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Controlled release preparation

A controlled-release preparation and cyclodextrin technology, which is applied in the direction of pill delivery, medical preparations containing active ingredients, coatings, etc., can solve the health hazards, unsafe, long-term problems of operators, etc.

Inactive Publication Date: 2010-12-22
钟术光
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The extensive use of organic solvents will have obvious limitations in the process: ① Unsafe, flammable and explosive; ② Toxic, harmful to the environment and the health of operators; ③ Dissolved coal is expensive and difficult to recycle
But there are also many defects: the water-soluble porogen exists in the coating film in the form of a single molecule, the pore size of the micropores is limited by the molecular size of the water-soluble porogen, and the molecular size of most water-soluble porogens is related to the vast majority. The molecular size of most drugs is almost the same, or even smaller, so it is not conducive to the penetration of most drugs, and the types and quantities of drugs that can be applied are limited
But the defect of this technology is also many: as, 1), the formation of micropore or the dissolving of porogen are subject to the acidic or alkaline strength of digestive juice or the height of pH value and the amount of digestive juice, yet, The pH value of the patient's digestive juice and the amount of digestive juice often change, which is affected by many factors, such as the patient's constitution, physical condition, diet, and the influence of factors such as the patient's circadian rhythm at different times of the day , the pH value of the digestive juice is also different; even, the strength of the peristaltic function of the digestive tract is also greatly affected by the formation of micropores or the dissolution of porogens, and the strength of the peristaltic function of the digestive tract is also affected by many factors such as patients The influence of physical fitness, physical condition, diet and circadian rhythm, etc.
2), the formation of micropores or the dissolution of porogens takes a relatively long time, and the release of drugs shows a relatively long time lag
3) The drug release (production) reproducibility or / and storage stability of the preparation is poor
However, the above two technologies did not further explain or study the water-soluble cyclodextrin used as porogen or porogen.

Method used

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preparation example Construction

[0135] The invention relates to a method for preparing a controlled-release preparation coated with a controlled-release film, especially a zero-order release controlled-release preparation. Each basic step in the preparation method of the controlled-release preparation is described in detail below.

[0136] 1), preparing a core material containing at least one drug

[0137] The method of preparing the core material containing at least one drug is not particularly limited. Usually the preparation method is that the pharmaceutically active substance, and / or non-pharmaceutical auxiliaries and other ingredients are passed through the direct extrusion method, the extrusion method of dry, wet or sintered granules, extrusion and subsequent rounding, wet or dry granulation or Pelletizing directly (for example on discs) or bonding of powder (powder layer) to active substance-free spheres (granules) or active substance-containing granules, or further tableting in a certain way, eg by ...

Embodiment 1

[0160] 1. Preparation of samples

[0161] 1), preparation of tablet core:

[0162]

[0163]

[0164] Diltiazem, fatty acid, citric acid, sodium chloride, lactose and povidone were mixed, and granulated with absolute ethanol solution; the wet granulated material was forced through an 18-mesh sieve and dried for 24 hours; after granulation, After mixing with stearic acid and magnesium stearate, it is molded into a tablet core of 420 mg, and the tablet is compressed with a 7 / 16 "deep concave die.

[0165] 2), the tablet core is coated according to the following prescription and process:

[0166] Coating Solution Prescription:

[0167]

[0168] The solids content of the aqueous dispersion was 16% by weight. The tablet cores were coated on a Hicoater / Fruend coater. Coating condition parameters: spray rate, 1ml / min; inlet temperature, 70-80°C; outlet temperature, 40-42°C; tablet core temperature, 40°C; coating layer thickness, 250-350μm.

[0169] 4), healing controlled...

Embodiment 2

[0174] The sulfobutyl (ether)-β-cyclodextrin (DS=1.30~1.45) in the coating solution prescription of Example 1 is replaced by hydroxybutenyl ether cyclodextrin (DS=2.43~2.56) to prepare Example 2 , and then changed to hydroxybutenyl ether cyclodextrin (DS=0.23~0.36) and urea to prepare comparative samples 3 and 4, and the others were all in embodiment 1.

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Abstract

The invention discloses a controlled release preparation coated by a controlled release coating, with improved comprehensive performance for zero-order release in particular. The polymer controlled release coating, covered on a core material containing medicaments, of the controlled release preparation contains a water-soluble cyclodextrin derivative dispersed in a single molecule state and / or in a micelle state, wherein the average hydroxy substituted number (or DS) of the water-soluble cyclodextrin derivative on each glucose unit is not less than 5. The invention discloses a preparation method for the controlled release preparation. The medicament release of the preparation is affected little in vivo or in vitro and is relatively quick, the time lag is relatively low, the bioavailability of the medicament is high, and the medicament release storage stability and the production repeatability are improved; and the mechanical strength of the controlled release coating of the preparation is also improved and the like.

Description

technical field [0001] The present invention relates to a controlled release preparation. More specifically, the present invention relates to a controlled-release preparation coated with an outer controlled-release coating film with improved comprehensive properties, especially a zero-order release controlled-release preparation. The controlled-release preparation is coated on a drug-containing core The polymer controlled-release coating contains water-soluble cyclodextrin derivatives whose average number of substituted hydroxyl groups (or DS) per glucose unit is not less than 5, which are dispersed in a unimolecular state and / or in a micelle state. The invention also relates to a preparation method of the controlled-release preparation. Background technique [0002] Some water-insoluble polymers control drug release by coating in controlled-release formulations, especially zero-order release controlled-release formulations. Due to the water insolubility of the polymer, it...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/36A61K9/16A61K47/40A61K45/00
CPCA61K9/2853A61K9/286
Inventor 钟术光
Owner 钟术光
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