CN1201665A - Slowly releasing implanted medicines of penicillins and preparation thereof - Google Patents
Slowly releasing implanted medicines of penicillins and preparation thereof Download PDFInfo
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- CN1201665A CN1201665A CN 97107072 CN97107072A CN1201665A CN 1201665 A CN1201665 A CN 1201665A CN 97107072 CN97107072 CN 97107072 CN 97107072 A CN97107072 A CN 97107072A CN 1201665 A CN1201665 A CN 1201665A
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- implanted
- medicines
- penicillins
- slowly releasing
- penicillin
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Abstract
A slow-released penicillin kind of medicines which can be grafted into body is prepared from penicillin kind of medicines, biodegradable polymer, retarder and pore-forming agent.The medicines in the form of rod or particle can be grafted into body for locally long acting in order to improve curative effect on chronic diseases. Its advantages include low dosage, and reduction of toxic by-effect to whole body.
Description
The present invention relates to a kind of antibiotic medicine novel formulation, novel form of a kind of penicillins of more specifically saying so and preparation method thereof.
Penicillins is a kind of anti-infectives commonly used, can be under high dilution some special microorganisms such as antibacterial, fungus, rickettsia, mycoplasma etc. be killed or inhibitory action.Be applicable to that A group Hemolytic streptococcus, B organize the various infection due to Hemolytic streptococcus, the streptococcus pneumoniae etc., as septicemia, pneumonia, meningitis, tonsillitis, otitis media, scarlet fever, erysipelas, lochiopyra, tetanus, syphilis, gonorrhea, relapsing fever, actinomycosis etc.
Penicillins is mainly from vein, intramuscular injection and oral administration, belong to the systemic administration pattern, when treating some chronic local disease, can only realize by whole body administration repeatedly, so on the one hand because the blood circulation amount causes local lesion not reach active drug concentration, unsatisfactory curative effect less.Most on the other hand medicines by normal structure repeatedly absorb, metabolism, easily cause Drug resistance and toxic and side effects to a certain degree.
The purpose of this invention is to provide a kind of slowly releasing implanted medicines of penicillins and preparation method thereof, after the penicillins slow releasing pharmaceutical implants, can improve lesions position active drug concentration and prolong drug and bacterial action time, the great amplitude of the total medication of clinical treatment is descended, improve curative effect, reduce administration number of times and general toxic and side effects.
The objective of the invention is to be achieved through the following technical solutions.
A kind of slowly releasing implanted medicines of penicillins, it is a kind ofly to be implanted into agent by containing the body that the following weight proportion raw material makes,
Penicillin medicine 30～95%
Slow release thing 5～68%
Blocker 0～20%
Porogen 0～20%
The slow release thing is meant biological degradation polyalcohol or biodegradation chemical compound
Blocker is meant lyophobic dust,
Porogen is meant water miscible low molecule.
Penicillin medicine is meant penicillin sodium, benzylpenicillin potassium, bristopen, cloxacillin sodium, ampicillin, amoxicillin, Carbenicillin, fluorine piperazine penicillin and penicillanic acid.
The biodegradation chemical compound is
A, chitin
B, gelatin
C, extra large bath acid sodium
D, glucosan
E, polyvidone
F, Polyethylene Glycol
G, polylactic acid
Blocker is selected from
A, stearic acid, calcium stearate,
B, higher fatty acids, high fatty alcohol,
C, glyceryl stearate;
Porogen is selected from sodium chloride, potassium chloride
Body is implanted into medicine rod or the medicine grain that agent is meant that internal lesions position is implanted.
