CN111035655A - Sodium phosphate composition and preparation method thereof - Google Patents
Sodium phosphate composition and preparation method thereof Download PDFInfo
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- CN111035655A CN111035655A CN201911360198.3A CN201911360198A CN111035655A CN 111035655 A CN111035655 A CN 111035655A CN 201911360198 A CN201911360198 A CN 201911360198A CN 111035655 A CN111035655 A CN 111035655A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/42—Phosphorus; Compounds thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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Abstract
The invention relates to a sodium phosphate composition, which is characterized by comprising the following components in parts by weight: each unit preparation contains 15g to 30g of sodium dihydrogen phosphate; 3 g-6 g of disodium hydrogen phosphate; 0.1-0.2 g of saccharin sodium, 0.01-0.03 g of lemon essence; 0.05g to 0.3g of dimeticone, 0.1g to 0.5g of silicon dioxide, 0.8g to 10g of glucose and 0.5g to 2.0g of cholestyramine resin; the invention also provides a preparation method of the sodium phosphate composition. The components of the invention have synergistic effect, and the finally prepared composition has stable property.
Description
Technical Field
The invention belongs to the field of pharmaceutical preparations, and particularly relates to a sodium phosphate composition for cleaning intestinal tracts.
Background
Sodium phosphate is used for cleaning the intestinal tract of a patient under colon X-ray and before intestinal endoscopy or operation, nonabsorbable negative and positive ions are dissociated from the sodium phosphate in the intestinal tract, a hypertonic environment is formed in the intestinal tract, water in the body enters the intestinal tract due to the property of a semipermeable membrane of the intestinal tract, and the water contained in the sodium phosphate and the water taken by the patient jointly generate mechanical stimulation to promote the movement of the intestinal tract. The sodium phosphate salt can increase the moisture in the intestinal tract and soften the stool, and can also activate the local nerve reflex of the intestinal mucosa layer to increase the peristalsis of the intestinal wall, improve the intestinal tract power and promote defecation.
Sodium phosphate is a high-quality drug for preparing intestinal tracts, and through years of clinical application in North America and all over the world, the safety, effectiveness, convenience and patient compliance of the drug are widely proved, and the sodium phosphate is the first brand drug for preparing intestinal tracts before surgical operation, colon X-ray and intestinal tract endoscopy in North America.
The western medicines include mannitol, magnesium sulfate, polyethylene glycol, etc. Wherein, mannitol and intestinal bacteria can generate hydrogen and methane, which are easy to cause explosion when the intestinal tract is treated by radio frequency, microwave and other electrical cautery, and currently, mannitol is forbidden to be used for cleaning the intestinal tract before surgical operation in European and American countries; magnesium sulfate has poor taste, and is easy to cause discomfort such as nausea, vomiting, abdominal pain, dehydration and the like when being taken by a plurality of patients; polyethylene glycol can achieve a good application effect, but a large dose of solution, usually 3-4 liters, must be taken at the same time, and the intestinal tract cleaning of a patient is seriously hindered.
Chinese patent CN 102232969B discloses a sodium phosphate composition and a preparation method thereof, wherein the composition comprises sodium dihydrogen phosphate, disodium hydrogen phosphate and simethicone; the composition has obvious clinical effect in cleaning the intestinal tract, excellent intestinal tract cleanliness, good patient tolerance and small water electrolyte disorder, but the composition adopts the sweetening agent and the essence to adjust the taste, but the taste of the solution is poor after the composition is prepared into the solution, and the patient can quickly release the product, so that the gastrointestinal tract irritation reaction of the product is stronger, the medication compliance of the patient is lower, and the stability of the product is poor.
The cholestyramine resin is anion exchange resin, has the functions of taste masking, stabilizing agent and slow release, is sold in most countries in Europe and America as an oral auxiliary material at present, has the safety proved to be a safe and nontoxic auxiliary material, and is widely applied to oral preparations.
