CN114557981A - Montelukast oral cavity dissolving film agent and preparation process thereof - Google Patents
Montelukast oral cavity dissolving film agent and preparation process thereof Download PDFInfo
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Abstract
The invention relates to a montelukast sodium oral cavity membrane dissolving agent and a preparation process thereof. The formula and the preparation process can improve the stability and the elution rate of the medicine, have good taste test, and can be applied to clinical experiments to further expand the production.
Description
Technical Field
The invention belongs to the field of pharmaceutical preparations, and particularly relates to a montelukast sodium oral cavity membrane dissolving agent and a preparation process thereof.
Background
Montelukast sodium is a leukotriene regulator developed and marketed by the moendong company, and is widely applied to prevention and long-term treatment of bronchial asthma, exercise-induced asthma and allergic rhinitis, particularly pediatric respiratory diseases. Is the only long-acting control drug which can be independently applied in recent years at home and abroad except inhalation hormone for treating asthma.
Montelukast sodium is a potent and selective leukotriene D4 receptor antagonist, and can selectively inhibit the increase of inflammatory factor leukotriene polypeptide caused by various stimulus factors (sulfur dioxide, sports, cold air, etc.) and various allergens (pollen, hair debris, etc.), thereby inhibiting the inflammatory response of the immediate phase and the delayed phase, and reducing or preventing a series of airway responses (bronchoconstriction, mucus secretion, increase of vascular permeability and eosinophilic granulocyte aggregation).
Regarding oral cavity dissolving films, there are also reports related to the prior art:
CN201210026670.1 discloses a fast-dissolving and stable oral montelukast sodium solid preparation and a preparation method thereof, wherein the preparation takes montelukast sodium as a raw material medicine, is matched with auxiliary materials such as a diluent, a disintegrating agent, an additive, an adhesive, a lubricant and the like, and adopts a pharmaceutically acceptable preparation process. The formula and the preparation process can improve the dissolution rate of the oral preparation, remarkably improve the dissolution rate of the oral preparation in dissolution media with pH1.0 and pH4.5, and improve the stability of the medicine.
Disclosure of Invention
The invention provides a montelukast oral cavity membrane dissolving agent and a preparation process thereof. The oral film dissolving agent has high elution rate, can quickly play a role, and has good compliance in taste test.
Specifically, the invention is realized by the following steps:
the oral cavity dissolving film agent of the montelukast sodium comprises the following components:
the film forming material is one or a mixture of more than two of polyvinyl alcohol, polyvinylpyrrolidone, polyethylene glycol polyvinyl acetate, polyvinyl acetate phthalate, polymethacrylate polymer, polyacrylic acid and glycerin monostearate.
Further preferably, the film-forming material is selected from polyvinyl alcohol and glycerol monostearate.
Calculated by weight ratio, the ratio of the polyvinyl alcohol to the glycerin monostearate is 1: 0.2-0.8.
The plasticizer is selected from one or two of dimethyl phthalate, glycerol triacetate, glycerol, propylene glycol, sorbitol, mannitol, dextran, carbomer and guar gum.
Preferably, the plasticizer is selected from the group consisting of a mixture of glycerin and carbomer.
The mixing ratio of the glycerol and the carbomer is 1:0.5-1.5 calculated by weight ratio.
The sweetener is one or more selected from aspartame, stevioside, aspartame, acesulfame, neotame and sucralose.
The sweetener is selected from stevioside and sucralose at a weight ratio of 3: 0.5-1.5.
The filler is one or more selected from lactose, dextrin, calcium sulfate, sucrose, cellulose, glucose, pregelatinized starch, microcrystalline cellulose, starch, mannitol, calcium sulfate and calcium hydrogen phosphate.
The disintegrant is selected from one or more of poloxamer, sodium carboxymethyl starch, cross-linked polyvinylpyrrolidone, cross-linked sodium carboxymethyl cellulose and low-substituted hydroxypropyl cellulose.
