CN114681414A - Cefdinir dispersible tablet pharmaceutical composition and preparation process thereof - Google Patents
Cefdinir dispersible tablet pharmaceutical composition and preparation process thereof Download PDFInfo
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- CN114681414A CN114681414A CN202011575544.2A CN202011575544A CN114681414A CN 114681414 A CN114681414 A CN 114681414A CN 202011575544 A CN202011575544 A CN 202011575544A CN 114681414 A CN114681414 A CN 114681414A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/542—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with heterocyclic ring systems
- A61K31/545—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine
- A61K31/546—Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. cephalosporins, cefaclor, or cephalexine containing further heterocyclic rings, e.g. cephalothin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
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Abstract
The invention relates to an oral medicinal preparation of cefdinir dispersible tablets and a preparation method of the oral medicinal preparation. The composition is characterized by comprising the following components: 40-60 parts of cefdinir, 10-20 parts of lactose, 25-50 parts of microcrystalline cellulose, 2-5 parts of hydroxypropyl cellulose, 5-10 parts of carboxymethyl cellulose calcium, 1-5 parts of polyoxyl (40) stearate, 2-4 parts of orange powder essence, 3-10 parts of aspartame, 1-3 parts of silicon dioxide and 14.5-5 parts of magnesium stearate. The invention takes the carboxymethyl cellulose calcium with specific proportion as a disintegrating agent and magnesium stearate polyoxyl (40) ester with specific proportion as a surfactant, and the prepared cefdinir dispersible tablet has good disintegration time limit, preparation stability and dissolubility, and is equivalent to the quality of the original research.
Description
Technical Field
The invention relates to the technical field of medicinal preparations, in particular to a medicinal composition of cefdinir dispersible tablets and a preparation method thereof.
Technical Field
Cefdinir is oral third-generation cephalosporin, has the advantages of wide antibacterial spectrum, low toxicity and the like, and is a medicament widely applied clinically. At present, various cefdinir preparations are sold in the market at home, and mainly comprise dispersible tablets, capsules, granules and tablets. Since cefdinir is a BCS IV drug, its dissolution is a key factor for absorption in vivo. At present, the cefdinir preparation sold on the market has the defects of slow disintegration and dissolution, low bioavailability, poor stability and the like. Therefore, how to improve and improve the stability, disintegration property and dissolution property of cefdinir preparation, thereby improving the stability, onset time, in vivo bioavailability and the like of the preparation is a technical problem to be solved at present. The invention provides a cefdinir dispersible tablet and a preparation method thereof. The invention solves the problems of slow disintegration and dissolution of preparation samples, and has the advantages of good taste, good dissolution performance, good drug stability, simple process operation, good reproducibility and the like.
Disclosure of Invention
The invention provides a cefdinir dispersible tablet and a preparation method thereof. The preparation takes cefdinir as a main drug, has the particle size range of D90 being less than or equal to 60 mu m, contains at least two fillers, at least one disintegrant, at least one surfactant, at least one adhesive, at least two flavoring agents, at least one glidant and at least one lubricant, and is characterized by comprising the following components: the filler is microcrystalline cellulose and lactose
The disintegrating agent is: calcium carboxymethylcellulose
The surfactant is: polyoxyl (40) stearate
The adhesive is: hydroxypropyl cellulose
The flavoring agent is: aspartame and orange powder essence
The glidant is as follows: silicon dioxide
The lubricant is: magnesium stearate
The preparation method of the cefdinir dispersible tablet pharmaceutical composition comprises the following steps:
1) cefdinir, microcrystalline cellulose, lactose, hydroxypropyl cellulose, carboxymethylcellulose calcium, polyoxyl (40) stearate, aspartame and orange powder essence are weighed and mixed uniformly in a proper proportion, and a dry granulating machine is adopted for granulating, wherein the granulating pressure is 40-60bar, and the mesh number of the granules is 14.
2) The silicon dioxide and the magnesium stearate with the prescription amount and the granules are put into a three-dimensional mixer for total mixing.
3) The tablets were pressed with a 9mm round dimple punch.
Advantageous effects
The invention takes the carboxymethyl cellulose calcium with specific proportion as a disintegrating agent and magnesium stearate polyoxy (40) ester with specific proportion as a surfactant, and the prepared cefdinir dispersible tablet has good disintegration time limit, preparation stability and solubility, which are equivalent to the quality of the original research, and the specific reason analysis is as follows:
(1) the carboxymethyl cellulose calcium contains a chelating structure and a calcium structure, and has better hydrophilicity than the common sodium carboxymethyl starch; in addition, the calcium carboxymethyl cellulose has good compatibility with cefdinir;
(2) magnesium stearate polyoxy (40) ester is a nonionic surfactant, can effectively improve the solubility of cefdinir in water, and can be rapidly dispersed and dissolved out.