The applicant finds that the taste of an aqueous solution of a product is remarkably improved, the stability of the product can be improved, the release of the product in the gastrointestinal tract can be obviously delayed, and the side effect of the product on the strong stimulation of the gastrointestinal tract can be reduced by adding cholestyramine resin on the basis of the existing sodium phosphate salt preparation through a large amount of tests and prescription screening in the process of developing the sodium phosphate salt preparation.
Disclosure of Invention
The invention provides a sodium phosphate composition, overcomes the defects and shortcomings in the background technology, and provides the sodium phosphate composition which has a good taste improvement effect, a better intestinal tract cleaning effect, can be slowly released, and has better product stability.
A sodium phosphate salt composition having the formula shown in table 1:
TABLE 1 ingredient Table of sodium phosphate salt composition
| Sodium dihydrogen phosphate | 15g～30g |
| Disodium hydrogen phosphate | 3g～6g |
| Dimethicone | 0.05g～0.3g |
| Silicon dioxide | 0.1g～0.5g |
| Saccharin sodium salt | 0.1g～0.2g |
| Glucose | 0.8g～10g |
| Lemon essence | 0.01g～0.03g |
| Cholestyramine resin | 0.5g～2.0g |
Wherein the sodium phosphate composition is prepared by the following method:
(1) firstly, crushing sodium dihydrogen phosphate, disodium hydrogen phosphate and saccharin sodium and sieving the crushed materials with a 80-mesh sieve;
(2) respectively weighing sodium dihydrogen phosphate, disodium hydrogen phosphate, dimeticone, cholestyramine resin and glucose according to the prescription amount, adding into a three-dimensional mixer, and fully mixing to uniformly mix;
(3) weighing silicon dioxide, saccharin sodium and lemon essence according to the prescription amount, adding into the three-dimensional mixer, and fully mixing to uniformly mix;
(4) subpackaging the mixed materials by using an aluminum-plastic composite film;
compared with the prior art, the invention has the advantages that: (1) the sodium dihydrogen phosphate, the disodium hydrogen phosphate and the saccharin sodium are crushed and sieved by a 80-mesh sieve, so that the mixing uniformity of the product can be well ensured; (2) adding cholestyramine resin, dimeticone and silicon dioxide into the product. The taste of the product after being prepared into solution can be well improved, the medication compliance of patients is increased, the quality stability of the product can be increased, the release of the product in the gastrointestinal tract is delayed, and the side effect of the product on the strong stimulation of the gastrointestinal tract is obviously improved.
Detailed Description
The present invention will be further described with reference to specific examples, but it should not be construed that the scope of the above-described subject matter of the present invention is limited to the examples. All the technologies realized based on the above contents of the present invention belong to the scope of the present invention. The auxiliary materials in the following examples can be replaced by the same type of pharmaceutically acceptable auxiliary materials, or reduced or increased.
