Crystal Growth,Structure and Morphology of Rifapentine Methanol Solvate

Rifapentine, an important antibiotic, was crystallized from methanol solvent in the form of its methanol solvate. The crystal structure of rifapentine methanol solvate belongs to monoclinic, space group P21, with the unit cell parameters of a = 1.2278（3） nm, b = 1.9768（4） rim, c = 1.2473（3） nm, Z= 2, and β = 112.35（3）. The parallelepiped.morphology was also predicted by Materials Studio simulation program.. The influence of intermolecular in-teraction was taken into account in the attachment energy model. The crystal shape fits the calculated morphology well, which was performed on the potential energy minimized model using a generic DREIDING 2.21 force fieldand developed minimization protocol with derived＇partial charges.

Effect of Rifapentine and Rifampicin on Anti-Tuberculosis

Objective: To investigate the clinical effect of rifapentine and rifampicin in the treatment of pulmonary tuberculosis. Methods: Seventy-two cases of patients with initial treatment of pulmonary tuberculosis who attended the First Hospital Affiliated to Hebei North University from February 2017 to August 2019 were selected. They were randomly divided into observation group and control group, with 36 cases in each group. The observation group was treated with isoniazid + rifapentine + ethambutol, while the control group was treated with isoniazid + rifampicin + ethambutol. The symptom relief, image absorption and adverse reactions were compared between the two groups. Results: The rate of symptom relief was 86.11% in the observation group and 94.44% in the control group, P < 0.05, which was statistically significant. Rifampin was more helpful than rifapentine in relieving clinical symptoms. The lesion absorption rate was 77.79% in the observation group and 88.89% in the control group, P < 0.05, and the difference was statistically significant. Rifampin was more beneficial to the absorption of TB lesions than rifapentine. The incidence of adverse reactions in the observation group was 16.67% much lower than that in the control group, which was 38.89%, indicating that the adverse reactions of rifapentine were less. Conclusion: Rifampicin is superior to rifapentine in clinical symptom relief and lesion absorption, but the incidence of adverse reactions is high.

抗结核新药Rifapentine在欧洲被定为罕见病治疗药物

赛诺菲-安万特肺结核药Rifapentine被欧盟委员会指定为罕见病治疗药物。Rifapentine属于利福霉素类产品，但在治疗分支杆菌性肺结核时效果更好，药物半衰期也更长，有助于提高患者依从性。目前这种药物已在美国有售，适应证为普通肺结核及药物敏感型肺结核，使用过程中与标准药联用疗程6个月。

Crystal modification of rifapentine using different solvents

Rifapentine crystals with different habits were prepared by recrystallization from selected solvents,such as methanol,ethanol,chloroform,and acetic acid.Scanning electron microscopy,X-ray powder diffractometry,infrared spectrometry,and differential scanning calorimetry were used to investigate the physicochemical characteristics of the prepared crystals.The comparative dissolution behaviors of the newly developed crystals and of rifapentine without being treated were also studied.Results show that the newly developed crystals were different from each other with respect to physical properties but were identical chemically.Needle-shaped crystals were obtained from methanol,ethanol,and chloroform solvents,and the block-shaped crystals were obtained from acetic acid solvent.X-ray diffraction spectra and differential scanning calorimetry investigation on those developed crystals clearly indicate that rifapentine has different crystal structure modification.When the crystal was obtained from acetic acid,the change of crystal habit was originated from the crystal structure modification.The dissolution rate of newly developed crystals was found to be higher than that of rifapentine without being treated.However,the modified crystal obtained from acetic acid shows the lower dissolution rate than crystals obtained from other solvents.