28 results about "Pilocarpine" patented technology

The invention discloses a culture medium and application thereof, and a method for in-vitro separation culture and adipogenic differentiation of precursor adipocytes in goat muscle, and relates to the technical field of cell culture, the culture medium comprises the following components: 8-12 [mu] g / mL of insulin, 8-12% by volume of fetal calf serum, 95-105 U / mL of penicillin, 95-105 [mu] g / mL of streptomycin and the like. On the basis of the prior art, a proper amount of liquiritin and pilocarpine are mainly added into a culture medium, and synergistic cooperation of the liquiritin and pilocarpine is found, so that the adipogenic differentiation capacity of cells such as mesenchymal stem cells and precursor adipocytes is remarkably improved, and the application range is wide. On the basis, the invention also provides a complete set of perfect in-vitro isolated culture and adipogenic differentiation method of the goat intramuscular precursor adipocytes, and a method and a way are provided for a series of researches developed through the goat primary intramuscular precursor adipocytes in the future.

The present application relates to an ophthalmic preparation and use thereof. Specifically, the present application relates to an ophthalmic preparation of pilocarpine and use thereof for treating eye diseases. The ophthalmic preparation of pilocarpine provided by the present application has the beneficial effects of good stability and less eye irritation.

The pilocarpine p-methyl phenylacetate crystal form A disclosed for the first time is good in solid stability, free of crystal transformation and convenient to store for a long time. And the preparation process is simple, good in reproducibility, stable and controllable, and beneficial to industrial large-scale production.

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to application of a Dan'e Fukang preparation in preparation of a medicine for treating perimenopausal syndrome. The invention provides application of a Dan'e Fukang preparation in preparation of a medicine for treating perimenopausal syndrome. Pharmacological experiments prove that Dan'e Fukang can reduce the number of activities of mice and prolong the sleep time of the barbital sodium of the mice, and has certain sedative, hypnotic and anxiety-resistant effects; the composition can effectively resist rat foot plantar sweat secretion caused by pilocarpine, and has a certain effect of resisting sweating; moreover, the traditional Chinese medicine composition has an obvious effect of reducing LH, FSH and T in climacteric rats, has an effect of increasing E2 in serum of the climacteric rats, and can be used for effectively treating the perimenopausal syndrome. Dan'e'fukang can reduce the total accumulated immobility time of the rat in the forced swimming experiment; the despair state time of a tail suspension experiment rat is obviously shortened, and a certain anti-depression effect is achieved. The Dan'e Fukang can provide more drug choices for clinical treatment of perimenopausal syndrome diseases.

The invention discloses a method for synthesizing a key intermediate of pilocarpine. The invention provides a method for synthesizing a key intermediate of pilocarpine. The method uses 2,2-dimethyl-1,3-dioxane-5-one as a starting material, synthesizes 4-ethyl-5-oxy-2,5-dihydrofuran-3-acetic acid through Horner-Wadsworth-Emmons olefination, hydrolysis, oxidation, Wittig reaction, hydrolysis, oxidation and the like, and then synthesizes the final product according to the steps in the document "Concise Synthesis of Both Enantiomers of Pilocarpine".

The application discloses a culture medium and application thereof, and a method for in-vitro separation and culture of goat intramuscular precursor fat cells and adipogenic differentiation of the cells, and relates to the technical field of cell culture. The culture medium comprises the following components: 8-12 mu g / mL insulin, 8-12% fetal bovine serum in volume fraction, 95-105 U / mL penicillin, 95-105 mu g / mL streptomycin, and the like. On the basis of the prior art, the application mainly adds appropriate glycyrrhizin and pilocarpine in the culture medium, and finds that the two components are in cooperation, and the adipogenic differentiation ability of cells such as mesenchymal stem cells and precursor fat cells is significantly improved, and the application range is wide. On the basis, the application further provides a complete method for in-vitro separation and culture of goat intramuscular precursor fat cells and adipogenic differentiation of the cells, and provides a method and a way for a series of researches on goat primary intramuscular precursor fat cells in the future.

Liquid oral pilocarpine formulations are described herein. Methods of using the liquid oral pilocarpine formulations are also provided.