Example 1
1. Prescription:
2. the process comprises the following steps:
(1) firstly, crushing sodium dihydrogen phosphate, disodium hydrogen phosphate and saccharin sodium and sieving the crushed materials with a 80-mesh sieve;
(2) respectively weighing sodium dihydrogen phosphate, disodium hydrogen phosphate, dimeticone, cholestyramine resin and glucose according to the prescription amount, adding into a three-dimensional mixer, and fully mixing to uniformly mix;
(3) weighing silicon dioxide, saccharin sodium and lemon essence according to the prescription amount, adding into the three-dimensional mixer, and fully mixing to uniformly mix;
(4) subpackaging the mixed materials by using an aluminum-plastic composite film;
example 2
1. Prescription:
2. the process comprises the following steps:
(1) firstly, crushing sodium dihydrogen phosphate, disodium hydrogen phosphate and saccharin sodium and sieving the crushed materials with a 80-mesh sieve;
(2) respectively weighing sodium dihydrogen phosphate, disodium hydrogen phosphate, dimeticone, cholestyramine resin and glucose according to the prescription amount, adding into a three-dimensional mixer, and fully mixing to uniformly mix;
(3) weighing silicon dioxide, saccharin sodium and lemon essence according to the prescription amount, adding into the three-dimensional mixer, and fully mixing to uniformly mix;
(4) subpackaging the mixed materials by using an aluminum-plastic composite film;
example 3
1. Prescription:
2. the process comprises the following steps:
(1) firstly, crushing sodium dihydrogen phosphate, disodium hydrogen phosphate and saccharin sodium and sieving the crushed materials with a 80-mesh sieve;
(2) respectively weighing sodium dihydrogen phosphate, disodium hydrogen phosphate, dimeticone, cholestyramine resin and glucose according to the prescription amount, adding into a three-dimensional mixer, and fully mixing to uniformly mix;
(3) weighing silicon dioxide, saccharin sodium and lemon essence according to the prescription amount, adding into the three-dimensional mixer, and fully mixing to uniformly mix;
(4) subpackaging the mixed materials by using an aluminum-plastic composite film;
example 4
1. Prescription:
2. the process comprises the following steps:
(1) firstly, crushing sodium dihydrogen phosphate, disodium hydrogen phosphate and saccharin sodium and sieving the crushed materials with a 80-mesh sieve;
(2) respectively weighing sodium dihydrogen phosphate, disodium hydrogen phosphate, dimeticone, cholestyramine resin and glucose according to the prescription amount, adding into a three-dimensional mixer, and fully mixing to uniformly mix;
(3) weighing silicon dioxide, saccharin sodium and lemon essence according to the prescription amount, adding into the three-dimensional mixer, and fully mixing to uniformly mix;
(4) subpackaging the mixed materials by using an aluminum-plastic composite film;
taste test
Mouth feel comparison experiments were carried out on the self-prepared product prepared in the above examples, and commercially available 1-sodium phosphate oral solution (Chengdukang pharmaceutical industry Co., Ltd., lot # 20140305), commercially available 2-sodium phosphate oral solution (Hubei noon pharmaceutical industry Co., Ltd., lot # 140401-2), and examples disclosed in Chinese patent CN 102232969B, respectively, and the experimental results are shown in Table 2:
TABLE 2 taste contrast experiment
| Sample name/mouthfeel comparison | Taste of the product |
| Example 1 | Smooth, slightly sweet and good taste |
| Example 2 | Smooth, slightly sweet and good taste |
| Example 3 | Smooth, slightly sweet and good taste |
| Example 4 | Smooth, slightly sweet and good taste |
| Commercial product 1 | Salty and sweet taste and poor mouthfeel |
| Commercial product 2 | Salty and sweet taste and poor mouthfeel |
| Prescription 1 | Salty and sweet taste and poor mouthfeel |
| Prescription 2 | The taste of the sweet and salty taste,has poor taste |
Remarking: recipe 1 and recipe 2 were prepared according to the examples disclosed in patent CN 102232969B, respectively.
And (4) conclusion: according to the results of taste experimental data, the taste masking agent cholestyramine resin is added into the product, so that the taste of the sodium phosphate oral preparation can be obviously improved, and the medication compliance of patients is increased.
In vitro dissolution rate test
1. Test conditions
(1) Slurry method (dissolution measurement second method)
(2) Rotating speed of 50 revolutions per minute
(3) Dissolution medium: pH6.8 phosphate buffer and water
(4) The sampling time is respectively as follows:
ph6.8 phosphate buffer: 5 minutes, 15 minutes, 30 minutes, 45 minutes and 60 minutes
Water: 5 minutes, 15 minutes, 30 minutes, 45 minutes and 60 minutes
2. Detection conditions are as follows: potentiometric titration method
3. The results of the release measurements are shown in table 3:
TABLE 3 Release degree test results
Remarking: recipe 1 and recipe 2 were prepared according to the examples disclosed in patent CN 102232969B, respectively.