The second purpose of the invention is to provide a preparation method of montelukast oral film agent, which comprises the following steps:
1) preparing slurry: adding the film-forming material into a 10% ethanol water solution under stirring, fully stirring and dissolving to obtain polymer gel; dissolving montelukast sodium in 20% of alkaline (pH value is 7.5-8.0) buffer solution, stirring uniformly to obtain a medicine-containing solution, sequentially adding a filling agent, a disintegrating agent, a plasticizer and a flavoring agent, and stirring uniformly; then adding the polymer gel into the solution, and uniformly mixing to obtain a montelukast sodium polymer gel solution;
2) film preparation: coating the montelukast sodium polymer gel solution on a plastic film in a blade mode, setting the coating thickness to be 80-200 mu m and the coating speed to be 6-10cm/min, and coating the slurry on a backing material;
3) and (3) drying: heating and drying at 50-70 deg.C;
4) uncovering the film: peeling the film agent from the plastic film, cutting into a certain size, sealing and packaging to obtain the plastic film.
Compared with the prior art, the invention achieves unexpected technical effects
The preparation method of the montelukast sodium preparation comprises the steps of dissolving the montelukast sodium preparation in an alkaline (pH value is 7.5-8.0) buffer solution, screening a film forming material and a plasticizer, optimizing the dosage, and obtaining the montelukast sodium preparation with high final stability and good elution effect. After the product of the invention is prepared, the taste is always difficult, and the screening of the sweetener and the screening of the dosage are adopted after the invention, and finally the most preferable result is obtained.
Drawings
FIG. 1: stability results for Montelukast oral cavity membrane dissolving agent film forming material selection
The impurities of month 0, month 3 and month 6 of example 1 were 0.18, 0.22 and 0.32 from bottom to top, respectively.
FIG. 2: elution rate results for montelukast oral cavity membrane dissolving agent film forming material selection
FIG. 3: stability results for Montelukast oral cavity membrane dissolving agent polyvinyl alcohol and glyceryl monostearate in no amount
FIG. 4: stability results for Montelukast oral film dissolving agent Glycerol and carbomer No amounts
FIG. 5: elution Rate results for Montelukast oral Membrane Agents polyvinyl alcohol and Glycerol monostearate No amount
FIG. 6: elution rate results for Montelukast oral cavity membrane dissolving agent glycerol and carbomer without dosage
FIG. 7: elution results of Montelukast oral cavity membrane dissolving agent plasticizer
FIG. 8: disintegration time limit of different plasticizers of montelukast oral cavity dissolving agent
FIG. 9: montelukast oral cavity dissolving agent taste scoring detection result
Detailed Description
In order to make the purpose and technical solution of the present invention more clear, the present invention is further described with reference to the following examples, but the scope of the present invention is not limited to these examples, and the examples are only used for explaining the present invention. It will be understood by those skilled in the art that various changes may be made and equivalents may be substituted without departing from the true scope of the invention.
Example 1: a preparation process of a montelukast oral cavity dissolving film agent comprises the following auxiliary materials and steps:
the preparation process comprises the following steps:
preparing slurry: adding the film-forming material into a 10% ethanol water solution under stirring, fully stirring and dissolving to obtain polymer gel; dissolving montelukast sodium in 20% of alkaline (pH value is 7.5-8.0) buffer solution, stirring uniformly to obtain a medicine-containing solution, sequentially adding a filling agent, a disintegrating agent, a plasticizer and a sweetening agent, and stirring uniformly; then adding the polymer gel into the solution, and uniformly mixing to obtain a montelukast sodium polymer gel solution;
film preparation: coating the montelukast sodium polymer gel solution on a plastic film in a blade mode, setting the coating thickness to be 100 mu m and the coating speed to be 6cm/min, and coating the slurry on a backing material;
and (3) drying: heating and drying at 50-70 deg.C; drying to water content of 3-6%.
