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Pharmaceutical composition for conducting infusion therapy in bladder lumen

A technology for treating drugs and compositions, applied in the field of carriers of low water-soluble drugs, can solve the problems of low bladder wall permeability, ectopic ventricular rhythm, aggravating the burden of liver and kidney functions, etc. The effect of reducing the amount of medication

Inactive Publication Date: 2017-03-08
曹庆杰 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Intravesical perfusion therapy also has problems such as being washed out by urine and low permeability of the bladder wall; and oral drug therapy can affect M receptors in other parts of the body, resulting in dry mouth, flushed skin, less sweating, gastrointestinal Low motivation, constipation, gastroesophageal reflux, dysuria and other adverse reactions, and even drowsiness, hallucinations, mydriasis, urinary retention, rapid heart rate, excitement, restlessness, convulsions, hallucinations, confusion and heterotopic chambers In severe cases such as abnormal heart rhythm, it will also increase the burden on liver and kidney function

Method used

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  • Pharmaceutical composition for conducting infusion therapy in bladder lumen

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0033] Prescription composition:

[0034] Chitosan

[0035] sodium triphosphate

[0036] Thioglycolic acid

[0037] Gemcitabine Hydrochloride

[0038] Preparation:

[0039] Add 1.5g of chitosan to 100ml of thioglycolic acid and 1g of concentrated sulfuric acid, stir in a water bath at 40°C for 24h, filter, wash with distilled water and ethanol, and dry in vacuum at 35°C to generate mercaptochitosan.

[0040] 2. Mercaptochitosan was dissolved in distilled water (2 mg / ml), and the pH was adjusted to 4.8; the concentration of sodium triphosphate aqueous solution was 1 mg / ml, and gemcitabine hydrochloride was dissolved in sodium triphosphate solution (5 mg / ml); stirred at room temperature The mercapto-chitosan solution was added dropwise to the sodium triphosphate solution in which gemcitabine was dissolved, then centrifuged for 1 hour at a speed of 13500 rpm, and the supernatant was discarded to generate chitosan particles encapsulated with gemcitabine.

[0041] 3. According...

example 2

[0043] Prescription composition:

[0044] Oxybutynin Hydrochloride

[0045] Chitosan

[0046] Hydroxypropylmethylcellulose

[0047] Poloxamer 407

[0048] Preparation:

[0049] Method 1 (group 1-9): glacial acetic acid was dissolved in half an amount of distilled water, and chitosan was added according to the percentage by weight shown in Table 1, and stirred slowly; Oxybutynin hydrochloride was dissolved in half an amount of distilled water; at room temperature, two The two solutions were mixed and stirred at a stirring rate of 500 rpm until a uniform gel was formed. Then add base, other additives and water as needed.

[0050] Method 2 (groups 10-13): at room temperature, add hydroxypropyl methylcellulose into distilled water dissolved in oxybutynin hydrochloride according to the weight percentage shown in Table 1, stir for 1 hour, and the speed is 500rpm, Generate target gels. Then add base, other additives and water as needed.

[0051] Method 3 (group 14-16): at 4°C...

example 3

[0055] Prescription composition:

[0056] Paclitaxel

[0057] ethyl acetate

[0058] polyvinyl alcohol

[0059] Polymethacrylate

[0060] Preparation method: 50 mg of polymethacrylate and 2.5 mg of paclitaxel were dissolved in 1.5 ml of ethyl acetate; the above solution was added into 15 ml of 2% polyvinyl alcohol solution by mass percentage, and emulsified for 5 minutes. The above emulsion was stirred at room temperature until the ethyl acetate was completely evaporated. Separate target microspheres, clear with distilled water, centrifuge at 4000rpm for 5 minutes, repeat 3 times; store in 4°C environment in the form of water suspension. Then add base, other additives and water as needed.

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Abstract

The invention relates to the field of pharmaceutical preparations, and in particular to a pharmaceutical composition for conducting infusion therapy in a bladder lumen. The pharmaceutical composition consists of major therapeutic drug ingredients, a bio-adhesive material, a drug penetration regulator, a release rate regulator, a matrix, other additives and the balance of water. The pharmaceutical composition can be used for controlling the slow release of major therapeutic drugs and improving remaining time of the major therapeutic drug ingredients in a bladder and a penetration efficiency on bladder wall mucosa, and in addition, the pharmaceutical composition, as a carrier of low-solubility drugs, can be applied to therapy in the bladder lumen; and the pharmaceutical composition can be used for treating bladder intra-lumen infections, unstable bladder and cystitis glandularis, and the pharmaceutical composition can be applied to chemotherapy, immunotherapy, biotherapy, gene therapy and prevention of bladder cancer.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a pharmaceutical composition that can be used for intravesical perfusion therapy, and is used to control the slow release of the main therapeutic drug components, improve the residence time of the main therapeutic drug components in the bladder cavity and enhance the effect on the bladder wall mucosa. Penetration efficiency, in addition, the pharmaceutical composition can also be used as a carrier of low water-soluble drugs for intravesical treatment; can be used for the treatment of intravesical infection, unstable bladder (including but not limited to overactive bladder, lower urinary tract irritation [LUST], etc.), cystitis glandularis, chemotherapy for bladder cancer or sarcoma, immunotherapy, biological therapy, gene therapy and prophylaxis. Background technique [0002] Bladder disease is an important research field of urology. Bladder cancer is the most common ma...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/36A61K31/7068A61K9/06A61K47/38A61K31/216A61K9/10A61K47/32A61K31/337A61P13/10
CPCA61K9/0034A61K9/0002A61K9/06A61K9/10A61K9/5036A61K31/216A61K31/337A61K31/7068A61K47/32A61K47/38
Inventor 曹庆杰程勇
Owner 曹庆杰
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