Degradable implated medicine release-controlling carrier with micropores and cavities and its preparing process

Abstract

The present invention discloses a kind of degradable implanted medicine release-controlling carrier system with micropores and cavities, and realizes long term linear release of medicine by means of the combined permeating diffusion and degrading diffusion. The carrier structure is prepared with degradable material lactic acid-glycolic acid polymer, which may be absorbed by human body under the action of body fluid and biological enzyme and has no need of being taking out, reducing patient's pain. The medicine releasing system is suitable for water soluble medicine mainly and has its microporesize, number and distribution designed reasonably based on the molecular weight of the medicine and the required release rate and period and the material parameters regulated. The degradable implanted medicine release-controlling carrier system has great medicine carrying amount, good regulating property and long term constant medicine release.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a multi-cavity degradable implantable controlled-release drug carrier with micropores and a preparation process thereof. Background technique [0002] The types of conventional medicaments are divided into traditional oral preparations, injection injections, external application ointments, etc. In addition, there are implantable long-term controlled release preparations. Regardless of the form, it is generally a matrix-type pharmaceutical preparation system in which the drug and adjuvant are mixed, that is, the drug is uniformly dissolved or dispersed in the drug adjuvant or carrier material, which not only has a low active ingredient , and it is usually expressed as a "first-order" drug release characteristic, that is, there is a sudden release of the drug during the drug release period, resulting in a large change in the blood drug concentration of the ...

AI Technical Summary

Problems solved by technology

For injectable drugs, it belongs to direct injection release, which has high bioavailability and quick effect, but often causes pain and inconvenience to patients

For biological drugs such as proteins, the above-mentioned traditional drug delivery methods often cannot meet the medical requirements well, so a preparation form capable of long-term constant release is needed

[0004] Controlled sustained-release preparations can achieve long-term stable drug administration, greatly reduce the number of times patients take drugs, and improve patient compliance and therapeutic effects. It has become a research hotspot in the field of medicine in recent years. There are several types of skin release and implantable. The oral type mainly includes various sustained-release capsules. There are a large number of sustained-release microspheres prepared by mixing degradable materials and drugs in the capsules. The drugs are encapsulated in the capsule according to the release time. Different degradable films mainly release drugs through the diffusion mechanism to reduce the drug burst release effect and prolong the drug release time. However, because the drug is still administered through the digestive tract, it is impossible to achieve a longer drug release cycle in the body, generally the longest The medicine is taken once every 24 hours, so that patients can reduce the number of daily doses. Transdermal preparations are mainly administered through external application, and the focus of research is how to effectively release macromolecular drugs into the subcutaneous. The implantable type mainly includes various osmotic pumps. The depot-based preparations mainly control the drug release rate through osmotic and semi-osmotic mechanisms to ensure long-term stable blood drug concentration. The latest research results also include implantable drug delivery devices with automatic control functions prepared by MEMS technology. Drug system, through the micro-control system to periodically open the sealing cover of the drug storage in the body, to release the drug regularly and quantitatively. However, the biggest defect of this drug delivery system is that after the drug is released, the system needs to be taken out again, which brings new benefits to the patient. Sustained-release preparations made of biodegradable materials are the mainstream of implantable drug delivery systems. At present, the most commonly used is to uniformly mix degradable materials and drugs to make tablets, and implant them into the body near the lesion. Gradually degrade the carrier material to carry out sustained and controlled drug release. However, this type of preparation still generally has the phenomenon of initial drug release hysteresis and burst release. In addition, due to drug saturation, the active ingredients in the preparation generally do not exceed 20%, and the maximum The biggest problem is that when the physical and chemical properties of the drug and the carrier material do not match, the preparation cannot be realized. Therefore, a new dosage form is to use degradable materials to prepare a cavity-type sustained-release carrier system, and the drug is encapsulated in multiple microcavities. In the body, as the carrier material degrades, the microcavity breaks and releases the drug one by one, which plays a sustained release role. This carrier system can not only greatly increase the effective content of the drug, but also is suitable for any drug. Multi-cavity sealing drugs can be better However, since the drug release cycle is restricted by the degradation cycle of the carrier material, the corresponding initial drug release hysteresis is also closely related to this, that is, the longer the sustained release cycle, the longer the initial drug release lag time. This is a pair of complementary contradictions. How to achieve long-term stable drug release and eliminate the hysteresis of initial drug release as much as possible is one of the key issues in developing this type of implantable sustained-release system and improving its clinical performance.

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