Uncovering the film: peeling the film agent from the plastic film, cutting into a certain size, sealing and packaging to obtain the plastic film.
Index detection
1. The stability results show that: examples the stability of the test substance (according to the test method for the substance in montelukast sodium chewable tablet standard) was evaluated at month 0, month 3 and month 6 of the accelerated test. See fig. 1.
2. The elution rate results show that: for the dissolution experiment at ph1.2, there was no significant difference in elution rate between examples 1-3 and comparative examples 1-3, as well as the commercially available montelukast sodium film. As shown in fig. 2.
As can be seen from fig. 1 and 2, a single commonly used film-forming material, such as polyvinyl alcohol, has a stability and elution that hardly meet the pharmacopoeial standards, and after using an effective combination, especially after using polyvinyl alcohol and glyceryl monostearate in combination, the stability is significantly improved and the elution rate is also significantly better than that of the single-weight type film-forming material.
Example 2: a preparation process of a montelukast oral cavity dissolving film agent comprises the following auxiliary materials and steps:
the preparation process comprises the following steps:
preparing slurry: adding the film-forming material into a 10% ethanol water solution under stirring, fully stirring and dissolving to obtain polymer gel; dissolving montelukast sodium in 20% alkaline (pH value of 7.5-8.0) buffer solution, stirring to obtain medicinal solution, sequentially adding lactose, stevioside, sucralose, poloxamer glycerol and carbomer, and stirring; then adding the polymer gel into the solution, and uniformly mixing to obtain a montelukast sodium polymer gel solution;
film preparation: coating the montelukast sodium polymer gel solution on a plastic film in a blade mode, setting the coating thickness to be 100 mu m and the coating speed to be 6cm/min, and coating the slurry on a backing material;
and (3) drying: heating and drying at 50-70 deg.C; drying to water content of 3-6%.
Uncovering the film: peeling the film agent from the plastic film, cutting into a certain size, sealing and packaging to obtain the plastic film.
(1) The elution rate results show that: dissolution experiments were carried out at pH1.2 for examples 1-3 and comparative examples 1-3, as shown in FIG. 7. On the basis of the polyvinyl alcohol and glyceryl monostearate and the determination of the amount, the selection of the plasticizer is selected and the effect of the elution rate of not all the plasticizers is found to be good, and it can be seen that the elution rate of the combination of glycerin and carbomer is preferably more than 95% at 5 min.
(2) Disintegration time limit: according to the orally disintegrating tablet standard, see in particular figure 8.
Example 3: a preparation process of a montelukast oral cavity dissolving film agent comprises the following auxiliary materials and steps:
the preparation process comprises the following steps:
preparing slurry: adding the film-forming material into a 10% ethanol water solution under stirring, fully stirring and dissolving to obtain polymer gel; dissolving montelukast sodium in 20% alkaline (pH 7.5-8.0) buffer solution, stirring to obtain medicinal solution, sequentially adding lactose, stevioside, sucralose, poloxamer glycerol and carbomer, and stirring; then adding the polymer gel into the solution, and uniformly mixing to obtain a montelukast sodium polymer gel solution;
film preparation: coating the montelukast sodium polymer gel solution on a plastic film in a blade mode, setting the coating thickness to be 100 mu m and the coating speed to be 6cm/min, and coating the slurry on a backing material;
and (3) drying: heating and drying at 50-70 deg.C; drying to water content of 3-6%.
Uncovering the film: peeling the film agent from the plastic film, cutting into a certain size, sealing and packaging to obtain the plastic film.
Index detection
1. The stability results show that: examples the stability of the test substance (according to the test method for the substance in montelukast sodium chewable tablet standard) was evaluated at month 0, month 3 and month 6 of the accelerated test. See fig. 3.
2. The elution rate results show that: dissolution experiments were carried out at pH1.2, and there was no significant difference in elution rates between examples 1-3 and comparative examples 1-3, as well as between commercially available montelukast sodium films. As shown in fig. 5.
