Microcapsule lyophilized powder and preparation method thereof

A technology of freeze-dried powder and microcapsules, applied in the field of preparation of microcapsules, can solve the problems of poor encapsulation capacity, serious burst release effect, poor thermal stability and the like

Inactive Publication Date: 2012-07-11
ZHEJIANG HISUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The reported preparation methods for encapsulating water-soluble drugs are mainly drying in liquid or reverse phase evaporation of double emulsion. Due to the complicated preparation process and the need for severe conditions such as heating, it is not suit

Method used

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  • Microcapsule lyophilized powder and preparation method thereof
  • Microcapsule lyophilized powder and preparation method thereof
  • Microcapsule lyophilized powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] Embodiment 1: Bevacizumab capsule-core microcapsules

[0099] Antibody drugs have the advantages of small amount and strong effect, but they are easily degraded in the body and last for a short time. In this example, bevacizumab was used as an object to prepare bevacizumab cored microcapsules, and the composition of bevacizumab cored microcapsules is shown in Table 2.

[0100] Table 2 Bevacizumab capsule-core microcapsule composition ratio

[0101] prescription Bevacizumab polymer hydrocolloid material Emulsifier polymer degradable material Freeze-dried support agent tert-butanol Prescription 1 0.05mg Gelatin 1mg Polyoxyethylene hydrogenated castor oil 10mg PLGA with a molecular weight of 20,000 (50:50) 1mg Poloxamer 188 100mg 2g Prescription 2 0.05mg Human albumin 1mg Polyoxyethylene hydrogenated castor oil 10mg PLGA with a molecular weight of 10,000 (50:50) 2mg Poloxamer 188 100mg 2g Prescription 3 0.05mg ...

Embodiment 2

[0106] Embodiment 2: the preparation of doxorubicin capsule core microcapsule

[0107] There are many anti-tumor chemical drugs, including doxorubicin, vincristine, topotecan, etc. Although they have definite anti-tumor effects, they lack targeting in vivo, so they have strong toxic and side effects, and a targeted delivery carrier is needed. In this example, doxorubicin was used as an object to prepare doxorubicin capsule-core microcapsules, and the composition of doxorubicin capsule-core microcapsules is shown in Table 3.

[0108] Table 3 Doxorubicin gel-core microcapsule composition distribution ratio

[0109] prescription Adriamycin polymer hydrocolloid material Emulsifier polymer degradable material Freeze-dried support agent pH regulator co-emulsifier Prescription 1 5mg Gelatin 1mg Polyoxyethylene hydrogenated castor oil 20mg 5 mg of PLGA (50:50) with a molecular weight of 10,000 Poloxamer 188 200mg Hydrochloric acid 0.01 Oleic ...

Embodiment 3

[0113] Example 3: Quality Evaluation of Adriamycin Microcapsules

[0114] In this example, the doxorubicin microcapsule freeze-dried powder prepared in Example 2 and the control group were used for quality comparison.

[0115] Microscopic morphology and particle size analysis: with embodiment 1.

[0116] Determination of encapsulation efficiency: Take 100 mg of the above lyophilized powder and add 1 g of water to form a microcapsule or nanoparticle solution, load the sample on a Sephadex G-50 gel column, use distilled water as the eluent, take different volumes of the eluted fraction, and separate Receive the eluted part of the microcapsules or nanoparticles loaded with doxorubicin, add chloroform to destroy the doxorubicin microcapsules or nanoparticles, extract doxorubicin to make doxorubicin solution, and use HPLC method to detect the content of doxorubicin hydrochloride (chromatographic Conditions: Venusil MP C18 column (416mm×250mm, 5μm), the mobile phase is acetonitrile...

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Abstract

The invention relates to microcapsules and a preparation method thereof. Each microcapsule has a structure of taking a polymeric hydrophilic colloid as a capsule core and a biodegradable polymer material as a capsule membrane; a water-soluble medicine is dispersed into the hydrophilic colloid capsule core; the microcapsules are prepared by the combination of multiple technologies such as a microemulsion technology, an ultra-low temperature quick-freezing technology and the like and a freeze-drying process; the particle sizes of the microcapsules can be controlled; the microcapsules are high in medicine loading capacity and medicine entrapment efficiency; and the microcapsules are uniform in particle size, microcapsule particles cannot be gathered, and the medicine release behavior is controllable. The microcapsules are applicable to the entrapment of water-soluble medicines, are particularly applicable to medicines with low thermal stability and macromolecular medicines such as protein, polypeptides, polysaccharides and the like, and can be applied to the injection and oral administration of multiple formulations for local or systemic treatment of mucous membranes, skins, wounds and orifices.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and more specifically, the invention relates to a preparation method of microcapsules. Background technique [0002] Microencapsulation technology (microencapsulation) is referred to as microencapsulation, which uses natural or synthetic polymer materials (called capsule materials) as the capsule wall shell to wrap solid or liquid drugs (called capsule core) Library-type microcapsules (microcapsule), referred to as microcapsules. If the drug is dissolved and / or dispersed in the polymer material matrix to form a skeleton-type tiny spherical entity, it is called a microsphere. The capsule materials commonly used in microcapsules can be divided into natural, semi-synthetic or synthetic polymer materials. [0003] In addition to the main drug, the core of the microcapsule can include additives to improve the quality of microencapsulation, such as stabilizers, diluents, blockers to control...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/34
Inventor 不公告发明人
Owner ZHEJIANG HISUN PHARMA CO LTD
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