CN102579534A - Bear bile cardio-reliever pill sustained release preparations - Google Patents

Abstract

The invention relates to bear bile cardio-reliever pill sustained release preparations, belongs to the development of new varieties of traditional Chinese medicine in the biological and new medical technology, and is the secondary development of famous traditional Chinese medicine and ethnic medicine. Nowadays, situation of cardiac-cerebral vascular disease (CCVD) preventing and treating is more and more serious, and in order to get rid of the threaten of CCVD outbreak before dawn, the most efficient method is to prepare medicine for treating the cardiovascular disease into sustained release preparations which can prolong medicine effects. Appropriate blood concentration can be provided for human body during a predetermined period based on needs, times of medicine taking are decreased, and good treatment effects can be obtained. The preparations are very convenient for sufferers, particularly patients taking medicine for a long time. According to the bear bile cardio-reliever pill sustained release preparations, ethocel is used as coating material to be prepared into membranes, and polyethylene glycol 6000 is added as porogen. When the sustained release coating containing the porogon contacts with water or digestive juice, the porogen part on the coating membranes is dissolved or falls off, the membranes form a micropore or spongy structure, and permeability of mediums and medicine is increased, accordingly, medicine release rate is adjusted.

Description

Fel Ursi JIUXIN DAN slow releasing preparation

Technical field

Present technique belongs to the exploitation of the Chinese medicine new varieties in biological and the new medicine technology, and the new compound preparation of being processed by Chinese medicine, natural drug is to the secondary development of famous-brand and high-quality Chinese patent medicine and ethnic drug.

Background technology

Along with the development of society, the variation of natural environment and people's rule of life, variation has also taken place in the human diseases spectrum.Nowadays, cardiovascular and cerebrovascular disease has become one of healthy maximum killer of harm humans, and the situation of control cardiovascular and cerebrovascular disease is more and more severeer.

In recent years, the incident of the sudden death of some celebrities both at home and abroad occurs repeatedly, and " arch-criminal " that cause dying suddenly---and cardiovascular and cerebrovascular disease is often in the burst of period in morning, so, be called by people during this period of time " devil's time ", become patient's " danger spot " together.

The medicine and the therapy of treatment cardiovascular and cerebrovascular disease are constantly weeded out the old and bring forth the new, but owing to drug effect falls short of, the same with a lot of similar medicines, be difficult to let the patient spend " devil's time " in comfort.According to relevant expert's introduction, accidents such as acute heart failure, acute myocardial infarction or sudden death have tangible timeliness.Be mainly in night during 21-24 and morning during 1-5 like acute left heart failure; Acute myocardial infarction, sudden cardiac death are mainly in morning during 4-6, and be another multiple peak of acute myocardial infarction evening during 19-24.But; The drug effect of general cardiovascular drugs approximately can only be kept 2-6 hour; The medicine of taking before sleeping morning time difference seldom metabolism finish; Make the heart that is in critical days can not get effective protection of medicine, thereby cardiovascular disease such as acute heart failure, acute myocardial infarction or sudden death are taken place frequently.

In order to break away from the threat of " devil's time ", the most effectively way is exactly to process slow releasing agent to the cardiovascular medicine of treatment, makes it to prolong EDD.

Yet the slow release problem of Chinese medicine compound is one hang-up of puzzlement medical scientific research worker always.As everyone knows, Western medicine so be easy to make its effective ingredient slowly to discharge, is kept the active drug concentration of long period with activation because composition is comparatively single, and prolonged the action time of once taking medicine.And Chinese medicine, especially Chinese medicine compound, the composition more complicated, it requires not only will remain valid the slow release of composition, but also will let all effective ingredient discharge according to set balanced proportion, could guarantee the permanent stable of therapeutical effect like this.Undoubtedly, want to capture this road difficulty, difficulty is really not little.

" early evening one, driving the flu puzzlement away " what's frequently heard can be repeated in detail for this advertising words.12 hours slow release method has been brought comfortable and convenient to patient, people need not pinch wrist-watch calculating and how long take medicine again in addition.Yet wanted to have one day and took medicine this thing only to need weekly or even every month once? The time concept that the drug release technology takes medicine for the more and more faster modern's another kind of rhythm of life.

For the Chinese Medicine industry of the shortage of capital, slow release method is one is worth good developing direction.

" drug release " is not a completely new concept, and global radiopharmacy has been seen the growth momentum that it is rising already.Annual; Each big pharmaceuticals of the world all will drop into substantial contribution in the research and development of new medicine; Yet long with respect to the new drug research and development time cycle, cost is high and drop into to reclaim and to have a big risk, serve as that the basis changes formulation method and has low-risk, short period, the rational advantage of repayment undoubtedly with the drug release technology of taking method with original medicine.General a kind of new medicine will pass through the time of several years or even more than ten years from studying clinical experiment again to official listing, and data show that having only 3/10ths sales volume to surpass average research and development in the new medicine of listing drops into.Drug release does not then need the so long research and development time, drops into and reduces to 1/15 of development new drug yet.The market of drug release enlarges in the world, expects 2005 and will reach 86,000,000,000 dollars.

Except the input of pharmaceuticals reduces and the key advantages place that is benefited in many ways and is only the drug release technology is arranged the reasonable repayment.The supplier of patient and medical services---medical institutions such as hospital also can benefit in this technology.Through drug release technology, the curative effect of medicine is enhanced, and takes more convenient saferly, feel also more comfortable, and with respect to the medicine of new research and development, price is wanted cheaply.Simultaneously, the efficient that the drug release technology also makes hospital's medicine drop into is able to strengthen, and extends to treatment outside the medical institutions.

