A kind of stable paricalcitol pharmaceutical composition and preparation method thereof

A paricalcitol and stable technology, applied in the field of pharmaceutical preparations, can solve the problems of unstable hygroscopicity of paricalcitol, inability to prepare oral preparations and the like

Active Publication Date: 2019-07-02
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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  • A kind of stable paricalcitol pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The prescription composition of Paricalcitol tablets

[0036] Paricalcitol 0.002g

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

[0038] Trehalose 2.5g

[0039] Starch slurry 7.00g

[0040] Povidone 4.50g

[0041] Lactose 70.23g

[0042] Talc 0.60g

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

[0044] Specific preparation method:

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

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

[0047] c. Crush the freeze-dried mixture I, pass a 100-mesh sieve, add 7.00g starch slurry, 4.50g povidone, 70.23g lactose according to the prescription ratio, mix for mor...

Embodiment 2

[0059] The prescription composition of Paricalcitol tablets

[0060] Paricalcitol 0.002g

[0061] Hydroxypropyl-γ-CD inclusion compound 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 tablets

[0068] Specific preparation method:

[0069] a. Weigh 0.004g of hydroxypropyl-γ-CD cyclodextrin and dissolve it in pure water, weigh 0.002g of Paricalcitol and add it to the cyclodextrin dissolution, 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-mentioned clathrate solution, freeze-dry it, pre-freeze at -30°C, vacuum at 75Pa, -20°C, and dry at 90 Pa, 20°C to obtain freeze-dried mixture I;

[0071] c. Crush the freeze-dried mixture I, pass a 100 mesh sieve, add 4.50g pectin, 8.00g sodium carboxymethyl starch, 70.10g maltose ...

Embodiment 3

[0080] The prescription composition of Paricalcitol tablets

[0081] Paricalcitol 0.002g

[0082] Hydroxypropyl-α-CD inclusion compound 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 tablets

[0089] Specific preparation method:

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

[0091] b. Weigh 1.00g of mannitol and dissolve it in the above inclusion compound solution, freeze-dry, pre-freeze at -30℃, 75Pa, vacuum at -20℃, and dry at 90 Pa, 20℃ to prepare freeze-dried mixture I ;

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

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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 specifically relates to a paricalcitol pharmaceutical composition that can be used for oral administration and a preparation method thereof. Background technique [0002] The chemical name of Paricalcitol (Limaprost) 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] Its main treatment is secondary hyperparathyroidism. Secondary hyperparathyroidism is characterized by elevated parathyroid hormone (PTH), accompanied by insufficient levels of active vitamin D. The source of vitamin D in the body is skin synthesis and dietary intake. Vitamin D needs to undergo two hydroxylation reactions in the liver and kidneys to combine to activate the vitamin D receptor (VDR). The endogenous VDR activator calci...

Claims

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Application Information

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