CN1150894C - Preparation of oral coated medicine grains - Google Patents
Preparation of oral coated medicine grainsInfo
- Publication number
- CN1150894C CN1150894C CNB001142054A CN00114205A CN1150894C CN 1150894 C CN1150894 C CN 1150894C CN B001142054 A CNB001142054 A CN B001142054A CN 00114205 A CN00114205 A CN 00114205A CN 1150894 C CN1150894 C CN 1150894C
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- medicines
- oral
- coating
- preparation
- coatings
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- Expired - Fee Related
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention provides a preparation technology of an oral preparation of which the medicinal granule has a coating layer. The oral preparation comprises chemical medicines, antibiotic medicines and Chinese medicines, wherein the chemical medicines comprise ibuprofen, aspirin, etc.; the antibiotic medicines comprise erythrocin, roxithromycin, clindamycin hydrochloride, etc.; the Chinese medicines comprise inner ester of common andrographis herb, berberine, etc. The present invention is characterized in that medicinal powder (40 to 100 meshes) is sprayed and coated by enteric or gastric coating materials in a spraying and coating device such as boiling drying granulator, one-step granulator and a multifunctional granulator in a fluidized state to evenly coat at least one coating layer to make coating granules; according to wrapping degree and varieties, an eluant capable of dissolving medicines but incapable of dissolving the coating materials is used for eluting the medicines not coated; then, the coating granules are made into an oral medicine preparation according to a traditional technology. The outside coating layer is instantly dissolved after the oral medicinal preparation prepared by the present invention enters the intestinal tract, which obviously reduces the stimulation of the medicines to the stomach and is capable of covering the bitter taste and the bad odor of the medicines.
Description
Technical field
The present invention relates to the preparation method of medicine, particularly a kind of drug particles has the preparation technology of the oral agents of coatings.
Background technology
By traditional handicraft, solving oral drugs is to make enteric coatel tablets or enteric coated capsule to the untoward reaction of stomach, various countries' pharmacopeia regulation enteric coatel tablets or capsule in simulated gastric fluid 2 hours must not disintegrate or dissolve.After entering intestinal, the disintegrate again of tablet or capsule is absorbed by small bowel then, enters blood, and its time that reaches effective haemoconcentration is long.But in traditional handicraft, the problem that solves drug flavor is to adopt sugar coating or gastric solubleness film-coat or encapsulated, adds sweeting agent simultaneously and comes flavoring, and this will bring a problem to children and diabetics medication.For children, when Swertia Tablet and capsule volume were excessive, the child was difficult to take, take if tablet smash to fragmentate or capsule taken apart, then can't avoid the bitterness problem, general granule, dry syrup just come flavoring with a large amount of sweeting agents, when bitterness is too heavy, its effect is also bad, and concerning diabetics, the diet of its every day all should be controlled the absorption of sugar, takes that to contain sugar high as coated tablet and granule, dry syrup and so on medicine can produce harmful effect to patient's the state of an illness.
The objective of the invention is to overcome above-mentioned deficiency, and provide a kind of employing 40-100 order granule coating technology to make tablet or capsule, make drug particles be wrapped one deck does not produce stimulation to the taste bud of lingual surface coating material equably, can not produce stomach stimulates, enter the coatings that to dissolve the outside behind the intestinal again rapidly, discharge medicine, the time that reaches effective blood drug concentration shortens greatly.Thereby not only reached the purpose of covering bitter taste of drug, significantly reduced the stimulation degree of medicine simultaneously stomach.
The objective of the invention is to solve by following scheme: the medicine of realizing coating comprises: chemical medicine such as ibuprofen, aspirin etc.; Tri-Biocin such as erythromycin, Roxithromycin, Clindamycin Hydrochloride etc.; Chinese medicine such as creat lactone, berberine etc.; being prepared as of its coated drugs: the thing powder 40-100 order of getting it filled; adopt enteric or gastric solubleness coating material; at airpillow-dry granulator, one-step-granulating method or multi-functional granulator; under fluidized state, carry out spray coating in the equipment of spray coating; wrap one deck coatings at least equably; make coated granule; according to parcel degree and the kind medicament elution that the insoluble eluant of separating the coating material will not wrap up with the solubilized medicine, make oral drug preparation by traditional handicraft then.
Described drug particles has the preparation technology of the oral formulations of coatings, and the equipment that carries out spray coating under fluidized state is: airpillow-dry granulator, one-step-granulating method or multi-functional granulator.
