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Calcitriol enteric capsule and preparation method thereof

An enteric-coated capsule, calcitriol technology, applied in the directions of capsule delivery, bone diseases, pharmaceutical formulations, etc., can solve the problems of monotonous dosage forms, low solubility of common organic solvents, and inability to exist stably for a long time, and achieves improved bioavailability. Effect

Active Publication Date: 2013-06-12
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 enteric-coated capsules 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 enteric capsule and preparation method thereof
  • Calcitriol enteric capsule and preparation method thereof
  • Calcitriol enteric capsule and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1 calcitriol enteric-coated capsule

[0030] The prescription is:

[0031] The core is made of the following components by weight percentage:

[0032]

[0033] The enteric coating layer contains 10% by weight of cellulose acetate phthalate.

[0034] The preparation method is:

[0035] 1) Weigh the raw and auxiliary materials of the prescription amount, pass through 80-mesh sieve respectively;

[0036] 2) Take the sieved starch and cellulose acetate phthalate and add distilled water respectively to make a binder solution and a coating solution;

[0037] 3) Mix the sieved calcitriol, meglumine, polyethylene glycol 400, polyethylene glycol 6000, starch and carboxymethyl starch sodium evenly in equal increments, and add the above binder solution to prepare into soft material;

[0038] 4) After granulating with a 40-mesh sieve, dry at 50°C for 30 minutes, pass through a 20-mesh sieve for granulation; then pass through a No. 4 sieve to remove fine powder, a...

Embodiment 2

[0040] Embodiment 2 calcitriol enteric-coated capsules

[0041] The prescription is:

[0042] The core is made of the following components by weight percentage:

[0043]

[0044] The enteric coating layer contains 20% by weight of cellulose acetate trimellitate.

[0045] The preparation method is:

[0046] 1) Weigh the raw and auxiliary materials of the prescription amount, and pass through a 120-mesh sieve for later use;

[0047] 2) Take the sieved pregelatinized starch and cellulose acetate trimellitate and add distilled water respectively to make a binder solution and a coating solution;

[0048] 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;

[0049] 4) After granulating with a 40-mesh sieve, dry at 70°C for 60 minutes, pass through a 20-mesh sieve for granulation; then pass through...

Embodiment 3

[0051] Embodiment 3 calcitriol enteric-coated capsules

[0052] The prescription is:

[0053] The core is made of the following components by weight percentage:

[0054]

[0055] The enteric coating layer contains 15% by weight of hydroxypropyl cellulose phthalate.

[0056] The preparation method is:

[0057] 1) Weigh the raw and auxiliary materials of the prescription amount, pass through a 100-mesh sieve for later use;

[0058] 2) Take the sieved povidone and hydroxypropyl cellulose phthalate and add distilled water respectively to make binder solution and coating solution;

[0059] 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;

[0060] 4) After granulating with a 40-mesh sieve, dry at 60°C for 45 minutes, pass through a 20-mesh sieve for granulation; then pass through a No. 4 sieve ...

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Abstract

The invention relates to a calcitriol enteric capsule and a preparation method thereof. The enteric capsule consists of a core and an enteric coating layer, wherein the enteric coating layer contains an enteric material accounting for 10-20% by weight, and the core 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 and an appropriate amount of binder. According to the enteric capsule, 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 enteric-coated capsule 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, t...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/593A61K47/34A61K47/18A61P3/02A61P3/14A61P19/10A61P19/08A61P17/06
Inventor 王明刚陈阳生任莉
Owner CP PHARMA QINGDAO CO LTD