CN102178694B - Liquid preparation of sodium ascorbyl phosphate - Google Patents

Abstract

The invention discloses a liquid preparation of sodium ascorbyl phosphate. Each 1,000 milliliters of liquid preparation contains 40 to 180 grams of Na2HPO4.7H2O, 100 to 480 grams of NaH2PO4.H2O, and 0.05 to 0.3 grams of preservative. The liquid preparation of the sodium ascorbyl phosphate has a remarkable preservative effect; and the solubility, dissolution speed and stability of the sodium ascorbyl phosphate, which is the mixture of the Na2HPO4.7H2O and NaH2PO4.H2O, are high.

Description

Liquid preparation of sodium ascorbyl phosphate

Technical field

The invention belongs to field of pharmaceutical preparations, relate to a kind of Pharmaceutical composition, be specifically related to a kind of liquid preparation of sodium ascorbyl phosphate and preparation method thereof.

Background technology

Sodium ascorbyl phosphate is used for clearing up intestinal before patient's colon X-light and intestinal splanchnoscopy or the operation, sodium ascorbyl phosphate goes out non-absorbent zwitterion at the intestinal internal disintegration, in intestinal, form height and ooze environment, because the character of intestinal semipermeable membrane, make the interior moisture content of body enter intestinal, common a kind of mechanical stimulus, the promotion intestinal movement of producing of the moisture content that the moisture content that itself is contained and patient take.Sodium ascorbyl phosphate makes the interior moisture content increase of intestinal soften stool, and the local nerve that sodium ascorbyl phosphate can also activate the intestinal mucosa layer reflects and the wriggling of increase intestinal wall, improves intestinal power, promotes defecation.

Chinese patent CN200910060341.7 discloses a kind of preparation method of sodium ascorbyl phosphate oral solution, its step comprises material dissolution, boiling sterilization, filtration sterilization, boiling sterilization refers in the solution of material dissolution step gained, the adding mass volume ratio is 0.02%～0.03% sodium benzoate, after solution stirring is even, 98 ℃～100 ℃ insulations 1～2 hour; Described filtration sterilization steps is cooled to below 40 ℃ for the solution with the boiling sterilization gained, and the adding mass volume ratio is 0.10%～0.13% essence, with 0.22 μ m microporous filter membrane solution is filtered again, obtains sodium ascorbyl phosphate oral solution.The method adopts the mode of high temperature to sterilize, and equipment needed thereby and consume energy all very greatly in productions brings a lot of inconvenience to industrialization.

Summary of the invention

The purpose of this invention is to provide a kind of liquid preparation of sodium ascorbyl phosphate.

A kind of liquid preparation of sodium ascorbyl phosphate provided by the invention, the described liquid preparation of every 1000ml contains the Na of 40～180g ₂HPO ₄7H ₂O, the NaH of 100～480g ₂PO ₄H ₂O, the antiseptic of 0.05～0.3g.

Described liquid preparation is preferably oral administration solution, contains the Na of 180g in every 1000ml oral administration solution ₂HPO ₄7H ₂O, the NaH of 480g ₂PO ₄H ₂O, the antiseptic of 0.3g also comprises the correctives of 0.4～1g, described correctives is preferably Fructus Citri tangerinae essence, saccharin sodium, described antiseptic is preferably sodium benzoate.

Described liquid preparation is preferably enema, contains the Na of 40～100g in every 1000ml enema ₂HPO ₄7H ₂O, the NaH of 100～200g ₂PO ₄H ₂O, the antiseptic of 0.1～0.3g, the EDTA-2Na of 0.1～0.5g, described antiseptic is preferably benzalkonium chloride.

This liquid preparation of sodium ascorbyl phosphate favorable anti-corrosion effect, sodium ascorbyl phosphate adopts Na ₂HPO ₄7H ₂O and NaH ₂PO ₄H ₂The mixture of O, its dissolubility is good, and dissolution velocity is fast, good stability.