Drawings
FIG. 1 comparison of stability test results of examples 1 to 2 and comparative examples 1 to 3
FIG. 2 comparison of dissolution Curve examination results of examples 1-2 and comparative examples 1-3
Detailed Description
Example 1: preparation examples
Preparation process
1) Cefdinir, microcrystalline cellulose, lactose, hydroxypropyl cellulose, carboxymethylcellulose calcium, polyoxyl (40) stearate, aspartame and orange powder essence are weighed and mixed uniformly in a proper proportion, and a dry granulating machine is adopted for granulating, wherein the granulating pressure is 40-60bar, and the mesh number of the granules is 14.
2) The silicon dioxide and the magnesium stearate with the prescription amount and the granules are put into a three-dimensional mixer for total mixing.
3) The tablets were pressed with a 9mm round dimple punch.
Example 2: preparation examples
Preparation process
1) Cefdinir, microcrystalline cellulose, lactose, hydroxypropyl cellulose, carboxymethylcellulose calcium, polyoxyl (40) stearate, aspartame and orange powder essence are weighed and mixed uniformly in a proper proportion, and a dry granulating machine is adopted for granulating, wherein the granulating pressure is 40-60bar, and the mesh number of the granules is 14.
2) The silicon dioxide and the magnesium stearate with the prescription amount and the granules are put into a three-dimensional mixer for total mixing.
3) The tablets were pressed with a 9mm round dimple punch.
Comparative example 1: sodium carboxymethyl starch as disintegrant
Preparation examples
Preparation process
1) Cefdinir, microcrystalline cellulose, lactose, hydroxypropyl cellulose, carboxymethyl starch sodium, polyoxyl (40) stearate, aspartame and orange powder essence are weighed and mixed uniformly according to a proper proportion, and a dry granulating machine is adopted for granulating, wherein the granulating pressure is 40-60bar, and the mesh number of the granules is 14.
2) The silicon dioxide and the magnesium stearate with the prescription amount and the granules are put into a three-dimensional mixer for total mixing.
3) The tablets were pressed with a 9mm round dimple punch.
Comparative example 2: the formula does not contain polyoxyl (40) stearate
Preparation examples
Preparation process
1) Weighing cefdinir, microcrystalline cellulose, lactose, hydroxypropyl cellulose, calcium carboxymethylcellulose, aspartame and orange powder essence in a proper proportion, uniformly mixing, and granulating by adopting a dry granulator under the granulating pressure of 40-60bar and the granule mesh number of 14 meshes.
2) The silicon dioxide and the magnesium stearate with the prescription amount and the granules are put into a three-dimensional mixer for total mixing.
3) The tablets were pressed with a 9mm round dimple punch.
Comparative example 3: sodium dodecyl sulfate as surfactant
Preparation examples
Preparation process
1) Weighing cefdinir, microcrystalline cellulose, lactose, hydroxypropyl cellulose, carboxymethylcellulose calcium, sodium dodecyl sulfate, aspartame and orange powder essence in a proper proportion, uniformly mixing, and granulating by adopting a dry granulator with the granulating pressure of 40-60bar and the mesh number of 14 meshes.
2) The prescribed amount of silicon dioxide and magnesium stearate and the granules are put into a three-dimensional mixer for total mixing.
3) The tablets were pressed with a 9mm round dimple punch.
Samples of the embodiments 1-3 of the invention are taken, accelerated stability inspection is carried out after the samples are simulated for commercial package according to the preparation stability test guiding principle (9001 of the fourth part of the 2015 year edition of Chinese pharmacopoeia), and samples are taken at 0 month, 1 month, 3 months and 6 months after the samples are placed, and the appearance characters and the total impurities of the samples are inspected, and the results are shown in the attached table 1.
TABLE 1 comparison of stability findings
The result shows that the preparation stability is best when the calcium carboxymethylcellulose is used as the disintegrant in example 1, and the stability is not significantly different from that in example 1 when different amounts of calcium carboxymethylcellulose are used in example 2; in the comparative example 1, sodium carboxymethyl starch is used as a disintegrant, so that the total impurity growth is rapid, the stability of the preparation is poor, and in the formula of the comparative example 2, no surfactant is added, so that the stability is not obviously different from that of the example 1; comparative example 3 the stability of sodium dodecyl sulfate used as a surfactant was significantly inferior to that of example 1.
According to the dissolution and release determination method (the second method in 0931 of the four parts of the national pharmacopoeia 2015), using 900mL and 0.1mol/L hydrochloric acid as dissolution media and 50rpm as rotation speed, sampling 10mL at 5, 10, 15 and 30min respectively, and calculating the dissolution amount of each tablet by using an ultraviolet spectrophotometry according to the samples of the examples 1-2 and the comparative examples 1-3. According to the disintegration time limit inspection method (general rule 0921), the inner diameter of the sieve pore of the stainless steel screen is 710um, and the water temperature is 15-25 ℃.