The present invention relates to intermediate compounds of pilocarpine and methods for preparing them. In particular, the present invention relates to compounds of formulas V and I for preparing pilocarpine, and methods for preparing them. In this method, the compound of formula II is used as a raw material, the compound of formula V is obtained after halogenation hydrolysis, oxidation and substitution reactions; the compound of formula V is then subjected to reduction and ring formation reactions to obtain the compound of formula I. The preparation method of the present invention has advantages such as mild reaction conditions, a simple reaction process, high overall yield and high purity, and is particularly suitable for industrial production. [Formula 1] JPEG2026512163000029.jpg42124

The present invention relates to an ophthalmic preparation and the use thereof. Specifically, the present invention relates to a pilocarpine ophthalmic preparation and the use thereof in the treatment of ocular diseases. The pilocarpine ophthalmic preparation provided in the present invention has the beneficial effects of a good stability and low ocular irritation.

Gel, ointment, lotion, or cream formulations containing an active pharmaceutical ingredient including a tropanil portion are provided herein. The gel, lotion, or cream formulations may contain at least one low molecular weight (LMW) compound or a pharmaceutically acceptable salt thereof. Also provided herein are gel, ointment, lotion, or cream formulations containing active pharmaceutical ingredients such as atropine, pilocarpine, physostigmine, or travoprost.

Described herein are formulations including pharmaceutical agents comprising ester and / or lactone ring structures, and methods of using the same. The invention is also directed to a method and ophthalmic pharmaceutical compositions including solution and semisolid dosage forms (i.e. ophthalmic creams, gels, lotions, serums, and / or ointments) of treating a patient with various ocular diseases including presbyopia and dry eyes. The method comprising instructing a patient to apply one strip of the ophthalmic composition to the eyelids that includes pilocarpine or other active pharmaceutical ingredients containing ester and / or lactone ring structures with and without the buffering system.

The present invention relates to a composition and the use of the composition in preparing a medicine for treating eye diseases. The composition comprises 0.5-1.5% by weight of a muscarinic acetylcholine receptor M3 agonist; 0.005-0.5% by weight of naphazoline, a pharmaceutically acceptable salt thereof, or a combination thereof; and 0.1-1% by weight of ketorolac tromethamine. The composition enhances the effect of a muscarinic acetylcholine receptor M3 agonist such as a pilocarpine active ingredient in treating presbyopia, while effectively and significantly reducing or even eliminating the side effects caused by the pilocarpine active ingredient.

A composition and a use of the composition in the preparation of a medicament for treating eye diseases. The composition includes 0.5-1.5% by weight of a muscarinic acetylcholine receptor M3 agonist; 0.005-0.5% by weight of naphazoline, a pharmaceutically acceptable salt thereof or a combination thereof; and 0.1-1% by weight of ketorolac tromethamine. While enhancing the effect of a muscarinic acetylcholine receptor M3 agonist such as a pilocarpine active ingredient in treating presbyopia, the composition effectively significantly reduces or even eliminates side effects caused by the pilocarpine active ingredient.

The present invention provides an ophthalmic preparation for correcting near vision, its preparation method and use, which are particularly suitable for treating presbyopia and mild hyperopia. The ophthalmic preparation contains pilocarpine, brimonidine, a compound containing a stin nucleus group structure, a non-steroidal anti-inflammatory drug, functional excipient A, a thickening agent, a complexing agent, a pH regulator, a bacteriostatic agent and sodium chloride. The experimental results show that the compound containing a stin nucleus group structure added to the ophthalmic preparation of the present invention has a synergistic effect with pilocarpine and brimonidine. In addition, adding functional excipient A to the ophthalmic preparation reduces the irritation of the preparation and improves the patient compliance. Compared with the commonly used drugs of the same kind clinically, the ophthalmic preparation of the present invention has the characteristics of higher efficacy and lower ocular irritation.

Provided herein are gels, ointments, lotions, or cream formulations comprising an active pharmaceutical ingredient comprising a tropane moiety. The gel, lotion, or cream formulation may comprise at least one low molecular weight (LMW) compound, or a pharmaceutically acceptable salt thereof. Also provided herein are gel, ointment, lotion, or cream formulations comprising an active agent, such as atropine, pilocarpine, hyacinth bean alkali, or travoprost.

Described herein are formulations including pharmaceutical agents comprising ester and / or lactone ring structures, and methods of using the same. The invention is also directed to a method and ophthalmic pharmaceutical compositions including solution and semisolid dosage forms (i.e. ophthalmic creams, gels, lotions, serums, and / or ointments) of treating a patient with various ocular diseases including presbyopia and dry eyes. The method comprising instructing a patient to apply one strip of the ophthalmic composition to the eyelids that includes pilocarpine or other active pharmaceutical ingredients containing ester and / or lactone ring structures with and without the buffering system.