The pharmaceutical industry of China is in the low research and development input stage always, and the research and development input of new product is merely the 1%-3% of sales volume, and sales volume is 300,000,000-600,000,000 dollars, and scale is very limited.The product of innovation is seldom mostly also carrying out the competition of low quality low price, and average profit on sales is less than 10%.Just under these circumstances, the pharmaceutical industry of accession to WTO back China will face the international trend of globalization and from the competition of external pharmaceuticals.Undoubtedly, the drug release technology of less investment instant effect will become the opportunity of development, and it can solve and lack new product, the limited problem of research and development input, brings the product of the better property rate of exchange.In fact, country all takes much count of the drug release technology all the time, once is put in the Seventh Five-Year Plan to Tenth-Five Year Plan, 863 Program and the national new product planning.

China is the native place of Chinese medicine, yet China every year need be from the nearly 600,000,000 dollars of Chinese medicines of external import, and reason just is that China's Chinese medicine drug release technology is not enough, lacks the development Experience of the modern preparation of Chinese medicine.Also Just because of this, the share in China plant amedica market in the world descends rapidly.In field such as the cancer treating medicine biological product and the vaccine of other suitable drug release technology, the also few of advantage of the pharmaceutical industry of China.Can predict the drug release technology and have huge and be full of the market of potentiality, can be widely applied to the biological product and the field of Chinese medicines, also can become the very strong driving force engine of pharmaceuticals industry development in China.

Summary of the invention

Slow releasing preparation can be on demand in the scheduled period for human body provides suitable blood drug level, reduce and take number of times and can obtain excellent curative.Its important feature is can make human body keep this kind haemoconcentration to reach the long time; And descend quickly unlike the ordinary preparation that kind; Thereby " peak valley " phenomenon that just can avoid the ordinary preparation frequent drug administration to be occurred increases safety, effectiveness and the adaptability of medicine.Because of having reduced the medication number of times, greatly facilitate the patient, particularly the patient of long-term prescription.

Oral slow-releasing preparation generally all is that the characteristics such as stripping, diffusion, infiltration and ion exchange through medicine are controlled.Under many situation, mainly be adjuvant through selecting to suit, adopt preparation technique to reach and delay the release purpose.The influence of the physicochemical property of design sustained release pharmaceutical formulation considered medicine own; Type like crystal formation; Absorb the combination rate with plasma protein in the dissolubility of medicine, partition coefficient, medicine stability and the body in Digestive system, the relation between medicine PKA value and biomembrane permeability etc.Simultaneously, to consider that also physiologic factor is to the slow release formulation Effect on Performance: the absorption of medicine, distribution, metabolism, pharmaceutically-active slow-release time, therapeutic index and disease condition etc.

Controlled release preparation is the one type of dosage form of polymeric membrane that is enclosed with the control drug release rate in the Drug Storage periphery, as required, can be prepared into multi-layered type, cylinder type, and ball-type or sheet type multi-form, and corresponding preparation method is arranged.As with the various controlled release tablet of ethyl cellulose, permeability acrylic resin coating, with the ethylene-vinyl acetate copolymer be release-controlled film pilocarpine week imitate eye mask, be the Progesterone intrauterine device of release-controlled film with silicone rubber, be that release-controlled film, polyisobutylene are the scopolamine percutaneous sticking plaster of Drug Storage with the capillary polypropylene.Be common wherein with various coated tablets and coated pellets.

Fel Ursi JIUXIN DAN slow releasing agent adopts the coated slow release preparation, is to select for use one or more to mix coating material to the pilule coating, is regarded as bank (coating) system, in the macromolecule coating material of this system, contains the pastille core.

The clothing film that wraps up on slow release of processing with packaging technique or the controlled release preparation is not single, pure entity, and coating material is coating separately, forms the clothing film with certain permeability and mechanical performance.Coating material must be made into coating solution with the righttest coating prescription, adopts the certain process coating, could form the film with reproducible continuous, the homogeneous of slow, controlled-release function and release.The clothing film is the mixture that contains several components mostly.

The specific embodiment

Fel Ursi JIUXIN DAN slow releasing preparation is a microporous membrane coated slow release preparation, and the micropore coating material adopts ethyl cellulose.When the release controlling coating material ethyl cellulose was processed the film of closure, often medicine can't dissolve from label or ball core, infiltrate.In membrane material solution, add soluble high-molecular material polyethylene glycol 6000 (PEG 6000) as the porogen of film, increase the permeability of coating membrane, to obtain the coated preparation of required rate of releasing drug, PEG plays the rapid release effect again simultaneously.

When containing the porogen sustained release coating and contacting with water or Digestive system, the porogen on the coating membrane is partly dissolved or comes off, and makes film form micropore or spongiosis, increases the permeability of medium and medicine, in order to the adjusting rate of releasing drug.

The ball core is placed in the coating pan, adopt turnadle pan coating, rotate the centrifugal force that produces by coating pan and constantly overturn.Utilize rolling spray coating technology, the coating solution that is made into ethyl cellulose and PEG 6000 carries out coating, coating solution is sprayed on the medicine of upset, makes it to form the layer of even thin film and obtain slow release effect on its surface.

Claims (2)

1. be the secondary development of Chinese patent medicine Fel Ursi JIUXIN DAN, process slow releasing preparation.

2. adopt the microporous membrane packaging technique, the coating solution that is made into ethyl cellulose and PEG 6000 carries out coating, reaches the slow release purpose.