CN101002767A - Dispersion tablets of penicillin V potassium, and its preparing method - Google Patents

Abstract

A dispersing tablet of distakaps V-K with high curative effect and low cost is prepared from the raw powder of distakaps V-K and assistants, and features no allergic reaction. Its preparing process is also disclosed.

Description

Dispersion tablets of penicillin V potassium and preparation method thereof

Technical field

The invention belongs to a kind of Western medicine preparation, specifically is a kind of dispersion tablets of penicillin V potassium and its preparation method thereof.

Background technology

Potassium v calcium is applicable to slight, moderate, the severe infections of treatment to the benzylpenicillin sensitivity, is applicable to the recurrence and the prevention bacterial endocarditis of surgical operation and prevention rheumatic fever, cholera.Responsive microbial ear, nose and pharyngeal infection, amygdala inflammation, pharyngitis, otitis media.Respiratory tract infection: pneumonia.Skin infection; As erysipelas, erysipeloid and dividing a word with a hyphen at the end of a line property erythema; Scarlet fever; The recurrence of prophylaxis of acute rheumatic fever; Prophylaxis of teeth, oral cavity, jaw portion and the postoperative endocarditis of upper respiratory tract.

Dispersible tablet can rapid disintegrate form uniform suspension in water, can quick acting after taking.And this dosage form takes after not only can disperseing in water, can also swallow, and chews, and contains and suckes, and greatly convenient for children, old man and the inconvenient patient of the solid of swallowing can expand the scope of clinical use.

But the present domestic dispersion tablets of penicillin V potassium dosage form that still do not have.

Summary of the invention

The purpose of this invention is to provide a kind of dispersion tablets of penicillin V potassium dosage form and preparation method thereof, make potassium v calcium take the back quick acting, and expand the scope of clinical use the patient.

Dispersion tablets of penicillin V potassium is characterized in that being made up of former powder of potassium v calcium and adjuvant, and the formulation by weight of its component is:

The former powder 250 of potassium v calcium

Polyvinylpolypyrrolidone 20-40

Stevioside 4-8

Starch 12-18

The low replacement---hyprolose 20-30

Micropowder silica gel 8-12

Magnesium stearate 1-3

Pulvis Talci 0.5-2

60% alcoholic solution is an amount of.

Described dispersion tablets of penicillin V potassium is characterized in that its formulation by weight is:

The former powder 250 of potassium v calcium

Polyvinylpolypyrrolidone 30

Stevioside 6

Starch 15

The low replacement---hyprolose 25

Micropowder silica gel 10

Magnesium stearate 2

Pulvis Talci 1

60% alcoholic solution is an amount of.

The preparation method of described dispersion tablets of penicillin V potassium is characterized in that may further comprise the steps:

1, preprocessing raw material and auxiliary material: former powder of potassium v calcium and adjuvant be micronization processes respectively, and be standby;

2, weighing with mix: take by weighing the former powder of potassium v calcium and starch by formula ratio and mix;

3, system soft material: add an amount of 60% alcoholic solution behind former powder of potassium v calcium and the starch mix homogeneously, constantly stirring and evenly mixing is made soft material;

4, granulate: the soft material that makes is made wet granular on granulator;

5, drying: with the wet granular oven dry that makes, temperature control 40 ^-50 ℃, dried pellet moisture should be controlled at≤and 2%;

6, granulate: dry good granule wants timely granulate in case the moisture absorption;

7, total mixing: accurately take by weighing dried granule and add in the three-dimensional stereo mixing machines, heavily convert required adjuvant, build seal cover, install guard rail, mix by dried granule;

8, tabletting, packing, warehouse-in.

Technical scheme of the present invention is as follows:

Prescription design of the present invention is optimized, and is a result of the test of prescription design optimization below

Prescription composition and consumption	1	2	3	4	5
						Potassium v calcium hangs down replacement-hyprolose stevioside polyvinylpolypyrrolidone starch	250 25 - 30 15	250 - 6 30 -	250 25 6 30 15	250 25 6 10 -	250 25 6 - 30

Disintegration time (second) dispersed homogeneous degree outward appearance

73 is qualified general

142 is qualified general

65 is qualified good

168 is qualified general

122 is qualified general

Dispersion tablets of penicillin V potassium dosage form constant product quality of the present invention, in the prescription screening process, adopt Optimized by Orthogonal Test, from product quality, safety and production cost, optimizing prescriptions, through research for many years, overcome dispersion tablets of penicillin V potassium and be prone to pitted skin, the inhomogeneous grade of color and luster influences the phenomenon of outward appearance, has reached to be uniformly dispersed, and dissolution rate is fast, peak reaching time of blood concentration is short, reach peak blood drug level height, blood drug level is kept length, the characteristics that bioavailability is high, improved patient's medication compliance greatly, clinical therapeutic efficacy has better obtained performance; Adopt the limit handling of penicillin V polymer content first, can prevent effectively that penicillin allergy from taking place, safety significantly improves; It is oral to can be made into suspension solution, makes things convenient for dysphagia person to use; Optimize recipe structure, adopt starch, and to the selection and the adjustment of all the other components of writing out a prescription, the prescription cost reduces by 20% as binding agent.

One, prescription is formed

The former powder 250g of potassium v calcium

Polyvinylpolypyrrolidone 30g

Stevioside 6g

Starch 15g

The low replacement---hyprolose 25g

Micropowder silica gel 10g

Magnesium stearate 2g

Pulvis Talci 1g

60% alcoholic solution is an amount of

Make 1000

Two, production technology

1, preprocessing raw material and auxiliary material: former powder of potassium v calcium and adjuvant micronization processes, standby.

2, weighing with mix: after the supplementary material micronization processes, accurately take by weighing the former powder of potassium v calcium and starch by recipe quantity and insert in the single shaft mixer and mixed 30 minutes.