The preferable weight proportion of each raw material components is:
A, penicillin medicine 30～80%
Biodegradation chemical compound 15～68%
Blocker 2～20%
Porogen 0～5%
The preferable weight proportion of each raw material components is:
A, penicillin medicine 49～80%
Biodegradation chemical compound 18～49%
Blocker 1～3%
Porogen 0.5～2%
Or
B, penicillin medicine 55～84%
Lactic acid polymer 15～44%
Blocker 0～2%
Porogen 1～4%
The preferable weight proportion of each raw material components is:
A, penicillin medicine 55～85%
Biodegradation chemical compound 15～45%
Or
B, penicillin medicine 60～90%
Polylactic acid 10～40%
The preferable weight proportion of each raw material components is:
A, penicillin medicine 50～80%
Chitin 20～45%
High fatty alcohol 0～5%
Or
B, penicillin medicine 30～80%
Gelatin 15～60%
High fatty alcohol 5～20%
Or
C, penicillin medicine 30～70%
Glucosan 25～65%
Sea bath acid sodium 5～10%
Or
D, penicillin medicine 30～80%
Polyethylene Glycol 18～65%
High fatty alcohol 2～10%
E, penicillin medicine 60～90%
Polylactic acid 10～35%
Porogen 0～5%
A kind of preparation method of slowly releasing implanted medicines of penicillins is to adopt fusion method, with each component mix homogeneously, inserts melt molding in the mould, cooling and demolding by proportioning.
A kind of preparation method of slowly releasing implanted medicines of penicillins is to adopt solvent method, in solvent, with each component mix homogeneously, inserts die for molding by proportioning, removes the back depanning of desolvating.
A kind of preparation method of slowly releasing implanted medicines of penicillins is to adopt the microsphere method of forming of filming, preparation medicine microspheres earlier, after film, then by proportioning combination forming in mould.
A kind of preparation method of slowly releasing implanted medicines of penicillins is to adopt the mixed-forming method, presses proportioning with each component mix homogeneously, in die for molding.
The present invention selects for use biological degradation polyalcohol and blocker, porogen as adjuvant.After biological degradation polyalcohol implants, under the effect of body fluid and enzyme etc., can be biodegradable into, excrete then, human body is had no side effect to existing micromolecular compound in the human body is absorbed by the body, metabolism.Blocker means the stearic acid lyophobic dust, and porogen means water-soluble substanceses such as sodium chloride, enters in the human body and progressively all can be organized absorption after the release.
The rate of release of penicillin medicine can be controlled or delay to biological degradation polyalcohol effectively, can be controlled at release time in 1～15 day scope.
As excipient, framework material and slow release material play a part bonding setting and slow release to biological degradation polyalcohol in prescription.Make the penicillins slow releasing pharmaceutical implant of making have required shape, intensity, toughness, multifrequency natures such as drug release feature and human body intermiscibility.
Blocker and porogen can slow down or increase the rate of release of penicillin medicine in prescription, regulate drug release feature.
The curative effect of Drug therapy disease depends primarily on the active drug concentration of lesions position and the product of action time.The penicillins slow releasing pharmaceutical is implanted into by body, can form effective drug level and keep sufficiently long time of contact with antibacterial at lesions position, realizes local long-acting medication.Patient dosage and medication number of times can significantly reduce, and the general toxic and side effects is expected big basic the elimination, improves a collection of chronic local pertinacious disease patient's cure rate most probably, reduces medical expense greatly, and new active treatment means are provided.
By the following examples, the invention will be further described.
Embodiment 1
On clean work station, with special coating pan with the 200g penicillin sodium, the pelletize of 5g high fatty alcohol, particle diameter is controlled at φ 0.2-0.5mm scope, gradation will contain in the 40g chitin solution input coating pan again, formation is kernel with the penicillin sodium microsphere, chitin is the microcapsule of peplos, in 40 ℃ of following dry solidifications 2 hours, drops into the solution uniform mixing that contains the 60g chitin again, be pressed into molding in the stainless steel mould, leave standstill and solidified 24 hours, again at 40 ℃, 0.09MPa dry 6 hours down, check, the encapsulation of sterilization back.
In 37 ℃ of constant temperature normal saline, soaked 7 days release amount about 90～95%.
Embodiment 2
On clean work station, earlier 15g polylactic acid (it is 8000 that molecular weight peak value GPC surveys) is ground with mortar, render in the special rustless steel agitator after crossing 200 mesh sieves, drop into again to mix behind the 100g bristopen and mix discharging thoroughly.Put into mould, slowly be heated to 60 ℃, keep 6 hours postcooling, depanning, the sterilization encapsulation of check back to room temperature.
In 37 ℃ of constant temperature normal saline, soaked 7 days release amount 80～90%.
Embodiment 3
On clean work station, the 50g ampicillin is rendered in the special rustless steel agitator, drop into again and pour in the special mould after 30% gelatin solution mixes, at 5KPa, slough solvent under 60 ℃, depanning, the sterilization encapsulation of check back.
In 37 ℃ of constant temperature normal saline, soaked 7 days release amount 100%.
Embodiment 4
On clean work station, get the 50g amoxicillin, put in the 50ml solution that contains the 4g sodium alginate, mix thoroughly, add the aqueous solution that contains the 25g glucosan again.Uniform mixing in special rustless steel blender is pressed into molding in the stainless steel mould, and at 65 ℃, dehydrate is 6 hours under 5～50MPa, check, the encapsulation of sterilization back.
In 37 ℃ of constant temperature normal saline, soaked 7 days release amount about 96～98%.
Embodiment 5
On clean work station, the 50g carbenicillin thrown to put into contain the 30g Polyethylene Glycol, in the 100ml solution of 6g high fatty alcohol, pour uniform mixing in the special rustless steel agitator into,, under the 0.01MPa mixture is dried to the clay shape at 50 ℃, be pressed into molding in the stainless steel mould again, at 60 ℃, 0.0MPa dry 4 hours down encapsulates after being cooled to room temperature, the demoulding, sterilization.
In 37 ℃ of constant temperature normal saline, soaked 7 days release amount 65～76%.Different embodiment drug release features relatively
| Embodiment | Cumulative release average percentage (%) in 37 ℃ of normal saline | ||||||
| ????1 | ????2 | ????3 | ????4 | ????5 | ????6 | ????7 | |
| ??1 ??2 ??3 ??4 ??5 | ????35 ????28 ????48 ????38 ????28 | ????50 ????46 ????71 ????51 ????41 | ????62 ????58 ????88 ????64 ????50 | ????72 ????67 ????95 ????75 ????58 | ????80 ????74 ????98 ????84 ????63 | ????87 ????81 ????99 ????92 ????68 | ????92 ????86 ????100 ????97 ????71 |
Claims (12)
1, a kind of slowly releasing implanted medicines of penicillins is characterized in that it is a kind ofly to be implanted into agent by containing the body that the following weight proportion raw material makes,
Penicillin medicine 30～95%
Slow release thing 5～68%
Blocker 0～20%
Porogen 0～20%
The slow release thing is meant biological degradation polyalcohol or biodegradation chemical compound,
Blocker is meant lyophobic dust,
Porogen is meant water miscible low molecule.
2, a kind of slowly releasing implanted medicines of penicillins according to claim 1 is characterized in that penicillin medicine is meant penicillin sodium, benzylpenicillin potassium, bristopen, cloxacillin sodium, ampicillin, amoxicillin, Carbenicillin, fluorine piperazine penicillin and penicillanic acid.
3, a kind of slowly releasing implanted medicines of penicillins according to claim 1 is characterized in that
The biodegradation chemical compound is
A, chitin
B, gelatin
C, extra large bath acid sodium
D, glucosan
E, polyvidone
F, Polyethylene Glycol
G, polylactic acid
Blocker is selected from
A, stearic acid, calcium stearate,
B, higher fatty acids, high fatty alcohol,
C, glyceryl stearate;
Porogen is selected from sodium chloride, potassium chloride
4, a kind of slowly releasing implanted medicines of penicillins according to claim 1 is characterized in that body is implanted into medicine rod or medicine grain that agent is meant that internal lesions position is implanted.