Another object of the present invention provides a kind of preparation method of liquid preparation of sodium ascorbyl phosphate, and the method comprises the following steps:

(1) dosing: first the antiseptic of recipe quantity is used the purified water stirring and dissolving of full dose 70%, added again Na ₂HPO ₄7H ₂O and NaH ₂PO ₄H ₂O, stirring and dissolving is added purified water to full dose, mixes namely to get to filter front stock solution pH, relative density and content in the middle of sampling detects;

(2) filter: after the intermediate detection is qualified, with 0.45 μ m filtering with microporous membrane solution;

(3) embedding: be ready to plastic bottle, carry out fill, after fill is good, timely sealing, capping plug, and sample presentation inspection;

(4) packing: after the fill the full inspection of sample qualified after, certified products are labelled, in the carton of packing into.

This preparation method is simple, does not need special equipment, energy savings.

The specific embodiment

The present invention is further illustrated below in conjunction with specific embodiment, but this should be interpreted as that the scope of the above-mentioned theme of the present invention only limits to following embodiment.All technology that realizes based on foregoing of the present invention all belong to scope of the present invention.Adjuvant in following examples can be replaced with pharmaceutically acceptable similar adjuvant, perhaps reduces, increases.

Embodiment 1

Prescription:

Preparation technology:

(1) dosing: with the benzalkonium chloride of recipe quantity and the purified water stirring and dissolving of EDTA-2Na usefulness full dose 70%, add again Na first ₂HPO ₄7H ₂O and NaH ₂PO ₄H ₂O, stirring and dissolving is added purified water to full dose, mixes namely to get to filter front stock solution pH, relative density and content in the middle of sampling detects;

(2) filter: after the intermediate detection is qualified, with 0.45 μ m filtering with microporous membrane solution;

(3) embedding: be ready to plastic bottle, carry out fill, after fill is good, timely sealing, capping plug, and sample presentation inspection;

(4) packing: after the fill the full inspection of sample qualified after, certified products are labelled, in the carton of packing into.

Embodiment 2

Prescription:

Preparation technology:

(1) dosing: with the benzalkonium chloride of recipe quantity and the purified water stirring and dissolving of EDTA-2Na usefulness full dose 70%, add again Na first ₂HPO ₄7H ₂O and NaH ₂PO ₄H ₂O, stirring and dissolving is added purified water to full dose, mixes namely to get to filter front stock solution pH, relative density and content in the middle of sampling detects;

(2) filter: after the intermediate detection is qualified, with 0.45 μ m filtering with microporous membrane solution;

(3) embedding: be ready to plastic bottle, carry out fill, after fill is good, timely sealing, capping plug, and sample presentation inspection;

(4) packing: after the fill the full inspection of sample qualified after, certified products are labelled, in the carton of packing into.

Embodiment 3

Prescription:

Preparation technology:

(1) dosing: with the benzalkonium chloride of recipe quantity and the purified water stirring and dissolving of EDTA-2Na usefulness full dose 70%, add again Na first ₂HPO ₄7H ₂O and NaH ₂PO ₄H ₂O, stirring and dissolving is added purified water to full dose, mixes namely to get to filter front stock solution pH, relative density and content in the middle of sampling detects;

(2) filter: after the intermediate detection is qualified, with 0.45 μ m filtering with microporous membrane solution;

(3) embedding: be ready to plastic bottle, carry out fill, after fill is good, timely sealing, capping plug, and sample presentation inspection;

(4) packing: after the fill the full inspection of sample qualified after, certified products are labelled, in the carton of packing into.

Embodiment 4

Prescription:

Preparation technology:

(1) dosing: first sodium benzoate, saccharin sodium, the Fructus Citri tangerinae essence of recipe quantity is used the purified water stirring and dissolving of full dose 70%, added again Na ₂HPO ₄7H ₂O and NaH ₂PO ₄H ₂O, the glycerol stirring and dissolving is added purified water to full dose, mixes namely to get to filter front stock solution pH, relative density and content in the middle of sampling detects;

(2) filter: after the intermediate detection is qualified, with 0.45 μ m filtering with microporous membrane solution;

(3) embedding: be ready to plastic bottle, carry out fill, after fill is good, timely sealing, capping plug, and sample presentation inspection;

(4) packing: after the fill the full inspection of sample qualified after, certified products are labelled, in the carton of packing into.

Experimental example 1

Embodiment 1～embodiment 4 samples carry out limit test of microbe:

The limit test of microbe result

The result shows that embodiment 1～embodiment 4 sample microbial limits are up to specification, the sample favorable anti-corrosion effect.

