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Pitavastatin calcium enteric sustained-release micropill preparation and preparation method thereof

A technology of pitavastatin calcium and sustained-release pellets, which is applied in the direction of bulk delivery, metabolic diseases, and active ingredients of heterocyclic compounds, and can solve problems such as poor stability, prone to configuration transformation, and inconsistent synthesis time periods. Achieve the effect of stable configuration, less adverse reactions, and stable blood drug concentration

Inactive Publication Date: 2011-05-11
QINGDAO HANHE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, pitavastatin calcium is prone to configuration transformation in a low pH environment and has poor stability. Common tablets are mainly used clinically. Usually, after taking 0.5 to 3 hours, the blood drug concentration reaches a peak and then disappears quickly. However, due to cholesterol The synthesis in the body is carried out from midnight to morning, so the blood concentration of the active ingredient does not coincide with the time period of cholesterol biosynthesis

Method used

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  • Pitavastatin calcium enteric sustained-release micropill preparation and preparation method thereof
  • Pitavastatin calcium enteric sustained-release micropill preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] A pitavastatin calcium enteric-coated sustained-release pellet preparation, the formula of which is as follows:

[0042] Contains Pill Hearts:

[0043] Pitavastatin Calcium 1g

[0044] Starch 30g

[0045] Sodium bicarbonate 20g

[0046] 5% PVP ethanol solution 50g

[0047] (5% PVP ethanol solution is the solution that PVP is dissolved in ethanol and forms, and its weight percentage is 5%);

[0048] Isolation layer:

[0049] Low-substituted hydroxypropyl cellulose 1g

[0050] 2% HPMC ethanol solution 50g

[0051] (2% HPMC ethanol solution is that HPMC is dissolved in ethanol, and its weight percentage is 2%);

[0052] Slow release layer:

[0053] Ethylcellulose 8g

[0054] PVP 2g

[0055] Triethyl citrate 5g

[0056] 95% ethanol (as solvent) 80g

[0057] Enteric layer:

[0058] Eudragit L 24g

[0059] Dibutyl sebacate 2g

[0060] Micronized silica gel 0.5g

[0061] 95% ethanol (as solvent) 100g

[0062] Preparation:

[0063] Take pitavastatin calcium raw ...

Embodiment 2

[0069] Pitavastatin Calcium 2g

[0070] Calcium hydrogen phosphate 15g

[0071] Sucrose 32g

[0072] 60% syrup (weight percentage) 10g

[0073] Sieve granulated sucrose, collect 40-60 mesh sugar cores as seed cores, weigh them and place them in a multi-functional coating granulation pot, use syrup as a binder, sprinkle pitavastatin calcium raw materials and calcium hydrogen phosphate Fine powder, made into pills, dried. Configure each layer of coating solution (coating solution is the isolation layer, slow-release layer and enteric layer), according to the prescription of embodiment 1, the coating solution is wrapped layer by layer on the micro-nine, control spray speed and spray volume, so that Keep the surface of the pellets moist but not sticky, blow hot air to dry, and repeat the operation to obtain controlled-release pellets with a particle size of about 1mm.

Embodiment 3

[0075] Starch blank pellets 100g

[0076] Pitavastatin Calcium 1g

[0077] Calcium citrate 5g

[0078] 2% PVP ethanol solution 120g

[0079] (2% PVP ethanol solution) is that PVP is dissolved in ethanol solution, and its weight percentage is 2%);

[0080] Isolation layer:

[0081] Hypromellose 2.5g

[0082] 95% ethanol solution (as solvent) 50g

[0083] Slow release layer:

[0084] Acrylic resin NE30D 18g

[0085] PEG1500 6g

[0086] Talc powder 3g

[0087] water 100g

[0088] Enteric layer:

[0089] Polyacrylic resin Eudragit L 45g

[0090] Dimethyl phthalate 2g

[0091] Talc powder 2g

[0092] 95% ethanol (as solvent) 120g

[0093] Preparation process: place 18-24 mesh blank pellets in a fluidized bed, dissolve pitavastatin calcium and calcium citrate in PVP ethanol solution and spray them into the fluidized bed. Then dissolve the hypromellose in 95% ethanol and spray it into the fluidized bed to cover the isolation layer. Mix acrylic resin NE30D and water, a...

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Abstract

The invention provides a pitavastatin calcium enteric sustained-release micropill preparation and a preparation method thereof, which can solve the problems that: (1) pitavastatin calcium is easily subjected to inversion of configuration under the condition that gastric juice has a low pH value, and has low stability, and (2) common tablets are released too quickly, so that active ingredients cannot fully achieve the effect of reducing cholesterol in the prior art. The technical scheme is that: the pitavastatin calcium enteric sustained-release micropill preparation comprises a medicine-containing pill core, an isolation layer, a sustained-release layer and an enteric layer from inside to outside, wherein the medicine-containing pill core comprises pitavastatin calcium and pharmaceutical excipients. The invention also provides a preparation method for the micropill preparation. The prepared micropill is not released in the gastric juice, and medicines are prevented from being exposed in the acid environment; by adopting microporous film coating technology, the medicines can be slowly released from the pill core, the blood concentration is kept balanced, the medicine taking frequency is reduced and the compliance of the patient is improved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pitavastatin calcium enteric-coated sustained-release pellet preparation and a preparation method thereof. Background technique [0002] Pitavastatin Calcium (Pitavastatin Calcium), the chemical name is bis {(3R, 5S, 6E)-7-[2-cyclopropyl-4-(fluorophenyl)quinoline-3-phenyl]-3, 5-dihydroxy-6-heptenoic acid ethyl ester} calcium salt, the first fully synthetic HMG-CoA reductase inhibitor developed by Nissan Chemical Co., Ltd. and Kowa Co., Ltd., was registered in Japan in November 1999 , and was first approved for marketing in Japan on July 17, 2003, and the listed dosage form is tablet. Pitavastatin Calcium is a third-generation statin drug. Compared with other statin drugs, it has the characteristics of effectively reducing LDL-C and TG levels, excellent pharmacokinetic indicators, long half-life, low drug interaction potential, and good safety. , known as a super sta...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/47A61P3/06
Inventor 牛佰慧曹瑞山李振霞王芳徐晓琳
Owner QINGDAO HANHE PHARMA
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