CN1557330A - Sustained release medication of clindamycinum - Google Patents
Sustained release medication of clindamycinum Download PDFInfo
- Publication number
- CN1557330A CN1557330A CNA200410002371XA CN200410002371A CN1557330A CN 1557330 A CN1557330 A CN 1557330A CN A200410002371X A CNA200410002371X A CN A200410002371XA CN 200410002371 A CN200410002371 A CN 200410002371A CN 1557330 A CN1557330 A CN 1557330A
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- Prior art keywords
- clindamycin
- slow releasing
- cellulose
- preparation
- adjuvant
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Abstract
The present invention relates to one kind of special preparation form of antiseptic Clindamycin, delayed releasing Clindamycin preparation. The Clindamycin preparation contains Clindamycin 1-80 wt%, supplementary material with the delayed releasing effect 1-90 wt%, and other supplementary material. The present invention can maintain the effective and smooth blood medicine concentration in long time, raised curative effect and good patient compliance.
Description
Technical fieldThe invention belongs to medical technical field, relate to a kind of novel form of antibiotic medicine clindamycin, is the slow releasing preparation of clindamycin specifically.
Background technologyClindamycin claims clindamycin, Clindamicin again, chemistry 6-by name (1-methyl-anti--4-propyl group-L-2-pyrrolidine formyl amino)-1-sulfo--7 (S)-chloro-6,7, the hot pyranoside of 8-three deoxidations-L-Su Shi-a-D-gala, its prodrug Clindamycin Hydrochloride commonly used, clindamycin phosphate, clindamycin hydrochloride palmitate etc. on the medicine, clindamycin is a kind of broad-spectrum antiseptic antibiotic medicine commonly used, especially the myelitic first-selected medicine of staphylococcus aureus.Drug half-life was at 2.4～5 hours in vivo but existing clindamycin oral formulations is owing to it, and effective blood medicine time is shorter, need take medicine every day 3～4 times, and gastrointestinal tract is had certain side reaction.
The existing peroral dosage form of clindamycin has dosage forms such as conventional tablet, capsule, does not see as yet both at home and abroad about the report of its slow releasing preparation and documents and materials etc.
Summary of the inventionThe clindamycin slow releasing preparation that the purpose of this invention is to provide a kind of blood drug level of can remaining valid the long period, minimizing medicining times.
In order to reach purpose of the present invention, preparation of the present invention contains following component by weight percentage:
Clindamycin 1～80%
Play the adjuvant 1～90% of slow releasing function
Other adjuvant surplus.
Clindamycin in the preparation of the present invention comprises Clindamycin Hydrochloride, clindamycin phosphate, clindamycin hydrochloride palmitate etc.
The adjuvant that plays slow releasing function is a hydroxypropyl emthylcellulose, hydroxypropylmethyl cellulose phthalate, methylcellulose, ethyl cellulose, hydroxy methocel, hydroxyethyl-cellulose, hydroxypropyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose, microcrystalline Cellulose, acrylic resin, polymethyl methacrylate, crospolyvinylpyrrolidone, sodium alginate, calcium alginate, carbomer, polyvinyl alcohol, Polyethylene Glycol, stearic acid, in the chitosan one or more; The adjuvant of above-described slow-release material comprises its various models or specification etc., as hydroxypropyl emthylcellulose K
4M, K
15M, E
50Deng; And the combination of different model or specification etc.
This preparation comprises with the slow releasing preparation of above-mentioned slow-release material as the various structures of skeleton, film chamber, gel, porous matrix type, comprises that also making microcapsule earlier makes preparation again, and these all are that those skilled in the art are familiar with known.These structures can make medicine discharge gradually, thereby have slow-releasing and controlled-releasing action and high bioavailability preferably, especially can keep comparatively ideal drug release rate.
Other adjuvant of slow releasing preparation of the present invention is one or more in the relevant pharmaceutic adjuvants such as diluent, disintegrating agent, porogen, wet adhesive, lubricant, solvent, stabilizing agent.These pharmaceutic adjuvants all are that those skilled in the art are familiar with known, the following material of the optional usefulness of diluent but be not limited to following material for example, as select in lactose, sucrose, mannitol, dextran, sorbitol, starch, pregelatinized Starch, dextrin, calcium sulfate, calcium hydrogen phosphate, the microcrystalline Cellulose one or more for use; Wet adhesive is selected one or more in polyvinylpyrrolidone, hydroxypropyl emthylcellulose, starch slurry, syrup, water, the ethanol for use; Lubricant is selected one or more in stearic acid, magnesium stearate, calcium stearate, Pulvis Talci, silicon dioxide, micropowder silica gel, Polyethylene Glycol, Stepanol MG, the sodium lauryl sulphate for use, or the like.
