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Drug core composition for controlled release administration and osmotic pump formulation comprising the drug core composition

A technology of composition and osmotic pressure enhancer, which is applied in the directions of drug delivery, medical preparations of inactive ingredients, sugar-coated pills, etc., can solve the problems of low solubility of low water-soluble drugs and the like

Active Publication Date: 2020-01-10
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The object of the present invention is to provide a drug core composition that has a significant solubilization effect on low water-soluble drugs and can control release, and solves the problem of low water-soluble drugs by using the amphiphilic polymer carrier Soluplus in the drug core composition. The problem of low solubility in water

Method used

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  • Drug core composition for controlled release administration and osmotic pump formulation comprising the drug core composition
  • Drug core composition for controlled release administration and osmotic pump formulation comprising the drug core composition
  • Drug core composition for controlled release administration and osmotic pump formulation comprising the drug core composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1（ test example 1）

[0047] Example 1 (Test Example 1): Determination of Phase Equilibrium Solubility

[0048] The solubility of cyclosporin A (CsA) in different concentrations of Soluplus aqueous solution was determined by shaking table method. Prepare a series of Soluplus solutions with different concentrations, take 10mL of the solution, put it in a 15mL glass test tube, and then add the excess drug. The samples were equilibrated for a sufficient period of time (48 h) in a preheated shaker with temperature settings of 15, 25 and 37 °C and a rotation speed of 100 rpm. The balanced sample solution was filtered with a mixed cellulose membrane to discard the initial filtrate, and the subsequent filtrate was diluted with pure methanol to an appropriate multiple, and 20 μL was taken and injected into a high-performance liquid chromatograph, and the peak area was recorded to calculate the drug concentration.

[0049] The phase equilibrium solubility of cyclosporine A in aqueous solutions of the amphi...

Embodiment 2（ test example 2）

[0050] Example 2 (Test Example 2): Effect of Sodium Dodecyl Sulfate (SDS) on the Soluplus Solubilizing Drug Ability

[0051] Fix the concentration of Soluplus (0.04%) unchanged, add different amounts of SDS, and investigate the effects of Soluplus / SDS (w / w) ratios of 50 / 1, 20 / 1, 10 / 1, 5 / 1 and 4 / 1 on the drug The effect of solubilization ability. Among them, SDS aqueous solution alone did not increase the equilibrium solubility of the drug at the maximum concentration used in this study (0.01%). Fill 100mL of different media into the glass cups respectively, at 37°C, with a mechanical paddle speed of 100rpm, and add DMSO solution equivalent to 1mL of CsA (the concentration of CsA is 100mg / mL) into each cup. Take 2 mL of the sample solution at 0.25, 1, 2, 4 and 24 hours respectively, quickly filter it with a disposable organic phase needle filter, discard 1 mL of the initial filtrate, take the subsequent filtrate and add pure acetonitrile to dilute an appropriate multiple, and ...

Embodiment 3

[0053] Example 3 (comparative example): prescription and preparation process of ordinary push-pull cyclosporin A-loaded osmotic pump tablets (PVP-PMs-T)

[0054] (1) chip

[0055]

[0056] The drug-containing layer is directly mixed with powder, and the CsA, PVP30, micropowder silica gel and PolyoxWSR N80 are mixed evenly according to the prescription amount by an equal-volume incremental method to obtain the drug-containing layer.

[0057]

[0058] The booster layer is granulated. Process: After mixing PEO, HPMC, NaCL, PVP K30 and iron red through a 60-mesh sieve evenly according to the prescription amount, add 95% ethanol liquid to make a soft material with a 24-mesh sieve. Granules, dried at 45°C for 2 hours, sieved with a 22-mesh sieve, then added magnesium stearate, mixed evenly, and set aside.

[0059] A 10.5# die is used for tableting, and the drug-containing layer and the booster layer are pressed into a double-layer tablet core, and the tableting pressure is be...

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Abstract

The invention provides a controlled release dosing medicine core composition and an osmotic pump preparation comprising the medicine core composition. The medicine core composition comprises, by weight, 100 parts of an amphiphilic polymer carrier Soluplus, 5-200 parts of medicines, 0-50 parts of a surface active agent, 0-200 parts of a framework material having the controlled release effect, 100-200 parts of an osmotic pressure accelerant having the controlled release effect and 0-20 parts of other auxiliary materials acceptable in pharmacy; the low-solubility medicines are medicines with the in-water solubility smaller than or equal to 1 mg / mL and comprise indissolvable or insoluble medicines with the solubility smaller than or equal to 0.1 mg / mL in water and medicines with the solubility larger than 0.1 mg / mL and very slightly soluble medicines smaller than or equal to 1 mg / mL; the surface active agent is an anion surface active agent; and the other auxiliary materials acceptable in pharmacy comprises one or more kinds of a bonding agent, a coloring agent and a lubricating agent.

Description

technical field [0001] The invention relates to the technical field of preparations, including providing a drug core composition suitable for controlled-release administration of low-water-soluble drugs and a controlled-release drug preparation containing the drug core. Background technique [0002] According to statistics, 80% of new drugs in the world are insoluble in water. These drugs have low oral bioavailability due to their extremely low water solubility. Choosing the appropriate solubilization technology can significantly improve the dissolution and oral absorption of drugs. Although the immediate-release preparations using solubilization technology can significantly improve bioavailability, they often bring about higher blood concentration fluctuations than ordinary preparations. The effect is unfavorable. Especially for some drugs with a narrow therapeutic window, severe blood drug concentration fluctuations are prone to acute toxicity, and the problem of drug saf...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/32A61K47/20A61K9/22A61K9/28A61K9/24A61K9/44A61K47/34
Inventor 甘勇俞洪珍朱春柳夏登宁俞淼荣
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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