As can be seen from fig. 3 and 5, the amount of the selected material is selected based on the selection of the film forming material, and it is found that the same technical effect can be obtained without any mixing ratio.
Example 4: a preparation process of a montelukast oral cavity dissolving film agent comprises the following auxiliary materials and steps:
the preparation process comprises the following steps:
preparing slurry: adding polyvinyl alcohol and glyceryl monostearate into 10% ethanol water solution under stirring, and dissolving to obtain polymer gel; dissolving montelukast sodium in 20% alkaline (pH 7.5-8.0) buffer solution, stirring to obtain medicinal solution, sequentially adding lactose, stevioside, sucralose, poloxamer glycerol and carbomer, and stirring; then adding the polymer gel into the solution, and uniformly mixing to obtain a montelukast sodium polymer gel solution;
film preparation: coating the montelukast sodium polymer gel solution on a plastic film in a blade mode, setting the coating thickness to be 100 mu m and the coating speed to be 6cm/min, and coating the slurry on a backing material;
and (3) drying: heating and drying at 50-70 deg.C; drying to water content of 3-6%.
Uncovering the film: peeling the film agent from the plastic film, cutting into a certain size, sealing and packaging to obtain the plastic film.
Index detection
1. The stability results show that: EXAMPLES the stability of the accelerated test was evaluated by testing the substances at 0, 3 and 6 months in accordance with the substance test method of Montelukast sodium chewable tablet standards. See in particular fig. 4.
2. The elution rate results show that: for the dissolution experiment at ph1.2, there was no significant difference in elution rate between examples 1-3 and comparative examples 1-3, as well as the commercially available montelukast sodium film. As shown in fig. 6.
As can be seen from fig. 4 and 6, it is found that the same technical effect can be obtained without any mixing ratio based on the selection and the determination of the amount of the plasticizer and the film-forming material. As a result, it was found that glycerin and carbomer can exert stabilizing and eluting effects within a certain ratio range.
Example 4: a preparation process of a montelukast oral cavity dissolving film agent comprises the following auxiliary materials and steps:
the preparation process comprises the following steps:
preparing slurry: adding polyvinyl alcohol and glyceryl monostearate into 10% ethanol water solution under stirring, and dissolving to obtain polymer gel; dissolving montelukast sodium in 20% alkaline (pH 7.5-8.0) buffer solution, stirring to obtain medicinal solution, sequentially adding lactose, stevioside, sucralose, poloxamer glycerol and carbomer, and stirring; then adding the polymer gel into the solution, and uniformly mixing to obtain a montelukast sodium polymer gel solution;
film preparation: coating the montelukast sodium polymer gel solution on a plastic film in a blade mode, setting the coating thickness to be 100 mu m and the coating speed to be 6cm/min, and coating the slurry on a backing material;
and (3) drying: heating and drying at 50-70 deg.C; drying to water content of 3-6%.
Uncovering the film: peeling the film agent from the plastic film, cutting into a certain size, sealing and packaging to obtain the plastic film.
Index detection:
taste evaluation criteria
And (4) evaluating the mouthfeel, namely extracting 5 persons of department departments immediately, and grading and evaluating the mouthfeel after 1 minute, wherein the detailed picture is shown in fig. 9.
Claims (10)
1. The oral cavity dissolving film agent of montelukast sodium is characterized by comprising the following components:
2. the oral cavity membrane dissolving agent according to claim 1, wherein the film forming material is one or two selected from the group consisting of polyvinyl alcohol, polyvinylpyrrolidone, polyethylene glycol polyvinyl acetate, polyvinyl acetate phthalate, polymethacrylate, a polymer of polymethacrylate, polyacrylic acid, glyceryl monostearate; further preferably, the film-forming material is selected from polyvinyl alcohol and glycerol monostearate.
3. The oral film dissolving agent of claim 2, wherein the ratio of the polyvinyl alcohol to the glyceryl monostearate is 1:0.2-0.8 by weight.