The dosage form of slow releasing preparation of the present invention comprises tablet, capsule, granule, pill etc.Also have, the solid sustained-release preparation that the utilization coating is made, also scalable release rate of drugs, tablet, capsule, granule, pill all can adopt coating method that pharmaceutical pack is rolled in the purpose that reaches slow release in the certain thickness clothing film, and coating material can be selected for use in the adjuvant that plays slow releasing function.
Advantage of the present invention be can the long period keep blood drug level, lasting medicine is stablized, is avoided blood medicine " peak valley " phenomenon, reduces medicining times, easy to use, good patient compliance, and the side reaction of medicine is less.
The specific embodimentCome clindamycin slow releasing preparation of the present invention done further specifying by the following examples, but do not represent the embodiment limitation of the present invention.
Embodiment 1.
Prescription: composition weight percent content
Clindamycin Hydrochloride 33%
Hydroxypropyl emthylcellulose (K
4M) 45%
Lactose 21.2%
Magnesium stearate 0.8%
Water is an amount of
Preparation method: behind Clindamycin Hydrochloride, hydroxypropyl emthylcellulose, lactose water wet granulation, granulate, add the magnesium stearate mixing, the control tablet weight, tabletting promptly gets the Clindamycin Hydrochloride slow releasing tablet.
Hydroxypropyl emthylcellulose is a hydrophilic polymer, as framework material, meets the expansion of water or Digestive system and forms the gel barrier in said preparation, and the diffusion of control Clindamycin Hydrochloride is to play the effect of slow release.Hydroxypropyl emthylcellulose (K wherein
4M) can be by not commensurability hydroxypropyl emthylcellulose (K
100LV), hydroxypropyl emthylcellulose (K
15MOr K
100M) or the carbomer replacement, use also capable of being combined is to adjust the drug release rate curve.
Embodiment 2.
Prescription: composition weight percent content
Clindamycin phosphate 40%
Sodium alginate 35%
Calcium alginate 5%
Lactose 19%
Magnesium stearate 1%
Water (or ethanol water) is an amount of
Preparation method: with clindamycin phosphate, sodium alginate, calcium alginate, the abundant mix homogeneously of lactose, add suitable quantity of water (or ethanol water) and make soft material, the back oven dry of granulating, granulate adds the magnesium stearate mixing, the control tablet weight, tabletting is promptly.Also can behind granulation, drying, granulate, granule be added in the Capsules, promptly make the clindamycin phosphate slow releasing capsule.
Embodiment 3.
Prescription: composition weight percent content
Clindamycin Hydrochloride 32%
Hydroxypropyl emthylcellulose (K
15M) 10%
Ethyl cellulose 5%
Sorbitol is an amount of
Microcrystalline Cellulose 20%
Pulvis Talci 1.5%
10% polyvinylpyrrolidone aqueous solution an amount of (in polyvinylpyrrolidone)
Preparation method: with Clindamycin Hydrochloride, hydroxypropyl emthylcellulose, ethyl cellulose, sorbitol, microcrystalline Cellulose mix homogeneously,, add the Pulvis Talci mixing behind the granulate with polyvinylpyrrolidone wet granulation, oven dry, the control tablet weight, tabletting is promptly.
Embodiment 4.
Prescription: composition weight percent content
Clindamycin hydrochloride palmitate 48%
Ethyl cellulose and stearic acid 20%
Microcrystalline Cellulose and dehydrated alcohol 10%
Stearic acid 15%
Pulvis Talci 6%
Magnesium stearate 1%
Preparation method is similar to the front.Stearic acid in vivo gradually corrosion make the principal agent clindamycin hydrochloride palmitate discharge slow releasing function gradually, ethyl cellulose is a not corrosion framework material, treats can excrete after principal agent has discharged.
Embodiment 5.
Prescription: composition weight percent content
Clindamycin phosphate 20%
Acrylic resin 18%
Lactose 20%
Starch 20%
Microcrystalline Cellulose 20%
Micropowder silica gel 2%
Preparation method: with clindamycin phosphate, acrylic resin, lactose mix homogeneously, the starch slurry with 8% is a binding agent, and above-mentioned material is made soft material, wet granulation, oven dry, add microcrystalline Cellulose and micropowder silica gel mixing behind the granulate, the control tablet weight, tabletting is promptly.
Embodiment 6.
Prescription: composition weight percent content
Clindamycin Hydrochloride 32%
Hydroxypropyl emthylcellulose (K
4M) 40%
Lactose is an amount of
1% carbomer alcoholic solution an amount of (in carbomer)
Magnesium stearate 1%
Pulvis Talci 1%
Preparation method: with Clindamycin Hydrochloride, hydroxypropyl emthylcellulose, lactose mix homogeneously, make soft material with 1% carbomer alcoholic solution, wet granulation, oven dry add magnesium stearate and Pulvis Talci mixing behind the granulate, the control tablet weight, and tabletting is promptly.
