CN1602870A - Dripping pills of bucinnazine hydrochloride and its preparation - Google Patents

Abstract

The invention bucinnazine hydrochloride pill, prepared by superfine crushing and pill producing techniques, can achieve the purposes of increasing disintegration and dispersion speeds, and dissolving-out speed and degree, quickly taking effect, improving drug stability, reducing auxiliary use, reducing production cost, being convenient to carry and take. Its compliance is good and it is especially suitable for children, the aged, patients in bed and patients difficult in swallowing to take.

Description

Bucinnazine hydrochloride drop pill and preparation method thereof

Technical field

The present invention relates to a kind of pharmaceutical product and preparation method thereof, specifically bucinnazine hydrochloride drop pill and preparation method thereof.

Background technology

Bucinnazine hydrochloride is a quickly-acting antalgic, pain to skin, mucosa, organ of locomotion (comprising joint, muscle, tendon etc.) has significant analgesia role, analgesic effect to internal organs pain is relatively poor, and unrestraint gastrointestinal peristalsis effect is poor to the analgesic effect of smooth muscle spasm.Compare with morphine, be difficult for into latently, but in various degree toleration is arranged.

After bucinnazine hydrochloride is oral, easily by gastrointestinal absorption, oral back onset in 10～30 minutes, analgesic effect was kept 3～6 hours, mainly discharged from urine and feces with metabolite.The oral formulations of list marketing at present only has tablet, clinically is used for various pain, as pain, urodynia and tumor pain etc. after neuralgia, postoperative pain, lumbago, the calcination.

Bucinnazine hydrochloride has foreign odor, bitter in the mouth, in water, dissolve, but its disintegration of tablet time is long, dissolution and dissolution rate are low, absorption difference, and bioavailability is low, the supplementary product consumption ratio is big, child, old people, bed patient and dysphagia patients are taken inconvenience, and compliance is poor, have influenced the performance of bucinnazine hydrochloride therapeutical effect.

The present invention makes the bucinnazine hydrochloride drop pill by using ultramicro communication technique and dropping pill formulation Technology exactly, thereby overcomes the above defective of bucinnazine hydrochloride sheet, and the therapeutical effect of bucinnazine hydrochloride is given full play to.

Summary of the invention

The bucinnazine hydrochloride drop pill of making by using ultramicro communication technique and dropping pill formulation Technology not only have disintegrate molten loose fast, dissolution and dissolution rate improve, steady quality, the pill volume is little, easy to carry and use, onset is rapid, compliance is good, be particularly suitable for the characteristics that child, old people, bed patient and dysphagia patients are taken, but also has working condition and production equipment is simple, production cost is low, compares the advantage that supplementary product consumption reduces with tablet, has demonstrated fully the new drug research exploitation spirit that people-oriented.

For achieving the above object, the present invention by the following technical solutions: the bucinnazine hydrochloride fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, abundant mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.

The chemical name of bucinnazine hydrochloride among the present invention (Bucinnazin Hydrochlride Hydrochloride) is the positive bytyry of 1--4-cinnamyl piperazine hydrochlorate, and molecular formula is C ₁₇H ₂₄N ₂OHCl, molecular weight are 308.85, and structural formula is

Substrate among the present invention includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.

Coolant among the present invention includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.

Below through detecting to beneficial effect of the present invention as directed

One, detects index and method

1. disintegrate (molten loosing) time limit: check according to inspection technique disintegration (two appendix XA of Chinese Pharmacopoeia version in 2000).

2. dissolution rate: sample thief, according to dissolution method (two appendix XC first methods of Chinese Pharmacopoeia version in 2000), 900ml is a solvent with hydrochloric acid solution (9 → 1000), rotating speed is that per minute 75 changes, operation in accordance with the law, in the time of 10,20,30,40 minutes, get solution 5ml, filter, precision is measured filtrate 2ml, put in the 100ml measuring bottle, be diluted to scale with hydrochloric acid solution (9 → 1000), shake up, according to spectrophotography (two appendix IV of Chinese Pharmacopoeia version in 2000 A), wavelength place at 252nm measures trap, presses C ₁₇H ₂₄N ₂Absorptance (the E of OHCl _1cm ^1%) be 671 calculating stripping quantities.