Above-mentioned drug particles has the preparation technology of the oral formulations of coatings, and described oral drug preparation is capsule or granule.
Above-mentioned drug particles has the preparation technology of the oral formulations of coatings, and described enteric-coating material is an acrylic acid II resin; Described gastric solubleness coating material is an acrylic acid IV resin.
Tablet that the present invention makes or capsule, it collapses at stomach and looses into tiny drug particles, because the drug particles outside is surrounded by the thin film clothing, medicine is not stripping or seldom stripping in gastric juice, and tiny granule is very fast to enter intestinal by pylorus, medicine just can not produce stimulation or stimulate very little stomach like this, and tiny drug particles is wanted much shorter by complete tablet or the required time of capsule of time ratio that stomach enters intestinal, enter behind the intestinal again the coatings of dissolving outside rapidly, discharge medicine, its time that reaches effective blood drug concentration shortens greatly; Compare with those gastric solubility preparations in addition, gastric solubility preparation is in the rapid disintegrate of stomach, and with drug release, medicine produces thus to the untoward reaction of stomach, is made of many fine hair owing to human small intestine's sorbent surface is long-pending simultaneously, up to 70m
2Its with the ratio of gastric surface area above 100 times, the overwhelming majority of digesting and assimilating of human body is finished in small intestinal, because granule coating has just been wrapped the coating material that is equivalent to the weight 1-10% of medicine own equably in the drug particles outside, compare with enteric coatel tablets or enteric coated capsule, the shared weight ratio of coatings is lower than or is equivalent to enteric coatel tablets or enteric coated capsule, and the surface area of granule ratio is far longer than slice, thin piece or capsule, the coatings thickness of coated granule than the coatings thickness of enteric coatel tablets want book many, so can not produce the problem that absorb to reduce in the intravital absorption of people after the granule coating.
Description of drawings
The present invention is further described below in conjunction with process chart:
Fig. 1 is the process chart of embodiment 1;
Fig. 2 is the process chart of embodiment 2.
The specific embodiment
The preparation technology that drug particles has the oral agents of coatings is: with 40-100 purpose drug powder; put into airpillow-dry granulator; carry out in the equipment of spray coating under the fluidized state such as one-step-granulating method or multi-functional granulator; open the air intake switch; regulate intake; make drug particles be the boiling shape; regulate 40-60 ℃ of inlet temperature; open spray switch; the coating solution (coating material that accounts for drug weight 1-10% is made with the appropriate solvent dissolving) for preparing is carried out spray coating with uniform vaporific spraying in the medicine, after coating solution has sprayed, continue to ventilate 30 minutes; make particle drying; according to kind, replaceable coating solution, or carry out secondary even coating repeatedly with same coating solution; after the granule taking-up; according to the parcel degree, available eluant carries out eluting with coated granule, with the medicine flush away that does not encase.
Embodiment 1:
As shown in Figure 1; With the Clindamycin Hydrochloride powder is example; the Clindamycin Hydrochloride raw material is sieved; get the Clindamycin Hydrochloride powder between the 60-100 order; put into the equipment of spray coatings such as airpillow-dry granulator, one-step-granulating method or multi-functional granulator; under fluidized state, use 5% alcoholic solution spray coating of the acrylic acid II resin of drug weight 3%; wrap one deck coatings at least equably; make coated granule; then with lactose, micropowder silica gel, magnesium stearate mix homogeneously; fill out back, polishing; aluminum-plastic packaged or the bottling, be packaged into finished product then.By the clindamycin capsule of above-mentioned explained hereafter, we are referred to as Wan Kening.
The curative effect situation contrast of the Wan Kening that common clindamycin capsule and the present invention make is as shown in the table:
The curative effect situation
Conclusion: 1, two groups of effective percentage there was no significant differences (P＞0.01).The adverse reaction rate of the Wan Kening that common clindamycin Hydrochloride capsule and the present invention make and untoward reaction symptom statistics are as follows:
| Wan Kening organizes (52 example) | Clindamycin group (50 example) | |
| The unchanged efficient that always has that takes a turn for the better is cured in the scorching acute attack of acute upper respiratory infection acute bronchitis pneumonia chronic bronchial | 17 19 11 5 45/52 12/52 1/52 98.1％ | 10 30 5 5 42/50 12/50 1/50 98％ |
The score of adverse reaction rate and untoward reaction symptom
Conclusion 2: adverse reaction rate is organized apparently higher than Wan Kening during clindamycin treatment respiratory tract infection.
| Disease | Wan Kening organizes (n=52) | Clindamycin group (n=50) | ||
| Feel sick or epigastric discomfort incidence rate (%) | Incidence of vomiting (%) | Feel sick or epigastric discomfort incidence rate (%) | Incidence of vomiting (%) | |
| Acute upper respiratory tract infection acute bronchitis acute episode of chronic bronchitis pneumonia | 5.9(0.06％) 47.4(4.26) 0(0) 9.1(0.09) | 0(0) 0(0) 0(0) 0(0) | 50.0(3.50) 70.0(17.50) 60.0(1.80) 60.0(3.00) | 20.0(0.40) 13.3(0.53) 0(0) 0(0) |
At above-mentioned comparison, the author has also observed respiratory tract infection patient 5 examples of original gastroduodenal ulcer or chronic gastritis, it is obvious to use the oral back of clindamycin gastrointestinal side effect, change oral Wan Kening into and still can adhere to treatment, show that Wan Kening behind technologic improvement more is applicable to outpatient service respiratory tract infection patient's treatment.
Model case:
Example 1: women 46 years old because of acute bronchitis is admitted to hospital, previously has the chronic gastritis medical history, give 0.3 every day of oral clindamycin three times, normal saline 250ml+ amikacin is 0.4 quiet simultaneously, in second day afternoon of medication epigastrium dull pain discomfort occurs, feel sick, poor appetite, rise morning next day, change into ten thousand can peaceful 0.3 orally, every day three times, all the other treat constant afternoon on the same day, above-mentioned symptom obviously alleviates, slight epigastric discomfort is only arranged, can stand, and adhere to that oral ten thousand can be peaceful 8 days.
Example 2: male 37 years old, because of acute upper respiratory tract infection is admitted to hospital, the medical history that duodenal ulcer is previously arranged, give 0.3 every day of oral clindamycin three times, 10% glucose 500ml+ SHUANGHUANLIAN is 3.0 quiet simultaneously, when oral same day dinner, epigastric discomfort occurs, feel sick, companion's vomiting 3 times, give motilium 10mg oral after, vomiting takes a turn for the better, and behind the morning next day oral once more clindamycin 0.3, occurs vomiting 1 time once more, change ten thousand can peaceful 0.3 every day three times oral, adhered to treating 5 days, conscious have bitter taste, a poor appetite, do not have feel sick, vomiting.
Example 3: male 19 years old, because of acute suppurative tonsillitis is admitted to hospital, previously the chronic gastritis medical history is arranged, give 0.3 every day of oral clindamycin three times after being admitted to hospital, 10% glucose 500ml+ SHUANGHUANLIAN is 3.0 quiet simultaneously, epigastrium pain, obviously nauseating appearred second day oral afternoon, patient requires to stop the oral medicine treatment, after persuasion, change give ten thousand can peaceful 0.3 every day three times oral, above-mentioned symptom disappears, and adheres to treating 5 days.
Embodiment 2:
As shown in Figure 2; with the Roxithromycin granule is example; the Roxithromycin raw material is sieved; get 40-100 order Roxithromycin powder; alcoholic solution with 12% acrylic resin IV number; at airpillow-dry granulator; in the equipment of spray coating such as one-step-granulating method or multi-functional granulator; spray coating under fluidized state; the coating amount is the 3-4% of drug weight; follow alcoholic solution or II with 5% acrylic resin II number; share for III number and carry out the coating second time; the parcel amount is the drug weight of 3-4%; then with this enwrapped granule with ether or with other to medicine dissolution, and the solution of insoluble II resin floods granule and stirs out, with buchner funnel sucking filtration eluting; with 55-60 ° of following temperature drying two hours; make the drug coating granule, add sucrose; protein sugar; the CMC-Na dextrin; starch is granulated with the alcohol-water solution of syrup or HPMC; with bag in the granule racking machine, be packaged into finished product at last.The Roxithromycin granule that makes with this technology, a child tastes comparison surplus ten, and its bitterness is covered substantially, and the mouthfeel of the Roxithromycin granule of producing than domestic other several families pharmaceutical factory is all good.Specifically see the following form:
Roxithromycin granule taste comparative result statistical table
| Name | Age | Sex | Product 1 | Product 2 | Product 3 |
| Luo Wentaozedong Dong Xiao department is contained Sun Lu Chen Yi old behaviour Peng little Chongqing Luo Li light Wang Jiangling | 8 8 5 2 2 8 8 9 9 12 | Male men and women man men and women man man | - - - - - - - + - - | + + - - - - + - + - | + + + + + + - - - - + + + + + + + + - - |
Test adopts double blind control to carry out.