Embodiment 7. clindamycin coated slow release sheets
Prescription: composition weight percent content
The sheet core is confused: Clindamycin Hydrochloride 50%
Polyvinylpyrrolidone 3%
Lactose 27%
Water is an amount of
Lubricant 20%
The coating part: acrylic resin is an amount of
10% polyvinylpyrrolidone alcoholic solution is an amount of
Preparation method: with Clindamycin Hydrochloride, polyvinylpyrrolidone, lactose mix homogeneously, water is made soft material with above-mentioned material, and wet granulation, oven dry add lubricant behind the granulate, the control tablet weight, and tabletting is made label.
Get acrylic resin and 10% polyvinylpyrrolidone alcoholic solution is an amount of, its dissolving as coating solution, is promptly got clindamycin coated slow release sheet to the label coating.
Acrylic resin is the undissolved clothing membrane material of gastrointestinal tract, adds an amount of polyvinylpyrrolidone as porogen in coating solution, dissolving in Digestive system and make and occur micropore on the clothing film, and medicine discharges from micropore, reaches the effect of slow release.
Claims (5)
1. clindamycin slow releasing preparation is characterized in that containing by weight percentage following composition:
Clindamycin 1～80%
Play the adjuvant 1～90% of slow releasing function
Other adjuvant surplus.
2. clindamycin slow releasing preparation according to claim 1, the adjuvant that it is characterized in that slow releasing function is a hydroxypropyl emthylcellulose, hydroxypropylmethyl cellulose phthalate, methylcellulose, ethyl cellulose, hydroxy methocel, hydroxyethyl-cellulose, hydroxypropyl cellulose, carboxymethyl cellulose, carboxyethyl cellulose, microcrystalline Cellulose, acrylic resin, polymethyl methacrylate, crospolyvinylpyrrolidone, sodium alginate, calcium alginate, carbomer, polyvinyl alcohol, Polyethylene Glycol, stearic acid, in the chitosan one or more.
3. clindamycin slow releasing preparation according to claim 1 is characterized in that other adjuvant is one or more in the relevant pharmaceutic adjuvants such as diluent, disintegrating agent, porogen, wet adhesive, lubricant, solvent, stabilizing agent.
4. clindamycin slow releasing preparation according to claim 1 is characterized in that the dosage form of preparation comprises tablet, capsule, granule, pill and their coated slow release preparation thereof.
5. according to any one described clindamycin slow releasing preparation in the claim 1 to 4, it is characterized in that clindamycin comprises Clindamycin Hydrochloride, clindamycin phosphate, clindamycin hydrochloride palmitate.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200410002371XA CN1557330A (en) | 2004-01-12 | 2004-01-12 | Sustained release medication of clindamycinum |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA200410002371XA CN1557330A (en) | 2004-01-12 | 2004-01-12 | Sustained release medication of clindamycinum |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1557330A true CN1557330A (en) | 2004-12-29 |
Family
ID=34350714
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA200410002371XA Pending CN1557330A (en) | 2004-01-12 | 2004-01-12 | Sustained release medication of clindamycinum |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1557330A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101401814B (en) * | 2008-11-06 | 2011-06-15 | 张宏宇 | Clindamycin phosphate oral patches |
| CN101744833B (en) * | 2008-12-02 | 2012-05-23 | 济南宏瑞创博医药科技开发有限公司 | Medicinal composition for treating bacterial vaginitis |
| CN107569473A (en) * | 2017-09-28 | 2018-01-12 | 南京易亨制药有限公司 | A kind of Sustained Release Ambroxol Hydrochloride Capsules and preparation method thereof |
| CN107595794A (en) * | 2017-03-21 | 2018-01-19 | 广州大光制药有限公司 | A kind of clindamycin hydrochloride palmitate particle and preparation method thereof |
-
2004
- 2004-01-12 CN CNA200410002371XA patent/CN1557330A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101401814B (en) * | 2008-11-06 | 2011-06-15 | 张宏宇 | Clindamycin phosphate oral patches |
| CN101744833B (en) * | 2008-12-02 | 2012-05-23 | 济南宏瑞创博医药科技开发有限公司 | Medicinal composition for treating bacterial vaginitis |
| CN107595794A (en) * | 2017-03-21 | 2018-01-19 | 广州大光制药有限公司 | A kind of clindamycin hydrochloride palmitate particle and preparation method thereof |
| CN107569473A (en) * | 2017-09-28 | 2018-01-12 | 南京易亨制药有限公司 | A kind of Sustained Release Ambroxol Hydrochloride Capsules and preparation method thereof |
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| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |