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Lipidosome-polymer particle preparation of topical anaesthetic and preparation method of lipidosome-polymer particle preparation

A technology of local anesthetics and liposomes, applied in the field of liposome-polymer particle preparations of local anesthetics and its preparation, can solve the problems of high equipment requirements, increased production risks, dose dumping, etc., and achieve simple preparation methods , Good controlled release effect, good sustained release effect

Active Publication Date: 2016-06-29
GUANGZHOU BOSITAO CONTROLLED RELEASE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] From the perspective of prescription development, the amount of synthetic phospholipid materials used in the existing process is large and the cost is extremely high. After deducting the basic costs such as production energy consumption, the cost of each tube is more than 500 yuan, which is contrary to the principle of economical energy saving required by pharmacoeconomics. Moreover, the use of phospholipids as the material of multivesicular liposomes generally has the defect of poor structural stability, and the drug may leak in the phospholipid vesicles, causing dose dumping; There are many key parameters to control, which greatly increases the production risk and increases the burden on the production enterprise

Method used

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  • Lipidosome-polymer particle preparation of topical anaesthetic and preparation method of lipidosome-polymer particle preparation

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] The prescription is shown in Table 1:

[0054]

[0055]

[0056] Carry out the following operations according to the formula in Table 1:

[0057] 1. Preparation of the inner aqueous phase: Disperse the prescribed amount of active drug (bupivacaine hydrochloride) and osmotic pressure regulator into the aqueous solution for injection whose pH is adjusted to 1.0 with hydrochloric acid, and stir until the materials are evenly dispersed in the inner aqueous phase solution, get the inner water phase;

[0058] 2. Preparation of the first organic phase: dissolving the polylactic acid-hydroxylactic acid copolymer of the prescribed amount in chloroform of a certain quality to obtain the first organic phase;

[0059] 3. Preparation of the second organic phase: respectively dissolving hydrogenated phospholipids and cholesterol in a certain amount of chloroform to obtain the second organic phase;

[0060] 4. Preparation of the external aqueous phase: dissolve the osmotic pre...

Embodiment 2

[0066] The prescription is shown in Table 2:

[0067]

[0068] Carry out the following operations according to the formula in Table 1:

[0069] 1. Preparation of the inner aqueous phase: Disperse the prescribed amount of active drug (bupivacaine hydrochloride) and osmotic pressure regulator into the aqueous solution for injection whose pH is adjusted to 1.0 with hydrochloric acid, and stir until the materials are evenly dispersed in the inner aqueous phase solution, get the inner water phase;

[0070] 2. Preparation of the first organic phase: dissolving the polylactic acid-hydroxylactic acid copolymer of the prescribed amount in chloroform of a certain quality to obtain the first organic phase;

[0071] 3. Preparation of the second organic phase: respectively dissolving hydrogenated phospholipids and cholesterol in a certain amount of chloroform to obtain the second organic phase;

[0072] 4. Preparation of the external aqueous phase: dissolve the osmotic pressure regula...

Embodiment 3

[0078] The prescription is shown in Table 3:

[0079]

[0080] Carry out the following operations according to the formula in Table 1:

[0081] 1. Preparation of the inner aqueous phase: Disperse the prescribed amount of active drug (bupivacaine hydrochloride) and osmotic pressure regulator into the aqueous solution for injection whose pH is adjusted to 1.0 with hydrochloric acid, and stir until the materials are evenly dispersed in the inner aqueous phase solution, get the inner water phase;

[0082] 2. Preparation of the first organic phase: dissolving the polylactic acid-hydroxylactic acid copolymer of the prescribed amount in chloroform of a certain quality to obtain the first organic phase;

[0083] 3. Preparation of the second organic phase: respectively dissolving hydrogenated phospholipids and cholesterol in a certain amount of chloroform to obtain the second organic phase;

[0084] 4. Preparation of the external aqueous phase: dissolve the osmotic pressure regula...

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Abstract

The invention relates to the field of pharmaceutic preparations, in particular to a lipidosome-polymer particle preparation of topical anaesthetic and a preparation method of the lipidosome-polymer particle preparation. The lipidosome-polymer particle preparation of the topical anaesthetic is prepared from, by mass, 150-250 parts of topical anaesthetic, 300-350 parts of PLGA, 100-150 parts of stabilizer, 400-430 parts of phospholipid and 100-105 parts of cholesterol. The preparation is small in grain size, stable in property and good in release effect. The average grain size of the preparation is 40.15 micrometers, and the encapsulation rate is 81.8%. After dissolution rate inspection is carried out for 72 hours in a buffer salt medium with the pH of 7.4, the dissolution rate exceeds 80%. Besides, the preparation is placed for 10 days at the temperature of 30 DEG C, and the permeability does not exceed 15% and is superior to that in the prior art. In addition, the preparation method of the preparation is simple, the requirement for production equipment is not high, and the production period is short.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a liposome-polymer microparticle preparation of a local anesthetic and a preparation method thereof. Background technique [0002] Postoperative pain (Postoperative Pain) is the pain that occurs immediately after surgery, which belongs to the category of acute nociceptive pain. If it is not fully controlled in the initial state, it is easy to develop into chronic postoperative pain. [0003] As the cornerstone of anesthesiology, local anesthetics are constantly innovating in terms of improving the clinical effects of drugs, reducing adverse reactions, and meeting the needs of clinical safety and comfort. Especially in the past 10 years, various new local anesthetics have been applied clinically, or are in the preclinical verification stage, and animal experiments have obtained gratifying results. Local anesthetics have the effect of blocking nerve impulse conduction, a...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/127A61K45/00A61K31/167A61K31/445A61K47/34A61K47/24A61K47/28A61P23/02
CPCA61K9/0019A61K9/127A61K9/501A61K9/5031A61K31/167A61K31/445A61K45/00
Inventor 梁兆丰岳占国刘荣
Owner GUANGZHOU BOSITAO CONTROLLED RELEASE PHARMA CO LTD
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