50g

[0064] Sodium carboxymethyl starch 8.00g

[0065] Maltose 70.10g

[0066] Magnesium Stearate 1.00g

[0067] Made into tablets 85mg / tablet, made into 1000 pieces

[0068] Specific preparation method:

[0069] a. Weigh 0.004g hydroxypropyl-γ-CD cyclodextrin and dissolve it in pure water, weigh 0.002g paricalcitol and add it to the cyclodextrin solution, stir until the solution is clear and transparent, forming a paricalcitol ring Dextrin inclusion compound;

[0070] b. Weigh 1.40g of dextran and dissolve it in the above clathrate solution, freeze-dry, pre-freeze at -30°C, vacuum at 75 Pa, -20°C, and dry at 90 Pa, 20°C to obtain freeze-dried mixture Ⅰ ;

[0071] c. Crush the freeze-dried mixture I, pass through a 100-mesh sieve, add 4.50 g of pectin, 8.00 g of sodium carboxymethyl starch,...

Embodiment 3

[0080] Prescription Composition of Paricalcitol Tablets

[0081] Paricalcitol 0.002g

[0082] Hydroxypropyl-α-CD inclusion complex 0.248g

[0083] Mannitol 1.00g

[0084] Hypromellose 10.00g

[0085] Low-substituted hydroxypropyl cellulose 10.00g

[0086] Sorbitol 63.25g

[0087] Micronized silica gel 0.50g

[0088] Made into tablets 85mg / tablet, made into 1000 pieces

[0089] Specific preparation method:

[0090] a. Weigh 0.248g hydroxypropyl-α-CD cyclodextrin and dissolve it in pure water, weigh 0.002g paricalcitol and add it to the cyclodextrin solution, stir until the solution is clear and transparent, forming a paricalcitol ring Dextrin inclusion compound;

[0091] b. Weigh 1.00 g of mannitol and dissolve it in the clathrate solution, freeze-dry, pre-freeze at -30°C, vacuum at 75 Pa at -20°C, and dry at 90 Pa at 20°C to obtain a freeze-dried mixture I;

[0092] c. Crush the freeze-dried mixture I, pass through a 100-mesh sieve, add 10.00g of hydroxypropylmethylc...

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Abstract

The invention discloses a high-stability paricalcitol pharmaceutical composition and a preparation method thereof. The medicinal composition comprises a cyclodextrin inclusion compound containing an active component paricalcitol and other pharmaceutically acceptable carriers, and is prepared by adopting a freeze-drying dry granulation process and strictly controlling temperature and humidity in the preparation process. The paricalcitol is included by cyclodextrin, and the freeze-drying and dry granulating preparation process is adopted, so that the defects that the main drug paricalcitol is extremely easily hygroscopic and extremely poor in stability and cannot be prepared into oral preparations can be greatly overcome, and the disintegration or main drug component dissolution cannot be influenced; and the paricalcitol pharmaceutical composition is not a coated tablet, so that the defect of slow dissolution of a conventional coated tablet can be avoided.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral paricalcitol pharmaceutical composition and a preparation method thereof. Background technique [0002] Paricalcitol (Limaprost) chemical name is: [0003] (1R,3R)-5-{2-[(1R,3aS,4E,7aR)-1-[(2R,3E,5S)-6-hydroxy-5,6-dimethylhept-3-en-2-yl ]-7a-methyl-octahydro-1H-inden-4-ylidene]ethylidene}cyclohexane-1,3-diol, the structural formula is as follows: [0004] formula one [0005] It mainly treats secondary hyperparathyroidism. Secondary hyperparathyroidism is characterized by elevated parathyroid hormone (PTH) with insufficient active vitamin D levels. The sources of vitamin D in the body are skin synthesis and dietary intake. Vitamin D needs to undergo two hydroxylation reactions in the liver and kidney to bind and then activate the vitamin D receptor (VDR). The endogenous VDR activator calcitriol [ 1, 25 (OH ) 2 D 3 ] is a hormone tha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/20A61K31/592A61P5/20A61K47/69
Inventor 孙沣陆潇筠卢迪肖萱张伟强周丽莹
Owner BEIJING TIDE PHARMA
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