CN114617898A

CN114617898A - Compound preparation prepared from clindamycin and cimetidine and preparation method thereof

Info

Publication number: CN114617898A
Application number: CN202210485266.4A
Authority: CN
Inventors: 王佑卿
Original assignee: Individual
Current assignee: Individual
Priority date: 2022-05-06
Filing date: 2022-05-06
Publication date: 2022-06-14

Abstract

The application provides a compound preparation prepared from clindamycin and cimetidine and a preparation method thereof. The active ingredients of the compound comprise clindamycin and cimetidine, and the proportion is 0.075-1.2: 0.01 to 0.4. The raw material medicaments are taken according to the corresponding parts by weight, and are added with proper auxiliary materials according to the preparation method of corresponding pharmaceutics, so that the raw material medicaments can be respectively prepared into granules, dry suspensions, tablets, capsules, injections and other formulations. The action mechanism of the antibacterial peptide is to inhibit the synthesis of bacterial protein to generate antibacterial action, and is mainly used for infection caused by gram-positive cocci and anaerobic bacteria. Cimetidine is a liver drug enzyme inhibitor, can delay the metabolism of the combined drug, and improve the blood concentration of the combined drug so as to improve the curative effect of the combined drug; meanwhile, cimetidine can also inhibit gastric acid secretion to relieve the stimulation of clindamycin to stomach. The two are prepared into a compound preparation, the effect of treating infection caused by sensitive bacteria is good, the side effect is low, the medication is safe, the taking is convenient, and the application effect is good.

Description

Compound preparation prepared from clindamycin and cimetidine and preparation method thereof

Technical Field

The application relates to the technical field of medicines, in particular to a compound preparation prepared from clindamycin and cimetidine and a preparation method thereof.

Background

Clindamycin, also known as clindamycin, is a derivative of lincomycin and has good antibacterial effect on various gram-positive cocci and anaerobic bacteria. Is suitable for treating respiratory system infection, urinary system infection, female pelvic cavity and genital infection, skin and soft tissue infection, bone and joint infection, abdominal cavity infection, etc. caused by gram-positive cocci and anaerobe. However, clinical medication finds that part of patients have poor curative effect and have serious gastrointestinal adverse reactions such as pseudomembranous enteritis and the like. Therefore, it is necessary to develop a compound preparation which can improve the curative effect of clindamycin and reduce the side effect of clindamycin and is safe and convenient to use.

Disclosure of Invention

Aiming at the defects of the single preparation, the application aims to provide a compound preparation prepared from clindamycin and cimetidine and a preparation method thereof. The compound preparation is prepared by taking clindamycin and cimetidine as main components and appropriate auxiliary materials corresponding to various dosage forms and adopting a preparation method of corresponding dosage forms in pharmaceutics, can improve the curative effect of clindamycin and reduce the side effect of clindamycin, and has the advantages of few medicine types, convenient medicine use and the like.

The technical scheme adopted by the application is as follows:

the compound preparation prepared from clindamycin and cimetidine is characterized in that active ingredients of the compound preparation comprise clindamycin and cimetidine in a ratio of 0.075-1.2: 0.01 to 0.4.

The further technical scheme is that the compound preparation can be one of granules, dry suspensions, tablets, capsules or injections; the tablet comprises a sustained release tablet, a controlled release tablet, an effervescent tablet, an enteric-coated tablet, a dispersible tablet and a common tablet; the capsule comprises a slow release capsule, a controlled release capsule and an enteric capsule; the injection comprises powder for injection, water injection and high-capacity injection.

The further technical scheme is that the active ingredients of the compound preparation comprise clindamycin and cimetidine, and the ratio is 0.08: 0.05.

the further technical scheme is that the active ingredients of the compound preparation comprise clindamycin and cimetidine, and the ratio is 0.15: 0.20.

the technical scheme is that the clindamycin is prepared from a medicinal clindamycin or a derivative raw material medicine of the medicinal clindamycin which is sold in the market, and the cimetidine is prepared from a medicinal cimetidine raw material medicine which is sold in the market.

The application also provides a preparation method of the compound preparation prepared from clindamycin and cimetidine, which comprises the following steps:

(1) taking corresponding parts of clindamycin and cimetidine raw material medicines for later use;

(2) taking appropriate amount of adjuvants corresponding to the prepared dosage form;

(3) according to the preparation method of the corresponding pharmaceutics, the corresponding granules, dry suspensions, tablets, capsules and injections can be respectively prepared.

The further technical proposal is that the auxiliary materials comprise a filling agent, an excipient, a solubilizer, a glidant, a diluent, a bonding agent, a disintegrant, a lubricant, a colorant, a preservative and other auxiliary materials which are suitable for the preparation formulation.

The further technical proposal is that the tablets comprise sustained release tablets, controlled release tablets, effervescent tablets, enteric-coated tablets, dispersible tablets and common tablets; the capsule comprises a slow release capsule, a controlled release capsule and an enteric capsule; the injection comprises powder for injection, water injection and large-volume injection.

The beneficial effect of this application lies in:

in the compound preparation prepared from clindamycin and cimetidine, the action mechanism of clindamycin is combined with bacterial ribosome 50S subunit to inhibit peptide chain extension, so that the synthesis of bacterial protein is inhibited, villous coats and surface A protein on the surfaces of bacteria can be effectively removed, and the bacteria are easily killed and phagocytized. Clindamycin can also improve the immunity of the organism and enhance the phagocytic and bactericidal capability of leucocytes. Cimetidine as liver drug enzyme inhibitor can delay metabolism of clindamycin, and improve blood concentration to improve therapeutic effect. And the cimetidine can also reduce the side effect of the combined medicament clindamycin by inhibiting gastric acid secretion. The two are prepared into a compound preparation, the curative effect is enhanced, the side effect is reduced, and the taking is convenient. Fully embodies the unexpected curative effect of the compound preparation prepared by clindamycin and cimetidine.

Detailed Description

The technical solutions in the embodiments of the present application will be clearly and completely described below with reference to the embodiments of the present application. It is to be understood that the embodiments described are only a few embodiments of the present application and not all embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present application.

The raw materials, auxiliary materials, reagents and the like used in the following examples are commercially available unless otherwise specified.

Example 1

A compound preparation prepared from clindamycin and cimetidine, wherein the weight ratio of clindamycin to cimetidine in the active ingredients of the compound preparation is 0.075: 0.05 and the balance of auxiliary materials. The preparation method comprises the following steps:

(1) weighing 75g of clindamycin raw material medicine and 50g of cimetidine raw material medicine for later use;

(2) taking a proper amount of required auxiliary materials which are suitable for the prepared dry suspension for later use;

(3) the dry suspension is prepared according to the preparation method of pharmaceutics, so that each generation contains 150mg of clindamycin and 100mg of cimetidine.

Example 2

A compound preparation prepared from clindamycin and cimetidine, wherein the weight ratio of clindamycin to cimetidine in the active ingredients of the compound preparation is 0.30: 0.20, and the balance of auxiliary materials. The preparation method comprises the following steps:

(1) weighing 30g of clindamycin raw material medicine and 20g of cimetidine raw material medicine for later use;

(2) taking a proper amount of required auxiliary materials which are suitable for the prepared capsule for standby;

(3) the capsules are prepared according to a pharmaceutical capsule preparation method, and each capsule contains 300mg of clindamycin and 200mg of cimetidine.

Test of drug efficacy

1. The drugs prepared in examples 1 and 2 were selected for clinical trials.

The control group was strictly established according to the design scheme of parallel, random, control experiment, and the clinical efficacy of the drugs prepared in examples 1 and 2 was observed.

2. Selection of pathologies

Inclusion cases: adult patients who meet the diagnosis standard of intra-abdominal infectious diseases are diagnosed by western medicine, such as: patients with peritonitis and intra-abdominal abscess are 18-75 years old, and informed consents can be brought into test cases;

adult patients who meet the diagnosis standard of skin soft tissue infection are diagnosed by western medicine, such as: patients with furuncle, carbuncle, abscess, cellulitis, trauma and postoperative infection, age 18-75 years old, with informed consent, can be included in the test cases.

Excluding cases: (1) those with a history of allergy to clindamycin or lincomycin; (2) patients in acute exacerbation; (3) patients with severe heart failure and cardiac function of grade IV should not be taken into the test cases; (4) if the patient does not meet the inclusion criteria, is not taking the medicine according to the regulations, cannot judge the curative effect or the data is not complete, the judgment of the curative effect is affected.

3. Test method

The grouping method comprises the following steps: observing by adopting random and control experiments, checking a treatment group and a control group on a random table by adopting a random control grouping method for the included test cases, and ensuring that the two groups of cases are close to each other in the aspects of disease property, sex, age, disease course and the like. The total number of cases was 320, 80 cases in each of the two treatment groups, and 80 cases in each of the two control groups.

4. Method of treatment

(1) Treatment 1 group: the basic treatment is the same as the control group, and the dry suspension prepared in the example 1 is taken at the same time, 2 generations of the dry suspension are taken at each time, 3 times a day are taken, and the treatment course is 7 days.

(2) Treatment 2 groups: the basic treatment is the same as the control group, and the capsules prepared in the example 2 are taken at the same time, 1 capsule is taken at a time, 3 times a day, and the treatment course is 7 days.

(3 control group:

the clindamycin capsules are commercially available to patients, each clindamycin capsule contains 150mg of clindamycin, 3 times a day, 2 capsules each time, 7 days of the treatment course, and the state of illness after the treatment course is finished is recorded.

If acute exacerbation occurs, the patient is treated conventionally in the acute attack stage.

5. Criteria for efficacy assessment

(1) Healing is achieved; the symptoms and physical signs basically disappear after the treatment course is over;

(2) the method has the following advantages: the disease condition changes from severe to moderate, or from moderate to mild, or the chief complaint is improved, and the signs are obviously improved.

(3) And (4) invalidation: there was no improvement or aggravation of symptoms and signs.

The total cure rate and the total effective rate are subject to the statistics of return diagnosis after 7 days of treatment.

6. The results of the treatment are shown in Table 1

TABLE 1 therapeutic results Table

As can be seen from the above table, the pharmaceutical preparation has definite curative effect and the total effective rate is more than 90%. The compound preparation provided by the application is used for treating intra-abdominal infectious diseases or skin soft tissue infectious diseases by combining clindamycin and cimetidine, and the treatment effect is more obvious than that of singly using clindamycin and is better than that of conventional treatment. Meanwhile, cimetidine can also reduce the side effects of clindamycin on the digestive system. After the treatment by adopting the medication scheme of clindamycin and cimetidine, the cure rate of patients is obviously improved, the treatment time is obviously shortened, and the unexpected curative effect is obtained by fully embodying the preparation of the clindamycin and cimetidine into compound preparations.

The above description is only for the purpose of illustrating the preferred embodiments of the present application and is not to be construed as limiting the present application, and all equivalent variations and modifications made within the scope of the present application are intended to be covered by the present application. Furthermore, it should be understood that although the present description refers to embodiments, not every embodiment may contain only a single embodiment, and such description is for clarity only, and those skilled in the art should integrate the description, and the embodiments may be combined as appropriate to form other embodiments understood by those skilled in the art.

Claims

1. The compound preparation prepared from clindamycin and cimetidine is characterized in that active ingredients of the compound preparation comprise clindamycin and cimetidine in a ratio of 0.075-1.2: 0.01 to 0.4.

2. The compound preparation prepared from clindamycin and cimetidine as claimed in claim 1, wherein the compound preparation can be one of granules, dry suspension, tablets, capsules or injections; the tablet comprises a sustained release tablet, a controlled release tablet, an effervescent tablet, an enteric-coated tablet, a dispersible tablet and a common tablet; the capsule comprises a slow release capsule, a controlled release capsule and an enteric capsule; the injection comprises powder for injection, water injection and large-volume injection.

3. The combination preparation of claim 1, wherein the active ingredients of the combination preparation comprise clindamycin and cimetidine in a ratio of 0.08: 0.05.

4. a combination formulation prepared from clindamycin and cimetidine according to claim 1, wherein the active ingredients of the combination formulation comprise clindamycin and cimetidine in a ratio of 0.15: 0.20.

5. the compound preparation prepared from clindamycin and cimetidine as claimed in claim 1, wherein the clindamycin is a commercial product of clindamycin or its derivative, and the cimetidine is a commercial product of cimetidine.

6. A method for preparing a compound preparation prepared from clindamycin and cimetidine is characterized by comprising the following steps:

(2) taking appropriate amount of required adjuvants corresponding to the prepared dosage form;

(3) according to the preparation method of corresponding pharmaceutics, corresponding auxiliary materials are added to prepare corresponding granules, dry suspensions, tablets, capsules or injections respectively.

7. The method of claim 6, wherein the excipients include fillers, excipients, solubilizers, glidants, diluents, binders, disintegrants, lubricants, colorants, preservatives and other excipients suitable for the formulation.