TABLE 2 Dispersion homogeneity and dissolution Curve examination
The results show that the stearic acid polyoxyl (40) lipid is used as the surfactant and the carboxymethyl cellulose calcium is used as the disintegrant in the examples 1 and 2, so that the time consumption for dispersing uniformity is short, the dissolution release is fast, and the dispersion uniformity and the dissolution release have certain correlation with the dosage of the disintegrant. Comparative example 1 adopts carboxymethyl starch sodium as disintegrant, dissolution release is faster, dispersion uniformity time consumption is shorter and has no significant difference with carboxymethyl cellulose calcium, comparative example 3 adopts sodium dodecyl sulfate, comparative example 2 does not add surfactant, and dispersion uniformity and dissolution release are significantly slower than example 3.
Clinical bioequivalence results:
bioequivalence studies were conducted with the sample of example 1 and the reference formulation, and the results showed that cefdinir dispersible tablets (CDNDT) are bioequivalent to the reference formulation (Ref).
Claims (2)
1. The cefdinir dispersible tablet pharmaceutical composition is characterized by comprising the following components:
40-60 parts of cefdinir
10-20 parts of lactose
25-50 parts of microcrystalline cellulose
2-5 parts of hydroxypropyl cellulose
5-10 parts of carboxymethyl cellulose calcium
1-5 parts of polyoxyl (40) stearate
2-4 parts of orange powder essence
3-10 parts of aspartame
1-3 parts of silicon dioxide
1.5-5 parts of magnesium stearate
The particle size range D90 of the micronized cefdinir is controlled to be less than or equal to 60 mu m.
2. A process for preparing a pharmaceutical composition according to claim 1, comprising the steps of:
1) weighing cefdinir, microcrystalline cellulose, lactose, hydroxypropyl cellulose, carboxymethylcellulose calcium, polyoxyl (40) stearate, aspartame and orange powder essence in a proper proportion, uniformly mixing, and granulating by adopting a dry granulator under the granulating pressure of 40-60bar, wherein the mesh number of the granules is 14 meshes;
2) the silicon dioxide and the magnesium stearate with the prescription amount and the particles are put into a three-dimensional mixer for total mixing;
3) the tablets were pressed with a 9mm round dimple punch.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011575544.2A CN114681414A (en) | 2020-12-28 | 2020-12-28 | Cefdinir dispersible tablet pharmaceutical composition and preparation process thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202011575544.2A CN114681414A (en) | 2020-12-28 | 2020-12-28 | Cefdinir dispersible tablet pharmaceutical composition and preparation process thereof |
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| Publication Number | Publication Date |
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| CN114681414A true CN114681414A (en) | 2022-07-01 |
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| CN202011575544.2A Pending CN114681414A (en) | 2020-12-28 | 2020-12-28 | Cefdinir dispersible tablet pharmaceutical composition and preparation process thereof |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101352424A (en) * | 2008-09-16 | 2009-01-28 | 天津市中央药业有限公司 | Cefdinir dispersible tablet and preparation method thereof |
| EP2366379A1 (en) * | 2010-02-25 | 2011-09-21 | Sanovel Ilac Sanayi ve Ticaret A.S. | Cefdinir formulation with improved dissolution rate |
| WO2012060787A1 (en) * | 2010-11-05 | 2012-05-10 | Mahmut Bilgic | Oral dosage forms comprising cefdinir and carboxymethyl cellulose calcium |
| CN103110595A (en) * | 2012-12-31 | 2013-05-22 | 广东博洲药业有限公司 | Cefdinir dispersible tablet and preparation method thereof |
| CN103977009A (en) * | 2014-05-22 | 2014-08-13 | 常州市亚邦医药研究所有限公司 | Orally-taken medicinal composition containing cefdinir and preparation method thereof |
-
2020
- 2020-12-28 CN CN202011575544.2A patent/CN114681414A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101352424A (en) * | 2008-09-16 | 2009-01-28 | 天津市中央药业有限公司 | Cefdinir dispersible tablet and preparation method thereof |
| EP2366379A1 (en) * | 2010-02-25 | 2011-09-21 | Sanovel Ilac Sanayi ve Ticaret A.S. | Cefdinir formulation with improved dissolution rate |
| WO2012060787A1 (en) * | 2010-11-05 | 2012-05-10 | Mahmut Bilgic | Oral dosage forms comprising cefdinir and carboxymethyl cellulose calcium |
| CN103110595A (en) * | 2012-12-31 | 2013-05-22 | 广东博洲药业有限公司 | Cefdinir dispersible tablet and preparation method thereof |
| CN103977009A (en) * | 2014-05-22 | 2014-08-13 | 常州市亚邦医药研究所有限公司 | Orally-taken medicinal composition containing cefdinir and preparation method thereof |
Non-Patent Citations (1)
| Title |
|---|
| 康帅: "头孢地尼胶囊的处方工艺研究", 《河北工业科技》, vol. 29, no. 4, pages 208 - 210 * |
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