3, system soft material: add an amount of 60% alcoholic solution behind former powder of potassium v calcium and the starch mix homogeneously, constantly stirring and evenly mixing is made soft material.

4, granulate: the soft material that makes is crossed 20 mesh sieves make wet granular on granulator.

5, drying: the wet granular that makes is put into drip pan, temperature control 40 ^-50 ℃, dry 70 minutes.Dried pellet moisture should be controlled at≤and 2%.

6, granulate: dry good granule wants timely granulate in case the moisture absorption is installed 18 mesh sieves and carried out granulate on pelletizing machine during granulate.

7, total mixing: accurately take by weighing dried granule and add in the three-dimensional stereo mixing machines, heavily convert required adjuvant, build seal cover, install guard rail, mixed 30 minutes by dried granule.

8, mixed semi-finished product are contained in the container of clean dried, sealing.

9, semi-finished product with full-automatic tablet machine tabletting, will be controlled tablet weight variation through the quality inspection center after the assay was approved in the tabletting process, and the semi-finished product that suppress are contained in the container of clean dried, sealing.All should flow with semi-finished product inside and outside the container and block, write the name of an article, specification, lot number, quantity, date and operator etc. exactly, in time send terminal, it is to be checked to put Holding Area.

10, semi-finished product are packed with full-automatic two aluminum compounding machines after the assay was approved through the quality inspection center, carry out finished product packing then.

11, finished product is put in storage through the quality inspection center after the assay was approved.

Three, quality index:

Inspection item	Unit	Controlling index
			Character	/	This product should be the off-white color sheet
Differentiate 1	/	Should be up to specification
			2	/	Should be positive reaction
3	/	Should be positive reaction
			Dispersed homogeneous degree	Minute	≤3
The penicillin V polymer	％	≤2
			Tablet weight variation	％	Must not mistake ± 5
Dissolution	％	≥77
			Friability	％	≤1
Microbial limit	Individual/g	Mycete≤80
			Assay	％	93.0 -107.0

Four, penicillin V polymer determination:

Penicillin V polymer: measure according to high performance liquid chromatography.

The preparation of reference substance solution: get the about 40mg of penicillin V reference substance, accurate claim surely, put in the 250ml measuring bottle, be dissolved in water and be diluted to scale, shake up, in contrast product solution.

Chromatographic condition and system suitability condition: with Sephadex G-10 is filler, and (PH7.0) (gets 21.85gNa with the 0.1mol/L phosphate buffer ₂HPO ₄12H ₂O and 6.08gNaH ₂PO ₄, 2H ₂O, be dissolved in water and be diluted to 1000ml, regulate PH to 7.0) be mobile phase A, with water is Mobile phase B, detects wavelength 268nm, is mobile phase with the mobile phase A, get blue dextran 2000 solution (1.0mg/m1) 50ul injecting chromatograph, the record chromatogram, theoretical cam curve should be not less than 800 with blue dextran 2000 peaks, and tailing factor should be 0.75 ^-1.50 between, other gets reference substance solution, is mobile phase with the Mobile phase B, repeats sample introduction 50ul, and the relative standard deviation of peak area value should be less than 2.0%.

Algoscopy: get 10 of this product, the accurate title, decided porphyrize, precision takes by weighing in right amount (being equivalent to penicillin V 250mg approximately), puts in the 50ml measuring bottle, adds the mobile phase A ultrasonic dissolution and is diluted to scale, shake up, the 0.45um filter membrane filters, and gets filtrate 50ul injecting chromatograph immediately, with the mobile phase A is that mobile phase is measured, the record chromatogram, other gets reference substance solution 50ul injecting chromatograph, is mobile phase with the Mobile phase B, the record chromatogram calculates by external standard method.This product contains the penicillin V polymer in penicillin V, must not cross 2.0%.

Claims (8)

1, dispersion tablets of penicillin V potassium is characterized in that being made up of former powder of potassium v calcium and adjuvant, its component

Formulation by weight is:

The former powder 250 of potassium v calcium

Polyvinylpolypyrrolidone 20-40

Stevioside 4-8

Starch 12-18

The low replacement--hyprolose 20-30

Micropowder silica gel 8-12

Magnesium stearate 1-3

Pulvis Talci 0.5-2

60% alcoholic solution is an amount of.

2, dispersion tablets of penicillin V potassium according to claim 1 is characterized in that its formulation by weight is:

The former powder 250 of potassium v calcium

Polyvinylpolypyrrolidone 30

Stevioside 6

Starch 15

The low replacement--hyprolose 25

Micropowder silica gel 10

Magnesium stearate 2

Pulvis Talci 1

60% alcoholic solution is an amount of.

3, the preparation method of dispersion tablets of penicillin V potassium according to claim 1 is characterized in that may further comprise the steps:

1, preprocessing raw material and auxiliary material: former powder of potassium v calcium and adjuvant be micronization processes respectively, and be standby;

2, weighing with mix: take by weighing the former powder of potassium v calcium and starch by formula ratio and mix;

3, system soft material: add an amount of 60% alcoholic solution behind former powder of potassium v calcium and the starch mix homogeneously, constantly stirring and evenly mixing is made soft material;

4, granulate: the soft material that makes is made wet granular on granulator;

5, drying: with the wet granular oven dry that makes, temperature control 40 ^-50 ℃, dried pellet moisture should be controlled at≤and 2%;

6, granulate: dry good granule wants timely granulate in case the moisture absorption;

7, total mixing: accurately take by weighing dried granule and add in the three-dimensional stereo mixing machines, heavily convert required adjuvant, build seal cover, install guard rail, mix by dried granule;

8, tabletting, packing, warehouse-in.