5, a kind of slowly releasing implanted medicines of penicillins according to claim 3 is characterized in that the preferable weight proportion of each raw material components is;
A, penicillin medicine 30～80%
Biodegradation chemical compound 15～68%
Blocker 2～20%
Porogen 0～5%
6, a kind of slowly releasing implanted medicines of penicillins according to claim 3 is characterized in that the preferable weight proportion of each raw material components is:
A, penicillin medicine 49～80%
Biodegradation chemical compound 18～49%
Blocker 1～3%
Porogen 0.5～2%
Or
B, penicillin medicine 55～84%
Lactic acid polymer 15～44%
Blocker 0～2%
Porogen 1～4%
7, a kind of slowly releasing implanted medicines of penicillins according to claim 3 is characterized in that the preferable weight proportion of each raw material components is:
A, penicillin medicine 55～85%
Biodegradation chemical compound 15～45%
Or
B, penicillin medicine 60～90%
Polylactic acid 10～40%
8, a kind of slowly releasing implanted medicines of penicillins according to claim 3 is characterized in that the preferable weight proportion of each raw material components is:
A, penicillin medicine 50～80%
Chitin 20～45%
High fatty alcohol 0～5%
Or
B, penicillin medicine 30～80%
Gelatin 15～60%
High fatty alcohol 5～20%
Or
C, penicillin medicine 30～70%
Glucosan 25～65%
Sea bath acid sodium 5～10%
Or
D, penicillin medicine 30～80%
Polyethylene Glycol 18～65%
High fatty alcohol 2～10%
E, penicillin medicine 60～90%
Polylactic acid 10～35%
Porogen 0～5%
9, a kind of preparation method of slowly releasing implanted medicines of penicillins is characterized in that by proportioning each component mix homogeneously is inserted melt molding in the mould, cooling and demolding.
10, a kind of preparation method of slowly releasing implanted medicines of penicillins is characterized in that in solvent, with each component mix homogeneously, inserts die for molding by proportioning, removes the back depanning of desolvating.
11, a kind of preparation method of slowly releasing implanted medicines of penicillins is characterized in that preparation medicine microspheres earlier, after film, then by proportioning combination forming in mould.
12, a kind of preparation method of slowly releasing implanted medicines of penicillins is characterized in that by proportioning with each component mix homogeneously, in die for molding.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN97107072A CN1112177C (en) | 1997-08-15 | 1997-08-15 | Slowly releasing implanted medicines of penicillins and preparation thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN97107072A CN1112177C (en) | 1997-08-15 | 1997-08-15 | Slowly releasing implanted medicines of penicillins and preparation thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1201665A true CN1201665A (en) | 1998-12-16 |
| CN1112177C CN1112177C (en) | 2003-06-25 |
Family
ID=5169261
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN97107072A Expired - Lifetime CN1112177C (en) | 1997-08-15 | 1997-08-15 | Slowly releasing implanted medicines of penicillins and preparation thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1112177C (en) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL78826A (en) * | 1986-05-19 | 1991-05-12 | Yissum Res Dev Co | Precursor composition for the preparation of a biodegradable implant for the sustained release of an active material and such implants prepared therefrom |
| CN1040840C (en) * | 1993-02-22 | 1998-11-25 | 唐山市骨科医院 | Embedding agent and manufacturing method |
-
1997
- 1997-08-15 CN CN97107072A patent/CN1112177C/en not_active Expired - Lifetime
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| Publication number | Publication date |
|---|---|
| CN1112177C (en) | 2003-06-25 |
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Effective date of registration: 20161108 Address after: Daoxiang road Hefei city Shushan new industrial park of Anhui Province, No. 9 building 230088 Patentee after: Hefei China Science and Technology Co., Ltd. Address before: 307, room 193, electronic city, No. 230001, Tunxi Road, Hefei, Anhui Patentee before: Zhongren Science and Technology Co., Ltd., Anhui Prov. |
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Granted publication date: 20030625 |
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