4. The oral film dissolving agent of claim 1, wherein the plasticizer is one or two selected from the group consisting of dimethyl phthalate, phthalic acid ester, triacetin, glycerin, propylene glycol, sorbitol, mannitol, dextran, carbomer, and guar gum, and preferably the plasticizer is a mixture of glycerin and carbomer.
5. The orally dissolving film formulation according to claim 4, wherein the ratio of the glycerin to the carbomer is 1:0.5 to 1.5, calculated as a weight ratio.
6. The oral film dissolving agent according to claim 1, wherein the sweetener is one or more selected from aspartame, stevioside, aspartame, acesulfame-k, neotame and sucralose.
7. The oral film dissolving agent of claim 6, wherein the sweetener is selected from stevioside and sucralose at a weight ratio of 3: 0.5-1.5.
8. The oral film dissolving agent according to claim 1, wherein the filler is one or more selected from lactose, dextrin, calcium sulfate, sucrose, cellulose, glucose, pregelatinized starch, microcrystalline cellulose, starch, mannitol, calcium sulfate and calcium hydrogen phosphate.
9. The orally disintegrating film of claim 1, wherein the disintegrating agent is selected from one or more of poloxamer, sodium carboxymethyl starch, crospovidone, croscarmellose sodium, and low substituted hydroxypropyl cellulose.
10. A method of preparing an orally dissolving film of any one of claims 1 to 9, comprising:
1) preparing slurry: adding the film-forming material into a 10% ethanol water solution under stirring, fully stirring and dissolving to obtain polymer gel; dissolving montelukast sodium in 20% of alkaline (pH value is 7.5-8.0) buffer solution, stirring uniformly to obtain a medicine-containing solution, sequentially adding a filling agent, a disintegrating agent, a plasticizer and a flavoring agent, and stirring uniformly; then adding the polymer gel into the solution, and uniformly mixing to obtain a montelukast sodium polymer gel solution;
2) film preparation: coating the montelukast sodium polymer gel solution on a plastic film in a blade mode, setting the coating thickness to be 80-200 mu m and the coating speed to be 6-10cm/min, and coating the slurry on a backing material;
3) and (3) drying: heating and drying at 50-70 deg.C;
4) uncovering the film: peeling the film agent from the plastic film, cutting into a certain size, sealing and packaging to obtain the plastic film.
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| CN202210197274.9A CN114557981A (en) | 2022-03-02 | 2022-03-02 | Montelukast oral cavity dissolving film agent and preparation process thereof |
| CN202310024275.8A CN115969820B (en) | 2022-03-02 | 2023-01-09 | Montelukast sodium oral film agent and preparation process thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN115969820A (en) * | 2022-03-02 | 2023-04-18 | 山东新时代药业有限公司 | Montelukast oral cavity dissolving film agent and preparation process thereof |
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| US20220047504A1 (en) * | 2020-05-27 | 2022-02-17 | Cure Pharmaceutical Holding Corp. | Oral dissolvable film with pores extending therethrough |
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| KR101074271B1 (en) * | 2009-06-25 | 2011-10-17 | (주)차바이오앤디오스텍 | Fast dissolving oral dosage form containing steviosides as a taste masking agent |
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| CN114557981A (en) * | 2022-03-02 | 2022-05-31 | 山东新时代药业有限公司 | Montelukast oral cavity dissolving film agent and preparation process thereof |
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- 2022-03-02 CN CN202210197274.9A patent/CN114557981A/en active Pending
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115969820A (en) * | 2022-03-02 | 2023-04-18 | 山东新时代药业有限公司 | Montelukast oral cavity dissolving film agent and preparation process thereof |
| CN115969820B (en) * | 2022-03-02 | 2023-08-04 | 山东新时代药业有限公司 | Montelukast sodium oral film agent and preparation process thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN115969820A (en) | 2023-04-18 |
| CN115969820B (en) | 2023-08-04 |
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