The present invention relates to an ophthalmic pharmaceutical composition comprising pilocarpine phenylacetate or pilocarpine phenylacetic acid derivative salt and an alpha receptor agonist or a pharmaceutically acceptable salt thereof. The pharmaceutical composition can effectively prolong the drug action time, the overall action effect is smoother and more stable, the eye hyperemia and redness phenomena are effectively improved, and the administration irritation is reduced.

The invention provides pilocarpine hydrochloride ion-sensitive in-situ gel eye drops and a preparation method thereof, and a long-acting ophthalmic preparation capable of retarding presbyopia in presbyopia diseases.

The disclosure relates to ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt. Aspects of the disclosure further relate to uses and preparations of ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt, for correcting presbyopia and other ocular conditions in a subject.

Described herein are methods and compositions for the treatment of ocular conditions and for the improvement of vision parameters using pharmaceutically acceptable ophthalmic pilocarpine formulations. A nonlimiting example of an ocular condition that may be treated with the methods and compositions disclosed herein is presbyopia.

The present invention relates to: an ophthalmic composition containing pilocarpine and having improved stability; and a use thereof.

The present invention is directed to compositions and methods for treating ocular conditions, including presbyopia, mild hyperopia, irregular astigmatism, hyperopic accommodative esotropia, and glaucoma. The compositions can also be used to potentiate or enhance interventions that retard, reverse, or modify the aging process of the crystalline lens and its surrounding tissues. The compositions include a cholinergic agent, such as a muscarinic acetylcholine receptor M3 agonist, and an alpha agonist having an imidazoline group or a non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity. It has been found that an alpha agonist having an imidazoline group or non-steroidal anti-inflammatory agent (NSAID) having COX-2 selectivity in combination with a cholinergic agent, such as pilocarpine, act synergistically to improve the accommodative and focusing ability of the eye while minimizing the side effects from each compound.

The invention relates to an intermediate compound of pilocarpine and a preparation method thereof. In particular, the present invention relates to compounds of formula V and formula I for preparing pilocarpine and methods for their preparation. The method comprises the following steps: by taking a compound in a formula II as a raw material, performing halogenation hydrolysis, oxidation and substitution reaction to obtain a compound in a formula V; and performing reduction reaction and cyclization reaction on the compound in the formula V to obtain the compound in the formula I. The preparation method has the advantages of mild reaction conditions, simple reaction process, high total yield, high purity and the like, and is very suitable for industrial production.

Liquid oral pilocarpine formulations are described herein. Methods of using the liquid oral pilocarpine formulations are also provided.

To provide ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt thereof.SOLUTION: Aspects of the disclosure further relate to uses and preparations of ophthalmic pharmaceutical compositions comprising pilocarpine or a pharmaceutically acceptable salt, for correcting presbyopia and other ocular conditions in a subject.SELECTED DRAWING: Figure 1

The invention relates to a preparation method of pilocarpine and an intermediate compound of pilocarpine. Specifically, the invention relates to key intermediates of formula (I) and formula (II) compounds for preparing pilocarpine and a preparation method of the key intermediates. According to one method, malic acid is used as a raw material and sequentially reacts with alcohol or sulfate, reacts with halogenated ethane and the like to obtain a compound shown in a formula (II), and finally reacts with a halogenating reagent to obtain a compound shown in a formula (I). According to the other method, n-butyraldehyde is used as a raw material and is subjected to a condensation reaction, an oxidation reaction, an esterification reaction and a sulfonylation reaction in sequence to obtain a compound shown in the formula (II), and finally the compound shown in the formula (I) is obtained after the compound reacts with a halogenation reagent. The preparation method disclosed by the invention has the advantages of mild reaction conditions, simple reaction process, high total yield of target products, high purity and the like, so that the preparation method is very suitable for industrial production.

The invention provides a synthesis method and a purification method of pilocarpine, and relates to the field of medical chemistry. According to the synthesis method disclosed by the invention, the free pilocarpine is prepared through alkali screening, so that the proliferation of impurities in the preparation process is reduced, and the purity and the yield of the pilocarpine are improved.