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Calcitriol tablet and preparation method thereof

A technology of calcitriol and polyethylene glycol, which is applied in the field of calcitriol tablets and its preparation, can solve the problems of low bioavailability, monotonous dosage form, sensitivity of calcitriol to light and air, etc., and achieve reduction Effect of Dosage and Bioavailability Improvement

Active Publication Date: 2014-04-30
CP PHARMA QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the main preparation forms of calcitriol are soft capsules and capsules; the dosage form is relatively monotonous, and calcitriol is sensitive to light and air, and has low solubility in common organic solvents. The stability of soft capsules and capsules Not good, extremely low content of active ingredients, low bioavailability
Calcitriol tablets are not reported in the prior art because they cannot exist stably for a long time and their bioavailability is not high

Method used

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  • Calcitriol tablet and preparation method thereof
  • Calcitriol tablet and preparation method thereof
  • Calcitriol tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 calcitriol tablet

[0042] The prescription for 1000 tablets is:

[0043] Calcitriol 1.5mg

[0044] Meglumine 6.0g

[0045] Macrogol 400 3.6g

[0046] Macrogol 6000 45g

[0047] Starch 210g

[0048] Sodium carboxymethyl starch 15g

[0049] Appropriate amount of pregelatinized starch

[0050] Magnesium Stearate Appropriate amount.

[0051] The preparation method is:

[0052] 1) Weigh the raw and auxiliary materials of the prescription amount, pass through 80-mesh sieve respectively;

[0053] 2) Take the sieved pregelatinized starch and add distilled water to make a binder solution;

[0054] 3) Mix the sieved calcitriol, meglumine, polyethylene glycol 400, polyethylene glycol 6000, starch and sodium carboxymethyl starch evenly in equal increments, and add the above binder solution to prepare into soft material;

[0055] 4) After granulating with a 40-mesh sieve, dry at 50°C for 30 minutes, pass through a 20-mesh sieve for granulation, add magnesium...

Embodiment 2

[0056] Example 2 Calcitriol Tablets

[0057] The prescription for 1000 tablets is:

[0058] Calcitriol 1.5mg

[0059] Meglumine 12g

[0060] Macrogol 400 5.4g

[0061] Macrogol 6000 75g

[0062] Lactose 150g

[0063] Low-substituted hydroxypropyl cellulose 30g

[0064] Proper amount of hydroxypropyl cellulose

[0065] Talc powder in moderation.

[0066] The preparation method is:

[0067] 1) Weigh the raw and auxiliary materials of the prescription amount, and pass through a 120-mesh sieve for later use;

[0068] 2) Take the sieved hydroxypropyl cellulose and add distilled water to make a binder solution;

[0069] 3) Mix the sieved calcitriol, meglumine, polyethylene glycol 400, polyethylene glycol 6000, lactose and low-substituted hydroxypropyl cellulose in equal increments, and add the above binder The solution is made into a soft material;

[0070] 4) After granulating with a 40-mesh sieve, dry at 70°C for 60 minutes, pass through a 20-mesh sieve for granulation,...

Embodiment 3

[0071] Example 3 Calcitriol Tablets

[0072] The prescription for 1000 tablets is:

[0073] Calcitriol 1.5mg

[0074] Meglumine 9.0g

[0075] Macrogol 400 4.5g

[0076] Macrogol 6000 60g

[0077] Dextrin 180g

[0078] Microcrystalline Cellulose 24.0g

[0079] Proper amount of povidone

[0080] Appropriate amount of micronized silica gel.

[0081] The preparation method is:

[0082] 1) Weigh the raw and auxiliary materials of the prescription amount, pass through a 100-mesh sieve for later use;

[0083] 2) Take the sieved povidone and add distilled water to make a binder solution;

[0084] 3) Mix the sieved calcitriol, meglumine, polyethylene glycol 400, polyethylene glycol 6000, dextrin and microcrystalline cellulose evenly in an equal increment method, and add the above binder solution to prepare into soft material;

[0085] 4) After granulating with a 40-mesh sieve, dry at 60°C for 45 minutes, pass through a 20-mesh sieve for granulation, add micropowder silica gel,...

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Abstract

The invention relates to a calcitriol tablet and a preparation method thereof. The tablet is prepared from the following ingredients in percentage by weight: 0.0005% of calcitriol, 2.0-4.0% of meglumine, 1.2-1.8% of polyethylene glycol 400, 15-25% of polyethylene glycol 6000, 50.0-70.0% of filler, 5.0-10.0% of disintegrant, an appropriate amount of binder and an appropriate amount of lubricant. According to the tablet, the content of calcitriol is remarkably increased, so that the drug dosage is reduced; and the stability of calcitriol to light and air is improved, and the bioavailability of calcitriol is also remarkably improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a calcitriol tablet and a preparation method thereof. Background technique [0002] Calcitriol is a white crystalline powder that is sensitive to light and air. Slightly soluble in methanol, ethanol, ethyl acetate. Tm is 111-115°C. It is one of the most important metabolic active products of vitamin D3 in the human body. It can promote the absorption of calcium in the small intestine and regulate the transport of inorganic salts in the bone. It is mainly used for osteoporosis and renal osteodystrophy in patients with chronic renal failure. , especially in patients requiring long-term hemodialysis; postoperative spontaneous and pseudohypoparathyroidism; vitamin D3-dependent rickets and hypophosphatemic vitamin D-resistant rickets; skin diseases such as psoriasis; and other vitamins D deficiency. Oral absorption of calcitriol is fast, peaking in 3 to 6 hours, t1 / 2 is about 3 t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/593A61K47/34A61K47/26A61P3/02A61P19/10A61P19/08A61P17/06
Inventor 王明刚陈阳生任莉
Owner CP PHARMA QINGDAO CO LTD