Two, commercially available bucinnazine hydrochloride sheet testing result

1. disintegration time: 32 minutes

2. dissolution rate:

Time (minute) 10 20 30 40

Dissolution (%) 48.7 86.5 93.4 92.5

Three, example 1 sample detection result

1. the molten diffusing time: 2 minutes

2. dissolution rate:

Time (minute) 10 20 30 40

Dissolution (%) 79.8 99.6 99.2 100.1

Four, example 2 sample detection results

1. the molten diffusing time: 2 minutes

2. dissolution rate:

Time (minute) 10 20 30 40

Dissolution (%) 81.3 97.6 98.4 99.8

Five, example 3 sample detection results

1. the molten diffusing time: 2 minutes

2. dissolution rate:

Time (minute) 10 20 30 40

Dissolution (%) 72.5 98.7 99.6 99.1

Six, example 4 sample detection results

1. the molten diffusing time: 3 minutes

2. dissolution rate:

Time (minute) 10 20 30 40

Dissolution (%) 69.8 95.6 96.7 98.2

Seven, example 5 sample detection results

1. the molten diffusing time: 4 minutes

2. dissolution rate:

Time (minute) 10 20 30 40

Dissolution (%) 85.4 99.0 99.2 98.3

Eight, example 6 sample detection results

1. the molten diffusing time: 4 minutes

2. dissolution rate

Time (minute) 10 20 30 40

Dissolution (%) 76.5 98.6 99.0 97.3

The specific embodiment

One, example 1

Prescription:

Bucinnazine hydrochloride 5g

Polyethylene glycol 6000 15g

Make 1000

Method for making: the bucinnazine hydrochloride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused polyethylene glycol 6000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.

Two, example 2

Prescription:

Bucinnazine hydrochloride 5g

Macrogol 4000 15g

Make 1000

Method for making: the bucinnazine hydrochloride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused Macrogol 4000 substrate, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.

Three, example 3

Prescription:

Bucinnazine hydrochloride 5g

Polyethylene glycol 6000 5g

Macrogol 4000 10g

Make 1000

Method for making: the bucinnazine hydrochloride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused Macrogol 4000 and the polyethylene glycol 6000 mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.

Four, example 4

Prescription:

Bucinnazine hydrochloride 5g

Glyceryl monostearate 15g

Make 1000

Method for making: the bucinnazine hydrochloride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in the fused glyceryl monostearate substrate, and mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.

Five, example 5

Prescription:

Bucinnazine hydrochloride 5g

Polyethylene glycol 6000 10g

Poloxamer 5g

Make 1000

Method for making: the bucinnazine hydrochloride fine powder that the micronizing of learning from else's experience is crossed 200 mesh sieves is added in fused polyethylene glycol 6000 and the poloxamer mixed-matrix, stirs evenly, and with the dimethicone coolant, the dropping preparation method pill, drying, promptly.

Six, example 6

Prescription:

Bucinnazine hydrochloride 5g

Glyceryl monostearate 15g

Poloxamer 1g

Make 1000

Method for making: get the mixing fine powders that bucinnazine hydrochloride and poloxamer cross 200 mesh sieves through micronizing and be added in the fused glyceryl monostearate substrate, mixing is a coolant with the frozen water, the dropping preparation method pill, and drying, promptly.

Claims (4)

1. bucinnazine hydrochloride drop pill and preparation method thereof is characterized in that: the bucinnazine hydrochloride fine powder of 1 weight portion through micronizing is added in 1～10 weight portion molten matrix, fully mixing, dropping preparation method is condensed into ball in coolant, remove coolant, drying, promptly.

2. the chemical name of the described bucinnazine hydrochloride of claim 1 (Bucinnazin Hydrochlride Hydrochloride) is the positive bytyry of 1--4-cinnamyl piperazine hydrochlorate, and molecular formula is C ₁₇H ₂₄N ₂OHCl, molecular weight are 308.85, and structural formula is

3. the described substrate of claim 1 includes but not limited to polyethylene glycol 6000, Macrogol 4000, polyethylene glycol 1500, cetomacrogol 1000, sodium stearate, glycerin gelatine, poloxamer, stearic acid, glycerol monostearate acid, insect wax etc.

4. the described coolant of claim 1 includes but not limited to dimethicone, liquid paraffin, vegetable oil, water, alcoholic solution etc.