From the above detection data, it can be seen that the sodium phosphate powder prepared by the process of the present formula is slowly released in 1 hour in both phosphate buffer solution with ph6.8 and water, while the colestyramine resin is not added to formula 1 and formula 2 prepared according to the examples disclosed in patent CN 102232969B, and is completely dissolved within five minutes, so that the addition of the colestyramine resin to the product can significantly delay the dissolution time of the product and improve the adverse irritation effect of the product on the gastrointestinal tract.
Long term stability study
The test conditions are as follows: the medicines are stored in an inverted manner in a medicine stability test box with the temperature of 25 +/-2 ℃ and the humidity of 60% +/-10%, and are sampled and inspected respectively at 3 rd, 6 th, 9 th, 12 th, 18 th, 24 th and 36 th months;
detection indexes are as follows: traits, content and microbial limits;
the products prepared according to the above examples and the examples disclosed in chinese patent CN 102232969B were examined according to the above stability test conditions, and the results are shown in table 4 below.
Table 4 stability test results
Remarking: recipe 1 and recipe 2 were prepared according to the examples disclosed in patent CN 102232969B, respectively.
From the above detection results, the product prepared according to the examples 1 and 2 disclosed in the patent CN 102232969B has a product quality close to the lower limit of the quality standard after being left for 24 months, and the content and the microorganism do not meet the requirements after being left for a long period of 36 months, but the product prepared by the formula and the preparation process has a greatly improved product stability, and the product quality still meets the quality standard after being left for 36 months, so that the product validity period is prolonged from 24 months to at least 36 months, and the product quality stability is improved by at least 50%.
Claims (2)
1. A sodium phosphate salt composition characterized by: the weight ratio of the combined medicine is as follows:
15-30 parts of sodium dihydrogen phosphate;
3-6 parts of disodium hydrogen phosphate;
0.05-0.3 part of dimeticone;
0.1-0.5 part of silicon dioxide;
0.1-0.2 part of saccharin sodium;
0.8-10 parts of glucose;
0.01-0.03 part of lemon essence;
0.5-2.0 parts of cholestyramine resin.
2. The process for preparing a sodium phosphate salt composition according to claim 1, wherein: comprises the following steps
1) Firstly, crushing sodium dihydrogen phosphate, disodium hydrogen phosphate and saccharin sodium and sieving the crushed materials with a 80-mesh sieve;
2) respectively weighing sodium dihydrogen phosphate, disodium hydrogen phosphate, dimeticone, cholestyramine resin and glucose according to the prescription amount, adding into a three-dimensional mixer, and fully mixing to uniformly mix;
3) weighing silicon dioxide, saccharin sodium and lemon essence according to the prescription amount, adding into the three-dimensional mixer, and fully mixing to uniformly mix;
4) and (3) subpackaging the mixed materials by using an aluminum-plastic composite film to obtain the sodium phosphate composition.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201911360198.3A CN111035655A (en) | 2019-12-25 | 2019-12-25 | Sodium phosphate composition and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201911360198.3A CN111035655A (en) | 2019-12-25 | 2019-12-25 | Sodium phosphate composition and preparation method thereof |
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| CN111035655A true CN111035655A (en) | 2020-04-21 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115957238A (en) * | 2022-12-14 | 2023-04-14 | 嘉实（湖南）医药科技有限公司 | A kind of preparation method of sodium phosphate salt granule |
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- 2019-12-25 CN CN201911360198.3A patent/CN111035655A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115957238A (en) * | 2022-12-14 | 2023-04-14 | 嘉实（湖南）医药科技有限公司 | A kind of preparation method of sodium phosphate salt granule |
| CN115957238B (en) * | 2022-12-14 | 2025-03-21 | 嘉实（湖南）医药科技有限公司 | A method for preparing sodium phosphate granules |
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Application publication date: 20200421 |