Experimental example 2

Embodiment 1 sample carries out influence factor's test

Sample is positioned over strong illumination (4500lx ± 500), high temperature (60 ℃) condition is carried out factors influencing, detect the quality index such as its appearance character, pH value, relative density and content respectively at sampling in the 5th day, the 10th day, and compare with 0 day testing result.Also having carried out simultaneously low-temperature test (placed 2 days at 2 ℃～8 ℃ cold compartment of refrigerator first, then under 40 ℃ of conditions, accelerate to investigate 2 days, circulate three times) and freezing-thawing test (placed 2 days at-10 ℃～-20 ℃ freezer compartment of refrigerator first, then under 40 ℃ of conditions, accelerate to investigate 2 days, circulate three times), result of the test is as follows:

Influence factor's study on the stability result

By above-mentioned result of the test as can be known, this product after placing 10 days under high light, the hot conditions, each index and relatively having no significant change in 0 day.Each index that low temperature and freezing-thawing test record and 0 day are more also without significant change, without crystallization.Therefore this product is to light, heat, and low temperature etc. are all stablized, and preserves at ambient temperature to get final product.

Experimental example 3

The sodium ascorbyl phosphate dissolution velocity test of different water of crystallization

The sodium ascorbyl phosphate mixture of getting an amount of different water of crystallization (is equivalent to Na ₂HPO ₄0.67mol and NaH ₂PO ₄3.45mol), add water to 1000ml under the stirring condition, stir and make the principal agent dissolving, investigate the dissolution time of the sodium phosphate of different water of crystallization.The result is as follows:

The test of sodium ascorbyl phosphate dissolution velocity

By above-mentioned result of the test as can be known, the sodium ascorbyl phosphate mixture is by Na ₂HPO ₄.7H ₂O and NaH ₂PO ₄.H ₂When O forms, dissolve at normal temperatures very fastly, can obviously shorten the dissolution time that feeds intake in the technique, significantly improve production efficiency, prevent the dosing overlong time and be subjected to microbial contamination.

Claims (8)

1. a liquid preparation of sodium ascorbyl phosphate is characterized in that, the described liquid preparation of every 1000ml contains the Na of 40～180g ₂HPO ₄7H ₂O, the NaH of 100～480g ₂PO ₄H ₂O, the antiseptic of 0.05～0.3g.

2. liquid preparation according to claim 1 is characterized in that, described liquid preparation is oral administration solution.

3. liquid preparation according to claim 2 is characterized in that, contains the Na of 180g in every 1000ml oral administration solution ₂HPO ₄7H ₂O, the NaH of 480g ₂PO ₄H ₂O, the antiseptic of 0.3g also comprises the correctives of 0.4～1g.

4. liquid preparation according to claim 3 is characterized in that, described correctives is Fructus Citri tangerinae essence, and saccharin sodium, described antiseptic are sodium benzoate.

5. liquid preparation according to claim 1 is characterized in that, described liquid preparation is enema.

6. liquid preparation according to claim 5 is characterized in that, contains the Na of 40～100g in every 1000ml enema ₂HPO ₄7H ₂O, the NaH of 100～200g ₂PO ₄H ₂O, the antiseptic of 0.1～0.3g, the EDTA-2Na of 0.1～0.5g.

7. liquid preparation according to claim 6 is characterized in that, described antiseptic is benzalkonium chloride.

8. the preparation method of the described liquid preparation of sodium ascorbyl phosphate of claim 1, the method comprises the following steps:

(1) dosing: first the antiseptic of recipe quantity is used the purified water stirring and dissolving of full dose 70%, added again Na ₂HPO ₄7H ₂O and NaH ₂PO ₄H ₂O, stirring and dissolving is added purified water to full dose, mixes namely to get to filter front stock solution pH, relative density and content in the middle of sampling detects;

(2) filter: after the intermediate detection is qualified, with 0.45 μ m filtering with microporous membrane solution;

(3) embedding: be ready to plastic bottle, carry out fill, after fill is good, timely sealing, capping plug, and sample presentation inspection;

(4) packing: after the fill the full inspection of sample qualified after, certified products are labelled, in the carton of packing into.