-expression mouthfeel hardship; + expression is uncertain; ++ the expression mouthfeel is good, sweet.
Product 1 and product 2 are Roxithromycin granules of buying from pharmacy, and product 3 is Roxithromycin granules made from coated granule.
Result of the test shows that with the mould granule of Luo Hong that coated granule is made, its taste is far better than the taste of other two kinds of Roxithromycin granules.
Claims (4)
1, a kind of drug particles has the preparation technology of the oral formulations of coatings, its Chinese medicine is a Tri-Biocin, be selected from erythromycin, Roxithromycin, Clindamycin Hydrochloride, it is characterized in that: get 40-100 purpose drug powder, adopt enteric or gastric solubleness coating material, under fluidized state, carry out spray coating in the equipment of spray coating, wrap one deck coatings at least equably, make a coating material, wherein the weight of coatings is the 1-10% of drug weight, according to parcel degree and kind, the medicament elution that the insoluble eluant of separating the coating material will not wrap up with the solubilized medicine is made oral drug preparation by traditional handicraft then.
2, drug particles according to claim 1 has the preparation technology of the oral formulations of coatings, it is characterized in that: the equipment that carries out spray coating under fluidized state is airpillow-dry granulator, one-step-granulating method or multi-functional granulator.
3, drug particles according to claim 1 has the preparation technology of the oral formulations of coatings, it is characterized in that: described oral drug preparation is capsule or granule.
4, drug particles according to claim 1 has the preparation technology of the oral formulations of coatings, it is characterized in that: described enteric-coating material is an acrylic acid II resin; Described gastric solubleness coating material is an acrylic acid IV resin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB001142054A CN1150894C (en) | 2000-04-17 | 2000-04-17 | Preparation of oral coated medicine grains |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB001142054A CN1150894C (en) | 2000-04-17 | 2000-04-17 | Preparation of oral coated medicine grains |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1318369A CN1318369A (en) | 2001-10-24 |
| CN1150894C true CN1150894C (en) | 2004-05-26 |
Family
ID=4583916
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB001142054A Expired - Fee Related CN1150894C (en) | 2000-04-17 | 2000-04-17 | Preparation of oral coated medicine grains |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1150894C (en) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101502492B (en) * | 2009-03-13 | 2013-11-27 | 上海微丸医药开发有限公司 | Method for preparing clarithromycin granule without bitter taste |
| CN101879141B (en) * | 2009-05-05 | 2013-07-17 | 烟台绿叶动物保健品有限公司 | Taste-masking tilmicosin gastric-soluble particle preparation |
| CN102716171B (en) * | 2012-06-28 | 2014-05-07 | 江西本草天工科技有限责任公司 | Compound common andrographis herb taste-masking particles and preparation method thereof |
| CN105769822A (en) * | 2014-12-26 | 2016-07-20 | 广州朗圣药业有限公司 | Preparation method of aspirin enteric microencapsulated capsule |
| CN105168171A (en) * | 2015-10-23 | 2015-12-23 | 成都乾坤动物药业有限公司 | Andrographolide enteric-coated tablet as well as preparation method and application thereof |
| CN110075085A (en) * | 2019-05-17 | 2019-08-02 | 南京望知星医药科技有限公司 | A kind of roxithromycin micro-capsule and preparation method thereof |
-
2000
- 2000-04-17 CN CNB001142054A patent/CN1150894C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN1318369A (en) | 2001-10-24 |
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Legal Events
| Date | Code | Title | Description |
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| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| EC01 | Cancellation of recordation of patent licensing contract |
Assignee: Chengong Pharmaceuticals Co., Ltd., Nanjing Assignor: Bao Changkang Contract record no.: 2010320001256 Date of cancellation: 20110124 |
|
| EE01 | Entry into force of recordation of patent licensing contract |
Assignee: Chengong Pharmaceuticals Co., Ltd., Nanjing Assignor: Bao Changkang Contract record no.: 2011320000023 Denomination of invention: Preparation of oral coated medicine grains Granted publication date: 20040526 License type: Exclusive License Open date: 20011024 Record date: 20110125 Assignee: Chengong Pharmaceuticals Co., Ltd., Nanjing Assignor: Bao Changkang Contract record no.: 2010320001256 Denomination of invention: Preparation of oral coated medicine grains Granted publication date: 20040526 License type: Exclusive License Open date: 20011024 Record date: 20101229 |
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| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20040526 Termination date: 20170417 |